(dor ZOLE a mide)
- Dorzolamide Hydrochloride
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Trusopt: 2% (10 mL)
Generic: 2% (10 mL)
Brand Names: U.S.
- Carbonic Anhydrase Inhibitor (Ophthalmic)
- Ophthalmic Agent, Antiglaucoma
Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor; also inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge from CNS neurons
Topical: Reaches systemic circulation where it accumulates in RBCs during chronic dosing as a result of binding to CA-II
In RBCs during chronic administration
To N-desethyl metabolite (less potent than parent drug)
Urine (as unchanged drug and metabolite, N-desethyl)
Duration of Action
8 to 12 hours
Terminal RBC half-life: 147 days; 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 4 months
Use: Labeled Indications
Elevated intraocular pressure: Treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma
Hypersensitivity to dorzolamide or any component of the formulation
Elevated intraocular pressure: Children, Adolescents, and Adults: Ophthalmic: Instill 1 drop in the affected eye(s) 3 times daily
Dosage adjustment in renal impairment:
CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer’s labeling.
CrCl <30 mL/minute: Use is not recommended (has not been studied).
Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling (have not been studied); use with caution.
Ophthalmic: If more than one topical ophthalmic drug is being used, administer the drugs at least 5 minutes apart. Remove contact lens prior to administration and wait 15 minutes before reinserting. Avoid allowing the tip of the dispensing container to contact the eye or surrounding structures.
Store at 15°C to 30°C (59°F to 86°F). Protect from light.
Alpha-/Beta-Agonists (Indirect-Acting): Carbonic Anhydrase Inhibitors may increase the serum concentration of Alpha-/Beta-Agonists (Indirect-Acting). Monitor therapy
Carbonic Anhydrase Inhibitors: May enhance the adverse/toxic effect of other Carbonic Anhydrase Inhibitors. The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Management: Avoid concurrent use of different carbonic anhydrase inhibitors if possible. Monitor patients closely for the occurrence of kidney stones and with regards to severity of metabolic acidosis. Avoid combination
Gastrointestinal: Bitter taste following administration (25%)
Ocular: Burning, stinging or discomfort immediately following administration (33%); superficial punctate keratitis (10% to 15%); signs and symptoms of ocular allergic reaction (10%)
1% to 5%: Ocular: Blurred vision, conjunctivitis, dryness, lid reactions, photophobia, redness, tearing
<1% (Limited to important or life-threatening): Allergic reaction (systemic), angioedema, bronchospasm, choriodal detachment (following filtration procedures), dyspnea, epistaxis, myopia (transient), ocular pain, paresthesia, pharyngitis, Stevens-Johnson syndrome, throat irritation, toxic epidermal necrolysis
Concerns related to adverse effects:
• Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.
• Ocular effects: Local ocular adverse effects (primarily conjunctivitis and lid reactions) were reported with chronic administration; many resolved upon discontinuation of drug therapy. Choroidal detachment has been reported after filtration procedures.
• Sulfonamide (“sulfa”) allergy: Dorzolamide is a sulfonamide; although administered ocularly, systemic absorption may occur and could result in hypersensitivity. Discontinue use if signs of hypersensitivity or a serious reaction occur.
• Systemic effects: Systemic absorption and adverse effects (similar to sulfonamides) including, blood dyscrasias, Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias may occur with ophthalmic use.
• Corneal endothelium: Use with caution in patients with low endothelial cell counts; may be at increased risk of corneal edema.
• Hepatic impairment: Use with caution in patients with hepatic impairment (has not been studied).
• Renal impairment: Use is not recommended in patients with severe renal impairment (CrCl <30 mL/minute) (has not been studied).
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed.
• Contact lens wearers: Some products contain benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting.
• Appropriate use: Should be used in combination with therapeutic interventions for the treatment of acute angle-closure glaucoma.
Ophthalmic exams and IOP periodically
Pregnancy Risk Factor
Adverse events have been observed in animal reproduction studies following systemic administration. IOP is usually lower during pregnancy. If topical medications for the treatment of glaucoma in pregnant women cannot be discontinued because small increases in IOP cannot be tolerated, the minimum effective dose should be used in combination with punctual occlusion to decrease exposure to the fetus (Johnson, 2001).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience blurred vision, parageusia, xerophthalmia, lacrimation, or sensitivity to light. Have patient report immediately to prescriber vision changes, ophthalmalgia, severe eye irritation, edema of eye or eyelid, or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about dorzolamide ophthalmic
- Other brands: Trusopt