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Information about Clonidine

Clonidine is a centrally active alpha-adrenergic agonist used predominantly as an antihypertensive agent, usually in combination with other agents.


Liver safety of Clonidine

Despite wide scale use for many years, clonidine has not been linked definitively to either serum aminotransferase elevations or clinically apparent liver injury.

Mechanism of action of Clonidine

Clonidine (klon' i deen) is an antihypertensive agent which acts by stimulation of the alpha 2A subtype of alpha adrenergic receptors in the brainstem, causing a reduction in the sympathic outflow of the central nervous system. Decreases in plasma levels of norepinephrine correlate closely with its antihypertensive effects. Clonidine is effective in lowering blood pressure and can be used alone or in combination with other antihypertensive medications. Clonidine is also used in several other conditions in which central nervous system sympathetic activity is believed to contribute including neuropathy, smoking and alcohol cessation, attention deficit disorder, vascular headache, menopausal symptoms, diabetic diarrhea, and restless leg syndrome.

FDA approval information for Clonidine

Clonidine was approved for use in the United States in 1974 and continues to be widely used with more than 11 million prescriptions being filled yearly. Current approved indications are for treatment of hypertension, but some preparations are also approved for cancer pain management and treatment of attention deficit disorder. Off label uses include treatment of Tourette syndrome, migraine headahces, stress and sleep disorders, and to alleviate symptoms of alcohol, nicotine or narcotic withdrawal.

Dosage and administration for Clonidine

Clonidine is available in tablets of 0.1, 0.2 and 0.3 mg generically and under the brand name of Catapres. Clonidine is also available in fixed combination with diuretics, as a solution for injection and in a transdermal formulation for application once weekly. The typical maintenance dose of clonidine in adults is 0.1 to 0.6 mg daily in 2 to 3 divided doses. Side effects are usually mild and include sedation, fatigue, bradycardia, dry mouth, headaches, dizziness, postural hypotension, male impotence and gastrointestinal upset. Sudden withdrawal can cause rebound hypertension.

Antihypertensive agents

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