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Home / Drugs / Starting with C / Clonidine
 
Clonidine
 

Clonidine, an imidazoline-derivative hypotensive agent is a centrally-acting α2-adrenergic agonist. It crosses the blood-brain barrier and acts in the hypothalamus to induce a decrease in blood pressure. It may also be administered as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone. Clonidine may be used for differential diagnosis of pheochromocytoma in hypertensive patients. Other uses for clonidine include 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 also exhibits some peripheral activity.
BrandsAdesipress
Catapres
Catapres-TTS
Catapresan
Catapressan
Catarpres
Catarpresan
Clonistada
Dixarit
Duraclon
Duraclont
Ipotensium
Isoglaucon
Tenso-Timelets
CategoriesAntihypertensive Agents
Analgesics
Sympatholytics
Adrenergic alpha-Agonists
Central Alpha-Agonists
ManufacturersBoehringer ingelheim
Aveva drug delivery systems inc
Mylan technologies inc
Tris pharma inc
Pharmaforce inc
Bioniche pharma usa llc
Actavis elizabeth llc
American therapeutics inc
Dava pharmaceuticals inc
Duramed pharmaceuticals inc sub barr laboratories inc
Impax laboratories inc
Interpharm inc
Mutual pharmaceutical co inc
Mylan pharmaceuticals inc
Par pharmaceutical inc
Sandoz inc
Teva pharmaceuticals usa inc
Unichem laboratories ltd
Vintage pharmaceuticals llc
Warner chilcott div warner lambert co
Watson laboratories inc
Shionogi pharma inc
PackagersAAIPharma Inc.
Actavis Group
Advanced Pharmaceutical Services Inc.
Alza Corp.
American Regent
Amerisource Health Services Corp.
Apotheca Inc.
APP Pharmaceuticals
A-S Medication Solutions LLC
Bioniche Pharma
Blenheim Pharmacal
Boehringer Ingelheim Ltd.
Bryant Ranch Prepack
Cardinal Health
Central Texas Community Health Centers
Comprehensive Consultant Services Inc.
Coupler Enterprises Inc.
DAVA Pharmaceuticals
Dept Health Central Pharmacy
Direct Dispensing Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Global Pharmaceuticals
Heartland Repack Services LLC
Innoviant Pharmacy Inc.
Lake Erie Medical and Surgical Supply
Liberty Pharmaceuticals
Major Pharmaceuticals
Mckesson Corp.
Medisca Inc.
Murfreesboro Pharmaceutical Nursing Supply
Mutual Pharmaceutical Co.
Mylan
Neighborcare Repackaging Inc.
Neuman Distributors Inc.
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
Par Pharmaceuticals
PCA LLC
PD-Rx Pharmaceuticals Inc.
Pharmaceutical Utilization Management Program VA Inc.
Pharmaforce Inc.
Pharmedix
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Qualitest
Rebel Distributors Corp.
Redpharm Drug
Remedy Repack
Richmond Pharmacy
Sandhills Packaging Inc.
Southwood Pharmaceuticals
Stat Rx Usa
Tya Pharmaceuticals
UDL Laboratories
Unichem Laboratories Ltd.
United Research Laboratories Inc.
Vangard Labs Inc.
Vintage Pharmaceuticals Inc.
West-Ward Pharmaceuticals
Xanodyne Pharmaceuticals Inc.
SynonymsChlornidinum
Clonidin
Clonidine HCl
Clonidinhydrochlorid
Clonidinum [INN-Latin]
ST 155BS

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).

pharmacology

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 such as inhibition of adenylyl cyclase, stimulation fo phospholipase D, stimulation of mitogen-activated protein kinases, stimulation of K+ currents and inhibition of Ca2+ currents. Three G-protein coupled α2-receptor subtypes have been identified: α2A, α2B, and α2C. Each subtype has a unique pattern of tissue distribution in the central nervous system and peripheral tissues. The α2A-receptor is widely distributed throughout the central nervous system; it is found in the locus coeruleus, brain stem nuclei, cerebral cortex, septum, hypothalamus, and hippocampus. α2A-receptors are also expressed in the kidneys, spleen, thymus, lung and salivary glands. The α2C-receptor is primarily expressed in the central nervous system, including the striatum, olfactory tubercle, hippocampus and cerebral cortex. Low levels of the α2C-subtype are also found in the kidneys. The α2B-receptor is located primarily in the periphery (kidney, liver, lung and heart) with low levels of expression in the thalamic nuclei of the central nervous system. The α2A- and α2C-receptors are located presynaptically and inhibit the released of noradrenaline from sympathetic nerves. Stimulation of these receptors decreases sympathetic tone, resulting in decreases in blood pressure and heart rate. Sedation and analgesia is mediated by centrally located α2A-receptors, while peripheral α2B-receptors mediate constriction of vascular smooth muscle. α2A-Receptors also mediate essential components of the analgesic effect of nitrous oxide in the spinal cord. Clonidine stimulates all three α2-receptor subtypes with similar potency. Its actions in the nervous system decreases blood pressure in patients with hypertension and decreases sympathetic overactivity in patients undergoing opioid withdrawal. Clonidine is also a potent sedative and analgesic and can prevent post-operative shivering in intensive and post-operative care. Its use in differential diagnosis of pheochromocytoma owes to the fact that hypertension in patients with pheochromocytoma is refractory to antihypertensive treatment with clonidine.

mechanism of action

See Pharmacology section above.

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.

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.

absorption

Well absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.

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.

drug interactions

Acebutolol: Increased hypertension when clonidine stopped

Amitriptyline: The tricyclic antidepressant, amitriptyline, decreases the effect of clonidine.

Amoxapine: The tricyclic antidepressant, amoxapine, decreases the effect of clonidine.

Atenolol: Increased hypertension when clonidine stopped

Betaxolol: Increased hypertension when clonidine stopped

Bevantolol: Increased hypertension when clonidine stopped

Bisoprolol: Increased hypertension when clonidine stopped

Carteolol: Increased hypertension when clonidine stopped

Carvedilol: Increased hypertension when clonidine stopped

Clomipramine: The tricyclic antidepressant, clomipramine, may decrease the effect of clonidine.

Desipramine: The tricyclic antidepressant, desipramine, decreases the effect of clonidine.

Doxepin: The tricyclic antidepressant, doxepin, decreases the effect of clonidine.

Esmolol: Increased hypertension when clonidine stopped

Imipramine: The tricyclic antidepressant, imipramine, decreases the effect of clonidine.

Labetalol: Increased hypertension when clonidine stopped

Metoprolol: Increased hypertension when clonidine stopped

Mirtazapine: Possible hypertensive crisis

Nadolol: Increased hypertension when clonidine stopped

Nortriptyline: The tricyclic antidepressant, nortriptyline, decreases the effect of clonidine.

Oxprenolol: Increased hypertension when clonidine stopped

Penbutolol: Increased hypertension when clonidine stopped

Pindolol: Increased hypertension when clonidine stopped

Practolol: Increased hypertension when clonidine stopped

Propranolol: Increased hypertension when clonidine stopped

Protriptyline: The tricyclic antidepressant, protriptyline, decreases the effect of clonidine.

Sotalol: Increased hypertension when clonidine stopped

Timolol: Increased hypertension when clonidine stopped

Treprostinil: Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Trimipramine: Trimipramine may reduce the antihypertensive effect of the alpha2-agonist, Clonidine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Clonidine should be withdrawn very gradually to reduce the risk of hypertensive crisis.