Ocular hypertension/glaucoma (open-angle): Ophthalmic: Instill 1 drop in the affected eye(s) 3 times daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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).
Dorzolamide and its metabolite (N-desethyl: less potent than parent) are excreted renally. Patients with renal impairment, particularly neonates and geriatric patients, should be monitored carefully for untoward effects due to reduced dorzolamide elimination.
There are no dosage adjustments provided in the manufacturer’s labeling (have not been studied); use with caution.
(For additional information see "Dorzolamide: Pediatric drug information")
Reduction of intraocular pressure:
Monotherapy: Infants, Children, and Adolescents: Ophthalmic: Instill 1 drop to affected eye(s) 3 times daily (Ott 2005; Quaranta 2018).
Combination therapy (with latanoprost): Limited data available: Infants, Children, and Adolescents: Ophthalmic: Instill 1 drop to affected eye(s) 2 times daily (Quaranta 2018).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling.
CrCl <30 mL/minute: All patients: Use is not recommended (has not been studied).
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic:
Trusopt: 2% (10 mL)
Generic: 2% (10 mL)
Yes
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic:
Trusopt: 2% (5 mL) [contains benzalkonium chloride]
Trusopt (Preservative Free): 2% (0.2 mL, 5 mL)
Generic: 2% (5 mL, 10 mL)
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. Use eyelid closure or nasolacrimal occlusion when applying topical medications to reduce systemic absorption.
Ophthalmic: Wash hands before use. Unscrew the cap by turning in the direction of the arrows on top of the cap. Pull lower eyelid down slightly to form a pocket for the eye drop and tilt head back; administer 1 drop. Apply gentle pressure to lacrimal sac immediately following instillation (1 minute) or instruct patient to gently close eyelid after administration to decrease systemic absorption of ophthalmic drops (Urtti 1993; Zimmerman 1984). Avoid contact of bottle tip with skin or eye; ocular solutions can become contaminated by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may occur from using contaminated solutions. Some solutions contain benzalkonium chloride; remove contact lenses prior to administration and wait at least 15 minutes after instillation before reinserting soft contact lenses. If more than one topical ophthalmic drug is being used, separate administration by at least 5 minutes.
Ocular hypertension/glaucoma (open-angle): Treatment of elevated intraocular pressure.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not always defined.
Dermatologic: Skin rash
Gastrointestinal: Bitter taste (~25% following administration), nausea
Genitourinary: Urolithiasis
Hypersensitivity: Local ocular hypersensitivity reaction (~10%)
Nervous system: Fatigue, headache
Neuromuscular & skeletal: Asthenia
Ocular: Burning sensation of eyes (~33%), eye discomfort (~33%), stinging of eyes (~33%), superficial punctate keratitis (10% to 15%), blurred vision (1% to 5%), conjunctivitis (1% to 5%), eyelid irritation (1% to 5%), eye redness (1% to 5%), lacrimation (1% to 5%), photophobia (1% to 5%), xerophthalmia (1% to 5%), iridocyclitis
<1%, postmarketing and/or case reports: Angioedema, bronchospasm, choroidal detachment (following filtration procedures), contact dermatitis, crusting of eyelid, dizziness, dyspnea, epistaxis, myopia (transient), ocular pain, paresthesia, pruritus, Stevens-Johnson syndrome, throat irritation, toxic epidermal necrolysis, urticaria, xerostomia
Hypersensitivity to dorzolamide or any component of the formulation
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.
Disease-related concerns:
• 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).
Special populations:
• 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.
Other warnings/precautions:
• Appropriate use: Should be used in combination with therapeutic interventions for the treatment of acute angle-closure glaucoma.
Substrate of CYP2C9 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Alpha-/Beta-Agonists (Indirect-Acting): Carbonic Anhydrase Inhibitors may increase the serum concentration of Alpha-/Beta-Agonists (Indirect-Acting). Risk C: Monitor therapy
Amantadine: Carbonic Anhydrase Inhibitors may increase the serum concentration of Amantadine. Risk C: 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. Risk X: Avoid combination
Because information related to dorzolamide use in pregnancy is limited, other agents may be preferred for the treatment of glaucoma in pregnant patients. Use of topical carbonic anhydrase inhibitors may be considered after the first trimester. In general, if ophthalmic agents are needed in pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease exposure to the fetus (Belkin 2020; Strelow 2020).
It is not known if dorzolamide is present in breast milk.
In general, topical carbonic anhydrase inhibitors are considered compatible with breastfeeding. Administering after breastfeeding may help decrease potential exposure to the infant via breast milk (Belkin 2020; Strelow 2020).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Ophthalmic exams (optic nerve and visual field assessment), serial measurement of intraocular pressure (IOP). Frequency of follow up based upon whether target IOP achieved, if there is any progression of damage, and how long disease has been controlled (AAO 2019).
Reversible inhibition of the enzyme carbonic anhydrase II and IV in the ciliary epithelium 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 to reduce intraocular pressure.
Duration of action: 8 to 12 hours
Absorption: Topical: Reaches systemic circulation where it accumulates in RBCs during chronic dosing as a result of binding to CA-II
Distribution: In RBCs during chronic administration
Protein binding: ~33%
Metabolism: To N-desethyl metabolite (less potent than parent drug)
Half-life elimination: 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
Excretion: Urine (as unchanged drug and metabolite, N-desethyl)
Solution (Dorzolamide HCl Ophthalmic)
2% (per mL): $4.08 - $6.68
Solution (Trusopt Ophthalmic)
2% (per mL): $9.10
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