HYPERSTAT SUMMARY
HYPERSTAT® I.V.
brand of diazoxide, USP
Injection
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.
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NEWS HIGHLIGHTS
Published Studies Related to Hyperstat (Diazoxide)
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.
Role of the nitric oxide on diazoxide-induced relaxation of the calf cardiac vein and coronary artery during cooling. [2009.06]
The effects of cooling (to 28 degrees C) on the vasodilation induced by diazoxide (10(-9)-3 x 10(-4) M) on carbachol-pre-contracted calf cardiac vein and coronary artery and the role of nitric oxide in these effects were analyzed. Diazoxide produced concentration-dependent relaxation of calf cardiac vein and coronary artery rings pre-contracted with carbachol (10(-6) M).
Weight loss in obese men by caloric restriction and high-dose diazoxide-mediated insulin suppression. [2008.12]
OBJECTIVE: To examine the concept whether high-dose diazoxide (DZX)-mediated insulin suppression, in combination with moderate caloric restriction and increased physical activity, can establish a weight loss of at least 15% in obese hyperinsulinaemic men... CONCLUSION: High-dose DZX-mediated insulin suppression, in combination with moderate caloric restriction and lifestyle advice, is associated with a clinically relevant degree of weight reduction. A more extensive exploration is warranted to optimize this mode of treatment and to further clarify its risks and benefits.
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.
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.
Diazoxide In the Management Of Hypoglycemic Neonates [Not yet recruiting]
Diazoxide is an oral hyperglycemic medication. Diazoxide has been proven effective for
treating hypoglycemia in infants and children with some types of persistent hyperinsulinemic
hypoglycemia. The mechanism of action results in decreased insulin secretion. One of the
causes of hypoglycemia in infants of diabetic mothers occurs due to a transient
hyperinsulinemic state postnatally. The investigators have clinical experience and success
using diazoxide in their unit for patients with hypoglycemia not adequately managed with
intravenous (iv) dextrose and enteral supplementation. In this randomized controlled study
the investigators expect that by using diazoxide as the initial treatment for infants of
diabetic mothers with asymptomatic hypoglycemia (blood glucose of 2. 5 to 2. 0mmol/L), the
investigators will be able to decrease the number of infants requiring an intravenous by at
least thirty percent.
Open-Label, Single- and Multiple-Dose Pharmacokinetic Study of Diazoxide Choline [Not yet recruiting]
This is a single-center, randomized, open-label, single- and multiple-dose, five-treatment,
two-period, four-way parallel study comparing the pharmacokinetics (PK) of Diazoxide Choline
Controlled-Release Tablet (DCCR) administered orally under fed and fasting conditions at two
dose levels.
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