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Identification
NameGuanfacine
Accession NumberDB01018  (APRD00075)
TypeSmall Molecule
GroupsApproved, Investigational
Description

A centrally acting antihypertensive agent. The drug lowers both systolic and diastolic blood pressure by activating the central nervous system alpha-2 adrenoreceptors, which results in reduced sympathetic outflow leading to reduced vascular tone. Its adverse reactions include dry mouth, sedation, and constipation. [PubChem]

Structure
Thumb
Synonyms
Estulic
Guanfacina
Guanfacinum
External Identifiers
  • SPD 503
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Intunivtablet, extended release1 mg/1oralShire US Manufacturing Inc.2009-09-02Not applicableUs
Intunivtablet, extended release2 mg/1oralTYA Pharmaceuticals2009-09-02Not applicableUs
Intunivtablet, extended release1 mg/1oralTYA Pharmaceuticals2009-09-02Not applicableUs
IntunivkitShire US Manufacturing Inc.2009-09-02Not applicableUs
Intunivtablet, extended release4 mg/1oralShire US Manufacturing Inc.2009-09-02Not applicableUs
Intunivtablet, extended release3 mg/1oralShire US Manufacturing Inc.2009-09-02Not applicableUs
Intunivtablet, extended release2 mg/1oralShire US Manufacturing Inc.2009-09-02Not applicableUs
Intuniv XRtablet (extended-release)3 mgoralShire Pharma Canada Ulc2013-08-06Not applicableCanada
Intuniv XRtablet (extended-release)1 mgoralShire Pharma Canada Ulc2013-08-06Not applicableCanada
Intuniv XRtablet (extended-release)4 mgoralShire Pharma Canada Ulc2013-08-06Not applicableCanada
Intuniv XRtablet (extended-release)2 mgoralShire Pharma Canada Ulc2013-08-06Not applicableCanada
Tenextablet2 mg/1oralPromius Pharma, LLC1986-10-27Not applicableUs
Tenextablet1 mg/1oralPromius Pharma, LLC1986-10-27Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Guanfacinetablet2 mg/1oralPhysicians Total Care, Inc.2003-07-31Not applicableUs
Guanfacinetablet, extended release1 mg/1oralTeva Pharmaceuticals USA Inc2015-06-02Not applicableUs
Guanfacinetablet2 mg/1oralEpic Pharma, LLC2013-12-02Not applicableUs
Guanfacinetablet2 mg/1oralActavis Pharma, Inc.1995-10-17Not applicableUs
Guanfacinetablet, extended release4 mg/1oralActavis Pharma, Inc.2014-12-01Not applicableUs
Guanfacinetablet1 mg/1oralEpic Pharma, LLC2013-12-02Not applicableUs
Guanfacinetablet1 mg/1oralActavis Pharma, Inc.1995-10-17Not applicableUs
Guanfacinetablet, extended release3 mg/1oralActavis Pharma, Inc.2014-12-01Not applicableUs
Guanfacinetablet, extended release4 mg/1oralAv Kare, Inc.2015-07-07Not applicableUs
Guanfacinetablet2 mg/1oralMylan Pharmaceuticals Inc.1997-01-28Not applicableUs
Guanfacinetablet, extended release2 mg/1oralActavis Pharma, Inc.2014-12-01Not applicableUs
Guanfacinetablet, extended release3 mg/1oralAv Kare, Inc.2015-07-07Not applicableUs
Guanfacinetablet2 mg/1oralGolden State Medical Supply, Inc.2014-04-22Not applicableUs
Guanfacinetablet1 mg/1oralMylan Pharmaceuticals Inc.1997-01-28Not applicableUs
Guanfacinetablet, extended release1 mg/1oralActavis Pharma, Inc.2014-12-01Not applicableUs
Guanfacinetablet, extended release2 mg/1oralAv Kare, Inc.2015-07-07Not applicableUs
Guanfacinetablet1 mg/1oralGolden State Medical Supply, Inc.2014-04-22Not applicableUs
Guanfacinetablet, extended release4 mg/1oralTeva Pharmaceuticals USA Inc2015-06-02Not applicableUs
Guanfacinetablet, extended release1 mg/1oralAv Kare, Inc.2015-07-07Not applicableUs
Guanfacinetablet1 mg/1oralREMEDYREPACK INC.2016-01-13Not applicableUs
Guanfacinetablet1 mg/1oralCardinal Health1997-01-27Not applicableUs
Guanfacinetablet, extended release3 mg/1oralTeva Pharmaceuticals USA Inc2015-06-02Not applicableUs
Guanfacinetablet1 mg/1oralCarilion Materials Management1995-10-17Not applicableUs
Guanfacinetablet1 mg/1oralCardinal Health1995-10-17Not applicableUs
