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dorzolamide (Trusopt)

 

Classes: Antiglaucoma, Carbonic Anhydrase Inhibitors

Dosing and uses of Trusopt (dorzolamide)

 

Adult dosage forms and strengths

ophthalmic solution

  • 2%

 

Ocular Hypertension

Instill 1 gtt in affected eye(s) q8hr

 

Pediatric dosage forms and strengths

ophthalmic solution

  • 2%

 

Ocular Hypertension

As in adults; 1 gtt in affected eye(s) q8hr

 

Trusopt (dorzolamide) adverse (side) effects

>10%

Ocular burning, stinging, discomfort (33%)

Bitter taste (25%)

Superficial punctate keratitis (10-15%)

Ocular allergic reactions (10%)

 

Frequency not defined

Blurred vision

Ocular dryness

Photophobia

Ocular redness

Tearing

Stevens-Johnson syndrome

Toxic epidermal necrolysis

Angioedema

Bronchospasm

Dyspnea

Epistaxis

 

Warnings

Contraindications

Hypersensitivity

Severe reanl impairment (CrCl<30 mL/min)

 

Cautions

Bacterial contamination can occur with multiple dose ophthalmic solutions and cause bacterial keratitis

Remove contact lenses, since the solution contains benzalkonium chloride which may be absorbed by some lenses

Absorbed systemically, potential risk of adverse effects similar to those for systemic sulfonamides (eg, Stevens-Johnson synd, blood dyscrasias, fulminant hepatic necrosis, and toxic necrolysis) may occur with ophthalmic use

Conjunctivitis and lid reactions reported with chronic administration (may resolve with discontinuation of drug therapy

Risk of corneal edema higher in patients with low endothelial cell counts; use catuion

Use concomitantly with oral carbonic anhydrase inhibitors not recommended

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Not known whether distributed into breast milk; Do not nurse

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Trusopt (dorzolamide)

Mechanism of action

Sulfonamide and carbonic anhydrase inhibitor that reduces the secretion of hydrogen ion at renal tubule and increases excretion of bicarbonate, potassium, sodium, and water, which in turn decreases aqueous humor secretion

 

Pharmacokinetics

Absorption: Yes

Duration: 8-12hr

Peak effect: 2 hr

Onset of action: 2 hr

Half-life: 120 days

Peak Plasma: 24 mcg/g (cornea); 27 mcg/g (iris/ciliary body), 7.8 mcg/mL (aqueous humor)

Protein bound: 33% (to plasma proteins)

Metabolism: Liver, by cytochrome P450 isozymes to N-desethyldorzolamide

Excretion: Urine (80%)