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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyMoxonidine
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
Structure for DB09242 (Moxonidine)
- 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]
Target Actions Organism AAlpha-2A adrenergic receptor agonistHuman ANischarin agonistHuman - 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
Drug Interaction Drug group 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Moxonidine. Experimental Acebutolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Acebutolol. Approved Aldesleukin The risk or severity of adverse effects can be increased when Moxonidine is combined with Aldesleukin. Approved Alfuzosin Alfuzosin may increase the hypotensive activities of Moxonidine. Approved, Investigational Aliskiren Moxonidine may increase the hypotensive activities of Aliskiren. Approved, Investigational Alprenolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Alprenolol. Approved, Withdrawn Ambrisentan Moxonidine may increase the hypotensive activities of Ambrisentan. Approved, Investigational Amifostine Moxonidine may increase the hypotensive activities of Amifostine. Approved, Investigational Amiloride The risk or severity of adverse effects can be increased when Moxonidine is combined with Amiloride. Approved Amineptine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Amineptine. Illicit, Withdrawn Amiodarone The risk or severity of adverse effects can be increased when Amiodarone is combined with Moxonidine. Approved, Investigational Amitriptyline The therapeutic efficacy of Moxonidine can be decreased when used in combination with Amitriptyline. Approved Amlodipine Moxonidine may increase the hypotensive activities of Amlodipine. Approved Amobarbital Amobarbital may increase the hypotensive activities of Moxonidine. Approved, Illicit Amphotericin B The risk or severity of adverse effects can be increased when Amphotericin B is combined with Moxonidine. Approved, Investigational Amyl Nitrite The risk or severity of adverse effects can be increased when Moxonidine is combined with Amyl Nitrite. Approved Apomorphine The risk or severity of adverse effects can be increased when Apomorphine is combined with Moxonidine. Approved, Investigational Apraclonidine The risk or severity of adverse effects can be increased when Moxonidine is combined with Apraclonidine. Approved Aripiprazole Aripiprazole may increase the hypotensive activities of Moxonidine. Approved, Investigational Arotinolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Arotinolol. Approved Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Moxonidine. Approved, Investigational Atenolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Atenolol. Approved Azilsartan medoxomil The risk or severity of adverse effects can be increased when Moxonidine is combined with Azilsartan medoxomil. Approved Barbexaclone Barbexaclone may increase the hypotensive activities of Moxonidine. Experimental Barbital Barbital may increase the hypotensive activities of Moxonidine. Illicit Barnidipine The risk or severity of adverse effects can be increased when Barnidipine is combined with Moxonidine. Approved Befunolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Befunolol. Experimental Benazepril Moxonidine may increase the hypotensive activities of Benazepril. Approved, Investigational Bendroflumethiazide Moxonidine may increase the hypotensive activities of Bendroflumethiazide. Approved Benmoxin Benmoxin may increase the hypotensive activities of Moxonidine. Withdrawn Bepridil Moxonidine may increase the hypotensive activities of Bepridil. Approved, Withdrawn Betaxolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Betaxolol. Approved Bethanidine Bethanidine may increase the hypotensive activities of Moxonidine. Approved Bevantolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Bevantolol. Approved Bietaserpine Moxonidine may increase the hypotensive activities of Bietaserpine. Experimental Bimatoprost Moxonidine may increase the hypotensive activities of Bimatoprost. Approved, Investigational Bisoprolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Bisoprolol. Approved Bopindolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Bopindolol. Approved Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Moxonidine. Approved, Investigational Bosentan Bosentan may increase the hypotensive activities of