Guanfacinetablet, extended release2 mg/1oralTeva Pharmaceuticals USA Inc2015-06-02Not applicableUs
Guanfacinetablet1 mg/1oralPhysicians Total Care, Inc.1995-10-17Not applicableUs
Guanfacine Extended-releasetablet, extended release2 mg/1oralSandoz Inc2015-06-03Not applicableUs
Guanfacine Extended-releasetablet, extended release1 mg/1oralSandoz Inc2015-06-03Not applicableUs
Guanfacine Extended-releasetablet, extended release4 mg/1oralPar Pharmaceutical Inc.2015-06-02Not applicableUs
Guanfacine Extended-releasetablet, extended release3 mg/1oralPar Pharmaceutical Inc.2015-06-02Not applicableUs
Guanfacine Extended-releasetablet, extended release2 mg/1oralPar Pharmaceutical Inc.2015-06-02Not applicableUs
Guanfacine Extended-releasetablet, extended release1 mg/1oralPar Pharmaceutical Inc.2015-06-02Not applicableUs
Guanfacine Extended-releasetablet, extended release4 mg/1oralSandoz Inc2015-06-03Not applicableUs
Guanfacine Extended-releasetablet, extended release3 mg/1oralSandoz Inc2015-06-03Not applicableUs
Guanfacine Hydrochloridetablet2 mg/1oralAmneal Pharmaceuticals of New York, LLC1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet, film coated, extended release1 mg/1oralMylan Pharmaceuticals Inc.2015-06-02Not applicableUs
Guanfacine Hydrochloridetablet1 mg/1oralAmneal Pharmaceuticals of New York, LLC1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet1 mg/1oralTYA Pharmaceuticals1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet2 mg/1oralMajor Pharmaceuticals1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet, film coated, extended release4 mg/1oralMylan Pharmaceuticals Inc.2015-06-02Not applicableUs
Guanfacine Hydrochloridetablet1 mg/1oralMajor Pharmaceuticals1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet, film coated, extended release3 mg/1oralMylan Pharmaceuticals Inc.2015-06-02Not applicableUs
Guanfacine Hydrochloridetablet2 mg/1oralAv Kare, Inc.1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet, film coated, extended release2 mg/1oralMylan Pharmaceuticals Inc.2015-06-02Not applicableUs
Guanfacine Hydrochloridetablet1 mg/1oralAv Kare, Inc.1998-11-25Not applicableUs
Guanfacine Hydrochloridetablet1 mg/1oralAmerican Health Packaging2014-05-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EstulicEgis
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Guanfacine Hydrochloride
Thumb
  • InChI Key: DGFYECXYGUIODH-UHFFFAOYSA-N
  • Monoisotopic Mass: 280.988945078
  • Average Mass: 282.554
DBSALT000509
Categories
UNII30OMY4G3MK
CAS number29110-47-2
WeightAverage: 246.093
Monoisotopic: 245.012267339
Chemical FormulaC9H9Cl2N3O
InChI KeyInChIKey=INJOMKTZOLKMBF-UHFFFAOYSA-N
InChI
InChI=1S/C9H9Cl2N3O/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13/h1-3H,4H2,(H4,12,13,14,15)
IUPAC Name
N-carbamimidoyl-2-(2,6-dichlorophenyl)acetamide
SMILES
NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylacetamides. These are amide derivatives of phenylacetic acids.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylacetamides
Direct ParentPhenylacetamides
Alternative Parents
Substituents
  • Phenylacetamide
  • 1,3-dichlorobenzene
  • Halobenzene
  • Chlorobenzene
  • Aryl halide
  • Aryl chloride
  • Guanidine
  • Carboxamide group
  • Carboximidamide
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Carbonyl group
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor use alone or in combination with other classes of antihypertensive agents in the management of hypertension. Has also been used for the treatment of attention deficit hyperactivity disorder (ADHD) in pediatric patients.
PharmacodynamicsGuanfacine is a phenylacetyl-guanidine derivative hypotensive and a centrally-acting, alpha(2)-adrenergic receptor agonist used alone or in combination with other drugs for the treatment of hypertension.
