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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyMoxonidine
This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Name
- Moxonidine
- Accession Number
- DB09242
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
Moxonidine is a new-generation centrally acting antihypertensive drug approved 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 or primary hypertension [7]. Effective as most first-line antihypertensives when used as monotherapy [2].
- Pharmacodynamics
Antihypertensive agent whose site of action is the Central Nervous System (CNS), specifically involving interactions with I1- imidazoline and alpha-2-adrenergic rececptors within the rostral ventrolateral medulla (RSV). [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 αlpha-2-adrenoreceptors in the RSV causing a reduction of sympathetic activity, reducing systemic vascular resistance and thus arterial blood pressure. [Label]
Moreover, since alpha-2-adrenergic receptors are considered the primary molecular target that facilitates the most common side effects of sedation and dry mouth that are elicited by most centrally acting antihypertensives, moxonidine differs from these other centrally acting antihypertensives by demonstrating only low affinity for central alpha-2-adrenoceptors compared to the aforementioned I1-imidazoline receptors [Label].
Target Actions Organism AAlpha-2A adrenergic receptor agonistHuman ANischarin agonistHuman - Absorption
90% of an oral dose is absorbed with negligible interference from food intake or first pass metabolism, resulting in a high bioavailability of 88%. [Label]
- Volume of distribution
1.8±0.4L/kg. [Label]
- Protein binding
About 10% of moxonidine is bound to plasma proteins. [Label]
- Metabolism
Biotransformation is unimportant [3] with 10-20% of moxonidine undergoing oxidation reactions to the primary 4,5-dehydromoxonidine metabolite and a guanidine derivative by opening of the imidazoline ring. [Label]
The antihypertensive effects of these 4,5-dehydromoxonidine and guanidine metabolites are only 1/10 and 1/100 the effect of moxonidine [Label].
Oxidation on either the methyl group (pyrimidine ring) or on the imidazole ring of moxonidine results in the formation of the hydroxylmethyl moxonidine metabolite or the hydroxy moxonidine metabolite [6]. The hydroxy moxonidine metabolite can be further oxidized to the dihydroxy metabolite or it can lose water to form the dehydrogenated moxonidine metabolite, which itself can be further oxidized to form an N-oxide [6]. Aside from these Phase I metabolites, Phase II metabolism of moxonidine is also evident with the presence of a cysteine conjugate metabolite minus chlorine [6]. Nevertheless, the identification of the hydroxy moxonidine metabolite with a high level of dehydrogenated moxonidine metabolite in human urine samples suggests that dehydrogenation from the hydroxy metabolite to the dehydrogenated moxonidine metabolite represents the primary metabolic pathway in humans [6].
The cytochromes P450 responsible for the metabolism of moxonidine in humans have not yet been determined [6].
Ultimately, the parent moxonidine compound was observed to be the most abundant component in different biological matrices of urinary excretion samples, verifying that metabolism only plays a modest role in the clearance of moxonidine in humans [6].
- Route of elimination
Elimination is nearly entirely via the kidneys with a majority (50 -75%) of overall moxonidine being eliminated unchanged through renal excretion. Ultimately, more than 90% of a dose is eliminated by way of the kidneys within the first 24 hours after administration, with only approximately 1% being eliminiated via faeces. [Label]
- Half life
Plasma elimination half life is 2.2 - 2.3 hours while renal elimination half life is 2.6-2.8 hours. [Label]
- Clearance
Administered twice daily due to short half life [Label].
However, lower dosage adjustments and close monitoring is necessary in elderly and renal impairment patients due to reduced clearance. In particular, the exposure AUC can increase by about 50% following a single dose and at steady state in elderly patients and moderately impaired renal function with GFR between 30-60 mL/min can cause AUC increases by 85% and decreases in clearence to 52 %. [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, severe bradyarrhythmia, sick sinus syndrome, second or third degree atrioventricular block, malignant arrhythmias. [Label]
- Used with caution in patients with history of severe coronary artery disease (CAD), unstable angina, angioneurotic edema. [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. [Label]
- Lack of specific therapeutic experience in cases of intermittent claudication, Raynaud's disease, Parkinson's disease, epileptic disorders, gluacoma, and depression suggest moxonidine should not be used in such instances [Label].
