Mecamylamine reduces blood pressure in both normotensive and hypertensive individuals. It has a gradual onset of action ( ¹ / ₂ to 2 hours) and a long-lasting 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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