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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/06 23:05:20」(JST)

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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 CCK_A and CCK_B 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.

References

^ Bunney, BS; Chiodo, LA; Freeman, AS (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. doi:10.1111/j.1749-6632.1985.tb29929.x. PMID 2862828.
^ 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.
^ Bergemann, W; Consentius, K; Braun, HE; Hirschmann, H; Marowski, B; Munck, A; Rehs, HU; Stopik, D; Wilke, G (1981). "Duodenal ulcer - multicenter double-blind study with proglumide". Medizinische Klinik 76 (8): 226–9. PMID 7231338.
^ 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.
^ Tang, J; Chou, J; Iadarola, M; Yang, HY; Costa, E (1984). "Proglumide prevents and curtails acute tolerance to morphine in rats". Neuropharmacology 23 (6): 715–8. doi:10.1016/0028-3908(84)90171-0. PMID 6462377.
^ 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.
^ Rezvani, A; Stokes, KB; Rhoads, DL; Way, EL (1987). "Proglumide exhibits delta opioid agonist properties". Alcohol and drug research 7 (3): 135–46. PMID 3030338.
^ Benedetti, F; Amanzio, M; Maggi, G (1995). "Potentiation of placebo analgesia by proglumide". Lancet 346 (8984): 1231. doi:10.1016/S0140-6736(95)92938-X. PMID 7475687.

English Journal

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. floy@unica.it
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

Japanese Journal

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

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「プログルミド」

Proglumide
Systematic (IUPAC) name
	(RS)-N2-benzoyl-N,N-dipropyl-α-glutamine
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ Prescription only
Routes	Oral
Pharmacokinetic data
Half-life	~24 hours
Identifiers
CAS number	6620-60-6
ATC code	A02BX06
PubChem	CID 4922
IUPHAR ligand	893
UNII	EPL8W5565D
ChEBI	CHEBI:32058
ChEMBL	CHEMBL316561
Synonyms	4-benzamido-5-(dipropylamino)-5-oxopentanoic acid
Chemical data
Formula	C18H26N2O4
Mol. mass	334.41 g/mol
	SMILES O=C(NC(CCC(O)=O)C(N(CCC)CCC)=O)C1=CC=CC=C1;
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英: proglumide
商: プロミド

[1] Bunney, BS; Chiodo, LA; Freeman, AS (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. doi:10.1111/j.1749-6632.1985.tb29929.x. PMID 2862828.

[2] 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.

[3] Bergemann, W; Consentius, K; Braun, HE; Hirschmann, H; Marowski, B; Munck, A; Rehs, HU; Stopik, D; Wilke, G (1981). "Duodenal ulcer - multicenter double-blind study with proglumide". Medizinische Klinik 76 (8): 226–9. PMID 7231338.

[4] 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.

[5] 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.

[6] 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.

[7] Tang, J; Chou, J; Iadarola, M; Yang, HY; Costa, E (1984). "Proglumide prevents and curtails acute tolerance to morphine in rats". Neuropharmacology 23 (6): 715–8. doi:10.1016/0028-3908(84)90171-0. PMID 6462377.

[8] 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.

[9] 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.

[10] Rezvani, A; Stokes, KB; Rhoads, DL; Way, EL (1987). "Proglumide exhibits delta opioid agonist properties". Alcohol and drug research 7 (3): 135–46. PMID 3030338.

[11] Benedetti, F; Amanzio, M; Maggi, G (1995). "Potentiation of placebo analgesia by proglumide". Lancet 346 (8984): 1231. doi:10.1016/S0140-6736(95)92938-X. PMID 7475687.

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proglumide