Dorzolamide
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Dorzolamide
Trusopt; with timolol as Cosopt
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Summary
Common uses
Primary open-angle glaucoma0, Ocular hypertension0
Pharmacy
Starting dose
1 drop in affected eye(s) TID (monotherapy); BID with timolol (Cosopt)
Preparations
2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF)
US FDA Max
TID per eye
Pharmacology
Routes
Topical ophthalmic
Onset
IOP lowering at 2 hours; max at 4 hours
Duration
8-12 hours (TID dosing needed)
Half-life
~4 months in erythrocytes (carbonic anhydrase binding in red cells; not relevant to topical IOP duration)[1]
Bioavailability
Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)[1]
Pregnancy
Limited data; weigh against alternatives.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Dorzolamide selectively inhibits carbonic anhydrase II (CA-II) in the ciliary epithelium, reducing bicarbonate formation and aqueous humor production; IOP falls ~18-22% from baseline.0 Compared with oral acetazolamide, topical CAI provides similar local efficacy without the systemic acidosis, paresthesias, and kidney stone risk of systemic CA inhibition. Sulfonamide structural class — caution in severe sulfa allergy[1].
References
[edit | edit source]- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Trusopt (dorzolamide HCl), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020408s050lbl.pdf