Brimonidine: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Indonesia prescribing information.

Generic Medicine Info

Indications and Dosage

Ophthalmic
Ocular hypertension, 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.

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.

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).

Pregnancy Category (US FDA)

Ophth/Topical: B

Patient Counseling Information

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.

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.

Action

Description:
Mechanism of 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).
Pharmacokinetics:
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).

Chemical Structure

Storage

Store between 15-25°C.

MIMS Class

Antiglaucoma Preparations

ATC Classification

S01EA05 - brimonidine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma.
D11AX21 - brimonidine ; Belongs to the class of other dermatologicals.

References

Actavis New Zealand Limited. Arrow-Brimonidine Ophthamic Solution data sheet 1 July 2013. Medsafe. http://www.medsafe.govt.nz/. Accessed 19/08/2016.

AFT Pharmaceuticals Ltd. Brimonidine AFT Ophthalmic Solution data sheet April 2013. Medsafe. http://www.medsafe.govt.nz/. Accessed 19/08/2016.

Anon. Brimonidine (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/08/2016.

Anon. Brimonidine (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/08/2016.

Brimonidine tartrate Solution/Drops (Regimed Medical). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/08/2016.

Buckingham R (ed). Brimonidine Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/08/2016.

Healthcare Logistics. Mirvaso Gel data sheet 20 January 2016. Medsafe. http://www.medsafe.govt.nz/. Accessed 19/08/2016.

Joint Formulary Committee. Brimonidine Tartrate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/08/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Brimonidine Tartrate (EENT). AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 19/08/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Brimonidine tartrate (Topical). AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 19/08/2016.

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