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Identification
NameMethazolamide
Accession NumberDB00703  (APRD00740)
TypeSmall Molecule
GroupsApproved
DescriptionA carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. [PubChem]
Structure
Thumb
Synonyms
Metazolamida
Methazolamid
Méthazolamide
Methazolamidum
Methenamide
Neptazane
Neptazaneat
External Identifiers
  • L 584601
  • L-584601
  • VVP-808
  • VVP808
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MethazolamideTablet50 mgOralAa Pharma Inc2002-07-25Not applicableCanada
Neptazane Tablets 25mgTablet25 mgOralWyeth Ayerst Canada Inc.1998-07-242000-08-02Canada
Neptazane Tablets 25mg USPTablet25 mgOralStorz, Division Of Wyeth Ayerst Canada Inc.1995-12-311999-08-12Canada
Neptazane Tablets 50mgTablet50 mgOralWyeth Ayerst Canada Inc.1998-12-232002-05-17Canada
Neptazane Tablets 50mgTablet50 mgOralStorz, Division Of Wyeth Ayerst Canada Inc.1993-12-311999-08-12Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MethazolamideTablet50 mg/1OralCarilion Materials Management2010-06-22Not applicableUs
MethazolamideTablet50 mg/1OralEffcon Laboratories, Inc.1994-07-18Not applicableUs
MethazolamideTablet50 mg/1OralSandoz Inc1993-06-30Not applicableUs
MethazolamideTablet25 mg/1OralFera Pharmaceuticals2010-06-222016-11-15Us
MethazolamideTablet25 mg/1OralEffcon Laboratories, Inc.1994-07-14Not applicableUs
MethazolamideTablet25 mg/1OralSandoz Inc1993-06-30Not applicableUs
MethazolamideTablet50 mg/1OralFera Pharmaceuticals2010-06-222016-11-15Us
MethazolamideTablet25 mg/1OralPaddock Laboratories, LLC2014-09-30Not applicableUs
MethazolamideTablet25 mg/1OralANI Pharmaceuticals, Inc.2014-11-06Not applicableUs
MethazolamideTablet50 mg/1OralPhysicians Total Care, Inc.2006-12-12Not applicableUs
MethazolamideTablet50 mg/1OralPaddock Laboratories, LLC2014-09-30Not applicableUs
MethazolamideTablet50 mg/1OralANI Pharmaceuticals, Inc.2014-11-06Not applicableUs
NeptazaneTablet50 mg/1OralFera Pharmaceuticals2010-06-222016-11-16Us
NeptazaneTablet25 mg/1OralPaddock Laboratories, LLC2015-01-12Not applicableUs
NeptazaneTablet50 mg/1OralPaddock Laboratories, LLC2015-01-12Not applicableUs
NeptazaneTablet25 mg/1OralFera Pharmaceuticals2010-06-222016-11-16Us
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NaptazaneFera Pharmaceuticals
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIW733B0S9SD
CAS number554-57-4
WeightAverage: 236.26
Monoisotopic: 236.003782482
Chemical FormulaC5H8N4O3S2
InChI KeyFLOSMHQXBMRNHR-UHFFFAOYSA-N
InChI
InChI=1S/C5H8N4O3S2/c1-3(10)7-4-9(2)8-5(13-4)14(6,11)12/h1-2H3,(H2,6,11,12)
IUPAC Name
N-(3-methyl-5-sulfamoyl-2,3-dihydro-1,3,4-thiadiazol-2-ylidene)acetamide
SMILES
CN1N=C(SC1=NC(C)=O)S(N)(=O)=O
Pharmacology
IndicationFor treatment of chronic open-angle glaucoma and acute angle-closure glaucoma
Structured Indications
PharmacodynamicsMethazolamide is topical carbonic anhydrase inhibitor. Methazolamide is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Methazolamide is a sulfonamide derivative; however, it does not have any clinically significant antimicrobial properties. Although methazolamide achieves a high concentration in the cerebrospinal fluid, it is not-considered an effective anticonvulsant. Methazolamide has a weak and transient diuretic effect, therefore use results in an increase in urinary volume, with excretion of sodium, potassium and chloride.
