Identification

Name
Moxonidine
Accession Number
DB09242
Type
Small Molecule
Groups
Approved
Description

Moxonidine is a new-generation centrally acting antihypertensive drug licensed for the treatment of mild to moderate essential hypertension. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction.

Structure
Thumb
Synonyms
  • (2R,4R)-1-[(2S)-5-[(aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8- quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid
External IDs
BDF-5896 / BDF5896 / BE5895 / LY-326869 / LY326869
International/Other Brands
Cynt / Physiotens (Solvay Pharmaceuticals)
Categories
UNII
CC6X0L40GW
CAS number
75438-57-2
Weight
Average: 241.677
Monoisotopic: 241.073037738
Chemical Formula
C9H12ClN5O
InChI Key
WPNJAUFVNXKLIM-UHFFFAOYSA-N
InChI
InChI=1S/C9H12ClN5O/c1-5-13-7(10)6(8(14-5)16-2)15-9-11-3-4-12-9/h3-4H2,1-2H3,(H2,11,12,15)
IUPAC Name
4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine
SMILES
COC1=NC(C)=NC(Cl)=C1NC1=NCCN1

Pharmacology

Indication

For the treatment of mild to moderate essential hypertension. Effective as most first-line antihypertensives when used as monotherapy. [2]

Structured Indications
Not Available
Pharmacodynamics

Centrally acting antihypertensive agent with site of action being the Central Nervous System (CNS), specifically the rostral ventrolateral medulla (RSV). [FDA Label]

Mechanism of action

Stimulation of central alpha 2-adrenergic receptors is associated with sympathoadrenal suppression and subsequent reduction of blood pressure. As this class was further explored it was discovered that sympathoadrenal activity can also be suppressed by a second pathway with a newly discovered drug target specific to imidazolines. [5] Specifically, Moxonidine binds the imidazoline receptor subtype 1 (I1) and to a lesser extent α2-adrenoreceptors in the RSV causing a reduction of sympathetic activity, reducing systemic vascular resistance and thus arterial blood pressure. [FDA Label]

TargetActionsOrganism
AAlpha-2A adrenergic receptor
agonist
Human
ANischarin
agonist
Human
Absorption

90% of oral dose is absorbed with negligible interference from food or first pass metabolism and thus a high bioavailability of 88%. [FDA Label]

Volume of distribution

1.8±0.4L/kg. [FDA Label]

Protein binding

About 10% of moxonidine is bound to plasma proteins. [FDA Label]

Metabolism

Biotransformation is unimportant [3] with 10-20% metabolized, mainly to 4,5-dehydromoxonidine and a guanidine derivative. [FDA Label]

Route of elimination

Almost entire eliminination is by the kidneys with majority (50 -75%) of overall monoxidine eliminated unchanged. [FDA Label]

Half life

Plasma elimination half life is 2.2 - 2.3 hours while renal elimination half life is 2.6-2.8 hours. [FDA Label]

Clearance

Administered twice daily due to short half life with dosage adjustment considered in elderly and renal impairment due to reduced clearance, GFR between 30-60 mL/min decreases clearence by 52 %. [FDA Label]

