Diazoxide 20mg/5ml oral solution
Prescription only
Requires a prescription from a doctor or prescriber
Oral solution
20mg/5ml
Oral
Drugs used in diabetes
Active ingredients:
Diazoxide
1 safety notice
Safety information for pregnancy and breastfeeding
Pregnancy
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]
Always consult your doctor or midwife before taking any medicine during pregnancy or while breastfeeding. Source: DrugBank (CC BY-NC 4.0).
Official documents, adverse reaction reporting, and safety monitoring
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Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Diazoxide
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Report a side effect
Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
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Suspected adverse reactions reported for Diazoxide
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Learn about EU pharmacovigilance and safety monitoring
EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
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Same therapeutic group
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
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Clinical guidelines and formulary information
British National Formulary
Diazoxide
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & product information
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
11 found
Half-life
9.5 to 24 hours
Mechanism
Diazoxide is a nondiuretic benzothiadiazine derivative used for the management of symptomatic hypoglycemia.
Food interactions
None known
Human targets
2 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
91%
Diazoxide is readily absorbed following oral administration; however, its absorption depends on the dissolution rate of the dosage form.
[A255627]…
[A255627]…
Half-life
9.5 to 24 hours
Following oral administration, the plasma half-life of diazoxide varies from 9.5…
Protein binding
91-93%
Diazoxide is highly (91-93%) protein-bound in plasma, primarily to albumin.
[L52720]
[L52720]
Volume of distribution
13 L
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]…
[A255627]…
Metabolism
54-60%
Diazoxide is mainly metabolized by CYP1A2 and to a minor extent by CYP3A4, producing hydroxymethyl (MI) and carboxy (M2) derivatives.
[L52720][A255627][A255657]…
[L52720][A255627][A255657]…
Elimination
Diazoxide and its metabolites are mainly eliminated through urine.…
Clearance
300 mg
In subjects with normal renal function given 300 mg of diazoxide intravenously, renal clearance was 4 ml/min.
[A255627]…
[A255627]…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
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]
In March 2025, an extended-release formulation of diazoxide choline was approved by the FDA for the treatment of hyperphagia in patients with Prader-Willi syndrome, becoming the first FDA-approved therapy for this condition.[L52720][L52725]
In March 2025, an extended-release formulation of diazoxide choline was approved by the FDA for the treatment of hyperphagia in patients with Prader-Willi syndrome, becoming the first FDA-approved therapy for this condition.[L52720][L52725]
Properties:
solid
Avg. mass: 230.67 Da
DrugBank indication
Oral diazoxide is indicated to manage hypoglycemia due to hyperinsulinism associated with conditions such as inoperable islet cell adenoma or carcinoma, and extrapancreatic malignancy in adults, or leucine sensitivity, islet cell hyperplasia, nesidioblastosis, extrapancreatic malignancy, islet cell adenoma, and adenomatosis in infants and children. In infants and children oral diazoxide may be used preoperatively as a temporary measure, and postoperatively, if hypoglycemia persists.
[L44612]
Diazoxide may also be used parentally or intravenously to treat hypertensive emergencies.
[A255632][L44622]
In addition, extended-release diazoxide choline is indicated for the treatment of hyperphagia in adults and pediatric patients 4 years of age and older with Prader-Willi syndrome (PWS).
[L52720]
[L44612]
Diazoxide may also be used parentally or intravenously to treat hypertensive emergencies.
[A255632][L44622]
In addition, extended-release diazoxide choline is indicated for the treatment of hyperphagia in adults and pediatric patients 4 years of age and older with Prader-Willi syndrome (PWS).
[L52720]
Also known as(79)
7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
Diazossido
Diazoxide
Diazoxido
Diazoxidum
IKATP
Inward rectifier K(+) channel Kir6.2
Potassium channel, inwardly rectifying subfamily J member 11
Dosage forms(14)
Powder (Not applicable) — 1 g/1g
Suspension (Oral) — 50 mg
Solution (Intravenous) — 300.000 mg
Injection (Intravenous) — 300 mg/20mL
Liquid (Intravenous) — 15 mg / mL
Capsule (Oral) — 25 MG
Capsule (Oral) — 100 mg
Suspension (Oral) — 50 mg/1mL
Molecular properties(19)
Drug interactions(1088)
Known interactions with other medications. Always consult a healthcare professional.