Mechanism of actionGuanfacine selectively stimulates central alpha(2)-adrenergic receptors, resulting in inhibition of sympathetic vasomotor centers, which contributes predominantly to the hypotensive effects of the drug. Central effects of guanfacine lead to reduced peripheral sympathetic nerve impulses from the vasomotor center to the heart and blood vessels. This results in a decrease in peripheral vascular resistance and a reduction in heart rate. The stimulation of peripheral alpha(2)-adrenergic receptors may also contribute to hypotensive effects.
Related Articles
AbsorptionRapid and complete, with an oral bioavailability of approximately 80%.
Volume of distribution
  • 6.3 L/kg
Protein bindingApproximately 70% bound to plasma proteins, independent of drug concentration.
Metabolism

Hepatic

SubstrateEnzymesProduct
Guanfacine
3-hydroxyguanfacine glucuronideDetails
Route of eliminationIn individuals with normal renal function, guanfacine and its metabolites are excreted primarily in the urine.
Half life17 hours (range 10-30 hours)
ClearanceNot Available
ToxicitySymptoms of overdose include drowsiness, lethargy, bradycardia and hypotension. LD50=165mg/kg (orally in mice)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9313
Blood Brain Barrier+0.9567
Caco-2 permeable-0.5101
P-glycoprotein substrateNon-substrate0.6778
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.9833
Renal organic cation transporterNon-inhibitor0.6443
CYP450 2C9 substrateNon-substrate0.7572
CYP450 2D6 substrateNon-substrate0.7948
CYP450 3A4 substrateNon-substrate0.6475
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.8893
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.7376
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6619
Ames testNon AMES toxic0.7223
CarcinogenicityNon-carcinogens0.8107
BiodegradationNot ready biodegradable0.9843
Rat acute toxicity2.7408 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9677
hERG inhibition (predictor II)Non-inhibitor0.9285
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Shire development inc
  • Amneal pharmaceutical
  • Mikah pharma llc
  • Mylan pharmaceuticals inc
  • Watson laboratories inc
  • Promius pharma llc
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg/1
Tabletoral2 mg/1
Tablet, extended releaseoral1 mg/1
Tablet, extended releaseoral2 mg/1
Tablet, extended releaseoral3 mg/1
Tablet, extended releaseoral4 mg/1
Tablet, film coated, extended releaseoral1 mg/1
Tablet, film coated, extended releaseoral2 mg/1
Tablet, film coated, extended releaseoral3 mg/1
Tablet, film coated, extended releaseoral4 mg/1
Kit
Tablet (extended-release)oral1 mg
Tablet (extended-release)oral2 mg
Tablet (extended-release)oral3 mg
Tablet (extended-release)oral4 mg
Prices
Unit descriptionCostUnit
Intuniv 1 mg 24 Hour tablet5.72USD tablet
Intuniv 2 mg 24 Hour tablet5.72USD tablet
Intuniv 3 mg 24 Hour tablet5.72USD tablet
Intuniv 4 mg 24 Hour tablet5.72USD tablet
Intuniv er 1 mg tablet5.5USD tablet
Intuniv er 2 mg tablet5.5USD tablet
Intuniv er 3 mg tablet5.5USD tablet
Intuniv er 4 mg tablet5.5USD tablet
Tenex 2 mg tablet4.3USD tablet
Tenex 1 mg tablet2.9USD tablet
Guanfacine HCl 2 mg tablet1.22USD tablet
Guanfacine 2 mg tablet1.18USD tablet
Guanfacine HCl 1 mg tablet0.91USD tablet
Guanfacine 1 mg tablet0.87USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5854290 Yes1996-03-212016-03-21Us
US6287599 Yes2001-06-202021-06-20Us
US6811794 Yes2003-01-042023-01-04Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point213-216U.S. Patent 3,632,645.
water solubility1892 mg/LNot Available
logP1.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.139 mg/mLALOGPS
logP2.28ALOGPS
logP1.74ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)12.94ChemAxon
pKa (Strongest Basic)6.65ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area78.97 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity69.63 m3·mol-1ChemAxon
Polarizability21.75 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

U.S. Patent 3,632,645.

General ReferencesNot Available
External Links
ATC CodesC02AC02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Guanfacine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Guanfacine.
AmifostineGuanfacine may increase the hypotensive activities of Amifostine.
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Guanfacine.
AprepitantThe serum concentration of Guanfacine can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Guanfacine can be increased when it is combined with Atazanavir.
AzelastineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Guanfacine.
BexaroteneThe serum concentration of Guanfacine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Guanfacine can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Guanfacine can be decreased when it is combined with Bosentan.
BretyliumBretylium may increase the bradycardic activities of Guanfacine.
BrimonidineBrimonidine may increase the antihypertensive activities of Guanfacine.
BuprenorphineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalButabarbital may increase the hypotensive activities of Guanfacine.
ButethalButethal may increase the hypotensive activities of Guanfacine.
CarbamazepineThe serum concentration of Guanfacine can be decreased when it is combined with Carbamazepine.
CeritinibGuanfacine may increase the bradycardic activities of Ceritinib.
ClarithromycinThe serum concentration of Guanfacine can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Guanfacine can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Guanfacine can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Guanfacine can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Guanfacine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Guanfacine can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Guanfacine can be decreased when it is combined with Deferasirox.
DiazoxideDiazoxide may increase the hypotensive activities of Guanfacine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
DuloxetineGuanfacine may increase the orthostatic hypotensive activities of Duloxetine.
EnzalutamideThe serum concentration of Guanfacine can be decreased when it is combined with Enzalutamide.
EsmololEsmolol may increase the bradycardic activities of Guanfacine.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
FluconazoleThe metabolism of Guanfacine can be decreased when combined with Fluconazole.
FosaprepitantThe serum concentration of Guanfacine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Guanfacine can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Guanfacine can be increased when it is combined with Fusidic Acid.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Guanfacine.
HexobarbitalHexobarbital may increase the hypotensive activities of Guanfacine.
HydrocodoneGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
IdelalisibThe serum concentration of Guanfacine can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Guanfacine can be increased when it is combined with Indinavir.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Guanfacine.
ItraconazoleThe serum concentration of Guanfacine can be increased when it is combined with Itraconazole.
IvabradineGuanfacine may increase the bradycardic activities of Ivabradine.
IvacaftorThe serum concentration of Guanfacine can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Guanfacine can be increased when it is combined with Ketoconazole.
LacosamideGuanfacine may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LevodopaGuanfacine may increase the orthostatic hypotensive activities of Levodopa.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Guanfacine.
LuliconazoleThe serum concentration of Guanfacine can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
MethohexitalMethohexital may increase the hypotensive activities of Guanfacine.
MethotrimeprazineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Guanfacine.
MetyrosineGuanfacine may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Guanfacine can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
MirtazapineMirtazapine may decrease the antihypertensive activities of Guanfacine.
MitotaneThe serum concentration of Guanfacine can be decreased when it is combined with Mitotane.
MolsidomineMolsidomine may increase the hypotensive activities of Guanfacine.
MoxonidineMoxonidine may increase the hypotensive activities of Guanfacine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
NadololGuanfacine may increase the atrioventricular blocking (AV block) activities of Nadolol.
NefazodoneThe serum concentration of Guanfacine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Guanfacine can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Guanfacine can be increased when it is combined with Netupitant.
NicorandilNicorandil may increase the hypotensive activities of Guanfacine.
ObinutuzumabGuanfacine may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Guanfacine.
OrphenadrineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Guanfacine can be increased when it is combined with Palbociclib.
ParaldehydeGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Paroxetine.
PentobarbitalPentobarbital may increase the hypotensive activities of Guanfacine.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Guanfacine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Guanfacine.
PhenobarbitalThe serum concentration of Guanfacine can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Guanfacine can be decreased when it is combined with Phenytoin.
PosaconazoleThe serum concentration of Guanfacine can be increased when it is combined with Posaconazole.
PramipexoleGuanfacine may increase the sedative activities of Pramipexole.
PrimidonePrimidone may increase the hypotensive activities of Guanfacine.
QuinineQuinine may increase the hypotensive activities of Guanfacine.
RifabutinThe serum concentration of Guanfacine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Guanfacine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Guanfacine can be decreased when it is combined with Rifapentine.
RisperidoneGuanfacine may increase the hypotensive activities of Risperidone.
RitonavirThe serum concentration of Guanfacine can be increased when it is combined with Ritonavir.
RituximabGuanfacine may increase the hypotensive activities of Rituximab.
RopiniroleGuanfacine may increase the sedative activities of Ropinirole.
RotigotineGuanfacine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Guanfacine.
RuxolitinibRuxolitinib may increase the bradycardic activities of Guanfacine.
SaquinavirThe serum concentration of Guanfacine can be increased when it is combined with Saquinavir.
