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Brimonidine information from DrugsUpdate  

See Available Brands of Brimonidine in India

P - Contraindicated in pregnancy
L - Cautioned while taken during lactation

Brimonidine (bri-MOE-ni-deen, brand names Alphagan and Alphagan-P) is a drug used to treat open-angle glaucoma or ocular hypertension. Alphagan is also used to induce miosis for people suffering from poor night vision after Lasik or PRK surgery.
It acts via decreasing synthesis of aqueous humor, and increasing the amount that drains from the eye. As a treatment for glaucoma, it is usually given in eyedrop form.
Brimonidine is an α2-adrenergic receptor agonist.
Alpha 2 agonists, through the activation of the Gi GPCR, inhibit the activity of adenylate cyclase. This reduces cAMP and hence Aqueous Humour production by the ciliary body.

Pharmacodynamics

Pharmacokinetics

After ocular administration of a 0.2% solution, plasma concentrations peaked within 1 to 4 hours and declined with a systemic half-life of approximately 3 hours. In humans, systemic metabolism of Brimonidine is extensive. It is metabolized primarily by the liver. Urinary excretion is the major route of elimination of the drug and its metabolites. Approximately 87% of an orally administered radioactive dose was eliminated within 120 hours, with 74% found in the urine.

Brimonidine Indications / Brimonidine Uses

In open angle glaucoma

Brimonidine Adverse Reactions / Brimonidine Side Effects

Oral dryness; ocular hyperaemia, burning and stinging; headache, blurring of vision; foreign body sensation, fatigue or drowsiness; conjunctival follicles, ocular allergic reactions and ocular pruritus. Corneal staining or erosion, photophobia, eyelid erythema, ocular ache and pain, ocular dryness, tearing; upper respiratory symptoms; eyelid oedema, conjunctival oedema, dizziness, blepharitis, ocular irritation; GI symptoms; asthaenia; conjunctival blanching, abnormal vision and muscular pain.

Precautions

General
Although Brimonidine tartrate ophthalmic solution 0.2% had minimal effect on blood pressure of patients in clinical studies, caution should be exercised in treating patients with severe cardiovascular disease.
Brimonidine tartrate ophthalmic solution 0.2% has not been studied in patients with hepatic or renal impairment; caution should be used in treating such patients.
Brimonidine tartrate ophthalmic solution 0.2% should be used with caution in patients with depression, cerebral or coronary insufficiency, Raynaud’s phenomenon, orthostatic hypotension or thromboangiitis obliterans.
During the studies there was a loss of effect in some patients. The IOP-lowering efficacy observed with Brimonidine tartrate ophthalmic solution 0.2% during the first month of therapy may not always reflect the long-term level of IOP reduction. Patients prescribed IOP-lowering medication should be routinely monitored for IOP.

Special Precautions

Patients wearing soft contact lenses should wait for at least 15 min after instilling brimonidine tartrate before inserting soft contact lenses. Renal or hepatic impairment. CV disease. Use with caution in patients with depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension or thromboangitis obliterans. Pregnancy, lactation.

Other Drug Interactions

Possibility of an additive or potentiating effect with CNS depressants e.g. alcohol, barbiturates, opiates, sedatives or anaesthetics. Caution when used with β-blockers (ophthalmic and systemic), antihypertensives or cardiac glycosides. TCAs can affect the metabolism and uptake of circulating amines.

Other Interactions

Information Not Available

Dosage

Ophthalmic
Open-angle glaucom
Adult: Instill 1 drop of a 0.2% solution bid-tid.

Food(before/after)

Information Not Available

List of Contraindications

Brimonidine and Pregnancy

Caution when used during pregnancy
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Brimonidine and Lactation

Caution when used during lactation

Brimonidine and Children

In a well-controlled clinical study conducted in pediatric glaucoma patients (ages 2 to 7 years) the most commonly observed adverse events with Brimonidine tartrate ophthalmic solution 0.2% dosed three times daily were somnolence (50% - 83% in patients ages 2 to 6 years) and decreased alertness. In pediatric patients 7 years of age or older (>20kg), somnolence appears to occur less frequently (25%). The most commonly observed adverse event was somnolence. Approximately 16% of patients on Brimonidine tartrate ophthalmic solution discontinued from the study due to somnolence.
The safety and effectiveness of Brimonidine tartrate ophthalmic solution 0.2% have not been studied in pediatric patients below the age of 2 years. Brimonidine tartrate ophthalmic solution 0.2% is not recommended for use in pediatric patients under the age of 2 years.

Brimonidine and Geriatic

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

Brimonidine and Other Contraindications

Hypersensitivity. Patients receiving MAO inhibitor therapy

Storage

Ophthalmic: Store at 15-25°C

Lab interference

Ophthalmic: Store at 15-25°C

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