Mechanism of actionMethazolamide is a potent inhibitor of carbonic anhydrase. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport.
TargetKindPharmacological actionActionsOrganismUniProt ID
Carbonic anhydrase 1Proteinyes
inhibitor
HumanP00915 details
Carbonic anhydrase 2Proteinyes
inhibitor
HumanP00918 details
Carbonic anhydrase 4Proteinyes
inhibitor
HumanP22748 details
Carbonic anhydrase 7Proteinyes
inhibitor
HumanP43166 details
Related Articles
AbsorptionMethazolamide is well absorbed from the gastrointestinal tract.
Volume of distribution
  • 17 to 23 L
Protein binding55%
MetabolismNot Available
Route of eliminationNot Available
Half life14 hours
ClearanceNot Available
ToxicityElectrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur in the case of an overdose.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamineMethazolamide may decrease the excretion rate of 2,5-Dimethoxy-4-ethylamphetamine which could result in a higher serum level.Experimental, Illicit
3,4-MethylenedioxyamphetamineMethazolamide may decrease the excretion rate of 3,4-Methylenedioxyamphetamine which could result in a higher serum level.Experimental, Illicit
3,4-MethylenedioxymethamphetamineMethazolamide may decrease the excretion rate of 3,4-Methylenedioxymethamphetamine which could result in a higher serum level.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamineMethazolamide may decrease the excretion rate of 4-Bromo-2,5-dimethoxyamphetamine which could result in a higher serum level.Experimental, Illicit
AcebutololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Acebutolol.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Acetazolamide.Approved, Vet Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Methazolamide.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Methazolamide.Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Methazolamide.Approved, Illicit
AliskirenThe risk or severity of adverse effects can be increased when Methazolamide is combined with Aliskiren.Approved, Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Methazolamide.Experimental, Illicit
AmifostineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Amifostine.Approved, Investigational
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Methazolamide.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Methazolamide.Approved
AmiodaroneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Amiodarone.Approved, Investigational
AmlodipineThe risk or severity of adverse effects can be increased when Amlodipine is combined with Methazolamide.Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Methazolamide.Approved, Illicit
AmphetamineMethazolamide may decrease the excretion rate of Amphetamine which could result in a higher serum level.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Methazolamide is combined with Amphotericin B.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Methazolamide is combined with Amyl Nitrite.Approved
ApomorphineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Apomorphine.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Apraclonidine.Approved
AripiprazoleAripiprazole may increase the hypotensive activities of Methazolamide.Approved, Investigational
ArotinololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Arotinolol.Approved
Arsenic trioxideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Arsenic trioxide.Approved, Investigational
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with Methazolamide.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Azilsartan medoxomil.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Methazolamide.Approved, Investigational
BarbexacloneBarbexaclone may increase the hypotensive activities of Methazolamide.Experimental
BarbitalBarbital may increase the hypotensive activities of Methazolamide.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Barnidipine.Approved
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Methazolamide.Approved, Investigational
BendroflumethiazideThe risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Methazolamide.Approved
BenzphetamineMethazolamide may decrease the excretion rate of Benzphetamine which could result in a higher serum level.Approved, Illicit
BepridilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bepridil.Approved, Withdrawn
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with Methazolamide.Approved
BezitramideThe risk or severity of adverse effects can be increased when Bezitramide is combined with Methazolamide.Experimental, Illicit, Withdrawn
BisoprololThe risk or severity of adverse effects can be increased when Bisoprolol is combined with Methazolamide.Approved
BortezomibThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bortezomib.Approved, Investigational
BretyliumThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bretylium.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Methazolamide.Approved
BrinzolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Brinzolamide.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bromocriptine.Approved, Investigational
BumetanideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bumetanide.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Bupivacaine.Approved, Investigational
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Methazolamide.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Methazolamide.Approved, Illicit, Vet Approved
CanagliflozinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Canagliflozin.Approved
CandesartanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Candesartan.Approved
CaptoprilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Captopril.Approved
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Methazolamide.Approved, Investigational
CarbetocinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Carbetocin.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Methazolamide.Illicit, Vet Approved
CarteololThe risk or severity of adverse effects can be increased when Carteolol is combined with Methazolamide.Approved
CarvedilolThe risk or severity of adverse effects can be increased when Methazolamide is combined with Carvedilol.Approved, Investigational
ChlorothiazideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Chlorothiazide.Approved, Vet Approved
ChlorphentermineMethazolamide may decrease the excretion rate of Chlorphentermine which could result in a higher serum level.Illicit, Withdrawn
ChlorpromazineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Chlorpromazine.Approved, Vet Approved
ChlorthalidoneThe risk or severity of adverse effects can be increased when Chlorthalidone is combined with Methazolamide.Approved
CilazaprilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Cilazapril.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Cilnidipine.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Methazolamide.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Clevidipine.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Clofarabine.Approved, Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Clomipramine.Approved, Vet Approved
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Methazolamide.Approved
ClozapineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Clozapine.Approved
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Methazolamide.Approved, Illicit
ConivaptanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Conivaptan.Approved, Investigational
DapagliflozinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Dapagliflozin.Approved
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Methazolamide.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Desflurane.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Methazolamide.Approved, Vet Approved
DextroamphetamineMethazolamide may decrease the excretion rate of Dextroamphetamine which could result in a higher serum level.Approved, Illicit
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Methazolamide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Methazolamide.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Methazolamide.Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Diclofenamide.Approved
DiethylpropionMethazolamide may decrease the excretion rate of Diethylpropion which could result in a higher serum level.Approved, Illicit
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Methazolamide.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Methazolamide.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Methazolamide.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Methazolamide.Experimental, Illicit
DiltiazemThe risk or severity of adverse effects can be increased when Diltiazem is combined with Methazolamide.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Methazolamide is combined with Dinutuximab.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Methazolamide.Approved, Illicit
DipyridamoleThe risk or severity of adverse effects can be increased when Methazolamide is combined with Dipyridamole.Approved
DorzolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Dorzolamide.Approved
DoxazosinThe risk or severity of adverse effects can be increased when Doxazosin is combined with Methazolamide.Approved
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Methazolamide.Investigational
DuloxetineMethazolamide may increase the orthostatic hypotensive activities of Duloxetine.Approved
EfonidipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Efonidipine.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Empagliflozin.Approved
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Methazolamide.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Methazolamide is combined with Enalaprilat.Approved
EplerenoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Methazolamide.Approved
EpoprostenolThe risk or severity of adverse effects can be increased when Methazolamide is combined with Epoprostenol.Approved
EprosartanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Eprosartan.Approved
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Methazolamide.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Methazolamide is combined with Etacrynic acid.Approved
EthoxzolamideThe risk or severity of adverse effects can be increased when Ethoxzolamide is combined with Methazolamide.Withdrawn
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Methazolamide.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Methazolamide.Illicit, Vet Approved
FelodipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Felodipine.Approved, Investigational
FenoldopamThe risk or severity of adverse effects can be increased when Methazolamide is combined with Fenoldopam.Approved
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Methazolamide.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Methazolamide.Approved
FimasartanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Fimasartan.Approved
FlecainideThe serum concentration of Flecainide can be increased when it is combined with Methazolamide.Approved, Withdrawn
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Methazolamide.Approved
FosphenytoinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Fosphenytoin.Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Methazolamide.Approved, Vet Approved
GuanfacineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Guanfacine.Approved, Investigational
HalothaneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Methazolamide.Approved, Illicit
