Ballicules.com

Mecamylamine

INVERSINE

Mecamylamine ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Mecamylamine ballicule

What it isGanglionic nicotinic antagonist; historical antihypertensive, studied in smoking cessation.

Why this oneIt is one of the few centrally acting nicotinic antagonists, which is why it was revisited for addiction.

What limits itBlocking both autonomic limbs causes constipation, retention and orthostasis. Largely obsolete.

Mecamylamine molecular structure (skeletal formula)
Molecular structure: Mecamylamine

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Hypertension (moderately severe to severe essential; uncomplicated malignant)Adult2.5 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

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Pregnancy Category C; use only if clearly needed.

Lactation Undefined

Cost

Mecamylamine (INVERSINE)
Strength#/mogeneric $/moCostPlus
2.5 mgtab60 BIDnot 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.

NO BOXED WARNINGS

Principal riskBlocking both autonomic limbs causes constipation, retention and orthostasis

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger3 / 4
Weight-gain liability0 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4

Legacy pregnancy categoryC

Defining liabilitySevere orthostatic hypotension, ileus and CNS toxicity

Open Mecamylamine in the interactive console ↗