Introduction. -The opium alkaloid noscapine (1) is widely used as cough depressant. Its antitussive effect is similar to that of codeine, while it does not show respiratory depression, constipation, and dependence liability. Recently, high-affinity binding sites were found for 1 in guinea-pig brain
Biphasic elimination of noscapine
β Scribed by Milo Gibaldi; Norman D. Weiner
- Publisher
- John Wiley and Sons
- Year
- 1966
- Tongue
- English
- Weight
- 303 KB
- Volume
- 55
- Category
- Article
- ISSN
- 0022-3549
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β¦ Synopsis
OSCAPINE, an isoquinoline alkaloid of opium, N is an antitussive agent which depresses the medullary centers and suppresses the cough reflex. Pharmacological and clinical investigations have confirmed the value of noscapine as a potent nonaddictive cough suppressant (I).
Despite the antiquity of this opium derivative, little is known concerning its absorption, distribution, and elimination in the body. In 1961, Vedso (2) studied the absorption and excretion of noscapine in man. More recently, Nayak et al.
(3) investigated the rate of metabolism, urinary excretion, and organ distribution of noscapine in
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Biologic dis osition studies of noscapine in the rabbit, rat, and mouse indicate a rapid rate o f biotransformation of this compound. When noscapine was administered intravenously to rabbits, it disappeared from the blood by first-order kinetics with a half-life of about 9 minutes. I n mice, the dru
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