Chemistry:Diazoxide
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| Trade names | Proglycem, Balila |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | By mouth, intravenous |
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| Protein binding | 90% |
| Metabolism | Liver oxidation and sulfate conjugation |
| Elimination half-life | 21-45 hours |
| Excretion | Kidney |
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| Formula | C8H7ClN2O2S |
| Molar mass | 230.67 g·mol−1 |
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| Melting point | 330 to 331 °C (626 to 628 °F) |
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Diazoxide, sold under the brand name Proglycem and others, is a medication used to treat low blood sugar due to a number of specific causes.[1] This includes islet cell tumors that cannot be removed and leucine sensitivity.[1] It can also be used in refractory cases of sulfonylurea toxicity.[2] It is generally taken by mouth.[1]
Common side effects include high blood sugar, fluid retention, low blood platelets, a fast heart rate, increased hair growth, and nausea.[1] Other severe side effects include pulmonary hypertension and heart failure.[1] It is chemically similar to thiazide diuretics.[1] It works by decreasing insulin release from the pancreas and increasing glucose release by the liver.[1]
Diazoxide was approved for medical use in the United States in 1973.[1] It is on the World Health Organization's List of Essential Medicines.[3][4] It is available as a generic medication.[5]
Medical uses
Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[6]
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)[7] or congenital hyperinsulinism.
Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[8]
Side effects
Diazoxide interferes with insulin release through its action on potassium channels.[9] 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.[2] 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.[10]
See also
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 "Diazoxide Monograph for Professionals" (in en). https://www.drugs.com/monograph/diazoxide.html.
- ↑ 2.0 2.1 "Pharmacological agents that directly modulate insulin secretion". Pharmacological Reviews 55 (1): 105–131. March 2003. doi:10.1124/pr.55.1.7. PMID 12615955.
- ↑ World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ↑ World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. WHO/MHP/HPS/EML/2021.02.
- ↑ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 708. ISBN 9780857113382.
- ↑ "Oedema formation with the vasodilators nifedipine and diazoxide: direct local effect or sodium retention?". Journal of Hypertension 14 (8): 1041–1045. August 1996. doi:10.1097/00004872-199608000-00016. PMID 8884561.
- ↑ "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. January 2007. doi:10.1210/en.2006-0738. PMID 17053028.
- ↑ "Allosteric potentiation by diazoxide of AMPA receptor currents and synaptic potentials". European Journal of Pharmacology 247 (3): 257–265. November 1993. doi:10.1016/0922-4106(93)90193-D. PMID 8307099.
- ↑ "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. April 1989. doi:10.1016/0006-2952(89)90327-4. PMID 2650685.
- ↑ "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.
External links
- "Diazoxide". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/diazoxide.
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