Diazoxide

Identification

Summary

Diazoxide is a non diuretic benzothiadiazine indicated for the management of hypoglycemia in patients who produce an excess of insulin caused by a variety of conditions.

Brand Names
Proglycem
Generic Name
Diazoxide
DrugBank Accession Number
DB01119
Background

Diazoxide is a non-diuretic benzothiadiazine derivative that activates ATP-sensitive potassium channels.5,7 It is chemically related to thiazide diuretics but does not inhibit carbonic anhydrase and does not have chloriuretic or natriuretic activity.1 Diazoxide is commonly used in the treatment of hyperinsulinaemic hypoglycemia due to its ability to inhibit insulin release.5 Diazoxide also exhibits hypotensive activity and reduces arteriolar smooth muscle and vascular resistance.1 When administered intravenously, diazoxide can be used to treat hypertensive emergencies;9 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.5,7

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 230.671
Monoisotopic: 229.991675875
Chemical Formula
C8H7ClN2O2S
Synonyms
  • 7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
  • Diazossido
  • Diazoxide
  • Diazoxido
  • Diazoxidum
External IDs
  • NSC-64198
  • NSC-76130
  • SCH 6783
  • SCH-6783
  • SRG 95213
  • SRG-95213

Pharmacology

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.7 Diazoxide may also be used parentally or intravenously to treat hypertensive emergencies.4,9

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofHyperinsulinemic hypoglycemia••••••••••••••••••••••••••••• ••••••••••
Management ofHyperinsulinemic hypoglycemia••••••••••••••••••••••••••••• ••••••••••
Management ofHyperinsulinemic hypoglycemia••••••••••••••••••••••••••••• ••••••••••
Management ofHyperinsulinemic hypoglycemia••••••••••••••••••••••••••••• ••••••••••
Management ofHyperinsulinemic hypoglycemia••••••••••••••••••••••••••••• ••••••••••
Contraindications & Blackbox Warnings
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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.9 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.7

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.9 Diazoxide administered orally may cause ketoacidosis and nonketotic hyperosmolar coma, especially in patients with other concurrent conditions.7 The use of intravenous or oral diazoxide may lead to the development of pulmonary hypertension in infants and neonates.7,9

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) channel 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.5 Therefore, the use of diazoxide produces an increase in glucose levels.7 Diazoxide is chemically related to thiazide diuretics but does not inhibit carbonic anhydrase and does not have chloriuretic or natriuretic activity.1 It also exhibits hypotensive activity by reducing arteriolar smooth muscle and vascular resistance.1 The mechanism of action of its hypotensive effect has not been fully elucidated; however, it is possible that it involves the antagonism of calcium.9

TargetActionsOrganism
AATP-sensitive inward rectifier potassium channel 11
inducer
Humans
UMitochondrial ATP synthase F1 domain
inhibitor
Humans
Absorption

Diazoxide is readily absorbed following oral administration; however, its absorption depends on the dissolution rate of the dosage form.3 Diazoxide has a bioavailability of 91%.2

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).3 Other sources show that the volume of distribution of diazoxide is 0.21 L/kg.2

Protein binding

The protein binding of diazoxide in normal adults can range from 77% to 94%, depending on the administered dose. In patients with renal failure, protein binding ranges between 77% and 87%. This reduction can be related to the lower levels of albumin in patients with renal failure.3

Metabolism

Diazoxide is metabolized in the liver through oxidation of the 3-methyl group, producing hydroxymethyl (MI) and carboxy (M2) derivatives.3,6 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.3

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.3

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.3

Clearance

In subjects with normal renal function given 300 mg of diazoxide intravenously, renal clearance was 4 ml/min.3 Other sources show that the clearance of diazoxide is 0.06 ml/min/kg.2

Adverse Effects
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Toxicity

The oral LD50 of diazoxide in rats and mice are 980 mg/kg and 444 mg/kg, respectively.8 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.7 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.7

