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Identification
NameDorzolamide
Accession NumberDB00869  (APRD00577, DB04507)
TypeSmall Molecule
GroupsApproved
DescriptionDorzolamide is a carbonic anhydrase (CA) inhibitor. It is used in ophthalmic solutions (Trusopt) to lower intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension.
Structure
Thumb
Synonyms
(4S-trans)-4-(ETHYLAMINO)-5,6-dihydro-6-methyl-4H-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide
(4S,6S)-4-Ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
(4S,trans)-4-(Ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide
4-Ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda*6*-thieno[2,3-b]thiopyran-2-sulfonic acid amide
4-Ethylamino-6-methyl-7,7-dioxo-4,5,6,7-tetrahydro-7lambda6-thieno[2,3-b]thiopyran-2-sulfonic acid amide
4S,6S-Dorzolamide
Dorzolamid
Dorzolamida
Dorzolamide
Dorzolamidum
External Identifiers
  • L 671152
  • MK 507
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dorzolamidesolution2.0 %ophthalmicAlcon Canada IncNot applicableNot applicableCanada
Dorzolamide Hydrochloridesolution20 mg/mLophthalmicPrasco Laboratories1994-12-09Not applicableUs
Dorzolamide Hydrochloride Ophthalmic Solutionsolution20 mgophthalmicBausch & Lomb IncNot applicableNot applicableCanada
Jamp-dorzolamidesolution2 %ophthalmicJamp Pharma CorporationNot applicableNot applicableCanada
Sandoz Dorzolamidesolution20 mgophthalmicSandoz Canada Incorporated2010-10-25Not applicableCanada
Trusoptsolution20 mg/mLophthalmicMerck Sharp & Dohme Corp.1994-12-09Not applicableUs
Trusoptsolution2 %ophthalmicMerck Canada Inc1996-12-31Not applicableCanada
Trusopt -(preservative-free Formulation)solution2 %ophthalmicMerck Canada Inc2006-02-01Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-dorzolamidesolution2 %ophthalmicApotex IncNot applicableNot applicableCanada
Dorzolamide HClsolution20 mg/mLophthalmicActavis Pharma, Inc.2015-02-17Not applicableUs
Dorzolamide HClsolution/ drops20 mg/mLophthalmicBausch & Lomb Incorporated2009-06-25Not applicableUs
Dorzolamide HClsolution/ drops22.3 mg/mLophthalmicPhysicians Total Care, Inc.2012-02-21Not applicableUs
Dorzolamide Hydrochloridesolution/ drops20 mg/mLophthalmicGolden State Medical Supply, Inc.2014-11-13Not applicableUs
Dorzolamide Hydrochloridesolution20 mg/mLophthalmicTeva Pharmaceuticals USA Inc2010-01-28Not applicableUs
Dorzolamide Hydrochloridesolution/ drops20 mg/mLophthalmicHi Tech Pharmacal Co., Inc.2008-10-28Not applicableUs
Dorzolamide Hydrochloridesolution/ drops20 mg/mLophthalmicSandoz Inc.2009-06-01Not applicableUs
Dorzolamide Hydrochloridesolution/ drops20 mg/mLophthalmicREMEDYREPACK INC.2013-11-18Not applicableUs
Dorzolamide Hydrochloride Ophthalmic Solution 2%, 10ml Ophthalmic Solution 2%, 10mlsolution22.3 mg/mLophthalmicAlvogen Inc.2013-12-16Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Act DorzotimololActavis Pharma Company
Apo-dorzo-timopApotex Inc
CosoptMerck Sharp & Dohme Corp.
Cosopt PFMerck Sharp & Dohme Corp.
Dorzolamide HCl /timolol MaleateREMEDYREPACK INC.
Dorzolamide HCl and Timolol MaleateActavis Pharma, Inc.
Dorzolamide Hydrochloride and Timolol MaleateBausch & Lomb Incorporated
Dorzolamide Hydrochloride and Timolol Maleate Ophthalmic SolutionBausch & Lomb Inc
Dorzolamide Hydrochloride-timolol MaleateLannett Company, Inc.
Dorzolamide Hydrochloride-timolol Maleate Ophthalmic Solution Sterile Ophthalmic SolutionAlvogen Inc.
