Peringatan Keamanan

The oral LD50 of diazoxide in rats and mice are 980 mg/kg and 444 mg/kg, respectively.L44617 In the mouse, rat, rabbit, dog, pig, and monkey, the oral administration of diazoxide leads to a rapid and transient rise in blood glucose levels. In rats given 400 mg/kg of diazoxide orally during subacute toxicity studies, growth retardation, edema, increases in liver and kidney weights, and adrenal hypertrophy were observed. Rats given doses up to 1080 mg/kg for three months developed hyperglycemia, an increase in liver weight and an increase in mortality.L44612 Toxicity is increased when diazoxide was administered at high dosages concomitantly with either chlorothiazide to rats or trichlormethiazide to dogs. Reproduction and teratology studies in different animal species suggest that diazoxide may interfere with normal fetal development, possibly due to the alteration of glucose metabolism.L44612

Diazoxide

DB01119

small molecule approved

Deskripsi

Diazoxide is a non-diuretic benzothiadiazine derivative that activates ATP-sensitive potassium channels.A255647,L44612 It is chemically related to thiazide diuretics but does not inhibit carbonic anhydrase and does not have chloriuretic or natriuretic activity.A190372 Diazoxide is commonly used in the treatment of hyperinsulinaemic hypoglycemia due to its ability to inhibit insulin release.A255647 Diazoxide also exhibits hypotensive activity and reduces arteriolar smooth muscle and vascular resistance.A190372 When administered intravenously, diazoxide can be used to treat hypertensive emergencies;L44622 however, this specific form of diazoxide is no longer available in the US. Diazoxide is usually well tolerated, and some of its more common side effects include fluid retention and electrolyte disturbances. In September 2015, the FDA issued a safety alert regarding post-marketing reports of pulmonary hypertension occurring in infants and neonates.A255647,L44612

Struktur Molekul 2D

Berat 230.671
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following oral administration, the plasma half-life of diazoxide varies from 9.5 to 24 hours in children with normal renal function and from 20 to 72 hours in adults with normal renal function.[A255627]
Volume Distribusi The apparent volume of distribution of diazoxide in adults with normal renal function is 13 L (21% of body weight), while in children with normal renal function, it is 2 L (33% of body weight).[A255627] Other sources show that the volume of distribution of diazoxide is 0.21 L/kg.[A4660]
Klirens (Clearance) In subjects with normal renal function given 300 mg of diazoxide intravenously, renal clearance was 4 ml/min.[A255627] Other sources show that the clearance of diazoxide is 0.06 ml/min/kg.[A4660]

Absorpsi

Diazoxide is readily absorbed following oral administration; however, its absorption depends on the dissolution rate of the dosage form.A255627 Diazoxide has a bioavailability of 91%.A4660

Metabolisme

Diazoxide is metabolized in the liver through oxidation of the 3-methyl group, producing hydroxymethyl (MI) and carboxy (M2) derivatives.A255627,A255657 The MI derivatives undergo subsequent sulphate conjugation. It is estimated that, in subjects with normal renal function, 54-60% of diazoxide is metabolized. Diazoxide metabolites are inactive and do not contribute to its cardiovascular activity. Additionally, diazoxide metabolites do not displace diazoxide from protein binding sites.A255627

Rute Eliminasi

Diazoxide and its metabolites are mainly eliminated through urine. Since diazoxide is extensively protein-bond, it has a slow excretion and a prolonged half-life. In subjects with normal renal function, the urinary excretion rates of diazoxide peak on the first day after oral administration.A255627