HexamethylenetetramineThe therapeutic efficacy of Hexamethylenetetramine can be decreased when used in combination with Methazolamide.Approved, Vet Approved
HexobarbitalHexobarbital may increase the hypotensive activities of Methazolamide.Approved
HydralazineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Hydralazine.Approved
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Hydrochlorothiazide.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Methazolamide.Approved, Illicit
HydroflumethiazideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Hydroflumethiazide.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Methazolamide.Approved, Illicit
Hydroxyamphetamine hydrobromideMethazolamide may decrease the excretion rate of Hydroxyamphetamine hydrobromide which could result in a higher serum level.Approved
IloprostThe risk or severity of adverse effects can be increased when Methazolamide is combined with Iloprost.Approved, Investigational
ImidaprilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Imidapril.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Imipramine.Approved
IndapamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Indapamide.Approved
IndoraminThe risk or severity of adverse effects can be increased when Methazolamide is combined with Indoramin.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Irbesartan.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Methazolamide is combined with Isocarboxazid.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Isoflurane.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Methazolamide is combined with Isosorbide Dinitrate.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Methazolamide is combined with Isosorbide Mononitrate.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Isoxsuprine.Approved, Withdrawn
IsradipineThe risk or severity of adverse effects can be increased when Isradipine is combined with Methazolamide.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Methazolamide.Approved
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Methazolamide.Approved
LacidipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Lacidipine.Approved
LercanidipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Lercanidipine.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Levobunolol.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Levobupivacaine.Approved
LevodopaMethazolamide may increase the orthostatic hypotensive activities of Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Methazolamide.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Methazolamide.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Levosimendan.Approved, Investigational
LisdexamfetamineMethazolamide may decrease the excretion rate of Lisdexamfetamine which could result in a higher serum level.Approved, Investigational
LisinoprilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Lisinopril.Approved, Investigational
LithiumThe serum concentration of Lithium can be decreased when it is combined with Methazolamide.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Methazolamide.Illicit
LofexidineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Lofexidine.Approved, Investigational
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Methazolamide.Approved
MannitolThe risk or severity of adverse effects can be increased when Methazolamide is combined with Mannitol.Approved, Investigational
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Methazolamide.Approved
MemantineMethazolamide may decrease the excretion rate of Memantine which could result in a higher serum level.Approved, Investigational
MephedroneMethazolamide may decrease the excretion rate of Mephedrone which could result in a higher serum level.Investigational
MephentermineMethazolamide may decrease the excretion rate of Mephentermine which could result in a higher serum level.Approved
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Methazolamide.Approved
MetforminThe risk or severity of adverse effects can be increased when Methazolamide is combined with Metformin.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Methazolamide.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Methazolamide.Approved, Illicit
MethamphetamineMethazolamide may decrease the excretion rate of Methamphetamine which could result in a higher serum level.Approved, Illicit
MethohexitalMethohexital may increase the hypotensive activities of Methazolamide.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Methazolamide.Approved
MethyldopaThe risk or severity of adverse effects can be increased when Methazolamide is combined with Methyldopa.Approved
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Methazolamide.Approved
MetipranololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Metipranolol.Approved
MetolazoneThe risk or severity of adverse effects can be increased when Metolazone is combined with Methazolamide.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Methazolamide.Approved, Investigational
MinoxidilThe risk or severity of adverse effects can be increased when Minoxidil is combined with Methazolamide.Approved
MMDAMethazolamide may decrease the excretion rate of MMDA which could result in a higher serum level.Experimental, Illicit
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Methazolamide.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Methazolamide.Approved, Investigational
MoxonidineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Moxonidine.Approved
NabiloneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nabilone.Approved, Investigational
NadololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nadolol.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Methazolamide.Approved