Med-dorzolamide-timololGeneric Medical Partners Inc
Mint-dorzolamide/timololMint Pharmaceuticals Inc
Mylan-dorzolamide/timololMylan Pharmaceuticals Ulc
PMS-dorzolamide-timololPharmascience Inc
Preservative-free CosoptMerck Canada Inc
Riva-dorzolamide/timololLaboratoire Riva Inc
Sandoz Dorzolamide/timololSandoz Canada Incorporated
Teva-dorzotimolTeva Canada Limited
Van-dorzolamide-timololVanc Pharmaceuticals Inc
Salts
Name/CASStructureProperties
Dorzolamide Hydrochloride
ThumbNot applicableDBSALT000931
Categories
UNII9JDX055TW1
CAS number120279-96-1
WeightAverage: 324.44
Monoisotopic: 324.02721908
Chemical FormulaC10H16N2O4S3
InChI KeyInChIKey=IAVUPMFITXYVAF-XPUUQOCRSA-N
InChI
InChI=1S/C10H16N2O4S3/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16)/t6-,8-/m0/s1
IUPAC Name
(2S,4S)-4-(ethylamino)-2-methyl-1,1-dioxo-2H,3H,4H-1λ⁶-thieno[2,3-b]thiopyran-6-sulfonamide
SMILES
CCN[[email protected]]1C[[email protected]](C)S(=O)(=O)C2=C1C=C(S2)S(N)(=O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 2,3,5-trisubstituted thiophenes. These are organic compounds containing a thiophene that is trisubstituted at the C-2, C3- and C5-positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassThiophenes
Sub Class2,3,5-trisubstituted thiophenes
Direct Parent2,3,5-trisubstituted thiophenes
Alternative Parents
Substituents
  • 2,3,5-trisubstituted thiophene
  • Aralkylamine
  • Thiopyran
  • Heteroaromatic compound
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfone
  • Sulfonamide
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Also used prophylatically for the inhibition of perioperative IOP increase (before neodynium yttrium aluminum garnet laser posterior capsulotomy).
PharmacodynamicsDorzolamide is topical CA inhibitor that is indicated for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Dorzolamide reduces IOP by approximately 17-23% in patients with elevater IOP.
Mechanism of actionDorzolamide is a sulfonamide and a highly specific carbonic anhydrase II (CA-II) inhibitor, which is the main CA isoenzyme involved in aqueous humor secretion. Inhibition of CA-II 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. Dorzolamide also accumulates in red blood cells as a result of CA-II binding, as CA-II is found predominantly in erythrocytes. However, sufficient CA-II activity remains so that adverse effects due to systemic CA inhibition are not observed.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding~33%
MetabolismNot Available
Route of eliminationDorzolamide is primarily excreted unchanged in the urine; the metabolite also is excreted in urine.
Half life4 months
ClearanceNot Available
ToxicityDizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9944
Blood Brain Barrier+0.6697
Caco-2 permeable-0.6627
P-glycoprotein substrateSubstrate0.5389
P-glycoprotein inhibitor INon-inhibitor0.8855
P-glycoprotein inhibitor IINon-inhibitor0.8398
Renal organic cation transporterNon-inhibitor0.9011
CYP450 2C9 substrateNon-substrate0.7755
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5096
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7547
Ames testNon AMES toxic0.6397
CarcinogenicityNon-carcinogens0.6933
BiodegradationNot ready biodegradable0.9946
Rat acute toxicity2.2365 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9446
hERG inhibition (predictor II)Non-inhibitor0.8706
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Alcon inc
  • Apotex inc
  • Bausch and lomb inc
  • Hi tech pharmacal co inc
  • Pharmaforce inc
  • Sandoz canada inc
  • Teva pharmaceuticals usa
  • Merck research laboratories div merck co inc
Packagers
Dosage forms
FormRouteStrength
Solutionophthalmic
Solutionophthalmic2.0 %
Solution/ dropsophthalmic20 mg/mL
Solution/ dropsophthalmic22.3 mg/mL
Solution/ dropsophthalmic
Solutionophthalmic22.3 mg/mL
Solutionophthalmic20 mg
Solutionophthalmic20 mg/mL
Solutionophthalmic2 %
Prices
Unit descriptionCostUnit
Trusopt 2% Solution 10ml79.25USD bottle
Dorzolamide HCl 2% Solution 10ml Bottle69.42USD bottle
Dorzolamide hcl 2% eye drops6.86USD ml
Trusopt 2% eye drops6.73USD ml
Trusopt (Preservative-Free) 2 % Solution3.93USD ml
Trusopt 2 % Solution3.93USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1329211 No1994-05-032011-05-03Canada
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point283-285 °CNot Available
logP-1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.699 mg/mLALOGPS
logP-0.5ALOGPS
logP-0.15ChemAxon
logS-2.7ALOGPS
pKa (Strongest Acidic)8.18ChemAxon
pKa (Strongest Basic)7.14ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area106.33 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity72.46 m3·mol-1ChemAxon
Polarizability31.55 Å3ChemAxon
Number of Rings2ChemAxon
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
References
Synthesis Reference

Laszlo Kovacs, Csaba Szabo, Erika Molnarne, Adrienne Kovacsne-Mezei, Claude Singer, Judith Aronhime, “Method of making dorzolamide hydrochloride.” U.S. Patent US20060155132, issued July 13, 2006.

