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Dorzolamide information from DrugsUpdate  

See Available Brands of Dorzolamide in India

P - Caution when used during pregnancy
L - Contraindicated in lactation

Dorzolamide (trade name Trusopt) is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. This drug, developed by Merck, was the first drug in human therapy (market introduction 1995) which resulted from structure-based drug design. Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.

Pharmacodynamics

When topically applied, Dorzolamide reaches the systemic circulation. To assess the potential for systemic carbonic anhydrase inhibition following topical administration, drug and metabolite concentrations in RBCs and plasma and carbonic anhydrase inhibition in RBCs were measured.
Dorzolamide accumulates in RBCs during chronic dosing as a result of binding to CA-II. The parent drug forms a single N-desethyl metabolite, which inhibits CA-II less potently than the parent drug but also inhibits CA-I. The metabolite also accumulates in RBCs where it binds primarily to CA-I. Plasma concentrations of Dorzolamide and metabolite are generally below the assay limit of quantitation (15nM). Dorzolamide binds moderately to plasma proteins (approximately 33%). Dorzolamide is primarily excreted unchanged in the urine; the metabolite also is excreted in urine. After dosing is stopped, Dorzolamide washes out of RBCs nonlinearly, resulting in a rapid decline of drug concentration initially, followed by a slower elimination phase with a half-life of about four months.
To stimulate the systemic exposure after long-term topical ocular administration, Dorzolamide was given orally to eight healthy subjects for up to 20 weeks. The oral dose of 2 mg b.i.d. closely approximates the amount of drug delivered by topical ocular administration of Dorzolamide Hydrochloride Ophthalmic Solution 2% t.i.d. Steady state was reached within 8 weeks. The inhibition of CA-II and total carbonic anhydrase activities was below the degree of inhibition anticipated to be necessary for a pharmacological effect on renal function and respiration in healthy individuals.

Pharmacokinetics

Dorzolamide is a carbonic anhydrase inhibitor that reduces formation of hydrogen and carbonate ions from CO2 and water thereby reducing aqueous humor secretion, thus lowering intraocular pressure.

Dorzolamide Indications / Dorzolamide Uses

Information Not Available

Dorzolamide Adverse Reactions / Dorzolamide Side Effects

Conjunctivitis; superficial punctate keratitis; ocular burning, stinging or itching; eyelid inflammation and crusting; blurred vision; lachrymation; anterior uveitis; transient myopia; corneal oedema; iridocyclitis; headache; dizziness; paraesthesia; asthenia; sinusitis; nausea; hypersensitivity reactions; bitter taste; epistaxis; urolithiasis; rhinitis.

Precautions

Monitor
Note baseline IOP before starting medication and monitor periodically during long-term treatment.
Renal Function
Not recommended for use in patients with severe renal function impairment.
Hepatic Function
Use with caution.
Bacterial keratitis
Can occur by using contaminated eye drops.
Concomitant use of oral carbonic anhydrase inhibitors
Not recommended.
Contact lenses
Do not administer while wearing soft contact lenses; preservative may be absorbed by soft contact lenses.
Overdosage
Symptoms
Electrolyte imbalance, acidotic state, possible CNS effects.

Special Precautions

Hepatic impairment; systemic absorption following topical admin; history of renal calculi or intraocular surgery; chronic corneal defects; risk of choroidal detachment when used after filtration procedures.

Other Drug Interactions

Enhance effects of amphetamines, ephedrine, quinidine. Reduce effects of methenamine and its compounds. Enhance antiepileptic-induced osteomalacia. Severe acidosis and increased CNS toxicity with aspirin. Increased excretion of lithium.

Other Interactions

Information Not Available

Dosage

Ophthalmic
Ocular hypertension, Open-angle glaucoma
Adult: As 2% eye drops: 1 drop tid; bid when used with a topical β-blocker.

Food(before/after)

Information Not Available

List of Contraindications

Dorzolamide and Pregnancy

Caution when used during pregnancy.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Dorzolamide and Lactation

Contraindicated in lactation

Dorzolamide and Children

Safety and efficacy not established

Dorzolamide and Geriatic

Information Not Available

Dorzolamide and Other Contraindications

Severe renal impairment; hypersensitivity; hyperchloraemic acidosis, Lactation

Storage

Ophthalmic: Store at 15-30°C

Lab interference

Ophthalmic: Store at 15-30°C

Dorzolamide brands in India:

Dortas Dorzox Dorzox-T Misopt Ocudor Ocudor-T Right Angle

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