Moxonidine. Approved, Investigational BQ-123 Moxonidine may increase the hypotensive activities of BQ-123. Investigational Bretylium Moxonidine may increase the hypotensive activities of Bretylium. Approved Brimonidine Brimonidine may increase the antihypertensive activities of Moxonidine. Approved Brofaromine Brofaromine may increase the hypotensive activities of Moxonidine. Experimental Bromocriptine The risk or severity of adverse effects can be increased when Bromocriptine is combined with Moxonidine. Approved, Investigational Bucindolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Bucindolol. Investigational Bufuralol Moxonidine may increase the atrioventricular blocking (AV block) activities of Bufuralol. Experimental, Investigational Bumetanide The risk or severity of adverse effects can be increased when Moxonidine is combined with Bumetanide. Approved Bupivacaine The risk or severity of adverse effects can be increased when Bupivacaine is combined with Moxonidine. Approved, Investigational Bupranolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Bupranolol. Approved Cadralazine Moxonidine may increase the hypotensive activities of Cadralazine. Experimental Cafedrine Moxonidine may increase the hypotensive activities of Cafedrine. Investigational Canagliflozin The risk or severity of adverse effects can be increased when Moxonidine is combined with Canagliflozin. Approved Candesartan Moxonidine may increase the hypotensive activities of Candesartan. Approved Candoxatril Moxonidine may increase the hypotensive activities of Candoxatril. Experimental Captopril Moxonidine may increase the hypotensive activities of Captopril. Approved Carbetocin The risk or severity of adverse effects can be increased when Carbetocin is combined with Moxonidine. Approved Caroxazone Caroxazone may increase the hypotensive activities of Moxonidine. Withdrawn Carteolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Carteolol. Approved Carvedilol Moxonidine may increase the atrioventricular blocking (AV block) activities of Carvedilol. Approved, Investigational Celiprolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Celiprolol. Approved, Investigational Chlorothiazide Moxonidine may increase the hypotensive activities of Chlorothiazide. Approved, Vet Approved Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Moxonidine. Approved, Vet Approved Chlorthalidone Moxonidine may increase the hypotensive activities of Chlorthalidone. Approved Cicletanine Moxonidine may increase the hypotensive activities of Cicletanine. Investigational Cilazapril Moxonidine may increase the hypotensive activities of Cilazapril. Approved Cilnidipine The risk or severity of adverse effects can be increased when Cilnidipine is combined with Moxonidine. Approved Clevidipine The risk or severity of adverse effects can be increased when Moxonidine is combined with Clevidipine. Approved Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Moxonidine. Approved, Investigational Clomipramine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Clomipramine. Approved, Vet Approved Clonidine Clonidine may increase the hypotensive activities of Moxonidine. Approved Cloranolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Cloranolol. Experimental Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Moxonidine. Approved Conivaptan The risk or severity of adverse effects can be increased when Conivaptan is combined with Moxonidine. Approved, Investigational Cryptenamine Moxonidine may increase the hypotensive activities of Cryptenamine. Approved Cyclobenzaprine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Cyclobenzaprine. Approved Cyclopenthiazide Moxonidine may increase the hypotensive activities of Cyclopenthiazide. Experimental Cyclothiazide Moxonidine may increase the hypotensive activities of Cyclothiazide. Approved Dapagliflozin The risk or severity of adverse effects can be increased when Moxonidine is combined with Dapagliflozin. Approved Debrisoquin Debrisoquin may increase the hypotensive activities of Moxonidine. Approved Delapril Moxonidine may increase the hypotensive activities of Delapril. Experimental Deserpidine Moxonidine may increase the hypotensive activities of Deserpidine. Approved Desflurane The risk or severity of adverse effects can be increased when Desflurane is combined with Moxonidine. Approved Desipramine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Desipramine. Approved Desvenlafaxine