|Systematic (IUPAC) name|
|Legal status||℞ Prescription only|
|Mol. mass||334.41 g/mol|
|N (what is this?)|
Proglumide (Milid) is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. It was used mainly in the treatment of stomach ulcers, 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, and can prevent or even reverse the development of tolerance to opioid drugs. 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.
Proglumide has also been shown to act as a δ-opioid agonist, which may contribute to its analgesic effects.
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. The supposed mechanism is an enhancement of the neural pathways of expectation.
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- Gonzalez-Puga, Cristina; Garcia-Navarro, Ana; Escames, Germaine; Leon, Josefa; Lopez-Cantarero, Manuel; Ros, Eduardo; Acuna-Castroviejo, Dario (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 39 (3): 243–50. doi:10.1111/j.1600-079X.2005.00239.x. PMID 16150104.
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- Tariq, M; Parmar, NS; Ageel, AM (1987). "Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats". The Journal of Pharmacology and Experimental Therapeutics 241 (2): 602–7. PMID 3572816.
- McCleane, GJ (2003). "The cholecystokinin antagonist proglumide enhances the analgesic effect of dihydrocodeine". The Clinical journal of pain 19 (3): 200–1. doi:10.1097/00002508-200305000-00008. PMID 12792559.
- Watkins, LR; Kinscheck, IB; Mayer, DJ (1984). "Potentiation of opiate analgesia and apparent reversal of morphine tolerance by proglumide". Science 224 (4647): 395–6. doi:10.1126/science.6546809. PMID 6546809.
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- Bernstein, ZP; Yucht, S; Battista, E; Lema, M; Spaulding, MB (1998). "Proglumide as a morphine adjunct in cancer pain management". Journal of pain and symptom management 15 (5): 314–20. doi:10.1016/s0885-3924(98)00003-7. PMID 9654837.
- McCleane, GJ (1998). "The cholecystokinin antagonist proglumide enhances the analgesic efficacy of morphine in humans with chronic benign pain". Anesthesia and Analgesia 87 (5): 1117–20. doi:10.1213/00000539-199811000-00025. PMID 9806692.
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- Humoral regulation of heart rate during digestion in pythons (Python molurus and Python regius).
- Enok S, Simonsen LS, Pedersen SV, Wang T, Skovgaard N.SourceZoophysiology, Department of Bioscience, Aarhus University, Denmark.
- American journal of physiology. Regulatory, integrative and comparative physiology.Am J Physiol Regul Integr Comp Physiol.2012 May 15;302(10):R1176-83. Epub 2012 Mar 14.
- Pythons exhibit a doubling of heart rate when metabolism increases several times during digestion. Pythons, therefore, represent a promising model organism to study autonomic cardiovascular regulation during the postprandial state, and previous studies show that the postprandial tachycardia is gover
- PMID 22422667
- Morphological evidence that pentagastrin regulates secretion in the human parotid gland.
- Loy F, Diana M, Isola R, Solinas P, Isola M, Conti G, Lantini MS, Cossu M, Riva A, Ekström J.SourceDepartment of Cytomorphology, University of Cagliari, Cagliari, Italy. email@example.com
- Journal of anatomy.J Anat.2012 May;220(5):447-53. doi: 10.1111/j.1469-7580.2012.01489.x. Epub 2012 Mar 14.
- Salivary secretion is principally regulated by autonomic nerves. However, recent evidence from in vivo animal experiments suggests that gastrointestinal peptide hormones can also influence saliva production. The aim of the present study was to define the secretagogue activity of the gastrin-analogue
- PMID 22414238
- Activation of Spinal Cholecystokinin and Neurokinin-1 Receptors Is Associated With the Attenuation of Intrathecal Morphine Analgesia Following Electroacupuncture Stimulation in Rats
- Fukazawa Yohji,Maeda Takehiko,Kiguchi Norikazu [他],TOHYA Kazuo,KIMURA Michio,KISHIOKA Shiroh
- Journal of pharmacological sciences 104(2), 159-166, 2007-06-20
- … proglumide, a CCK-receptor antagonist (0.01 μg). …
- NAID 10024314411
- The Cholecystokinin Antagonist Proglumide Has an Analgesic Effect in Chronic Pancreatitis
- MCCLEANE GARY J.
- Pancreas 21(3), 324-325, 2000-10-01
- NAID 10016701288
- The cholecystokinin antagonist proglumide enhances the analgesic efficacy of morphine in humans with chronic benign pain
- MCCLEANE GJ.
- Anesth Analg 87, 1117-1120, 1998
- NAID 30025706595
- Proglumide (Milid) is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. It was used mainly in the treatment of stomach ulcers , ...
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