Brimoct

Alpha-Agonist

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Brimoct®

2 mg/ml Brimonidine Tartrate

5 ml Ophthalmic Solution

S3 Reg. No. 45/15.4/0688

Package Insert

Each ml of BRIMOCT Ophthalmic Solution contains Brimonidine Tartrate 2,0 mg

Other ingredients are: Citric Acid Monohydrate

Polyvinyl Alcohol

Purified Water

Sodium Chloride

Sodium Citrate Dihydrate

Sodium Hydroxide

Preservative: Benzalkonium Chloride 0,005 % m/v

A.15.4 Ophthalmic Preparations. Other

Brimonidine a selective alpha-2-adrenergic receptor agonist.

Following topical administration to the eye, brimonidine tartrate, a selective alpha-2-adrenergic receptor agonist, reduces intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. Peak ocular hypotensive effect occurs at two hours post-dosing. Due to its selectivity brimonidine tartrate has minimal effect on cardiovascular and pulmonary parameters.

Brimonidine has a dual mechanism of action as suggested by fluorophotometric studies done in animals and humans. It lowers intraocular pressure by reducing aqueous humour production and by increasing uveoscleral outflow.

Following topical ocular administration of 0,2 % brimonidine solution, plasma concentrations peaked within 0,5 to 2,5 hours and declined with a systemic half life of approximately 2 hours. Systemic metabolism of brimonidine in humans is extensive and occurs primarily by the liver. The major route of elimination of the medicine and its metabolites is by urinary excretion.

BRIMOCT ophthalmic solution is indicated for lowering intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

BRIMOCT is contraindicated in patients with hypersensitivity to brimonidine tartrate, benzalkonium chloride or any other ingredient in BRIMOCT. BRIMOCT is also contraindicated in patients receiving monoamine oxidase (MAO) inhibitor therapy.

Safety and efficacy of BRIMOCT in children younger than 2 years of age have not been established. However due to potentially serious adverse central nervous system effects, including apnoea and lethargy, reported in infants treated with topical brimonidine tartrate, the use of BRIMOCT is not recommended for use in paediatric patients under the age of two.

As the possibility of adverse effects on the corneal permeability, and the danger of disruption of the corneal epithelium with prolonged or repeated usage of benzalkonium chloride preserved ophthalmological preparations, cannot be excluded, regular ophthalmological examination is required.

Caution should be exercised in the use of benzalkonium chloride preserved topical medication over an extended period in patients with extensive ocular surface disease.

The use of BRIMOCT may result in dry eyes and therefore should be used with caution in patients with dry eye syndrome.

Patients that use intraocular lowering medication should be routinely monitored for intraocular pressure.

Brimonidine had minimal effects on the blood pressure of patients in clinical studies however caution should be exercised in treating patients with severe cardiovascular disease.

BRIMOCT should be used with caution in patients with Raynaud’s phenomenon, cerebral or coronary insufficiency, depression, orthostatic hypotension, or thromboangiitis obliterans.

BRIMOCT ophthalmic solution has not been studied in patients with renal or hepatic impairment and therefore caution should be exercised in treating such patients.

Benzalkonium chloride may be absorbed by soft contact lenses. Patients wearing soft contact lenses should be instructed to wait at least 15 minutes after instilling BRIMOCT ophthalmic solution to insert soft contact lenses. The overall difference in safety and efficacy between the elderly and other adult patients has not been observed.

BRIMOCT may cause fatigue and/or drowsiness in some patients. Patients who engage in hazardous activities should therefore be cautioned of the potential for a decrease in mental alertness.

BRIMOCT may sting, burn or cause itchiness and blurred vision just after instillation. Patients should be advised to not drive, use machinery or do any activity that requires clear vision, until they are sure that they can perform such activities safely.

BRIMOCT has the possibility of an additive or potentiating effect when used with CNS depressants (alcohol, sedatives, barbiturates, opiates or anaesthetics).

Caution in using concomitant medicines such as beta blockers (ophthalmic and systemic), antihypertensive and/or cardiac glycosides is advised, since alpha agonists as a class, may reduce pulse and blood pressure.