US20060155132
General References
  1. Plummer CE, MacKay EO, Gelatt KN: Comparison of the effects of topical administration of a fixed combination of dorzolamide-timolol to monotherapy with timolol or dorzolamide on IOP, pupil size, and heart rate in glaucomatous dogs. Vet Ophthalmol. 2006 Jul-Aug;9(4):245-9. [PubMed:16771760 ]
  2. Grover S, Apushkin MA, Fishman GA: Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa. Am J Ophthalmol. 2006 May;141(5):850-8. Epub 2006 Mar 20. [PubMed:16546110 ]
  3. Almeida GC Jr, Faria e Souza SJ: Effect of topical dorzolamide on rabbit central corneal thickness. Braz J Med Biol Res. 2006 Feb;39(2):277-81. Epub 2006 Feb 2. [PubMed:16470316 ]
  4. Martens-Lobenhoffer J, Banditt P: Clinical pharmacokinetics of dorzolamide. Clin Pharmacokinet. 2002;41(3):197-205. [PubMed:11929320 ]
  5. Balfour JA, Wilde MI: Dorzolamide. A review of its pharmacology and therapeutic potential in the management of glaucoma and ocular hypertension. Drugs Aging. 1997 May;10(5):384-403. [PubMed:9143858 ]
  6. Ponticello GS, Sugrue MF, Plazonnet B, Durand-Cavagna G: Dorzolamide, a 40-year wait. From an oral to a topical carbonic anhydrase inhibitor for the treatment of glaucoma. Pharm Biotechnol. 1998;11:555-74. [PubMed:9760696 ]
External Links
ATC CodesS01EC03
AHFS Codes
  • 52:10.00
PDB Entries
FDA labelDownload (569 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Dorzolamide.
AbirateroneThe metabolism of Dorzolamide can be decreased when combined with Abiraterone.
AcebutololDorzolamide may increase the hypotensive activities of Acebutolol.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Dorzolamide.
AlfuzosinAlfuzosin may increase the hypotensive activities of Dorzolamide.
AliskirenDorzolamide may increase the hypotensive activities of Aliskiren.
AlprenololAlprenolol may increase the hypotensive activities of Dorzolamide.
AmbrisentanDorzolamide may increase the hypotensive activities of Ambrisentan.
AmifostineDorzolamide may increase the hypotensive activities of Amifostine.
AmiodaroneThe metabolism of Dorzolamide can be decreased when combined with Amiodarone.
AmlodipineAmlodipine may increase the hypotensive activities of Dorzolamide.
AprepitantThe serum concentration of Dorzolamide can be increased when it is combined with Aprepitant.
AtazanavirThe metabolism of Dorzolamide can be decreased when combined with Atazanavir.
AtenololAtenolol may increase the hypotensive activities of Dorzolamide.
AtomoxetineThe metabolism of Dorzolamide can be decreased when combined with Atomoxetine.
BenazeprilBenazepril may increase the hypotensive activities of Dorzolamide.
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Dorzolamide.
BenmoxinBenmoxin may increase the hypotensive activities of Dorzolamide.
BepridilDorzolamide may increase the hypotensive activities of Bepridil.
BetaxololBetaxolol may increase the hypotensive activities of Dorzolamide.
BethanidineBethanidine may increase the hypotensive activities of Dorzolamide.
BexaroteneThe serum concentration of Dorzolamide can be decreased when it is combined with Bexarotene.
BimatoprostDorzolamide may increase the hypotensive activities of Bimatoprost.
BisoprololBisoprolol may increase the hypotensive activities of Dorzolamide.
BoceprevirThe metabolism of Dorzolamide can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Dorzolamide can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Dorzolamide can be decreased when it is combined with Bosentan.
BosentanDorzolamide may increase the hypotensive activities of Bosentan.
