Identification

Name
Lofexidine
Accession Number
DB04948
Type
Small Molecule
Groups
Approved, Investigational
Description

Lofexidine is a non-opioid centrally acting alpha2-adrenergic receptor agonist that was first approved for the treatment of opioid withdrawal in the United Kingdom in 1992.[2] It was first studied for use as an antihypertensive in 1980, but its researched was stopped as it was found less effective for the treatment of hypertension than clonidine.[6] Lofexidine was then repurposed for the treatment of opioid withdrawal, as it was seen to be more economical and have fewer side effects than clonidine.[5] Lofexidine was developed by US Woldmeds LLC and it was approved by the FDA on May 16, 2018.[8]

Structure
Thumb
Synonyms
  • 2-(alpha-(2,6-Dichlorophenoxy)ethyl)2-imidazoline
  • Lofexidina
  • Lofexidinum
Product Ingredients
IngredientUNIICASInChI Key
Lofexidine hydrochlorideV47G1SDI1B21498-08-8DWWHMKBNNNZGHF-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LucemyraTablet, film coated.2 mg/1OralUs World Meds, Llc2018-06-18Not applicableUs
International/Other Brands
Britlofex (Britannia)
Categories
UNII
UI82K0T627
CAS number
31036-80-3
Weight
Average: 259.132
Monoisotopic: 258.03266843
Chemical Formula
C11H12Cl2N2O
InChI Key
KSMAGQUYOIHWFS-UHFFFAOYSA-N
InChI
InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)
IUPAC Name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
SMILES
CC(OC1=C(Cl)C=CC=C1Cl)C1=NCCN1

Pharmacology

Indication

Lofexidine is indicated for mitigation of symptoms associated with acute withdrawal from opioids and for facilitation of the completion of opioid discontinuation treatment. It is the first non-opioid medication for the symptomatic management of opioid discontinuation.[9]

Opioid withdrawal syndrome is a debilitating manifestation of opioid dependence.[3] This condition is extremely unpleasant lasting several days with some of the main features being abdominal pain, nausea, diarrhea, mydriasis, lacrimation, and piloerection. These symptoms are often observed after abrupt reductions in the opioid dose and can be resolved by re-administration of the opioid.[4]

Associated Conditions
Pharmacodynamics

In clinical trials, lofexidine presented more severe opioid withdrawal effects than observed with methadone. On the other hand, in clinical trials of methadone withdrawal, lofexidine effectively reduced withdrawal symptoms, especially hypotension.[5] The clinical reports have also indicated that lofexidine presents a better outcome when used briefly.[6] In phase 3 clinical trials, lofexidine was shown to generate a significantly higher completion rate of opioid discontinuation. Some pharmacological studies were performed and there were no off-target effects reported.[9]

Mechanism of action

Lofexidine is a potent alpha2-adrenergic receptor agonist with some moderate agonistic affinity towards Alpha-1A adrenergic receptor and 5-HT1a, 5-HT7, 5HT2c and 5HT1d receptors.[9]

The alpha2-adrenergic receptor is normally targeted by norepinephrine and its activation inhibits the synthesis of cAMP which in turn leads to potassium efflux and suppression of neural firing and inhibition of norepinephrine release. All of this activity can reduce the heart rate, blood pressure, and attenuate sympathetic stress response.[9]

Opioids inhibit cAMP in the noradrenergic neurons and their discontinuation produces a rise in the level of cAMP. This will generate an increase in norepinephrine which is associated with the symptoms of withdrawal. The magnitude of the effect is augmented by chronic opioid use due to the compensatory mechanisms of continuous negative feedback. Therefore, chronic opioid use translates into an exacerbated production of cAMP and norepinephrine release.[9]

Lofexidine replaces the opioid-driven inhibition of cAMP production by activating the alpha2-adrenergic receptor and moderating the symptoms of opioid withdrawal. This effect is performed without interacting with opioid receptors which mediate other activities of opioid dependence or addiction.[9]

TargetActionsOrganism
AAlpha-2A adrenergic receptor
agonist
Human
NAlpha-1A adrenergic receptor
agonist
Human
N5-hydroxytryptamine receptor 1A
agonist
Human
N5-hydroxytryptamine receptor 7
agonist
Human
N5-hydroxytryptamine receptor 2C
agonist
Human
N5-hydroxytryptamine receptor 1D
agonist
Human
Absorption

Lofexidine has a good oral bioavailability and the peak plasma concentration occurs after 2-5 hours of oral administration.[6] The bioavailability is registered to be even higher than 72%.[7] About 30% of the administered dose of lofexidine is lost during first-pass metabolism. The absorption is registered to be very rapidly recirculated in the gut. After oral administration of 0.8 mg of lofexidine, a maximal dose of 1.26 ng/ml is achieved after 3 hours.[9]

Volume of distribution

Lofexidine has a volume of distribution of 300 L, indicating that it distributes readily into the tissues.[9]

Protein binding

The protein binding of lofexidine is determined to be moderate and it represents about 55% of the administered dose.[9]

Metabolism

Lofexidine metabolic ratio is highly variable among people.[6] It is metabolized mainly by the activity of CYP2D6 and in a minor degree by CYP1A2 and CYP2C19. These enzymes catalyze the hydroxylation of lofexidine and the opening of imidazoline ring to form N-(2-aminoethyl)-2-(2,6-dichlorophenoxy)propanamide. This metabolite is deamidated and forms 2-(2,6-dichlorophenoxy) propionic acid and 2,6-dichlorophenol. These three main metabolites are inactive.[9]

Route of elimination

The elimination of lofexidine is primarily through the renal system and it represents 94% of the administered dose while elimination in feces corresponds to only 0.93%.[6] From the eliminated dose in urine, about 10% is formed by unchanged drug and 5% is constituted by the first hydrolysis product N-(2-aminoethyl)-2-(2,6-dichlorophenoxy)propanamide. 2,6-dichlorophenol represents the majority of the administered dose by occupying about 80% of the administered dose.[9]

Half life

The reported elimination half-life of lofexidine is 11 hours.[7]

Clearance

The total elimination clearance following intravenous administration is 17.6 L/h.[9]

Toxicity

Lofexidine did not exhibit genotoxic, mutagenic nor mutagenic potential. Administration at gestational period showed a reduction in the neonatal weight, survival, and increased abortion.[9]

