Chemical Property of Diazoxide
Chemical Property:
- Melting Point:>310°C
- Refractive Index:1.6300 (estimate)
- Boiling Point:414.8°Cat760mmHg
- PKA:pKa 8.5 (Uncertain)
- Flash Point:204.7°C
- PSA：66.91000
- Density:1.61g/cm3
- LogP:2.52700
- Storage Temp.:Store at RT
- Solubility.:0.1 M NaOH: soluble
- Water Solubility.:Soluble in 0.1M NaOH. Insoluble in water or in methanol.
- XLogP3:1.2
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:3
- Rotatable Bond Count:0
- Exact Mass:229.9916763
- Heavy Atom Count:14
- Complexity:360
- Purity/Quality:
-
97% *data from raw suppliers
Diazoxide *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:Xn
- Statements:
22-36/37/38
- Safety Statements:
22-26-36
- MSDS Files:
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SDS file from LookChem
Total 1 MSDS from other Authors
Useful:
- Canonical SMILES:CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl
- Recent ClinicalTrials:Novel Approach for the Prevention of Hypoglycemia Associated Autonomic Failure (HAAF)
- Recent EU Clinical Trials:Use of diazoxide in hypoglycaemia
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Description
Diazoxide is a nondiuretic derivative of thiazides that dramatically reduces blood pressure
by direct relaxation of smooth muscles of the arterioles, possibly as a result of calcium channel activation of smooth musculature in arterioles. It has a weak effect on the venous
system and on the heart. In addition to hypotensive action, diazoxide causes a sharp increase
in the level of glucose in the blood as a result of the inhibition of insulin release from adrenal
glands. Some of the undesirable effects are water and sodium ion retention in the body
and increased concentrations of uric acid in the blood. It is used in urgent situations where
blood pressure needs to be reduced in severe hypertension. Diazoxide is not used for essential
hypertension. A synonym of this drug is hyperstat.
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Uses
Diazoxide has traditionally been used therapeutically for its
antihypertensive and hyperglycemic properties. It acts as
a potent arteriolar vasodilator in the short-term treatment of
acute hypertension, malignant hypertension, and occasionally,
in cases of pregnancy-induced hypertension. By relaxing
peripheral arterioles of smooth muscle cells, peripheral
vascular resistance is reduced. In rare cases, cardiac and
pulmonary effects have occurred in neonates and in infants. In
the treatment of hypertensive crisis with 300 mg of IV diazoxide,
angina, myocardial and cerebral infarction, ischemia, and
optic nerve damage could ensue. Diazoxide is used also in the
management of hypoglycemia secondary to hyperinsulinism in
adults with inoperable islet cell adenoma or carcinoma, or
extrapancreatic malignancy; and in infants and children with
leucine sensitivity, islet cell hyperplasia, nesidioblastosis,
extrapancreatic malignancy, islet cell adenoma, or adenomatosis.
In the treatment of hypoglycemia due to hyperinsulinism,
diazoxide is an oral agent that decreases insulin release
from the pancreas, enhancing glycogenolysis and inhibiting the
uptake of glucose. wound healing agent Diazoxide reduces status epilepticus neuron damage in diabetes.
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Therapeutic Function
Antihypertensive
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Biological Functions
Diazoxide (Hyperstat) is chemically similar to the thiazide
diuretics. It is devoid of diuretic activity and
causes Na+ and water retention. Diazoxide is a very potent
vasodilator and is available only for intravenous use in the treatment of hypertensive emergencies. The
mechanism by which diazoxide relaxes vascular smooth
muscle is related to its ability to activate potassium
channels and produce a hyperpolarization of the cell
membrane.
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Clinical Use
Diazoxide is used by intravenous injection as a rapidly acting antihypertensiveagent for emergency reduction of blood pressurein hospitalized patients with accelerated or malignanthypertension. More than 90% is bound to serum protein, andcaution is needed when it is used in conjunction with otherprotein-bound drugs that may be displaced by diazoxide.The injection is given rapidly by the intravenous route toensure maximal effect. The initial dose is usually 1 mg/kg ofbody weight, with a second dose given if the first injectiondoes not lower blood pressure satisfactorily within 30 minutes.Further doses may be given at 4- to 24-hour intervalsif needed. Oral antihypertensive therapy is begun as soon aspossible. In contrast to the acute clinical uses of glucagon, diazoxidefinds use in chronic hypoglycemic conditions: inoperableislet cell adenoma or carcinomas, extrapancreatic malignanciesof insulin-secreting cells, or islet cell hyperplasias. Inchildren, additional indications include congenital hyperinsulinemia124and leucine sensitivity. Experimentally, diazoxideis among an array of ATP-sensitive potassium channel openersbeing studied for intermittently bringing aboutβ-cell rest.
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Drug interactions
Potentially hazardous interactions with other drugsAntihypertensives and vasodilators: enhanced
hypotensive effect.MAOIs: withdraw at least 14 days before starting
diazoxidePhenytoin: may reduce phenytoin levels.
