Details of the Drug

General Information of Drug (ID: DML1538)

Drug Name

Diazoxide

Synonyms

Aroglycem; Diazossido; Diazoxido; Diazoxidum; Dizoxide; Eudemine; Hyperstat; Hypertonalum; Mutabase; Proglicem; Proglycem; Diazossido [DCIT]; Diazossido [Italian]; D 9035; SRG 95213; Sch 6783; Diazoxido [INN-Spanish]; Diazoxidum [INN-Latin]; Hyperstat (TN); SRG-95213; Sch-6783; Diazoxide [USAN:INN:BAN]; Diazoxide (JAN/USP/INN); 2H-1,2, 4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide; 2H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide; 7-Chloro-3-methyl-1lambda~4~,2,4-benzothiadiazin-1-ol 1-oxide; 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide; 7-Cloro-3-metil-2H-1,2,4-benzotiodiazina-1,1-diossido; 7-Cloro-3-metil-2H-1,2,4-benzotiodiazina-1,1-diossido [Italian]; 7-chloro-3-methyl-4H-1

Indication

Disease Entry	ICD 11	Status	REF
Congenital hyperinsulinism	5A4Y	Approved	[1]
Hyperinsulinemia	5A4Y	Approved	[1]
Hypertension	BA00-BA04	Approved	[2]
Hypertensive emergency	BA03	Approved	[1]
Insulinoma	2C10.1	Approved	[1]
Malignant essential hypertension	BA00	Approved	[1]
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Therapeutic Class

Antihypertensive Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

230.67

Logarithm of the Partition Coefficient (xlogp)

1.2

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption: The drug is rapidly absorbed following oral administration []
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Bioavailability: 90% of drug becomes completely available to its intended biological destination(s) [4]
Clearance: The drug present in the plasma can be removed from the body at the rate of 0.06 mL/min/kg [5]
Elimination: 35% of drug is excreted from urine in the unchanged form [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 28 +/- 8.3 hours [5]
Metabolism: The drug is metabolized via the hepatic []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 34.68095 micromolar/kg/day [6]
Unbound Fraction: The unbound fraction of drug in plasma is 0.06% [5]
Vd: Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.21 L/kg [5]
Water Solubility: The ability of drug to dissolve in water is measured as 0.15 mg/mL [3]

Chemical Identifiers

Formula: C8H7ClN2O2S
IUPAC Name: 7-chloro-3-methyl-4H-1lambda6,2,4-benzothiadiazine 1,1-dioxide
Canonical SMILES: CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl
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)
InChIKey: GDLBFKVLRPITMI-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 3019
ChEBI ID: CHEBI:4495
CAS Number: 364-98-7
DrugBank ID: DB01119
TTD ID: D07WEP
ACDINA ID: D01001