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7-NitroindazoleThe therapeutic efficacy of 7-Nitroindazole can be increased when used in combination with Lofexidine.Experimental
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe metabolism of Lofexidine can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.Experimental
AbirateroneThe serum concentration of Lofexidine can be increased when it is combined with Abiraterone.Approved
AcebutololLofexidine may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved, Investigational
AcemetacinThe therapeutic efficacy of Lofexidine can be decreased when used in combination with Acemetacin.Approved, Experimental, Investigational
AcepromazineThe therapeutic efficacy of Acepromazine can be increased when used in combination with Lofexidine.Approved, Vet Approved
AceprometazineThe therapeutic efficacy of Aceprometazine can be increased when used in combination with Lofexidine.Approved
AdipiplonThe therapeutic efficacy of Adipiplon can be increased when used in combination with Lofexidine.Investigational
AgomelatineThe therapeutic efficacy of Agomelatine can be increased when used in combination with Lofexidine.Approved, Investigational
AldesleukinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Aldesleukin.Approved
AlfaxaloneThe therapeutic efficacy of Alfaxalone can be increased when used in combination with Lofexidine.Vet Approved
AlfentanilThe therapeutic efficacy of Alfentanil can be increased when used in combination with Lofexidine.Approved, Illicit
AlfuzosinAlfuzosin may increase the hypotensive activities of Lofexidine.Approved, Investigational
AliskirenLofexidine may increase the hypotensive activities of Aliskiren.Approved, Investigational
AllopregnanoloneThe therapeutic efficacy of Allopregnanolone can be increased when used in combination with Lofexidine.Investigational
AlphacetylmethadolThe risk or severity of QTc prolongation can be increased when Lofexidine is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe therapeutic efficacy of Alphaprodine can be increased when used in combination with Lofexidine.Illicit
AlprazolamThe therapeutic efficacy of Alprazolam can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
AlprenololLofexidine may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmbrisentanLofexidine may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineLofexidine may increase the hypotensive activities of Amifostine.Approved, Investigational
AmilorideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Amiloride.Approved
AmineptineAmineptine may decrease the antihypertensive activities of Lofexidine.Illicit, Withdrawn
AmiodaroneThe metabolism of Lofexidine can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe therapeutic efficacy of Amisulpride can be increased when used in combination with Lofexidine.Approved, Investigational
AmitriptylineThe therapeutic efficacy of Amitriptyline can be increased when used in combination with Lofexidine.Approved
AmitriptylinoxideAmitriptylinoxide may decrease the antihypertensive activities of Lofexidine.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Lofexidine.Approved
AmobarbitalThe therapeutic efficacy of Amobarbital can be increased when used in combination with Lofexidine.Approved, Illicit
AmoxapineThe therapeutic efficacy of Amoxapine can be increased when used in combination with Lofexidine.Approved
AmperozideThe therapeutic efficacy of Amperozide can be increased when used in combination with Lofexidine.Experimental
AmphetamineThe metabolism of Lofexidine can be decreased when combined with Amphetamine.Approved, Illicit, Investigational
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Lofexidine.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Lofexidine is combined with Amyl Nitrite.Approved
ApalutamideThe serum concentration of Lofexidine can be decreased when it is combined with Apalutamide.Approved, Investigational
ApomorphineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Lofexidine.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Apraclonidine.Approved
AripiprazoleAripiprazole may increase the hypotensive activities of Lofexidine.Approved, Investigational
ArmodafinilThe metabolism of Lofexidine can be decreased when combined with Armodafinil.Approved, Investigational
ArotinololLofexidine may increase the atrioventricular blocking (AV block) activities of Arotinolol.Investigational
Arsenic trioxideThe risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Lofexidine.Approved, Investigational
ArtemetherThe metabolism of Lofexidine can be decreased when combined with Artemether.Approved
ArticaineThe therapeutic efficacy of Articaine can be increased when used in combination with Lofexidine.Approved
AsenapineThe therapeutic efficacy of Asenapine can be increased when used in combination with Lofexidine.Approved
AtenololLofexidine may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
AtomoxetineThe metabolism of Lofexidine can be decreased when combined with Atomoxetine.Approved
AvanafilAvanafil may increase the antihypertensive activities of Lofexidine.Approved
AzaperoneThe therapeutic efficacy of Azaperone can be increased when used in combination with Lofexidine.Investigational, Vet Approved
AzelastineThe therapeutic efficacy of Azelastine can be increased when used in combination with Lofexidine.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Lofexidine is combined with Azilsartan medoxomil.Approved, Investigational
AzithromycinThe metabolism of Lofexidine can be decreased when combined with Azithromycin.Approved
BaclofenThe therapeutic efficacy of Baclofen can be increased when used in combination with Lofexidine.Approved
BarbexacloneBarbexaclone may increase the hypotensive activities of Lofexidine.Experimental
BarbitalThe therapeutic efficacy of Barbital can be increased when used in combination with Lofexidine.Illicit
BarnidipineLofexidine may increase the antihypertensive activities of Barnidipine.Approved
BefunololLofexidine may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
BenazeprilBenazepril may increase the hypotensive activities of Lofexidine.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Lofexidine.Approved
BenmoxinThe metabolism of Lofexidine can be decreased when combined with Benmoxin.Withdrawn
BenperidolThe therapeutic efficacy of Benperidol can be increased when used in combination with Lofexidine.Approved, Investigational
BenzocaineThe therapeutic efficacy of Benzocaine can be increased when used in combination with Lofexidine.Approved, Investigational
Benzyl alcoholThe therapeutic efficacy of Benzyl alcohol can be increased when used in combination with Lofexidine.Approved
Benzylpenicilloyl PolylysineLofexidine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BepridilBepridil may increase the hypotensive activities of Lofexidine.Approved, Withdrawn
BetaxololLofexidine may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved, Investigational
BethanidineBethanidine may increase the hypotensive activities of Lofexidine.Approved
BevantololLofexidine may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BietaserpineBietaserpine may increase the hypotensive activities of Lofexidine.Experimental
BimatoprostBimatoprost may increase the hypotensive activities of Lofexidine.Approved, Investigational
BisoprololLofexidine may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BopindololLofexidine may increase the atrioventricular blocking (AV block) activities of Bopindolol.Approved
BortezomibThe risk or severity of adverse effects can be increased when Bortezomib is combined with Lofexidine.Approved, Investigational
BosentanBosentan may increase the hypotensive activities of Lofexidine.Approved, Investigational
BQ-123Lofexidine may increase the hypotensive activities of BQ-123.Investigational
BretyliumBretylium may increase the hypotensive activities of Lofexidine.Approved
BrexpiprazoleThe therapeutic efficacy of Brexpiprazole can be increased when used in combination with Lofexidine.Approved, Investigational
BrimonidineBrimonidine may increase the antihypertensive activities of Lofexidine.Approved
BrofaromineThe metabolism of Lofexidine can be decreased when combined with Brofaromine.Experimental
BromazepamThe therapeutic efficacy of Bromazepam can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
BromisovalThe therapeutic efficacy of Bromisoval can be increased when used in combination with Lofexidine.Experimental
BromocriptineBromocriptine may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved, Investigational
BromperidolThe therapeutic efficacy of Bromperidol can be increased when used in combination with Lofexidine.Approved, Investigational
BrompheniramineThe therapeutic efficacy of Brompheniramine can be increased when used in combination with Lofexidine.Approved
BrotizolamThe therapeutic efficacy of Brotizolam can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
BucindololLofexidine may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolLofexidine may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BumetanideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Bumetanide.Approved
BunazosinBunazosin may decrease the vasoconstricting activities of Lofexidine.Investigational
BupivacaineThe therapeutic efficacy of Bupivacaine can be increased when used in combination with Lofexidine.Approved, Investigational
BupranololLofexidine may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
BuprenorphineThe therapeutic efficacy of Buprenorphine can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Lofexidine can be decreased when combined with Bupropion.Approved
BuspironeThe therapeutic efficacy of Buspirone can be increased when used in combination with Lofexidine.Approved, Investigational
ButabarbitalThe therapeutic efficacy of Butabarbital can be increased when used in combination with Lofexidine.Approved, Illicit
ButacaineThe therapeutic efficacy of Butacaine can be increased when used in combination with Lofexidine.Vet Approved
ButalbitalThe therapeutic efficacy of Butalbital can be increased when used in combination with Lofexidine.Approved, Illicit
ButambenThe therapeutic efficacy of Butamben can be increased when used in combination with Lofexidine.Approved, Withdrawn
ButethalThe therapeutic efficacy of Butethal can be increased when used in combination with Lofexidine.Approved, Illicit
ButorphanolThe therapeutic efficacy of Butorphanol can be increased when used in combination with Lofexidine.Approved, Illicit, Vet Approved
ButriptylineButriptyline may decrease the antihypertensive activities of Lofexidine.Approved
CabergolineCabergoline may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved
CadralazineCadralazine may increase the hypotensive activities of Lofexidine.Experimental
CafedrineLofexidine may increase the hypotensive activities of Cafedrine.Investigational
CaffeineThe metabolism of Lofexidine can be decreased when combined with Caffeine.Approved
CanagliflozinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Canagliflozin.Approved
CandesartanLofexidine may increase the hypotensive activities of Candesartan.Experimental
Candesartan cilexetilCandesartan cilexetil may increase the hypotensive activities of Lofexidine.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Lofexidine.Experimental
CanertinibThe therapeutic efficacy of Canertinib can be increased when used in combination with Lofexidine.Investigational
CaptoprilCaptopril may increase the hypotensive activities of Lofexidine.Approved
CarbamazepineThe therapeutic efficacy of Carbamazepine can be increased when used in combination with Lofexidine.Approved, Investigational
CarbetocinThe risk or severity of adverse effects can be increased when Carbetocin is combined with Lofexidine.Approved, Investigational
CarbinoxamineThe therapeutic efficacy of Carbinoxamine can be increased when used in combination with Lofexidine.Approved
CarfentanilThe therapeutic efficacy of Carfentanil can be increased when used in combination with Lofexidine.Illicit, Investigational, Vet Approved
CarisoprodolThe therapeutic efficacy of Carisoprodol can be increased when used in combination with Lofexidine.Approved
CaroxazoneThe metabolism of Lofexidine can be decreased when combined with Caroxazone.Withdrawn
CarteololLofexidine may increase the atrioventricular blocking (AV block) activities of Carteolol.Approved
CarvedilolLofexidine may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CelecoxibThe metabolism of Lofexidine can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololLofexidine may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
CetirizineThe therapeutic efficacy of Cetirizine can be increased when used in combination with Lofexidine.Approved
Chloral hydrateThe therapeutic efficacy of Chloral hydrate can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational, Vet Approved
ChloramphenicolThe metabolism of Lofexidine can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlordiazepoxideThe therapeutic efficacy of Chlordiazepoxide can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
ChlormezanoneThe therapeutic efficacy of Chlormezanone can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
ChloroprocaineThe therapeutic efficacy of Chloroprocaine can be increased when used in combination with Lofexidine.Approved
ChloroquineThe metabolism of Lofexidine can be decreased when combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Lofexidine.Approved, Vet Approved
ChlorphenamineThe therapeutic efficacy of Chlorphenamine can be increased when used in combination with Lofexidine.Approved
ChlorpromazineThe therapeutic efficacy of Chlorpromazine can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
ChlorprothixeneThe therapeutic efficacy of Chlorprothixene can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Lofexidine.Approved
ChlorzoxazoneThe therapeutic efficacy of Chlorzoxazone can be increased when used in combination with Lofexidine.Approved
CholecalciferolThe metabolism of Lofexidine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CicletanineLofexidine may increase the hypotensive activities of Cicletanine.Investigational
CilazaprilCilazapril may increase the hypotensive activities of Lofexidine.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Cilnidipine is combined with Lofexidine.Approved, Investigational
CimetidineThe metabolism of Lofexidine can be decreased when combined with Cimetidine.Approved, Investigational
CinacalcetThe metabolism of Lofexidine can be decreased when combined with Cinacalcet.Approved
CinchocaineThe therapeutic efficacy of Cinchocaine can be increased when used in combination with Lofexidine.Approved, Vet Approved
CitalopramThe metabolism of Lofexidine can be decreased when combined with Citalopram.Approved
ClemastineThe therapeutic efficacy of Clemastine can be increased when used in combination with Lofexidine.Approved, Investigational
ClevidipineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Clevidipine.Approved, Investigational
ClidiniumThe therapeutic efficacy of Clidinium can be increased when used in combination with Lofexidine.Approved
ClobazamThe therapeutic efficacy of Clobazam can be increased when used in combination with Lofexidine.Approved, Illicit
ClofarabineThe risk or severity of adverse effects can be increased when Clofarabine is combined with Lofexidine.Approved, Investigational
clomethiazoleThe therapeutic efficacy of clomethiazole can be increased when used in combination with Lofexidine.Investigational
ClomipramineThe therapeutic efficacy of Clomipramine can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
ClonazepamThe therapeutic efficacy of Clonazepam can be increased when used in combination with Lofexidine.Approved, Illicit
ClonidineThe therapeutic efficacy of Clonidine can be increased when used in combination with Lofexidine.Approved