Desvenlafaxine may decrease the antihypertensive activities of Moxonidine. Approved Dexmedetomidine The risk or severity of adverse effects can be increased when Moxonidine is combined with Dexmedetomidine. Approved, Vet Approved Diazoxide Diazoxide may increase the hypotensive activities of Moxonidine. Approved Dibenzepin The therapeutic efficacy of Moxonidine can be decreased when used in combination with Dibenzepin. Experimental Diclofenamide The risk or severity of adverse effects can be increased when Moxonidine is combined with Diclofenamide. Approved diethylnorspermine Moxonidine may increase the hypotensive activities of diethylnorspermine. Investigational Dihydralazine Moxonidine may increase the hypotensive activities of Dihydralazine. Investigational Diltiazem Moxonidine may increase the hypotensive activities of Diltiazem. Approved Dinutuximab The risk or severity of adverse effects can be increased when Moxonidine is combined with Dinutuximab. Approved Dipyridamole The risk or severity of adverse effects can be increased when Moxonidine is combined with Dipyridamole. Approved Dorzolamide Moxonidine may increase the hypotensive activities of Dorzolamide. Approved Dosulepin The therapeutic efficacy of Moxonidine can be decreased when used in combination with Dosulepin. Approved Doxazosin Doxazosin may increase the hypotensive activities of Moxonidine. Approved Doxepin The therapeutic efficacy of Moxonidine can be decreased when used in combination with Doxepin. Approved Duloxetine Moxonidine may increase the orthostatic hypotensive activities of Duloxetine. Approved Efonidipine Moxonidine may increase the hypotensive activities of Efonidipine. Approved Empagliflozin The risk or severity of adverse effects can be increased when Moxonidine is combined with Empagliflozin. Approved Enalapril Moxonidine may increase the hypotensive activities of Enalapril. Approved, Vet Approved Enalaprilat Moxonidine may increase the hypotensive activities of Enalaprilat. Approved Endralazine Moxonidine may increase the hypotensive activities of Endralazine. Experimental Epanolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Epanolol. Experimental Eplerenone The risk or severity of adverse effects can be increased when Moxonidine is combined with Eplerenone. Approved Epoprostenol Moxonidine may increase the hypotensive activities of Epoprostenol. Approved Eprosartan Moxonidine may increase the hypotensive activities of Eprosartan. Approved Esmirtazapine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Esmirtazapine. Investigational Esmolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Esmolol. Approved Etacrynic acid The risk or severity of adverse effects can be increased when Moxonidine is combined with Etacrynic acid. Approved Felodipine Moxonidine may increase the hypotensive activities of Felodipine. Approved, Investigational Fenoldopam Moxonidine may increase the hypotensive activities of Fenoldopam. Approved Ferulic acid Moxonidine may increase the hypotensive activities of Ferulic acid. Experimental Fimasartan The risk or severity of adverse effects can be increased when Fimasartan is combined with Moxonidine. Approved Fosinopril Moxonidine may increase the hypotensive activities of Fosinopril. Approved Furazolidone Furazolidone may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Furosemide The risk or severity of adverse effects can be increased when Moxonidine is combined with Furosemide. Approved, Vet Approved Guanabenz Moxonidine may increase the hypotensive activities of Guanabenz. Approved Guanadrel Moxonidine may increase the hypotensive activities of Guanadrel. Approved Guanazodine Moxonidine may increase the hypotensive activities of Guanazodine. Experimental Guanethidine Guanethidine may increase the hypotensive activities of Moxonidine. Approved Guanfacine Guanfacine may increase the hypotensive activities of Moxonidine. Approved, Investigational Guanoclor Moxonidine may increase the hypotensive activities of Guanoclor. Experimental Guanoxabenz Moxonidine may increase the hypotensive activities of Guanoxabenz. Experimental Guanoxan Moxonidine may increase the hypotensive activities of Guanoxan. Experimental Halothane The risk or severity of adverse effects can be increased when Halothane is combined with Moxonidine. Approved, Vet Approved Harmaline Harmaline may increase the hypotensive activities of Moxonidine. Experimental Hexamethonium Moxonidine may