NCX 4016The risk or severity of adverse effects can be increased when NCX 4016 is combined with Methazolamide.Investigational
NebivololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nebivolol.Approved, Investigational
NesiritideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nesiritide.Approved, Investigational
NicardipineThe risk or severity of adverse effects can be increased when Nicardipine is combined with Methazolamide.Approved
NicorandilNicorandil may increase the hypotensive activities of Methazolamide.Approved
NifedipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nifedipine.Approved
NilvadipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nilvadipine.Approved
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Methazolamide.Approved
NisoldipineThe risk or severity of adverse effects can be increased when Nisoldipine is combined with Methazolamide.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nitrendipine.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nitric Oxide.Approved
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Methazolamide.Investigational
NitroglycerinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nitroglycerin.Approved, Investigational
NitroprussideThe risk or severity of adverse effects can be increased when Nitroprusside is combined with Methazolamide.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Methazolamide.Approved, Illicit
ObinutuzumabThe risk or severity of adverse effects can be increased when Methazolamide is combined with Obinutuzumab.Approved
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Methazolamide.Approved, Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Methazolamide.Approved
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Methazolamide.Approved, Illicit
OxprenololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Oxprenolol.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Methazolamide.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Methazolamide.Approved, Investigational, Vet Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Methazolamide is combined with Paclitaxel.Approved, Vet Approved
PapaverineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Papaverine.Approved
PenbutololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Penbutolol.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Methazolamide.Approved, Vet Approved
PentobarbitalPentobarbital may increase the hypotensive activities of Methazolamide.Approved, Vet Approved
PerindoprilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Methazolamide.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Phenelzine.Approved
PhenobarbitalPhenobarbital may increase the hypotensive activities of Methazolamide.Approved
PhenoxybenzamineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Phenoxybenzamine.Approved
PhentermineMethazolamide may decrease the excretion rate of Phentermine which could result in a higher serum level.Approved, Illicit
PhentolamineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Phentolamine.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Phenytoin.Approved, Vet Approved
PindololThe risk or severity of adverse effects can be increased when Methazolamide is combined with Pindolol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Pipamperone.Approved
PiritramideThe risk or severity of adverse effects can be increased when Piritramide is combined with Methazolamide.Investigational
PramipexoleThe risk or severity of adverse effects can be increased when Methazolamide is combined with Pramipexole.Approved, Investigational
PrazosinThe risk or severity of adverse effects can be increased when Prazosin is combined with Methazolamide.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Primidone.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Methazolamide is combined with Propofol.Approved, Investigational, Vet Approved
PropranololThe risk or severity of adverse effects can be increased when Propranolol is combined with Methazolamide.Approved, Investigational
PseudoephedrineMethazolamide may decrease the excretion rate of Pseudoephedrine which could result in a higher serum level.Approved
QuetiapineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Quetiapine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Quinapril.Approved, Investigational
QuinidineMethazolamide may decrease the excretion rate of Quinidine which could result in a higher serum level.Approved
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Methazolamide.Approved
RasagilineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Rasagiline.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Methazolamide.Approved
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Methazolamide.Approved
RiociguatThe risk or severity of adverse effects can be increased when Methazolamide is combined with Riociguat.Approved
RisperidoneMethazolamide may increase the hypotensive activities of Risperidone.Approved, Investigational
RitobegronMethazolamide may decrease the excretion rate of Ritobegron which could result in a higher serum level.Investigational
RopiniroleThe risk or severity of adverse effects can be increased when Methazolamide is combined with Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Ropivacaine.Approved
RotigotineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Rotigotine.Approved
SacubitrilThe risk or severity of adverse effects can be increased when Methazolamide is combined with Sacubitril.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Methazolamide.Approved, Vet Approved
SecobarbitalSecobarbital may increase the hypotensive activities of Methazolamide.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Selegiline.Approved, Investigational, Vet Approved