BretyliumDorzolamide may increase the hypotensive activities of Bretylium.
BrimonidineDorzolamide may increase the hypotensive activities of Brimonidine.
BrimonidineBrimonidine may increase the antihypertensive activities of Dorzolamide.
BrinzolamideThe risk or severity of adverse effects can be increased when Dorzolamide is combined with Brinzolamide.
BupranololDorzolamide may increase the hypotensive activities of Bupranolol.
CandesartanCandesartan may increase the hypotensive activities of Dorzolamide.
CandoxatrilCandoxatril may increase the hypotensive activities of Dorzolamide.
CapecitabineThe metabolism of Dorzolamide can be decreased when combined with Capecitabine.
CaptoprilDorzolamide may increase the hypotensive activities of Captopril.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Dorzolamide.
CarbamazepineThe metabolism of Dorzolamide can be increased when combined with Carbamazepine.
CaroxazoneCaroxazone may increase the hypotensive activities of Dorzolamide.
CarteololCarteolol may increase the hypotensive activities of Dorzolamide.
CarvedilolDorzolamide may increase the hypotensive activities of Carvedilol.
CeliprololDorzolamide may increase the hypotensive activities of Celiprolol.
CeritinibThe serum concentration of Dorzolamide can be increased when it is combined with Ceritinib.
ChlorothiazideDorzolamide may increase the hypotensive activities of Chlorothiazide.
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Dorzolamide.
CholecalciferolThe metabolism of Dorzolamide can be decreased when combined with Cholecalciferol.
CilazaprilDorzolamide may increase the hypotensive activities of Cilazapril.
ClarithromycinThe metabolism of Dorzolamide can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Dorzolamide can be decreased when combined with Clemastine.
ClonidineClonidine may increase the hypotensive activities of Dorzolamide.
ClotrimazoleThe metabolism of Dorzolamide can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Dorzolamide can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Dorzolamide can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Dorzolamide can be decreased when combined with Crizotinib.
CryptenamineCryptenamine may increase the hypotensive activities of Dorzolamide.
CyclosporineThe metabolism of Dorzolamide can be decreased when combined with Cyclosporine.
CyclothiazideCyclothiazide may increase the hypotensive activities of Dorzolamide.
DabrafenibThe serum concentration of Dorzolamide can be decreased when it is combined with Dabrafenib.
DarunavirThe metabolism of Dorzolamide can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Dorzolamide can be increased when it is combined with Dasatinib.
DebrisoquinDorzolamide may increase the hypotensive activities of Debrisoquin.
DeferasiroxThe serum concentration of Dorzolamide can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Dorzolamide can be decreased when combined with Delavirdine.
DeserpidineDorzolamide may increase the hypotensive activities of Deserpidine.
DexamethasoneThe serum concentration of Dorzolamide can be decreased when it is combined with Dexamethasone.
DiazoxideDiazoxide may increase the hypotensive activities of Dorzolamide.
DiclofenamideThe risk or severity of adverse effects can be increased when Dorzolamide is combined with Diclofenamide.
DihydroergotamineThe metabolism of Dorzolamide can be decreased when combined with Dihydroergotamine.
DiltiazemDiltiazem may increase the hypotensive activities of Dorzolamide.
DoxazosinDoxazosin may increase the hypotensive activities of Dorzolamide.
DoxycyclineThe metabolism of Dorzolamide can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Dorzolamide can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Dorzolamide can be decreased when it is combined with Efavirenz.
EfonidipineDorzolamide may increase the hypotensive activities of Efonidipine.
EnalaprilEnalapril may increase the hypotensive activities of Dorzolamide.
EnalaprilatDorzolamide may increase the hypotensive activities of Enalaprilat.
EnzalutamideThe serum concentration of Dorzolamide can be decreased when it is combined with Enzalutamide.
EpoprostenolDorzolamide may increase the hypotensive activities of Epoprostenol.
EprosartanDorzolamide may increase the hypotensive activities of Eprosartan.
ErythromycinThe metabolism of Dorzolamide can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Dorzolamide can be decreased when it is combined with Eslicarbazepine acetate.
EthoxzolamideThe risk or severity of adverse effects can be increased when Ethoxzolamide is combined with Dorzolamide.
EtravirineThe serum concentration of Dorzolamide can be decreased when it is combined with Etravirine.
FelodipineDorzolamide may increase the hypotensive activities of Felodipine.
FenoldopamFenoldopam may increase the hypotensive activities of Dorzolamide.
