Proglumide
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Proglumide
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| Systematic (IUPAC) name | |
| 4-(benzoylamino)-5-(dipropylamino)-5-oxopentanoic acid | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C18H26N2O4 |
| Mol. mass | 334.41 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Proglumide (Milid) is a drug which inhibits gastrointestinal motility and reduces gastric secretions.
Proglumide acts as a cholecystokinin antagonist,[1] which blocks both the CCK-A and CCK-B subtypes.[2] It was used mainly in the treatment of stomach ulcers,[3][4] although it has now been largely replaced by newer drugs for this application.
An interesting side effect of proglumide is that it enhances the analgesia produced by opioid drugs,[5] and can prevent or even reverse the development of tolerance to opioid drugs.[6][7] This can make it a useful adjuvant treatment to use alongside opioid drugs in the treatment of chronic pain conditions such as cancer, where opioid analgesics may be required for long periods and development of tolerance reduces clinical efficacy of these drugs.[8][9]
Proglumide has also been shown to act as a δ-opioid agonist, which may contribute to its analgesic effects.[10]
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[edit] See also
[edit] References
- ^ Bunney BS, Chiodo LA, Freeman AS. Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system. Annals of the New York Academy of Sciences. 1985;448:345-51.
- ^ González-Puga C, García-Navarro A, Escames G, León J, López-Cantarero M, Ros E, Acuña-Castroviejo D. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. Journal of Pineal Research. 2005 Oct;39(3):243-50. PMID 16150104
- ^ Bergemann W, Consentius K, Braun HE, Hirschmann H, Marowski B, Munck A, Rehs HU, Stopik D, Wilke G. Duodenal ulcer - multicenter double-blind study with proglumide. (German) Medizinische Klinik. 1981 Apr 10;76(8):226-9.
- ^ Tariq M, Parmar NS, Ageel AM. Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats. Journal of Pharmacology and Experimental Therapeutics. 1987 May;241(2):602-7.
- ^ McCleane GJ. The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine. Clinical Journal of Pain. 2003 May-Jun;19(3):200-1.
- ^ Watkins LR, Kinscheck IB, Mayer DJ. Potentiation of opiate analgesia and apparent reversal of morphine tolerance by proglumide. Science. 1984 Apr 27;224(4647):395-6.
- ^ Tang J, Chou J, Iadarola M, Yang HY, Costa E. Proglumide prevents and curtails acute tolerance to morphine in rats. Neuropharmacology. 1984 Jun;23(6):715-8.
- ^ Bernstein ZP, Yucht S, Battista E, Lema M, Spaulding MB. Proglumide as a morphine adjunct in cancer pain management. Journal of Pain and Symptom Management. 1998 May;15(5):314-20.
- ^ McCleane GJ. The cholecystokinin antagonist proglumide enhances the analgesic efficacy of morphine in humans with chronic benign pain. Anesthesia and Analgesia. 1998 Nov;87(5):1117-20.
- ^ Rezvani A, Stokes KB, Rhoads DL, Way EL. Proglumide exhibits delta opioid agonist properties. Alcohol and Drug Research. 1987;7(3):135-46.
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