Bimoptic eye drops 0.3 mg / ml, 3 ml

Reduction of increased intraocular pressure in open-angle glaucoma and ophthalmic hypertension in adults (as monotherapy or in combination with beta-blockers).

The drug is used topically.

The recommended dose is 1 drop into the affected eye (s) 1 time / day, in the evening. You cannot instill the drug more often than 1 time / day, because more frequent use can reduce the effect of lowering intraocular pressure. When using more than one ophthalmic drug for topical use, it is necessary to observe an interval of 5 minutes between the introduction of each of them. The drug is not recommended for use in children and adolescents under the age of 18 due to the lack of data on the safety and efficacy of the drug. The drug has not been studied in patients with moderate to severe renal or hepatic impairment and should therefore be used with caution in these patients. In patients with mild liver dysfunction (in history) or increased ALT activity,ACT and / or the level of bilirubin (in history), the drug did not adversely affect the functional state of the liver for 24 months.

Eye drops in the form of a clear solution from colorless to light yellow.

1 ml

bimatoprost 300 mcg

Excipients: citric acid monohydrate - 0.14 mg, sodium phosphate disubstituted heptahydrate - 2.68 mg, sodium chloride - 8.3 mg, benzalkonium chloride - 0.05 mg, sodium hydroxide solution 1M or hydrochloric acid solution 1M - up to pH 7.3 ± 0.1, purified water - up to 1 ml

• Age under 18;

• hypersensitivity to the active substance or to any of the excipients.

The drug should be used with caution in patients with known risk factors for macular edema (for example, in patients with aphakia, pseudophakia, and rupture of the posterior lens capsule); a history of severe eye infections (eg, caused by herpes simplex virus) or iritis / uveitis.

pharmachologic effect

Bimatoprost is a powerful ophthalmic antihypertensive agent. Is it synthetic prostamide, structurally related to prostaglandin F2? (PGF2?), Which does not act through known prostaglandin receptors. Bimatoprost selectively mimics the effects of recently discovered biosynthesized substances, prostamides. However, the structure of the prostamide receptors has not yet been identified.

Bimatoprost reduces intraocular pressure by increasing the outflow of aqueous humor through the trabecular network and increasing uveoscleral outflow.

The decrease in intraocular pressure begins approximately 4 hours after the first injection, the maximum effect is achieved after approximately 8-12 hours. The effect lasts for at least 24 hours.

According to clinical studies, there was no significant effect of the drug on heart rate and blood pressure.

Pediatric population

There are no data on the efficacy and safety of using bimatoprost in patients under 18 years of age.

Pharmacokinetics

Suction

Bimatoprost penetrates well into the human cornea and sclera in vitro. After instillation in adults, the systemic exposure of bimatoprost is very small, no accumulation of the drug was noted. After the introduction of one drop of Bimoptic Rompharm into both eyes 1 time / day for 2 weeks, the concentration in the blood reached a maximum 10 minutes after the dose was administered, and within 1.5 hours this indicator was below the detection level (0.025 ng / ml). The average values ??of Cmax and AUC0-24h were approximately the same on the 7th and 14th days - approximately 0.08 ng / ml and 0.09 ng ? h / ml, respectively, which indicates that the equilibrium concentration of bimatoprost was achieved during the first week of instillation ...

Distribution

Bimatoprost is moderately distributed in body tissues, systemic equilibrium Vd is 0.67 l / kg. In human blood, bimatoprost is found mainly in plasma. Plasma protein binding of bimatoprost is about 88%.

Metabolism

Bimatoprost reaches the systemic circulation, mainly unchanged. Then oxidation, N-deethylation and glucuronidation occurs with the formation of a number of metabolites.

Withdrawal

Bimatoprost is excreted mainly by the kidneys. Up to 67% of the intravenous dose in healthy adult volunteers was excreted in the urine, 25% of the dose was excreted in the feces. T1 / 2 after intravenous administration was approximately 45 minutes, the total clearance from the blood was 1.5 l / h / kg.

Side effect

From the nervous system: often - headache; infrequently - dizziness.

From the side of the organ of vision: very often - conjunctival injection, itching in the eyes, growth of eyelashes; often - superficial punctate keratitis, corneal erosion, burning in the eyes, eye irritation, allergic conjunctivitis, blepharitis, decreased visual acuity, asthenopia, conjunctival edema, foreign body sensation in the eye, dry eye, eye pain, photophobia, lacrimation, discharge from the eyes , blurred vision, increased pigmentation of the iris, darkening of the eyelashes; infrequently - retinal hemorrhagic disorders, uveitis, cystic macular edema, iritis, blepharospasm, eyelid retraction, periorbital erythema; frequency unknown - enophthalmos.

From the side of the cardiovascular system: often - arterial hypertension.

On the part of the skin and subcutaneous tissue: infrequently - hirsutism.

Others: infrequently - asthenia.

