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Inversine (Mecamylamine Hydrochloride) - Description and Clinical Pharmacology

 
 



DESCRIPTION

INVERSINE® (Mecamylamine HCl) is a potent, oral antihypertension agent and ganglion blocker, and is a secondary amine. It is N,2,3,3-tetramethyl-bicyclo [2.2.1] heptan- 2 -amine hydrochloride. Its empirical formula is C11H21N • HCl and its structural formula is:

It is a white, odorless, or practically odorless, crystalline powder, is highly stable, soluble in water and has a molecular weight of 203.75.

INVERSINE is supplied as tablets for oral use, each containing 2.5 mg mecamylamine HCl. Inactive ingredients are acacia, calcium phosphate, D&C Yellow 10, FD&C Yellow 6, lactose, magnesium stearate, starch, and talc.

CLINICAL PHARMACOLOGY

Mecamylamine reduces blood pressure in both normotensive and hypertensive individuals. It has a gradual onset of action (1/2 to 2 hours) and a longlasting effect (usually 6 to 12 hours or more). A small oral dosage often produces a smooth and predictable reduction of blood pressure. Although this antihypertensive effect is predominantly orthostatic, the supine blood pressure is also significantly reduced.

Pharmacokinetics and Metabolism

Mecamylamine is almost completely absorbed from the gastrointestinal tract, resulting in consistent lowering of blood pressure in most patients with hypertensive cardiovascular disease. Mecamylamine is excreted slowly in the urine in the unchanged form. The rate of its renal elimination is influenced markedly by urinary pH. Alkalinization of the urine reduces, and acidification promotes, renal excretion of mecamylamine.

Mecamylamine crosses the blood-brain and placental barriers.

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