betaxolol ophthalmic (Rx)

>10%

Ocular effects

• Short term discomfort (<25%)

Frequency Not Defined

Ocular

• Blurred vision
• Corneal punctate keratitis
• Itching and/or foreign body sensation erythema
• Inflammation
• Ocular pain and/or discharge
• Ocular drynes
• Photophobia

Systemic

• Bradycardia, congestive heart failure, heart block
• Depression, dizziness, headache, insomnia, lethargy, vertigo
• Hair loss, hives, toxic epidermal necrolysis
• Glossitis
• Bronchospasm, dyspnea
• Increase in signs and symptoms of myasthenia gravis

Contraindications

Hypersensitivity, sinus bradycardia, cardiogenic shock, >1st deg AV block, overt cardiac failure

Cautions

As with many topically applied ophthalmic drugs, this drug is absorbed systemically; same adverse reactions found with systemic administration of beta-adrenergic receptor inhibitors may occur with topical administration; that includes severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and death due to cardiac failure, reported with topical application of beta-adrenergic receptor inhibitors

Beta-adrenergic receptor inhibitors should be administered with caution in patients subject to hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents; beta-adrenergic receptor inhibitors may mask the signs and symptoms of acute hypoglycemia

Beta-adrenergic receptor inhibitors may mask certain clinical signs (eg, tachycardia) of hyperthyroidism; patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic receptor inhibitors, which might precipitate a thyroid storm

Beta-adrenergic receptor inhibitors reported to potentiate muscle weakness consistent with certain myasthenic symptoms (eg, diplopia, ptosis, and generalized weakness)

Exercise caution in the treatment of glaucoma patients with excessive restriction of pulmonary function; there have been reports of asthmatic attacks and pulmonary distress during betaxolol treatment

Although rechallenges of some such patients with ophthalmic betaxolol have not adversely affected pulmonary function test results, the possibility of adverse pulmonary effects in patients sensitive to beta-adrenergic receptor inhibitors cannot be ruled out

While taking beta-adrenergic receptor inhibitors, patients with history of atopy or history of severe anaphylactic reaction to variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens; such patients may be unresponsive to usual doses of epinephrine used to treat anaphylactic reactions

In patients with angle-closure glaucoma, immediate treatment objective is to reopen the angle; this may require constricting the pupil; therapy has little or no effect on pupil and should not be used alone in treatment of angle-closure glaucoma

Because of potential effects of beta-adrenergic receptor inhibitors on blood pressure and pulse, these inhibitors should be used with caution in patients with vascular insufficiency; if signs or symptoms suggesting reduced cerebral blood flow or Raynaud’s phenomenon develop following initiation of therapy with this drug, alternative therapy should be considered

Bacterial keratitis may occur with use of multiple-dose containers of topical ophthalmic products when these containers are inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface; instruct patients on appropriate instillation techniques

Choroidal detachment after filtration procedures reported with administration of aqueous suppressant therapy

The preservative benzalkonium chloride may be absorbed by soft contact lenses; contact lenses should be removed during instillation of the drug but may be reinserted 15 minutes after instillation

Surgical anesthesia

• The necessity or desirability of withdrawal of beta-adrenergic receptor inhibitors prior to major surgery is controversial; beta-adrenergic receptor inhibitors impair the ability of the heart to respond to beta adrenergically mediated reflex stimuli; this may augment the risk of general anesthesia in surgical procedures
• Some patients receiving beta-adrenergic receptor inhibitors have experienced protracted, severe hypotension during anesthesia; difficulty in restarting and maintaining the heartbeat has also been reported
• In patients undergoing elective surgery, consider gradual withdrawal of beta-adrenergic receptor inhibitors
• If necessary, during surgery, the effects of beta-adrenergic receptor inhibitors may be reversed by sufficient doses of adrenergic agonists

Pregnancy Category: C

Lactation: Excretion in milk unknown; use with caution

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.

Mechanism of Action

Selective beta1-blocker; reduces intraocular pressure by reducing production of aqueous humor

Pharmacokinetics

Onset: Within 30 min

Duration: 12 hr

Excretion: Urine (80%)