- Carcinogenicity and genotoxicity does not appear significant. [Label]
- Concurrent administration of other hypotensives or sedative and hypnotics can enhance the hypotensive effect and intensify sedation respectively. [Label]
- Avoid concurrent Tricyclic Antidepressant (TCA) use to avoid reduction of monoxidine efficacy. [Label]
- Generally well tolerated with dry mouth and headache the most common adverse effects [Label]
- Symptoms of overdose correlate with pharmacodynamic properties:hypotension, sedation, orthostatic dysregulation, bradycardia, dry mouth with no specific counter-treatment known. [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, Investigational Acemetacin The therapeutic efficacy of Moxonidine can be decreased when used in combination with Acemetacin. Approved, Experimental, Investigational Acepromazine Acepromazine may decrease the vasoconstricting activities of Moxonidine. Approved, Vet 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 Moxonidine may increase the atrioventricular blocking (AV block) activities of Amiodarone. Approved, Investigational Amitriptyline The therapeutic efficacy of Moxonidine can be decreased when used in combination with Amitriptyline. Approved Amitriptylinoxide The therapeutic efficacy of Moxonidine can be decreased when used in combination with Amitriptylinoxide. Approved, Investigational Amlodipine Moxonidine may increase the hypotensive activities of Amlodipine. Approved Amobarbital Amobarbital may increase the hypotensive activities of Moxonidine. Approved, Illicit Amoxapine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Amoxapine. Approved Amphetamine Amphetamine may increase the hypotensive activities of Moxonidine. Approved, Illicit, Investigational 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. Investigational Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Moxonidine. Approved, Investigational Asenapine Moxonidine may increase the atrioventricular blocking (AV block) activities of Asenapine. Approved Atenolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Atenolol. Approved Avanafil Avanafil may increase the antihypertensive activities of Moxonidine. Approved Azilsartan medoxomil The risk or severity of adverse effects can be increased when Moxonidine is combined with Azilsartan medoxomil. Approved, Investigational Barbexaclone Barbexaclone may increase the hypotensive activities of Moxonidine. Experimental Barbital Barbital may increase the hypotensive activities of Moxonidine. Illicit Barnidipine Moxonidine may increase the antihypertensive activities of Barnidipine. 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 Benzylpenicilloyl Polylysine Moxonidine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent. Approved Bepridil Moxonidine may increase the hypotensive activities of Bepridil. Approved, Withdrawn Betaxolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Betaxolol. Approved, Investigational 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 Brexpiprazole Brexpiprazole may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational Brimonidine Brimonidine may increase the antihypertensive activities of Moxonidine. Approved Brofaromine Brofaromine may increase the hypotensive activities of Moxonidine. Experimental Bromocriptine Bromocriptine may increase the hypertensive and vasoconstricting activities of 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 Bunazosin Bunazosin may decrease the vasoconstricting activities of Moxonidine. Investigational 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 Butriptyline The therapeutic efficacy of Moxonidine can be decreased when used in combination with Butriptyline. Approved Cabergoline Cabergoline may increase the hypertensive and vasoconstricting activities of Moxonidine. 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. Experimental Candesartan cilexetil Moxonidine may increase the hypotensive activities of Candesartan cilexetil. 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, Investigational 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, Investigational, 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, Investigational Clevidipine The risk or severity of adverse effects can be increased when Moxonidine is combined with Clevidipine. Approved, Investigational 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, Investigational, 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 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 Dapiprazole Dapiprazole may decrease the vasoconstricting activities of Moxonidine. Approved Debrisoquin Debrisoquin may increase the hypotensive activities of Moxonidine. Approved, Investigational Delapril Moxonidine may increase the hypotensive activities of Delapril. Investigational 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, Investigational Desvenlafaxine Desvenlafaxine may increase the tachycardic activities of Moxonidine. Approved, Investigational Dexmedetomidine The risk or severity of adverse effects can be increased when Moxonidine is combined with Dexmedetomidine. Approved, Vet Approved Dextroamphetamine Dextroamphetamine may decrease the vasoconstricting activities of Moxonidine. Approved, Illicit 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, Investigational Diethylnorspermine Moxonidine may increase the hypotensive activities of Diethylnorspermine. Investigational Dihydralazine Moxonidine may increase the hypotensive activities of Dihydralazine. Approved, Investigational Dihydroergotamine Dihydroergotamine may increase the hypertensive and vasoconstricting activities of Moxonidine. Approved, Investigational Diltiazem Moxonidine may increase the hypotensive activities of Diltiazem. Approved, Investigational Dimetacrine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Dimetacrine. Approved, Withdrawn Dinutuximab The risk or severity of adverse effects can be increased when Moxonidine is combined with Dinutuximab. Approved, Investigational 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, Investigational Dronedarone Dronedarone may decrease