Order Bimatoprost 0.3 mg/ml eye drops

What is Bimatoprsot?

Bimat eye drops are used by patients who have been diagnosed with intra ocular high pressure, a state which can lead to glaucoma. Left untreated, glaucoma can lead to blindness. By reducing intra ocular pressure, the risk of blindness associated to this condition is drastically reduced.

Structural formula

Bimatoprost

Russian name

Bimatoprost

Latin name of the substance Bimatoprost

Bimatoprostum ( genus Bimatoprosti)

Chemical name

7- [3,5-Dihydroxy-5-phenylpent-1-enyl) cyclopentyl] -N-ethylhept-5-enamide

Gross formula

25 H 37 NO 4

Pharmacological group of the substance Bimatoprost

  • Ophthalmic agents

Nosological classification (ICD-10)

H02 Other diseases of the eyelidsH40.0 Suspected glaucomaH40.1 Primary open-angle glaucoma

CAS code

155206-00-1

Pharmacology

Pharmacological action – antiglaucoma, prostaglandin-like, lowering intraocular pressure, stimulating the growth of eyelashes .

Pharmacodynamics

Bimatoprost reduces IOP in humans by increasing the outflow of aqueous humor through the trabecular meshwork and uveoscleral outflow. The decrease in IOP begins approximately 4 hours after the first application and the maximum effect is achieved approximately after 8-12 hours. The effect lasts for at least 24 hours.

Bimatoprost is a potent ophthalmic antihypertensive agent. It is a synthetic prostamide, structurally related to PGF 2alpha , which does not act through the known PG receptors . Bimatoprost selectively mimics the effects of recently discovered biosynthesized substances, prostamides. However, the structure of prostamide receptors has not yet been identified.

Limited information is available on the effectiveness of bimatoprost in the treatment of pseudoexfoliative and pigmentary glaucoma, as well as on the experience of using bimatoprost in the treatment of angle-closure glaucoma in patients who have previously undergone iridotomy.

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

In the treatment of hypotrichosis, the exact mechanism of action of bimatoprost is unknown, however, it is assumed that eyelash growth occurs due to an increase in the number of eyelashes, as well as an increase in the duration of the hair follicle growth phase or eyelash growth phase.

Children. 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 cornea and sclera of the human eye in vitro . When instilling in adults, the systemic exposure of bimatoprost is very small, no accumulation of drugs was noted. After applying a 0.03% solution of bimatoprost, 1 drop in both eyes once a day for 2 weeks, C max in the blood was reached within 10 minutes after instillation, and within 1.5 hours this indicator was below the detection level (0.025 ng / ml). The average values ​​of C max and AUC 0-24 were approximately the same on the 7th and 14th day – approximately 0.08 ng / ml and 0.09 ng · h / ml, respectively, which indicates that C ss bimatoprost was achieved within the first week of instillations.

Distribution. Bimatoprost is moderately distributed in the tissues of the body, systemic V ss  – 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 glucuronization occurs with the formation of a number of metabolites.

Excretion. Bimatoprost is excreted mainly through the kidneys. To 67% w / w of the administered dose in healthy adult volunteers excreted in the urine, 25% of the dose excreted in the feces. T 1/2 after / in the administration was approximately 45 minutes; total clearance from blood – 1.5 l / h / kg.

Application of the substance Bimatoprost

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

Treatment of hypotrichosis of the eyelashes (insufficient eyelash growth).

Contraindications

Hypersensitivity; pregnancy; lactation period; age up to 18 years.

Restrictions on use

As an antiglaucoma drug . Caution should be exercised when used in the therapy of patients with known risk factors for macular edema (for example, patients with aphakia, patients with pseudophakia and rupture of the posterior lens capsule);

– should be used with caution in patients with a history of severe eye infections (eg, caused by herpes simplex virus) or iritis / uveitis;

– 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 heart block more severe than the first degree or in patients with uncontrolled congestive heart failure. A limited number of cases of bradycardia or hypotension have been observed with bimatoprost. Bimatoprost should be used with caution in the treatment of patients prone to low heart rate or low blood pressure;

– the effect of bimatoprost has not been studied in patients with inflammatory diseases of the organ of vision, neovascular, inflammatory, angle-closure glaucoma, congenital glaucoma or narrow-angle glaucoma.