Interaksi Obat

768 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Diazoxide is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Diazoxide is combined with Levodopa.
Risperidone Diazoxide may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Diazoxide.
Amifostine Diazoxide may increase the hypotensive activities of Amifostine.
Valsartan Diazoxide may increase the hypotensive activities of Valsartan.
Ramipril Diazoxide may increase the hypotensive activities of Ramipril.
Esmolol Diazoxide may increase the hypotensive activities of Esmolol.
Betaxolol Diazoxide may increase the hypotensive activities of Betaxolol.
Reserpine Diazoxide may increase the hypotensive activities of Reserpine.
Remikiren Diazoxide may increase the hypotensive activities of Remikiren.
Torasemide Diazoxide may increase the hypotensive activities of Torasemide.
Bethanidine Diazoxide may increase the hypotensive activities of Bethanidine.
Guanadrel Diazoxide may increase the hypotensive activities of Guanadrel.
Metoprolol Diazoxide may increase the hypotensive activities of Metoprolol.
Isradipine Diazoxide may increase the hypotensive activities of Isradipine.
Olmesartan Diazoxide may increase the hypotensive activities of Olmesartan.
Chlorthalidone Diazoxide may increase the hypotensive activities of Chlorthalidone.
Nitroprusside Diazoxide may increase the hypotensive activities of Nitroprusside.
Atenolol Diazoxide may increase the hypotensive activities of Atenolol.
Diltiazem Diazoxide may increase the hypotensive activities of Diltiazem.
Minoxidil Diazoxide may increase the hypotensive activities of Minoxidil.
Timolol Diazoxide may increase the hypotensive activities of Timolol.
Treprostinil Diazoxide may increase the hypotensive activities of Treprostinil.
Amlodipine Diazoxide may increase the hypotensive activities of Amlodipine.
Nimodipine Diazoxide may increase the hypotensive activities of Nimodipine.
Nisoldipine Diazoxide may increase the hypotensive activities of Nisoldipine.
Bendroflumethiazide Diazoxide may increase the hypotensive activities of Bendroflumethiazide.
Prazosin Diazoxide may increase the hypotensive activities of Prazosin.
Fosinopril Diazoxide may increase the hypotensive activities of Fosinopril.
Trandolapril Diazoxide may increase the hypotensive activities of Trandolapril.
Metolazone Diazoxide may increase the hypotensive activities of Metolazone.
Lercanidipine Diazoxide may increase the hypotensive activities of Lercanidipine.
Benazepril Diazoxide may increase the hypotensive activities of Benazepril.
Bosentan Diazoxide may increase the hypotensive activities of Bosentan.
Propranolol Diazoxide may increase the hypotensive activities of Propranolol.
Clonidine Diazoxide may increase the hypotensive activities of Clonidine.
Enalapril Diazoxide may increase the hypotensive activities of Enalapril.
Doxazosin Diazoxide may increase the hypotensive activities of Doxazosin.
Labetalol Diazoxide may increase the hypotensive activities of Labetalol.
Cyclothiazide Diazoxide may increase the hypotensive activities of Cyclothiazide.
Bisoprolol Diazoxide may increase the hypotensive activities of Bisoprolol.
Candoxatril Diazoxide may increase the hypotensive activities of Candoxatril.
Nicardipine Diazoxide may increase the hypotensive activities of Nicardipine.
Guanabenz Diazoxide may increase the hypotensive activities of Guanabenz.
Mecamylamine Diazoxide may increase the hypotensive activities of Mecamylamine.
Losartan Diazoxide may increase the hypotensive activities of Losartan.
Moexipril Diazoxide may increase the hypotensive activities of Moexipril.
Phentolamine Diazoxide may increase the hypotensive activities of Phentolamine.
Eplerenone Diazoxide may increase the hypotensive activities of Eplerenone.
Lisinopril Diazoxide may increase the hypotensive activities of Lisinopril.
Nitroglycerin Diazoxide may increase the hypotensive activities of Nitroglycerin.
Metyrosine Diazoxide may increase the hypotensive activities of Metyrosine.
Hydroflumethiazide Diazoxide may increase the hypotensive activities of Hydroflumethiazide.
Cryptenamine Diazoxide may increase the hypotensive activities of Cryptenamine.
Perindopril Diazoxide may increase the hypotensive activities of Perindopril.
Candesartan cilexetil Diazoxide may increase the hypotensive activities of Candesartan cilexetil.
Tolazoline Diazoxide may increase the hypotensive activities of Tolazoline.
Fenoldopam Diazoxide may increase the hypotensive activities of Fenoldopam.
Indapamide Diazoxide may increase the hypotensive activities of Indapamide.
Tadalafil Diazoxide may increase the hypotensive activities of Tadalafil.
Alprenolol Diazoxide may increase the hypotensive activities of Alprenolol.
Eprosartan Diazoxide may increase the hypotensive activities of Eprosartan.
Chlorothiazide Diazoxide may increase the hypotensive activities of Chlorothiazide.
Quinapril Diazoxide may increase the hypotensive activities of Quinapril.
Omapatrilat Diazoxide may increase the hypotensive activities of Omapatrilat.
Phenoxybenzamine Diazoxide may increase the hypotensive activities of Phenoxybenzamine.
Pindolol Diazoxide may increase the hypotensive activities of Pindolol.
Telmisartan Diazoxide may increase the hypotensive activities of Telmisartan.
Methyldopa Diazoxide may increase the hypotensive activities of Methyldopa.
Hydrochlorothiazide Diazoxide may increase the hypotensive activities of Hydrochlorothiazide.
Guanfacine Diazoxide may increase the hypotensive activities of Guanfacine.
Trichlormethiazide Diazoxide may increase the hypotensive activities of Trichlormethiazide.
Felodipine Diazoxide may increase the hypotensive activities of Felodipine.
Irbesartan Diazoxide may increase the hypotensive activities of Irbesartan.
Nitrendipine Diazoxide may increase the hypotensive activities of Nitrendipine.
Deserpidine Diazoxide may increase the hypotensive activities of Deserpidine.
Pentolinium Diazoxide may increase the hypotensive activities of Pentolinium.
Trimethaphan Diazoxide may increase the hypotensive activities of Trimethaphan.
Carvedilol Diazoxide may increase the hypotensive activities of Carvedilol.
Bretylium Diazoxide may increase the hypotensive activities of Bretylium.
Terazosin Diazoxide may increase the hypotensive activities of Terazosin.
Guanethidine Diazoxide may increase the hypotensive activities of Guanethidine.
Rescinnamine Diazoxide may increase the hypotensive activities of Rescinnamine.
Acebutolol Diazoxide may increase the hypotensive activities of Acebutolol.
Captopril Diazoxide may increase the hypotensive activities of Captopril.
Nadolol Diazoxide may increase the hypotensive activities of Nadolol.
Epoprostenol Diazoxide may increase the hypotensive activities of Epoprostenol.
Bepridil Diazoxide may increase the hypotensive activities of Bepridil.
Hydralazine Diazoxide may increase the hypotensive activities of Hydralazine.
Bevantolol Diazoxide may increase the hypotensive activities of Bevantolol.
Practolol Diazoxide may increase the hypotensive activities of Practolol.
Polythiazide Diazoxide may increase the hypotensive activities of Polythiazide.
Cilazapril Diazoxide may increase the hypotensive activities of Cilazapril.
Saprisartan Diazoxide may increase the hypotensive activities of Saprisartan.
Spirapril Diazoxide may increase the hypotensive activities of Spirapril.
Penbutolol Diazoxide may increase the hypotensive activities of Penbutolol.
Mibefradil Diazoxide may increase the hypotensive activities of Mibefradil.
Oxprenolol Diazoxide may increase the hypotensive activities of Oxprenolol.
Pargyline Diazoxide may increase the hypotensive activities of Pargyline.