Toxicity
  • Contraindicated due to known hypersensitivity to an ingredient(Physiotens tablets contain lactose), heart failure, severe renal impairment, < 16 years old, >75 years old, bradycardia, certain arrhythmias. [FDA Label]
  • Used with caution in pateints with severe coronary artery disease (CAD), unstable angina, angioneurotic edema, moderate renal impairment. [FDA Label]
  • Pregnancy Category B3:Avoid use during pregnancy (inadequate data in pregnant woman) and lactation (maternal blood stream transfer to breast milk shown) unless benefit clearly justifies risk. [FDA Label]
  • Carcinogenicity and genotoxicity does not appear significant. [FDA Label]
  • Concurrent administration of other hypotensives or sedative and hypnotics can enhance the hypotensive effect and intensify sedation respectively. [FDA Label]
  • Avoid concurrent Tricyclic Antidepressant (TCA) use to avoid reduction of monoxidine efficacy. {FDA label]
  • Generally well tolerated with dry mouth and headache the most common adverse effects [FDA Label]
  • Symptoms of overdose correlate with pharmacodynamic properties:hypotension, sedation,orthostatic dysregulation,bradycardia,dry mouth with no specific treatment known. [FDA Label]
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Moxonidine.Experimental
AcebutololMoxonidine may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved
AldesleukinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Aldesleukin.Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Moxonidine.Approved, Investigational
AliskirenMoxonidine may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlprenololMoxonidine may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmbrisentanMoxonidine may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineMoxonidine may increase the hypotensive activities of Amifostine.Approved, Investigational
AmilorideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Amiloride.Approved
AmineptineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Amineptine.Illicit, Withdrawn
AmiodaroneThe risk or severity of adverse effects can be increased when Amiodarone is combined with Moxonidine.Approved, Investigational
AmitriptylineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Amitriptyline.Approved
AmlodipineMoxonidine may increase the hypotensive activities of Amlodipine.Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Moxonidine.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Moxonidine.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Moxonidine is combined with Amyl Nitrite.Approved
ApomorphineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Moxonidine.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Apraclonidine.Approved
AripiprazoleAripiprazole may increase the hypotensive activities of Moxonidine.Approved, Investigational
ArotinololMoxonidine may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved
Arsenic trioxideThe risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Moxonidine.Approved, Investigational
AtenololMoxonidine may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Moxonidine is combined with Azilsartan medoxomil.Approved
BarbexacloneBarbexaclone may increase the hypotensive activities of Moxonidine.Experimental
BarbitalBarbital may increase the hypotensive activities of Moxonidine.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Barnidipine is combined with Moxonidine.Approved
BefunololMoxonidine may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
BenazeprilMoxonidine may increase the hypotensive activities of Benazepril.Approved, Investigational
BendroflumethiazideMoxonidine may increase the hypotensive activities of Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Moxonidine.Withdrawn
BepridilMoxonidine may increase the hypotensive activities of Bepridil.Approved, Withdrawn
BetaxololMoxonidine may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved
BethanidineBethanidine may increase the hypotensive activities of Moxonidine.Approved
BevantololMoxonidine may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BietaserpineMoxonidine may increase the hypotensive activities of Bietaserpine.Experimental
BimatoprostMoxonidine may increase the hypotensive activities of Bimatoprost.Approved, Investigational
BisoprololMoxonidine may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BopindololMoxonidine 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 Moxonidine.Approved, Investigational
BosentanBosentan may increase the hypotensive activities of Moxonidine.Approved, Investigational
BQ-123Moxonidine may increase the hypotensive activities of BQ-123.Investigational
BretyliumMoxonidine may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Moxonidine.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Moxonidine.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Moxonidine.Approved, Investigational
BucindololMoxonidine may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolMoxonidine may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BumetanideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Bumetanide.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Moxonidine.Approved, Investigational
BupranololMoxonidine may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
CadralazineMoxonidine may increase the hypotensive activities of Cadralazine.Experimental
CafedrineMoxonidine may increase the hypotensive activities of Cafedrine.Investigational
CanagliflozinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Canagliflozin.Approved
CandesartanMoxonidine may increase the hypotensive activities of Candesartan.Approved
CandoxatrilMoxonidine may increase the hypotensive activities of Candoxatril.Experimental
CaptoprilMoxonidine may increase the hypotensive activities of Captopril.Approved
CarbetocinThe risk or severity of adverse effects can be increased when Carbetocin is combined with Moxonidine.Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Moxonidine.Withdrawn
