Adult: For the management of acute hypertensive crises associated with acute glomerular nephritis, acute hypertensive encephalopathy, cerebral haemorrhage, CHF, and refractory hypertension: As solution for inj: 1-3 mg/kg (Max: 150 mg) via rapid IV inj within 30 seconds, then repeated every 5-15 minutes if required. Doses are given undiluted. Dosage and treatment recommendations may vary among individual products and between countries (refer to specific product information or local guidelines).
Oral Hypoglycaemia
Adult: For the management of intractable cases or hypoglycaemia due to hyperinsulinism associated with inoperable islet cell adenoma/carcinoma or extrahepatic malignancy: As tab/oral susp: Initially, 3-5 mg/kg daily in 2 or 3 equally divided doses, then adjusted based on response. Maintenance: 3-8 mg/kg daily in 2 or 3 equally divided doses. Higher doses may be required for patients with refractory hypoglycaemia. Dose must be individualised according to the severity of condition, blood glucose levels, and clinical response. Discontinue therapy if not effective after 2-3 weeks. Use diazoxide when other specific medical or surgical treatments for hypoglycaemia are unsuccessful or not feasible. Dosage and treatment recommendations may vary among individual products and between countries (refer to specific product information or local guidelines). Child: For the management of hypoglycaemia due to hyperinsulinism associated with leucine sensitivity, nesidioblastosis, extrahepatic malignancy, islet cell hyperplasia/adenoma, or adenomatosis: Infants As oral susp: Initially, 10 mg/kg daily in 3 divided doses given every 8 hours, then adjusted based on clinical response. Maintenance: 8-15 mg/kg daily in 2 or 3 divided doses given every 12 hours or 8 hours; Children As tab/oral susp: Initially, 3-5 mg/kg daily in 2 or 3 equally divided doses, then adjusted based on clinical response. Maintenance: 3-8 mg/kg daily in 2 or 3 equally divided doses. Dose must be individualised according to the severity of condition, blood glucose levels, and clinical response. Consider use in combination with thiazide diuretic to minimise fluid retention. Discontinue therapy if not effective after 2-3 weeks. Dosage and treatment recommendations may vary among individual products and between countries (refer to specific product information or local guidelines).
Renal Impairment
Dose reduction may be required.
Incompatibility
IV: Incompatible with hydralazine hydrochloride, lidocaine hydrochloride and propranolol hydrochloride.
Contraindications
Hypersensitivity to diazoxide or other thiazides. Functional hypoglycaemia (oral).
Special Precautions
Patient with impaired cardiac or cerebral circulation, aortic coarctation, aortic stenosis, arteriovenous shunt, heart failure or other cardiac disorders; hyperuricaemia or history of gout. Administration of IV diazoxide during labour may cause cessation of uterine contractions; an oxytocic agent may be given to reinstate labour. If oral diazoxide is administered during labour, caution is recommended. Avoid extravasation (IV). Renal impairment. Neonates and infants, especially those with hyperbilirubinaemia or risk factors for pulmonary hypertension (e.g. meconium aspiration syndrome, transient tachypnoea of newborn, respiratory distress syndrome, sepsis, pneumonia, congenital heart disease, congenital diaphragmatic hernia). Children. Pregnancy and lactation.
Adverse Reactions
Significant: Hyperglycaemic crisis, including ketoacidosis and nonketotic hyperosmolar coma; oedema due to salt and water retention (which may precipitate heart failure); development of abnormal facial features (particularly when used for hypoglycaemia in children treated for >4 years); pulmonary hypertension (reversible upon discontinuation), particularly when used for hypoglycaemia in neonates and infants. Blood and lymphatic system disorders: Leucopenia, transient neutropenia, thrombocytopenia. Cardiac disorders: Palpitation, tachycardia. Eye disorders: Blurred vision, transient cataracts, diplopia, lacrimation. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, dysgeusia; necrotising enterocolitis (particularly in infants with underlying co-morbidity). General disorders and administration site conditions: Inj site pain or warmth (IV). Immune system disorders: Hypersensitivity reactions. Investigations: Increased AST and alkaline phosphatase; decreased CrCl, decreased Hb and/or haematocrit. Metabolism and nutrition disorders: Hyperuricaemia, anorexia. Nervous system disorders: Headache, dizziness. Renal and urinary disorders: Azotaemia, haematuria, albuminuria. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Pruritus, rash, dermatitis, hirsutism; hypertrichosis lanuginosa (particularly in children). Vascular disorders: Hypotension; flushing, transient myocardial or cerebral ischaemia (IV).
