Dorzolamide
- Atc Codes:S01EC03
- CAS Codes:130693-82-2#120279-96-1
- PHARMGKB ID:130693-82-2#120279-96-1
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Dorzo-Vision, Trusopt; Belgium: Trusopt; Bulgaria: Dorzopt, Trusopt; Cyprus: Trusopt; Czech Republic: Trusopt; Denmark: Dorzolamid, Trusopt; Estonia: Trusopt; Finland: Dorzolamid, Dorzolamide, Trusopt; France: Trusopt; Germany: Dorzolamid, Trusopt; Greece: Dorolad, Dorzolamide, Optodrop, Trusopt; Ireland: Trusopt; Italy: Trusopt; Latvia: Dorzolamide, Trusopt; Lithuania: Trusopt; Malta: Trusopt; Netherlands: Dorzolamide, Trusopt; Poland: Dolopt, Dorzolamid, Dorzolamide, Trusopt; Portugal: Dorzolamida, Proglau, Trusopt; Romania: Dorzolamide, Dorzopt, Trusopt; Slovakia: Dorzolamid, Trusopt; Slovenia: Trusopt; Spain: Trusopt; Sweden: Dorzolamid, Trusopt; UK: Trusopt.
North America
Canada: Trusopt; USA: Dorzolamide, Trusopt.
Latin America
Argentina: Dorlamida, Trusopt; Brazil: Dorzolamida, Ocupress-União Química, Trusopt; Mexico: Trusopt.
Asia
Japan: Trusopt.
Drug combinations
Dorzolamide and Timolol
Chemistry
Dorzolamide Hydrochloride: C~10~H~16~N~2~O~4~S~3~ HCl. Mw: 360.90. (1) 4H-Thieno[2,3-b]thiopyran-2-sulfonamide, 4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide, monohydrochloride, (4S-trans)-; (2)(4S,6S)-4-(Ethylamino)-5,6-dihydro-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide, monohydrochloride. CAS-130693-82-2; CAS-120279-96-1 (dorzolamide)(1992).
Pharmacologic Category
Antiglaucoma Agents; Carbonic Anhydrase Inhibitors. (ATC-Code: S01EC03).
Mechanism of action
Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor. Inhibits carbonic anhydrase in CNS to retard abnormal and excessive discharge from CNS neurons.
Therapeutic use
Reduction of elevated IOP in open-angle glaucoma or ocular hypertension. Dorzolamide and timolol in a fixed-combination ophthalmic solution is used topically to reduce elevated IOP in patients with open-angle glaucoma or ocular hypertension who have not responded adequately (i.e. failed to achieve target IOP) to a topical β-adrenergic blocking agent.
Pregnancy and lactiation implications
The drug should be used during pregnancy only when potential benefits justify possible risks to the fetus.
Unlabeled use
Topical dorzolamide has been used prophylactically before neodymium yttrium aluminum garnet (Nd:YAG) lasar posterior capsulotomy.
Contraindications
Hypersensitivity to dorzolamide or any component of the formulation (e.g. benzalkonium chloride). Fixed-combination preparation with timolol contraindicated in bronchial asthma or history of bronchial asthma and in severe chronic obstructive pulmonary disease, sinus bradycardia, atrioventricular block greater than first degree, overt cardiac failure, or cardiogenic shock.
Warnings and precautions
Risk of serious adverse events (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, other blood dyscrasias) associated with sulfonamide therapy. Discontinue dorzolamide if serious reactions or signs or symptoms of hypersensitivity occur. Avoid use in sulfonamide allergy. Conjunctivitis or lid reactions reported with long-term therapy (may resolve upon discontinuance of therapy). Choroidal detachment reported with administration of aqueous suppressant therapy (e.g. dorzolamide, timolol) following filtration procedures. Not studied in hepatic impairment (use with caution). Not recommended in severe renal impairment (CrCl <30 mL/minute), since dorzolamide and its metabolite are excreted mainly by the kidneys. Product contains benzalkonium chloride which may be absorbed by soft contact lenses.