Clonidine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO HTN Initial: 50-100 mcg tid, increased every 2nd or 3rd day. Maintenance: 300-1,200 mcg/day, some may require ≥1,800 mcg/day. Max: 2,400 mcg/day. Menopausal flushing; Migraine prophylaxis 50 mcg bid, increased to 75 mcg bid if no remission after 2 wk. IV Hypertensive crisis 150-300 mcg may repeat up to max of 750 mcg over 24 hr. Transdermal HTN As patch releasing 100-300 mcg/24 hr: Apply a patch once wkly. Epidural Severe cancer pain Initial: 30 mcg/hr, in combination w/ an opioid.
Dosage Details
Epidural
Severe cancer pain
Adult: Initially, 30 mcg/hr as a continuous infusion in combination w/ an opioid, adjust according to response.

Intravenous
Hypertensive crisis
Adult: 150-300 mcg given by slow inj over 10-15 min, may be repeated up to max of 750 mcg over a 24 hr period.

Oral
Hypertension
Adult: Initially, 50-100 mcg tid, increased every 2nd or 3rd day according to response. Maintenance: 300-1,200 mcg daily, some may require ≥1,800 mcg daily. Max: 2,400 mcg daily.

Oral
Menopausal flushing, Prophylaxis of migraine
Adult: 50 mcg bid, increased to 75 mcg bid if no remission after 2 wk.

Transdermal
Hypertension
Adult: As patch releasing 100-300 mcg/24 hr: Apply a patch once wkly.
Renal Impairment
Dosage adjustment needed.
Administration
May be taken with or without food.
Contraindications
Severe bradyarrhythmia secondary to 2nd- or 3rd-degree AV block or sick sinus syndrome.
Special Precautions
Patient w/ cerebrovascular disease, ischaemic heart disease including MI, occlusive peripheral vascular disorders (e.g. Raynaud's disease), or those w/ history of depression. Avoid abrupt withdrawal. Renal impairment. Pregnancy and lactation.
Adverse Reactions
Headache, dizziness, drowsiness, dry mouth, constipation, depression, anxiety, nausea, fatigue, anorexia, parotid pain, paraesthesia, delusional perception, sleep disturbances, vivid dreams, impotence and loss of libido, urinary retention or incontinence, orthostatic hypotension, itching or burning sensations in the eye, accommodation disorder, decreased lacrimation, fluid retention, pruritus and rashes (transdermal), bradycardia (including sinus bradycardia w/ AV block), other ECG disturbances, heart failure, hallucinations, cramp, Raynaud's syndrome, gynaecomastia, transient abnormalities in LFTs.
Epidural/IV/Parenteral/PO/Transdermal: C
Patient Counseling Information
May impair ability to drive or operate machinery. May cause dryness of eyes in patients who wear contact lenses.
MonitoringParameters
Monitor BP (standing and sitting/supine), mental status, heart rate.
Overdosage
Symptoms: Lethargy, pupillary constriction, hypotension, hypothermia, bradycardia, decreased or absent reflexes, irritability, miosis, weakness, somnolence (including coma) and resp depression (including apnoea). Paradoxical HTN may occur. Management: Perform gastric lavage following recent ingestion or admin activated charcoal and/or a cathartic. Supportive treatment may include admin of atropine sulfate for symptomatic bradycardia; IV fluids and/or inotropic sympathomimetic agents for hypotension; vasodilators for HTN. Naloxone may be used as adjunct for clonidine-induced resp depression, hypotension and/or coma.
Drug Interactions
Increased hypotensive effect w/ other antihypertensives e.g. diuretics, β-blockers, vasodilators, Ca antagonists, ACE inhibitors. Reduced antihypertensive effect and induced orthostatic hypotension w/ TCAs or neuroleptics w/ α-receptor blocking properties. Reduced therapeutic effect w/ NSAIDs. Potentiation of bradycardic rhythm disturbances w/ a substances w/ negative chronotropic or dromotropic effect (e.g. β-blocker, digitalis glycosides. May potentiate CNS depressant effect of barbiturates or other sedating drugs. May prolong the duration of pharmacologic effect of epidural local anaesth (epidural).
Food Interaction
May potentiate CNS depressant effect of alcohol.
Action
Description: Clonidine stimulates α2-adrenoceptors in the brain stem which results in reduced sympathetic outflow from the CNS, and a decrease in peripheral resistance, heart rate, BP and renal vascular resistance.
Onset: 0.5-1 hr (oral); 2-3 days (transdermal).
Duration: 6-10 hr (oral).
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Absorbed through the skin (transdermal). Bioavailability: 70-80% (oral); approx 60% (transdermal). Time to peak plasma concentration: Approx 3-5 hr (oral).
Distribution: It crosses the placenta; enters breast milk. Volume of distribution: 2.9 L/kg. Plasma protein binding: Approx 20-40%.
Metabolism: Hepatically metabolised (approx 50%); undergoes enterohepatic recirculation.
Excretion: Via urine, as unchanged drug (40-60%) and metabolites; faeces (approx 20%). Elimination half-life: 6-24 hr.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store between 20-25°C.
ATC Classification
S01EA04 - clonidine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma.
N02CX02 - clonidine ; Belongs to the class of other antimigraine preparations.
C02AC01 - clonidine ; Belongs to the class of imidazoline receptor agonists, centrally-acting antiadrenergic agents. Used in the treatment of hypertension.
Disclaimer: This information is independently developed by MIMS based on Clonidine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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