diazoxide

ジアゾキシド 　

WordNet

1. vasodilator (trade name Hyperstat) used to treat severe hypertension (同)Hyperstat

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/07/31 14:46:38」(JST)

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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 cat.	C (AU) C (US)
Legal status	POM (UK) ℞-only (US)
Routes	Oral, intravenous
Pharmacokinetic data
Protein binding	90%
Metabolism	Hepatic oxidation and sulfate conjugation
Half-life	21-45 hours
Excretion	Renal
Identifiers
CAS number	364-98-7 Y
ATC code	C02DA01 V03AH01
PubChem	CID 3019
IUPHAR ligand	2409
DrugBank	DB01119
ChemSpider	2911 Y
UNII	O5CB12L4FN Y
KEGG	D00294 Y
ChEBI	CHEBI:4495 Y
ChEMBL	CHEMBL181 Y
Chemical data
Formula	C8H7ClN2O2S
Mol. 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) Y Key:GDLBFKVLRPITMI-UHFFFAOYSA-N Y
Y (what is this?)  (verify)

Diazoxide (INN; brand name Proglycem) 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 which inhibits the generation of an action potential.

Uses

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

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) or congenital hyperinsulinism.

Diazoxide acts as a positive allosteric modulator of the AMPA receptor, suggesting potential application as a cognitive enhancer.

Synthesis

Diazoxide can be prepared from dichloronitrobenzene:

Diazoxide synthesis.

Side effects

Diazoxide interferes with insulin release through its action on potassium channels. The efflux of potassium, as an effect of Diazoxide, will lead to hyperpolarization of cell membrane that leads to decrease calcium influx. The low calcium will decrease the release of insulin. Therefore this medicine is not given to non-insulin dependent diabetic patients.

References

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

• Prolonged hyperglycemia & hyperinsulinemia increases BDNF mRNA expression in the posterior ventromedial hypothalamus and the dorsomedial hypothalamus of fed female rats.

• Negrón AL1, Beymer M2, Yu G3, Warren KA3, Acosta-Martínez M4.
• Neuroscience.Neuroscience.2015 Sep 10;303:422-32. doi: 10.1016/j.neuroscience.2015.07.018. Epub 2015 Jul 10.
• Brain-derived neurotrophic factor (BDNF) plays a key role in neuronal development, synaptic plasticity, and the central control of energy homeostasis. Peripheral metabolic signals such as leptin and glucose regulate hypothalamic BDNF gene expression. However, the effects of long-term hyperglycemia a
• PMID 26166726

• The mechanistic target of rapamycin (mTOR) pathway and S6 Kinase mediate diazoxide preconditioning in primary rat cortical neurons.

• Dutta S1,2, Rutkai I2, Katakam PV1,2, Busija DW1,2.
• Journal of neurochemistry.J Neurochem.2015 Sep;134(5):845-56. doi: 10.1111/jnc.13181. Epub 2015 Jul 1.
• We examined the role of the mechanistic target of rapamycin (mTOR) pathway in delayed diazoxide (DZ)-induced preconditioning of cultured rat primary cortical neurons. Neurons were treated for 3 days with 500 μM DZ or feeding medium and then exposed to 3 h of continuous normoxia in Dulbecco's mod
• PMID 26016889

• Dynamics of Enhanced Mitochondrial Respiration in Female Compared with Male Rat Cerebral Arteries.

• Rutkai I1, Dutta S2, Katakam PV2, Busija DW2.
• American journal of physiology. Heart and circulatory physiology.Am J Physiol Heart Circ Physiol.2015 Aug 14:ajpheart.00231.2015. doi: 10.1152/ajpheart.00231.2015. [Epub ahead of print]
• OBJECTIVE: Mitochondrial respiration has never been directly examined in intact cerebral arteries. We tested the hypothesis that mitochondrial energetics of large cerebral arteries ex vivo are sex-dependent. Approach and results: The Seahorse XFe24 analyzer was used to examine mitochondrial respirat
• PMID 26276815

Japanese Journal

• インスリノーマ (特集 低血糖患者の診療)

• 泉山 肇
• 内分泌・糖尿病・代謝内科 30(2), 154-157, 2010-02
• NAID 40017666344

• 症例報告 成人発症nesidioblastosisによる難治性低血糖症に対してジアゾキサイドが長期にわたり有効であった1例

• 新生 忠司,岡田 洋右,吉村 暁子 [他]
• 糖尿病 53(11), 803-809, 2010-11
• NAID 40017423810

Related Links

• ジアゾキシド【diazoxide】の意味 - 国語辞書 - goo辞書

ジアゾキシド【diazoxide】とは。意味や解説。主に新生児・乳幼児に発症する高インスリン血性低血糖症の治療薬。商品名アログリセム。膵臓のβ(ベータ)細胞に作用してインスリンの分泌を抑制し、血糖を上昇させる。[補説]米国の製薬 ...

• 稲穂の会 【病気・薬について】

高インスリン血性低血糖症とジアゾキサイド（diazoxide）についての簡単な説明です。 この疾患は非常に稀なため、情報量も極端に少なく、得られる情報がほとんどない状態です。 また最近になって解明されつつある疾患のため、名称 ...

Related Pictures

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★リンクテーブル★

リンク元	「ATP感受性Kチャネル」「ジアゾキシド」

「ATP感受性Kチャネル」

　　[★]

英

ATP-sensitive K+ channel, ATP-sensitive K channel, ATP-sensitive potassium channel, KATP

同

ATP感受性カリウムチャネル, ATP依存性Kチャネル, ATP依存性カリウムチャネル, KATPチャネル

GOO. 1616

• ATP共役して作用するチャネル

Kir 6.2とSUR1からなる。

Kir 6.2にATPが結合してチャネルを抑制する

SUR1にはADP、diazoxide(チャネルの作動薬)、スルホニルウレアとmeglitinide(チャネルの阻害薬)が結合する。

「ジアゾキシド」

　　[★]

英

diazoxide

同

Hyperstat, Proglycem、アログリセム