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Potassium channel unspecific (KC)	TT1VOHK	NOUNIPROTAC	Modulator	[7]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
ATP-sensitive inward rectifier potassium channel 11 (KCNJ11)	OTPUUELV	KCJ11_HUMAN	Gene/Protein Processing	[8]
Bcl-2-like protein 1 (BCL2L1)	OTRC5K9O	B2CL1_HUMAN	Gene/Protein Processing	[9]
Catenin beta-1 (CTNNB1)	OTZ932A3	CTNB1_HUMAN	Gene/Protein Processing	[10]
G1/S-specific cyclin-D1 (CCND1)	OT8HPTKJ	CCND1_HUMAN	Gene/Protein Processing	[10]
Interleukin-10 (IL10)	OTIRFRXC	IL10_HUMAN	Protein Interaction/Cellular Processes	[11]
Interleukin-6 (IL6)	OTUOSCCU	IL6_HUMAN	Protein Interaction/Cellular Processes	[11]
Nuclear factor NF-kappa-B p105 subunit (NFKB1)	OTNRRD8I	NFKB1_HUMAN	Gene/Protein Processing	[9]
Tumor necrosis factor (TNF)	OT4IE164	TNFA_HUMAN	Protein Interaction/Cellular Processes	[11]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Diazoxide (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Cariprazine	DMJYDVK	Moderate	Additive hypotensive effects by the combination of Diazoxide and Cariprazine.	Bipolar disorder [6A60]	[12]
Isocarboxazid	DMAF1NB	Moderate	Additive hypotensive effects by the combination of Diazoxide and Isocarboxazid.	Depression [6A70-6A7Z]	[13]
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of Diazoxide and OPC-34712.	Depression [6A70-6A7Z]	[12]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Diazoxide caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[14]
Procarbazine	DMIK367	Moderate	Additive hypotensive effects by the combination of Diazoxide and Procarbazine.	Hodgkin lymphoma [2B30]	[13]
ITI-007	DMUQ1DO	Moderate	Additive hypotensive effects by the combination of Diazoxide and ITI-007.	Insomnia [7A00-7A0Z]	[12]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of Diazoxide and Ozanimod.	Multiple sclerosis [8A40]	[13]
Safinamide	DM0YWJC	Moderate	Additive hypotensive effects by the combination of Diazoxide and Safinamide.	Parkinsonism [8A00]	[13]
Rasagiline	DM3WKQ4	Moderate	Additive hypotensive effects by the combination of Diazoxide and Rasagiline.	Parkinsonism [8A00]	[13]
Levomepromazine	DMIKFEL	Moderate	Additive hypotensive effects by the combination of Diazoxide and Levomepromazine.	Psychotic disorder [6A20-6A25]	[12]
Quetiapine	DM1N62C	Moderate	Additive hypotensive effects by the combination of Diazoxide and Quetiapine.	Schizophrenia [6A20]	[12]
Aripiprazole	DM3NUMH	Moderate	Additive hypotensive effects by the combination of Diazoxide and Aripiprazole.	Schizophrenia [6A20]	[12]
Iloperidone	DM6AUFY	Moderate	Additive hypotensive effects by the combination of Diazoxide and Iloperidone.	Schizophrenia [6A20]	[12]
Paliperidone	DM7NPJS	Moderate	Additive hypotensive effects by the combination of Diazoxide and Paliperidone.	Schizophrenia [6A20]	[12]
Molindone	DMAH70G	Moderate	Additive hypotensive effects by the combination of Diazoxide and Molindone.	Schizophrenia [6A20]	[12]
Thiothixene	DMDINC4	Moderate	Additive hypotensive effects by the combination of Diazoxide and Thiothixene.	Schizophrenia [6A20]	[12]
Amisulpride	DMSJVAM	Moderate	Additive hypotensive effects by the combination of Diazoxide and Amisulpride.	Schizophrenia [6A20]	[12]
Asenapine	DMSQZE2	Moderate	Additive hypotensive effects by the combination of Diazoxide and Asenapine.	Schizophrenia [6A20]	[12]
Trimeprazine	DMEMV9D	Moderate	Additive hypotensive effects by the combination of Diazoxide and Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[15]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
Hydrochloric acid	E00015	313	Acidulant
methylparaben	E00149	7456	Antimicrobial preservative
Propylparaben sodium	E00567	23679044	Antimicrobial preservative
Sodium benzoate	E00432	517055	Antimicrobial preservative; lubricant
Sunset yellow FCF	E00255	17730	Colorant
Carboxymethylcellulose sodium	E00621	Not Available	Adsorbent; Binding agent; Disintegrant; Emulsifying agent; Suspending agent; Viscosity-controlling agent
Ethanol	E00023	702	Antimicrobial preservative; Penetration agent; Solvent
Magnesium aluminum silicate	E00462	3084116	Adsorbent; Binding agent; Disintegrant; Suspending agent; Viscosity-controlling agent
Poloxamer 188	E00645	Not Available	Emulsifying agent; Solubilizing agent; Surfactant
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Sodium hydroxide	E00234	14798	Alkalizing agent
Water	E00035	962	Solvent
Sorbitan tristearate	E00516	17800859	Dispersing agent; Emulsifying agent; Solubilizing agent; Surfactant; Suspending agent; Vaccine adjuvant
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Diazoxide 1.5g/30ml suspension	1.5g/30ml	Suspension	Oral

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References

1	Diazoxide FDA Label
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2409).
3	BDDCS applied to over 900 drugs
4	Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
5	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6	Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
7	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8	Combined contributions of over-secreted glucagon-like peptide 1 and suppressed insulin secretion to hyperglycemia induced by gatifloxacin in rats. Toxicol Appl Pharmacol. 2013 Feb 1;266(3):375-84. doi: 10.1016/j.taap.2012.11.015. Epub 2012 Nov 28.
9	Diazoxide-mediated preconditioning against apoptosis involves activation of cAMP-response element-binding protein (CREB) and NFkappaB. J Biol Chem. 2004 Nov 5;279(45):46748-54. doi: 10.1074/jbc.M406217200. Epub 2004 Aug 23.
10	Diazoxide-mediated growth inhibition in human lung cancer cells via downregulation of beta-catenin-mediated cyclin D1 transcription. Lung. 2009 Jan-Feb;187(1):61-7. doi: 10.1007/s00408-008-9127-1. Epub 2008 Dec 4.
11	Antihypertensive drugs clonidine, diazoxide, hydralazine and furosemide regulate the production of cytokines by placentas and peripheral blood mononuclear cells in normal pregnancy. J Hypertens. 2006 May;24(5):915-22. doi: 10.1097/01.hjh.0000222762.84605.03.
12	Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
13	Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]
14	Petro DJ, Vannucci RC, Kulin HE "Diazoxide-diphenylhydantoin interaction." J Pediatr 89 (1976): 331-2. [PMID: 940040]
15	Product Information. Clozaril (clozapine). Novartis Pharmaceuticals, East Hanover, NJ.