the vasoconstricting activities of Moxonidine. Approved Droperidol Droperidol may decrease the vasoconstricting activities of Moxonidine. Approved, Vet Approved Duloxetine Moxonidine may increase the orthostatic hypotensive activities of Duloxetine. Approved Efonidipine Moxonidine may increase the hypotensive activities of Efonidipine. Approved, Investigational 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 Epinephrine Epinephrine may decrease the vasoconstricting activities of Moxonidine. Approved, Vet Approved 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 Ergoloid mesylate Ergoloid mesylate may increase the hypertensive and vasoconstricting activities of Moxonidine. Approved Ergonovine Ergonovine may increase the hypertensive and vasoconstricting activities of Moxonidine. Approved Ergotamine Ergotamine may increase the hypertensive and vasoconstricting activities of Moxonidine. Approved Esatenolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Esatenolol. Experimental Escitalopram Escitalopram may decrease the vasoconstricting activities of Moxonidine. Approved, 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, Investigational 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, Investigational Flupentixol Flupentixol may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational, Withdrawn Fosinopril Moxonidine may increase the hypotensive activities of Fosinopril. Approved Fostamatinib Fostamatinib may increase the antihypertensive activities of Moxonidine. Approved, Investigational Furazolidone Furazolidone may increase the hypotensive activities of Moxonidine. Approved, Investigational, 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, Investigational Guanadrel Moxonidine may increase the hypotensive activities of Guanadrel. Approved Guanazodine Moxonidine may increase the hypotensive activities of Guanazodine. Experimental Guanethidine Moxonidine may increase the hypotensive activities of Guanethidine. 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 Hyaluronidase Hyaluronidase may increase the vasoconstricting activities of Moxonidine. Approved, Investigational 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, Investigational Iloperidone Iloperidone may decrease the vasoconstricting activities of Moxonidine. Approved Iloprost The risk or severity of adverse effects can be increased when Iloprost is combined with 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, Investigational 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, Investigational 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, Investigational 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, Investigational 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 Levobetaxolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Levobetaxolol. 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, Investigational Levodopa Moxonidine may increase the orthostatic hypotensive activities of Levodopa. Approved Levomilnacipran Levomilnacipran may increase the tachycardic activities of Moxonidine. Approved, Investigational 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 Lisdexamfetamine Lisdexamfetamine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational 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, Investigational 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, Investigational Melitracen The therapeutic efficacy of Moxonidine can be decreased when used in combination with Melitracen. Experimental, Investigational 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 Methotrimeprazine Methotrimeprazine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational 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. Approved, Investigational Methylergometrine Methylergometrine may increase the hypertensive and vasoconstricting activities of Moxonidine. Approved 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, Investigational Mibefradil Moxonidine may increase the hypotensive activities of Mibefradil. Investigational, Withdrawn Milnacipran Milnacipran may increase the tachycardic activities of Moxonidine. Approved, Investigational Minaprine Minaprine may increase the hypotensive activities of Moxonidine. Approved Minoxidil Minoxidil may increase the hypotensive activities of Moxonidine. Approved, Investigational 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, Investigational Moexipril Moxonidine may increase the hypotensive activities of Moexipril. Approved Molsidomine Molsidomine may increase the hypotensive activities of Moxonidine. Approved, Investigational 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 atrioventricular blocking (AV block) activities of Nebivolol. Approved, Investigational Nefazodone Nefazodone may decrease the vasoconstricting activities of Moxonidine. Approved, Withdrawn 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, Investigational Nicergoline Nicergoline may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational Nicorandil Nicorandil may increase the hypotensive activities of Moxonidine. Approved, Investigational 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, Investigational Nimodipine Moxonidine may increase the hypotensive activities of Nimodipine. Approved, Investigational Nisoldipine Moxonidine may increase the hypotensive activities of Nisoldipine. Approved Nitrendipine Moxonidine may increase the hypotensive activities of Nitrendipine. Approved, Investigational 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, Investigational Nitrous acid The risk or severity of adverse effects can be increased when Moxonidine is combined with Nitrous acid. Approved, Investigational 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, Investigational Octamoxin Octamoxin may increase the hypotensive activities of Moxonidine. Withdrawn Olanzapine Olanzapine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational 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 Paliperidone Paliperidone may decrease the vasoconstricting activities of Moxonidine. Approved Papaverine The risk or severity of