Proglumid

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Proglumid
(IUPAC) ime
(RS)-N2-benzoyl-N,N-dipropyl-α-glutamine
Klinički podaci
Identifikatori
CAS broj 6620-60-6
ATC kod A02BX06
PubChem[1][2] 4922
ChEMBL[3] CHEMBL316561 YesY
Hemijski podaci
Formula C18H26N2O4 
Mol. masa 334.41 g/mol
SMILES eMolekuli & PubHem
Sinonimi 4-benzamido-5-(dipropilamino)-5-oksopentanoidna kiselina
Farmakokinetički podaci
Poluvreme eliminacije ~24 sata
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Prescription only
Način primene Oralno

Proglumid (Milid) je lek koji inhibira gastrointestinalnu motilnost i redukuje želudačnu sekreciju. On deluje kao holecistokininski antagonist,[4] koji blokira oba tipa receptora, CCKA i CCKB.[5] On se uglavnom koristi za lečenje čireva na dvanaestopalačnom crevu,[6][7] mada je u znatnoj meri bio zamenjen novijim lekovima za tu namenu.

Interesantna nuspojava proglumida je da uvećava analgeziju proizvedenu opioidnim lekovima,[8] i da može da spreči ili čak preokrene razvoj tolerancije na opioidne lekove.[9][10] 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.[11][12]

Za proglumid je takođe bilo pokazano da deluje kao δ-opioidni agonist, što može da doprinese njegovom analgetskom dejstvu.[13]

Vidi još[uredi - уреди | uredi izvor]

Literatura[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. 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.
  5. 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. DOI 10.1111/j.1600-079X.2005.00239.x PMID 16150104
  6. 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.
  7. 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.
  8. McCleane GJ. The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine. Clinical Journal of Pain. 2003 May-Jun;19(3):200-1.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. Rezvani A, Stokes KB, Rhoads DL, Way EL. Proglumide exhibits delta opioid agonist properties. Alcohol and Drug Research. 1987;7(3):135-46.

Spoljašnje veze[uredi - уреди | uredi izvor]


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