Generic
Brinzolamide + Brimonidine Tartrate
21 brands available in the market
At a glance
Brinzolamide 1% + Brimonidine Tartrate 0.2% Eye Prep is a combination medication used for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Brinzolamide reduces aqueous humour secretion and Brimonidine reduces aqueous humour production and increases uveoscleral outflow, together lowering intraocular pressure.
Description
Brinzolamide 1% + Brimonidine Tartrate 0.2% Eye Prep is a combination medication used for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It contains Brinzolamide (a carbonic anhydrase inhibitor) and Brimonidine Tartrate (an alpha-2 adrenergic receptor agonist).
Brinzolamide inhibits carbonic anhydrase in the ciliary processes, decreasing aqueous humour secretion, presumably by slowing bicarbonate ion formation with subsequent reduction in sodium and fluid transport. Brimonidine Tartrate reduces aqueous humour production and increases uveoscleral outflow, lowering IOP. Brinzolamide has a peak ocular hypotensive effect at 2-3 hours, while Brimonidine peaks at 2 hours post-dosing.
Indications
- Open-angle glaucoma
- Ocular hypertension
Therapeutic class
Drugs for miotics and glaucoma
Pharmacological class
Carbonic Anhydrase Inhibitor + Alpha-2 Adrenergic Agonist Combination
Pharmacology
Brinzolamide (carbonic anhydrase inhibitor) and Brimonidine Tartrate (alpha-2 adrenergic receptor agonist) each decrease elevated intraocular pressure. Brinzolamide inhibits carbonic anhydrase in the ciliary processes to decrease aqueous humour secretion. Brimonidine Tartrate has a dual mechanism of action by reducing aqueous humour production and increasing uveoscleral outflow.
Mechanism of action
Brinzolamide inhibits carbonic anhydrase in the ciliary body, reducing aqueous humour secretion. Brimonidine Tartrate activates alpha-2 receptors, reducing aqueous humour production and increasing uveoscleral outflow. Together, these mechanisms significantly lower intraocular pressure.
Dosage
Adults: Instill 1 drop in the affected eye(s) three times daily. Shake well before use.
Children (2 years and older): Instill 1 drop in the affected eye(s) 2-3 times daily.
Children under 2 years: Contraindicated.
Note: If more than one topical ophthalmic drug is being used, administer at least 5 minutes apart. Apply pressure on the corner of the eye (close to the nose) for about 1 minute after instillation (to reduce systemic absorption). Use within 1 month of opening.
Administration
For ophthalmic use only. Shake well before use. Wash hands before use. If using soft contact lenses, remove them before applying the drops and wait at least 15 minutes before reinserting (benzalkonium chloride may be absorbed by soft contact lenses). Do not touch the dropper tip to any surface or your eye (to avoid contamination). Hold the dropper close to the eye without touching it and place the drop inside the lower eyelid. Wipe off extra liquid.
Missed dose
If you miss a dose, apply it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Common (approximately 3-5% of patients): Blurred vision, eye irritation, dysgeusia (bad taste), dry mouth, eye allergy.
Brinzolamide-related (5-10%): Blurred vision, bitter/sour/unusual taste. (1-5%): Blepharitis, dermatitis, dry eye, foreign body sensation, headache, hyperemia, ocular discharge, ocular discomfort, keratitis, eye pain, pruritus, rhinitis.
Brimonidine-related (10-30%): Dry mouth, ocular hyperemia, burning and stinging, headache, blurred vision, foreign body sensation, fatigue/drowsiness, conjunctival follicles, ocular allergic reactions, ocular pruritus.
Avoid driving or operating machinery until you know how this medicine affects you.
Precautions & warnings
- May cause blurred or abnormal vision after use (especially at night or in reduced lighting); do not drive or operate machinery until vision is clear.
- Apply pressure on the corner of the eye (close to the nose) for about 1 minute after instillation (to reduce systemic absorption and minimize drug transfer to breast milk).
- Use within 1 month of opening.
- Remove soft contact lenses before use and wait at least 15 minutes before reinserting.
- Brinzolamide is a sulfonamide; although administered topically, it is absorbed systemically. Serious sulfonamide-related reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia) may occur.
- Brimonidine may potentiate syndromes associated with vascular insufficiency (depression, cerebral/coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, thromboangiitis obliterans); caution required.
- Not recommended in severe renal impairment.
Contraindications
- Hypersensitivity to brinzolamide, brimonidine tartrate, or any ingredient
- Neonates and infants (under 2 years of age)
Drug interactions
- High-dose salicylate therapy: May cause toxicity.
- CNS depressants (alcohol, barbiturates, opiates, sedatives, anesthetics): Additive or potentiating effects (caution required).
- Antihypertensives, cardiac glycosides: Caution required.
- Tricyclic antidepressants (TCAs): May affect the metabolism and uptake of circulating amines.
- MAO inhibitors: Interactions may occur.
- Oral carbonic anhydrase inhibitors: Additive systemic effects.
Food interactions
No food interactions found/established.
Use in pregnancy
May be unsafe during pregnancy (Category C). Limited human studies available; animal studies have shown harmful effects on the developing baby. Use during pregnancy only if potential benefit justifies potential risk to the fetus.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
It is not known whether this combination is excreted in human milk following topical ocular administration. Because many drugs are excreted in human milk and due to potential serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug.
Pediatric use
Contraindicated in children under 2 years (severe somnolence and decreased alertness seen in 50-83% of patients 2-6 years old with brimonidine). Children 2 years and older: 1 drop 2-3 times daily.
Geriatric use
No overall differences in safety or effectiveness have been observed between elderly and adult patients.
Renal / hepatic impairment
Hepatic impairment: Caution required in liver disease; consult your doctor.
Overdose effects
Oral overdose: Electrolyte imbalance, acidotic state, and possible nervous system effects may occur. Monitor serum electrolytes (especially potassium) and blood pH. Brimonidine overdose may cause hypotension. Treatment: Supportive and symptomatic therapy; maintain a patent airway.
Storage conditions
Store at room temperature, protected from light. Do not touch dropper tip to any surface. Do not use more than 1 month after first opening. Shake well before use. Do not freeze.
Chemical structure
Brinzolamide 1% + Brimonidine Tartrate 0.2%