FlecainideThe serum concentration of Flecainide can be increased when it is combined with Dorzolamide.
FloxuridineThe metabolism of Dorzolamide can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Dorzolamide can be decreased when combined with Fluconazole.
FluorouracilThe metabolism of Dorzolamide can be decreased when combined with Fluorouracil.
FluvastatinThe metabolism of Dorzolamide can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Dorzolamide can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Dorzolamide can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Dorzolamide can be increased when it is combined with Fosaprepitant.
FosinoprilFosinopril may increase the hypotensive activities of Dorzolamide.
FosphenytoinThe metabolism of Dorzolamide can be increased when combined with Fosphenytoin.
FurazolidoneFurazolidone may increase the hypotensive activities of Dorzolamide.
Fusidic AcidThe serum concentration of Dorzolamide can be increased when it is combined with Fusidic Acid.
GemfibrozilThe metabolism of Dorzolamide can be decreased when combined with Gemfibrozil.
GuanabenzGuanabenz may increase the hypotensive activities of Dorzolamide.
GuanadrelGuanadrel may increase the hypotensive activities of Dorzolamide.
GuanethidineDorzolamide may increase the hypotensive activities of Guanethidine.
GuanfacineDorzolamide may increase the hypotensive activities of Guanfacine.
HexamethoniumDorzolamide may increase the hypotensive activities of Hexamethonium.
HexamethylenetetramineThe therapeutic efficacy of Hexamethylenetetramine can be decreased when used in combination with Dorzolamide.
HydracarbazineHydracarbazine may increase the hypotensive activities of Dorzolamide.
HydralazineDorzolamide may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideDorzolamide may increase the hypotensive activities of Hydrochlorothiazide.
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Dorzolamide.
IdelalisibThe serum concentration of Dorzolamide can be increased when it is combined with Idelalisib.
IloprostIloprost may increase the hypotensive activities of Dorzolamide.
ImatinibThe metabolism of Dorzolamide can be decreased when combined with Imatinib.
IndapamideIndapamide may increase the hypotensive activities of Dorzolamide.
IndenololDorzolamide may increase the hypotensive activities of Indenolol.
IndinavirThe metabolism of Dorzolamide can be decreased when combined with Indinavir.
IndoraminDorzolamide may increase the hypotensive activities of Indoramin.
IproclozideIproclozide may increase the hypotensive activities of Dorzolamide.
IproniazidIproniazid may increase the hypotensive activities of Dorzolamide.
IrbesartanDorzolamide may increase the hypotensive activities of Irbesartan.
IsavuconazoniumThe metabolism of Dorzolamide can be decreased when combined with Isavuconazonium.
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Dorzolamide.
IsradipineIsradipine may increase the hypotensive activities of Dorzolamide.
ItraconazoleThe metabolism of Dorzolamide can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Dorzolamide can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Dorzolamide can be decreased when combined with Ketoconazole.
LabetalolLabetalol may increase the hypotensive activities of Dorzolamide.
LacidipineDorzolamide may increase the hypotensive activities of Lacidipine.
LatanoprostLatanoprost may increase the hypotensive activities of Dorzolamide.
LeflunomideThe metabolism of Dorzolamide can be decreased when combined with Leflunomide.
LercanidipineLercanidipine may increase the hypotensive activities of Dorzolamide.
LisinoprilLisinopril may increase the hypotensive activities of Dorzolamide.
LithiumThe serum concentration of Lithium can be decreased when it is combined with Dorzolamide.
LofexidineDorzolamide may increase the hypotensive activities of Lofexidine.
LopinavirThe metabolism of Dorzolamide can be decreased when combined with Lopinavir.
LosartanLosartan may increase the hypotensive activities of Dorzolamide.
LovastatinThe metabolism of Dorzolamide can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Dorzolamide can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Dorzolamide can be decreased when it is combined with Lumacaftor.
MacitentanDorzolamide may increase the hypotensive activities of Macitentan.
ManidipineDorzolamide may increase the hypotensive activities of Manidipine.
MebanazineMebanazine may increase the hypotensive activities of Dorzolamide.
MecamylamineMecamylamine may increase the hypotensive activities of Dorzolamide.
MemantineDorzolamide may decrease the excretion rate of Memantine which could result in a lower serum level and potentially a reduction in efficacy.
MetforminThe risk or severity of adverse effects can be increased when Dorzolamide is combined with Metformin.
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Dorzolamide.
