Bimatan, eye drops 0.03% 2.5ml

Antiglaucoma agent. Bimatoprost is a synthetic prostamide structurally related to prostaglandin F2α, which does not act through known prostaglandin receptors. Bimatoprost selectively mimics the effects of recently discovered biosynthesized substances, prostamides. However, the structure of the prostaglandin receptors has not yet been identified.

Pharmacokinetics

Bimatoprost penetrates well into the human cornea and sclera in vitro. After instillation in adults, systemic exposure of bimatoprost is very low and no accumulation of the active substance has been noted.

After administration of one drop of the drug in both eyes once daily for 2 weeks, the blood concentration reached a maximum 10 min after administration of the dose, and within 1.5 h it was below the level of determination (0.025 ng/ml).

The mean Cmax and AUC0-24 h values were approximately the same on days 7 and 14, approximately 0.08 ng/mL and 0.09 ng×h/mL, respectively, indicating that the Css of bimatoprost was achieved within 1 week of instillation. Bimatoprost is moderately distributed in body tissues, and Vd at equilibrium is 0.67 L/kg. In human blood bimatoprost is mainly in plasma.

The binding of bimatoprost to plasma proteins is about 88%. Bimatoprost reaches the systemic bloodstream mainly in unchanged form. Then there is oxidation, N-deletylation and glucuronidation with the formation of a number of metabolites.

Bimatoprost is excreted mainly by the kidneys. Up to 67% of the dose administered by injection into healthy adult volunteers was excreted with the urine, 25% – in the feces. T1/2 after IV administration was approximately 45 min, total blood clearance was 1.5 l/h/kg.

Bimatoprost decreases intraocular pressure by increasing aqueous outflow through the trabecular meshwork and increasing uveoscleral outflow.

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

According to clinical studies, no significant effect of bimatoprost on HR and BP has been noted.

Indications

Open-angle glaucoma and ophthalmic hypertension in adults (as monotherapy or in combination with beta-adrenoblockers).

Active ingredient

Bimatoprost

Composition

1 ml:

The active substance:

• bimatoprost 0.3 mg;

Excipients:

• benzalkonium chloride – 0.05 mg,
• sodium chloride – 8.3 mg,
• citric acid monohydrate – 0.14 mg,
• sodium hydrophosphate heptahydrate – 2.68 mg,
• sodium hydroxide – to pH 7.3,
• hydrochloric acid – to pH 7.3,
• water d / i – to 1 ml.

How to take, the dosage

The recommended dose is one drop of bimatoprost in the affected eye(s) once daily in the evening. Do not exceed the recommended dose.

If more than one ophthalmic drug is used for topical administration, an interval of 5 minutes should be observed between each administration.

Interaction

The hypotensive effect of bimatoprost when used in combination with other prostaglandin analogues in the treatment of ophthalmic hypertension or glaucoma has been observed to decrease.

Special Instructions

There is no experience with bimatoprost in patients with concomitant respiratory dysfunction, which requires caution in such patients. No significant adverse effects on the respiratory system have been observed in clinical studies in patients with respiratory dysfunction.

The effects of bimatoprost on patients with grade II or III AV blockade and on patients with uncontrolled congestive heart failure have not been studied.

Patients should be informed of the possibility of eyelash growth, darkening of the eyelid skin, and increased iris pigmentation before starting treatment.

Some of these changes may be permanent and can lead to differences in appearance between eyes when only one eye is treated. Changes in iris pigmentation occur slowly and may not be noticeable for months or years. Most often, the change in iris color is permanent.

The change in iris color has more to do with an increase in melanin in melanocytes than with an increase in melanocytes. The long-term effects of increased iris pigmentation are unknown.

In typical cases, brown pigmentation typically spreads from the area around the pupil to the root of the iris, resulting in the entire iris or parts of the iris becoming more brown. Bimatoprost has no effect on iris nevi and lentigos. Periorbital pigmentation is reversible in some patients.

Contraindications

Hypersensitivity to bimatoprost; age less than 18 years.

Bimatoprost should be used with caution in patients with known risk factors for macular edema (e.g., patients with aphakia, patients with artifactia and posterior lens capsule rupture); patients with a history of severe eye infections (e.g., caused by herpes simplex virus) or iritis/veitis.

Side effects

Definition of adverse reaction frequency categories: very common (&le1/10); common (&le1/100 to <1/10); infrequent (&le1/1000 to <1/100); rare (&le1/10 000 to <1/1000); very rare (<1/10 000), frequency unknown (frequency cannot be estimated based on available data).

Nervous system disorders: frequent – headache; infrequent – dizziness.

An organ of vision: very often – conjunctival injection, itching in the eyes, eyelash growth; common – superficial pitting keratitis, corneal erosion, burning eyes, eye irritation, allergic conjunctivitis, blepharitis, decreased visual acuity, asthenopia, conjunctival edema, foreign body feeling in the eye, dry eye, eye pain, photophobia, lacrimation, eye discharge, visual disturbance, increased iris pigmentation, darkened lashes; infrequent – hemorrhagic retinal disorders, uveitis, cystoid macular edema, iritis, blepharospasm, eyelid retraction, periorbital erythema; frequency unknown – enophthalmus. In very rare cases, corneal calcification has been noted when using phosphate-containing eye drops in patients with concomitant significant corneal damage.

Cardiovascular system disorders: often – arterial hypertension.

Hepatobiliary system disorders: frequent – abnormal biochemical parameters of liver function.

Skin and subcutaneous tissue: infrequent – hirsutism.

General reactions: infrequent – asthenia.

Overdose

No cases of overdose have been reported with topical administration. In case of overdose, treatment should be symptomatic and supportive.

Pregnancy use

It is contraindicated in children and adolescents under 18 years of age.

There are no data from clinical trials of bimatoprost in pregnancy. The use of bimatoprost in pregnancy is not recommended unless there are strict indications.

Preclinical animal studies have shown reproductive toxicity when bimaptoprost is used at high, maternal toxic doses.

It is not known whether bimaptoprost is excreted with breast milk in humans. In animal studies, bimatoprost has been shown to be excreted with breast milk. The decision to continue/terminate breastfeeding or to continue/terminate treatment with bimatoprost should be made based on the benefit of breastfeeding for the baby and the benefit of therapy for the mother.

Similarities

Bimoptic