CA
US
AU
UK
DE
FR
IT
ES
DA
FI
NO
NL
SV
Tradename
Monopreparation: Latisse (Allergan). Combined medication: Hanforth (Allergan).
Chemical name: (5Z) -7 - {(1R, 2R, 3R, 5S) -3,5-dihydroxy-2 - [(1E, 3S) -3-hydroxy-5-phenyl-1-penten-1-yl ] cyclopentyl} -N-ethyl-5-heptenamide
Molecular formula: C25H37NO4
Molar mass: 415.57
CAS Number: 155206-00-1
Solubility: Soluble in ethanol (50 mg/ml), methanol, DMSO (25 mg/ml), DMF (25 mg/ml).
Release form, composition
Latisse - eye drops, 0.3 mg/ml bimatoprost in a dropper vial 3.0 ml. Transparent colorless liquid, insoluble in water.
Gunfort - eye drops, 0.3 mg/ml bimatoprost + 6.8 mg/ml timolol maleate in a dropper vial 3.0 ml. Transparent colorless or slightly yellowish liquid.
Excipients in (1 ml.)
Latisse - benzalkonium chloride (0.05 mg), sodium chloride, sodium phosphate dibasic, citric acid, sodium hydroxide or hydrochloric acid, purified water.
Hanforth - benzalkonium chloride (0.05 mg), sodium chloride, sodium phosphate dibasic heptahydrate, citric acid monohydrate, sodium hydroxide or hydrochloric acid, purified water.
Pharmachologic effect
Bimatoprost is a synthetic prostamide, structurally related to prostaglandins F2. However, the action that reduces IOP in this drug is not in binding to prostaglandin receptors, but in selective imitation of the effect of prostamides. The exact mechanism of action of bimatoprost is not known, since no receptors have been found in the human body for the time being.
The effect of reducing IOP is to increase outflow through the trabecular meshwork and uveoscleral outflow of intraocular fluid. The effect of the drug begins to appear about 4 hours after administration and reaches a maximum after 8-12 hours. Its duration is at least 24 hours.
Pharmacokinetics
Bimatoprost well penetrates the cornea and sclera of a person. It has a very small systemic effect after instillation, it is not capable of cumulation. So, with a single injection per day, the maximum concentration in the blood of it comes after 10 minutes, and decreases to the lower limit of sensitivity of laboratory methods (about 0.025 ng/ml) for 1.5 hours. The half-life for intravenous injection is about 45 minutes.
Plasma proteins bind approximately 88% of bimatoprost. The remaining amount is in free form. Removal of the drug is carried out mainly by the kidneys: up to 67% of it is excreted in the urine, 25% in the feces.
Dosing regimen
The recommended dose is 1 drop in the evening in the affected eye. Increasing the frequency of instillations may reduce the therapeutic effect of the drug. If the next dose was missed, the use of the drug should be continued without changing the scheme, that is, no more than 1 drop per day in the affected eye. At the same time taking bimatoprost with other prostaglandin analogues, it is necessary to carefully monitor the level of IOP.
Indications for use
Ophthalmic hypertension and open-angle glaucoma.
Clinical researches
According to the results of the study in patients with an initial average IOP level of 26 mm Hg. st. (P0) in the treatment of 0.03% solution of bimatoprost there was a decrease of 7-8 mm Hg. st. When comparing the effects of 0.01% and 0.03% solution of the drug in patients with an average IOP of 23.5 mm Hg. st. the hypotensive effect in the first case was 7.5 mm Hg. st, which is 0.5 mm Hg. st. 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 due to an increase in the amount of pigment in melanocytes, but this is not accompanied by an increase in the number of the latter. The severity of manifestations depends on the duration of the reception. After the abolition of bimatoprost, pigmentation of the iris often does not 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.
In some cases, there is a reversible in the case of the withdrawal of bimatoprost increased growth, thickness and number of eyelashes.
The drug is prescribed with caution in patients with active intraocular inflammatory process (for example, uveitis, iritis) because of its possible increase. There is also evidence of recurrent corneal infiltrates or eye infection with bimatoprost. In this regard, more careful monitoring of patients using this drug is necessary if there is a history of viral damage to the eye (for example, herpes simplex virus).
Admission bimatoprost in rare cases may contribute to the development of macular edema. For this reason, it is not recommended to use the drug in patients at risk of developing this pathology (aphakia, damage to the posterior capsule as a result of cataract extraction, diabetic retinopathy).
The effect of bimatoprost in the treatment of angle-closure and narrow-angle, uveal, neovascular and congenital glaucoma has not been studied.
Bimatoprost should be used with caution in patients with renal and hepatic insufficiency.
The effect of bimatoprost has not been studied in patients with impaired respiratory function. However, there is evidence of a possible deterioration of bronchial asthma, dyspnea, and chronic obstructive pulmonary disease.
It is necessary to use the drug with caution in this group of patients.