ClopenthixolThe therapeutic efficacy of Clopenthixol can be increased when used in combination with Lofexidine.Experimental
CloranololLofexidine may increase the atrioventricular blocking (AV block) activities of Cloranolol.Experimental
ClorazepateThe therapeutic efficacy of Clorazepate can be increased when used in combination with Lofexidine.Approved, Illicit
ClothiapineThe therapeutic efficacy of Clothiapine can be increased when used in combination with Lofexidine.Experimental
ClotrimazoleThe metabolism of Lofexidine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Clozapine can be increased when used in combination with Lofexidine.Approved
CobicistatThe serum concentration of Lofexidine can be increased when it is combined with Cobicistat.Approved
CocaineThe therapeutic efficacy of Cocaine can be increased when used in combination with Lofexidine.Approved, Illicit
CodeineThe therapeutic efficacy of Codeine can be increased when used in combination with Lofexidine.Approved, Illicit
ConivaptanThe risk or severity of adverse effects can be increased when Conivaptan is combined with Lofexidine.Approved, Investigational
CryptenamineCryptenamine may increase the hypotensive activities of Lofexidine.Approved
CurcuminThe metabolism of Lofexidine can be decreased when combined with Curcumin.Approved, Investigational
CyclizineThe therapeutic efficacy of Cyclizine can be increased when used in combination with Lofexidine.Approved
CyclobenzaprineThe therapeutic efficacy of Cyclobenzaprine can be increased when used in combination with Lofexidine.Approved
CyclopenthiazideLofexidine may increase the hypotensive activities of Cyclopenthiazide.Experimental
CyclopropaneThe therapeutic efficacy of Cyclopropane can be increased when used in combination with Lofexidine.Experimental
CyclothiazideCyclothiazide may increase the hypotensive activities of Lofexidine.Approved
CyproheptadineThe therapeutic efficacy of Cyproheptadine can be increased when used in combination with Lofexidine.Approved
Cyproterone acetateThe serum concentration of Lofexidine can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Lofexidine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DantroleneThe therapeutic efficacy of Dantrolene can be increased when used in combination with Lofexidine.Approved, Investigational
DapagliflozinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Dapagliflozin.Approved
DapiprazoleThe therapeutic efficacy of Dapiprazole can be increased when used in combination with Lofexidine.Approved
DarifenacinThe metabolism of Lofexidine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Lofexidine can be increased when it is combined with Darunavir.Approved
DebrisoquinDebrisoquin may increase the hypotensive activities of Lofexidine.Approved, Investigational
DeferasiroxThe serum concentration of Lofexidine can be increased when it is combined with Deferasirox.Approved, Investigational
DelaprilLofexidine may increase the hypotensive activities of Delapril.Investigational
DelavirdineThe metabolism of Lofexidine can be decreased when combined with Delavirdine.Approved
DeramciclaneThe therapeutic efficacy of Deramciclane can be increased when used in combination with Lofexidine.Investigational
DeserpidineLofexidine may increase the hypotensive activities of Deserpidine.Approved
DesfluraneThe therapeutic efficacy of Desflurane can be increased when used in combination with Lofexidine.Approved
DesipramineThe therapeutic efficacy of Desipramine can be increased when used in combination with Lofexidine.Approved, Investigational
DesloratadineThe therapeutic efficacy of Desloratadine can be increased when used in combination with Lofexidine.Approved, Investigational
DesvenlafaxineDesvenlafaxine may increase the tachycardic activities of Lofexidine.Approved, Investigational
DetomidineThe therapeutic efficacy of Detomidine can be increased when used in combination with Lofexidine.Vet Approved
DexbrompheniramineThe therapeutic efficacy of Dexbrompheniramine can be increased when used in combination with Lofexidine.Approved
DexmedetomidineThe therapeutic efficacy of Dexmedetomidine can be increased when used in combination with Lofexidine.Approved, Vet Approved
DextroamphetamineDextroamphetamine may decrease the vasoconstricting activities of Lofexidine.Approved, Illicit
DextromoramideThe therapeutic efficacy of Dextromoramide can be increased when used in combination with Lofexidine.Experimental, Illicit
DextropropoxypheneThe therapeutic efficacy of Dextropropoxyphene can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational, Withdrawn
DezocineThe therapeutic efficacy of Dezocine can be increased when used in combination with Lofexidine.Approved, Investigational
DiazepamThe therapeutic efficacy of Diazepam can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational, Vet Approved
DiazoxideDiazoxide may increase the hypotensive activities of Lofexidine.Approved
DibenzepinDibenzepin may decrease the antihypertensive activities of Lofexidine.Experimental
DiclofenamideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Diclofenamide.Approved, Investigational
Diethyl etherThe therapeutic efficacy of Diethyl ether can be increased when used in combination with Lofexidine.Experimental
DiethylnorspermineLofexidine may increase the hypotensive activities of Diethylnorspermine.Investigational
DifenoxinThe therapeutic efficacy of Difenoxin can be increased when used in combination with Lofexidine.Approved, Illicit
DihydralazineDihydralazine may increase the hypotensive activities of Lofexidine.Approved, Investigational
DihydrocodeineThe therapeutic efficacy of Dihydrocodeine can be increased when used in combination with Lofexidine.Approved, Illicit
DihydroergocornineDihydroergocornine may increase the hypertensive activities of Lofexidine.Approved
DihydroergocristineDihydroergocristine may increase the hypertensive activities of Lofexidine.Approved, Experimental
DihydroergocryptineDihydroergocryptine may increase the hypertensive activities of Lofexidine.Experimental
DihydroergotamineDihydroergotamine may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved, Investigational
DihydroetorphineThe therapeutic efficacy of Dihydroetorphine can be increased when used in combination with Lofexidine.Experimental, Illicit
DihydromorphineThe therapeutic efficacy of Dihydromorphine can be increased when used in combination with Lofexidine.Experimental, Illicit
DiltiazemDiltiazem may increase the hypotensive activities of Lofexidine.Approved, Investigational
DimenhydrinateThe therapeutic efficacy of Dimenhydrinate can be increased when used in combination with Lofexidine.Approved
DimetacrineDimetacrine may decrease the antihypertensive activities of Lofexidine.Approved, Withdrawn
DinutuximabThe risk or severity of adverse effects can be increased when Lofexidine is combined with Dinutuximab.Approved, Investigational
DiphenhydramineThe therapeutic efficacy of Diphenhydramine can be increased when used in combination with Lofexidine.Approved, Investigational
DiphenoxylateThe therapeutic efficacy of Diphenoxylate can be increased when used in combination with Lofexidine.Approved, Illicit
DipyridamoleThe risk or severity of adverse effects can be increased when Lofexidine is combined with Dipyridamole.Approved
DixyrazineThe therapeutic efficacy of Dixyrazine can be increased when used in combination with Lofexidine.Experimental
DoramectinThe therapeutic efficacy of Doramectin can be increased when used in combination with Lofexidine.Vet Approved
DorzolamideDorzolamide may increase the hypotensive activities of Lofexidine.Approved
DosulepinDosulepin may decrease the antihypertensive activities of Lofexidine.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Lofexidine.Approved
DoxepinThe therapeutic efficacy of Doxepin can be increased when used in combination with Lofexidine.Approved, Investigational
DoxylamineThe therapeutic efficacy of Doxylamine can be increased when used in combination with Lofexidine.Approved, Vet Approved
DPDPEThe therapeutic efficacy of DPDPE can be increased when used in combination with Lofexidine.Experimental
DronedaroneThe metabolism of Lofexidine can be decreased when combined with Dronedarone.Approved
DroperidolThe therapeutic efficacy of Droperidol can be increased when used in combination with Lofexidine.Approved, Vet Approved
DrotebanolThe therapeutic efficacy of Drotebanol can be increased when used in combination with Lofexidine.Experimental, Illicit
DroxidopaLofexidine may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineLofexidine may increase the orthostatic hypotensive activities of Duloxetine.Approved
DyclonineThe therapeutic efficacy of Dyclonine can be increased when used in combination with Lofexidine.Approved
EcgonineThe therapeutic efficacy of Ecgonine can be increased when used in combination with Lofexidine.Experimental, Illicit
EcopipamThe therapeutic efficacy of Ecopipam can be increased when used in combination with Lofexidine.Investigational
EfavirenzThe therapeutic efficacy of Efavirenz can be increased when used in combination with Lofexidine.Approved, Investigational
EfonidipineLofexidine may increase the hypotensive activities of Efonidipine.Approved, Investigational
EliglustatThe metabolism of Lofexidine can be decreased when combined with Eliglustat.Approved
EltanoloneThe therapeutic efficacy of Eltanolone can be increased when used in combination with Lofexidine.Investigational
EmpagliflozinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Empagliflozin.Approved
EnalaprilEnalapril may increase the hypotensive activities of Lofexidine.Approved, Vet Approved
EnalaprilatLofexidine may increase the hypotensive activities of Enalaprilat.Approved
EndralazineEndralazine may increase the hypotensive activities of Lofexidine.Experimental
EnfluraneThe therapeutic efficacy of Enflurane can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
EntacaponeThe therapeutic efficacy of Entacapone can be increased when used in combination with Lofexidine.Approved, Investigational
EpanololLofexidine may increase the atrioventricular blocking (AV block) activities of Epanolol.Experimental
EpinephrineEpinephrine may decrease the vasoconstricting activities of Lofexidine.Approved, Vet Approved
EplerenoneThe risk or severity of adverse effects can be increased when Lofexidine is combined with Eplerenone.Approved
EpoprostenolEpoprostenol may increase the hypotensive activities of Lofexidine.Approved
EprosartanEprosartan may increase the hypotensive activities of Lofexidine.Approved
Ergoloid mesylateErgoloid mesylate may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved
ErgonovineErgonovine may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved
ErgotamineErgotamine may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved
EsatenololLofexidine may increase the atrioventricular blocking (AV block) activities of Esatenolol.Experimental
EscitalopramEscitalopram may decrease the vasoconstricting activities of Lofexidine.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Lofexidine can be decreased when combined with Eslicarbazepine acetate.Approved
EsmololLofexidine may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
EsomeprazoleThe metabolism of Lofexidine can be decreased when combined with Esomeprazole.Approved, Investigational
EstazolamThe therapeutic efficacy of Estazolam can be increased when used in combination with Lofexidine.Approved, Illicit
EszopicloneThe therapeutic efficacy of Eszopiclone can be increased when used in combination with Lofexidine.Approved, Investigational
Etacrynic acidThe risk or severity of adverse effects can be increased when Lofexidine is combined with Etacrynic acid.Approved, Investigational
EthanolThe therapeutic efficacy of Ethanol can be increased when used in combination with Lofexidine.Approved
EthchlorvynolThe therapeutic efficacy of Ethchlorvynol can be increased when used in combination with Lofexidine.Approved, Illicit, Withdrawn
EthosuximideThe therapeutic efficacy of Ethosuximide can be increased when used in combination with Lofexidine.Approved
EthotoinThe therapeutic efficacy of Ethotoin can be increased when used in combination with Lofexidine.Approved
Ethyl carbamateThe therapeutic efficacy of Ethyl carbamate can be increased when used in combination with Lofexidine.Withdrawn
Ethyl chlorideThe therapeutic efficacy of Ethyl chloride can be increased when used in combination with Lofexidine.Approved, Experimental, Investigational
Ethyl loflazepateThe therapeutic efficacy of Ethyl loflazepate can be increased when used in combination with Lofexidine.Approved, Illicit
EthylmorphineThe therapeutic efficacy of Ethylmorphine can be increased when used in combination with Lofexidine.Approved, Illicit
EtidocaineThe therapeutic efficacy of Etidocaine can be increased when used in combination with Lofexidine.Approved
EtifoxineThe therapeutic efficacy of Etifoxine can be increased when used in combination with Lofexidine.Investigational, Withdrawn
EtizolamThe therapeutic efficacy of Etizolam can be increased when used in combination with Lofexidine.Approved
EtomidateThe therapeutic efficacy of Etomidate can be increased when used in combination with Lofexidine.Approved
EtorphineThe therapeutic efficacy of Etorphine can be increased when used in combination with Lofexidine.Illicit, Vet Approved
EtravirineThe metabolism of Lofexidine can be decreased when combined with Etravirine.Approved
EzogabineThe therapeutic efficacy of Ezogabine can be increased when used in combination with Lofexidine.Approved, Investigational
FelbamateThe therapeutic efficacy of Felbamate can be increased when used in combination with Lofexidine.Approved
FelodipineFelodipine may increase the hypotensive activities of Lofexidine.Approved, Investigational
FencamfamineThe therapeutic efficacy of Fencamfamine can be increased when used in combination with Lofexidine.Approved, Illicit, Withdrawn
FenoldopamFenoldopam may increase the hypotensive activities of Lofexidine.Approved
FentanylThe therapeutic efficacy of Fentanyl can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational, Vet Approved
Ferulic acidLofexidine may increase the hypotensive activities of Ferulic acid.Experimental
FexofenadineThe therapeutic efficacy of Fexofenadine can be increased when used in combination with Lofexidine.Approved, Investigational
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Lofexidine.Approved, Investigational
FlibanserinThe therapeutic efficacy of Flibanserin can be increased when used in combination with Lofexidine.Approved, Investigational
FluanisoneThe therapeutic efficacy of Fluanisone can be increased when used in combination with Lofexidine.Experimental
FluconazoleThe metabolism of Lofexidine can be decreased when combined with Fluconazole.Approved, Investigational
FludiazepamThe therapeutic efficacy of Fludiazepam can be increased when used in combination with Lofexidine.Approved, Illicit
FlunarizineThe therapeutic efficacy of Flunarizine can be increased when used in combination with Lofexidine.Approved
FlunitrazepamThe therapeutic efficacy of Flunitrazepam can be increased when used in combination with Lofexidine.Approved, Illicit
FluoxetineThe metabolism of Lofexidine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe therapeutic efficacy of Flupentixol can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
FluphenazineThe therapeutic efficacy of Fluphenazine can be increased when used in combination with Lofexidine.Approved
FlurazepamThe therapeutic efficacy of Flurazepam can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
FluspirileneThe therapeutic efficacy of Fluspirilene can be increased when used in combination with Lofexidine.Approved, Investigational
Fluticasone propionateThe therapeutic efficacy of Fluticasone propionate can be increased when used in combination with Lofexidine.Approved