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbaloparatideThe risk or severity of adverse effects can be increased when Diazoxide is combined with Abaloparatide.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Diazoxide.
AcebutololDiazoxide may increase the hypotensive activities of Acebutolol.
AceclofenacThe therapeutic efficacy of Diazoxide can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Diazoxide can be decreased when used in combination with Acemetacin.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Diazoxide choline2U8NRZ7P8L1098065-76-9Not applicable
International/Other Brands
Eudemine (Mercury)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
HyperstatInjection300 mg/20mLIntravenousMerck Sharp & Dohme Limited1973-01-222006-07-31US flag
Hyperstat Inj 15mg/mlLiquid15 mg / mLIntravenousSchering Plough1973-12-312003-07-14Canada flag
ProglycemSuspension50 mg/1mLOralTeva Pharmaceuticals USA, Inc.1990-09-30Not applicableUS flag
ProglycemCapsule100 mgOralMerck Ltd.1985-12-31Not applicableCanada flag
Proglycem Susp 50mg/mlSuspension50 mg / mLOralSchering Plough1984-12-312006-03-23Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DiazoxideSuspension50 mg/1mLOralPar Pharmaceutical, Inc2020-07-21Not applicableUS flag
DiazoxideSuspension50 mg/1mLOralE5 Pharma, Llc2019-12-11Not applicableUS flag
Diazoxide Oral SolutionSuspension50 mg/1mLOralTriRx Huntsville Pharmaceutical Services LLC2023-01-06Not applicableUS flag

Categories

ATC Codes
G01AE10 — Combinations of sulfonamidesC02DA01 — DiazoxideV03AH01 — Diazoxide
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 1,2,4-benzothiadiazine-1,1-dioxides. These are aromatic heterocyclic compounds containing a 1,2,4-benzothiadiazine ring system with two S=O bonds at the 1-position.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Thiadiazines
Sub Class
Benzothiadiazines
Direct Parent
1,2,4-benzothiadiazine-1,1-dioxides
Alternative Parents
Imidolactams / Benzenoids / Aryl chlorides / Organosulfonic acids and derivatives / Azacyclic compounds / Amidines / Organopnictogen compounds / Organochlorides / Organic oxides / Hydrocarbon derivatives
Substituents
1,2,4-benzothiadiazine-1,1-dioxide / Amidine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Hydrocarbon derivative / Imidolactam / Organic nitrogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
sulfone, organochlorine compound, benzothiadiazine (CHEBI:4495)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
O5CB12L4FN
CAS number
364-98-7
InChI Key
GDLBFKVLRPITMI-UHFFFAOYSA-N
InChI
InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11)
IUPAC Name
7-chloro-3-methyl-4H-1lambda6,2,4-benzothiadiazine-1,1-dione
SMILES
CC1=NS(=O)(=O)C2=C(N1)C=CC(Cl)=C2

References

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.

General References
  1. Koch-Weser J: Diazoxide. N Engl J Med. 1976 Jun 3;294(23):1271-3. doi: 10.1056/NEJM197606032942306. [Article]
  2. Kirsten R, Nelson K, Kirsten D, Heintz B: Clinical pharmacokinetics of vasodilators. Part I. Clin Pharmacokinet. 1998 Jun;34(6):457-82. [Article]
  3. 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. [Article]
  4. Vidt DG: Diazoxide for hypertensive crisis. Am Fam Physician. 1975 May;11(5):128-30. [Article]
  5. 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. [Article]
  6. 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. [Article]
  7. FDA Approved Drug Products: Proglycem (diazoxide) oral capsules, suspension [Link]
  8. MSD: Diazoxide (<15%) formulation SDS [Link]
  9. New Zealand Drug Data Sheet: DBL (diazoxide) injection for intravenous use [Link]
Human Metabolome Database
HMDB0015251
KEGG Drug
D00294
KEGG Compound
C06949
PubChem Compound
3019
PubChem Substance
46508027
ChemSpider
2911
BindingDB
86248
RxNav
3327
ChEBI
4495
ChEMBL
CHEMBL181
ZINC
ZINC000003872277
Therapeutic Targets Database
DAP000956
PharmGKB
PA449285
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
20J
Drugs.com
Drugs.com Drug Page
Wikipedia
Diazoxide
PDB Entries
4lv9