CarteololMoxonidine may increase the atrioventricular blocking (AV block) activities of Carteolol.Approved
CarvedilolMoxonidine may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CeliprololMoxonidine may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
ChlorothiazideMoxonidine may increase the hypotensive activities of Chlorothiazide.Approved, Vet Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Moxonidine.Approved, Vet Approved
ChlorthalidoneMoxonidine may increase the hypotensive activities of Chlorthalidone.Approved
CicletanineMoxonidine may increase the hypotensive activities of Cicletanine.Investigational
CilazaprilMoxonidine may increase the hypotensive activities of Cilazapril.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Cilnidipine is combined with Moxonidine.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Clevidipine.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Clofarabine is combined with Moxonidine.Approved, Investigational
ClomipramineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Clomipramine.Approved, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Moxonidine.Approved
CloranololMoxonidine may increase the atrioventricular blocking (AV block) activities of Cloranolol.Experimental
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Moxonidine.Approved
ConivaptanThe risk or severity of adverse effects can be increased when Conivaptan is combined with Moxonidine.Approved, Investigational
CryptenamineMoxonidine may increase the hypotensive activities of Cryptenamine.Approved
CyclobenzaprineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Cyclobenzaprine.Approved
CyclopenthiazideMoxonidine may increase the hypotensive activities of Cyclopenthiazide.Experimental
CyclothiazideMoxonidine may increase the hypotensive activities of Cyclothiazide.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Dapagliflozin.Approved
DebrisoquinDebrisoquin may increase the hypotensive activities of Moxonidine.Approved
DelaprilMoxonidine may increase the hypotensive activities of Delapril.Experimental
DeserpidineMoxonidine may increase the hypotensive activities of Deserpidine.Approved
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Moxonidine.Approved
DesipramineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Desipramine.Approved
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Moxonidine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Dexmedetomidine.Approved, Vet Approved
DiazoxideDiazoxide may increase the hypotensive activities of Moxonidine.Approved
DibenzepinThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Dibenzepin.Experimental
DiclofenamideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Diclofenamide.Approved
diethylnorspermineMoxonidine may increase the hypotensive activities of diethylnorspermine.Investigational
DihydralazineMoxonidine may increase the hypotensive activities of Dihydralazine.Investigational
DiltiazemMoxonidine may increase the hypotensive activities of Diltiazem.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Moxonidine is combined with Dinutuximab.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Moxonidine is combined with Dipyridamole.Approved
DorzolamideMoxonidine may increase the hypotensive activities of Dorzolamide.Approved
DosulepinThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Dosulepin.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Moxonidine.Approved
DoxepinThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Doxepin.Approved
DuloxetineMoxonidine may increase the orthostatic hypotensive activities of Duloxetine.Approved
EfonidipineMoxonidine may increase the hypotensive activities of Efonidipine.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Empagliflozin.Approved
EnalaprilMoxonidine may increase the hypotensive activities of Enalapril.Approved, Vet Approved
EnalaprilatMoxonidine may increase the hypotensive activities of Enalaprilat.Approved
EndralazineMoxonidine may increase the hypotensive activities of Endralazine.Experimental
EpanololMoxonidine may increase the atrioventricular blocking (AV block) activities of Epanolol.Experimental
EplerenoneThe risk or severity of adverse effects can be increased when Moxonidine is combined with Eplerenone.Approved
EpoprostenolMoxonidine may increase the hypotensive activities of Epoprostenol.Approved
EprosartanMoxonidine may increase the hypotensive activities of Eprosartan.Approved
EsmirtazapineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Esmirtazapine.Investigational
EsmololMoxonidine may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Moxonidine is combined with Etacrynic acid.Approved
FelodipineMoxonidine may increase the hypotensive activities of Felodipine.Approved, Investigational
FenoldopamMoxonidine may increase the hypotensive activities of Fenoldopam.Approved
Ferulic acidMoxonidine may increase the hypotensive activities of Ferulic acid.Experimental
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Moxonidine.Approved
FosinoprilMoxonidine may increase the hypotensive activities of Fosinopril.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Moxonidine.Approved, Vet Approved
FurosemideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Furosemide.Approved, Vet Approved
GuanabenzMoxonidine may increase the hypotensive activities of Guanabenz.Approved
GuanadrelMoxonidine may increase the hypotensive activities of Guanadrel.Approved
GuanazodineMoxonidine may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineGuanethidine may increase the hypotensive activities of Moxonidine.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Moxonidine.Approved, Investigational
GuanoclorMoxonidine may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzMoxonidine may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanMoxonidine may increase the hypotensive activities of Guanoxan.Experimental
