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Hyperstat (Diazoxide) - Summary



brand of diazoxide, USP

HYPERSTAT I. V. Injection is a non-diuretic benzothiadiazine antihypertensive agent. Each ampule (20 mL) contains 300 mg diazoxide, USP, in a clear, sterile, colorless aqueous solution; the pH is adjusted to approximately 11.6 with sodium hydroxide.

HYPERSTAT I.V. Injection is indicated for short-term use in the emergency reduction of blood pressure in severe, nonmalignant and malignant hypertension in hospitalized adults; and in acute severe hypertension in hospitalized children, when prompt and urgent decrease of diastolic pressure is required. Treatment with orally effective antihypertensive agents should not be instituted until blood pressure has stabilized. The use of HYPERSTAT I.V. Injection for longer than 10 days is not recommended.

HYPERSTAT I.V. Injection is ineffective against hypertension due to pheochromocytoma.

See all Hyperstat indications & dosage >>


Published Studies Related to Hyperstat (Diazoxide)

Six months of diazoxide treatment at bedtime in newly diagnosed subjects with type 1 diabetes does not influence parameters of {beta}-cell function and autoimmunity but improves glycemic control. [2010.03]
OBJECTIVE Continuous beta-cell rest with diazoxide preserves residual endogenous insulin production in type 1 diabetes. However, side effects have hampered therapeutic usefulness... CONCLUSIONS Six months of low-dose diazoxide was without side effects and did not measurably affect insulin production but was associated with improved metabolic control.

Diazoxide protects myocardial mitochondria, metabolism, and function during cardiac surgery: a double-blind randomized feasibility study of diazoxide-supplemented cardioplegia. [2009.04]
OBJECTIVES: The study was designed to assess whether diazoxide-mediated cardioprotection might be used in human subjects during cardiac surgery... CONCLUSIONS: Supplementing blood cardioplegia with diazoxide is safe and improves myocardial protection during cardiac surgery, possibly through its influence on the mitochondria.

No effect of inhibition of insulin secretion by diazoxide on weight loss in hyperinsulinaemic obese subjects during an 8-week weight-loss diet. [2007.07]
AIM: Obesity is positively associated with hyperinsulinaemia, and it has been suggested that hyperinsulinaemia may contribute to maintain the obese state in insulin-resistant obese individuals. The aim of the present study was to investigate the effect of inhibition of insulin secretion by diazoxide on weight loss in obese, normoglycaemic (fasting plasma glucose of > or =6.1 mmol/l), hyperinsulinaemic (fasting plasma insulin of > or =100 pmol/l) adults during a 2.5 MJ/day energy-deficient diet... CONCLUSION: These findings do not suggest that hyperinsulinaemia per se contributes to maintenance of the obese state, and insulin secretion inhibition seems not a promising drug target.

Diazoxide-mediated insulin suppression in obese men: a dose-response study. [2005.05]
BACKGROUND: It has been suggested that diazoxide (DZX)-mediated insulin suppression may be useful to promote weight loss in obese subjects. AIM: To assess the DZX-dose range that is safe to use in obese hyperinsulinaemic men... CONCLUSION: DZX-mediated insulin suppression is dose dependent in normal and in obese men. However, the efficacy of DZX is much less in obese than in non-obese subjects. This is attributed to weight-dependent differences in distribution volume that lead to markedly lower plasma DZX levels in obese subjects. Weight-adjusted doses will be needed to achieve biologically effective plasma DZX levels. Extrapolation of the data suggests that effective insulin suppression in obese men will at least require a daily dose of 3.2-4.2 mg/kg.

Diazoxide decreases ischemia-reperfusion injury in a rat model of lung transplantation. [2011.09]
BACKGROUND: Ischemia-reperfusion injury (IRI) is a significant factor contributing to primary graft failure in lung transplantation. Given a pivotal role of mitochondria in IRI-related molecular events, the effects of diazoxide, a selective opener of mitochondrial adenosine-5'-triphosphate (ATP)-sensitive potassium channels (mitoK(ATP)), on IRI were investigated in a rat model of lung transplantation... CONCLUSIONS: These data provide evidence for substantial protective effects of diazoxide in an in vivo rat lung IRI model. Pharmacological modulation of mitoK(ATP) may be a potential strategy to reduce IRI-induced primary graft failure in lung transplantation. Copyright (c) 2011 Elsevier Inc. All rights reserved.

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Clinical Trials Related to Hyperstat (Diazoxide)

Open-Label Pharmacokinetic Study of Diazoxide Choline Coated vs. Uncoated Formulations [Active, not recruiting]

Diazoxide Choline in Hypertriglyceridemia [Recruiting]
Hypertriglyceridemia affects 30% of the population in the US. Very high level of triglycerides is a known risk factor for pancreatitis. In addition, studies have shown that hypertriglyceridemia is an independent risk factor for cardiovascular disease.

Diazoxide is a KATP channel opener. It has been approved by the FDA as an oral suspension for the treatment of hyperinsulinemic hypoglycemic conditions and as an IV solution for malignant hypertension. Preclinical and clinical studies suggest that diazoxide can be a potential therapeutic agent for hypertriglyceridemia.

Diazoxide choline is a novel, highly crystalline proprietary salt of diazoxide, which has been formulated as a controlled-release tablet suitable for once per day dosing. This current study is designed to assess the effect of diazoxide choline on triglycerides in subjects with baseline hypertriglyceridemia. In addition, the effects on other lipid parameters, glucose and insulin, body weight as well as the safety and tolerability of diazoxide choline will be assessed.

DZX Mediated Insulin Suppression in Obese Men [Recruiting]
The purpose of this study is to determine whether there is an additive effect of metformine on the weight reduction of obese hyperinsulinemic men who are treated with diazoxide.

Diazoxide-Mediated Insulin Suppression in Hyperinsulinemic Obese Men [Completed]
The purpose of this study is to explore diazoxide efficacy in treatment of obese men and assessment of maximal insulin suppression in obese men without hyperglycaemia.

Obesity is associated with markedly elevated plasma insulin levels throughout the day. The concept is that obese subjects predominantly develop lean tissue resistance against the glucoregulatory actions of insulin, but remain relatively sensitive to the lipogenic and antilipolytic effects of insulin in adipose tissue. According to this theory, suppression of hyperinsulinism by diazoxide, a well known inhibitor of glucose stimulated insulin secretion, might be useful to treat obesity because it will help to reverse the process of lipid storage.

Efficacy of Diazoxide in Type 1 Diabetes [Active, not recruiting]
The purpose of this study is to find out if Diazoxide can partly retain insulin production in newly diagnosed type 1 diabetes patients.

more trials >>

Page last updated: 2011-12-09

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