SevofluraneThe risk or severity of adverse effects can be increased when Methazolamide is combined with Sevoflurane.Approved, Vet Approved
Sodium NitriteThe risk or severity of adverse effects can be increased when Methazolamide is combined with Sodium Nitrite.Approved
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Methazolamide.Approved
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Methazolamide.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Methazolamide is combined with Streptokinase.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Methazolamide.Approved, Investigational
TamsulosinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Tamsulosin.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Methazolamide.Approved
TelmisartanThe risk or severity of adverse effects can be increased when Methazolamide is combined with Telmisartan.Approved, Investigational
TerazosinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Terazosin.Approved
ThalidomideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the hypotensive activities of Methazolamide.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Methazolamide.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Methazolamide.Approved
TimololThe risk or severity of adverse effects can be increased when Timolol is combined with Methazolamide.Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Methazolamide.Approved
TolazolineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Tolazoline.Approved, Vet Approved
TolcaponeThe risk or severity of adverse effects can be increased when Methazolamide is combined with Tolcapone.Approved, Withdrawn
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Methazolamide.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Methazolamide.Approved, Investigational
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Methazolamide.Approved
TranylcypromineThe risk or severity of adverse effects can be increased when Methazolamide is combined with Tranylcypromine.Approved
TretinoinThe risk or severity of adverse effects can be increased when Methazolamide is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Methazolamide.Approved
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Methazolamide.Approved, Investigational
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Methazolamide.Approved
Food Interactions
  • Take with food, more than 6 hours before bedtime increase liquid intake.
References
Synthesis ReferenceNot Available
General References
  1. Iyer GR, Bellantone RA, Taft DR: In vitro characterization of the erythrocyte distribution of methazolamide: a model of erythrocyte transport and binding kinetics. J Pharmacokinet Biopharm. 1999 Feb;27(1):45-66. [PubMed:10533697 ]
  2. Shirato S, Kagaya F, Suzuki Y, Joukou S: Stevens-Johnson syndrome induced by methazolamide treatment. Arch Ophthalmol. 1997 Apr;115(4):550-3. [PubMed:9109770 ]
  3. Skorobohach BJ, Ward DA, Hendrix DV: Effects of oral administration of methazolamide on intraocular pressure and aqueous humor flow rate in clinically normal dogs. Am J Vet Res. 2003 Feb;64(2):183-7. [PubMed:12602587 ]
External Links
ATC CodesS01EC05
AHFS Codes
  • 52:10.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7104
Blood Brain Barrier+0.8117
Caco-2 permeable-0.6196
P-glycoprotein substrateNon-substrate0.8509
P-glycoprotein inhibitor INon-inhibitor0.9245
P-glycoprotein inhibitor IINon-inhibitor0.8896
Renal organic cation transporterNon-inhibitor0.8909
CYP450 2C9 substrateNon-substrate0.6189
CYP450 2D6 substrateNon-substrate0.8512
CYP450 3A4 substrateNon-substrate0.6898
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.6861
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8681
Ames testNon AMES toxic0.7032
CarcinogenicityNon-carcinogens0.7679
BiodegradationNot ready biodegradable0.9138
Rat acute toxicity2.2388 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9942
hERG inhibition (predictor II)Non-inhibitor0.9021
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Applied analytical industries
  • Mikart inc
  • Sandoz inc
  • Teva pharmaceuticals usa
  • Lederle laboratories div american cyanamid co
Packagers
Dosage forms
FormRouteStrength
TabletOral50 mg
TabletOral25 mg/1
TabletOral50 mg/1
TabletOral25 mg
Prices
Unit descriptionCostUnit
Methazolamide powder27.0USD g
Methazolamide 50 mg tablet0.77USD tablet
Neptazane 25 mg tablet0.6USD tablet
Apo-Methazolamide 50 mg Tablet0.5USD tablet
Methazolamide 25 mg tablet0.49USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point213.5 °CPhysProp
water solubility3500 mg/LYALKOWSKY,SH & DANNENFELSER,RM (1992)
logP0.13HANSCH,C ET AL. (1995)
logS-1.83ADME Research, USCD
pKa7.30Not Available
Predicted Properties
PropertyValueSource
Water Solubility1.74 mg/mLALOGPS
logP-0.2ALOGPS
logP-0.59ChemAxon
logS-2.1ALOGPS
pKa (Strongest Acidic)7.21ChemAxon
pKa (Strongest Basic)-3.6ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area105.19 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity51.3 m3·mol-1ChemAxon
Polarizability20.99 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as thiadiazole sulfonamides. These are heterocyclic compounds containing a thiazole ring substituted by at least one sulfonamide group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassThiadiazoles
Direct ParentThiadiazole sulfonamides
Alternative Parents
Substituents
  • 1,3,4-thiadiazole-2-sulfonamide
  • Heteroaromatic compound
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • N-acylimine
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Organic oxide
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Reversible hydration of carbon dioxide. Can hydrates cyanamide to urea.