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Moxonidine.Approved, Vet Approved
HarmalineHarmaline may increase the hypotensive activities of Moxonidine.Experimental
HexamethoniumMoxonidine may increase the hypotensive activities of Hexamethonium.Experimental
HexobarbitalHexobarbital may increase the hypotensive activities of Moxonidine.Approved
HydracarbazineHydracarbazine may increase the hypotensive activities of Moxonidine.Experimental
HydralazineHydralazine may increase the hypotensive activities of Moxonidine.Approved
HydrochlorothiazideMoxonidine may increase the hypotensive activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideMoxonidine may increase the hypotensive activities of Hydroflumethiazide.Approved
IloprostIloprost may increase the hypotensive activities of Moxonidine.Approved, Investigational
ImidaprilThe risk or severity of adverse effects can be increased when Imidapril is combined with Moxonidine.Investigational
ImipramineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Imipramine.Approved
IndapamideMoxonidine may increase the hypotensive activities of Indapamide.Approved
IndenololMoxonidine may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndoraminIndoramin may increase the hypotensive activities of Moxonidine.Withdrawn
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Moxonidine.Approved
IprindoleThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Iprindole.Experimental
IproclozideIproclozide may increase the hypotensive activities of Moxonidine.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Moxonidine.Withdrawn
IrbesartanMoxonidine may increase the hypotensive activities of Irbesartan.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Moxonidine.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Moxonidine.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Moxonidine is combined with Isosorbide Dinitrate.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Moxonidine is combined with Isosorbide Mononitrate.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Isoxsuprine.Approved, Withdrawn
IsradipineMoxonidine may increase the hypotensive activities of Isradipine.Approved
KetanserinMoxonidine may increase the hypotensive activities of Ketanserin.Investigational
LabetalolMoxonidine may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LacidipineMoxonidine may increase the hypotensive activities of Lacidipine.Approved
LandiololMoxonidine may increase the atrioventricular blocking (AV block) activities of Landiolol.Investigational
LatanoprostMoxonidine may increase the hypotensive activities of Latanoprost.Approved, Investigational
LercanidipineMoxonidine may increase the hypotensive activities of Lercanidipine.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Moxonidine is combined with Levobunolol.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Moxonidine.Approved
LevodopaMoxonidine may increase the orthostatic hypotensive activities of Levodopa.Approved
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Moxonidine.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Levosimendan is combined with Moxonidine.Approved, Investigational
LinsidomineMoxonidine may increase the hypotensive activities of Linsidomine.Experimental
LisinoprilMoxonidine may increase the hypotensive activities of Lisinopril.Approved, Investigational
LofepramineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Lofepramine.Experimental
LofexidineMoxonidine may increase the hypotensive activities of Lofexidine.Approved, Investigational
LosartanMoxonidine may increase the hypotensive activities of Losartan.Approved
MacitentanMoxonidine may increase the hypotensive activities of Macitentan.Approved
ManidipineMoxonidine may increase the hypotensive activities of Manidipine.Approved
MannitolThe risk or severity of adverse effects can be increased when Moxonidine is combined with Mannitol.Approved, Investigational
MebanazineMebanazine may increase the hypotensive activities of Moxonidine.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Moxonidine.Approved
MepindololMoxonidine may increase the atrioventricular blocking (AV block) activities of Mepindolol.Experimental
MethazolamideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Methazolamide.Approved
MethohexitalMethohexital may increase the hypotensive activities of Moxonidine.Approved
MethoserpidineMoxonidine may increase the hypotensive activities of Methoserpidine.Experimental
MethyclothiazideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Methyclothiazide.Approved
MethyldopaMoxonidine may increase the hypotensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Moxonidine.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Moxonidine.Approved, Investigational
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Moxonidine.Approved
MetipranololMoxonidine may increase the hypotensive activities of Metipranolol.Approved
MetolazoneMoxonidine may increase the hypotensive activities of Metolazone.Approved
MetoprololMoxonidine may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
MetyrosineMoxonidine may increase the hypotensive activities of Metyrosine.Approved
MianserinThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Mianserin.Approved
MibefradilMoxonidine may increase the hypotensive activities of Mibefradil.Withdrawn
MilnacipranMilnacipran may decrease the antihypertensive activities of Moxonidine.Approved
MinaprineMinaprine may increase the hypotensive activities of Moxonidine.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Moxonidine.Approved
MirodenafilMirodenafil may increase the antihypertensive activities of Moxonidine.Investigational
MirtazapineMirtazapine may decrease the antihypertensive activities of Moxonidine.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Moxonidine.Approved
