Proglumide

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Proglumide
200px
Systematic (IUPAC) name
(RS)-N2-benzoyl-N,N-dipropyl-α-glutamine
Clinical data
Routes of
administration		 Oral
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Biological half-life ~24 hours
Identifiers
CAS Number 6620-60-6
ATC code A02BX06 (WHO)
PubChem CID 4922
IUPHAR/BPS 893
Synonyms 4-benzamido-5-(dipropylamino)-5-oxopentanoic acid
Chemical data
Formula C18H26N2O4
Molar mass 334.41 g/mol[[Script error: No such module "String".]]
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Proglumide (Milid) is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist,[1] which blocks both the CCKA and CCKB 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]

Proglumide also works as a placebo effect amplifier for pain conditions. When injected visibly to a subject, its analgesic effect is bigger than a similarly administered placebo. When injected secretly, it does not have any effect, whereas standard pain drugs have an effect, even if they are administered without the subject's awareness [11]. The supposed mechanism is an enhancement of the neural pathways of expectation.

See also

References

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  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 Academy of Sciences. 1985;448:345-51.
  2. ↑ 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
  3. ↑ 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.
  4. ↑ 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.
  5. ↑ McCleane GJ. The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine. Clinical Journal of Pain. 2003 May-Jun;19(3):200-1.
  6. ↑ 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.
  7. ↑ 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.
  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.
  9. ↑ 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.
  10. ↑ Rezvani A, Stokes KB, Rhoads DL, Way EL. Proglumide exhibits delta opioid agonist properties. Alcohol and Drug Research. 1987;7(3):135-46.
  11. ↑ Benedetti F, Amanzio M, Maggi G Potentiation of placebo analgesia by proglumide. Lancet. 1995 Nov 4;346(8984):1231.
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