Bidin LS

Dosage Form & Strength

The recommended dose is one drop of Brimonidine in the affected eye(s) three times daily, approximately 8 hours apart. Brimonidine ophthalmic solution may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure If more than one topical ophthalmic product is to be used, the different products should be instilled at least 5 minutes apart

Dosage in Special Population

Pregnancy Category B: Brimonidine should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus Nursing Mothers It is not known whether brimonidine tartrate is excreted in human milk, although in animal studies, brimonidine tartrate has been shown to be excreted in breast milk. Because of the potential for serious adverse reactions from brimonidine tartrate in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Brimonidine tartratehas not been studied in patients with hepatic impairment Brimonidine tartrate has not been studied in patients with renal impairment The effect of dialysis on brimonidine pharmacokinetics in patients with renal failure is not known

Indications

Bidin LS is indicated for the treatment of Glaucoma & ocular hypertension

Contraindications

Brimonidine is contraindicated in neonates and infants (under the age of 2 years) Brimonidine is contraindicated in patients who have exhibited a hypersensitivity reaction to any component of this medication in the past

Adverse Effects

Most common adverse reactions reported in conjunction with ALT: transient conjunctival blanching (50%) and upper lid retraction (30%). Adverse reactions reported in 1% to 4% of the patients: drowsiness/tiredness, dizziness, corneal edema, and ocular irritation (encompassing foreign body sensation, ocular pain and discomfort).

Drug Interactions

Antihypertensives/Cardiac Glycosides: Because Brimonidine may reduce blood pressure, caution in using drugs such as antihypertensives and/or cardiac glycosides with Brimonidine is advised CNS Depressants: Although specific drug interaction studies have not been conducted with Brimonidine, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, or anesthetics) should be considered Tricyclic Antidepressants: Tricyclic antidepressants have been reported to blunt the hypotensive effect of systemic clonidine. It is not known whether the concurrent use of these agents with Brimonidine, in humans can lead to resulting interference with the IOP lowering effect. Caution is advised in patients taking tricyclic antidepressants which can affect the metabolism and uptake of circulating amines Monoamine Oxidase Inhibitors: Monoamine oxidase (MAO) inhibitors may theoretically interfere with the metabolism of brimonidine and potentially result in an increased systemic side-effect such as hypotension Caution is advised in patients taking MAO inhibitors which can affect the metabolism and uptake of circulating amines

Mechanism of Action

Brimonidine is a relatively selective alpha-2 adrenergic receptor agonist with a peak ocular hypotensive effect occurring at two hours postdosing Brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow

Pharmacokinetics

The half life of Brimonidine in Bidin LS is 3 hours

Absorption, Distribution, Metabolism & Excretion

Absorption: After ocular administration of either a 0.1% or 0.2% solution, plasma concentrations peaked within 0.5 to 2.5 hours and declined with a systemic half-life of approximately 2 hours Distribution: The protein binding of brimonidine has not been studied Metabolism: In humans, brimonidine is extensively metabolized by the liver Excretion Urinary excretion is the major route of elimination of brimonidine and its metabolites. Approximately 87% of an orally-administered radioactive dose of brimonidine was eliminated within 120 hours, with 74% found in the urine

Drug Use in Pregnancy

Pregnancy Category B: Teratogenicity studies have been performed in animals Brimonidine tartrate was not teratogenic when given orally during gestation days 6 through 15 in rats and days 6 through 18 in rabbits. The highest doses of brimonidine tartrate in rats (2.5 mg/kg/day) and rabbits (5.0 mg/kg/day) achieved AUC exposure values 360- and 20-fold higher, or 260- and 15-fold higher, respectively, than similar values estimated in humans treated with Brimonidine 0.1% or 0.15%, 1 drop in both eyes three times daily. There are no adequate and well-controlled studies in pregnant women; however, in animal studies,brimonidine crossed the placenta and entered into the fetal circulation to a limited extent Because animal reproduction studies are not always predictive of human response, Brimonidine should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus Nursing Mothers It is not known whether brimonidine tartrate is excreted in human milk, although in animal studies, brimonidine tartrate has been shown to be excreted in breast milk. Because of the potential for serious adverse reactions from brimonidine tartrate in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother Brimonidine tartrate is contraindicated in children under the age of 2 years Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and other adult patients. Brimonidine tartratehas not been studied in patients with hepatic impairment Brimonidine tartrate has not been studied in patients with renal impairment The effect of dialysis on brimonidine pharmacokinetics in patients with renal failure is not known

Drug Use in Renal Impairment

Brimonidine tartrate has not been studied in patients with renal impairment The effect of dialysis on brimonidine pharmacokinetics in patients with renal failure is not known

Drug Use in Hepatic Impairment

Pregnancy Category B: Teratogenicity studies have been performed in animals Brimonidine tartrate was not teratogenic when given orally during gestation days 6 through 15 in rats and days 6 through 18 in rabbits. The highest doses of brimonidine tartrate in rats (2.5 mg/kg/day) and rabbits (5.0 mg/kg/day) achieved AUC exposure values 360- and 20-fold higher, or 260- and 15-fold higher, respectively, than similar values estimated in humans treated with Brimonidine 0.1% or 0.15%, 1 drop in both eyes three times daily. There are no adequate and well-controlled studies in pregnant women; however, in animal studies,brimonidine crossed the placenta and entered into the fetal circulation to a limited extent Because animal reproduction studies are not always predictive of human response, Brimonidine should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus Nursing Mothers It is not known whether brimonidine tartrate is excreted in human milk, although in animal studies, brimonidine tartrate has been shown to be excreted in breast milk. Because of the potential for serious adverse reactions from brimonidine tartrate in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother

Drug Use in Pediatric Population

Brimonidine tartrate is contraindicated in children under the age of 2 years

Drug Use in Geriatric Population

Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and other adult patients.