MethyldopaDorzolamide may increase the hypotensive activities of Methyldopa.
Methylene blueMethylene blue may increase the hypotensive activities of Dorzolamide.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Dorzolamide.
MetipranololDorzolamide may increase the hypotensive activities of Metipranolol.
MetolazoneMetolazone may increase the hypotensive activities of Dorzolamide.
MetoprololMetoprolol may increase the hypotensive activities of Dorzolamide.
MibefradilDorzolamide may increase the hypotensive activities of Mibefradil.
MifepristoneThe metabolism of Dorzolamide can be decreased when combined with Mifepristone.
MinaprineMinaprine may increase the hypotensive activities of Dorzolamide.
MinoxidilMinoxidil may increase the hypotensive activities of Dorzolamide.
MitotaneThe serum concentration of Dorzolamide can be decreased when it is combined with Mitotane.
MoclobemideMoclobemide may increase the hypotensive activities of Dorzolamide.
ModafinilThe serum concentration of Dorzolamide can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the hypotensive activities of Dorzolamide.
MolsidomineMolsidomine may increase the hypotensive activities of Dorzolamide.
MoxonidineDorzolamide may increase the hypotensive activities of Moxonidine.
NadololDorzolamide may increase the hypotensive activities of Nadolol.
NafcillinThe serum concentration of Dorzolamide can be decreased when it is combined with Nafcillin.
NebivololDorzolamide may increase the hypotensive activities of Nebivolol.
NefazodoneThe metabolism of Dorzolamide can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Dorzolamide can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Dorzolamide can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Dorzolamide can be decreased when combined with Nevirapine.
NialamideNialamide may increase the hypotensive activities of Dorzolamide.
NicardipineNicardipine may increase the hypotensive activities of Dorzolamide.
NicorandilDorzolamide may increase the hypotensive activities of Nicorandil.
NiguldipineDorzolamide may increase the hypotensive activities of Niguldipine.
NilotinibThe metabolism of Dorzolamide can be decreased when combined with Nilotinib.
NilvadipineDorzolamide may increase the hypotensive activities of Nilvadipine.
NimodipineNimodipine may increase the hypotensive activities of Dorzolamide.
NisoldipineNisoldipine may increase the hypotensive activities of Dorzolamide.
NitrendipineDorzolamide may increase the hypotensive activities of Nitrendipine.
NitroprussideNitroprusside may increase the hypotensive activities of Dorzolamide.
ObinutuzumabDorzolamide may increase the hypotensive activities of Obinutuzumab.
OctamoxinOctamoxin may increase the hypotensive activities of Dorzolamide.
OlaparibThe metabolism of Dorzolamide can be decreased when combined with Olaparib.
OlmesartanOlmesartan may increase the hypotensive activities of Dorzolamide.
OmapatrilatDorzolamide may increase the hypotensive activities of Omapatrilat.
OmeprazoleThe metabolism of Dorzolamide can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Dorzolamide can be increased when it is combined with Osimertinib.
OxprenololDorzolamide may increase the hypotensive activities of Oxprenolol.
PalbociclibThe serum concentration of Dorzolamide can be increased when it is combined with Palbociclib.
PargylineDorzolamide may increase the hypotensive activities of Pargyline.
PenbutololDorzolamide may increase the hypotensive activities of Penbutolol.
PentobarbitalThe metabolism of Dorzolamide can be increased when combined with Pentobarbital.
PentoliniumDorzolamide may increase the hypotensive activities of Pentolinium.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Dorzolamide.
PerindoprilPerindopril may increase the hypotensive activities of Dorzolamide.
PhenelzinePhenelzine may increase the hypotensive activities of Dorzolamide.
PheniprazinePheniprazine may increase the hypotensive activities of Dorzolamide.
PhenobarbitalThe metabolism of Dorzolamide can be increased when combined with Phenobarbital.
PhenoxybenzamineDorzolamide may increase the hypotensive activities of Phenoxybenzamine.
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Dorzolamide.
PhentolaminePhentolamine may increase the hypotensive activities of Dorzolamide.
PhenytoinThe metabolism of Dorzolamide can be increased when combined with Phenytoin.
PinacidilDorzolamide may increase the hypotensive activities of Pinacidil.
PindololDorzolamide may increase the hypotensive activities of Pindolol.
PirlindolePirlindole may increase the hypotensive activities of Dorzolamide.
PivhydrazinePivhydrazine may increase the hypotensive activities of Dorzolamide.
