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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2018/11/10 22:36:45」(JST)
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| Clinical data | |
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| Trade names | Proglycem |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Oral, intravenous |
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| Pharmacokinetic data | |
| Protein binding | 90% |
| Metabolism | Hepatic oxidation and sulfate conjugation |
| Elimination half-life | 21-45 hours |
| Excretion | Renal |
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| ECHA InfoCard | 100.006.063 |
| Chemical and physical data | |
| Formula | C8H7ClN2O2S |
| Molar mass | 230.672 g/mol |
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Diazoxide (INN; brand name Proglycem[1]) is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels, preventing calcium flux across the sarcolemma and activation of the contractile apparatus.
In the United States, this agent is only available in the oral form and is typically given in hospital settings.[2]
Contents
- 1 Medical uses
- 2 Side effects
- 3 See also
- 4 References
Medical uses
Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[3]
Diazoxide also inhibits the secretion of insulin by opening ATP-sensitive potassium channel of beta cells of the pancreas, thus it is used to counter hypoglycemia in disease states such as insulinoma (a tumor producing insulin)[4] or congenital hyperinsulinism.
Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[5]
Side effects
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Diazoxide interferes with insulin release through its action on potassium channels.[6] Diazoxide is one of the most potent openers of the K+ ATP channels present on the insulin producing beta cells of the pancreas. Opening these channels leads to hyperpolarization of cell membrane, a decrease in calcium influx, and a subsequently reduced release of insulin.[7] This mechanism of action is the mirror opposite of that of sulfonylureas, a class of medications used to increase insulin release in Type 2 Diabetics. Therefore, this medicine is not given to non-insulin dependent diabetic patients.
The Food and Drug Administration published a Safety Announcement in July 2015 highlighting the potential for development of pulmonary hypertension in newborns and infants treated with this drug.[2]
See also
- Hydrochlorothiazide (HCTZ)
- AMPA receptor positive allosteric modulator
- Glucose-elevating agent
References
- ^ Diazoxide, drugs.com
- ^ a b "FDA Drug Safety Communication: FDA warns about a serious lung condition in infants and newborns treated with Proglycem (diazoxide)" (Press release). Food and Drug Administration. July 16, 2015. Retrieved 2015-07-19.
- ^ van Hamersvelt HW, Kloke HJ, de Jong DJ, Koene RA, Huysmans FT (August 1996). "Oedema formation with the vasodilators nifedipine and diazoxide: direct local effect or sodium retention?". Journal of Hypertension. 14 (8): 1041–5. doi:10.1097/00004872-199608000-00016. PMID 8884561.
- ^ Huang Q, Bu S, Yu Y, et al. (January 2007). "Diazoxide prevents diabetes through inhibiting pancreatic beta-cells from apoptosis via Bcl-2/Bax rate and p38-beta mitogen-activated protein kinase". Endocrinology. 148 (1): 81–91. doi:10.1210/en.2006-0738. PMID 17053028.
- ^ Randle, John C.R.; Biton, Catherine; Lepagnol, Jean M. (15 November 1993). "Allosteric potentiation by diazoxide of AMPA receptor currents and synaptic potentials". European Journal of Pharmacology. 247 (3): 257–65. doi:10.1016/0922-4106(93)90193-D. PMID 8307099.
- ^ Panten, Uwe; Burgfeld, Johanna; Goerke, Frank; Rennicke, Michael; Schwanstecher, Mathias; Wallasch, Andreas; Zünkler, Bernd J.; Lenzen, Sigurd (1989-04-15). "Control of insulin secretion by sulfonylureas, meglitinide and diazoxide in relation to their binding to the sulfonylurea receptor in pancreatic islets". Biochemical Pharmacology. 38 (8): 1217–1229. doi:10.1016/0006-2952(89)90327-4.
- ^ Doyle, Máire E.; Egan, Josephine M. (2003-03-01). "Pharmacological Agents That Directly Modulate Insulin Secretion". Pharmacological Reviews. 55 (1): 105–131. doi:10.1124/pr.55.1.7. ISSN 1521-0081. PMID 12615955.
Nonsympatholytic vasodilatory antihypertensives (C02) | |||||
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| Nitrovasodilator |
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| (arteriolar) Potassium channel opener |
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| (arteriolar) Calcium channel blocker |
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Other therapeutic products (V03AG–V03AZ) | |
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| Treatment of hypercalcemia |
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| Treatment of hypoglycaemia |
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| Medical gases |
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| Nerve depressants |
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Ion channel modulators | |||||||||||||||||||||||||
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See also: Receptor/signaling modulators • Transient receptor potential channel modulators | |||||||||||||||||||||||||
Ionotropic glutamate receptor modulators | |
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[Category:AMPA receptor positive allosteric modulators]
English Journal
- Eriodictyol stimulates insulin secretion through cAMP/PKA signaling pathway in mice islets.
- Hameed A1, Hafizur RM2, Hussain N3, Raza SA1, Rehman M3, Ashraf S1, Ul-Haq Z1, Khan F1, Abbas G3, Choudhary MI4.
- European journal of pharmacology.Eur J Pharmacol.2018 Feb 5;820:245-255. doi: 10.1016/j.ejphar.2017.12.015. Epub 2017 Dec 8.
- PMID 29229531
- Local antinociceptive action of fluoxetine in the rat formalin assay: role of l-arginine/nitric oxide/cGMP/KATP channel pathway.
- Ghorbanzadeh B1, Mansouri MT2, Naghizadeh B2, Alboghobeish S2.
- Canadian journal of physiology and pharmacology.Can J Physiol Pharmacol.2018 Feb;96(2):165-172. doi: 10.1139/cjpp-2017-0003. Epub 2017 Aug 8.
- PMID 28787580
- Randomised controlled trial of diazoxide for small for gestational age neonates with hyperinsulinaemic hypoglycaemia provided early hypoglycaemic control without adverse effects.
- Balachandran B1, Mukhopadhyay K1, Sachdeva N2, Walia R2, Attri SV1.
- Acta paediatrica (Oslo, Norway : 1992).Acta Paediatr.2018 Jan 31. doi: 10.1111/apa.14252. [Epub ahead of print]
- PMID 29385640
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