MoexiprilMoxonidine may increase the hypotensive activities of Moexipril.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Moxonidine.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Moxonidine.Approved, Investigational
MuzolimineMoxonidine may increase the hypotensive activities of Muzolimine.Experimental
NabiloneThe risk or severity of adverse effects can be increased when Moxonidine is combined with Nabilone.Approved, Investigational
NadololMoxonidine may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NaftopidilMoxonidine may increase the hypotensive activities of Naftopidil.Investigational
NebivololMoxonidine may increase the hypotensive activities of Nebivolol.Approved, Investigational
NesiritideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Nesiritide.Approved, Investigational
NialamideNialamide may increase the hypotensive activities of Moxonidine.Withdrawn
NicardipineMoxonidine may increase the hypotensive activities of Nicardipine.Approved
NicorandilNicorandil may increase the hypotensive activities of Moxonidine.Approved
NifedipineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Nifedipine.Approved
NiguldipineMoxonidine may increase the hypotensive activities of Niguldipine.Experimental
NilvadipineMoxonidine may increase the hypotensive activities of Nilvadipine.Approved
NimodipineMoxonidine may increase the hypotensive activities of Nimodipine.Approved
NisoldipineMoxonidine may increase the hypotensive activities of Nisoldipine.Approved
NitrendipineMoxonidine may increase the hypotensive activities of Nitrendipine.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Nitric Oxide.Approved
NitroglycerinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Nitroglycerin.Approved, Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Moxonidine.Approved
NortriptylineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Nortriptyline.Approved
ObinutuzumabMoxonidine may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Moxonidine.Withdrawn
OlmesartanMoxonidine may increase the hypotensive activities of Olmesartan.Approved, Investigational
OmapatrilatMoxonidine may increase the hypotensive activities of Omapatrilat.Investigational
OpipramolThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Opipramol.Investigational
OxprenololMoxonidine may increase the atrioventricular blocking (AV block) activities of Oxprenolol.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Moxonidine is combined with Paclitaxel.Approved, Vet Approved
PapaverineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Papaverine.Approved
PargylinePargyline may increase the hypotensive activities of Moxonidine.Approved
PenbutololMoxonidine may increase the atrioventricular blocking (AV block) activities of Penbutolol.Approved, Investigational
PentobarbitalPentobarbital may increase the hypotensive activities of Moxonidine.Approved, Vet Approved
PentoliniumMoxonidine may increase the hypotensive activities of Pentolinium.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Moxonidine.Approved, Investigational
PerindoprilMoxonidine may increase the hypotensive activities of Perindopril.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Moxonidine.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Moxonidine.Withdrawn
PhenobarbitalPhenobarbital may increase the hypotensive activities of Moxonidine.Approved
PhenoxybenzamineMoxonidine may increase the hypotensive activities of Phenoxybenzamine.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Moxonidine.Withdrawn
PhentolamineMoxonidine may increase the hypotensive activities of Phentolamine.Approved
PinacidilPinacidil may increase the hypotensive activities of Moxonidine.Withdrawn
PindololMoxonidine may increase the atrioventricular blocking (AV block) activities of Pindolol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Moxonidine is combined with Pipamperone.Approved
PirlindolePirlindole may increase the hypotensive activities of Moxonidine.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Moxonidine.Withdrawn
PolythiazideMoxonidine may increase the hypotensive activities of Polythiazide.Approved
PractololMoxonidine may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PramipexoleThe risk or severity of adverse effects can be increased when Moxonidine is combined with Pramipexole.Approved, Investigational
PrazosinPrazosin may increase the hypotensive activities of Moxonidine.Approved
PrimidonePrimidone may increase the hypotensive activities of Moxonidine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Moxonidine is combined with Propofol.Approved, Investigational, Vet Approved
PropranololMoxonidine may increase the atrioventricular blocking (AV block) activities of Propranolol.Approved, Investigational
ProtriptylineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Protriptyline.Approved
QuetiapineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Quetiapine.Approved
QuinaprilMoxonidine may increase the hypotensive activities of Quinapril.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Moxonidine.Approved
RamiprilMoxonidine may increase the hypotensive activities of Ramipril.Approved
RasagilineRasagiline may increase the hypotensive activities of Moxonidine.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Moxonidine is combined with Remifentanil.Approved
RemikirenMoxonidine may increase the hypotensive activities of Remikiren.Approved
RescinnamineMoxonidine may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Moxonidine.Approved
RilmenidineMoxonidine may increase the hypotensive activities of Rilmenidine.Investigational
RiociguatMoxonidine may increase the hypotensive activities of Riociguat.Approved
RisperidoneMoxonidine may increase the hypotensive activities of Risperidone.Approved, Investigational
RituximabMoxonidine may increase the hypotensive activities of Rituximab.Approved
RopiniroleThe risk or severity of adverse effects can be increased when Moxonidine is combined with Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Ropivacaine.Approved
RotigotineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Rotigotine.Approved
SacubitrilThe risk or severity of adverse effects can be increased when Moxonidine is combined with Sacubitril.Approved
SafrazineSafrazine may increase the hypotensive activities of Moxonidine.Withdrawn
SaprisartanMoxonidine may increase the hypotensive activities of Saprisartan.Experimental
SecobarbitalSecobarbital may increase the hypotensive activities of Moxonidine.Approved, Vet Approved
SelegilineSelegiline may increase the hypotensive activities of Moxonidine.Approved, Investigational, Vet Approved
SelexipagMoxonidine may increase the hypotensive activities of Selexipag.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Moxonidine is combined with Sevoflurane.Approved, Vet Approved
SildenafilSildenafil may increase the antihypertensive activities of Moxonidine.Approved, Investigational
SitaxentanMoxonidine may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
Sodium NitriteThe risk or severity of adverse effects can be increased when Moxonidine is combined with Sodium Nitrite.Approved
SotalolMoxonidine may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
SpiraprilMoxonidine may increase the hypotensive activities of Spirapril.Approved
SpironolactoneThe risk or severity of adverse effects can be increased when Moxonidine is combined with Spironolactone.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Moxonidine is combined with Streptokinase.Approved
SufentanilThe risk or severity of adverse effects can be increased when Moxonidine is combined with Sufentanil.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Moxonidine.Approved, Investigational
TalinololMoxonidine may increase the atrioventricular blocking (AV block) activities of Talinolol.Investigational
TamsulosinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Tamsulosin.Approved, Investigational
TelmisartanMoxonidine may increase the hypotensive activities of Telmisartan.Approved, Investigational
TemocaprilMoxonidine may increase the hypotensive activities of Temocapril.Experimental, Investigational
TerazosinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Terazosin.Approved
TerlipressinMoxonidine may increase the hypotensive activities of Terlipressin.Approved, Investigational
TertatololMoxonidine may increase the atrioventricular blocking (AV block) activities of Tertatolol.Experimental
TetrahydropalmatineMoxonidine may increase the hypotensive activities of Tetrahydropalmatine.Investigational
ThalidomideThe risk or severity of adverse effects can be increased when Moxonidine is combined with Thalidomide.Approved, Investigational, Withdrawn
TheodrenalineMoxonidine may increase the hypotensive activities of Theodrenaline.Investigational
ThiamylalThiamylal may increase the hypotensive activities of Moxonidine.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Moxonidine.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Thioridazine.Withdrawn
TianeptineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Tianeptine.Approved
TiboloneMoxonidine may increase the hypotensive activities of Tibolone.Approved
TicrynafenMoxonidine may increase the hypotensive activities of Ticrynafen.Withdrawn
TimololMoxonidine may increase the atrioventricular blocking (AV block) activities of Timolol.Approved
TizanidineThe risk or severity of adverse effects can be increased when Moxonidine is combined with Tizanidine.Approved
TolazolineMoxonidine may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
TolcaponeThe risk or severity of adverse effects can be increased when Moxonidine is combined with Tolcapone.Approved, Withdrawn
TolonidineMoxonidine may increase the hypotensive activities of Tolonidine.Experimental
ToloxatoneToloxatone may increase the hypotensive activities of Moxonidine.Approved
TorasemideMoxonidine may increase the hypotensive activities of Torasemide.Approved
TrandolaprilMoxonidine may increase the hypotensive activities of Trandolapril.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Moxonidine.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Moxonidine.Approved
TravoprostMoxonidine may increase the hypotensive activities of Travoprost.Approved
TreprostinilMoxonidine may increase the hypotensive activities of Treprostinil.Approved, Investigational
TretinoinThe risk or severity of adverse effects can be increased when Moxonidine is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneThe risk or severity of adverse effects can be increased when Moxonidine is combined with Triamterene.Approved
TrichlormethiazideMoxonidine may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Moxonidine.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Moxonidine.Approved
TrimipramineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Trimipramine.Approved
UdenafilUdenafil may increase the antihypertensive activities of Moxonidine.Approved, Investigational
UnoprostoneMoxonidine may increase the hypotensive activities of Unoprostone.Approved
UrapidilMoxonidine may increase the hypotensive activities of Urapidil.Investigational
ValsartanMoxonidine may increase the hypotensive activities of Valsartan.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Moxonidine.Approved
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Moxonidine.Approved
VerapamilThe risk or severity of adverse effects can be increased when Moxonidine is combined with Verapamil.Approved
VincamineMoxonidine may increase the hypotensive activities of Vincamine.Experimental
VinpocetineMoxonidine may increase the hypotensive activities of Vinpocetine.Investigational
XipamideMoxonidine may increase the hypotensive activities of Xipamide.Experimental
XylometazolineMoxonidine may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Moxonidine.Approved, Vet Approved
ZofenoprilMoxonidine may increase the hypotensive activities of Zofenopril.Experimental
Food Interactions
Not Available