Monitoring Parameters
Closely monitor blood glucose levels regularly during treatment (oral); blood pressure until the patient is stabilised then hourly thereafter (IV). Monitor serum electrolytes, BUN, renal function, and serum AST levels; urine glucose and ketones (especially under stress conditions and during prolonged treatment); CBC with differential (particularly on prolonged use); serum uric acid (especially in patients with hyperuricaemia or history of gout). In neonates and infants, perform thorough cardiac evaluation and consider echocardiogram at baseline and periodically thereafter. Closely monitor neonates and infants for signs of respiratory distress (particularly those with risk factors for pulmonary hypertension).
Overdosage
Symptoms: Marked hyperglycaemia (which may be associated with ketoacidosis) and hypotension. Management: Symptomatic treatment. Prompt administration of insulin and restoration of fluid and electrolyte balance may be done for severe hyperglycaemia; oral hypoglycaemic agents may be given for less severe hypoglycaemia. Manage hypotension with IV fluids, then sympathomimetic agents may be needed for severe cases.
Drug Interactions
May increase the risk of hyperglycaemia with phenytoin, corticosteroids, and estrogen-progestogen combinations. May potentiate the hyperglycaemic, hyperuricaemic, or hypotensive effects with diuretics. May enhance the hypotensive effects of other antihypertensive agents. May displace other highly protein-bound agents (e.g. warfarin) resulting in higher levels of these agents.
Lab Interference
May result in false-negative insulin response to glucagon. May decrease serum cortisol concentrations. May increase serum renin and IgG concentrations.
Action
Description: Mechanism of Action: Diazoxide, a nondiuretic benzothiadiazine derivative, is used for symptomatic hypoglycaemia (oral) and as an antihypertensive agent (IV). Orally, it increases plasma glucose concentration by inhibiting insulin secretion of the pancreatic β cells and by increasing the hepatic release of glucose. When given intravenously, it reduces peripheral vascular resistance and blood pressure by causing direct vasodilation in the smooth muscle of peripheral arterioles. Onset: Hyperglycaemic effect: Within 1 hour (oral). Hypotensive effect: <5 minutes (IV). Duration: Hyperglycaemic effect: ≤8 hours (oral). Pharmacokinetics: Absorption: Readily absorbed from the gastrointestinal tract. Distribution: Crosses the placenta and blood-brain barrier. Plasma protein binding: >90%. Metabolism: Partially metabolised in the liver. Excretion: Via urine (50% as unchanged drug); faeces. Terminal elimination half-life: 21-45 hours.
Chemical Structure
Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3019, Diazoxide. https://pubchem.ncbi.nlm.nih.gov/compound/Diazoxide. Accessed July 26, 2024.
Storage
Tab/oral susp: Store between 15-30°C. Protect from light. Solution for IV inj: Store below 25°C. Do not freeze. Protect from light and heat.
V03AH01 - diazoxide ; Belongs to the class of drugs used in the treatment of hypoglycemia. C02DA01 - diazoxide ; Belongs to the class of thiazide derivative agents acting on arteriolar smooth muscle. Used in the treatment of hypertension.
References
Anon. Diazoxide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 02/05/2024.Buckingham R (ed). Diazoxide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/05/2024.Diazoxide. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 12/07/2024.Diazoxide. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/05/2024.Diazoxide. UpToDate Lexidrug, Pediatric and Neonatal Lexi-Drugs Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 12/07/2024.Eudemine 50 mg Tablets (RPH Pharmaceuticals AB). MHRA. https://products.mhra.gov.uk. Accessed 02/05/2024.Joint Formulary Committee. Diazoxide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/05/2024.Paediatric Formulary Committee. Diazoxide. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 12/07/2024.Pfizer New Zealand Limited. DBL Diazoxide Injection data sheet 11 December 2023. Medsafe. http://www.medsafe.govt.nz. Accessed 02/05/2024.Proglycem Suspension (Teva Pharmaceuticals USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/07/2024.
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