indication

Foe the treatment of hypertension

pharmacology

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.

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.

toxicity

Possible human carcinogen. May cause reproductive harm. ORL-RAT LD₅₀ 420 mg/kg; IPR-RAT LD₅₀ 44 mg/kg; IVN-RAT LD₅₀ 15 mg/kg; ORL-MUS LD₅₀ 200 mg/kg; SCU-MUS LD₅₀ 52 mg/kg; IPR-RBT LD₅₀ 7 mg/kg

route of elimination

Reserpine is extensively metabolized to inactive compounds. It is slowly excreted via the urine and feces.

drug interactions

Dobutamine: Increased arterial pressure

Dopamine: Increased arterial pressure

Ephedra: Increased arterial pressure

Ephedrine: Increased arterial pressure

Epinephrine: Increased arterial pressure

Fenoterol: Increased arterial pressure

Isoproterenol: Increased arterial pressure

Mephentermine: Increased arterial pressure

Metaraminol: Increased arterial pressure

Methoxamine: Increased arterial pressure

Norepinephrine: Increased arterial pressure

Orciprenaline: Increased arterial pressure

Phenylephrine: Increased arterial pressure

Phenylpropanolamine: Increased arterial pressure

Pirbuterol: Increased arterial pressure

Procaterol: Increased arterial pressure

Pseudoephedrine: Increased arterial pressure

Salbutamol: Increased arterial pressure

Terbutaline: Increased arterial pressure

Tetrabenazine: Reserpine may increase the adverse/toxic effects of Tetrabenazine. Concomitant therapy is contraindicated.

Topotecan: The p-glycoprotein inhibitor, Reserpine, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.

Tranylcypromine: Addition of Reserpine to Tranylcypromine therapy may induce paradoxical Reserpine effects, including peripheral hypertension and central exciation. Close monitoring for adverse effects is required. Addition of Tranylcypromine to Reserpine therapy may be less of a concern.

Treprostinil: Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Triprolidine: The CNS depressants, Triprolidine and Reserpine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.