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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 typically given in hospital.^[2]

Uses

Diazoxide is used as a vasodilator in the treatment of acute hypertension or malignant hypertension.^[3]

Diazoxide also inhibits the secretion of insulin from 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

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 increased 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]

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.

UpToDate Contents

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1. 乳児の持続性高インスリン血症性低血糖症の治療および合併症 treatment and complications of persistent hyperinsulinemic hypoglycemia of infancy
2. インスリノーマ insulinoma
3. 幼児の持続性高インスリン血症性低血糖症の病因、臨床的特徴、および診断 pathogenesis clinical features and diagnosis of persistent hyperinsulinemic hypoglycemia of infancy
4. 非膵島細胞腫瘍性低血糖 nonislet cell tumor hypoglycemia
5. スルホニル尿素剤中毒 sulfonylurea agent poisoning

English Journal

Glucose use in fasted rats under sevoflurane anesthesia and propofol anesthesia.

Sato K, Kitamura T, Kawamura G, Mori Y, Sato R, Araki Y, Yamada Y.SourceDepartment of Anesthesiology, Faculty of Medicine, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8655, Japan. tyy-kitamura@m7.dion.ne.j.
Anesthesia and analgesia.Anesth Analg.2013 Sep;117(3):627-33. doi: 10.1213/ANE.0b013e31829e4028. Epub 2013 Jul 18.
BACKGROUND: We previously reported the marked differences in the effects of sevoflurane anesthesia and propofol anesthesia on glucose use in fed rats; however, we could not elucidate mechanisms underlying the differences.METHODS: We used fasted rats in this study. After surgical preparation under se
PMID 23868888

Diazoxide postconditioning induces mitochondrial protein S-Nitrosylation and a redox-sensitive mitochondrial phosphorylation/translocation of RISK elements: no role for SAFE.

Penna C, Perrelli MG, Tullio F, Angotti C, Camporeale A, Poli V, Pagliaro P.SourceDipartimento di Scienze Cliniche e Biologiche, Facoltà di Medicina e Chirurgia S. Luigi Gonzaga, Università di Torino, Regione Gonzole 10, 10043, Orbassano, TO, Italy.
Basic research in cardiology.Basic Res Cardiol.2013 Sep;108(5):371. doi: 10.1007/s00395-013-0371-z. Epub 2013 Jul 20.
Postconditioning (PostC) can be obtained either with brief cycles of ischemia/reperfusion (I-PostC) or with a direct targeting of mitochondria with Diazoxide (pharmacological PostC, P-PostC). I-PostC may induce the activation of RISK and SAFE pathways and may favor nitric oxide production with S-Nit
PMID 23872876

Management of malignant insulinoma.

Ferrer-García JC, Iranzo González-Cruz V, Navas-Desolís S, Civera-Andrés M, Morillas-Ariño C, Merchante-Alfaro A, Caballero-Díaz C, Sánchez-Juan C, Camps Herrero C.SourceDepartment of Endocrinology and Nutrition, Consorcio Hospital General Universitario de Valencia, Valencia, Spain.
Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico.Clin Transl Oncol.2013 Sep;15(9):725-31. doi: 10.1007/s12094-012-0996-7. Epub 2013 Mar 5.
AIM: Malignant insulinoma is an infrequent functional endocrine tumor of the pancreas. Adequate therapy is a demanding challenge for oncologists and endocrinologists.OBJECTIVE: To evaluate the results of multidisciplinary management of malignant insulinoma.MATERIALS AND METHODS: Retrospective review
PMID 23460559

Related Pictures

effects of diazoxide on Proglycem Foto Primedicin Metacam (Meloxicam) Oral Suspension Best IMAGE proglycem-02.jpg ジアゾキシド50mg/mL 30mL (proglycem) Proglycem 50mg/ml Label for NDC 0575-6200-30

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「ジアゾキシド」

Diazoxide
Systematic (IUPAC) name
	7-Chloro-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide
Clinical data
Trade names	Proglycem
AHFS/Drugs.com	monograph
Pregnancy; category	AU: C; US: C (Risk not ruled out); ;
Legal status	UK: POM (Prescription only); US: ℞-only;
Routes of; administration	Oral, intravenous
Pharmacokinetic data
Protein binding	90%
Metabolism	Hepatic oxidation and sulfate conjugation
Biological half-life	21-45 hours
Excretion	Renal
Identifiers
CAS Number	364-98-7
ATC code	C02DA01 V03AH01
PubChem	CID: 3019
IUPHAR/BPS	2409
DrugBank	DB01119
ChemSpider	2911
UNII	O5CB12L4FN
KEGG	D00294
ChEBI	CHEBI:4495
ChEMBL	CHEMBL181
Chemical data
Formula	C8H7ClN2O2S
Molecular mass	230.672 g/mol
	SMILES Clc1ccc2c(c1)S(=O)(=O)/N=C(\N2)C ;
	InChI 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) ; Key:GDLBFKVLRPITMI-UHFFFAOYSA-N ;
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　　[★]

英: diazoxide
同: Hyperstat, Proglycem、アログリセム

[1] Diazoxide, drugs.com

[:0-2] "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.

[pmid8884561-3] 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.

[pmid17053028-4] 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.

[5] 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.

[6] 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.

[7] 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.

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案内

Proglycem