Bimatoprost is a synthetic prostamide, structurally linked to prostaglandins F2α. However, the action of reducing IOP in this drug is not related to prostaglandin receptors, but selectively simulating the effect of prostamides. The exact mechanism of action of bimatoprost is not known, because there are no receptors for it in the human body at present.
The effect of PIO reduction is to increase the flow through the trabecular network and the uveoscleral flow of intraocular fluid. The effect of the drug starts to appear at about 4 hours after administration and reaches a maximum after 8-12 hours. Its duration is at least 24 hours.
The bimatoprost penetrates well into the cornea and into the sclera of a person. It has a very small systemic effect after instillation, it is not capable of cumulation. So, with one injection per day, the maximum concentration in his blood comes after 10 minutes and decreases to the lower limit of sensitivity of the laboratory methods (about 0.025 ng / ml) for 1.5 hours. The intravenous half-life is approximately 45 minutes.
Plasma proteins bind about 88% of bimatoprost. The remaining amount is in free form. Excretion of the drug is mainly through the kidneys: up to 67% of it is excreted in the urine, 25% in the faeces.
Dosage scheme: The recommended dose is 1 drop at night in the affected eye. Increasing the frequency of instillations may reduce the therapeutic effect of the drug. If the next dose is missed, the drug should be continued without changing the schedule, ie no more than one drop per day in the affected eye. At the same time, taking bimatoprost together with other prostaglandin analogues, IOP levels should be carefully monitored.
Instructions for use: Hypertension and open-angle glaucoma.
Clinical studies : According to the results of the study, in patients with an average initial IOP level of 26 mm Hg. Art. (P0) In the treatment with 0.03% bimatoprost solution there was a decrease of 7-8 mm Hg. Art. When comparing the effects of 0.01% and 0.03% drug solution in patients with an average IOP of 23.5 mm Hg. Art. The hypotensive effect in the first case was 7.5 mm Hg. st, which is 0.5 mm Hg. Art. Less than the drug with a higher concentration.
Contraindications: Hypersensitivity to bimatoprost.
Precautions and warnings: Bimatoprost often causes increased pigmentation of the iris, eyelids and eyelashes. These effects are manifested by an increase in the amount of pigment in melanocytes, but this is not accompanied by an increase in the number of pigment. The severity of the events depends on the duration of the reception. After elimination of bimatoprost, the pigmentation of the iris does not often return to the original, while the pigmentation of the eyelids and eyelashes may decrease. The long-term effects of this effect have not been studied.
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