SecobarbitalSecobarbital may increase the hypotensive activities of Guanfacine.
SiltuximabThe serum concentration of Guanfacine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Guanfacine can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
St. John's WortThe serum concentration of Guanfacine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Guanfacine can be increased when it is combined with Stiripentol.
SuvorexantGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TadalafilTadalafil may increase the antihypertensive activities of Guanfacine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Guanfacine.
TelaprevirThe serum concentration of Guanfacine can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Guanfacine can be increased when it is combined with Telithromycin.
ThalidomideGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TocilizumabThe serum concentration of Guanfacine can be decreased when it is combined with Tocilizumab.
TofacitinibTofacitinib may increase the bradycardic activities of Guanfacine.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Guanfacine.
TreprostinilTreprostinil may increase the hypotensive activities of Guanfacine.
Valproic AcidThe serum concentration of Valproic Acid can be increased when it is combined with Guanfacine.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Guanfacine.
VardenafilVardenafil may increase the antihypertensive activities of Guanfacine.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Guanfacine.
VoriconazoleThe serum concentration of Guanfacine can be increased when it is combined with Voriconazole.
YohimbineYohimbine may decrease the antihypertensive activities of Guanfacine.
ZolpidemGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Avery RA, Franowicz JS, Studholme C, van Dyck CH, Arnsten AF: The alpha-2A-adrenoceptor agonist, guanfacine, increases regional cerebral blood flow in dorsolateral prefrontal cortex of monkeys performing a spatial working memory task. Neuropsychopharmacology. 2000 Sep;23(3):240-9. [PubMed:10942848 ]
  2. Sagvolden T: The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD). Behav Brain Funct. 2006 Dec 15;2:41. [PubMed:17173664 ]
  3. Yuan R, Wu Z, Kostenyuk IA, Burns JK: G-protein-coupled alpha2A-adrenoreceptor agonists differentially alter citrus leaf and fruit abscission by affecting expression of ACC synthase and ACC oxidase. J Exp Bot. 2005 Jul;56(417):1867-75. Epub 2005 May 31. [PubMed:15928018 ]
  4. Birnbaum SG, Podell DM, Arnsten AF: Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats. Pharmacol Biochem Behav. 2000 Nov;67(3):397-403. [PubMed:11164065 ]
  5. Millan MJ: Evidence that an alpha 2A-adrenoceptor subtype mediates antinociception in mice. Eur J Pharmacol. 1992 May 14;215(2-3):355-6. [PubMed:1356794 ]
  6. Stahl SM: Mechanism of action of alpha 2A-adrenergic agonists in attention-deficit/hyperactivity disorder with or without oppositional symptoms. J Clin Psychiatry. 2010 Mar;71(3):223-4. doi: 10.4088/JCP.09bs05899pur. [PubMed:20331927 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Epinephrine 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 clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Uhlen S, Wikberg JE: Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound. Eur J Pharmacol. 1991 Sep 17;202(2):235-43. [PubMed:1666366 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Clement B, Demesmaeker M: Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine. Arch Pharm (Weinheim). 1997 Oct;330(9-10):303-6. [PubMed:9396389 ]
  2. Guillouzo A, Le Bigot JF, Guguen-Guillouzo C, Kiechel JR: Presence of phase I and phase II drug metabolizing enzymes in cultured human foetal hepatocytes. Biochem Pharmacol. 1982 Jul 15;31(14):2427-30. [PubMed:6751332 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Clement B, Demesmaeker M: Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine. Arch Pharm (Weinheim). 1997 Oct;330(9-10):303-6. [PubMed:9396389 ]
  2. Guillouzo A, Le Bigot JF, Guguen-Guillouzo C, Kiechel JR: Presence of phase I and phase II drug metabolizing enzymes in cultured human foetal hepatocytes. Biochem Pharmacol. 1982 Jul 15;31(14):2427-30. [PubMed:6751332 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Clement B, Demesmaeker M: Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine. Arch Pharm (Weinheim). 1997 Oct;330(9-10):303-6. [PubMed:9396389 ]
  2. Guillouzo A, Le Bigot JF, Guguen-Guillouzo C, Kiechel JR: Presence of phase I and phase II drug metabolizing enzymes in cultured human foetal hepatocytes. Biochem Pharmacol. 1982 Jul 15;31(14):2427-30. [PubMed:6751332 ]
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Drug created on June 13, 2005 07:24 / Updated on July 01, 2016 03:05