FluvoxamineThe therapeutic efficacy of Fluvoxamine can be increased when used in combination with Lofexidine.Approved, Investigational
FosinoprilFosinopril may increase the hypotensive activities of Lofexidine.Approved
FosphenytoinThe therapeutic efficacy of Fosphenytoin can be increased when used in combination with Lofexidine.Approved, Investigational
FospropofolThe therapeutic efficacy of Fospropofol can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
FostamatinibFostamatinib may increase the antihypertensive activities of Lofexidine.Approved, Investigational
FurazolidoneThe metabolism of Lofexidine can be decreased when combined with Furazolidone.Approved, Investigational, Vet Approved
FurosemideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Furosemide.Approved, Vet Approved
GabapentinThe therapeutic efficacy of Gabapentin can be increased when used in combination with Lofexidine.Approved, Investigational
Gabapentin EnacarbilThe therapeutic efficacy of Gabapentin Enacarbil can be increased when used in combination with Lofexidine.Approved, Investigational
Gamma Hydroxybutyric AcidThe therapeutic efficacy of Gamma Hydroxybutyric Acid can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
GemfibrozilThe metabolism of Lofexidine can be decreased when combined with Gemfibrozil.Approved
GepironeThe therapeutic efficacy of Gepirone can be increased when used in combination with Lofexidine.Investigational
GlutethimideThe therapeutic efficacy of Glutethimide can be increased when used in combination with Lofexidine.Approved, Illicit
GuanabenzGuanabenz may increase the hypotensive activities of Lofexidine.Approved, Investigational
GuanadrelGuanadrel may increase the hypotensive activities of Lofexidine.Approved
GuanazodineLofexidine may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineGuanethidine may increase the hypotensive activities of Lofexidine.Approved
GuanfacineThe therapeutic efficacy of Guanfacine can be increased when used in combination with Lofexidine.Approved, Investigational
GuanoclorLofexidine may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzLofexidine may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanLofexidine may increase the hypotensive activities of Guanoxan.Experimental
HalazepamThe therapeutic efficacy of Halazepam can be increased when used in combination with Lofexidine.Approved, Illicit, Withdrawn
HaloperidolThe therapeutic efficacy of Haloperidol can be increased when used in combination with Lofexidine.Approved
HalothaneThe therapeutic efficacy of Halothane can be increased when used in combination with Lofexidine.Approved, Vet Approved
HarmalineThe metabolism of Lofexidine can be decreased when combined with Harmaline.Experimental
HeroinThe therapeutic efficacy of Heroin can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
HexamethoniumLofexidine may increase the hypotensive activities of Hexamethonium.Experimental
HexobarbitalThe therapeutic efficacy of Hexobarbital can be increased when used in combination with Lofexidine.Approved
HyaluronidaseHyaluronidase may increase the vasoconstricting activities of Lofexidine.Approved, Investigational
HydracarbazineThe metabolism of Lofexidine can be decreased when combined with Hydracarbazine.Experimental
HydralazineHydralazine may increase the hypotensive activities of Lofexidine.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Lofexidine.Approved, Vet Approved
HydrocodoneThe therapeutic efficacy of Hydrocodone can be increased when used in combination with Lofexidine.Approved, Illicit
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Lofexidine.Approved, Investigational
HydromorphoneThe therapeutic efficacy of Hydromorphone can be increased when used in combination with Lofexidine.Approved, Illicit
HydroxyzineThe therapeutic efficacy of Hydroxyzine can be increased when used in combination with Lofexidine.Approved
IloperidoneThe therapeutic efficacy of Iloperidone can be increased when used in combination with Lofexidine.Approved
IloprostThe risk or severity of adverse effects can be increased when Iloprost is combined with Lofexidine.Approved, Investigational
ImidaprilThe risk or severity of adverse effects can be increased when Imidapril is combined with Lofexidine.Investigational
ImipramineThe therapeutic efficacy of Imipramine can be increased when used in combination with Lofexidine.Approved
IndapamideIndapamide may increase the hypotensive activities of Lofexidine.Approved
IndenololLofexidine may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndinavirThe metabolism of Lofexidine can be decreased when combined with Indinavir.Approved
IndiplonThe therapeutic efficacy of Indiplon can be increased when used in combination with Lofexidine.Investigational
IndoraminIndoramin may increase the hypotensive activities of Lofexidine.Withdrawn
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Lofexidine.Approved, Investigational
IprindoleIprindole may decrease the antihypertensive activities of Lofexidine.Experimental
IproclozideThe metabolism of Lofexidine can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Lofexidine can be decreased when combined with Iproniazid.Withdrawn
IrbesartanIrbesartan may increase the hypotensive activities of Lofexidine.Approved, Investigational
IsocarboxazidThe metabolism of Lofexidine can be decreased when combined with Isocarboxazid.Approved
IsofluraneThe therapeutic efficacy of Isoflurane can be increased when used in combination with Lofexidine.Approved, Vet Approved
IsoniazidThe metabolism of Lofexidine can be decreased when combined with Isoniazid.Approved, Investigational
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Lofexidine is combined with Isosorbide Dinitrate.Approved, Investigational
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Lofexidine is combined with Isosorbide Mononitrate.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Isoxsuprine.Approved, Withdrawn
IsradipineIsradipine may increase the hypotensive activities of Lofexidine.Approved, Investigational
KetamineThe therapeutic efficacy of Ketamine can be increased when used in combination with Lofexidine.Approved, Vet Approved
KetanserinKetanserin may increase the hypotensive activities of Lofexidine.Investigational
KetazolamThe therapeutic efficacy of Ketazolam can be increased when used in combination with Lofexidine.Approved
KetobemidoneThe therapeutic efficacy of Ketobemidone can be increased when used in combination with Lofexidine.Approved, Investigational
KetoconazoleThe metabolism of Lofexidine can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolLofexidine may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LacidipineLofexidine may increase the hypotensive activities of Lacidipine.Approved, Investigational
LamotrigineThe therapeutic efficacy of Lamotrigine can be increased when used in combination with Lofexidine.Approved, Investigational
LandiololLofexidine may increase the atrioventricular blocking (AV block) activities of Landiolol.Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Lofexidine.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Lofexidine.Approved, Investigational
LevetiracetamThe therapeutic efficacy of Levetiracetam can be increased when used in combination with Lofexidine.Approved, Investigational
LevobetaxololLofexidine may increase the atrioventricular blocking (AV block) activities of Levobetaxolol.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Lofexidine is combined with Levobunolol.Approved
LevobupivacaineThe therapeutic efficacy of Levobupivacaine can be increased when used in combination with Lofexidine.Approved, Investigational
LevocabastineThe therapeutic efficacy of Levocabastine can be increased when used in combination with Lofexidine.Approved, Investigational
LevocetirizineThe therapeutic efficacy of Levocetirizine can be increased when used in combination with Lofexidine.Approved
LevodopaLofexidine may increase the orthostatic hypotensive activities of Levodopa.Approved
Levomethadyl AcetateThe risk or severity of QTc prolongation can be increased when Lofexidine is combined with Levomethadyl Acetate.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the tachycardic activities of Lofexidine.Approved, Investigational
LevorphanolThe therapeutic efficacy of Levorphanol can be increased when used in combination with Lofexidine.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Levosimendan is combined with Lofexidine.Approved, Investigational
LidocaineThe therapeutic efficacy of Lidocaine can be increased when used in combination with Lofexidine.Approved, Vet Approved
LinsidomineLofexidine may increase the hypotensive activities of Linsidomine.Experimental
LisdexamfetamineLisdexamfetamine may decrease the vasoconstricting activities of Lofexidine.Approved, Investigational
LisinoprilLisinopril may increase the hypotensive activities of Lofexidine.Approved, Investigational
LisurideLisuride may increase the hypertensive activities of Lofexidine.Approved, Investigational
Lithium cationThe therapeutic efficacy of Lithium can be increased when used in combination with Lofexidine.Experimental
LobeglitazoneThe metabolism of Lofexidine can be decreased when combined with Lobeglitazone.Approved, Investigational
LofentanilThe therapeutic efficacy of Lofentanil can be increased when used in combination with Lofexidine.Illicit
LofepramineLofepramine may decrease the antihypertensive activities of Lofexidine.Experimental
LopinavirThe metabolism of Lofexidine can be decreased when combined with Lopinavir.Approved
LoprazolamThe therapeutic efficacy of Loprazolam can be increased when used in combination with Lofexidine.Experimental
LoratadineThe therapeutic efficacy of Loratadine can be increased when used in combination with Lofexidine.Approved, Investigational
LorazepamThe therapeutic efficacy of Lorazepam can be increased when used in combination with Lofexidine.Approved
LorcaserinThe metabolism of Lofexidine can be decreased when combined with Lorcaserin.Approved
LormetazepamThe therapeutic efficacy of Lormetazepam can be increased when used in combination with Lofexidine.Approved
LosartanLosartan may increase the hypotensive activities of Lofexidine.Approved
LoxapineThe therapeutic efficacy of Loxapine can be increased when used in combination with Lofexidine.Approved
LuliconazoleThe serum concentration of Lofexidine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Lofexidine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Lofexidine can be decreased when combined with Lumefantrine.Approved
LurasidoneThe therapeutic efficacy of Lurasidone can be increased when used in combination with Lofexidine.Approved, Investigational
Lysergic Acid DiethylamideLysergic Acid Diethylamide may increase the hypertensive activities of Lofexidine.Illicit, Investigational, Withdrawn
MacitentanLofexidine may increase the hypotensive activities of Macitentan.Approved
Magnesium sulfateThe therapeutic efficacy of Magnesium sulfate can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
ManidipineLofexidine may increase the hypotensive activities of Manidipine.Approved, Investigational
MannitolThe risk or severity of adverse effects can be increased when Lofexidine is combined with Mannitol.Approved, Investigational
MaprotilineThe therapeutic efficacy of Maprotiline can be increased when used in combination with Lofexidine.Approved, Investigational
MebanazineThe metabolism of Lofexidine can be decreased when combined with Mebanazine.Withdrawn
MebicarThe therapeutic efficacy of Mebicar can be increased when used in combination with Lofexidine.Experimental
MecamylamineMecamylamine may increase the hypotensive activities of Lofexidine.Approved, Investigational
MeclizineThe therapeutic efficacy of Meclizine can be increased when used in combination with Lofexidine.Approved
MedazepamThe therapeutic efficacy of Medazepam can be increased when used in combination with Lofexidine.Experimental
MedetomidineThe therapeutic efficacy of Medetomidine can be increased when used in combination with Lofexidine.Vet Approved
MelatoninThe therapeutic efficacy of Melatonin can be increased when used in combination with Lofexidine.Approved, Nutraceutical, Vet Approved
MelitracenMelitracen may decrease the antihypertensive activities of Lofexidine.Experimental, Investigational
MelperoneThe therapeutic efficacy of Melperone can be increased when used in combination with Lofexidine.Approved, Investigational
MepindololLofexidine may increase the atrioventricular blocking (AV block) activities of Mepindolol.Experimental
MepivacaineThe therapeutic efficacy of Mepivacaine can be increased when used in combination with Lofexidine.Approved, Vet Approved
MeprobamateThe therapeutic efficacy of Meprobamate can be increased when used in combination with Lofexidine.Approved, Illicit
MeptazinolThe therapeutic efficacy of Meptazinol can be increased when used in combination with Lofexidine.Experimental
MesoridazineThe therapeutic efficacy of Mesoridazine can be increased when used in combination with Lofexidine.Approved, Investigational
MetaxaloneThe therapeutic efficacy of Metaxalone can be increased when used in combination with Lofexidine.Approved
MetergolineMetergoline may increase the hypertensive activities of Lofexidine.Experimental
MethadoneThe therapeutic efficacy of Methadone can be increased when used in combination with Lofexidine.Approved
Methadyl AcetateThe risk or severity of QTc prolongation can be increased when Lofexidine is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe therapeutic efficacy of Methapyrilene can be increased when used in combination with Lofexidine.Withdrawn
MethaqualoneThe therapeutic efficacy of Methaqualone can be increased when used in combination with Lofexidine.Illicit, Withdrawn
MethazolamideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Methazolamide.Approved
MethocarbamolThe therapeutic efficacy of Methocarbamol can be increased when used in combination with Lofexidine.Approved, Vet Approved
MethohexitalThe therapeutic efficacy of Methohexital can be increased when used in combination with Lofexidine.Approved
MethoserpidineLofexidine may increase the hypotensive activities of Methoserpidine.Experimental
MethotrimeprazineThe therapeutic efficacy of Methotrimeprazine can be increased when used in combination with Lofexidine.Approved, Investigational
MethoxyfluraneThe therapeutic efficacy of Methoxyflurane can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
MethsuximideThe therapeutic efficacy of Methsuximide can be increased when used in combination with Lofexidine.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Methyclothiazide.Approved
MethyldopaMethyldopa may increase the hypotensive activities of Lofexidine.Approved
MethylecgonineThe therapeutic efficacy of Methylecgonine can be increased when used in combination with Lofexidine.Experimental
Methylene blueThe metabolism of Lofexidine can be decreased when combined with Methylene blue.Approved, Investigational
MethylergometrineMethylergometrine may increase the hypertensive and vasoconstricting activities of Lofexidine.Approved
MethylnaltrexoneThe risk or severity of adverse effects can be increased when Lofexidine is combined with Methylnaltrexone.Approved
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Lofexidine.Approved, Investigational
MethylphenobarbitalThe therapeutic efficacy of Methylphenobarbital can be increased when used in combination with Lofexidine.Approved
MethysergideMethysergide may increase the hypertensive activities of Lofexidine.Approved
MetipranololMetipranolol may increase the hypotensive activities of Lofexidine.Approved
MetolazoneMetolazone may increase the hypotensive activities of Lofexidine.Approved
MetoprololLofexidine may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
MetyrosineLofexidine may increase the hypotensive activities of Metyrosine.Approved
MexiletineThe metabolism of Lofexidine can be decreased when combined with Mexiletine.Approved, Investigational
