Luxphene, eye drops 0.2% 5 ml

Brimonidine is a selective α2-adrenoreceptor agonist.

In instillation of 0.2% brimonidine solution decreases intraocular pressure by 10-12 mm Hg with a maximum effect after 2 hours and duration of action of 12 hours.

Brimonidine has a double mechanism of action: it decreases the intraocular pressure by reducing the synthesis of the intraocular fluid and increasing the uveoscleral outflow.

Pharmacokinetics

In instillation of eye drops, Cmax of the drug in blood plasma is reached after 0.5-2.5 hours. Binding to blood proteins when administered locally is 29%. Systemic absorption of brimonidine is delayed. After using the drug 2 times per day for 10 days the plasma concentration of brimonidine is still low (0.06 ng/ml on average).

The drug is metabolized mainly in the liver. Brimonidine and its metabolites are excreted by the kidneys. T1/2 is about 2 h.

Indications

Elevated intraocular pressure, Glaucoma

• Open angle glaucoma,
• ophthalmohypertension (in monotherapy and in combination with other drugs that reduce intraocular pressure).

Active ingredient

Brimonidine

Composition

1 ml – brimonidine tartrate 2 mg.

Supplementary substances:

benzalkonium chloride – 0.052 mg,

polyvinyl alcohol – 14 mg,

sodium chloride – 6.9 mg,

sodium citrate dihydrate – 4.7 mg,

citric acid monohydrate – 0.48 mg,

hydrochloric acid – to pH 6.45,

sodium hydroxide – to pH 6.45,

water – to 1 ml.

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How to take, the dosage

Topically.

Push one drop of the drug 2 times a day.

The duration of treatment is determined by the doctor.

Interaction

Brimonidine at a concentration of 2 mg/ml may increase the effect of substances affecting the central nervous system (alcohol, barbiturates, opioids, sedatives and anesthetics). Caution should be exercised in case of administration of drugs which can affect blood absorption and metabolism of adrenaline, noradrenaline and other so-called biogenic amines (chlorpromazine, methylphenidate, reserpine).

In some patients, a slight decrease in blood pressure has been noted after the use of brimonidine solution at a concentration of 2 mg/ml. Caution should be exercised when using simultaneously with hypotensive drugs and/or drugs of the group of cardiac glycosides (foxglove).

In concomitant systemic administration of adrenoreceptor agonists or antagonists (e.g., isoprenaline or prazosin) for the first time, as well as changes in the dose of these simultaneously administered systemic drugs (regardless of the route of administration), interactions with alpha adrenoreceptor agonists or effects on their effects may occur.

Special Instructions

Contact lenses should be removed before using the product. The time interval between using the drug and reinserting contact lenses should be at least 15 min.

Impact on ability to drive vehicles and other mechanisms requiring high concentration

The drug may cause a state of fatigue or drowsiness, reduced visual clarity, so during the treatment with the drug one should refrain from driving vehicles and operating moving mechanisms.

Contraindications

• High sensitivity to the drug components;
• concomitant therapy with monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants;
• children under 2 years old;
• breastfeeding period.

With caution: when the drug is used in patients with severe, unstable and uncontrolled cardiovascular disease, with cerebral or coronary insufficiency, depression, orthostatic hypotension, Raynaud’s disease, obliterating thrombangiitis; with liver or renal function disorders; childhood age from 2 to 18 years.

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Side effects

The incidence of side effects is classified as follows: very common (>1/10), common (>1/100 to1/1000 to1/10,000 to

Perhaps, visual organs:

very common – allergic conjunctivitis, conjunctival hyperemia, itching of eyelid skin and ocular mucosa;

often – burning sensation; conjunctival folliculosis and follicular conjunctivitis, local allergic eye mucosal reactions (including keratoconjunctivitis); blepharitis, blepharoconjunctivitis, blurred vision, cataracts, conjunctival edema, conjunctival hemorrhage, conjunctivitis, retention lacrimation, mucous discharge from eyes, dry and irritated mucous membrane of eyes, pain, eyelid edema, redness of eyelids, sensation of a foreign body in the eye, keratitis, eyelid lesions, photosensitivity, superficial, stained keratopathy, lacrimation, visual field loss, functional vitreous body lesion, vitreous hemorrhage, floating opacities in the vitreous and decreased visual acuity;

infrequent – corneal erosion, barley.

Anxiety of the central nervous system:

often – headache, drowsiness, insomnia, dizziness.

Cardiovascular system disorders:

often – increased blood pressure;

infrequently – decreased blood pressure.

Respiratory system disorders:

often – bronchitis, cough, shortness of breath;

infrequently – dry nasal mucosa, apnea.

Gastrointestinal tract disorders:

often – gastrointestinal disorders – dyspepsia, dryness of the oral mucosa

Skin and subcutaneous fatty tissue:

often – rashes.

Infectious and parasitic diseases:

often – flu-like syndrome, infectious disease (chills and respiratory infection), rhinitis, sinusitis, including infectious.

Laboratory findings:

often hypercholesterolemia.

Other:

often – general allergic reactions, asthenia, fatigue;

infrequently – change in taste sensation.

In children, apnea, bradycardia, decreased blood pressure, hypothermia, and muscle hypotension have been reported.

In addition, the following effects have been reported:

An organ of vision: frequency unknown – iritis, keratoconjunctivitis, miosis.

Acts of the central nervous system: depression.

Cardiovascular system: bradycardia, tachycardia.

Gastrointestinal tract: nausea.

Skin and subcutaneous fatty tissue: local skin reactions (erythema, itching, facial edema, rash and vasodilation of the eyelid skin vessels).

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Overdose

In accidental oral administration of the drug the following symptoms are possible: depression of the central nervous system, drowsiness, depression and loss of consciousness, decreased blood pressure, bradycardia, decreased body temperature, cyanosis of the skin, apnea.

In case of accidental ingestion of the drug: supportive symptomatic therapy, control of airway patency.

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Similarities

Mirwazo Derm.