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brinzolamide (Azopt)

 

Classes: Antiglaucoma, Carbonic Anhydrase Inhibitors

Dosing and uses of Azopt (brinzolamide)

 

Adult dosage forms and strengths

ophthalmic suspension

  • 1%

 

Ocular Hypertension or Open-Angle Glaucoma

1 gtt in affected eye q8hr

 

Administration

May be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure; if more than one topical ophthalmic drug being used, administer at least ten min apart

 

Pediatric dosage forms and strengths

Safety & efficacy not established

 

Azopt (brinzolamide) adverse (side) effects

1-10%

Blurred vision (1-5%)

Bitter, sour or unusual taste (1-5%)

Blepharitis (1-5%)

Dermatitis (1-5%)

Dry eye (1-5%)

Foreign body sensation (1-5%)

Headache (1-5%)

Hyperemia (1-5%)

Ocular discharge (1-5%)

Ocular discomfort (1-5%)

Ocular keratitis (1-5%)

Ocular pain (1-5%)

Ocular pruritus (1-5%)

Rhinitis (1-5%)

 

<1%

Allergic reactions

Alopecia

Chest pain

Conjunctivitis

Diarrhea

Diplopia

Dizziness

Dry mouth

Dyspnea

Dyspepsia

Eye fatigue

Hypertonia

Keratoconjunctivitis

Keratopathy

Kidney pain

Lid margin crusting or sticky sensation

Nausea

Pharyngitis

Tearing

Urticaria

Stevens-Johnson syndrome

Toxic epidermal necrolysis

Fulminant hepatic necrosis

Agranulocytosis

Aplastic anemia

Other blood dyscrasias

 

Warnings

Contraindications

Hypersensitivity

Severe renal impairment (CrCl <30 mL/min)

 

Cautions

Hepatic impairment

Corneal edema may occur in patients with low endothelial cell counts

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Not known if distributed in breast milk; not recommedned (discontinue drug or 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 Azopt (brinzolamide)

Mechanism of action

Inhibits carbonic anhydrase inhibitor, which in turn causes aqueous humor secretion to decreases

 

Pharmacokinetics

Half-Life: 3.5-4 mo

Absorption: Some systemic

Distribution: to RBCs

Protein binding: 60%

Excretion: Urine