adverse effects can be increased when Moxonidine is combined with Papaverine. Approved, Investigational 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, Investigational, 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, Investigational 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. Approved Pindolol Moxonidine may increase the atrioventricular blocking (AV block) activities of Pindolol. Approved, Investigational Pipamperone The risk or severity of adverse effects can be increased when Moxonidine is combined with Pipamperone. Approved, Investigational Pirlindole Pirlindole may increase the hypotensive activities of Moxonidine. Approved Pivhydrazine Pivhydrazine may increase the hypotensive activities of Moxonidine. Withdrawn Pizotifen Pizotifen may decrease the vasoconstricting activities of Moxonidine. Approved Platelet Activating Factor Moxonidine may increase the atrioventricular blocking (AV block) activities of Platelet Activating Factor. Experimental 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 Procaine Procaine may increase the hypotensive activities of Moxonidine. Approved, Investigational, Vet Approved Procarbazine Procarbazine may increase the hypotensive activities of Moxonidine. Approved, Investigational Promazine Promazine may decrease the vasoconstricting activities of Moxonidine. Approved, Vet Approved Propafenone Moxonidine may increase the atrioventricular blocking (AV block) activities of Propafenone. Approved Propericiazine Propericiazine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational Propiomazine Propiomazine may decrease the vasoconstricting activities of Moxonidine. Approved Propiverine Propiverine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational 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 Quinidine Quinidine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational Quinine Quinine may increase the hypotensive activities of Moxonidine. Approved Racepinephrine Racepinephrine may decrease the vasoconstricting 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, Investigational Rilmenidine Moxonidine may increase the hypotensive activities of Rilmenidine. Approved, 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 Silodosin Silodosin may decrease the vasoconstricting activities of Moxonidine. Approved Sitaxentan Moxonidine may increase the hypotensive activities of Sitaxentan. Approved, Investigational, Withdrawn Sotalol Moxonidine may increase the atrioventricular blocking (AV block) activities of Sotalol. Approved Spirapril Moxonidine may increase the hypotensive activities of Spirapril. Approved Spironolactone Spironolactone may decrease the vasoconstricting activities of Moxonidine. Approved Streptokinase The risk or severity of adverse effects can be increased when Moxonidine is combined with Streptokinase. Approved, Investigational 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 Terbutaline Moxonidine may increase the atrioventricular blocking (AV block) activities of Terbutaline. 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 Theophylline Theophylline may increase the antihypertensive activities of Moxonidine. Approved Thiamylal Thiamylal may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Thiopental Thiopental may increase the hypotensive activities of Moxonidine. Approved, Vet Approved Thioproperazine Thioproperazine may decrease the vasoconstricting activities of Moxonidine. Approved Thioridazine The risk or severity of adverse effects can be increased when Moxonidine is combined with Thioridazine. Approved, Withdrawn Tianeptine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Tianeptine. Approved, Investigational Tibolone Moxonidine may increase the hypotensive activities of Tibolone. Approved, Investigational 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, Investigational 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 Tranylcypromine Tranylcypromine may increase the hypotensive activities of Moxonidine. Approved, Investigational Travoprost Moxonidine may increase the hypotensive activities of Travoprost. Approved Trazodone Trazodone may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational 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 Trifluoperazine Trifluoperazine may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational Trimazosin Trimazosin may increase the hypotensive activities of Moxonidine. Experimental Trimethaphan Trimethaphan may increase the hypotensive activities of Moxonidine. Approved, Investigational 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, Investigational 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 increase the tachycardic 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, Investigational Yohimbine Yohimbine may decrease the antihypertensive activities of Moxonidine. Approved, Investigational, Vet Approved Ziprasidone Ziprasidone may decrease the vasoconstricting activities of Moxonidine. Approved Zofenopril Moxonidine may increase the hypotensive activities of Zofenopril. Experimental Zuclopenthixol Zuclopenthixol may decrease the vasoconstricting activities of Moxonidine. Approved, Investigational - 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]
- He MM, Abraham TL, Lindsay TJ, Schaefer HC, Pouliquen IJ, Payne C, Czeskis B, Shipley LA, Oliver SD, Mitchell MI: Metabolism and disposition of the antihypertensive agent moxonidine in humans. Drug Metab Dispos. 2003 Mar;31(3):334-42. [PubMed:12584161]
- Electronic Medicines Compedium Physiotens (Moxonidine) Monograph [Link]
- External Links
- Human Metabolome Database
- HMDB0041938
- 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 High Blood Pressure (Hypertension) 1 3 Terminated Prevention Cardiac Diseases / Vascular Surgery 1 4 Completed Treatment High Blood Pressure (Hypertension) / 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 High Blood Pressure (Hypertension) / Obesity, Abdominal 1 4 Unknown Status Treatment Schizophrenic Disorders 1 Not Available Active Not 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 July 02, 2018 19:13