clonidine CATAPRES
Class: Alpha 2 Adrenergic Agonist/Aryl-2-aminoimidazolineFDA Indications: Hypertension
Off-Label Use: ADHD, ODD, Conduct Disorder, Tourette's Disorder, Opioid Withdrawal, Nicotine Withdrawal, Glaucoma, Alcohol Withdrawal (in Conjunction With Benzodiazepines), Migraines, Pheochromocytoma, PTSD, Anxiety
Prescribing
Forms: 0.1, 0.2, 0.3mg tablet; 0.1, 0.2mg extended-release tablets (Kapvay)Dose Range: 0.05-0.4 mg/day
Starting: for ADHD, 0.1 mg qhs, can ↑ by 0.1mg/day each week with dosing divided (larger dose @hs); max dose generally 0.4mg/day
Stopping: Discontinuation should be done incrementally over ≥ 2-4 days, as discontinuation symptoms are common and can be severe (for example, rapid rise in blood pressure, rare hypertensive encephalopathy, rare cerebrovascular accident, and rare death)
Precautions
Contraindications: Caution w/ concomitantly use with agents known to affect sinus node function or AV nodal conduction, e.g., digitalis, calcium channel blockers and beta-blockersSerious Side Effects: Hypotension, syncope, ↓ HR, AV block, angioedema, depression
Side Effects: sedation/somnolence, dizziness, headache, weakness/asthenia, xerostomia
Pharmacodynamics
1° MOA: Nonselective α2-adrenergic receptor agonism—its action at α2A enhances PFC functioning → strengthens working memory, ↓ susceptibility to distraction, ↑ attention, ↑ behavioral inhibition, & ↑ impulse controlTarget: α2A, α2B, α2C, I1, α1 (mild)
Pharmacokinetics
t½: 12.7 (6-20)° TMAX: 1-3°Substrate of: 1A2, 2D6, 3A4
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - can potentiate the action of, other CNS depressants, such as opiates or other analgesics, barbiturates or other sedatives, anesthetics, or alcohol
Misc
- - sedation is common and may be intolerable for many patients
- - ↓ autonomic symptoms of opioid withdrawal, i.e. sweating, diarrhea, cramping nausea, anxiety & irritability (BUT NOT AS EFFECTIVE in treating myalgia, restlessness, insomnia and cravings)
- - remember, if using in setting of alcohol or benzodiazepine withdrawal, clonidine may decrease vital signs and tremor but will not prevent seizures (like beta-blockers, they can 'mask' autonomic signs of withdrawal w/o addressing seizure risk)
Special Populations
Category C—Limited Human Data—Animal Data Suggest Risk
Limited Human Data—Probably Compatible
Prescribe with caution d/t ↑ risk of adverse CNS effects; may cause bradycardia and orthostatic hypotension; generally not recommended
Patients with renal impairment may require a reduced dose of clonidine
No dosage adjustment necessary
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