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingBasic ScienceHyperglycemia / Metabolism Disorder, Glucose / Type 2 Diabetes Mellitus1
4Active Not RecruitingPreventionHypoglycemia / Hypoglycemia Unawareness / Type 1 Diabetes Mellitus1
4CompletedPreventionType 1 Diabetes Mellitus1
4CompletedTreatmentType 1 Diabetes Mellitus1
4WithdrawnTreatmentGastroenteropancreatic Neuroendocrine Tumors1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Ivax Pharmaceuticals
  • Medisca Inc.
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
SuspensionOral5 g
PowderNot applicable1 g/1g
SuspensionOral50 mg
SolutionIntravenous300.000 mg
InjectionIntravenous300 mg/20mL
LiquidIntravenous15 mg / mL
CapsuleOral25 MG
CapsuleOral100 mg
SuspensionOral50 mg/1mL
SuspensionOral50 mg / mL
Injection, powder, for solutionIntramuscular300 mg/1
Prices
Unit descriptionCostUnit
Proglycem 50 mg/ml Suspension 30ml Bottle197.05USD bottle
Diazoxide powder85.07USD g
Proglycem 100 mg Capsule1.65USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)330ºCTopliss, J.G., Sperber, N. and Rubin, A.A.; U.S. Patent 2,986,573; May 30, 1961; assigned to Schering Corporation. Topliss, J.G., Sperber, N. and Rubin, A.A.; U.S. Patent 3,345,365; October 3, 1967; assigned to Schering Corporation.
water solubility2850 mg/LNot Available
logP1.20HANSCH,C ET AL. (1995)
pKa8.74SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.552 mg/mLALOGPS
logP1.09ALOGPS
logP1Chemaxon
logS-2.6ALOGPS
pKa (Strongest Acidic)14.48Chemaxon
pKa (Strongest Basic)-2.6Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area58.53 Å2Chemaxon
Rotatable Bond Count0Chemaxon
Refractivity54.84 m3·mol-1Chemaxon
Polarizability20.98 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.5923
Caco-2 permeable-0.5765
P-glycoprotein substrateNon-substrate0.6817
P-glycoprotein inhibitor INon-inhibitor0.6924
P-glycoprotein inhibitor IINon-inhibitor0.6927
Renal organic cation transporterNon-inhibitor0.8107
CYP450 2C9 substrateNon-substrate0.5606
CYP450 2D6 substrateNon-substrate0.8064
CYP450 3A4 substrateNon-substrate0.5774
CYP450 1A2 substrateInhibitor0.9108
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7977
Ames testNon AMES toxic0.7888
CarcinogenicityNon-carcinogens0.8304
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3408 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9233
hERG inhibition (predictor II)Non-inhibitor0.9271
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-002f-6950000000-4652e68635ff120be097
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-001i-1790000000-6ba824b6749ffd4b177d
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-01tc-4900000000-771b855118fab0901dba
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0090000000-e862bca94c5672c9f532
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0090000000-23cdf34c4eb3479d62ab
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0590000000-b597fe9df00aeb0e5c42
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-0910000000-2dc8c72c747ff34f5534
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-004i-1900000000-dded4e98b05043368b90
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-0190000000-9f83244458c5cc11c589
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0bu3-1950000000-80f36d9e4aae5c2acf9c
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004l-6900000000-49c0abb20e85be8d5cdc
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004i-9200000000-044096d3b3178a811986
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004i-9000000000-7a02d106750c03894a70
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-0a4l-0980000000-1d3e60eb1a3a4d4a314a
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-1790000000-6ba824b6749ffd4b177d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01tc-4900000000-771b855118fab0901dba
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0190000000-cd76ab2a3c4f8de8e6cd
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0090000000-db250e3d1416295b1046