The hypotensive effects of systemic clonidine have been reported to be blunted by tricyclic antidepressants. It is not known whether the concurrent use of these agents with BRIMOCT ophthalmic solution can lead to an interference with the IOP lowering effect.

There is no information available regarding the level of circulating catecholamines after BRIMOCT administration. However, since tricyclic antidepressants may affect the metabolism and uptake of circulating amines, caution is advised in patients using these antidepressants.

Pregnancy:

The safety and efficacy of BRIMOCT in pregnant women have not been established.

Lactation:

It has not been established whether BRIMOCT is excreted in human milk. A decision should be made on whether to discontinue BRIMOCT or discontinue breastfeeding, taking into account the importance of the medicine to the mother.

Benzalkonium chloride may be absorbed by soft contact lenses. Patients wearing soft contact lenses should be instructed to wait at least 15 minutes after instilling BRIMOCT ophthalmic solution to insert soft contact lenses [See “Warnings and Special precautions”].

The recommended dose is one drop of BRIMOCT in the affected eye(s) twice daily, approximately 12 hours apart.

BRIMOCT may be used concomitantly with other topical ophthalmic medicinal products to lower ocular pressure. The topical ophthalmic products should be administered at least 5 minutes apart if more than one product is being used.

The most undesirable side-effects relate to the ocular system and may include

Conjunctival hyperaemia, eye pruritus. Allergic conjunctivitis.

Frequent:

Burning sensation, stinging, foreign body sensation, follicular conjunctivitis, photophobia, eye pain, eye dryness, conjunctival oedema, blepharitis, eye irritation, eye discharge, conjunctival haemorrhage.

Conjunctival folliculosis, conjunctivitis, epiphora, visual field defects, visual disturbances, worsened visual acuity, superficial punctate keratopathy, vitreous floaters.

Less frequent:

Corneal erosion.

Frequency unknown:

Iritis, miosis.

 

Nervous system disorders:

Frequent:

Headache, dizziness.

Less Frequent:

Taste perversion, somnolence in adults and infants.

 

Psychiatric disorders:

Less frequent:

Insomnia, depression, anxiety, syncope.

 

 

Vascular disorders:

Frequent:

Hypertension.

Frequency unknown:

Hypotension in adults and infants.

 

Musculoskeletal disorders:

Frequency unknown:

Hypotonia in infants.

 

Cardiac disorders:

Less frequent:

Palpitations.

Frequency unknown:

Bradycardia in adults and infants, tachycardia.

 

Immune system disorders:

Frequent:

Allergic reactions.

 

Skin and subcutaneous tissue disorders:

Frequent:

Rash. Eyelid erythema, eyelid oedema.

Frequency unknown:

Eye pruritus, vasodilation.

 

Respiratory, thoracic and mediastinal disorders:

Frequent:

Cough, dyspnoea.

Less frequent:

Nasal dryness.

Frequency unknown:

Apnoea in infants.

 

Gastrointestinal disorders:

Frequent:

Oral dryness, dyspepsia.

 

 

 

Infections and infestations:

Frequent:

Sinusitis, sinus infection, flu syndrome, bronchitis, rhinitis, pharyngitis.

 

General disorders and administration site condition:

Frequent:

Asthenia.

Frequency unknown:

Hypothermia in infants.

Treatment, in the event of an oral overdose, includes supportive and symptomatic therapy. A patent airway should be maintained.

Clear, transparent, yellowish solution without suspending particles.

BRIMOCT® ophthalmic solution is supplied in an opaque white sterile dropper bottle with a white sterile capillary plug and a purple sterile cap, containing 5 ml solution. The dropper bottle is contained in an outer cardboard carton.

Store at or below 25 oC. Keep well closed. Protect from light. Do not refrigerate.

Do not use more than 30 days after opening.

KEEP OUT OF REACH OF CHILDREN.

45/15.4/0688

Actor Pharma (Pty) Ltd
Unit 7, Royal Palm Business Estate
646 Washington Street, Halfway House, Midrand, 1685
Gauteng