Drug intelligence / Profile preview

rauwolfia

Development stage
Phase 3
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Rauwolfia refers to medicinal preparations derived from the dried rhizome and roots of *Rauwolfia serpentina*, a plant in the Apocynaceae family commonly known as Indian snakeroot. The therapeutic activity of the drug is attributed to its complex mixture of indole alkaloids, most notably reserpine, ajmaline, ajmalicine, deserpidine, and rescinnamine. Its primary mechanism of action involves the irreversible inhibition of the vesicular monoamine transporters (VMAT1 and VMAT2), which prevents the storage of monoamine neurotransmitters such as norepinephrine, serotonin, and dopamine in synaptic vesicles. This leads to the depletion of these neurotransmitters from both peripheral and central axon terminals, resulting in a reduction in sympathetic tone and peripheral vascular resistance. Historically, rauwolfia was a staple in the treatment of hypertension and was one of the first effective antipsychotics used for mental disorders like schizophrenia. However, its clinical use has significantly declined in modern medicine due to a high incidence of side effects, including severe depression, sedation, and bradycardia. It remains recognized by the German Commission E for the treatment of hypertension and insomnia.

Brand names
SerpinaRaudixinRauvalWolfina
Other names
Rauwolfia serpentinaIndian snakerootSarpagandha
02

Targets

VMAT1 (Vesicular monoamine transporter type 1)VMAT2 (Vesicular monoamine transporter 2)

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