increase the hypotensive activities of Hexamethonium. Experimental Hexobarbital Hexobarbital may increase the hypotensive activities of Moxonidine. Approved Hydracarbazine Hydracarbazine may increase the hypotensive activities of Moxonidine. Experimental Hydralazine Hydralazine may increase the hypotensive activities of Moxonidine. Approved Hydrochlorothiazide Moxonidine may increase the hypotensive activities of Hydrochlorothiazide. Approved, Vet Approved Hydroflumethiazide Moxonidine may increase the hypotensive activities of Hydroflumethiazide. Approved Iloprost Iloprost may increase the hypotensive activities of Moxonidine. Approved, Investigational Imidapril The risk or severity of adverse effects can be increased when Imidapril is combined with Moxonidine. Investigational Imipramine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Imipramine. Approved Indapamide Moxonidine may increase the hypotensive activities of Indapamide. Approved Indenolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Indenolol. Withdrawn Indoramin Indoramin may increase the hypotensive activities of Moxonidine. Withdrawn Iobenguane The therapeutic efficacy of Iobenguane can be decreased when used in combination with Moxonidine. Approved Iprindole The therapeutic efficacy of Moxonidine can be decreased when used in combination with Iprindole. Experimental Iproclozide Iproclozide may increase the hypotensive activities of Moxonidine. Withdrawn Iproniazid Iproniazid may increase the hypotensive activities of Moxonidine. Withdrawn Irbesartan Moxonidine may increase the hypotensive activities of Irbesartan. Approved, Investigational Isocarboxazid Isocarboxazid may increase the hypotensive activities of Moxonidine. Approved Isoflurane The risk or severity of adverse effects can be increased when Isoflurane is combined with Moxonidine. Approved, Vet Approved Isosorbide Dinitrate The risk or severity of adverse effects can be increased when Moxonidine is combined with Isosorbide Dinitrate. Approved Isosorbide Mononitrate The risk or severity of adverse effects can be increased when Moxonidine is combined with Isosorbide Mononitrate. Approved Isoxsuprine The risk or severity of adverse effects can be increased when Moxonidine is combined with Isoxsuprine. Approved, Withdrawn Isradipine Moxonidine may increase the hypotensive activities of Isradipine. Approved Ketanserin Moxonidine may increase the hypotensive activities of Ketanserin. Investigational Labetalol Moxonidine may increase the atrioventricular blocking (AV block) activities of Labetalol. Approved Lacidipine Moxonidine may increase the hypotensive activities of Lacidipine. Approved Landiolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Landiolol. Investigational Latanoprost Moxonidine may increase the hypotensive activities of Latanoprost. Approved, Investigational Lercanidipine Moxonidine may increase the hypotensive activities of Lercanidipine. Approved, Investigational Levobunolol The risk or severity of adverse effects can be increased when Moxonidine is combined with Levobunolol. Approved Levobupivacaine The risk or severity of adverse effects can be increased when Levobupivacaine is combined with Moxonidine. Approved Levodopa Moxonidine may increase the orthostatic hypotensive activities of Levodopa. Approved Levomilnacipran Levomilnacipran may decrease the antihypertensive activities of Moxonidine. Approved Levosimendan The risk or severity of adverse effects can be increased when Levosimendan is combined with Moxonidine. Approved, Investigational Linsidomine Moxonidine may increase the hypotensive activities of Linsidomine. Experimental Lisinopril Moxonidine may increase the hypotensive activities of Lisinopril. Approved, Investigational Lofepramine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Lofepramine. Experimental Lofexidine Moxonidine may increase the hypotensive activities of Lofexidine. Approved, Investigational Losartan Moxonidine may increase the hypotensive activities of Losartan. Approved Macitentan Moxonidine may increase the hypotensive activities of Macitentan. Approved Manidipine Moxonidine may increase the hypotensive activities of Manidipine. Approved Mannitol The risk or severity of adverse effects can be increased when Moxonidine is combined with Mannitol. Approved, Investigational Mebanazine Mebanazine may increase the hypotensive activities of Moxonidine. Withdrawn Mecamylamine Mecamylamine may increase