Gene Name:
CA1
Uniprot ID:
P00915
Molecular Weight:
28870.0 Da
References
  1. Ilies MA, Masereel B, Rolin S, Scozzafava A, Campeanu G, Cimpeanu V, Supuran CT: Carbonic anhydrase inhibitors: aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activity. Bioorg Med Chem. 2004 May 15;12(10):2717-26. [PubMed:15110853 ]
  2. Winum JY, Casini A, Mincione F, Starnotti M, Montero JL, Scozzafava A, Supuran CT: Carbonic anhydrase inhibitors: N-(p-sulfamoylphenyl)-alpha-D-glycopyranosylamines as topically acting antiglaucoma agents in hypertensive rabbits. Bioorg Med Chem Lett. 2004 Jan 5;14(1):225-9. [PubMed:14684332 ]
  3. Iyer GR, Bellantone RA, Taft DR: In vitro characterization of the erythrocyte distribution of methazolamide: a model of erythrocyte transport and binding kinetics. J Pharmacokinet Biopharm. 1999 Feb;27(1):45-66. [PubMed:10533697 ]
  4. Scozzafava A, Briganti F, Ilies MA, Supuran CT: Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes. J Med Chem. 2000 Jan 27;43(2):292-300. [PubMed:10649985 ]
  5. Lindskog S: Structure and mechanism of carbonic anhydrase. Pharmacol Ther. 1997;74(1):1-20. [PubMed:9336012 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption. Stimulates the chloride-bicarbonate ex...
Gene Name:
CA2
Uniprot ID:
P00918
Molecular Weight:
29245.895 Da
References
  1. Mincione F, Scozzafava A, Supuran CT: The development of topically acting carbonic anhydrase inhibitors as antiglaucoma agents. Curr Pharm Des. 2008;14(7):649-54. [PubMed:18336310 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Reversible hydration of carbon dioxide. May stimulate the sodium/bicarbonate transporter activity of SLC4A4 that acts in pH homeostasis. It is essential for acid overload removal from the retina and retina epithelium, and acid release in the choriocapillaris in the choroid.
Gene Name:
CA4
Uniprot ID:
P22748
Molecular Weight:
35032.075 Da
References
  1. Mincione F, Scozzafava A, Supuran CT: The development of topically acting carbonic anhydrase inhibitors as antiglaucoma agents. Curr Pharm Des. 2008;14(7):649-54. [PubMed:18336310 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Reversible hydration of carbon dioxide.
Gene Name:
CA7
Uniprot ID:
P43166
Molecular Weight:
29658.235 Da
References
  1. Mincione F, Scozzafava A, Supuran CT: The development of topically acting carbonic anhydrase inhibitors as antiglaucoma agents. Curr Pharm Des. 2008;14(7):649-54. [PubMed:18336310 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Uwai Y, Saito H, Hashimoto Y, Inui KI: Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1. J Pharmacol Exp Ther. 2000 Oct;295(1):261-5. [PubMed:10991988 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23