| Indication | For the treatment of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension |
| Pharmacodynamics | Mecamylamine is a potent, oral antihypertensive agent and ganglion blocker, and is a secondary amine. Mecamylamine is indicated for the management of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension. Mecamylamine reduces blood pressure in both normotensive and hypertensive individuals. 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. Mecamylamine crosses the blood-brain and placental barriers. |
| Mechanism of action | Mecamylamine is a ganglionic blocker which prevents stimulation of postsynaptic receptors by acetylcholine released from presynaptic nerve endings. The hypotensive effect of Mecamylamine is attributed to reduction in sympathetic tone, vasodilation, and reduced cardiac output, and is primarily postural. |
| Absorption | Mecamylamine is almost completely absorbed from the gastrointestinal tract |
| Volume of distribution | Not Available |
| Protein binding | 40% |
| Metabolism | Not Available |
| Route of elimination | 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. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Not Available |