Diazoxide


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Hypertensive crisis
Adult: 1-3 mg/kg w/in 30 seconds (max: 150 mg), repeated after 5-15 min if required.
Child: ≥1 mth Same as adult dose.

Oral
Hypoglycaemia
Adult: Initially, 3-5 mg/kg daily in 2 or 3 divided doses. Maintenance: 3-8 mg/kg daily up to 10-15 mg/kg daily in patients w/ refractory hypoglycaemia or insulinoma.
Child: Neonates: Initially, 5 mg/kg bid. Maintenance: 1.5-3 mg/kg bid or tid up to 7 mg/kg tid may be required in some cases. ≥1 mth Initially, 1.7 mg/kg tid. Maintenance: 1.5-3 mg/kg bid or tid up to 5 mg/kg tid may be required in some cases.
Renal Impairment
Dose reductions may be necessary.
Tương kỵ
Incompatible w/ hydralazine HCl, lidocaine HCl and propranolol HCl.
Chống chỉ định
Management of functional hypoglycaemia.
Thận trọng
Patient in whom retention of Na and water may be hazardous (e.g. impaired cardiac or cerebral circulation); patient w/ aortic coarctation, arteriovenous shunt, heart failure or other cardiac disorders in which increase in cardiac output could be detrimental; hyperuricaemia or history of gout; patient w/ risk factors for pulmonary HTN. Renal impairment. Childn. Pregnancy and lactation.
Phản ứng phụ
Inappropriate hypotension and hyperglycaemia, including ketoacidosis and hyperosmolar nonketotic coma; oedema due to salt and water retention, precipitating heart failure; dysgeusia, nausea, anorexia and other GI disturbances, mild hyperuricaemia, extrapyramidal symptoms, eosinophilia and thrombocytopenia, dyspnoea, hypertrichosis, headache, dizziness, tinnitus, blurred vision; hypersensitivity, manifested as rashes, leucopenia and fever. IV: Coronary ischaemia leading to angina, cardiac arrhythmias, marked ECG changes, tachycardia, palpitations, bradycardia; cerebral ischaemia leading to confusion, convulsions, loss of consciousness and neurological deficit; impaired renal function, vasodilatation symptoms, burning sensation in the vein used for inj; pulmonary HTN in neonates and infants.
MonitoringParameters
Monitor BP, glucose levels, white cell and platelet count regularly in prolonged therapy. Regularly assess bone and psychological maturation and growth in childn. Monitor serum uric acid in uremic patients.
Quá liều
Symptoms: Marked hyperglycaemia associated w/ ketoacidosis, severe hypotension. Management: Promptly treat hyperglycaemia w/ insulin and restore fluid and electrolyte balance. If necessary, control hypotension w/ sympathomimetic agents.
Tương tác
Enhanced hyperglycaemic, hyperuricemic or hypotensive effects w/ diuretics. Increased risk of hypotension w/ other antihypertensive drugs or vasodilators. Increased risk of hyperglycaemia w/ concomitant phenytoin, corticosteroids or oestrogen-progestogen combinations. May displace other highly protein-bound drugs (e.g. coumarin and its derivatives) resulting in higher blood levels of these substances.
Lab Interference
False-negative insulin response to glucagon.
Tác dụng
Description: Diazoxide increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the β-cells of the pancreas, and may increase the hepatic output of glucose. When given IV, it produces a fall in BP by causing vasodilation of the arterioles, thus a reduction in peripheral resistance. It has an antidiuretic action and produces fluid and electrolyte retention.
Onset: Hyperglycaemic: W/in 1 hr (oral).
Duration: Hyperglycaemic: ≤8 hr (oral). Antihypertensive effect: 3-12 hr (IV).
Pharmacokinetics:
Absorption: Readily absorbed from the GI tract.
Distribution: Crosses the placenta and blood-brain barrier. Plasma protein binding: >90%.
Metabolism: Partially metabolised in the liver via oxidation and sulphate conjugation.
Excretion: Via urine as unchanged drug (50%) and metabolites; faeces (small amounts). Plasma half-life: Approx 20-45 hr.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Diazoxide, CID=3019, https://pubchem.ncbi.nlm.nih.gov/compound/Diazoxide (accessed on Jan. 21, 2020)

Bảo quản
Oral susp: Store between 2-30°C. Protect from light, heat and freezing. Inj soln: Store below 25°C. Protect from light. Avoid excessive heat and freezing.
Phân loại MIMS
Phân loại ATC
C02DA01 - diazoxide ; Belongs to the class of thiazide derivative agents acting on arteriolar smooth muscle. Used in the treatment of hypertension.
References
Anon. Diazoxide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/02/2016.

Buckingham R (ed). Diazoxide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2016.

Eudemine 50 mg Tablets (RPH Pharmaceuticals AB). MHRA. https://products.mhra.gov.uk/. Accessed 10/02/2016.

Hospira NZ Limited. DBL Diazoxide injection datasheet 08 March 2012. Medsafe. http://www.medsafe.govt.nz/ . Accessed 10/02/2016.

Joint Formulary Committee. Diazoxide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/02/2016.

Proglycem diazoxide suspension (Teva Branded Pharmaceutical Products R&D, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/02/2016.

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