Duloxetine
Major
The risk or severity of orthostatic hypotension and syncope can be increased when Diazoxide is combined with Duloxetine.
The risk or severity of hypotension and orthostatic hypotension can be increased when Diazoxide is combined with Levodopa.
Risperidone
Moderate
Diazoxide may increase the hypotensive activities of Risperidone.
Alfuzosin may increase the hypotensive activities of Diazoxide.
Amifostine
Moderate
Diazoxide may increase the hypotensive activities of Amifostine.
Diazoxide may increase the hypotensive activities of Valsartan.
Diazoxide may increase the hypotensive activities of Ramipril.
Diazoxide may increase the hypotensive activities of Esmolol.
Diazoxide may increase the hypotensive activities of Betaxolol.
Diazoxide may increase the hypotensive activities of Reserpine.
Diazoxide may increase the hypotensive activities of Remikiren.
Torasemide
Moderate
Diazoxide may increase the hypotensive activities of Torasemide.
Bethanidine
Moderate
Diazoxide may increase the hypotensive activities of Bethanidine.
Diazoxide may increase the hypotensive activities of Guanadrel.
Metoprolol
Moderate
Diazoxide may increase the hypotensive activities of Metoprolol.
Isradipine
Moderate
Diazoxide may increase the hypotensive activities of Isradipine.
Olmesartan
Moderate
Diazoxide may increase the hypotensive activities of Olmesartan.
Chlorthalidone
Moderate
Diazoxide may increase the hypotensive activities of Chlorthalidone.
Nitroprusside
Moderate
Diazoxide may increase the hypotensive activities of Nitroprusside.
Diazoxide may increase the hypotensive activities of Atenolol.
Diazoxide may increase the hypotensive activities of Diltiazem.
Diazoxide may increase the hypotensive activities of Minoxidil.
Diazoxide may increase the hypotensive activities of Timolol.
Treprostinil
Moderate
Diazoxide may increase the hypotensive activities of Treprostinil.
Amlodipine
Moderate
Diazoxide may increase the hypotensive activities of Amlodipine.
Nimodipine
Moderate
Diazoxide may increase the hypotensive activities of Nimodipine.
Nisoldipine
Moderate
Diazoxide may increase the hypotensive activities of Nisoldipine.
Bendroflumethiazide
Moderate
Diazoxide may increase the hypotensive activities of Bendroflumethiazide.
Diazoxide may increase the hypotensive activities of Prazosin.
Fosinopril
Moderate
Diazoxide may increase the hypotensive activities of Fosinopril.
Trandolapril
Moderate
Diazoxide may increase the hypotensive activities of Trandolapril.
Metolazone
Moderate
Diazoxide may increase the hypotensive activities of Metolazone.
Lercanidipine
Moderate
Diazoxide may increase the hypotensive activities of Lercanidipine.
Benazepril
Moderate
Diazoxide may increase the hypotensive activities of Benazepril.
Diazoxide may increase the hypotensive activities of Bosentan.
Propranolol
Moderate
Diazoxide may increase the hypotensive activities of Propranolol.
Diazoxide may increase the hypotensive activities of Clonidine.
Diazoxide may increase the hypotensive activities of Enalapril.
Diazoxide may increase the hypotensive activities of Doxazosin.
Diazoxide may increase the hypotensive activities of Labetalol.
Cyclothiazide
Moderate
Diazoxide may increase the hypotensive activities of Cyclothiazide.
Bisoprolol
Moderate
Diazoxide may increase the hypotensive activities of Bisoprolol.
Candoxatril
Moderate
Diazoxide may increase the hypotensive activities of Candoxatril.
Nicardipine
Moderate
Diazoxide may increase the hypotensive activities of Nicardipine.
Diazoxide may increase the hypotensive activities of Guanabenz.
Mecamylamine
Moderate
Diazoxide may increase the hypotensive activities of Mecamylamine.
Diazoxide may increase the hypotensive activities of Losartan.
Diazoxide may increase the hypotensive activities of Moexipril.
