Diazoxide

Diazoxide is antihypertensive agent. Diazoxide is a relatively long acting parentrally administerd vasodilator. Diazoxide is useful in hypertensive emergencies to lower the blood pressure and to increase blood sugar level in hypoglycemia.


Brands
Adult Dose
Dose: 2.143 mg/kg
Single Dose: 2.1 (2.143)
Frequency: 24 hourly
Route: IV
Instructions: Initially every 5-15 minutes, repeated as required
Neonatal
Paedriatic
Characteristics
. It is of Synthetic origin and belongs to Benzothiadiazine. It belongs to Potassium Channel (ATP sensitive) opener pharmacological group on the basis of mechanism of action and also classified in Vasodilators pharmacological group.The Molecular Weight of Diazoxide is 230.70. Its pKa is 8.5.
Contraindications
Diazoxide is contraindicated in conditions like Diabetes mellitus,Anuria,Thiamine deficiency,Trauma,Intracranial hemorrhage,Acute ischaemic stroke,Sepsis,Hypophosphataemia,Haemodilution.
Effects
The severe or irreversible adverse effects of Diazoxide, which give rise to further complications include Tachycardia, Rashes, Fever, Thrombocytopenia, Pancreatitis, Lymphadenopathy, Lymphadenopathy, Neutropenia, Palpitation, Gout, Hepatorenal changes, Chest pain.Diazoxide produces potentially life-threatening effects which include Congestive heart failure, Hypotension, Hyperosmolar non-ketotic diabetic coma, Diabetic ketoacidosis, Water retention, Sodium retention. which are responsible for the discontinuation of Diazoxide therapy.The signs and symptoms that are produced after the acute overdosage of Diazoxide include Hyperglycemia, Ketoacidosis.The symptomatic adverse reactions produced by Diazoxide are more or less tolerable and if they become severe, they can be treated symptomatically, these include Weakness, Dizziness, Headache, Nausea, Vomiting, Restlessness, Palpitation, Constipation, Abdominal pain, Pruritus, Flushing, Tremor, Hirsutism, Loss of taste, Reaction at injection site, Dysgeusia, Transient cataract, dizziness.
Indications
Diazoxide is primarily indicated in conditions like Carbohydrate depletion, Dehydration, Duodenal ulceration associated with H. Pylori, Fluid depletion, Hypertensive emergencies, Hypertensive encephalopathy, Hypoglycaemia, and can also be given in adjunctive therapy as an alternative drug of choice in Cerebral oedema, Reflux oesophagitis, Schizophrenia and other psychoses, Varicose veins.
Interactions
Diazoxide is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAlcoholEnhanced hypotensive effect when Diazoxide given with Alcohol.AldesleukinHypotensive effects may be enhanced by the concomitant administration of Diazoxide.AlprostadilEnhanced hypotensive effects when alprostadil given with Diazoxide.Amlodipine (Besylate)Enhanced hypotensive effect when Diazoxide given with Amlodipine.BaclofenEnhanced hypootensive effect when Diazoxide given with Baclofen.Beclomethasone (Dipropionate)Hypotensive effect of Diazoxide antagonised by Beclomethasone.CandesartanEnhanced hypotensive effect when Diazoxide given with Candesartan.CaptoprilEnhanced hypotensive effect when Diazoxide given with Captopril.Carbenoxolone (Na)Hypotensive effect of diazoxide antagonised by Carbenoxolone.Chlormethiazole (Edisylate)ChlorothiazideChlorpromazine (HCl)Enhanced hypotensive effect when Diazoxide Chlorpromazine.ChlorthalidoneCisplatinClonidine (HCl)Enhanced hypotensive effect when Diazoxide given with Clonidine.DexamethasoneHypotensive effect of Diazoxide antagonised by Dexamethasone.DiazepamEnhanced hypotensive effect when Diazoxide given Diazepam.Enalapril (Maleate)Enhanced hypotensive effect when Diazoxide given with Enalapril.EnfluraneEnhanced hypotensive effect when Diazoxide given with Enflurane.EplerenoneConcomitant use with diazoxide, MAOIs, pentoxifylline, prostacyclin analogues may enhance hypotensive effect of antihypertensives.Estrogens ConjugatedHypotensive effect of diazoxide antagonised by Estrogens.Ethacrynic AcidFluphenazineEnhanced hypotensive effect when Diazoxide given with Fluphenazine.FosphenytoinFrusemide or FurosemideEnhanced hypotensive effect when Diazoxide given with Frusemide.GlibenclamideDiazoxide antagonises hypoglycaemic effect of antidiabetics.GliclazideHalothaneEnhanced hypotensive effect when Diazoxide given with general anesthetics (Halothane).Human InsulinHydralazine (HCl)Enhanced hypotensive effect when Diazoxide given with Hydralazine.Hydralazine (HCl)HydrochlorothiazideEnhanced hypotensive effect when Diazoxide given with Hydrochlorothiaide.IbuprofenHypotensive effect of when diazoxide antagonised by Ibuprofen.IndomethacinHypotensive effect of diazoxide antagonised by NSAIDs (Indomethacin).Insulin AspartDiazoxide antagonises hypoglycaemic effect of antidiabetics (insulin).Insulin LisproLevodopaEnhanced hypootensive effect when Diazoxide given with Levodopa.Losartan (K)Enhanced hypotensive effect when Diazoxide given with Losartan.MethyldopaEnhanced hypootensive effect when Diazoxide given with Methyldopa.MoxisylyteEnhanced hypootensive effect when Diazoxide given with Moxisylyte.MoxonidineEnhanced hypootensive effect when Diazoxide given with Moxonidine.NifedipineEnhanced hypotensive effect when Diazoxide given with Nifedipine.PhenelzineEnhanced hypotensive effect when Diazoxide gven with MAOIs (e.g.Phenelzine).Phenytoin (Na)PioglitazonePrazosinEnhanced hypotensive effect when Diazoxide given with Prazosin.Propranolol (HCl)Enhanced hypotensive effect when Diazoxide given with Propranolol.Ritodrine (HCl)Diazoxide may potentiate cardiovascular effects of intravenous ritodrine, especially cardiac arrhythmias or hypotension.TerazosinEnhanced hypotensive effect when Diazoxide given with Terazosin.TizanidineEnhanced hypootensive effect when Diazoxide given with Tizanidine.Tranylcypromine (Sulphate)Enhanced hypotensive effect when Diazoxide gven with MAOIs (e.g. Tranylcypromine). These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Fluorimetric Methods of measuring Cortisol in Urine
Risks
Drug should not be given to Pregnant Mothers, and Cardiac / Hypertensive Patients.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Caps, Susp Store in a well closed container, at room temperature, Below 30°C or in refrigerator. Do not Freeze. Protect from Sunlight and Heat.
Warnings
Prolong treatment with diazoxide requires regular monitoring of urine for glucose and ketones, especially under stress conditions. Observed patients closely when initiate the treatment, monitor clinical response and blood glucose until condition of patients is being stabilized. It requires close and frequent blood pressure monitoring. It should be used with caution in patients with impaired cerebral or cardiac circulation.
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