Clonidine

Indications
 Oral
Hypertension
Adult: Initially, 50-100 mcg tid. As modified-release preparation: 50-100 mcg once or twice daily. Max: 2400 mcg daily.
Child: 2-18 yr: Initially 0.5-1 mcg/kg tid, increase gradually if necessary. Max: 25 mcg/kg daily in divided doses (not exceeding 1.2 mg daily).
Renal impairment: Supplemental doses after haemodialysis are not necessary.
CrCl (ml/min)Dosage Recommendation
<1050-75% of usual dose.

Oral
Prophylaxis of migraine
Adult: 50 mcg bid increased to 75 mcg bid if no remission after 2 wk.
Renal impairment: Supplemental doses after haemodialysis are not necessary.
CrCl (ml/min)Dosage Recommendation
<1050-75% of usual dose

Oral
Menopausal flushing
Adult: 50 mcg bid increased to 75 mcg bid if no remission after 2 wk.
Renal impairment: Supplemental doses after haemodialysis are not necessary.
CrCl (ml/min)Dosage Recommendation
<1050-75% of usual dose

Transdermal
Hypertension
Adult: Apply a patch once wkly, delivering 100-300 mcg of clonidine base daily at a constant rate.
Renal impairment: Supplemental doses after haemodialysis are not necessary.
CrCl (ml/min)Dosage Recommendation
<1050-75% of usual dose.

Intravenous
Hypertensive crisis
Adult: 150-300 mcg by slow inj over 10-15 min. Max: 750 mcg over 24 hr.
Child: 2-18 yr: 2-6 mcg/kg as a single dose. Max: 300 mcg.
Renal impairment: Supplemental doses after haemodialysis are not necessary.
CrCl (ml/min)Dosage Recommendation
<1050-75% of usual dose.

Epidural
Severe cancer pain
Adult: Initially, 30 mcg/hr as continuous infusion in combination with an opioid, adjusted according to patient's response.
Contraindications
 Hypersensitivity. Disorders of cardiac pacemaker activity and conduction. Pregnancy and lactation.
Warnings / Precautions
 Withdraw gradually, renal impairment, tasks that require mental alertness. Cerebrovascular disease, ischaemic heart disease, MI. IV inj should be administered slowly. Occlusive peripheral vascular disorders, history of depression.
Adverse Reactions
 Dry mouth, drowsiness, dizziness, headache, constipation, impotence, vivid dreams, urinary retention; dry, itching, burning sensation in the eye; fluid or electrolyte imbalance, GI upset, paralytic ileus, orthostatic hypotension, weakness, sedation, pruritus, myalgia, urticaria, nausea, insomnia, arrhythmias, agitation. Reduced GI motility at times may cause paralytic ileus.
Potentially Fatal: Transient hypertension or profound hypotension, respiratory depression, convulsion. Clonidine withdrawal syndrome could be life threatening. Bradycardia, coma and disturbances in conduction (in individuals with preexisting diseases of SA/AV nodes, overdose or on digitalis).
Overdose Reactions
 Symptoms include profound hypotension, transient hypertension, weakness, vomiting, irritability, diminished or absent reflexes, tiredness, somnolence, drowsiness, deep sedation, irritability, skin pallor, hypothermia, decreased or irregular heart rate, dry mouth, constricted pupils with poor reaction to light, respiratory depression, hypoventilation, dysrhythmias, apnoea, coma, and seizures. May be treated by gastric lavage using activated charcoal and/or cathartic agents. Treatment is usually supportive and symptomatic, with an adequate airway established and maintained since respiratory depression or apnoea may follow. Supportive care may include atropine sulfate for bradycardia, IV fluids and/or vasopressor agents for hypotension, and vasodilators (IV furosemide, diazoxide or phentolamine) for hypertension. Naloxone may be useful for the management of respiratory depression, hypotension, and/or coma. Monitor BP for paradoxical hypertension. Seizures may be controlled with IV benzodiazepine (e.g. diazepam). Haemodialysis is of limited value as only 5% of circulating drug is removed.
Drug Interactions
 Hypotensive action may be potentiated by diuretics and vasodilators. Effects of clonidine antagonised by TCAs and centrally-acting alpha-blockers. May enhance toxicity due to digitalis, lithium. May antagonise oral hypoglycaemics.
Potentially Fatal: Hypnosedatives, antihistamines and alcohol may cause excessive drowsiness in patients on clonidine. Withdrawal of clonidine in patients receiving noncardioselective β-blockers may result in rebound BP. Acute severe hypotension following concomitant administration of clonidine and chlorpromazine or haloperidol.
See Below for More clonidine Drug Interactions
Lab Interactions
 Transient abnormalities in liver function tests.
Mechanism of Actions
 Clonidine stimulates alpha-2 receptors in brain stem which results in reduced sympathetic outflow from the CNS and a decrease in peripheral resistance leading to reduced BP and pulse rate. It does not alter normal haemodynamic response to exercise at recommended dosages.
Onset: 2-3 days (transdermal).
Duration: Maintained for 8 hr after removal of system (transdermal).
Absorption: Well absorbed from the GI tract (oral); peak plasma concentrations after 3-5 hr. Absorbed from the skin (transdermal).
Distribution: 20-40% protein bound.
Metabolism: Hepatic: 50% of the dose.
Excretion: Via urine within 24 hr (as 40-60% as unchanged drug), via faeces (20% of the dose); 6-24 hr (elimination half-life), prolonged to 41 hr in renal impairment.
Administration
 May be taken with or without food.
Storage Conditions
 Epidural: Store below 30°C. Intravenous: Store below 30°C. Oral: Store below 30°C. Transdermal: Store below 30°C.
ATC Classification
 C02AC01 - clonidine ; Belongs to the class of imidazoline receptor agonists, centrally-acting antiadrenergic agents. Used in the treatment of hypertension.
N02CX02 - clonidine ; Belongs to the class of other antimigraine preparations.
S01EA04 - clonidine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma.
Storage
 Epidural: Store below 30°C. Intravenous: Store below 30°C. Oral: Store below 30°C. Transdermal: Store below 30°C.
Available As
  • Clonidine 100 mcg
  • Clonidine 150 mcg

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