Included as part of the PRECAUTIONS section.
Topically applied beta-adrenergic blocking agents may be absorbed systemically.
The same adverse reactions found with systemic administration of beta-adrenergic
blocking agents may occur with topical administration. For example, severe respiratory
reactions and cardiac reactions, including death due to bronchospasm in patients
with asthma, and rarely death in association with cardiac failure, have been
reported with topical application of beta-adrenergic blocking agents.
BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) Ophthalmic Suspension has been shown to have a minor effect
on heart rate and blood pressure in clinical studies. Caution should be used
in treating patients with a history of cardiac failure or heart block. Treatment
with BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) Ophthalmic Suspension should be discontinued at the first
signs of cardiac failure.
Bronchospasm and Obstructive Pulmonary Disease
Caution should be exercised 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 has not adversely affected pulmonary
function test results, the possibility of adverse pulmonary effects in patients
sensitive to beta-blockers cannot be ruled out.
Beta-adrenergic blocking agents may mask certain clinical signs (e.g., tachycardia)
of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be
managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents,
which might precipitate a thyroid storm.
Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent
with certain myasthenic symptoms (e.g., diplopia, ptosis and generalized weakness).
Consideration should be given to the gradual withdrawal of beta-adrenergic
blocking agents prior to general anesthesia because of the reduced ability of
the heart to respond to beta-adrenergically mediated sympathetic reflex stimuli.
Beta-adrenergic blocking agents should be administered with caution in patients
subject to spontaneous hypoglycemia or to diabetic patients (especially those
with labile diabetes) who are receiving insulin or oral hypoglycemic agents.
Beta-adrenergic receptor blocking agents may mask the signs and symptoms of
While taking beta-blockers, patients with a history of atopy or a history of
severe anaphylactic reaction to a variety of allergens may be more reactive
to repeated accidental, diagnostic, or therapeutic challenge with such allergens.
Such patients may be unresponsive to the usual doses of epinephrine used to
treat anaphylactic reactions.
In patients with angle-closure glaucoma, the immediate treatment objective
is to reopen the angle by constriction of the pupil with a miotic agent. Racemic
betaxolol has little or no effect on the pupil. It is expected that levobetaxolol
will also have little or no effect on the pupil. When BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) Ophthalmic
Suspension is used to reduce elevated intraocular pressure in angle-closure
glaucoma, it should be used with a miotic and not alone.
Carcinogenesis, Mutagenesis, Impairment of Fertility
In lifetime studies in mice at oral doses of 6, 20 and 60 mg/kg/day and in
rats at oral doses of 3, 12 and 48 mg/kg/day, betaxolol HCl demonstrated no carcinogenic effect. Levobetaxolol was not mutagenic in the Ames assay, chromosomal
aberration, mouse lymphoma, and cell transformation assays in vitro. Levobetaxolol
demonstrated potential mutagenicity in the sister chromatid exchange assay in
Chinese Hamster Ovarian cell in vitro in the presence of metabolic activation
Use In Specific Populations
Pregnancy Category C
Reproduction, teratology, and peri- and postnatal studies have been conducted
with orally administered betaxolol HCl and levobetaxolol HCl in rats and rabbits.
There was evidence of drug related postimplantation loss in rabbits with levobetaxolol
HCl at 12 mg/kg/day and sternebrae malformations at 4 mg/kg/day. No other adverse
effects on reproduction were noted at subtoxic dose levels.
There are no adequate and well-controlled studies in pregnant women. BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension)
Ophthalmic Suspension should be used during pregnancy only if the potential
benefit justifies the potential risk to the fetus.
It is not known whether BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) Ophthalmic Suspension is excreted in
human milk. Because many drugs are excreted in human milk, caution should be
exercised when BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) Ophthalmic Suspension is administered to nursing
The safety and IOP-lowering effects of BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) Ophthalmic Suspension
have been demonstrated in pediatric patients in a three-month controlled trial.
No overall differences in safety or effectiveness have been observed between
elderly and other adult patients.