References

General References
  1. Cohn JN, Pfeffer MA, Rouleau J, Sharpe N, Swedberg K, Straub M, Wiltse C, Wright TJ: Adverse mortality effect of central sympathetic inhibition with sustained-release moxonidine in patients with heart failure (MOXCON). Eur J Heart Fail. 2003 Oct;5(5):659-67. [PubMed:14607206]
  2. Fenton C, Keating GM, Lyseng-Williamson KA: Moxonidine: a review of its use in essential hypertension. Drugs. 2006;66(4):477-96. [PubMed:16597164]
  3. Prichard BN, Owens CW, Graham BR: Pharmacology and clinical use of moxonidine, a new centrally acting sympatholytic antihypertensive agent. J Hum Hypertens. 1997 Aug;11 Suppl 1:S29-45. [PubMed:9321737]
  4. Prichard BN, Graham BR: I1 imidazoline agonists. General clinical pharmacology of imidazoline receptors: implications for the treatment of the elderly. Drugs Aging. 2000 Aug;17(2):133-59. [PubMed:10984201]
  5. Ernsberger P, Haxhiu MA, Graff LM, Collins LA, Dreshaj I, Grove DL, Graves ME, Schafer SG, Christen MO: A novel mechanism of action for hypertension control: moxonidine as a selective I1-imidazoline agonist. Cardiovasc Drugs Ther. 1994 Mar;8 Suppl 1:27-41. [PubMed:8068578]
External Links
Human Metabolome Database
HMDB41938
KEGG Drug
D05087
KEGG Compound
C07451
PubChem Compound
4810
PubChem Substance
310265145
ChemSpider
4645
BindingDB
50050093
ChEBI
7009
ChEMBL
CHEMBL19236
Wikipedia
Moxonidine
ATC Codes
C02LC05 — Moxonidine and diureticsC02AC05 — Moxonidine
FDA label
Download (108 KB)
MSDS
Download (56.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentHypertensive1
3TerminatedPreventionCardiac Diseases / Vascular Surgery1
4CompletedTreatmentHypertensive / Metabolic Syndromes / Obesity, Abdominal1
4CompletedTreatmentNonvalvular Atrial Fibrillation1
4CompletedTreatmentPolycystic Ovaries Syndrome1
4Unknown StatusNot AvailableBMI >27 kg/m2 / BMI >30 kg/m21
4Unknown StatusTreatmentDiabetic Nephropathies1
4Unknown StatusTreatmentHypertensive / Obesity, Abdominal1
4Unknown StatusTreatmentSchizophrenic Disorders1
Not AvailableRecruitingBasic ScienceArterial Hypertension / Osteopenia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)197 – 205MSDS
water solubility<1 mg/mLMSDS
Predicted Properties
PropertyValueSource
Water Solubility0.114 mg/mLALOGPS
logP1.01ALOGPS
logP1.54ChemAxon
logS-3.3ALOGPS
pKa (Strongest Basic)7.26ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area71.43 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity63.41 m3·mol-1ChemAxon
Polarizability23.57 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