Phentolamine
Moderate
Diazoxide may increase the hypotensive activities of Phentolamine.
Eplerenone
Moderate
Diazoxide may increase the hypotensive activities of Eplerenone.
Showing 50 of 1088 interactions
Toxicity & overdose
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]
[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]
How it works
Mechanism of action
Diazoxide is a nondiuretic benzothiadiazine derivative used for the management of symptomatic hypoglycemia. By binding to the sulfonylurea receptor (SUR) subunit of the ATP-sensitive potassium channel (KATP) on the membrane of pancreatic beta‐cells, diazoxide promotes a potassium efflux from beta-cells. This hyperpolarizes the cell membrane and prevents the influx of calcium to the pancreatic beta‐cells. Without a sufficient amount of calcium in the cell, insulin release is inhibited.[A255647] Therefore, the use of diazoxide produces an increase in glucose levels.[L44612] Diazoxide is chemically related to thiazide diuretics but does not inhibit carbonic anhydrase and does not have chloriuretic or natriuretic activity.[A190372] It also exhibits hypotensive activity by reducing arteriolar smooth muscle and vascular resistance.[A190372] The mechanism of action of its hypotensive effect has not been fully elucidated; however, it is possible that it involves the antagonism of calcium.[L44622]
Pharmacodynamics
Diazoxide is a potassium channel activator that enhances cell membrane permeability to potassium ions. By promoting a vasodilatory effect on the smooth muscle in peripheral arterioles, diazoxide lowers blood pressure and peripheral vascular resistance. Diazoxide-induced decreases in blood pressure lead to reflex increases in heart rate and cardiac output.[L44622] The oral administration of diazoxide increases blood glucose in a dose-dependent manner. In patients with normal renal function, this effect is observed within an hour and lasts no more than eight hours. The hypotensive effects of diazoxide are usually not detected when administered orally.[L44612]
Diazoxide administered intravenously may lead to sodium and water retention, severe hypotension, transient myocardial or cerebral ischaemia and gastrointestinal upsets such as nausea, vomiting and abdominal discomfort.[L44622] Diazoxide administered orally may cause ketoacidosis and nonketotic hyperosmolar coma, especially in patients with other concurrent conditions.[L44612] The use of intravenous or oral diazoxide may lead to the development of pulmonary hypertension in infants and neonates.[L44612][L44622]
Diazoxide administered intravenously may lead to sodium and water retention, severe hypotension, transient myocardial or cerebral ischaemia and gastrointestinal upsets such as nausea, vomiting and abdominal discomfort.[L44622] Diazoxide administered orally may cause ketoacidosis and nonketotic hyperosmolar coma, especially in patients with other concurrent conditions.[L44612] The use of intravenous or oral diazoxide may lead to the development of pulmonary hypertension in infants and neonates.[L44612][L44622]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
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]
[A255627]
Diazoxide has a bioavailability of 91%.
[A4660]
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]
[A255627]
Protein binding
Diazoxide is highly (91-93%) protein-bound in plasma, primarily to albumin.
[L52720]
[L52720]
Volume of distribution
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]
[A255627]
Other sources show that the volume of distribution of diazoxide is 0.21 L/kg.
[A4660]
Metabolism
Diazoxide is mainly metabolized by CYP1A2 and to a minor extent by CYP3A4, producing hydroxymethyl (MI) and carboxy (M2) derivatives.
[L52720][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]
In patients with Prader-Willi syndrome, only metabolite M1 (3-hydroxymethyl-7-chloro-1,2,4- benzothiadiazine-1,1-dioxide) is detectable in circulation.
[L52720]
[L52720][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]
In patients with Prader-Willi syndrome, only metabolite M1 (3-hydroxymethyl-7-chloro-1,2,4- benzothiadiazine-1,1-dioxide) is detectable in circulation.
[L52720]
Route of elimination
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]
[A255627]
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]
[A255627]
Other sources show that the clearance of diazoxide is 0.06 ml/min/kg.
[A4660]
Drug targets(2)
Proteins and enzymes this drug interacts with in the body
ATP-sensitive inward rectifier potassium channel 11
KCNJ11
inducer
Specific functionankyrin binding
Cellular location
Membrane
General function & pharmacology
Inward rectifier potassium channel that forms the pore of ATP-sensitive potassium channels (KATP), regulating potassium permeability as a function of cytoplasmic ATP and ADP concentrations in many different cells .
