ベジトラミド

DEA NFLIS-Drug Category -> Narcotic Analgesics

DEA Schedule II Controlled Substance -> Opiates

Pharmaceuticals -> Listed in ZINC15

Pharmaceuticals -> Synthetic Cannabinoids or Psychoactive Compounds

N - Nervous system

QN - Nervous system

Bezitramide acts in the body to relieve pain with a potency 20 times that of methadone. Its duration of action is relatively long, lasting up to 12 hours post oral administration, after the achievement of steady state. Its onset of action is slow, with a peak in analgesic effect noted between 2.5-3.5 hours after dosing. It is noted to illicit a strong antitussive effect, which could be of benefit to patients with bronchial carcinoma.

Bezitramide is a prodrug which undergoes rapid hydrolysis of a proprionyl-group to form the major metabolite, R-4618. R-4618 has analgesic properties similar to the parent compound. Metabolism occurs in the gastrointestinal tract under both acidic and alkaline conditions.

Bezitramide has poor water solubility, thus administration is restricted to the oral route.

Less than 0.3% of the dose was excreted unchanged in the urine. High concentrations in feces suggested incomplete absorption of biliary excretion. Experiments in rats demonstrated extensive (up to 70%) biliary excretion, and less than 3% urinary excretion.