PolythiazideDorzolamide may increase the hypotensive activities of Polythiazide.
PosaconazoleThe metabolism of Dorzolamide can be decreased when combined with Posaconazole.
PrazosinPrazosin may increase the hypotensive activities of Dorzolamide.
PrimidoneThe risk or severity of adverse effects can be increased when Dorzolamide is combined with Primidone.
PrimidoneThe metabolism of Dorzolamide can be increased when combined with Primidone.
PropranololPropranolol may increase the hypotensive activities of Dorzolamide.
PyrimethamineThe metabolism of Dorzolamide can be decreased when combined with Pyrimethamine.
QuinaprilDorzolamide may increase the hypotensive activities of Quinapril.
QuinidineDorzolamide may decrease the excretion rate of Quinidine which could result in a lower serum level and potentially a reduction in efficacy.
QuinineQuinine may increase the hypotensive activities of Dorzolamide.
RamiprilRamipril may increase the hypotensive activities of Dorzolamide.
RanolazineThe metabolism of Dorzolamide can be decreased when combined with Ranolazine.
RasagilineRasagiline may increase the hypotensive activities of Dorzolamide.
RemikirenRemikiren may increase the hypotensive activities of Dorzolamide.
RescinnamineDorzolamide may increase the hypotensive activities of Rescinnamine.
ReserpineReserpine may increase the hypotensive activities of Dorzolamide.
RifabutinThe metabolism of Dorzolamide can be increased when combined with Rifabutin.
RifampicinThe metabolism of Dorzolamide can be increased when combined with Rifampicin.
RifapentineThe metabolism of Dorzolamide can be increased when combined with Rifapentine.
RiociguatDorzolamide may increase the hypotensive activities of Riociguat.
RitonavirThe metabolism of Dorzolamide can be decreased when combined with Ritonavir.
RituximabDorzolamide may increase the hypotensive activities of Rituximab.
SafrazineSafrazine may increase the hypotensive activities of Dorzolamide.
SaprisartanDorzolamide may increase the hypotensive activities of Saprisartan.
SaquinavirThe metabolism of Dorzolamide can be decreased when combined with Saquinavir.
SecobarbitalThe metabolism of Dorzolamide can be increased when combined with Secobarbital.
SelegilineSelegiline may increase the hypotensive activities of Dorzolamide.
SelexipagDorzolamide may increase the hypotensive activities of Selexipag.
SildenafilSildenafil may increase the antihypertensive activities of Dorzolamide.
SiltuximabThe serum concentration of Dorzolamide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Dorzolamide can be increased when it is combined with Simeprevir.
SitaxentanDorzolamide may increase the hypotensive activities of Sitaxentan.
SorafenibThe metabolism of Dorzolamide can be decreased when combined with Sorafenib.
SpiraprilDorzolamide may increase the hypotensive activities of Spirapril.
St. John's WortThe serum concentration of Dorzolamide can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Dorzolamide can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Dorzolamide can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Dorzolamide can be decreased when combined with Sulfamethoxazole.
SulfisoxazoleThe metabolism of Dorzolamide can be decreased when combined with Sulfisoxazole.
TadalafilTadalafil may increase the antihypertensive activities of Dorzolamide.
TelaprevirThe metabolism of Dorzolamide can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Dorzolamide can be decreased when combined with Telithromycin.
TelmisartanDorzolamide may increase the hypotensive activities of Telmisartan.
TemocaprilDorzolamide may increase the hypotensive activities of Temocapril.
TerlipressinDorzolamide may increase the hypotensive activities of Terlipressin.
TiboloneDorzolamide may increase the hypotensive activities of Tibolone.
TicagrelorThe metabolism of Dorzolamide can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Dorzolamide can be decreased when combined with Ticlopidine.
TicrynafenDorzolamide may increase the hypotensive activities of Ticrynafen.
TimololTimolol may increase the hypotensive activities of Dorzolamide.
TocilizumabThe serum concentration of Dorzolamide can be decreased when it is combined with Tocilizumab.
TolazolineTolazoline may increase the hypotensive activities of Dorzolamide.
TolbutamideThe metabolism of Dorzolamide can be decreased when combined with Tolbutamide.
ToloxatoneToloxatone may increase the hypotensive activities of Dorzolamide.
TorasemideTorasemide may increase the hypotensive activities of Dorzolamide.
TrandolaprilTrandolapril may increase the hypotensive activities of Dorzolamide.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Dorzolamide.