PMID:29286281 PMID:34815345
Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium.
Can be blocked by extracellular barium (By similarity). In pancreatic cells, it forms KATP channels with ABCC8/SUR1 .
PMID:29286281 PMID:34815345
Can form cardiac and smooth muscle-type KATP channels with ABCC9
PMID:29286281 PMID:34815345
Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium.
Can be blocked by extracellular barium (By similarity). In pancreatic cells, it forms KATP channels with ABCC8/SUR1 .
PMID:29286281 PMID:34815345
Can form cardiac and smooth muscle-type KATP channels with ABCC9
ATP synthase peripheral stalk subunit OSCP, mitochondrial
ATP5PO
inhibitor
Specific functionATP hydrolysis activity
Cellular location
Mitochondrion
General function & pharmacology
Subunit OSCP, of the mitochondrial membrane ATP synthase complex (F(1)F(0) ATP synthase or Complex V) that produces ATP from ADP in the presence of a proton gradient across the membrane which is generated by electron transport complexes of the respiratory chain .
PMID:37244256
ATP synthase complex consist of a soluble F(1) head domain - the catalytic core - and a membrane F(1) domain - the membrane proton channel .
PMID:37244256
These two domains are linked by a central stalk rotating inside the F(1) region and a stationary peripheral stalk .
PMID:37244256
During catalysis, ATP synthesis in the catalytic domain of F(1) is coupled via a rotary mechanism of the central stalk subunits to proton translocation (Probable). In vivo, can only synthesize ATP although its ATP hydrolase activity can be activated artificially in vitro (By similarity). Part of the complex F(0) domain .
PMID:37244256
Part of the complex F(0) domain and the peripheric stalk, which acts as a stator to hold the catalytic alpha(3)beta(3) subcomplex and subunit a/ATP6 static relative to the rotary elements (By similarity)
PMID:37244256
ATP synthase complex consist of a soluble F(1) head domain - the catalytic core - and a membrane F(1) domain - the membrane proton channel .
PMID:37244256
These two domains are linked by a central stalk rotating inside the F(1) region and a stationary peripheral stalk .
PMID:37244256
During catalysis, ATP synthesis in the catalytic domain of F(1) is coupled via a rotary mechanism of the central stalk subunits to proton translocation (Probable). In vivo, can only synthesize ATP although its ATP hydrolase activity can be activated artificially in vitro (By similarity). Part of the complex F(0) domain .
PMID:37244256
Part of the complex F(0) domain and the peripheric stalk, which acts as a stator to hold the catalytic alpha(3)beta(3) subcomplex and subunit a/ATP6 static relative to the rotary elements (By similarity)
Metabolizing enzymes(2)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP1A2Cytochrome P450 1A2
substrate
inhibitor
CYP3A4Cytochrome P450 3A4
substrate
Transporters(3)
Proteins that transport this drug across cell membranes
Solute carrier family 22 member 6
SLC22A6
substrate
inhibitor
Specific functionalpha-ketoglutarate transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate .
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
Organic anion transporter 3
SLC22A8
substrate
inhibitor
Specific functionorganic anion transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient .
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
substrate
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
Carriers(1)
Proteins that carry this drug through the body
Albumin
ALB
binder
Specific functionantioxidant activity
Cellular location
Secreted
General function & pharmacology
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc .
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).
Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).
Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017
Scientific references(6)
Koch-Weser J.
Diazoxide.
New England Journal of Medicine
1976 Jun 3294(23):1271-3. doi: 10.1056/NEJM197606032942306
Kirsten R., Nelson K., Kirsten D., Heintz B.
Clinical Pharmacokinetics of Vasodilators.
Clinical Pharmacokinetics
199834(6):457-482. doi: 10.2165/00003088-199834060-00003
Pearson R.M.
Pharmacokinetics and response to diazoxide in renal failure.
Clinical Pharmacokinetics
1977 May-Jun2(3):198-204. doi: 10.2165/00003088-197702030-00004
Vidt D.G.
