Detail of "42408-82-2"

Reference

Progress report on studies from the clinical pharmacology section of the Addiction Research Center

Progress report on studies from the clinical pharmacology section of the Addiction Research Center. Jasinski, Donald R.; Pevnick, Jeffrey S.; Griffith, John D.; Gorodetzky, Charles W.; Cone, Edward J. (Addict. Res. Cent., Natl. Inst. Drug Abuse, Lexington, Ky., USA). Probl. Drug Depend., 112-48 (English) 1976. CODEN: PDDEDE. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In human subjects made dependent to butorphanol [42408-82-2], a withdrawal syndrome was produced which more closely resembled cyclazocine abstinence than morphine abstinence. In nontolerant, nondependent subjects, orally administered oxilorphan [42281-59-4] was 1 to 1/2 times as potent as s.c. administered oxilorphan in its pharmacol. effects, and its onset of action was slower. In another study, oxilorpham (0.6 mg/700 kg, s.c.) given 4 and 12 h before morphine sulfate (25 mg/70 kg) clearly blocked its miotic effects and its subjective effects. In human subjects, Wy-16225 [57236-36-9] was identified predominantly as an opiate, produced an atypical pattern of opiate-like symptoms and signs, and produced dose-related increases on the various scales measuring morphine-like effects. In human subjects, both phentermine [122-09-8] and L-ephedrine [299-42-3] produced typical amphetaminelike subjective and physiol. effects. In normal subjects, buprenorphine (I) [52485-79-7] was a morphinelike agent which may be a partial agonist, was relatively nontoxic during chronic administration, had an extremely long duration of action, and effectively blocked the effects of morphine during chronic administration. I also had a lesser abuse potential than methadone. Thus, I may have utility as a maintenance drug in the treatment of narcotic addicts. After oral administration of 3 doses, propoxyphene-HCl [1639-60-7] was somewhat more rapidly absorbed than propoxyphene napsylate [26570-10-5], giving greater propoxyphene concns. in blood in the 1st 2 h after drug administration and showing peak mean levels at 2 h compared to 3 h for the napsylate. Peak norpropoxyphene [42576-07-8] levels were 10-75% greater than propoxyphene levels after propoxyphene administration and occurred 2-6 h later. Very small amts. of dinorpropoxyphene [42576-07-8] were found. During chronic administration of propoxyphene napsylate in one morphine-dependent subject, propoxyphene-levels in plasma reached approx. const. values of 800-1,000 ng/mL after 7 days. Norpropoxyphene plasma levels increased rapidly during propoxyphene administration for 2 weeks, then leveled off, whereas dinorpropoxyphene levels increased gradually and continuously during the entire 3 weeks of propoxyphene administration. Following abrupt withdrawal, propoxyphene was detectable in the plasma for 8 days, whereas the 2 metabolites were detected on the 10th day after withdrawal.

Annual report of the analgesic studies section of the Memorial Sloan-Kettering Cancer Center

Annual report of the analgesic studies section of the Memorial Sloan-Kettering Cancer Center. Houde, R. W.; Wallenstein, S. L.; Rogers, A.; Kaiko, R. F. (Mem. Sloan-Kettering Cancer Cent., New York, N. Y., USA). Probl. Drug Depend., 149-68 (English) 1976. CODEN: PDDEDE. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Butorphanol [42408-82-2] and butorphanol tartrate [61005-22-9] (given i.m.) were 4.95 and 3.39 times more potent as analgesics than morphine sulfate in patients. The side effects obsd. with butorphanol were, in addn. to the morphine side effects, sweating, feelings of weakness, floating feelings, and psychotomimetic reactions (the last symptom was obsd. at higher butorphanol concns.). Nalbuphine [20594-83-6] (givn i.m.) was about 3 times more potent as an analgesic than pentazocine, though at equianalgesic doses, it appeared to have a much lower peak effect and a longer duration of action. Both drugs produced morphine-like side effects, but pentazocine produced a greater no. of psychotomimetic reactions. SU-19713B [64401-24-7] given orally was 0.95 times as potent as codeine at releiving pain, and the time effect curves were similar. Sleepiness was the main side effect obsd. after both drugs. Propiram fumarate [13717-04-9] (given orally) was about 0.08 times as potent as morphine sulfate (given i.m.). The time effect curves for oral propiram and i.m. morphine sulfate were quite similar. Tilidine [20380-58-9] (given orally) was 0.07 times as potent as morphine sulfate as an analgesic. Side effects for both drugs were similar. Buprenorphine-HCl [53152-21-9] (i.m.) was 25 times more potent than morphine sulfate (i.m.) in patients with pain. Side effects for both drugs were similar. The analgesic activities of SP 106 (benzopyronopyridine) [49637-08-3] and codeine (given orally) were compared.