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Diazoxide

Medication used to treat low blood sugar and high blood pressure From Wikipedia, the free encyclopedia

Diazoxide

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.[2] This includes islet cell tumors that cannot be removed and leucine sensitivity.[2] It can also be used in refractory cases of sulfonylurea toxicity.[3] It is generally taken by mouth.[2]

Quick Facts Clinical data, Trade names ...
Diazoxide
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Clinical data
Trade namesProglycem
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth, intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding90%
MetabolismLiver oxidation and sulfate conjugation
Elimination half-life21-45 hours
ExcretionKidney
Identifiers
  • 7-Chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.006.063
Chemical and physical data
FormulaC8H7ClN2O2S
Molar mass230.67 g·mol−1
3D model (JSmol)
Melting point330 to 331 °C (626 to 628 °F)
  • Clc1ccc2c(c1)S(=O)(=O)/N=C(\N2)C
  • InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11) Y
  • Key:GDLBFKVLRPITMI-UHFFFAOYSA-N Y
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Common side effects include high blood sugar, fluid retention, low blood platelets, a fast heart rate, increased hair growth, and nausea.[2] Other severe side effects include pulmonary hypertension and heart failure.[2] It is chemically similar to thiazide diuretics.[2] It works by decreasing insulin release from the pancreas and increasing glucose release by the liver.[2]

Diazoxide was approved for medical use in the United States in 1973.[2] It is on the World Health Organization's List of Essential Medicines.[4][5] It is available as a generic medication.[6]

Medical uses

Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.[7]

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)[8] or congenital hyperinsulinism.

Diazoxide acts as a positive allosteric modulator of the AMPA and kainate receptors, suggesting potential application as a cognitive enhancer.[9]

Side effects

Diazoxide interferes with insulin release through its action on potassium channels.[10] 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.[3] 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.[11]

Research

Diazoxide, formulated as its choline salt diazoxide choline, is an experimental antiobesity drug being tested in people with Prader-Willi syndrome[12][13][14] and monogenic obesity caused by mutations in the SH2B1, PCSK1, or SIM1 genes.[15]

References

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