On the part of laboratory and instrumental studies: often - a deviation from the norm of the biochemical parameters of the liver function.

In very rare cases, corneal calcification has been observed with the use of phosphate-containing eye drops in patients with concomitant significant damage to the cornea.

Application during pregnancy and lactation

There are no data from clinical studies of the use of bimatoprost in pregnant women. According to animal studies, reproductive toxicity has been demonstrated when used in high doses that are toxic to the mother's body. It is not recommended to use bimatoprost during pregnancy in the absence of strict indications.

It is not known whether bimatoprost is excreted in human breast milk. In animal studies, it has been shown that bimatoprost is excreted in breast milk. The decision to continue / stop breastfeeding or continue / stop treatment with Bimoptic Rompharm should be made taking into account the benefits of breastfeeding for the child and the benefits of therapy with the drug for the mother.

There is no information on the effect of bimatoprost on fertility.

Application for violations of liver function

The drug should be used with caution in patients with moderate to severe hepatic impairment.

In patients with mild liver dysfunction (history) or increased ALT, ACT and / or bilirubin levels (history), the drug did not adversely affect the functional state of the liver for 24 months.

Application for impaired renal function

The drug should be used with caution in patients with moderate to severe renal insufficiency.

Application in children

The use of the drug under the age of 18 is contraindicated.

special instructions

Before starting treatment, patients should be informed about the possibility of eyelash growth, darkening of the eyelid skin and an increase in iris pigmentation. Some of these changes can be permanent and can lead to differences in appearance between the eyes when only one eye is treated. Pigmentation changes in the iris are slow and may not be noticeable for months or years. Most often, the color change in the iris is permanent. The change in the color of the iris is more associated with an increase in the melanin content in melanocytes than with an increase in the number of melanocytes. The long-term effects of increased iris pigmentation are unknown. Typically, brown pigment spreads from the area around the pupil to the root of the iris,as a result, all or parts of the iris become more brownish. The use of bimatoprost does not affect the nevi and lentigo of the iris. Pigmentation of periorbital tissue is reversible in some patients.

There are reports of the possibility of developing cystic macular edema during the period of bimatoprost therapy (the incidence of this adverse event is infrequent (? 1/1000 to <1/100)), which requires caution when using the drug in the treatment of patients with risk factors for macular edema (patients with aphakia, pseudoaphakia and rupture of the posterior capsule of the lens).

There is no experience with the use of bimatoprost in patients with concomitant impaired respiratory function, which requires caution in such patients. When conducting clinical studies in patients with impaired respiratory function, no significant adverse effects on the respiratory system were noted.

The effect of bimatoprost has not been studied in patients with more severe I degree heart block or in patients with uncontrolled congestive heart failure.

The drug contains a preservative benzalkonium chloride, which can be absorbed by soft contact lenses. Eye irritation and discoloration of soft contact lenses may also occur due to the presence of benzalkonium chloride. It is necessary to remove contact lenses before instillation and reinstall them 15 minutes after instillation of the drug.

Benzalkonium chloride, used as a preservative in eye drops, can cause acupuncture keratopathy and / or toxic ulcerative keratopathy. Care should be taken when using the drug in patients with dry eye syndrome, with damage to the cornea and in the case of the simultaneous use of several types of eye drops containing benzalkonium chloride. It is required to control the state of the cornea with prolonged use of the drug in this category of patients.

There are reports of the possibility of developing bacterial keratitis associated with the use of reusable vials of eye drops. Dropper vials were unintentionally contaminated by patients with concomitant diseases of the organ of vision. The risk of developing bacterial keratitis was higher in patients with impaired corneal epithelium integrity. It is necessary to warn patients about the need to avoid contact of the tip of the dropper bottle with the surface of the eye and other surfaces in order to avoid damage to the organ of vision and bacterial contamination of the drug.

Influence on the ability to drive vehicles and use mechanisms

The drug has little effect on the ability to drive vehicles and work with mechanisms. As with the use of other eye drops, if temporary blurred vision occurs after instillation, it is necessary to wait until the patient's visual perception is restored before driving a car or operating machinery.

Overdose

There were no cases of overdose with topical application.

Treatment: in case of an overdose, symptomatic and supportive therapy is performed.

Drug interactions

Special studies regarding the interaction of Bimoptic Rompharm with other drugs have not been conducted. Drug interactions are not expected in the human body. systemic concentrations of bimatoprost are extremely low (less than 0.2 ng / ml) after instillation of the drug Bimoptic Rompharm, eye drops, 0.3 mg / ml.

In clinical studies, bimatoprost was used simultaneously with several different ophthalmic beta-blockers, but no interaction was observed.

The simultaneous use of bimatoprost and other antiglaucoma drugs, except for ophthalmic beta-blockers, has been studied in the course of studies of the efficacy and safety of combination therapy. There was a decrease in the hypotensive effect of bimatoprost when it was used together with other analogs of prostaglandins in the treatment of ophthalmic hypertension or glaucoma.