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

Taxonomy

Description
This compound belongs to the class of organic compounds known as halopyrimidines. These are aromatic compounds containing a halogen atom linked to a pyrimidine ring. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazines
Sub Class
Pyrimidines and pyrimidine derivatives
Direct Parent
Halopyrimidines
Alternative Parents
Aminopyrimidines and derivatives / Alkyl aryl ethers / Aryl chlorides / Imidazolines / Heteroaromatic compounds / Guanidines / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Organopnictogen compounds
show 2 more
Substituents
Alkyl aryl ether / Aminopyrimidine / Halopyrimidine / Aryl chloride / Aryl halide / Heteroaromatic compound / 2-imidazoline / Guanidine / Ether / Azacycle
show 12 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
pyrimidines, organohalogen compound (CHEBI:7009)

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. Zhu QM, Lesnick JD, Jasper JR, MacLennan SJ, Dillon MP, Eglen RM, Blue DR Jr: Cardiovascular effects of rilmenidine, moxonidine and clonidine in conscious wild-type and D79N alpha2A-adrenoceptor transgenic mice. Br J Pharmacol. 1999 Mar;126(6):1522-30. [PubMed:10217548]
  2. Stone LS, Fairbanks CA, Wilcox GL: Moxonidine, a mixed alpha(2)-adrenergic and imidazoline receptor agonist, identifies a novel adrenergic target for spinal analgesia. Ann N Y Acad Sci. 2003 Dec;1009:378-85. [PubMed:15028616]
  3. Buccafusco JJ, Lapp CA, Westbrooks KL, Ernsberger P: Role of medullary I1-imidazoline and alpha 2-adrenergic receptors in the antihypertensive responses evoked by central administration of clonidine analogs in conscious spontaneously hypertensive rats. J Pharmacol Exp Ther. 1995 Jun;273(3):1162-71. [PubMed:7791087]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Phosphatidylinositol binding
Specific Function
Acts either as the functional imidazoline-1 receptor (I1R) candidate or as a membrane-associated mediator of the I1R signaling. Binds numerous imidazoline ligands that induces initiation of cell-si...
Gene Name
NISCH
Uniprot ID
Q9Y2I1
Uniprot Name
Nischarin
Molecular Weight
166627.105 Da
References
  1. Ernsberger P, Damon TH, Graff LM, Schafer SG, Christen MO: Moxonidine, a centrally acting antihypertensive agent, is a selective ligand for I1-imidazoline sites. J Pharmacol Exp Ther. 1993 Jan;264(1):172-82. [PubMed:8380858]
  2. Buccafusco JJ, Lapp CA, Westbrooks KL, Ernsberger P: Role of medullary I1-imidazoline and alpha 2-adrenergic receptors in the antihypertensive responses evoked by central administration of clonidine analogs in conscious spontaneously hypertensive rats. J Pharmacol Exp Ther. 1995 Jun;273(3):1162-71. [PubMed:7791087]

Drug created on October 23, 2015 14:26 / Updated on October 02, 2017 06:14