the hypotensive activities of Moxonidine. Approved Mepindolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Mepindolol. Experimental Methazolamide The risk or severity of adverse effects can be increased when Moxonidine is combined with Methazolamide. Approved Methohexital Methohexital may increase the hypotensive activities of Moxonidine. Approved Methoserpidine Moxonidine may increase the hypotensive activities of Methoserpidine. Experimental Methyclothiazide The risk or severity of adverse effects can be increased when Moxonidine is combined with Methyclothiazide. Approved Methyldopa Moxonidine may increase the hypotensive activities of Methyldopa. Approved Methylene blue Methylene blue may increase the hypotensive activities of Moxonidine. Investigational Methylphenidate Methylphenidate may decrease the antihypertensive activities of Moxonidine. Approved, Investigational Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Moxonidine. Approved Metipranolol Moxonidine may increase the hypotensive activities of Metipranolol. Approved Metolazone Moxonidine may increase the hypotensive activities of Metolazone. Approved Metoprolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Metoprolol. Approved, Investigational Metyrosine Moxonidine may increase the hypotensive activities of Metyrosine. Approved Mianserin The therapeutic efficacy of Moxonidine can be decreased when used in combination with Mianserin. Approved Mibefradil Moxonidine may increase the hypotensive activities of Mibefradil. Withdrawn Milnacipran Milnacipran may decrease the antihypertensive activities of Moxonidine. Approved Minaprine Minaprine may increase the hypotensive activities of Moxonidine. Approved Minoxidil Minoxidil may increase the hypotensive activities of Moxonidine. Approved Mirodenafil Mirodenafil may increase the antihypertensive activities of Moxonidine. Investigational Mirtazapine Mirtazapine may decrease the antihypertensive activities of Moxonidine. Approved Moclobemide Moclobemide may increase the hypotensive activities of Moxonidine. Approved Moexipril Moxonidine may increase the hypotensive activities of Moexipril. Approved Molsidomine Molsidomine may increase the hypotensive activities of Moxonidine. Approved Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Moxonidine. Approved, Investigational Muzolimine Moxonidine may increase the hypotensive activities of Muzolimine. Experimental Nabilone The risk or severity of adverse effects can be increased when Moxonidine is combined with Nabilone. Approved, Investigational Nadolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Nadolol. Approved Naftopidil Moxonidine may increase the hypotensive activities of Naftopidil. Investigational Nebivolol Moxonidine may increase the hypotensive activities of Nebivolol. Approved, Investigational Nesiritide The risk or severity of adverse effects can be increased when Moxonidine is combined with Nesiritide. Approved, Investigational Nialamide Nialamide may increase the hypotensive activities of Moxonidine. Withdrawn Nicardipine Moxonidine may increase the hypotensive activities of Nicardipine. Approved Nicorandil Nicorandil may increase the hypotensive activities of Moxonidine. Approved Nifedipine The risk or severity of adverse effects can be increased when Moxonidine is combined with Nifedipine. Approved Niguldipine Moxonidine may increase the hypotensive activities of Niguldipine. Experimental Nilvadipine Moxonidine may increase the hypotensive activities of Nilvadipine. Approved Nimodipine Moxonidine may increase the hypotensive activities of Nimodipine. Approved Nisoldipine Moxonidine may increase the hypotensive activities of Nisoldipine. Approved Nitrendipine Moxonidine may increase the hypotensive activities of Nitrendipine. Approved Nitric Oxide The risk or severity of adverse effects can be increased when Moxonidine is combined with Nitric Oxide. Approved Nitroglycerin The risk or severity of adverse effects can be increased when Moxonidine is combined with Nitroglycerin. Approved, Investigational Nitroprusside Nitroprusside may increase the hypotensive activities of Moxonidine. Approved Nortriptyline The therapeutic efficacy of Moxonidine can be decreased when used in combination with Nortriptyline. Approved Obinutuzumab Moxonidine may increase the hypotensive activities of Obinutuzumab. Approved Octamoxin Octamoxin may increase the hypotensive activities of Moxonidine. Withdrawn Olmesartan