Chemical formula: C₁₁H₁₀BrN₅ Molecular mass: 292.135 g/mol PubChem compound: 2435
Brimonidine interacts in the following cases:
Although specific drug interactions studies have not been conducted with brimonidine, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, or anaesthetics) should be considered.
Caution is advised when initiating (or changing the dose of) a concomitant systemic agent (irrespective of pharmaceutical form) which may interact with α-adrenergic agonists or interfere with their activity i.e. agonists or antagonists of the adrenergic receptor e.g. (isoprenaline, prazosin).
Brimonidine has not been studied in patients with hepatic impairment; caution should be used in treating such patients.
Brimonidine has not been studied in patients with renal impairment; caution should be used in treating such patients.
After the application of brimonidine, clinically insignificant decreases in blood pressure were noted in some patients. Caution is advised when using drugs such as antihypertensives and/or cardiac glycosides concomitantly with brimonidine.
No data on the level of circulating catecholamines after Alphagan administration are available. Caution, however, is advised in patients taking medications which can affect the metabolism and uptake of circulating amines e.g. chlorpromazine, methylphenidate, reserpine.
Brimonidine should be used with caution in patients with Raynaud’s phenomenon.
Brimonidine should be used with caution in patients with orthostatic hypotension.
Brimonidine should be used with caution in patients with depression.
Caution should be exercised in treating patients with severe or unstable and uncontrolled cardiovascular disease.
Brimonidine should be used with caution in patients with thromboangiitis obliterans.
Brimonidine should be used with caution in patients with cerebral or coronary insufficiency.
There are no or limited amount of data from the use of brimonidine in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of brimonidine during pregnancy.
It is unknown whether brimonidine/metabolites are excreted in human milk. A risk to the newborns/infants cannot be excluded. Brimonidine should not be used during breast-feeding.
Brimonidine did not present any special reproductive or developmental hazard in animal species.
Brimonidine may cause fatigue and/or drowsiness, which may impair the ability to drive or operate machinery. Brimonidine may cause blurred and/or abnormal vision, which may impair the ability to drive or to use machinery, especially at night or in reduced lighting. The patient should wait until these symptoms have cleared before driving or using machinery.
Brimonidine has no or negligible influence on the ability to drive and use machines.
The most commonly reported ADRs are oral dryness, ocular hyperaemia and burning/stinging, all occurring in 22 to 25% of patients. They are usually transient and not commonly of a severity requiring discontinuation of treatment.
Symptoms of ocular allergic reactions occurred in 12.7% of subjects (causing withdrawal in 11.5% of subjects) in clinical trials with the onset between 3 and 9 months in the majority of patients.
Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness. The following terminologies have been used in order to classify the occurrence of undesirable effects: Very Common (≥1/10); Common (≥1/100 to <1/10); Uncommon (≥1/1,000 to <1/100); Rare (≥1/10,000 to <1/1,000); Very rare (<1/10,000), not known (cannot be estimated from the available data).
Uncommon: systemic allergic reactions
Uncommon: depression
Very rare: insomnia
Very common: headache, drowsiness
Common: dizziness, abnormal taste
Very rare: syncope
Very common:
Common:
Very rare: iritis, miosis
Uncommon: palpitations/arrhythmias (including bradycardia and tachycardia)
Very rare: hypertension, hypotension
Common: upper respiratory symptoms
Uncommon: nasal dryness
Rare: dyspnoea
Very common: oral dryness
Common: gastrointestinal symptoms
Very common: fatigue
Common: asthenia
The following adverse reactions have been identified during post-marketing use of brimonidine in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made
Not known:
Eye disorders:
Skin and subcutaneous tissue disorders:
In cases where brimonidine has been used as part of the medical treatment of congenital glaucoma, symptoms of brimonidine overdose such as loss of consciousness, lethargy, somnolence, hypotension, hypotonia, bradycardia, hypothermia, cyanosis, pallor, respiratory depression and apnoea have been reported in neonates and infants receiving brimonidine.
In a 3-month, phase 3 study in children aged 2-7 years with glaucoma, inadequately controlled by beta-blockers, a high prevalence of somnolence (55%) was reported with brimonidine as adjunctive treatment. In 8% of children, this was severe and led to discontinuation of treatment in 13%. The incidence of somnolence decreased with increasing age, being least in the 7-year-old age group (25%), but was more affected by weight, occurring more frequently in those children weighing ≤20 kg (63%) compared to those weighing >20 kg (25%).
The most commonly reported adverse reactions are erythema, pruritus, flushing and skin burning sensation, all occurring in 1.2 to 3.3% of patients in clinical studies. They are typically mild to moderate in severity, and usually do not require discontinuation of treatment. Aggravated erythema, flushing and skin burning sensation have been reported during the post-marketing period.
The adverse reactions are classified by System Organ Class and frequency, using the following convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), not known (cannot be estimated from the available data) and were reported with brimonidine either in clinical studies, or during the post-marketing experience (identified by an asterix (*) in the following table).
Adverse reactions:
| System Organ Class | Frequency | Adverse reactions |
|---|---|---|
| Cardiac disorders | Rare | Bradycardia* |
| Nervous system disorders | Uncommon | Headache, paraesthesia |
| Eye disorders | Uncommon | Eyelid oedema |
| Vascular disorders | Common | Flushing, pallor at the application site* |
| Uncommon | Dizziness* | |
| Rare | Hypotension* | |
| Respiratory, thoracic and mediastinal disorders | Uncommon | Nasal congestion |
| Gastrointestinal disorders | Uncommon | Dry mouth |
| Skin and subcutaneous tissue disorders | Common | Erythema, pruritus, rosacea, skin burning sensation |
| Uncommon | Acne, allergic contact dermatitis, contact dermatitis, dermatitis, dry skin, pain of skin, skin discomfort, rash papular, skin irritation, skin warm, swelling face*, urticaria* | |
| Rare | Angioedema* | |
| General disorders and administration site conditions | Uncommon | Feeling hot, peripheral coldness |
* Adverse reactions reported from post-marketing data.
Post-marketing cases of bradycardia, hypotension (including orthostatic hypotension) and dizziness have been reported, some of which required hospitalisation. Some cases involved application of brimonidine following laser procedures.
No meaningful differences in the safety profiles were observed between the elderly subject population and subjects 18 to 65 years of age.
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