MianserinThe therapeutic efficacy of Lofexidine can be decreased when used in combination with Mianserin.Approved, Investigational
MibefradilMibefradil may increase the hypotensive activities of Lofexidine.Investigational, Withdrawn
MidazolamThe therapeutic efficacy of Midazolam can be increased when used in combination with Lofexidine.Approved, Illicit
MidostaurinThe metabolism of Lofexidine can be decreased when combined with Midostaurin.Approved, Investigational
MilnacipranMilnacipran may increase the tachycardic activities of Lofexidine.Approved, Investigational
MinaprineThe metabolism of Lofexidine can be decreased when combined with Minaprine.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Lofexidine.Approved, Investigational
MirabegronThe metabolism of Lofexidine can be decreased when combined with Mirabegron.Approved
MirodenafilMirodenafil may increase the antihypertensive activities of Lofexidine.Investigational
MirtazapineMirtazapine may decrease the antihypertensive activities of Lofexidine.Approved
MoclobemideThe metabolism of Lofexidine can be decreased when combined with Moclobemide.Approved, Investigational
ModafinilThe metabolism of Lofexidine can be decreased when combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the hypotensive activities of Lofexidine.Approved
MolindoneThe therapeutic efficacy of Molindone can be increased when used in combination with Lofexidine.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Lofexidine.Approved, Investigational
MorphineThe therapeutic efficacy of Morphine can be increased when used in combination with Lofexidine.Approved, Investigational
MoxonidineMoxonidine may increase the hypotensive activities of Lofexidine.Approved, Investigational
MuzolimineLofexidine may increase the hypotensive activities of Muzolimine.Experimental
NabiloneThe therapeutic efficacy of Nabilone can be increased when used in combination with Lofexidine.Approved, Investigational
NadololLofexidine may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NaftopidilLofexidine may increase the hypotensive activities of Naftopidil.Investigational
NalbuphineThe therapeutic efficacy of Nalbuphine can be increased when used in combination with Lofexidine.Approved
NaloxegolThe risk or severity of adverse effects can be increased when Lofexidine is combined with Naloxegol.Approved
NaltrexoneThe bioavailability of Naltrexone can be decreased when combined with Lofexidine.Approved, Investigational, Vet Approved
NebivololLofexidine may increase the atrioventricular blocking (AV block) activities of Nebivolol.Approved, Investigational
NefazodoneNefazodone may decrease the vasoconstricting activities of Lofexidine.Approved, Withdrawn
NelfinavirThe metabolism of Lofexidine can be decreased when combined with Nelfinavir.Approved
NesiritideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Nesiritide.Approved, Investigational
NevirapineThe metabolism of Lofexidine can be decreased when combined with Nevirapine.Approved
NialamideThe metabolism of Lofexidine can be decreased when combined with Nialamide.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Lofexidine.Approved, Investigational
NicergolineNicergoline may increase the hypertensive activities of Lofexidine.Approved, Investigational
NicorandilNicorandil may increase the hypotensive activities of Lofexidine.Approved, Investigational
NifedipineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Nifedipine.Approved
NiguldipineLofexidine may increase the hypotensive activities of Niguldipine.Experimental
NilotinibThe metabolism of Lofexidine can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineLofexidine may increase the hypotensive activities of Nilvadipine.Approved, Investigational
NimodipineNimodipine may increase the hypotensive activities of Lofexidine.Approved, Investigational
NisoldipineNisoldipine may increase the hypotensive activities of Lofexidine.Approved
NitrazepamThe therapeutic efficacy of Nitrazepam can be increased when used in combination with Lofexidine.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Lofexidine.Approved, Investigational
Nitric OxideThe risk or severity of adverse effects can be increased when Lofexidine is combined with Nitric Oxide.Approved
NitroglycerinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Nitroglycerin.Approved, Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Lofexidine.Approved, Investigational
Nitrous acidThe risk or severity of adverse effects can be increased when Lofexidine is combined with Nitrous acid.Approved, Investigational
Nitrous oxideThe therapeutic efficacy of Nitrous oxide can be increased when used in combination with Lofexidine.Approved, Vet Approved
NordazepamThe therapeutic efficacy of Nordazepam can be increased when used in combination with Lofexidine.Approved
NorfluraneThe therapeutic efficacy of Norflurane can be increased when used in combination with Lofexidine.Approved, Investigational
NormethadoneThe therapeutic efficacy of Normethadone can be increased when used in combination with Lofexidine.Approved, Illicit
NortriptylineThe therapeutic efficacy of Nortriptyline can be increased when used in combination with Lofexidine.Approved
ObinutuzumabLofexidine may increase the hypotensive activities of Obinutuzumab.Approved, Investigational
OctamoxinThe metabolism of Lofexidine can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe therapeutic efficacy of Olanzapine can be increased when used in combination with Lofexidine.Approved, Investigational
OlmesartanOlmesartan may increase the hypotensive activities of Lofexidine.Approved, Investigational
OlopatadineThe therapeutic efficacy of Olopatadine can be increased when used in combination with Lofexidine.Approved
OmapatrilatOmapatrilat may increase the hypotensive activities of Lofexidine.Investigational
OmeprazoleThe metabolism of Lofexidine can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe therapeutic efficacy of Ondansetron can be increased when used in combination with Lofexidine.Approved
OpipramolOpipramol may decrease the antihypertensive activities of Lofexidine.Investigational
OpiumThe therapeutic efficacy of Opium can be increased when used in combination with Lofexidine.Approved, Illicit
OrphenadrineThe therapeutic efficacy of Orphenadrine can be increased when used in combination with Lofexidine.Approved
OsanetantThe therapeutic efficacy of Osanetant can be increased when used in combination with Lofexidine.Investigational
OsimertinibThe serum concentration of Lofexidine can be decreased when it is combined with Osimertinib.Approved
OxazepamThe therapeutic efficacy of Oxazepam can be increased when used in combination with Lofexidine.Approved
OxprenololThe therapeutic efficacy of Oxprenolol can be increased when used in combination with Lofexidine.Approved
OxybuprocaineThe therapeutic efficacy of Oxybuprocaine can be increased when used in combination with Lofexidine.Approved, Investigational
OxycodoneThe therapeutic efficacy of Oxycodone can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
OxymorphoneThe therapeutic efficacy of Oxymorphone can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Lofexidine is combined with Paclitaxel.Approved, Vet Approved
PaliperidoneThe therapeutic efficacy of Paliperidone can be increased when used in combination with Lofexidine.Approved
PanobinostatThe serum concentration of Lofexidine can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Lofexidine can be decreased when combined with Pantoprazole.Approved
PapaverineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Papaverine.Approved, Investigational
ParaldehydeThe therapeutic efficacy of Paraldehyde can be increased when used in combination with Lofexidine.Approved, Investigational
PargylineThe metabolism of Lofexidine can be decreased when combined with Pargyline.Approved
ParoxetineParoxetine can cause an increase in the absorption of Lofexidine resulting in an increased serum concentration and potentially a worsening of adverse effects.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Lofexidine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenbutololLofexidine may increase the atrioventricular blocking (AV block) activities of Penbutolol.Approved, Investigational
PenfluridolThe therapeutic efficacy of Penfluridol can be increased when used in combination with Lofexidine.Experimental
PentazocineThe therapeutic efficacy of Pentazocine can be increased when used in combination with Lofexidine.Approved, Vet Approved
PentobarbitalThe therapeutic efficacy of Pentobarbital can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
PentoliniumPentolinium may increase the hypotensive activities of Lofexidine.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Lofexidine.Approved, Investigational
PerampanelThe therapeutic efficacy of Perampanel can be increased when used in combination with Lofexidine.Approved
PerazineThe therapeutic efficacy of Perazine can be increased when used in combination with Lofexidine.Approved, Investigational
PergolidePergolide may increase the hypertensive activities of Lofexidine.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilPerindopril may increase the hypotensive activities of Lofexidine.Approved
PerospironeThe therapeutic efficacy of Perospirone can be increased when used in combination with Lofexidine.Approved
PerphenazineThe therapeutic efficacy of Perphenazine can be increased when used in combination with Lofexidine.Approved
PethidineThe therapeutic efficacy of Pethidine can be increased when used in combination with Lofexidine.Approved
PhenazocineThe therapeutic efficacy of Phenazocine can be increased when used in combination with Lofexidine.Experimental
PhenelzineThe metabolism of Lofexidine can be decreased when combined with Phenelzine.Approved
PhenibutThe therapeutic efficacy of Phenibut can be increased when used in combination with Lofexidine.Experimental
PheniprazineThe metabolism of Lofexidine can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe therapeutic efficacy of Phenobarbital can be increased when used in combination with Lofexidine.Approved, Investigational
PhenoperidineThe therapeutic efficacy of Phenoperidine can be increased when used in combination with Lofexidine.Experimental
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Lofexidine.Approved
PhenoxyethanolThe therapeutic efficacy of Phenoxyethanol can be increased when used in combination with Lofexidine.Approved
PhenoxypropazineThe metabolism of Lofexidine can be decreased when combined with Phenoxypropazine.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Lofexidine.Approved
PhenytoinThe therapeutic efficacy of Phenytoin can be increased when used in combination with Lofexidine.Approved, Vet Approved
PimozideThe therapeutic efficacy of Pimozide can be increased when used in combination with Lofexidine.Approved
PinacidilPinacidil may increase the hypotensive activities of Lofexidine.Approved
PindololLofexidine may increase the atrioventricular blocking (AV block) activities of Pindolol.Approved, Investigational
PipamperoneThe therapeutic efficacy of Pipamperone can be increased when used in combination with Lofexidine.Approved, Investigational
PipotiazineThe therapeutic efficacy of Pipotiazine can be increased when used in combination with Lofexidine.Approved, Investigational
PiritramideThe therapeutic efficacy of Piritramide can be increased when used in combination with Lofexidine.Approved, Investigational
PirlindoleThe metabolism of Lofexidine can be decreased when combined with Pirlindole.Approved
PitolisantThe metabolism of Lofexidine can be decreased when combined with Pitolisant.Approved, Investigational
PivhydrazineThe metabolism of Lofexidine can be decreased when combined with Pivhydrazine.Withdrawn
PizotifenThe therapeutic efficacy of Pizotifen can be increased when used in combination with Lofexidine.Approved
Platelet Activating FactorLofexidine may increase the atrioventricular blocking (AV block) activities of Platelet Activating Factor.Experimental
PolythiazidePolythiazide may increase the hypotensive activities of Lofexidine.Approved
PomalidomideThe therapeutic efficacy of Pomalidomide can be increased when used in combination with Lofexidine.Approved
PractololLofexidine may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PramipexoleThe risk or severity of adverse effects can be increased when Lofexidine is combined with Pramipexole.Approved, Investigational
PramocaineThe therapeutic efficacy of Pramocaine can be increased when used in combination with Lofexidine.Approved
PrazepamThe therapeutic efficacy of Prazepam can be increased when used in combination with Lofexidine.Approved, Illicit
PrazosinPrazosin may increase the hypotensive activities of Lofexidine.Approved
PregabalinThe therapeutic efficacy of Pregabalin can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
PrilocaineThe therapeutic efficacy of Prilocaine can be increased when used in combination with Lofexidine.Approved
PrimidoneThe therapeutic efficacy of Primidone can be increased when used in combination with Lofexidine.Approved, Vet Approved
ProcaineThe therapeutic efficacy of Procaine can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
ProcarbazineThe metabolism of Lofexidine can be decreased when combined with Procarbazine.Approved, Investigational
ProchlorperazineThe therapeutic efficacy of Prochlorperazine can be increased when used in combination with Lofexidine.Approved, Vet Approved
PromazineThe therapeutic efficacy of Promazine can be increased when used in combination with Lofexidine.Approved, Vet Approved
PromethazineThe therapeutic efficacy of Promethazine can be increased when used in combination with Lofexidine.Approved, Investigational
PropafenoneLofexidine may increase the atrioventricular blocking (AV block) activities of Propafenone.Approved
PropanididThe therapeutic efficacy of Propanidid can be increased when used in combination with Lofexidine.Experimental
ProparacaineThe therapeutic efficacy of Proparacaine can be increased when used in combination with Lofexidine.Approved, Vet Approved
PropericiazinePropericiazine may decrease the vasoconstricting activities of Lofexidine.Approved, Investigational
PropiomazinePropiomazine may decrease the vasoconstricting activities of Lofexidine.Approved
PropiverinePropiverine may decrease the vasoconstricting activities of Lofexidine.Approved, Investigational
PropofolThe therapeutic efficacy of Propofol can be increased when used in combination with Lofexidine.Approved, Investigational, Vet Approved
PropoxycaineThe therapeutic efficacy of Propoxycaine can be increased when used in combination with Lofexidine.Approved
PropranololLofexidine may increase the atrioventricular blocking (AV block) activities of Propranolol.Approved, Investigational
ProtriptylineThe therapeutic efficacy of Protriptyline can be increased when used in combination with Lofexidine.Approved
ProxibarbalThe therapeutic efficacy of Proxibarbal can be increased when used in combination with Lofexidine.Experimental
PSD502The therapeutic efficacy of PSD502 can be increased when used in combination with Lofexidine.Investigational
QuazepamThe therapeutic efficacy of Quazepam can be increased when used in combination with Lofexidine.Approved, Illicit
QuetiapineThe therapeutic efficacy of Quetiapine can be increased when used in combination with Lofexidine.Approved
QuinaprilQuinapril may increase the hypotensive activities of Lofexidine.Approved, Investigational
QuinidineThe metabolism of Lofexidine can be decreased when combined with Quinidine.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Lofexidine.Approved
QuinisocaineThe therapeutic efficacy of Quinisocaine can be increased when used in combination with Lofexidine.Experimental
RacepinephrineRacepinephrine may decrease the vasoconstricting activities of Lofexidine.Approved