Moxonidine may increase the hypotensive activities of Olmesartan. Approved, Investigational Omapatrilat Moxonidine may increase the hypotensive activities of Omapatrilat. Investigational Opipramol The therapeutic efficacy of Moxonidine can be decreased when used in combination with Opipramol. Investigational Oxprenolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Oxprenolol. Approved Paclitaxel The risk or severity of adverse effects can be increased when Moxonidine is combined with Paclitaxel. Approved, Vet Approved Papaverine The risk or severity of adverse effects can be increased when Moxonidine is combined with Papaverine. Approved Pargyline Pargyline may increase the hypotensive activities of Moxonidine. Approved Penbutolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Penbutolol. Approved, Investigational Pentobarbital Pentobarbital may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Pentolinium Moxonidine may increase the hypotensive activities of Pentolinium. Approved Pentoxifylline Pentoxifylline may increase the hypotensive activities of Moxonidine. Approved, Investigational Perindopril Moxonidine may increase the hypotensive activities of Perindopril. Approved Phenelzine Phenelzine may increase the hypotensive activities of Moxonidine. Approved Pheniprazine Pheniprazine may increase the hypotensive activities of Moxonidine. Withdrawn Phenobarbital Phenobarbital may increase the hypotensive activities of Moxonidine. Approved Phenoxybenzamine Moxonidine may increase the hypotensive activities of Phenoxybenzamine. Approved Phenoxypropazine Phenoxypropazine may increase the hypotensive activities of Moxonidine. Withdrawn Phentolamine Moxonidine may increase the hypotensive activities of Phentolamine. Approved Pinacidil Pinacidil may increase the hypotensive activities of Moxonidine. Withdrawn Pindolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Pindolol. Approved Pipamperone The risk or severity of adverse effects can be increased when Moxonidine is combined with Pipamperone. Approved Pirlindole Pirlindole may increase the hypotensive activities of Moxonidine. Approved Pivhydrazine Pivhydrazine may increase the hypotensive activities of Moxonidine. Withdrawn Polythiazide Moxonidine may increase the hypotensive activities of Polythiazide. Approved Practolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Practolol. Approved Pramipexole The risk or severity of adverse effects can be increased when Moxonidine is combined with Pramipexole. Approved, Investigational Prazosin Prazosin may increase the hypotensive activities of Moxonidine. Approved Primidone Primidone may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Propofol The risk or severity of adverse effects can be increased when Moxonidine is combined with Propofol. Approved, Investigational, Vet Approved Propranolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Propranolol. Approved, Investigational Protriptyline The therapeutic efficacy of Moxonidine can be decreased when used in combination with Protriptyline. Approved Quetiapine The risk or severity of adverse effects can be increased when Moxonidine is combined with Quetiapine. Approved Quinapril Moxonidine may increase the hypotensive activities of Quinapril. Approved, Investigational Quinine Quinine may increase the hypotensive activities of Moxonidine. Approved Ramipril Moxonidine may increase the hypotensive activities of Ramipril. Approved Rasagiline Rasagiline may increase the hypotensive activities of Moxonidine. Approved Remifentanil The risk or severity of adverse effects can be increased when Moxonidine is combined with Remifentanil. Approved Remikiren Moxonidine may increase the hypotensive activities of Remikiren. Approved Rescinnamine Moxonidine may increase the hypotensive activities of Rescinnamine. Approved Reserpine Reserpine may increase the hypotensive activities of Moxonidine. Approved Rilmenidine Moxonidine may increase the hypotensive activities of Rilmenidine. Investigational Riociguat Moxonidine may increase the hypotensive activities of Riociguat. Approved Risperidone Moxonidine may increase the hypotensive activities of Risperidone. Approved, Investigational Rituximab Moxonidine may increase the hypotensive activities of Rituximab. Approved Ropinirole The risk or severity of adverse effects can be increased when Moxonidine is combined with Ropinirole. Approved, Investigational Ropivacaine The risk or severity