Treatment of Malignant Hypertension and Hypertensive Crisis. Hypertension, Cardiovascular Disease, Analgesics, and Endocrine Disorders. 1981;:29-36. doi: 10.
1016/b978-0-12-788950-4
50010-8
Chen S.C., Dastamani A., Pintus D., Yau D., Aftab S., Bath L., Swinburne C., Hunter L., Giardini A., Christov G., Senniappan S., Banerjee I., Shaikh M.G., Shah P.
Diazoxide-induced pulmonary hypertension in hyperinsulinaemic hypoglycaemia: Recommendations from a multicentre study in the United Kingdom.
Clinical Endocrinol (Oxf)
2019 Dec91(6):770-775. doi: 10.1111/cen.14096. Epub 2019 Oct 1
Dayton P.G., Pruitt A.W., Faraj B.A., Israili Z.H.
METABOLISM AND DISPOSITION OF DIAZOXIDEA Mini-Review.
Drug Metabolism and Disposition
19753(3):226-229. doi: 10.1016/s0090-9556(25)05717-4
ATC classification(3 codes)
ATC G01AE10
ATC C02DA01
ATC V03AH01
Affected organisms(1)
Humans and other mammals
International brands(1)
Salt forms(1)
Diazoxide choline(DBSALT003365)
Experimental properties(4)
External resources(1)
Protein Data Bank entries(1)
Commercial products(13)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Diazoxide
Additional database identifiers
Drugs Product Database (DPD)
9557
ChemSpider
2911
BindingDB
50237612
PDB
20J
Guide to Pharmacology
2409
ZINC
ZINC000003872277
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6257
GenAtlas
KCNJ11
GeneCards
KCNJ11
GenBank Gene Database
D50582
GenBank Protein Database
1088445
UniProt Accession
KCJ11_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:823
GeneCards
ATP5F1A
GenBank Gene Database
X59066
GenBank Protein Database
28938
UniProt Accession
ATPA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:830
GeneCards
ATP5F1B
GenBank Gene Database
X03559
GenBank Protein Database
28940
UniProt Accession
ATPB_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:837
GenAtlas
ATP5D
GeneCards
ATP5F1D
GenBank Gene Database
X63422
GenBank Protein Database
12586
UniProt Accession
ATPD_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:838
GeneCards
ATP5F1E
UniProt Accession
ATP5E_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:833
GeneCards
ATP5F1C
GenBank Gene Database
D16562
GenBank Protein Database
665586
UniProt Accession
ATPG_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:850
GeneCards
ATP5PO
UniProt Accession
ATPO_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2596
GenAtlas
CYP1A2
GeneCards
CYP1A2
GenBank Gene Database
Z00036
Guide to Pharmacology
1319
UniProt Accession
CP1A2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:399
GenAtlas
ALB
GeneCards
ALB
GenBank Gene Database
V00494
GenBank Protein Database
28590
UniProt Accession
ALBU_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10970
GenAtlas
hROAT1
GeneCards
SLC22A6
GenBank Gene Database
AF057039
GenBank Protein Database
3831566
Guide to Pharmacology
1025
UniProt Accession
S22A6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10972
GeneCards
SLC22A8
GenBank Gene Database
AF097491
GenBank Protein Database
4378059
Guide to Pharmacology
1027
UniProt Accession
S22A8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
International reference pricing
3 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $1.65/capsule
To $197.05/bottle
Proglycem 100 mg Capsule
$1.65/capsule
Diazoxide powder
$85.07/g
Proglycem 50 mg/ml Suspension 30ml Bottle
$197.05/bottle
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
6 active patents
12178823
United States
Approved 12 Nov 2015 · Expires 12 Nov 2035
9y 7m
9757384
United States
Approved 12 Nov 2015 · Expires 12 Nov 2035
9y 7m
12343348
United States
Approved 12 Nov 2015 · Expires 12 Nov 2035
9y 7m
12419895
United States
Approved 12 Nov 2015 · Expires 12 Nov 2035
9y 7m
7799777
United States
Approved 5 Mar 2009 · Expires 5 Mar 2029
2y 11m
The earliest active patent expires December 2026. Generic versions may become available after this date.
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 27 days ago(8 Mar 2026)