Clonidine: Effective Central Alpha-2 Agonist for Hypertension & ADHD
Clonidine
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Synonyms
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Clonidine hydrochloride is a centrally acting alpha-2 adrenergic agonist, representing a cornerstone therapeutic agent in the management of hypertension and attention-deficit/hyperactivity disorder (ADHD). Its unique mechanism of action, modulating sympathetic outflow from the central nervous system, provides a distinct pharmacological profile. This comprehensive product card details its specifications, clinical applications, and essential safety information for healthcare professionals.
Features
- Active Ingredient: Clonidine Hydrochloride
- Pharmacologic Class: Central Alpha-2 Adrenergic Agonist
- Available Formulations: Oral tablets (0.1 mg, 0.2 mg, 0.3 mg), transdermal patches (releasing 0.1 mg, 0.2 mg, 0.3 mg per 24 hours)
- Bioavailability: Approximately 75–95% (oral)
- Protein Binding: 20–40%
- Metabolism: Hepatic (50% via CYP2D6, remainder via other pathways)
- Half-Life: 12–16 hours (range 6–23 hours)
- Excretion: Primarily renal (40–60% as unchanged drug)
Benefits
- Provides reliable blood pressure control through central sympathetic inhibition
- Offers an alternative or adjunctive treatment option for patients with resistant hypertension
- Demonstrates efficacy in managing ADHD symptoms, particularly in combination therapies
- Available in transdermal formulation for improved compliance and steady-state delivery
- Useful in managing opioid withdrawal symptoms and reducing perioperative sympathetic response
- May reduce hot flashes in menopausal women and treat Tourette syndrome tics
Common use
Clonidine is FDA-approved for the treatment of hypertension. It is used both as monotherapy and in combination with other antihypertensive agents, particularly diuretics. Its off-label uses are extensive and evidence-supported, including the management of ADHD in children and adults, often as an adjunct to stimulants or for patients who cannot tolerate them. It is also employed in symptom management during opioid and alcohol withdrawal, for reducing menopausal hot flashes, and as a preventive treatment for migraine headaches. In perioperative settings, it is used to attenuate hemodynamic responses to intubation and surgical stress.
Dosage and direction
Hypertension (Adults): Initial dose: 0.1 mg orally twice daily. Maintenance dose: May be increased by 0.1 mg/day at weekly intervals. Usual range: 0.2–0.6 mg/day in divided doses. Maximum dose: 2.4 mg/day.
ADHD (Children >6 years and Adults): Initial dose: 0.05 mg at bedtime. May increase by 0.05 mg/day every 3–7 days. Typical maintenance: 0.1–0.3 mg/day divided BID or TID, or given at bedtime.
Transdermal Patch: Apply once every 7 days to a hairless area of intact skin on upper arm or torso. Start with 0.1 mg/24 hr system. Dosage may be adjusted after 1–2 weeks.
Dosage must be individualized. Renal impairment requires dosage adjustment. Abrupt discontinuation must be avoided due to rebound hypertension risk.
Precautions
Monitor blood pressure and heart rate regularly, especially during initiation and titration. Use with caution in patients with severe coronary insufficiency, recent myocardial infarction, cerebrovascular disease, or chronic renal failure. May cause sedation; advise patients regarding operating machinery or driving. Dry mouth and constipation are common; recommend symptomatic management. Orthostatic hypotension may occur; advise patients to rise slowly from sitting/lying positions. Periodic eye examinations recommended with long-term use (rare reports of retinopathy).
Contraindications
Hypersensitivity to clonidine or any component of the formulation. Do not use in patients with sinus node dysfunction or sick sinus syndrome (unless pacemaker present). Contraindicated in advanced heart block (second or third degree). Not recommended during pregnancy unless potential benefit justifies potential risk to fetus.
Possible side effect
Common (>10%): Dry mouth, drowsiness, sedation, dizziness, constipation. Less common (1–10%): Fatigue, headache, hypotension, nausea, erectile dysfunction. Rare (<1%): Bradycardia, vivid dreams/nightmares, depression, rash, urticaria, alopecia, hyperglycemia, congestive heart failure, AV block. Transdermal-specific: Skin reactions (erythema, pruritus, contact dermatitis) at application site.
Drug interaction
Enhanced CNS depression: With alcohol, barbiturates, benzodiazepines, other sedatives. Enhanced bradycardia/AV block: With beta-blockers, digoxin, calcium channel blockers. Hypotensive effects potentiated: By other antihypertensives, nitrates, phosphodiesterase-5 inhibitors. Tricyclic antidepressants may antagonize antihypertensive effect. Cytochrome interactions: Moderate CYP2D6 inhibitor; may increase levels of substrates like metoprolol, desipramine.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next dose, the missed dose should be skipped. Doubling up on doses is not recommended due to the risk of excessive hypotension and bradycardia. For the transdermal patch, if detachment occurs, a new patch may be applied to a different skin site.
Overdose
Manifests as profound hypotension, bradycardia, respiratory depression, hypothermia, drowsiness, diminished reflexes, and vomiting. Management is supportive: ensure airway patency, administer IV fluids for hypotension. Atropine may be used for bradycardia. Vasopressors like dopamine or norepinephrine may be required for refractory hypotension. Tolazoline has been used as an antidote but is not commonly available; naloxone is ineffective.
Storage
Store at controlled room temperature (20–25°C or 68–77°F). Protect from light and moisture. Keep oral tablets in their original container, tightly closed. Transdermal patches should remain in their sealed pouch until use. Keep out of reach of children and pets.
Disclaimer
This information is intended for healthcare professionals and is not a substitute for clinical judgment. Prescribing decisions should be based on the individual patient’s condition, contraindications, and the most current prescribing information. The prescriber should be familiar with the complete product labeling.
Reviews
“Clonidine remains a valuable agent in our antihypertensive arsenal, particularly for patients with sympathetic overactivity. Its transdermal formulation significantly improves adherence in our non-compliant population.” – Cardiologist, 15 years experience
“As an adjunctive therapy for ADHD, clonidine has transformed our approach to patients with comorbid tics or sleep disturbances. The evening dosing significantly improves sleep onset.” – Child Psychiatrist, 10 years experience
“The ability to modulate sympathetic outflow makes clonidine indispensable in our pain management and addiction medicine protocols, especially for opioid withdrawal symptom control.” – Anesthesiologist/Pain Specialist, 12 years experience