of adverse effects can be increased when Moxonidine is combined with Ropivacaine. Approved Rotigotine The risk or severity of adverse effects can be increased when Moxonidine is combined with Rotigotine. Approved Sacubitril The risk or severity of adverse effects can be increased when Moxonidine is combined with Sacubitril. Approved Safrazine Safrazine may increase the hypotensive activities of Moxonidine. Withdrawn Saprisartan Moxonidine may increase the hypotensive activities of Saprisartan. Experimental Secobarbital Secobarbital may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Selegiline Selegiline may increase the hypotensive activities of Moxonidine. Approved, Investigational, Vet Approved Selexipag Moxonidine may increase the hypotensive activities of Selexipag. Approved Sevoflurane The risk or severity of adverse effects can be increased when Moxonidine is combined with Sevoflurane. Approved, Vet Approved Sildenafil Sildenafil may increase the antihypertensive activities of Moxonidine. Approved, Investigational Sitaxentan Moxonidine may increase the hypotensive activities of Sitaxentan. Approved, Investigational, Withdrawn Sodium Nitrite The risk or severity of adverse effects can be increased when Moxonidine is combined with Sodium Nitrite. Approved Sotalol Moxonidine may increase the atrioventricular blocking (AV block) activities of Sotalol. Approved Spirapril Moxonidine may increase the hypotensive activities of Spirapril. Approved Spironolactone The risk or severity of adverse effects can be increased when Moxonidine is combined with Spironolactone. Approved Streptokinase The risk or severity of adverse effects can be increased when Moxonidine is combined with Streptokinase. Approved Sufentanil The risk or severity of adverse effects can be increased when Moxonidine is combined with Sufentanil. Approved, Investigational Tadalafil Tadalafil may increase the antihypertensive activities of Moxonidine. Approved, Investigational Talinolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Talinolol. Investigational Tamsulosin The risk or severity of adverse effects can be increased when Moxonidine is combined with Tamsulosin. Approved, Investigational Telmisartan Moxonidine may increase the hypotensive activities of Telmisartan. Approved, Investigational Temocapril Moxonidine may increase the hypotensive activities of Temocapril. Experimental, Investigational Terazosin The risk or severity of adverse effects can be increased when Moxonidine is combined with Terazosin. Approved Terlipressin Moxonidine may increase the hypotensive activities of Terlipressin. Approved, Investigational Tertatolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Tertatolol. Experimental Tetrahydropalmatine Moxonidine may increase the hypotensive activities of Tetrahydropalmatine. Investigational Thalidomide The risk or severity of adverse effects can be increased when Moxonidine is combined with Thalidomide. Approved, Investigational, Withdrawn Theodrenaline Moxonidine may increase the hypotensive activities of Theodrenaline. Investigational Thiamylal Thiamylal may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Thiopental Thiopental may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Thioridazine The risk or severity of adverse effects can be increased when Moxonidine is combined with Thioridazine. Withdrawn Tianeptine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Tianeptine. Approved Tibolone Moxonidine may increase the hypotensive activities of Tibolone. Approved Ticrynafen Moxonidine may increase the hypotensive activities of Ticrynafen. Withdrawn Timolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Timolol. Approved Tizanidine The risk or severity of adverse effects can be increased when Moxonidine is combined with Tizanidine. Approved Tolazoline Moxonidine may increase the hypotensive activities of Tolazoline. Approved, Vet Approved Tolcapone The risk or severity of adverse effects can be increased when Moxonidine is combined with Tolcapone. Approved, Withdrawn Tolonidine Moxonidine may increase the hypotensive activities of Tolonidine. Experimental Toloxatone Toloxatone may increase the hypotensive activities of Moxonidine. Approved Torasemide Moxonidine may increase the hypotensive activities of Torasemide. Approved Trandolapril Moxonidine may increase the hypotensive activities of Trandolapril. Approved Trans-2-Phenylcyclopropylamine Trans-2-Phenylcyclopropylamine