Propiram. A review of its pharmacodynamic and pharmacokinetic properties, and clinical use as an analgesic.
Propiram is an orally administered opioid analgesic with partial morphine-like agonist and weak antagonist properties. Analgesic efficacy of propiram, usually 50 or 100mg, appears comparable to that of standard dosages of other oral opioid drugs [i.e. pentazocine, pethidine (meperidine)] in patients with acute pain of moderate to severe intensity arising from various gynaecological and surgical procedures, and may be superior to codeine in gynaecological and postoperative dental pain. Some evidence of a more rapid onset of action for propiram than for these opioid agents, and a longer duration of action for propiram than for codeine, is encouraging but remains to be substantiated in more extensive clinical use. The tolerability profile of propiram resembles those of others in its class, with drowsiness, nausea and vomiting, and dizziness experienced most frequently in controlled trials. The apparently low propensity of propiram for development of physical dependence and psychotomimetic effects requires confirmation with wider clinical experience. Available data thus indicate that propiram is an effective, orally administered opioid analgesic suitable for providing relief of acute moderate to severe pain arising from various surgical or gynaecological procedures, and that the drug is likely to become a useful alternative in such conditions where opioid analgesia is appropriate.
Goa
Karen L
KL
Adis International Limited, Private Bag 65901, 41 Centorian Drive, Mairangi Bay, Auckland 10, New Zealand.
Brogden
Rex N
RN
Adis International Limited, Private Bag 65901, 41 Centorian Drive, Mairangi Bay, Auckland 10, New Zealand.
D000284:Administration, Oral; D000700:Analgesics / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D002986:Clinical Trials as Topic; D004361:Drug Tolerance; D006801:Humans; D007408:Intestinal Absorption; D010146:Pain / Q000188:drug therapy*; D011597:Psychomotor Performance / Q000187:drug effects; D011725:Pyridines / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use*; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism; D012119:Respiration / Q000187:drug effects; D014018:Tissue Distribution
D000700:Analgesics; D011725:Pyridines; D011957:Receptors, Opioid; C002107:propiram