Clonidine

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Catapresan, Isoglaucon; Belgium: Catapressan, Dixarit; Bulgaria: Chlophazolin; Czech Republic: Aruclonin; Denmark: Catapresan; Finland: Catapresan; France: Catapressan; Germany: Catapresan, Clonid-Ophtal, Clonidin, Clonistada, Haemiton, Isoglaucon, Paracefan; Greece: Catapres, Catapresan; Ireland: Catapres, Clonidine, Dixarit; Italy: Catapresan, Isoglaucon; Latvia: Chlophazolin; Luxembourg: Catapressan, Dixarit; Malta: Catapress; Netherlands: Catapresan, Clonidine; Poland: Catapresan, Iporel; Portugal: Catapresan, Edolglau; Romania: Clonidina; Slovakia: Aruclonin; Spain: Catapresan; Sweden: Catapresan; UK: Catapres, Clonidine, Dixarit.

North America

Canada: Catapres, Clonidine, Dixarit; USA: Catapres, Clonidine, Duraclon, Jenloga.

Latin America

Argentina: Clonidina; Brazil: Atensina, Clonidin; Mexico: Catapresan, Clonidina, Epiclodina.

Asia

Japan: Catapres.

Drug combinations

Clonidine and Chlorthalidone

Chemistry

Clonidine Hydrochloride: C~9~H~9~Cl~2~N~3~ HCl. Mw: 266.55. (1) Benzenamine, 2,6-dichloro-N-2-imidazolidinylidene-, monohydrochloride; (2) 2-[(2,6-Dichlorophenyl)imino]imidazolidine monohydrochloride. CAS-4205-91-8; CAS-4205-90-7 (clonidine)(1969).

Pharmacologic Category

Sympathomimetic (Adrenergic) Agents; α-Adrenergic Agonists. Hypotensive Agents; Central α-Agonists. (ATC-Code: C02AC01; N02CX02; S01EA04).

Mechanism of action

Stimulates α~2~-adrenoceptors in the brain stem, thus activating an inhibitory neuron, resulting in reduced sympathetic outflow from the CNS, producing a decrease in peripheral resistance, renal vascular resistance, heart rate, and blood pressure. Epidural clonidine may produce pain relief by acting at spinal presynaptic and postjunctional α~2~-adrenoceptors and preventing pain signal transmission.

Therapeutic use

Mild-to-moderate hypertension. Diagnosis of pheochromocytoma and growth hormone deficiency.

Pregnancy and lactiation implications

Clonidine crosses the placenta. Potential of rebound hypertension with abrupt discontinuation (use with caution). Not recommended during lactation.

Unlabeled use

Heroin or nicotine withdrawal. Severe pain. Dysmenorrhea. Vasomotor symptoms associated with menopause. Ethanol dependence. Prophylaxis of migraines. Glaucoma. Diabetes-associated diarrhea. Impulse control disorder, attention-deficit hyperactivity disorder, clozapine-induced sialorrhea.

Contraindications

Hypersensitivity to clonidine or any component. Epidural injection is contraindicated in patients receiving anticoagulation therapy and in bleeding diathesis or an infection at the injection site. Administration of epidural clonidine above the C~4~ dermatome.

Warnings and precautions

May cause significant CNS depression, and significant xerostomia. Use with caution in the following situations: severe coronary insufficiency, including recent myocardial infarction and conduction disturbances (including sinus node dysfunction), cerebrovascular disease, chronic renal impairment, and in the elderly (higher risk for CNS depressive effects). Epidural clonidine is not recommended for perioperative, obstetrical, or postpartum pain. The epidural route may lead to cardiovascular instability (hypotension, bradycardia). Should be administered via a continuous epidural infusion device. May contain conducting metal (e.g. aluminum). Gradual withdrawal is needed if drug needs to be stopped.

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