may increase the hypotensive activities of Moxonidine. Experimental Tranylcypromine Tranylcypromine may increase the hypotensive activities of Moxonidine. Approved Travoprost Moxonidine may increase the hypotensive activities of Travoprost. Approved Treprostinil Moxonidine may increase the hypotensive activities of Treprostinil. Approved, Investigational Tretinoin The risk or severity of adverse effects can be increased when Moxonidine is combined with Tretinoin. Approved, Investigational, Nutraceutical Triamterene The risk or severity of adverse effects can be increased when Moxonidine is combined with Triamterene. Approved Trichlormethiazide Moxonidine may increase the hypotensive activities of Trichlormethiazide. Approved, Vet Approved Trimazosin Trimazosin may increase the hypotensive activities of Moxonidine. Experimental Trimethaphan Trimethaphan may increase the hypotensive activities of Moxonidine. Approved Trimipramine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Trimipramine. Approved Udenafil Udenafil may increase the antihypertensive activities of Moxonidine. Approved, Investigational Unoprostone Moxonidine may increase the hypotensive activities of Unoprostone. Approved Urapidil Moxonidine may increase the hypotensive activities of Urapidil. Investigational Valsartan Moxonidine may increase the hypotensive activities of Valsartan. Approved, Investigational Vardenafil Vardenafil may increase the antihypertensive activities of Moxonidine. Approved Venlafaxine Venlafaxine may decrease the antihypertensive activities of Moxonidine. Approved Verapamil The risk or severity of adverse effects can be increased when Moxonidine is combined with Verapamil. Approved Vincamine Moxonidine may increase the hypotensive activities of Vincamine. Experimental Vinpocetine Moxonidine may increase the hypotensive activities of Vinpocetine. Investigational Xipamide Moxonidine may increase the hypotensive activities of Xipamide. Experimental Xylometazoline Moxonidine may increase the hypotensive activities of Xylometazoline. Approved Yohimbine Yohimbine may decrease the antihypertensive activities of Moxonidine. Approved, Vet Approved Zofenopril Moxonidine may increase the hypotensive activities of Zofenopril. Experimental - Food Interactions
- Not Available
References
- General References
- 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]
- Fenton C, Keating GM, Lyseng-Williamson KA: Moxonidine: a review of its use in essential hypertension. Drugs. 2006;66(4):477-96. [PubMed:16597164]
- 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]
- 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]
- 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 diuretics
- C02LC — Imidazoline receptor agonists in combination with diuretics
- C02L — ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION
- C02 — ANTIHYPERTENSIVES
- C — CARDIOVASCULAR SYSTEM
- FDA label
- Download (108 KB)
- MSDS
- Download (56.5 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Treatment Hypertensive 1 3 Terminated Prevention Cardiac Diseases / Vascular Surgery 1 4 Completed Treatment Hypertensive / Metabolic Syndromes / Obesity, Abdominal 1 4 Completed Treatment Nonvalvular Atrial Fibrillation 1 4 Completed Treatment Polycystic Ovaries Syndrome 1 4 Unknown Status Not Available BMI >27 kg/m2 / BMI >30 kg/m2 1 4 Unknown Status Treatment Diabetic Nephropathies 1 4 Unknown Status Treatment Hypertensive / Obesity, Abdominal 1 4 Unknown Status Treatment Schizophrenic Disorders 1 Not Available Recruiting Basic Science Arterial Hypertension / Osteopenia 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 197 – 205 MSDS water solubility <1 mg/mL MSDS - Predicted Properties
Property Value Source Water Solubility 0.114 mg/mL ALOGPS logP 1.01 ALOGPS logP 1.54 ChemAxon logS -3.3 ALOGPS pKa (Strongest Basic) 7.26 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 6 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 71.43 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 63.41 m3·mol-1 ChemAxon Polarizability 23.57 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not 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
- 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]
- 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]
- 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
- 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]
- 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