Pharmacology Of Dorzolamide

Indication For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Also used prophylatically for the inhibition of perioperative IOP increase (before neodynium yttrium aluminum garnet laser posterior capsulotomy).
Pharmacodynamics Dorzolamide is topical CA inhibitor that is indicated for the reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers. Dorzolamide reduces IOP by approximately 17-23% in patients with elevater IOP.
Mechanism of action Dorzolamide is a sulfonamide and a highly specific carbonic anhydrase II (CA-II) inhibitor, which is the main CA isoenzyme involved in aqueous humor secretion. Inhibition of CA-II in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. Dorzolamide also accumulates in red blood cells as a result of CA-II binding, as CA-II is found predominantly in erythrocytes. However, sufficient CA-II activity remains so that adverse effects due to systemic CA inhibition are not observed.
Absorption Not Available
Volume of distribution Not Available
Protein binding ~33%
Metabolism Not Available
Route of elimination Dorzolamide is primarily excreted unchanged in the urine; the metabolite also is excreted in urine.
Half life 4 months
Clearance Not Available
Toxicity Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest

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