TranylcypromineTranylcypromine may increase the hypotensive activities of Dorzolamide.
TravoprostTravoprost may increase the hypotensive activities of Dorzolamide.
TreprostinilTreprostinil may increase the hypotensive activities of Dorzolamide.
TrichlormethiazideDorzolamide may increase the hypotensive activities of Trichlormethiazide.
TrimazosinDorzolamide may increase the hypotensive activities of Trimazosin.
TrimethaphanDorzolamide may increase the hypotensive activities of Trimethaphan.
TrimethoprimThe metabolism of Dorzolamide can be decreased when combined with Trimethoprim.
UdenafilUdenafil may increase the antihypertensive activities of Dorzolamide.
UnoprostoneDorzolamide may increase the hypotensive activities of Unoprostone.
Valproic AcidThe metabolism of Dorzolamide can be decreased when combined with Valproic Acid.
ValsartanValsartan may increase the hypotensive activities of Dorzolamide.
VardenafilVardenafil may increase the antihypertensive activities of Dorzolamide.
VenlafaxineThe metabolism of Dorzolamide can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Dorzolamide can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Dorzolamide can be decreased when combined with Voriconazole.
XylometazolineDorzolamide may increase the hypotensive activities of Xylometazoline.
YohimbineYohimbine may decrease the antihypertensive activities of Dorzolamide.
ZafirlukastThe metabolism of Dorzolamide can be decreased when combined with Zafirlukast.
ZiprasidoneThe metabolism of Dorzolamide can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

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. Lachmann C, Jorg KM, Trinkmann R: [Postoperative behavior of intraocular pressure after posterior Nd:YAG laser capsulotomy--critical evaluation in preventive administration of local carbonic anhydrase II inhibitor dorzolamide hydrochloride (Trusopt)]. Klin Monbl Augenheilkd. 1998 Dec;213(6):326-30. [PubMed:10048009 ]
  2. Wong BK, Bruhin PJ, Barrish A, Lin JH: Nonlinear dorzolamide pharmacokinetics in rats: concentration-dependent erythrocyte distribution and drug-metabolite displacement interaction. Drug Metab Dispos. 1996 Jun;24(6):659-63. [PubMed:8781782 ]
  3. Berg JT, Ramanathan S, Gabrielli MG, Swenson ER: Carbonic anhydrase in mammalian vascular smooth muscle. J Histochem Cytochem. 2004 Aug;52(8):1101-6. [PubMed:15258186 ]
  4. Hasegawa T, Hara K, Hata S: Binding of dorzolamide and its metabolite, N-deethylated dorzolamide, to human erythrocytes in vitro. Drug Metab Dispos. 1994 May-Jun;22(3):377-82. [PubMed:8070313 ]
  5. Maren TH, Conroy CW, Wynns GC, Levy NS: Ocular absorption, blood levels, and excretion of dorzolamide, a topically active carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30. [PubMed:9029437 ]
  6. Sugrue MF: Pharmacological and ocular hypotensive properties of topical carbonic anhydrase inhibitors. Prog Retin Eye Res. 2000 Jan;19(1):87-112. [PubMed:10614682 ]
  7. Sugrue MF: The preclinical pharmacology of dorzolamide hydrochloride, a topical carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1996 Fall;12(3):363-76. [PubMed:8875343 ]
  8. Srinivas SP, Ong A, Zhai CB, Bonanno JA: Inhibition of carbonic anhydrase activity in cultured bovine corneal endothelial cells by dorzolamide. Invest Ophthalmol Vis Sci. 2002 Oct;43(10):3273-8. [PubMed:12356834 ]
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Sugrue MF: The preclinical pharmacology of dorzolamide hydrochloride, a topical carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1996 Fall;12(3):363-76. [PubMed:8875343 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Hasegawa T, Hara K, Hata S: Binding of dorzolamide and its metabolite, N-deethylated dorzolamide, to human erythrocytes in vitro. Drug Metab Dispos. 1994 May-Jun;22(3):377-82. [PubMed:8070313 ]
  2. Maren TH, Conroy CW, Wynns GC, Levy NS: Ocular absorption, blood levels, and excretion of dorzolamide, a topically active carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1997 Feb;13(1):23-30. [PubMed:9029437 ]
  3. Sugrue MF: The preclinical pharmacology of dorzolamide hydrochloride, a topical carbonic anhydrase inhibitor. J Ocul Pharmacol Ther. 1996 Fall;12(3):363-76. [PubMed:8875343 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
substrate
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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23