RacloprideThe therapeutic efficacy of Raclopride can be increased when used in combination with Lofexidine.Investigational
RamelteonThe therapeutic efficacy of Ramelteon can be increased when used in combination with Lofexidine.Approved, Investigational
RamiprilRamipril may increase the hypotensive activities of Lofexidine.Approved
RanolazineThe metabolism of Lofexidine can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe metabolism of Lofexidine can be decreased when combined with Rasagiline.Approved
RemifentanilThe therapeutic efficacy of Remifentanil can be increased when used in combination with Lofexidine.Approved
RemikirenRemikiren may increase the hypotensive activities of Lofexidine.Approved
RemoxiprideThe therapeutic efficacy of Remoxipride can be increased when used in combination with Lofexidine.Approved, Withdrawn
RescinnamineLofexidine may increase the hypotensive activities of Rescinnamine.Approved
ReserpineThe therapeutic efficacy of Reserpine can be increased when used in combination with Lofexidine.Approved, Investigational
RifampicinThe metabolism of Lofexidine can be increased when combined with Rifampicin.Approved
RilmenidineRilmenidine may increase the hypotensive activities of Lofexidine.Approved, Investigational
RiociguatLofexidine may increase the hypotensive activities of Riociguat.Approved
RisperidoneLofexidine may increase the hypotensive activities of Risperidone.Approved, Investigational
RitanserinThe therapeutic efficacy of Ritanserin can be increased when used in combination with Lofexidine.Investigational
RitonavirThe metabolism of Lofexidine can be decreased when combined with Ritonavir.Approved, Investigational
RituximabLofexidine may increase the hypotensive activities of Rituximab.Approved
RolapitantThe metabolism of Lofexidine can be decreased when combined with Rolapitant.Approved, Investigational
RomifidineThe therapeutic efficacy of Romifidine can be increased when used in combination with Lofexidine.Vet Approved
RopiniroleThe risk or severity of adverse effects can be increased when Lofexidine is combined with Ropinirole.Approved, Investigational
RopivacaineThe therapeutic efficacy of Ropivacaine can be increased when used in combination with Lofexidine.Approved
RotigotineThe risk or severity of adverse effects can be increased when Lofexidine is combined with Rotigotine.Approved
RucaparibThe metabolism of Lofexidine can be decreased when combined with Rucaparib.Approved, Investigational
SacubitrilThe risk or severity of adverse effects can be increased when Lofexidine is combined with Sacubitril.Approved
SafrazineThe metabolism of Lofexidine can be decreased when combined with Safrazine.Withdrawn
SaprisartanSaprisartan may increase the hypotensive activities of Lofexidine.Experimental
ScopolamineThe therapeutic efficacy of Scopolamine can be increased when used in combination with Lofexidine.Approved, Investigational
SecobarbitalThe therapeutic efficacy of Secobarbital can be increased when used in combination with Lofexidine.Approved, Vet Approved
SelegilineThe metabolism of Lofexidine can be decreased when combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagLofexidine may increase the hypotensive activities of Selexipag.Approved
SepranoloneThe therapeutic efficacy of Sepranolone can be increased when used in combination with Lofexidine.Investigational
SertindoleThe therapeutic efficacy of Sertindole can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
SertralineThe metabolism of Lofexidine can be decreased when combined with Sertraline.Approved
SevofluraneThe therapeutic efficacy of Sevoflurane can be increased when used in combination with Lofexidine.Approved, Vet Approved
SildenafilSildenafil may increase the antihypertensive activities of Lofexidine.Approved, Investigational
SilodosinSilodosin may decrease the vasoconstricting activities of Lofexidine.Approved
SimeprevirThe metabolism of Lofexidine can be decreased when combined with Simeprevir.Approved
SitaxentanLofexidine may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
Sodium oxybateThe therapeutic efficacy of Sodium oxybate can be increased when used in combination with Lofexidine.Approved
SotalolLofexidine may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
SpiraprilSpirapril may increase the hypotensive activities of Lofexidine.Approved
SpironolactoneSpironolactone may decrease the vasoconstricting activities of Lofexidine.Approved
StiripentolThe therapeutic efficacy of Stiripentol can be increased when used in combination with Lofexidine.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Lofexidine is combined with Streptokinase.Approved, Investigational
SufentanilThe therapeutic efficacy of Sufentanil can be increased when used in combination with Lofexidine.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be increased when used in combination with Lofexidine.Approved, Investigational
SultoprideThe therapeutic efficacy of Sultopride can be increased when used in combination with Lofexidine.Experimental
SuvorexantThe therapeutic efficacy of Suvorexant can be increased when used in combination with Lofexidine.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Lofexidine.Approved, Investigational
TalinololLofexidine may increase the atrioventricular blocking (AV block) activities of Talinolol.Investigational
TamsulosinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Tamsulosin.Approved, Investigational
TandospironeThe therapeutic efficacy of Tandospirone can be increased when used in combination with Lofexidine.Investigational
TapentadolThe therapeutic efficacy of Tapentadol can be increased when used in combination with Lofexidine.Approved
TasimelteonThe therapeutic efficacy of Tasimelteon can be increased when used in combination with Lofexidine.Approved, Investigational
TelmisartanTelmisartan may increase the hypotensive activities of Lofexidine.Approved, Investigational
TemazepamThe therapeutic efficacy of Temazepam can be increased when used in combination with Lofexidine.Approved, Investigational
TemocaprilLofexidine may increase the hypotensive activities of Temocapril.Experimental, Investigational
Tenofovir disoproxilThe metabolism of Lofexidine can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerazosinTerazosin may decrease the vasoconstricting activities of Lofexidine.Approved
TerbinafineThe metabolism of Lofexidine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerbutalineLofexidine may increase the atrioventricular blocking (AV block) activities of Terbutaline.Approved
TergurideTerguride may increase the hypertensive activities of Lofexidine.Experimental
TeriflunomideThe serum concentration of Lofexidine can be decreased when it is combined with Teriflunomide.Approved
TerlipressinTerlipressin may increase the hypotensive activities of Lofexidine.Approved, Investigational
TertatololLofexidine may increase the atrioventricular blocking (AV block) activities of Tertatolol.Experimental
TetrabenazineThe therapeutic efficacy of Tetrabenazine can be increased when used in combination with Lofexidine.Approved, Investigational
TetracaineThe therapeutic efficacy of Tetracaine can be increased when used in combination with Lofexidine.Approved, Vet Approved
TetrahydropalmatineThe therapeutic efficacy of Tetrahydropalmatine can be increased when used in combination with Lofexidine.Investigational
TetrodotoxinThe therapeutic efficacy of Tetrodotoxin can be increased when used in combination with Lofexidine.Investigational
ThalidomideThe therapeutic efficacy of Thalidomide can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
TheodrenalineLofexidine may increase the hypotensive activities of Theodrenaline.Investigational
TheophyllineThe metabolism of Lofexidine can be decreased when combined with Theophylline.Approved
ThiamylalThe therapeutic efficacy of Thiamylal can be increased when used in combination with Lofexidine.Approved, Vet Approved
ThiopentalThe therapeutic efficacy of Thiopental can be increased when used in combination with Lofexidine.Approved, Vet Approved
ThioproperazineThioproperazine may decrease the vasoconstricting activities of Lofexidine.Approved
ThioridazineThe therapeutic efficacy of Thioridazine can be increased when used in combination with Lofexidine.Approved, Withdrawn
ThiothixeneThe therapeutic efficacy of Thiothixene can be increased when used in combination with Lofexidine.Approved
TiagabineThe therapeutic efficacy of Tiagabine can be increased when used in combination with Lofexidine.Approved, Investigational
TianeptineTianeptine may decrease the antihypertensive activities of Lofexidine.Approved, Investigational
TiaprideThe therapeutic efficacy of Tiapride can be increased when used in combination with Lofexidine.Approved, Investigational
TiboloneLofexidine may increase the hypotensive activities of Tibolone.Approved, Investigational
TiclopidineThe metabolism of Lofexidine can be decreased when combined with Ticlopidine.Approved
TicrynafenTicrynafen may increase the hypotensive activities of Lofexidine.Withdrawn
TiletamineThe therapeutic efficacy of Tiletamine can be increased when used in combination with Lofexidine.Vet Approved
TilidineThe therapeutic efficacy of Tilidine can be increased when used in combination with Lofexidine.Experimental
TimololLofexidine may increase the atrioventricular blocking (AV block) activities of Timolol.Approved
TipranavirThe metabolism of Lofexidine can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineThe therapeutic efficacy of Tizanidine can be increased when used in combination with Lofexidine.Approved, Investigational
TolazolineTolazoline may increase the hypotensive activities of Lofexidine.Approved, Vet Approved
TolcaponeThe therapeutic efficacy of Tolcapone can be increased when used in combination with Lofexidine.Approved, Withdrawn
TolonidineLofexidine may increase the hypotensive activities of Tolonidine.Experimental
ToloxatoneThe metabolism of Lofexidine can be decreased when combined with Toloxatone.Approved
TopiramateThe therapeutic efficacy of Topiramate can be increased when used in combination with Lofexidine.Approved
TorasemideTorasemide may increase the hypotensive activities of Lofexidine.Approved
TramadolThe therapeutic efficacy of Tramadol can be increased when used in combination with Lofexidine.Approved, Investigational
TrandolaprilTrandolapril may increase the hypotensive activities of Lofexidine.Approved
TranylcypromineThe therapeutic efficacy of Tranylcypromine can be increased when used in combination with Lofexidine.Approved, Investigational
TravoprostTravoprost may increase the hypotensive activities of Lofexidine.Approved
TrazodoneThe therapeutic efficacy of Trazodone can be increased when used in combination with Lofexidine.Approved, Investigational
TreprostinilTreprostinil may increase the hypotensive activities of Lofexidine.Approved, Investigational
TretinoinThe risk or severity of adverse effects can be increased when Lofexidine is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneThe risk or severity of adverse effects can be increased when Lofexidine is combined with Triamterene.Approved
TriazolamThe therapeutic efficacy of Triazolam can be increased when used in combination with Lofexidine.Approved, Investigational
Tricaine methanesulfonateThe therapeutic efficacy of Tricaine methanesulfonate can be increased when used in combination with Lofexidine.Vet Approved
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Lofexidine.Approved, Vet Approved
TrichloroethyleneThe therapeutic efficacy of Trichloroethylene can be increased when used in combination with Lofexidine.Approved
TrifluoperazineThe therapeutic efficacy of Trifluoperazine can be increased when used in combination with Lofexidine.Approved, Investigational
TrifluperidolThe therapeutic efficacy of Trifluperidol can be increased when used in combination with Lofexidine.Experimental
TriflupromazineThe therapeutic efficacy of Triflupromazine can be increased when used in combination with Lofexidine.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Lofexidine.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Lofexidine.Approved, Investigational
TrimipramineThe therapeutic efficacy of Trimipramine can be increased when used in combination with Lofexidine.Approved
TriprolidineThe therapeutic efficacy of Triprolidine can be increased when used in combination with Lofexidine.Approved
UdenafilUdenafil may increase the antihypertensive activities of Lofexidine.Approved, Investigational
UnoprostoneLofexidine may increase the hypotensive activities of Unoprostone.Approved, Investigational
UrapidilUrapidil may decrease the vasoconstricting activities of Lofexidine.Investigational
Valproic AcidThe therapeutic efficacy of Valproic Acid can be increased when used in combination with Lofexidine.Approved, Investigational
ValsartanValsartan may increase the hypotensive activities of Lofexidine.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Lofexidine.Approved
VemurafenibThe serum concentration of Lofexidine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the tachycardic activities of Lofexidine.Approved
VeraliprideThe therapeutic efficacy of Veralipride can be increased when used in combination with Lofexidine.Experimental
VerapamilThe risk or severity of adverse effects can be increased when Lofexidine is combined with Verapamil.Approved
VigabatrinThe therapeutic efficacy of Vigabatrin can be increased when used in combination with Lofexidine.Approved
VincamineLofexidine may increase the hypotensive activities of Vincamine.Experimental
VinpocetineLofexidine may increase the hypotensive activities of Vinpocetine.Investigational
Vinyl etherThe therapeutic efficacy of Vinyl ether can be increased when used in combination with Lofexidine.Experimental
VoriconazoleThe metabolism of Lofexidine can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe therapeutic efficacy of Vortioxetine can be increased when used in combination with Lofexidine.Approved, Investigational
XenonThe therapeutic efficacy of Xenon can be increased when used in combination with Lofexidine.Experimental
XipamideLofexidine may increase the hypotensive activities of Xipamide.Experimental
XylazineThe therapeutic efficacy of Xylazine can be increased when used in combination with Lofexidine.Vet Approved
XylometazolineLofexidine may increase the hypotensive activities of Xylometazoline.Approved, Investigational
YohimbineYohimbine may decrease the antihypertensive activities of Lofexidine.Approved, Investigational, Vet Approved
ZaleplonThe therapeutic efficacy of Zaleplon can be increased when used in combination with Lofexidine.Approved, Illicit, Investigational
ZiconotideThe therapeutic efficacy of Ziconotide can be increased when used in combination with Lofexidine.Approved
ZiprasidoneThe therapeutic efficacy of Ziprasidone can be increased when used in combination with Lofexidine.Approved
ZofenoprilLofexidine may increase the hypotensive activities of Zofenopril.Experimental
ZolazepamThe therapeutic efficacy of Zolazepam can be increased when used in combination with Lofexidine.Vet Approved
ZolpidemThe therapeutic efficacy of Zolpidem can be increased when used in combination with Lofexidine.Approved
ZonisamideThe therapeutic efficacy of Zonisamide can be increased when used in combination with Lofexidine.Approved, Investigational
ZopicloneThe therapeutic efficacy of Zopiclone can be increased when used in combination with Lofexidine.Approved
ZotepineThe therapeutic efficacy of Zotepine can be increased when used in combination with Lofexidine.Approved, Investigational, Withdrawn
ZucapsaicinThe metabolism of Lofexidine can be decreased when combined with Zucapsaicin.Approved, Investigational
ZuclopenthixolThe therapeutic efficacy of Zuclopenthixol can be increased when used in combination with Lofexidine.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference

U.S. Patent 3,966,757.

General References
  1. Walsh SL, Strain EC, Bigelow GE: Evaluation of the effects of lofexidine and clonidine on naloxone-precipitated withdrawal in opioid-dependent humans. Addiction. 2003 Apr;98(4):427-39. [PubMed:12653813]
  2. Haney M, Hart CL, Vosburg SK, Comer SD, Reed SC, Foltin RW: Effects of THC and lofexidine in a human laboratory model of marijuana withdrawal and relapse. Psychopharmacology (Berl). 2008 Mar;197(1):157-68. doi: 10.1007/s00213-007-1020-8. Epub 2007 Dec 27. [PubMed:18161012]
  3. Rehni AK, Jaggi AS, Singh N: Opioid withdrawal syndrome: emerging concepts and novel therapeutic targets. CNS Neurol Disord Drug Targets. 2013 Feb 1;12(1):112-25. [PubMed:23244430]
  4. Juurlink DN, Dhalla IA: Dependence and addiction during chronic opioid therapy. J Med Toxicol. 2012 Dec;8(4):393-9. doi: 10.1007/s13181-012-0269-4. [PubMed:23073725]
  5. Ries R. and Miller S. (2009). Principles of Addiction Medicine (4th ed.). Lippincott Williams & Wilkins. [ISBN:978-0-7817-7477-2]
  6. Strain E. and Stitzer M. (2006). The treatment of Opiod Dependence. The Johns Hopkins University Press. [ISBN:0-8018-8303-2]
  7. Zaragoza Dorwald F. (2012). Lead optimization for medicinal chemists. Wiley-VCH.
  8. FDA News [Link]
  9. FDA reports [Link]
External Links
Human Metabolome Database
HMDB0015606
PubChem Compound
30668
PubChem Substance
46508453
ChemSpider
28460
BindingDB
50019646
ChEBI
51368
ChEMBL
CHEMBL17860
Therapeutic Targets Database
DAP000064
PharmGKB
PA164744510
Wikipedia
Lofexidine
ATC Codes
N07BC04 — Lofexidine
FDA label
Download (530 KB)
MSDS
Download (72.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceNormal Healthy Volunteers1
1CompletedBasic ScienceNormal Healthy Volunteers Will be Treated With Lofexidine to Understand the Absolute Bioavailability and Mass Balance Recovery of the Product / Normal Healthy Volunteers Will be Treated With Lofexidine to Understand the Absolute Bioavailbility and Mass Balance Recovery of the Product1
1CompletedBasic ScienceRenally Impaired Subjects1
1CompletedTreatmentBuprenorphine Withdrawal Syndrome / Opioid Dependence1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentHepatic Failure1
1CompletedTreatmentHeroin Dependence1
1CompletedTreatmentMethadone Withdrawal Syndrome / Opioid Dependence2
1CompletedTreatmentOpioid-Related Disorders1
1CompletedTreatmentOpioid-Related Disorders / Substance-Related Disorders2
1TerminatedTreatmentCocaine Related Disorders1
2CompletedBasic ScienceMarijuana Dependence1
2CompletedTreatmentOpioid-Related Disorders1
2, 3CompletedTreatmentCannabis Dependence / Marijuana Dependence1
3CompletedTreatmentAcute Opioid Withdrawal Syndrome / Opioid Dependence1
3CompletedTreatmentOpiate Addiction1
3CompletedTreatmentOpiate withdrawal symptoms1
3CompletedTreatmentOpioid-Related Disorders1
4CompletedTreatmentOpiate Dependent Patients Who Are Undergoing Inpatient Detoxification in Singapore1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral.2 mg/1
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)221-223U.S. Patent 3,966,757.
boiling point (°C)421.5 ºC at 760 mm Hg'MSDS'
water solubilitySoluble'MSDS'
logP5.37FDA Advisory Committee Briefing Document.
pKa9.43FDA Advisory Committee Briefing Document.
Predicted Properties
PropertyValueSource
Water Solubility0.147 mg/mLALOGPS
logP3.31ALOGPS
logP2.66ChemAxon
logS-3.2ALOGPS
pKa (Strongest Basic)7.67ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area33.62 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity64.41 m3·mol-1ChemAxon
Polarizability25.11 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9969
Blood Brain Barrier+0.9582
Caco-2 permeable+0.539
P-glycoprotein substrateSubstrate0.7119
P-glycoprotein inhibitor INon-inhibitor0.9326
P-glycoprotein inhibitor IINon-inhibitor0.8089
Renal organic cation transporterInhibitor0.6897
CYP450 2C9 substrateNon-substrate0.744
CYP450 2D6 substrateNon-substrate0.6421
CYP450 3A4 substrateNon-substrate0.5055
CYP450 1A2 substrateInhibitor0.8023
CYP450 2C9 inhibitorNon-inhibitor0.739
CYP450 2D6 inhibitorInhibitor0.6616
CYP450 2C19 inhibitorNon-inhibitor0.6593
CYP450 3A4 inhibitorNon-inhibitor0.9304
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5075
Ames testNon AMES toxic0.7322
CarcinogenicityNon-carcinogens0.913
BiodegradationNot ready biodegradable0.996
Rat acute toxicity2.9567 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6244
hERG inhibition (predictor II)Non-inhibitor0.7293
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0bta-5090000000-966c69c881b261c7d39d

