RESERPINE 0.25MG TABLET

Indications

• Hypertension
• Mild to moderate hypertension

Dosage

Children: Refer to BNF for Children for specific dosing guidelines.

Adults: Refer to BNF for specific dosing guidelines.

Mechanism of action

Reserpine's mechanism of action involves the inhibition of the ATP/Mg2+ pump that is responsible for sequestering neurotransmitters into storage vesicles within presynaptic neurons. This results in a depletion of catecholamines, such as norepinephrine, dopamine, and serotonin, leading to reduced sympathetic nervous system activity. The antihypertensive effects arise from adrenergic neuronal blockade due to the depletion of catecholamine-containing granules in postganglionic sympathetic neurons. Central effects, including changes in serotonin levels, contribute to its overall therapeutic profile.

Pharmacodynamics

Reserpine functions as an adrenergic blocking agent, effectively managing hypertension by disrupting the storage of norepinephrine in vesicles. The depletion of catecholamines from sympathetic nerve endings diminishes their physiological effects, lowering blood pressure by reducing cardiac output and peripheral vascular resistance. Reserpine also raises serum prolactin levels by blocking the release of prolactin-inhibiting factor, which can have implications in certain clinical conditions.

Pharmacokinetics

Reserpine is absorbed from the gastrointestinal tract and has a long duration of action. It is metabolized in the liver and has a relatively low bioavailability due to extensive first-pass metabolism. The elimination half-life varies but is generally prolonged, allowing for once-daily dosing in many cases. The drug's effects may persist even after discontinuation due to its action on neurotransmitter depletion.

Contra-indications

• Severe depression
• Peptic ulcer disease
• History of hypersensitivity to reserpine

Adverse effects

• Sedation
• Drowsiness
• Depression
• Nasal congestion
• Diarrhea
• Abdominal cramps
• Bradycardia
• Hypotension

Interactions

• Monoamine oxidase inhibitors (MAOIs) - may enhance effects leading to severe hypotension
• Tricyclic antidepressants - may reduce the antihypertensive effect of reserpine
• Digoxin - may increase the risk of bradycardia
• Antihypertensive agents - additive effect leading to hypotension

Precautions

• Use with caution in patients with a history of mental illness
• Monitor blood pressure regularly
• Use with caution in patients with renal impairment
• Avoid abrupt withdrawal to prevent rebound hypertension

Pregnancy

Use in pregnancy only if the potential benefit justifies the potential risk to the fetus. Category C.

Breast-feeding

Not recommended during breastfeeding due to potential effects on the neonate.

Storage

Store in a tightly closed container at room temperature, away from light and moisture.

Formulations

• Tablets

Mechanism of action

Reserpine's mechanism of action is through inhibition of the ATP/Mg²⁺ pump responsible for the sequestering of neurotransmitters into storage vesicles located in the presynaptic neuron. The neurotransmitters that are not sequestered in the storage vesicle are readily metabolized by monoamine oxidase (MAO) causing a reduction in catecholamines. ... DEPLETES OR RELEASES SEROTONIN (5-HYDROXYTRYPTAMINE), DOPAMINE ... NOREPINEPHRINE FROM ... BRAIN & ... BODY ... DEFICIENCY OF DOPAMINE IN BRAIN ... IN STRIATUM, SUBSTANTIA NIGRA ... PALLIDUM. ... HYPOTHERMIC EFFECT ... RELATED TO SEROTONIN DEPLETION OF HYPOTHALAMIC REGION. HYPOTHALMUS CONTAINS ... HIGHEST CONCN OF SEROTONIN. ... ANTIHYPERTENSIVE ACTION ... DERIVES FROM ADRENERGIC NEURONAL BLOCKADE CONSEQUENT TO DEPLETION OF CATECHOLAMINE-CONTAINING GRANULES OF POSTGANGLIONIC SYMPATHETIC NEURON. MECHANISM OF CENTRAL EFFECTS IS UNKNOWN. IT DEPLETES BOTH BRAIN SEROTONIN & CATECHOLAMINES. ... REPORTED TO INHIBIT GROWTH OF LEUKEMIA IN L1210 CELLS IN MALE MICE ... AND TO SUPPRESS GROWTH OF SARCOMA 37 IN MICE. ... RESERPINE DID NOT AFFECT GROWTH OF TRANSPLANTED MAMMARY ADENOCARCINOMAS IN C3H MICE. IT BLOCKS RELEASE OF PROLACTIN-INHIBITING FACTOR & THUS RAISES SERUM PROLACTIN LEVELS. Peripheral-Acting Adrenergic Antagonist /from table/ For more Mechanism of Action (Complete) data for RESERPINE (8 total), please visit the HSDB record page.

Pharmacodynamics

Reserpine is an adrenergic blocking agent used to treat mild to moderate hypertension via the disruption of norepinephrine vesicular storage. The antihypertensive actions of Reserpine are a result of its ability to deplete catecholamines from peripheral sympathetic nerve endings. These substances are normally involved in controlling heart rate, force of cardiac contraction and peripheral resistance.