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0090000000-05266a50e778eb8f82e3
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0090000000-8bbf90d1353050a9bb40
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0930000000-998f4d5207651f9f5640
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-000t-4900000000-7b6b6f2cc0ed1b50d8c6
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-142.7307676
predicted
DarkChem Lite v0.1.0
[M-H]-141.30731
predicted
DeepCCS 1.0 (2019)
[M+H]+143.7884676
predicted
DarkChem Lite v0.1.0
[M+H]+143.69765
predicted
DeepCCS 1.0 (2019)
[M+Na]+142.9699676
predicted
DarkChem Lite v0.1.0
[M+Na]+149.75845
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inducer
Curator comments
Diazoxide binds to the Kir6.2 subunit of the ATP-sensitive K+ channel present in both plasma and mitochondrial membranes.
General Function
Voltage-gated potassium channel activity
Specific Function
This receptor is controlled by G proteins. 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 ...
Gene Name
KCNJ11
Uniprot ID
Q14654
Uniprot Name
ATP-sensitive inward rectifier potassium channel 11
Molecular Weight
43540.375 Da
References
  1. D'hahan N, Moreau C, Prost AL, Jacquet H, Alekseev AE, Terzic A, Vivaudou M: Pharmacological plasticity of cardiac ATP-sensitive potassium channels toward diazoxide revealed by ADP. Proc Natl Acad Sci U S A. 1999 Oct 12;96(21):12162-7. [Article]
  2. Sakura H, Trapp S, Liss B, Ashcroft FM: Altered functional properties of KATP channel conferred by a novel splice variant of SUR1. J Physiol. 1999 Dec 1;521 Pt 2:337-50. [Article]
  3. Shindo T, Katayama Y, Horio Y, Kurachi Y: MCC-134, a novel vascular relaxing agent, is an inverse agonist for the pancreatic-type ATP-sensitive K(+) channel. J Pharmacol Exp Ther. 2000 Jan;292(1):131-5. [Article]
  4. de Lonlay P, Fournet JC, Touati G, Groos MS, Martin D, Sevin C, Delagne V, Mayaud C, Chigot V, Sempoux C, Brusset MC, Laborde K, Bellane-Chantelot C, Vassault A, Rahier J, Junien C, Brunelle F, Nihoul-Fekete C, Saudubray JM, Robert JJ: Heterogeneity of persistent hyperinsulinaemic hypoglycaemia. A series of 175 cases. Eur J Pediatr. 2002 Jan;161(1):37-48. [Article]
  5. Russ U, Lange U, Loffler-Walz C, Hambrock A, Quast U: Binding and effect of K ATP channel openers in the absence of Mg2+. Br J Pharmacol. 2003 May;139(2):368-80. [Article]
  6. Guo W, Chen N, Chen Y, Xia Q, Shen Y: Activation of Mitochondrial ATP-Sensitive Potassium Channel Contributes to Protective Effect in Prolonged Myocardial Preservation. Conf Proc IEEE Eng Med Biol Soc. 2005;4:4027-30. [Article]
  7. Garlid KD, Paucek P, Yarov-Yarovoy V, Murray HN, Darbenzio RB, D'Alonzo AJ, Lodge NJ, Smith MA, Grover GJ: Cardioprotective effect of diazoxide and its interaction with mitochondrial ATP-sensitive K+ channels. Possible mechanism of cardioprotection. Circ Res. 1997 Dec;81(6):1072-82. doi: 10.1161/01.res.81.6.1072. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transmembrane transporter activity
Specific Function
Mitochondrial membrane ATP synthase (F(1)F(0) ATP synthase or Complex V) produces ATP from ADP in the presence of a proton gradient across the membrane which is generated by electron transport comp...

Components:
References
  1. Comelli M, Metelli G, Mavelli I: Downmodulation of mitochondrial F0F1 ATP synthase by diazoxide in cardiac myoblasts: a dual effect of the drug. Am J Physiol Heart Circ Physiol. 2007 Feb;292(2):H820-9. [Article]
  2. Jasova M, Kancirova I, Murarikova M, Farkasova V, Waczulikova I, Ravingerova T, Ziegelhoffer A, Ferko M: Stimulation of mitochondrial ATP synthase activity - a new diazoxide-mediated mechanism of cardioprotection. Physiol Res. 2016 Sep 19;65 Suppl 1:S119-27. doi: 10.33549/physiolres.933411. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. 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. [Article]

Drug created at June 13, 2005 13:24 / Updated at June 23, 2024 23:40