Dosage/Direction for Use
Ophthalmic Ocular hypertension Adult: As 0.1, 0.15 or 0.2% soln: Instill 1 drop into affected eye(s) bid or tid (approx 8 or 12 hrly). Ophthalmic Open-angle glaucoma Adult: As 0.1, 0.15 or 0.2% soln: Instill 1 drop into affected eye(s) bid or tid (approx 8 or 12 hrly). Topical/Cutaneous Rosacea Adult: As 0.33% gel: Apply pea-sized amount once daily as a thin layer across the entire face covering each of the 5 areas of the face (forehead, nose, chin and each cheek). |
Contraindications
Childn <2 yr. Concomitant use of MAOIs.
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Special Precautions
Patient w/ severe or unstable and uncontrolled CV disease, mental depression, orthostatic hypotension, cerebral or coronary insufficiency, Raynaud's phenomenon, or thromboangiitis obliterans. Renal or hepatic impairment. Patient Counselling This drug may cause fatigue and/or drowsiness, if affected, do not drive or operate machinery. Avoid exposure to excessive sunlight and UV irradiation (topical). Remove contact lenses prior to ophth admin and reinsert after 15 min. Monitoring Parameters Monitor IOP routinely.
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Adverse Reactions
Erythema, pruritus, flushing, burning sensation, paraesthesia. nasopharyngitis, increased IOP, contact dermatitis, skin irritation, dry skin, acne, papular rash, worsening of rosacea, pain of skin, warm skin, swelling face, nasal congestion, angioedema, peripheral coldness, upper resp tract infection (topical). Ocular hyperaemia, burning/ stinging sensation, blurred vision, ocular allergic reaction, conjunctival follicles, corneal staining/erosion, photophobia, eyelid erythema, ocular dryness, ocular pain, conjunctival blanching, conjunctival discharge, iritis, iridocyclitis, miosis, fatigue, drowsiness, dizziness, asthenia, abnormal taste, blepharitis, depression, nasal dryness, palpitation, arrhythmias, hypotension, syncope, headache, blurred vision, dry mouth, eyelid oedema (ophth).
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Drug Interactions
TCAs (e.g. imipramine) and tetracyclic antidepressants (e.g. mianserin) that affect the metabolism and uptake of circulating amines may interfere w/ IOP-lowering effect brimonidine. Additive IOP-lowering and CV effects w/ β-blockers, antihypertensives, cardiac glycosides. Additive or potentiating effect w/ CNS depressants (e.g. barbiturates, opiates, sedatives or anaesthetics).
Potentially Fatal: Interfered metabolism and increased adverse effect when used w/ MAOIs (e.g. selegiline). |
Food Interaction
Additive CNS depressant effect w/ alcohol.
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Action
Brimonidine is an α2-adrenoceptor agonist. As an ophthalmic agent, it works to reduce aqueous humour production and increase uveoscleral flow, thus lowering intraocular pressure (IOP). Topically, it reduces erythema through direct cutaneous vasoconstriction.
Onset: Rapid (ophth). Duration: ≥12 hr (ophth). Absorption: Time to peak plasma concentration: Approx 0.5-4 hr (ophth); approx after 15 days (topical). Metabolism: Extensive hepatic metabolism. Excretion: Via urine. Elimination half-life: Approx 2-3 hr (ophth). |
Storage
Ophthalmic: Store between 15-25°C. Topical/Cutaneous: Store between 15-25°C.
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CIMS Class
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ATC Classification
S01GA07 - brimonidine
D11AX21 - brimonidine ; Belongs to the class of other dermatologicals. S01EA05 - brimonidine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma. |