Drug intelligence / Profile preview

papaverine

Development stage
Phase 4
Lead developer
Phebra
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Rectal, Intracavernosal
01

Overview

Papaverine is an opium alkaloid antispasmodic drug primarily used to treat visceral spasms and vasospasms, including those involving the intestines, heart, or brain. It is also occasionally used in the treatment of erectile dysfunction and acute mesenteric ischemia. Unlike other opium alkaloids such as morphine, papaverine does not have analgesic properties and differs structurally and pharmacologically from them. Its main mechanism of action involves direct smooth muscle relaxation by inhibiting phosphodiesterases (notably cAMP and cGMP phosphodiesterase), leading to increased intracellular levels of cAMP and cGMP, which results in vasodilation. Papaverine may also inhibit calcium ion channels in smooth muscle cells. It is approved for use as a vasodilator to improve blood flow in conditions associated with poor circulation or vascular spasm.[1][2][3][5][6]. Recent research has shown that papaverine can act as a radiosensitizer for hypoxic tumors by inhibiting mitochondrial complex I[8].

Brand names
Pavabid
Other names
papaverine hydrochloride
02

Targets

ND1 (Mitochondrial electron transport chain complex I)PDE10A (Phosphodiesterase 10A)CaV (Voltage-gated calcium channel protein complex)

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