As a drug for the treatment of eyelash hypotrichosis. Afakia; pseudophakia; damage to the posterior capsule of the lens; the presence of risk factors for the development of macular edema; long course of diabetes mellitus; high content of Xc; nephropathy; arterial hypertension, especially with high DBP numbers; patients with uveitis, due to the possible progression of this disease.

Application during pregnancy and lactation

FDA category of action on the fetus – C.

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.

In animal studies, miscarriages were observed with oral administration of bimatoprost at a dose that was 33–97 times higher than recommended for topical use. When used in a dose that was 41 times higher than the therapeutic dose, there was a decrease in the gestation period, an increase in the frequency of fetal death, and a decrease in the body weight of newborns.

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. Animal studies have shown that bimatoprost is excreted in breast milk. If it is necessary to use bimatoprost during breastfeeding, it is necessary to make a decision to stop breastfeeding or bimatoprost therapy, taking into account the benefits of breastfeeding for the child and the need for therapy for the mother.

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

Side effects of the substance Bimatoprost

When used as an antiglaucoma drug

The following adverse events were observed during clinical trials of bimatoprost in the form of 0.03% eye drops and in the post-registration period.

Frequency of occurrence is given in accordance with the following classification: very common (≥1 / 10); often (≥1 / 100 to </ 10); infrequently (≥1 / 1000 to <1/100); rarely (≥1 / 10,000 to <1 / 1,000); very rare (<1/10000) and with unknown frequency (cannot be estimated from available data).

In each group, adverse effects are presented in order of decreasing severity.

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

From the side of the organs of vision: very often – injection of conjunctival vessels, 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, dryness of the mucous membrane of the eyes, redness of the eyelids, pain in the eyes, photophobia, discharge from the eyes, blurred vision, itching of the eyelid skin, decreased visual acuity, asthenopia, conjunctival edema, foreign body sensation in the eye, dry eye, eye pain, photophobia, lacrimation, eye discharge, blurred vision, increased iris pigmentation, darkening of eyelashes; infrequently – retinal hemorrhagic disorders, uveitis, cystic macular edema, iritis, blepharospasm, eyelid retraction, periorbital erythema; with an unknown frequency – enophthalmos.

From the side of the vessels: often – hypertension.

On the part of the skin and subcutaneous tissues: infrequently – hirsutism.

General disorders and disorders at the injection site: infrequently – asthenia.

Data from laboratory and instrumental studies: often – a deviation from the norm of biochemical parameters of liver function.

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

When used as a drug for the treatment of eyelash hypotrichosis

General information about adverse reactions when using bimatoprost in the form of 0.03% drops for topical application was obtained in a multicenter, randomized, double-blind, placebo-controlled study in parallel groups involving 278 adult patients who received therapy with the study drug for 4 months.

Itchy eyes, conjunctival hyperemia, eyelid hyperpigmentation, eye irritation, dry eye syndrome, eyelid redness. The listed adverse reactions were observed in less than 4% of cases.

The frequency of occurrence of adverse events according to post-registration use data cannot be determined due to the lack of information on the size of the population in which the development of each of the adverse events was noted, as well as the spontaneous nature of reports of adverse events in this period. Additionally, in the post-registration period, the following adverse reactions were reported: burning sensation of the eyelids, swelling of the conjunctiva, irritation of the eyelids, edema of the eyelids, itching of the eyelid skin, hyperpigmentation of the iris, hypersensitivity reactions (local allergic reactions), lacrimation, madarosis and trichorexis (temporary loss of eyelashes from several pieces to whole areas and temporary fragility of the eyelashes, respectively), changes in the skin of the eyelids and periorbital area, including deepening of the eyelid folds, spotty rash or erythematous rashes,

Interaction

Special studies of interaction with other drugs have not been conducted. No interaction is expected in the human body, as systemic concentrations of bimatoprost are extremely low (less than 0.2 ng / ml) after topical application of bimatoprost in ophthalmology.

