Proglumid

Proglumid
Klinički podaci
Način primeneOralno
Pravni status
Pravni status
  • ℞ (Prescription only)
Identifikatori
CAS broj6620-60-6 Зелена квачицаДа
ATC kodA02BX06 (WHO)
PubChemCID 4922
IUPHAR/BPS893
ChEMBLCHEMBL316561 Зелена квачицаДа
Sinonimi4-benzamido-5-(dipropilamino)-5-oksopentanoidna kiselina

Proglumid (Milid) je lek koji inhibira gastrointestinalnu motilnost i redukuje želudačnu sekreciju. On deluje kao holecistokininski antagonist,[1] koji blokira oba tipa receptora, CCKA i CCKB.[2] On se uglavnom koristi za lečenje čireva na dvanaestopalačnom crevu,[3][4] mada je u znatnoj meri bio zamenjen novijim lekovima za tu namenu.

Interesantna nuspojava proglumida je da uvećava analgeziju proizvedenu opioidnim lekovima,[5] i da može da spreči ili čak preokrene razvoj tolerancije na opioidne lekove.[6][7] To ga čini korisnim pomoćnim tretmanom za upotrebu zajedno sa opioidnim lekovima u lečenju hroničnih bolnih oboljenja kao što je rak, gde opioidni analgetici mogu da budu neophodni tokom dužih perioda, i razvoj tolerancije redukuje kliničku efikasnost tih lekova.[8][9]

Za proglumid je takođe bilo pokazano da deluje kao δ-opioidni agonist, što može da doprinese njegovom analgetskom dejstvu.[10]

Vidi još

Reference

  1. ^ Bunney, B. S.; Chiodo, L. A.; Freeman, A. S. (1985). „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. 448: 345—51. 
  2. ^ González-Puga, C.; García-Navarro, A.; Escames, G.; León, J.; López-Cantarero, M.; Ros, E.; Acuña-Castroviejo, D. (2005). „Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: Synergism with pharmacological levels of melatonin”. Journal of Pineal Research. 16150104 (3): 243—250. PMID 16150104. S2CID 20187767. doi:10.1111/j.1600-079X.2005.00239.x. 
  3. ^ Bergemann W, Consentius K, Braun HE, Hirschmann H, Marowski B, Munck A, Rehs HU, Stopik D, Wilke G. (април 1981). „Duodenal ulcer - multicenter double-blind study with proglumide”. Medizinische Klinik. 76 (8): 226—9. 
  4. ^ Tariq, M.; Parmar, N. S.; Ageel, A. M. (мај 1987). „Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats”. Journal of Pharmacology and Experimental Therapeutics. 241 (2): 602—7. 
  5. ^ McCleane, G. J. (2003 May-Jun). „The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine”. Clinical Journal of Pain. 19 (3): 200—1.  Проверите вредност парамет(а)ра за датум: |date= (помоћ)
  6. ^ Watkins, L. R.; Kinscheck, I. B.; Mayer, D. J. (април 1984). „Potentiation of opiate analgesia and apparent reversal of morphine tolerance by proglumide”. Science. 224 (4647): 395—6. 
  7. ^ Tang J, Chou J, Iadarola M, Yang HY, Costa E (јун 1984). „Proglumide prevents and curtails acute tolerance to morphine in rats”. Neuropharmacology. 23 (6): 715—8. 
  8. ^ Bernstein, Z. P.; Yucht, S; Battista, E.; Lema, M; Spaulding, M. B. (мај 1998). „Proglumide as a morphine adjunct in cancer pain management”. Journal of Pain and Symptom Management. 15 (5): 314—20. .
  9. ^ McCleane, G. J. (новембар 1998). „The cholecystokinin antagonist proglumide enhances the analgesic efficacy of morphine in humans with chronic benign pain.”. Anesthesia and Analgesia. 87 (5): 1117—20. 
  10. ^ Rezvani A, Stokes KB, Rhoads DL, Way EL (1987). „Proglumide exhibits delta opioid agonist properties”. Alcohol and Drug Research. 7 (3): 135—46. 

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