Target Protein

ATP-sensitive inward rectifier potassium channel 11 KCNJ11
Mitochondrial ATP synthase F1 domain ATP5F1A

Referensi & Sumber

Synthesis reference: Topliss, J.G., Sperber, N. and Rubin, A.A. U.S. Patent 2,986,573; May 30, 1961; assigned to Schering Corporation. https://patentimages.storage.googleapis.com/a7/52/ac/b4aae51fc2087d/US2986573.pdf Topliss, J.G., Sperber, N. and Rubin, A.A.; U.S. Patent 3,345,365; October 3, 1967; assigned to Schering Corporation.
Artikel (PubMed)
  • PMID: 772431
    Koch-Weser J: Diazoxide. N Engl J Med. 1976 Jun 3;294(23):1271-3. doi: 10.1056/NEJM197606032942306.
  • PMID: 9646008
    Kirsten R, Nelson K, Kirsten D, Heintz B: Clinical pharmacokinetics of vasodilators. Part I. Clin Pharmacokinet. 1998 Jun;34(6):457-82.
  • PMID: 328207
    Pearson RM: Pharmacokinetics and response to diazoxide in renal failure. Clin Pharmacokinet. 1977 May-Jun;2(3):198-204. doi: 10.2165/00003088-197702030-00004.
  • PMID: 1130248
    Vidt DG: Diazoxide for hypertensive crisis. Am Fam Physician. 1975 May;11(5):128-30.
  • PMID: 31520536
    Chen SC, Dastamani A, Pintus D, Yau D, Aftab S, Bath L, Swinburne C, Hunter L, Giardini A, Christov G, Senniappan S, Banerjee I, Shaikh MG, Shah P: Diazoxide-induced pulmonary hypertension in hyperinsulinaemic hypoglycaemia: Recommendations from a multicentre study in the United Kingdom. Clin Endocrinol (Oxf). 2019 Dec;91(6):770-775. doi: 10.1111/cen.14096. Epub 2019 Oct 1.
  • PMID: 238822
    Dayton PG, Pruitt AW, Faraj BA, Israili ZH: Metabolism and disposition of diazoxide. A mini-review. Drug Metab Dispos. 1975 May-Jun;3(3):226-9.

Contoh Produk & Brand

Produk: 10 • International brands: 1
Produk
  • Diazoxide
    Powder • 1 g/1g • Not applicable • US
  • Diazoxide
    Suspension • 50 mg/1mL • Oral • US • Generic • Approved
  • Diazoxide
    Suspension • 50 mg/1mL • Oral • US • Generic • Approved
  • Diazoxide Oral Solution
    Suspension • 50 mg/1mL • Oral • US • Generic • Approved
  • Hyperstat
    Injection • 300 mg/20mL • Intravenous • US • Approved
  • Hyperstat Inj 15mg/ml
    Liquid • 15 mg / mL • Intravenous • Canada • Approved
  • Proglycem
    Suspension • 50 mg/1mL • Oral • US • Approved
  • Proglycem
    Capsule • 100 mg • Oral • Canada • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Eudemine — Mercury

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