Ballicules › Drugs › Mecamylamine
Mechanism of action: Mecamylamine ballicule
What it is Ganglionic nicotinic antagonist; historical antihypertensive, studied in smoking cessation.
Why this one It is one of the few centrally acting nicotinic antagonists, which is why it was revisited for addiction.
What limits it Blocking both autonomic limbs causes constipation, retention and orthostasis. Largely obsolete.
Molecular structure: Mecamylamine
FDA-approved for
hypertension (historical) (1956)
FDA label
Read the full label on DailyMed ↗
FDA dosing Population Start Target Max
Hypertension (moderately severe to severe essential; uncomplicated malignant) Adult 2.5 mg BID ~25 mg/day in ~3 divided doses
Titration Increase by 2.5 mg increments at intervals of not less than 2 days until desired response.
Renal Contraindicated in uremia; give with great discretion, if at all, when renal insufficiency is manifested by rising/elevated BUN.
Hepatic Undefined
Instructions Give after meals for more gradual absorption; keep timing relative to meals consistent. Give the larger dose at noon (and perhaps evening); morning dose small or omitted. Reduce dose of concomitant antihypertensives to avoid excessive hypotension (continue thiazides at usual dose).
Available strengths
Contraindications Mild, moderate, or labile hypertension; uncooperative patients. Coronary insufficiency or recent myocardial infarction. Uremia. Concurrent antibiotics or sulfonamides (with ganglion blockers). Glaucoma; organic pyloric stenosis.
Cautions Orthostatic/postural hypotension and syncope. Paralytic ileus (may be preceded by small, frequent liquid stools). CNS effects: convulsions, tremor, choreiform movements, mental aberrations, paresthesias.
Adverse reactions ileus/constipation nausea, vomiting, anorexia orthostatic dizziness/syncope, postural hypotension dry mouth, glossitis urinary retention, impotence, decreased libido blurred vision, dilated pupils weakness, fatigue, sedation
Pregnancy Pregnancy Category C; use only if clearly needed.
Lactation Undefined
Cost Mecamylamine (INVERSINE)
Strength #/mo generic $/mo CostPlus 2.5 mg tab 60 BID not offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Mecamylamine is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.
Principal risk Blocking both autonomic limbs causes constipation, retention and orthostasis
Classes and tags
Clinical profile
Therapeutic safety burden 2 / 4
Overdose danger 3 / 4
Weight-gain liability 0 / 4
Sedation liability 2 / 4
QT / Torsades 0 / 4
Direct muscarinic antagonism 0 / 4
Legacy pregnancy category C
Defining liability Severe orthostatic hypotension, ileus and CNS toxicity
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