Brimonidine Tartrate (0.2%)
Indications
Brimonidine 0.2% ophthalmic solution is
indicated for lowering intraocular pressure in patients with open-angle
glaucoma or ocular hypertension
Description
Brimonidine Tartrate ophthalmic solution
0.2% is an alpha adrenergic receptor agonist. It has a peak ocular
hypotensive effect occurring at two hours postdosing. Fluorophotometric
studies in animals and humans suggest that Brimonidine Tartrate has a
dual mechanism of action by reducing aqueous humor production and
increasing uveoscleral outflow.
Pharmacology
Brimonidine is an α-2 adrenoreceptor
agonist that is more selective for the α-2 adrenoreceptor than α-1.
Topical administration of Brimonidine Tartrate eye drops decreases
intraocular pressure (IOP) in humans. When used as directed Brimonidine
Tartrate have the action of reducing elevated IOP with minimal effect on
cardiovascular parametres. Brimonidine Tartrate eye drops have a rapid
onset of action with the peak ocular hypotensive effect occurring at two
hours post-dosing. The duration of effect is 12 hours or greater.
Fluorophotometric studies in animals and humans suggest that Brimonidine
Tartrate has a dual mechanism of action. Brimonidine Tartrate eye drops
lower IOP by reducing aqueous humor production and enhancing
uveoscleral outflow.
Dosage & Administration
The recommended dose is one drop of
Brimonidine Tartrate ophthalmic solution 0.2% in the affected eye(s)
three times daily, approximately 8 hours apart. Brimonidine Tartrate
ophthalmic solution 0.2% may be used concomitantly with other topical
ophthalmic drug products to lower intraocular pressure. If more than one
topical ophthalmic product is being used, the products should be
administered at least 5 minutes apart.
Interaction
Although specific drug interaction studies
have not been conducted with Brimonidine Tartrate ophthalmic solution
0.2%, the possibility of an additive or potentiating effect with CNS
depressants (alcohol, barbiturates, opiates, sedatives, or anesthetics)
should be considered. Alpha-agonists, as a class, may reduce pulse and
blood pressure. Caution in using concomitant drugs such as beta-blockers
(ophthalmic and systemic), antihypertensives and/or cardiac glycosides
is advised. Tricyclic antidepressants have been reported to blunt the
hypotensive effect of systemic clonidine. It is not known whether the
concurrent use of these agents with Brimonidine Tartrate ophthalmic
solution 0.2% in humans can lead to resulting interference with the IOP
lowering effect. No data on the level of circulating catecholamines
after administration of Brimonidine Tartrate ophthalmic solution 0.2%
are available. Caution, however, is advised in patients taking Tricyclic
antidepressants which can affect the metabolism and uptake of
circulating amines.
Contraindications
Brimonidine Tartrate ophthalmic solution
0.2% is contraindicated in patients with hypersensitivity to Brimonidine
Tartrate. It is also contraindicated in patients receiving monoamine
oxidase (MAO) inhibitor therapy.
Side Effects
Adverse events occurring in approximately
10-30% of the subjects, in descending order of incidence, included oral
dryness, ocular hyperemia, burning and stinging, headache, blurring,
foreign body sensation, fatigue/drowsiness, conjunctival follicles,
ocular allergic reactions, and ocular pruritus. Events occurring in
approximately 3-9% of the subjects, in descending order included corneal
staining/erosion, photophobia, eyelid erythema, ocular ache/pain,
ocular dryness, tearing, upper respiratory symptoms, eyelid edema,
conjunctival edema, dizziness, blepharitis, ocular irritation,
gastrointestinal symptoms, asthenia, conjunctival blanching, abnormal
vision and muscular pain. The following adverse reactions were reported
in less than 3% of the patients: lid crusting, conjunctival hemorrhage,
abnormal taste, insomnia, conjunctival discharge, depression,
hypertension, anxiety, palpitations/arrhythmias, nasal dryness and
syncope.
Pregnancy & Lactation
There are no adequate and well-controlled
studies in pregnant women. In animal studies, Brimonidine crossed the
placenta and entered into the fetal circulation to a limited extent.
Brimonidine Tartrate ophthalmic solution 0.2% should be used during
pregnancy only if the potential benefit to the mother justifies the
potential risk to the fetus. It is not known whether this drug is
excreted in human milk; in animal studies Brimonidine Tartrate was
excreted in breast milk. A decision should be made whether to
discontinue nursing or to discontinue the drug, taking into account the
importance of the drug to the mother.
Precautions & Warnings
Although Brimonidine Tartrate ophthalmic
solution 0.2% had minimal effect on blood pressure of patients in
clinical studies, caution should be exercised in treating patients with
severe cardiovascular disease. Brimonidine Tartrate ophthalmic solution
0.2% should be used with caution in patients with depression, cerebral
or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension
or thromboangiitis obliterans.
Therapeutic Class
Drugs for miotics and glaucoma
Storage Conditions
Store below 30°C in a cool and dry place
protected from light. Keep out of reach of children. Do not touch the
dropper tip to surfaces since this may contaminate the solution. Do not
use after 30 days of first opening.
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