Taxonomy

Description
This compound belongs to the class of organic compounds known as dichlorobenzenes. These are compounds containing a benzene with exactly two chlorine atoms attached to it.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Halobenzenes
Direct Parent
Dichlorobenzenes
Alternative Parents
Phenoxy compounds / Phenol ethers / Alkyl aryl ethers / Imidolactams / Aryl chlorides / Imidazolines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Carboxamidines / Azacyclic compounds
show 3 more
Substituents
Phenoxy compound / 1,3-dichlorobenzene / Phenol ether / Alkyl aryl ether / Aryl chloride / Aryl halide / Imidolactam / 2-imidazoline / Amidine / Carboxylic acid amidine
show 15 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
aromatic ether, imidazoles, carboxamidine, dichlorobenzene (CHEBI:51368)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Jin Y, Verstappen A, Elko E, Cammarata P, Yorio T: Effects of lofexidine, an alpha 2-adrenoreceptor agonist, on ocular blood flow and ion transport of rabbit iris-ciliary body. J Ocul Pharmacol. 1992 Spring;8(1):23-33. [PubMed:1357064]
  2. Strang J, Bearn J, Gossop M: Lofexidine for opiate detoxification: review of recent randomised and open controlled trials. Am J Addict. 1999 Fall;8(4):337-48. [PubMed:10598217]
  3. Erb S, Hitchcott PK, Rajabi H, Mueller D, Shaham Y, Stewart J: Alpha-2 adrenergic receptor agonists block stress-induced reinstatement of cocaine seeking. Neuropsychopharmacology. 2000 Aug;23(2):138-50. [PubMed:10882840]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Agonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. FDA reports [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. FDA reports [Link]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Efflux transmembrane transporter activity
Specific Function
Drug efflux transporter present in a number of stem cells that acts as a regulator of cellular differentiation. Able to mediate efflux from cells of the rhodamine dye and of the therapeutic drug do...
Gene Name
ABCB5
Uniprot ID
Q2M3G0
Uniprot Name
ATP-binding cassette sub-family B member 5
Molecular Weight
138639.48 Da
References
  1. FDA reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. FDA reports [Link]

Drug created on October 21, 2007 16:23 / Updated on July 02, 2018 20:37