Shire is developing propiram (Dirame, under license from Bayer), a non-addictive analgesic for the relief of moderate-to-severe pain. It is intended for the management of cancer pain, traumatic and post-surgical pain, and pain associated with dental surgery and childbirth [201830]. Propiram is effective for the treatment of mild-to-moderate pain and is more active than codeine, while showing no addictive potential. In July 2001, Shire confirmed that the product was undergoing phase III trials and anticipated launch in its first market to take place in 2003 [317541], [415823]. In June 2001, ABN AMRO predicted launch in 2003 with sales of $16 million in 2003 rising to $24 million in 2005 [422762].

01 Sep 1993·DrugsQ1 · MEDICINE

A Review of its Pharmacodynamic and Pharmacokinetic Properties, and Clinical Use as an Analgesic

Q1 · MEDICINE

Review

Author: Brogden, Rex N ; Goa, Karen L

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.

01 Jun 1988·NeuropharmacologyQ2 · MEDICINE

Partial agonists of the morphine type: Facilitative effects on electrophysiologically recorded C-fiber reflexes in the cat

Q2 · MEDICINE

Article

Author: H.E. Shannon ; J.A. Bell

The purpose of the present study was to examine the effects of the partial agonists of the morphine type, buprenorphine, profadol and propiram on the spinally-mediated C-fiber reflex. Buprenorphine, profadol and propiram facilitated the C-fiber reflex. In the presence of naltrexone, the effects of buprenorphine were changed to depression of the C-fiber reflex. Profadol and propiram continued to facilitate the C-fiber reflex in the presence of naltrexone. The present results suggest that buprenorphine facilitated the C-fiber reflex by blocking endogenous opioid peptide inhibition of the C-fiber reflex whereas profadol and propiram facilitated it by a non-opioid mechanism.

100 Deals associated with Propiram fumarate

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Musculoskeletal Pain	Phase 3	-	Shire Pharmaceuticals Services Ltd.	-
Musculoskeletal Pain	Phase 3	-	Bayer AG	-
Musculoskeletal Pain	Phase 3	GB	-	-
Musculoskeletal Pain	Phase 3	US	Shire Pharmaceuticals Group	-
Pain, Postoperative	Phase 3	-	Bayer AG	-
Pain, Postoperative	Phase 3	GB	-	-
Pain, Postoperative	Phase 3	-	Shire Pharmaceuticals Services Ltd.	-

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