In clinical studies, bimatoprost was used in conjunction with several different beta-blockers for topical use in ophthalmology, but no interaction was observed.

The simultaneous use of bimatoprost and other antiglaucoma drugs , except for ophthalmic beta-blockers, has not 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 in the form of eye drops when used together with other analogs of PG in the treatment of ophthalmic hypertension or glaucoma.

Overdose

There were no cases of overdose with topical application.

In case of overdose, treatment should be symptomatic and supportive.

Route of administration

Conjunctivally, locally.

Precautions for substance Bimatoprost

Influence on IOP . Bimatoprost reduces IOP when it is instilled directly into the conjunctival cavity of patients with increased IOP . In clinical studies, the use of bimatoprost in the form of drops for topical application was accompanied by a decrease in IOP both in patients with high IOP and with its normal values, but did not reach clinically significant values. With the combined use of bimatoprost in the form of drops for topical use and analogs of PG ( including bimatoprost in the form of eye drops) used to reduce IOPin patients with intraocular hypertension, a decrease in the hypotensive effect is possible. If the patient receives treatment with analogs of PG , consultation with the attending physician and monitoring of IOP are necessary when prescribing additional therapy with bimatoprost in the form of drops for topical use.

At-risk groups. Caution should be exercised when used in patients with acute inflammatory diseases of the inner membranes of the eyeball, for example, with uveitis (since the use of bimatoprost may aggravate the course of inflammation), in patients with aphakia, pseudoaphakia with rupture of the posterior lens capsule or with risk factors for the development of macular edema.

Pigmentation of the iris.Increased pigmentation of the iris is possible, especially with dark pigments, this effect may be irreversible. Increased pigmentation of the iris was observed with instillation of eye drops. Changes in pigmentation are primarily associated with an increase in melanin content, as well as an increase in the number of melanocytes. The duration of the pigmentation enhancing effect is unknown. Changes in the color of the iris during treatment may go unnoticed for a period from several months to several years. There is no evidence of the clinical relevance of increased iris pigmentation in the long term. As a rule, when using bimatoprost, brown pigmentation around the pupil spreads concentrically to the periphery of the iris, as a result of which the entire iris or individual sectors acquire a brownish color. The use of bimatoprost does not affect the accumulation of pigment on the iris (nevi and freckles). A significant increase in the pigmentation of the iris is not an indication for the cancellation of bimatoprost in the form of drops for topical application.

Eyelid skin pigmentation. Bimatoprost has been reported to cause darkening of the eyelids and periorbital region.

It is assumed that pigmentation may increase during the entire period of use of bimatoprost, but in most patients it is reversible and gradually disappears when the drug is discontinued .

Hair growth outside the treatment area. Hair growth is possible in those areas of the skin to which bimatoprost was accidentally applied in the form of drops for topical application. It is important to apply the drugs only to the skin of the edge of the upper eyelid along the lash line using the supplied sterile applicator; avoid contact with facial skin.

In case of any symptoms on the part of the organ of vision ( including an eye injury, an infectious complication), with a sudden decrease in visual acuity, the need for a planned ophthalmic operation, as well as in the event of undesirable reactions, you should contact an ophthalmologist to resolve the issue of the possibility of further treatment with bimatoprost.

With hypotrichosis of the eyelashes, the effect of treatment develops gradually, in most patients within 2 months. Patients should be warned that the effect of bimatoprost is inconsistent, and a gradual return to its original state is expected after discontinuation of drug use . In addition, there may be differences in the length of the eyelashes, their thickness, color intensity, the total number of eyelashes or uneven growth, and / or a change in the direction of eyelash growth.

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

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