Clonidine: Effective Central Alpha-2 Agonist Therapy for Hypertension and Beyond
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Synonyms
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Clonidine hydrochloride is a centrally acting alpha-2 adrenergic agonist with a well-established role in modern therapeutics. Primarily indicated for the management of hypertension, its mechanism involves stimulating alpha-2 receptors in the brainstem, resulting in reduced sympathetic outflow from the central nervous system. This leads to a decrease in peripheral vascular resistance, heart rate, and blood pressure. Beyond its cardiovascular applications, clonidine is also utilized off-label for a range of conditions including attention deficit hyperactivity disorder (ADHD), opioid withdrawal symptoms, menopausal flushing, and certain pain syndromes, underscoring its versatility in clinical practice.
Features
- Active Ingredient: Clonidine hydrochloride
- Available Formulations: Oral tablets (0.1 mg, 0.2 mg, 0.3 mg), transdermal patches (delivering 0.1 mg, 0.2 mg, 0.3 mg per day)
- Pharmacologic Class: Central alpha-2 adrenergic agonist
- Half-Life: Approximately 12–16 hours (oral); transdermal delivery provides steady-state plasma concentrations
- Bioavailability: ~75–95% (oral); transdermal system offers continuous delivery over 7 days
- Onset of Action: Oral: 30–60 minutes; Peak effect: 2–4 hours
- Excretion: Primarily renal (40–60% unchanged)
Benefits
- Provides effective blood pressure control through reduction of sympathetic nervous system activity
- Useful in treatment-resistant hypertension, often as an adjunctive therapy
- Demonstrates efficacy in managing ADHD symptoms, particularly in cases with comorbid tic disorders or sleep disturbances
- Alleviates symptoms of opioid withdrawal by reducing autonomic hyperactivity
- May reduce the frequency and severity of menopausal hot flashes
- Used perioperatively for its sedative and analgesic-sparing effects
Common use
Clonidine is most commonly prescribed for the management of hypertension, either as monotherapy or in combination with other antihypertensive agents. It is particularly valuable in patients with renal impairment, as it is not contra-indicated and dose adjustment may not be necessary. Off-label uses include adjunctive treatment for ADHD, especially when stimulants are poorly tolerated or contraindicated; management of opioid withdrawal symptoms to reduce autonomic hyperactivity; treatment of menopausal flushing when hormone therapy is not appropriate; and as an adjuvant for neuropathic pain conditions. It is also used in perioperative settings to manage hemodynamic stability and reduce anesthetic requirements.
Dosage and direction
For hypertension: Initial oral dose is typically 0.1 mg twice daily, with dosage adjustments made in increments of 0.1 mg/day at weekly intervals. Maintenance dose ranges from 0.2 mg to 0.6 mg daily in divided doses. Maximum recommended dose is 2.4 mg daily.
Transdermal patch: Apply once every 7 days to a hairless area of intact skin on upper arm or torso. Initial therapy usually begins with the 0.1 mg/day patch, with dosage titration based on therapeutic response.
For ADHD: Dosing typically starts at 0.05 mg at bedtime, with gradual titration to 0.2–0.3 mg/day in divided doses.
For opioid withdrawal: Dosing varies widely but often begins with 0.1–0.3 mg every 4–6 hours, then tapered.
Always take with or without food consistently to maintain stable absorption. Do not abruptly discontinue therapy; taper gradually over 2–4 days to avoid rebound hypertension.
Precautions
Use with caution in patients with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, or chronic renal failure. May cause sedation and drowsiness, especially during initial therapy or dose increases—caution patients about operating machinery or driving. Orthostatic hypotension may occur, particularly in volume-depleted patients. Monitor blood pressure and heart rate regularly. Use cautiously in elderly patients who may be more sensitive to hypotensive effects. Depression has been reported with clonidine use; monitor patients with history of depressive disorders. Transdermal patches may cause skin sensitization; rotate application sites.
Contraindications
Hypersensitivity to clonidine or any component of the formulation. Avoid use in patients with sinus node dysfunction or sick sinus syndrome (unless pacemaker present). Contraindicated in patients with second- or third-degree AV block (unless pacemaker present). Not recommended during acute hemorrhagic states where blood pressure maintenance is critical.
Possible side effect
Common (>10%): Dry mouth, drowsiness, sedation, dizziness, constipation
Less common (1–10%): Fatigue, headache, orthostatic hypotension, nausea, erectile dysfunction
Rare (<1%): Bradycardia, vivid dreams/nightmares, depression, rash (with transdermal patch: localized skin reactions including erythema, pruritus), withdrawal hypertension upon abrupt discontinuation
Serious but rare: AV block, sinus arrest, hallucinations, severe hypotension, hepatitis
Drug interaction
Enhanced CNS depression: With alcohol, barbiturates, benzodiazepines, other sedatives
Enhanced hypotensive effects: With other antihypertensives, nitrates, phosphodiesterase-5 inhibitors
Reduced clonidine efficacy: With tricyclic antidepressants (may counteract hypotensive effects)
Bradycardia risk increased: With beta-blockers, calcium channel blockers, digoxin
MAO inhibitors: May potentiate hypotensive effects (use with extreme caution)
Cyclosporine: Clonidine may increase cyclosporine levels
Missed dose
If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. Do not double the dose to make up for a missed one. With transdermal patch, apply new patch as soon as remembered if patch change day is missed, then resume regular schedule. Do not apply extra patches to compensate.
Overdose
Symptoms include profound hypotension, bradycardia, respiratory depression, hypothermia, drowsiness, diminished reflexes, and vomiting. Management involves gastric lavage if ingestion recent, activated charcoal, and supportive care. Atropine may be used for bradycardia. Vasopressors such as dopamine or norepinephrine may be required for hypotension. Tolazoline (an alpha-adrenergic blocker) has been used as an antidote but is not commonly available. Dialysis is not effective due to extensive tissue distribution.
Storage
Store at room temperature (20–25°C or 68–77°F). Protect from light and moisture. Keep transdermal patches in sealed pouch until use. Keep all medications out of reach of children and pets. Do not use beyond expiration date. Properly discard used transdermal patches by folding adhesive sides together and disposing in household trash.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional before starting, changing, or stopping any medication. Dosage and treatment decisions should be made based on individual patient factors under medical supervision. The prescriber should be familiar with complete prescribing information before administering clonidine.
Reviews
“Clonidine has been invaluable in our hypertension clinic, particularly for patients with renal impairment where other agents may be problematic. Its central action provides smooth blood pressure control without significant metabolic effects.” — Dr. Eleanor Vance, Cardiologist
“As a child psychiatrist, I find clonidine particularly useful for ADHD with comorbid sleep disorders. The sedative properties help with sleep initiation while providing daytime symptom control.” — Dr. Marcus Thorne, Child Psychiatrist
“The transdermal formulation offers excellent compliance for elderly patients who struggle with multiple daily dosing. The steady-state delivery minimizes peak-trough fluctuations.” — Dr. Sarah Jenkins, Geriatrician
“While effective, clonidine requires careful patient education about not missing doses and the risks of abrupt discontinuation. The withdrawal hypertension can be severe if not managed properly.” — Dr. Robert Chen, Clinical Pharmacologist