Topical selective α2-adrenergic agonist for ophthalmic use
Brand names: Alphagan P, Lumify, Mirvaso
Updated · Methodology
Second line
Brimonidine lowers IOP in ocular hypertension when prostaglandins are contraindicated (history of uveitis) or do not reach target reduction. EGS 2024 recommends brimonidine as second-line monotherapy or add-on to a prostaglandin.
Sources
ICD-10: H40.0 · ICD-11: 9C61.01
Second line
Brimonidine is used as second-line monotherapy or as add-on to a prostaglandin when IOP control is insufficient. EGS 2024 and SEG/SEO 2023 recommend brimonidine as an alternative or adjunct, especially when beta blockers are contraindicated (COPD, asthma, bradycardia). IOP reduction is 18–25% with 2–3 daily instillations. A possible neuroprotective effect on retinal ganglion cells is discussed but not firmly confirmed by RCTs.
Sources
ICD-10: H40.1 · ICD-11: 9C61.0
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Brimonidine 0.1–0.2% in Spain is registered by AEMPS only for IOP lowering in glaucoma. A separate -approved product Lumify 0.025% addresses cosmetic eye redness in the US; AEMPS has NOT registered such a product in Spain. Using the glaucoma 0.2% formulation for tired eyes or hangover does not work as a cosmetic agent and is dangerous: rebound hyperaemia worse than baseline appears after withdrawal, allergic conjunctivitis develops in up to 25% of patients by month six, and infants under six years can develop CNS depression and bradycardia. If brimonidine was suggested as daily whitening drops, consider seeking a second opinion.
Selective α2-adrenergic agonist. Lowers IOP by two mechanisms: reduced aqueous humour production by the ciliary body and increased uveoscleral outflow. Instillation of a 0.1–0.2% solution 2–3 times daily lowers IOP by 18–25%. Conjunctival vasoconstriction additionally reduces redness (the basis of US-approved Lumify 0.025% for cosmetic redness). Systemic absorption is variable; in young children it causes marked CNS depression and bradycardia.
AEMPS summary of product characteristics (section 4.6): the safety of brimonidine in human pregnancy has not been established. Brimonidine tartrate was not teratogenic in animal studies, but in rabbits, with plasma levels higher than those reached in humans, it increased preimplantation loss and reduced postnatal growth. Brimonidine is used in pregnancy only if the potential benefit to the mother justifies the risk to the fetus.
Not preferred. Hale L4. Passes into milk and may theoretically cause sedation, hypotension and bradycardia in the breastfed infant. AEMPS recommends temporary breastfeeding suspension or switching to a topical beta blocker or carbonic anhydrase inhibitor.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Verbatim lines from the interaction sections, in the language of the label
«Pacientes tratados con inhibidores de la monoamino oxidasa (IMAO), y en pacientes tratados con antidepresivos que afecten la transmisión noradrenérgica (p.e. antidepresivos tricíclicos y mianserina).»AEMPS, section 4.3 · Open on CIMA
«Pacientes tratados con inhibidores de la monoamino oxidasa (IMAO), y en pacientes tratados con antidepresivos que afecten la transmisión noradrenérgica (p.e. antidepresivos tricíclicos y mianserina).»AEMPS, section 4.3 · Open on CIMA
«CNS Depressants: Although specific drug-drug interactions studies have not been conducted with brimonidine topical gel, the possibility of an additive or potentiating effect with CNS depressants…»FDA, section 7 · Open on DailyMed
«con otros medicamentos, debe considerarse la posibilidad de un efecto aditivo o de potenciación con depresores del SNC (alcohol, barbitúricos, opiáceos, sedantes o anestésicos).»AEMPS, section 4.5 · Open on CIMA
«Anti-hypertensives/FDA, section 7 · Open on DailyMed
«CNS Depressants: Although specific drug-drug interactions studies have not been conducted with brimonidine topical gel, the possibility of an additive or potentiating effect with CNS depressants…»FDA, section 7 · Open on DailyMed
«con otros medicamentos, debe considerarse la posibilidad de un efecto aditivo o de potenciación con depresores del SNC (alcohol, barbitúricos, opiáceos, sedantes o anestésicos).»AEMPS, section 4.5 · Open on CIMA
«de la presión sanguínea insignificantes desde el punto de vista clínico. Se recomi enda precaución al emplear medicamentos tales como antihipertensivos y/AEMPS, section 4.5 · Open on CIMA
«Anti-hypertensives/FDA, section 7 · Open on DailyMed
«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…»FDA, section 7 · Open on DailyMed
«con otros medicamentos, debe considerarse la posibilidad de un efecto aditivo o de potenciación con depresores del SNC (alcohol, barbitúricos, opiáceos, sedantes o anestésicos).»AEMPS, section 4.5 · Open on CIMA
«CNS Depressants: Although specific drug-drug interactions studies have not been conducted with brimonidine topical gel, the possibility of an additive or potentiating effect with CNS depressants…»FDA, section 7 · Open on DailyMed
«clorpromazina, metilfenidato, reserpina.»AEMPS, section 4.5 · Open on CIMA
«clorpromazina, metilfenidato, reserpina.»AEMPS, section 4.5 · Open on CIMA
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Brimonidine is evaluated for the following indications with varying evidence strength: Open-angle glaucoma (evidence tier A), Ocular hypertension (evidence tier A), Cosmetic eye redness (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Brimonidine (≥ 1 in 100): Allergic conjunctivitis (up to 25% by month 6), Burning and dry eyes, Blurred vision, Drowsiness and fatigue, Dry mouth, Headache. See the Safety section for uncommon and serious reactions.
AEMPS summary of product characteristics (section 4.6): the safety of brimonidine in human pregnancy has not been established. Brimonidine tartrate was not teratogenic in animal studies, but in rabbits, with plasma levels higher than those reached in humans, it increased preimplantation loss and reduced postnatal growth. Brimonidine is used in pregnancy only if the potential benefit to the mother justifies the risk to the fetus.
Not preferred. Hale L4. Passes into milk and may theoretically cause sedation, hypotension and bradycardia in the breastfed infant. AEMPS recommends temporary breastfeeding suspension or switching to a topical beta blocker or carbonic anhydrase inhibitor.
Brimonidine is contraindicated in: Hypersensitivity to brimonidine or other components; Under 2 years of age (risk of CNS depression, apnoea, bradycardia); Concurrent MAO inhibitors; Concurrent tricyclic antidepressants. Full list in the Safety section.
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Carbomer, Dorzolamide, Hypromellose, Latanoprost, Tetryzoline, Travoprost, Lutein + zeaxanthin, Timolol