Proglumide

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Proglumide
Systematic (IUPAC) name
4-(benzoylamino)-5-(dipropylamino)-5-oxopentanoic acid
Identifiers
CAS number 6620-60-6
ATC code ?
PubChem 4922
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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Routes ?

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Proglumide (Milid) is a drug which inhibits gastrointestinal motility and reduces gastric secretions.

Proglumide acts as a cholecystokinin antagonist.[1] It was used mainly in the treatment of stomach ulcers,[2][3] 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,[4] and can prevent or even reverse the development of tolerance to opioid drugs.[5][6] 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.[7][8]



See also

References

  1. 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 Acadamy of Sciences. 1985;448:345-51.
  2. 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.
  3. 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.
  4. McCleane GJ. The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine. Clinical Journal of Pain. 2003 May-Jun;19(3):200-1.
  5. 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.
  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.
  7. 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.
  8. 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.

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