Brimonidine

Registered South African indications: 

• Lowering of intraocular pressure in patients with open angle glaucoma or ocular hypertension

Registered South African contraindications

2mg/ml eye drops

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to benzalkonium chloride
• Coadministration with monoamine oxidase inhibitors
• Children younger than 2 years
  - Due to potentially serious adverse central nervous system effects, including apnoea and lethargy, reported in infants treated with topical brimonidine tartrate, the use of brimonidine tartrate eye drops is not recommended for use in paediatric patients under the age of two

1.5mg/ml eye drops

• Hypersensitivity to the active ingredient or any of its excipients
• Neonates and infants (under the age of 2 years)

Contraindications registered in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Neonates and infants
• Coadministration with monoamine oxidase inhibitors
• Coadministration with antidepressants which affect noradrenergic transmission (e.g. tricyclic antidepressants and mianserin)

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Children aged 2-7 years and/or weighing ≤20kg
• Severe or unstable cardiovascular disease
• Depression 
• Cerebral or coronary insufficiency
• Raynaud's phenomenon
• Orthostatic hypotension 
• Thromboangiitis obliterans
• Concomitant use of soft contact lenses

Forms avail. in SA and covered in this monograph: opd

South African registered indications and dosages

Lowering of intraocular pressure in patients with open angle glaucoma or ocular hypertension

2mg/ml & 1.5mg/ml eye drops

• Ophthalmic (opd): 1 drop into affected eye(s), twice dly approx. 12hrs apart

Brimonidine may be used concomitantly with other topical ophthalmic medicinal products to lower intraocular pressure. If more than one topical ophthalmic product is being used, the product should be administered at least 5 minutes apart

Paed. forms avail. in SA and covered in this monograph: opd

South African registered indications and dosages

Lowering of intraocular pressure in patients with open angle glaucoma or ocular hypertension

2mg/ml & 1.5mg/ml eye drops

Younger than 2 years

• Contraindicated

Older than 2 years

• See adult dosage

Children of 2 years of age and above, especially those in the 2-7 age range and/or weighing ≤20kg, should be treated with caution and closely monitored due to the high incidence and severity of somnolence

Pregnancy

• Caution
• The safety of use during human pregnancy has not been established. In animal studies, brimonidine tartrate did not cause any teratogenic effects. In rabbits, brimonidine tartrate, at plasma levels higher than are achieved during therapy in humans, has been shown to cause increased preimplantation loss and postnatal growth reduction. Brimonidine should be used during pregnancy only if the potential benefit to the mother outweighs the potential risk to the foetus

Breastfeeding

• Caution; not recommended
• It is not known if brimonidine is excreted in human milk. The compound is excreted in the milk of the lactating rat. Brimonidine should not be used by women nursing infants
• A decision must be made whether to discontinue breastfeeding or discontinue brimonidine taking into account the benefit of breastfeeding for the child and the benefit of therapy for the mother

• Caution; no dose adjustment recommended

• Caution; no dose adjustment recommended

• No dose adjustment recommended 

Central Nervous System Disorders

• Headache
• Drowsiness
• Dizziness
• Abnormal taste
• Syncope
• Fatigue 
• Depression
• Insomnia
• Asthenia

Cardiovascular Disorders

• Hypertension
• Hypotension
• Palpitations
• Arrhythmias

Respiratory Disorders

• Upper respiratory symptoms
• Nasal dryness
• Dyspnoea

Gastrointestinal Disorders

• Oral dryness

Skin and Subcutaneous Tissue Disorders

• Skin reactions
• Eyelid pruritus

Sensory Disorders

• Ocular irritation
• Blurred vision
• Allergic blepharitis
• Allergic blepharoconjunctivitis
• Allergic conjunctivitis
• Follicular conjunctivitis
• Photophobia
• Corneal erosion and staining
• Ocular dryness
• Conjunctival blanching
• Abnormal vision
• Conjunctivitis
• Iritis
• Miosis
• Anterior uveitis

• Monoamine oxidase inhibitors
• Antidepressants which affect noradrenergic transmission
• Tricyclic antidepressants
• Mianserin
• Central nervous system depressants
• Medications which can affect the metabolism and uptake of circulating amines e.g. chlorpromazine, methylphenidate, reserpine
• Antihypertensives
• Cardiac glycosides
• Adrenergic receptor agonists
• Adrenergic receptor antagonists

None routine

Brimonidine tartrate is a selective alpha-2 adrenergic receptor agonist. Topical administration of brimonidine tartrate decreases intraocular pressure with minimal effect on cardiovascular or pulmonary parameters. It has a rapid onset of action, with peak ocular hypotensive effect seen at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humour production and increasing uveoscleral outflow.

Eye drops (per ml) 1.5mg

• Alphagan Purite (Allergan) originator

Eye drops (per ml) 2mg

• Brimoct (Actor)

COMBINATION PREPARATIONS

Brimonidine tartrate/ Timolol

Eye drops (per ml) 2mg/5mg

• Combigan (Allergan) originator