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QuickView for Clonidine (compound)

Name: Clonidine
PubChem Compound ID: 20179
Description: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
Molecular formula: C9H10Cl3N3
Molecular weight: 266.554 g/mol
2-((2,6-Dichlorophenyl)imino)imidazolidine monohydrochloride; Benzenamine, 2,6-dichloro-N-2-imidazolidinylidene-, hydrochloride; Catapres (TN); 57665-50-6; Clonidine hydrochloride; Catapresan; 2-Imidazoline, 2-(2,6-dichloroanilino)-, monohydrochloride; 1H-Imidazol-2-amine, N-(2,6-dichlorophenyl)-4,5-dihydro-, monohydrochloride (9CI); Dixarit; Capresin.
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Name: Clonidine
Name (isomeric): DB00575
Drug Type: small molecule
Description: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
ST 155BS; Clonidin; Clonidinum [INN-Latin]; Clonidinhydrochlorid; Clonidine HCl; Chlornidinum
Brand: Catapressan, Clonistada, Tenso-Timelets, Duraclont, Ipotensium, Catapres, Catapres-TTS, Duraclon, Adesipress, Dixarit, Catarpresan, Isoglaucon, Catarpres, Catapresan
Brand name mixture: Combipres 0.1/15 Tab(Chlorthalidone + Clonidine Hydrochloride)
Category: Central Alpha-Agonists, Sympatholytics, Adrenergic alpha-Agonists, Analgesics, Antihypertensive Agents
CAS number: 4205-90-7
Indication: May be used as an adjunct in the treatment of hypertension, as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone, for differential diagnosis of pheochromocytoma in hypertensive patients, prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD).
Clonidine is an α-adrenergic agent that acts specifically on α2-receptors. α2-receptors regulate a number of signaling pathways mediated by multiple Gi proteins, Gαi1, Gαi2, and G&alphai3. Stimulation of α2-receptors mediates effects suc...
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Mechanism of Action: See Pharmacology section above.
Absorption: Well absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.
Protein binding: 20-40%, primarily to albumin
Biotransformation: Hepatic. Metabolized via minor pathways. The major metabolite, p-hydroxyclonidine, is present in concentrations less than 10% of those of unchanged clonidine in urine. Four metabolites have been detected, but only p-hydroxyclonidine has been identified.
Half Life: 6-20 hours; 40-60% is excreted in urine unchanged, 20% is excreted in feces. Less than 10% is excreted by p-hydroxyclonidine.
Toxicity: Oral LD50 is 150 mg/kg in rat and 30 mg/kg in dog. Symptoms of overdose include constriction of pupils of the eye, drowsiness, high blood pressure followed by a drop in pressure, irritability, low body temperature, slowed breathing, slowed heartbeat, slowed reflexes, and weakness.
Affected organisms: Humans and other mammals
Food interaction:
Avoid alcohol.
Take without regard to meals.
Drug interaction:
ImipramineThe tricyclic antidepressant, imipramine, decreases the effect of clonidine.
BevantololIncreased hypertension when clonidine stopped
EsmololIncreased hypertension when clonidine stopped
PractololIncreased hypertension when clonidine stopped
DesipramineThe tricyclic antidepressant, desipramine, decreases the effect of clonidine.
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