Brimonidine - instructions for use, dose, side effects, contraindications

Pharmacodynamics: Alpha₁-adrenomimetic. Stimulates extra-synaptic alpha₂-adrenoceptor vessels and leads to narrowing of blood vessels. As a result, the secretion of intraocular fluid by the ciliary body. At the same time, the uveoscleral outflow increases due to an increase in prostaglandin release due to alpha-adrenergic stimulation and relaxation of the ciliary muscle. Local application of the drug causes a decrease in intraocular pressure in humans with little effect on the cardiovascular and respiratory system.

Pharmacokinetics:

With repeated use (2 times a day for 10 days) there was a slight cumulation of the drug in the blood. After topical application, the average half-elimination period (half-life) from the systemic blood flow was about 3 hours.
On 29% it is associated with blood plasma proteins. Brimonidine reversibly binds to melanin in the tissues of the eye, in vitro and in vivo. Metabolized in the liver under the influence of aldehyde oxidase and cytochrome P450. After oral administration, it is well absorbed and quickly excreted. Most of the dose (about 75%) is excreted as metabolites in urine for 5 days.

Indications:

ABOUTopen-angle glaucoma; as a monotherapy in the contraindication of the use of local beta-adrenoreceptor blockers; in the complex therapy with other drugs to reduce intraocular pressure with inefficiency of monotherapy.

ICD-10

VII.H40-H42.H40.1 Primary open angle glaucoma

Contraindications:

Hypersensitivity to the active substance or to any other component of the drug; childhood; During pregnancy and breastfeeding.

Carefully:

In severe or unstable and uncontrolled cardiovascular diseases; depression, cerebral circulatory insufficiency, coronary insufficiency, Raynaud's syndrome, orthostatic hypotension or obliterating thromboangiitis; with hepatic or renal insufficiency.

When allergic reactions occur, the drug is stopped.

Pregnancy and lactation:

The study on the safety of the drug in pregnant women was not carried out, so the drug is not used during pregnancy. Information on the excretion of brimonidine into breast milk is not enough, so the drug should not be used during breastfeeding.

Dosing and Administration:

1 drop of brimonidine is instilled in the affected eye 2 times a day at regular intervals (after 12 hours).
If more than one kind of eye drops is prescribed, they should be instilled at intervals of 5-15 minutes.
Correction of a dose for the elderly is not required.

Side effects:

From the cardiovascular system: palpitations / arrhythmias, arterial hypertension / hypotension.

From the side of the central nervous system: headache, drowsiness; dizziness.

On the part of the eye: eye irritation (hyperemia, inflammation and burning, itching, sensation of foreign body, follicular conjunctivitis), photophobia, corneal erosion and keratopathy, dry eyes, paleness of conjunctiva, visual impairment, conjunctivitis.

On the part of the respiratory system: symptoms of upper respiratory tract disease; sometimes - dryness of the nasal mucosa.

From the gastrointestinal tract: dry mouth; Gastrointestinal symptoms.

General disorders: fatigue, asthenia.

From the immune system: allergic reactions.

From the psyche: possible depression, insomnia.

Overdose:

In adults, an overdose for ophthalmic use drug is not marked. With the occasional oral administration of brimonidine, a change in blood pressure was observed, which returned to normal within 24 hours. There are cases of serious side effects in children with occasional oral administration of the drug: central nervous system depression, short-term coma or loss of consciousness, arterial hypotension, bradycardia, hypothermia and apnea. In case of an oral overdose of others alpha₁agonists reported on the appearance of such symptoms: arterial hypotension, asthenia, vomiting, lethargy, sedation, bradycardia, arrhythmia, miosis, apnea, hypothermia, respiratory depression and convulsions.

Interaction:

Brimonidine in the form of drops of the eye enhances the effect of drugs, including barbiturates, which depress the central nervous system when used together.

Simultaneous use of brimonidine with cardiac glycosides and antihypertensive drugs requires caution.

Important caution when sharing the use of brimonidine and antidepressants.

Inhibitors monoamine oxidase may aggravate systemic adverse drug reactions of brimonidine.

Special instructions:

Brimonidine can cause fatigue, drowsiness, visual impairment, which can affect the ability to drive vehicles and mechanisms.

Instructions

Brimonidine (Brimonidinum)