Reserpine is an oral antihypertensive medication that acts through inhibitor of alpha-adrenergic transmission and was one of the first antihypertensive agents introduced into clinical practice. Despite widescale use for many years, reserpine has not been shown to cause clinically apparent liver injury.
Reserpine (re ser' peen) was one of the first antihypertensive agents developed for use in humans. It is an alkaloid extract of the Rauwolifia serpentine (thus its name) which is a climbing shrub found in India. Reserpine is thought to act by binding to adrenergic storage vesicles in neurons, inhibiting their capacity to concentrate and store norepinephrine and dopamine. The antihypertensive effect of reserpine correlates with the depletion of sympathetic amines in both the central nervous system and periphery. Reserpine is effective in lowering blood pressure and can be used alone or in combination with other antihypertensive medications. Reserpine was approved for use in the United States in 1955 but is currently rarely used, largely because of its central nervous system effects and the availability of many better tolerated and more potent antihypertensive medications. Reserpine continues to be available in generic forms as tablets of 0.1 and 0.25 mg. The typical maintenance dose in adults is 0.05 to 0.25 mg once daily. Side effects are common and include sedation, difficulty concentrating, fatigue, depression, dry mouth, headaches, dizziness, postural hypotension, male impotence and gastrointestinal upset.
Serum aminotransferase elevations during reserpine therapy are uncommon, but specific rates of such elevations in comparison to placebo treatment have not been reported. Despite many decades of use, reserpine has been implicated in few instances of clinically apparent acute liver injury, and none of them were particularly convincing. Published cases were marked by jaundice and abdominal pain arising a year after starting reserpine, but in combination with other known hepatotoxic agents (dihydrazine, phenobarbital, quinidine). The few cases that have been reported were self-limiting and resolved within a few months of stopping therapy.
Mechanism of Injury
Reserpine is metabolized by the cytochrome P450 (CYP) system to a major degree but neither induces or inhibits CYP activity, which may account in part for its relative lack of hepatotoxicity.
Drug Class: Antihypertensive Agents
Reserpine – Generic
|DRUG||CAS REGISTRY NUMBER||MOLECULAR FORMULA||STRUCTURE|