The safety of using bimatoprost in the presence of intracardiac blockades or progressive heart failure has not been evaluated, but there are isolated reports in the literature about the development of bradycardia or hypotension against the background of its administration. It is recommended to prescribe the drug with caution in patients with low heart rate and low blood pressure.
Due to the presence of benzalkonium chloride, it is necessary to monitor the state of the cornea with prolonged use due to the risk of developing pinpoint and / or toxic ulcerative keratopathy, especially in patients with "dry" eye syndrome and using contact lenses.
The risk category for the use of the drug during pregnancy by the FDA is C. In animal studies, it has been established that bimatoprost has a teratogenic effect in doses far exceeding the maximum for humans. Adequate research on women has not been conducted. The possibility of excretion of the drug and its metabolites into mother's milk has not been studied, but this fact has been established in animal experiments. For this reason, the appointment of the drug is possible in cases where the effect for the mother outweighs the potential risk of side effects for the fetus or child.
Currently, there is no data on the effect of bimatoprost on human fertility. The drug also had no carcinogenic and mutagenic effect in experiments on animals.
The safety of the drug in children under 18 years of age has not been evaluated.
Possible short-term blurring of vision or other visual disorders. When they occur, you must refrain from driving.
Side effects
The most frequent side effect is conjunctival hyperemia (15-45% of cases). It progressively decreases to almost complete disappearance by the third year of application of bimatoprost. In 0.5-3% this is the reason for the abolition of the drug. Other common side effects are eyelash growth, itching (15-45%).
In 1-10% of cases dryness, burning, pain, irritation in the eye, visual impairment, foreign body sensation, pigmentation of the periocular area, blepharitis, cataracts, superficial keratitis, periorbital erythema, darkening of the eyelashes, discharge from the eye, tearing, photophobia can be detected , allergic conjunctivitis, asthenopia, increased pigmentation of the iris, conjunctival edema, hyposagism, abnormal hair growth.
In less than 1% of cases, intraocular inflammation (iritis) occurs.
Of the systemic side effects, colds and upper respiratory infections are the most common (about 10%). About 1-5% of patients may complain of headache, increased liver enzymes in laboratory tests, asthenic condition.
Drug interaction
The interaction of bimatoprost with other medicinal substances is unlikely due to its extremely low concentration in the blood after instillation into the eye. As shown by preclinical studies, the drug is biotransformed in various ways, does not affect the liver enzymes involved in the metabolism of other drugs.
Studies have not shown interactions with various types of ?-blockers when used together. Interaction with other antiglaucoma drugs has not been studied.
Overdose
So far, no overdose has been reported. If they occur, symptomatic treatment is required.
Do you know exactly how to care for your eyes correctly?
No one will argue that the eyes are the mirror of the soul. In the eyes you can "drown" as in the ocean. All women want to have beautiful eyes and the most expressive look. If you properly care for your eyes, you can not only affect the appearance of your eyes, but also significantly improve your vision.
Eyelids deserve special attention. To care for them, it is advisable to use only special products, which are marked "Skin care for the eyelids."
It is also worth remembering in which direction it is necessary to apply care products and massage the skin in the eye area.
Massage lines applying creams around the eyes
- Applying cream and massage the skin in the eye area is carried out in the directions of the least stretching of the skin.
- On the upper eyelids - from the inner to the outer corner of the eye.
- On the lower eyelids - from external to internal.
ATTENTION! Such a procedure as moisturizing is especially relevant in summer, and in a cold season with moisturizing creams you need to be careful: the moisture on the skin, combined with the cold, turns into ice. Therefore, at this time of the year it is recommended to use more fat facial creams.
In the morning (not less than half an hour before leaving the house) clean the skin, and then easily apply a thin layer of rich cream so that it is completely absorbed. At night - after thoroughly cleaning the skin - also pamper your face, neck and decollete with a rich cream. The cream can be left on the face for no longer than two hours. At bedtime, remove the excess with a soft cloth.
Keep in mind that in extreme cold the main dose of the cream should be applied in the evening.
If you think that moisturizing cosmetics is an expensive pleasure, then pay attention to the effective remedies that nature itself offers.
Making cream at home is easy. But know the measure: do not test on your face more than one type of cream per week.
And further. If you have sensitive to sensitive skin, be especially careful - experimental doses should be minimal. Choose the most suitable recipes for your skin.
Home cosmetics does not contain preservatives. But, on the other hand, it is impossible to keep homemade creams for a long time even in the refrigerator. Prepare drugs in small quantities and use them while they are fresh. Their shelf life in the refrigerator is up to seven days.
Home remedies against bruises and circles
However, there are home remedies that will help restore the tone and healthy color to the sensitive skin under the eyes. For example, to get rid of circles and bruises under the eyes will help a compress from the infusion of sage. At bedtime, brew 1 teaspoon in 100 ml of boiling water and cover the jar with a lid for 15 minutes. Cool one part in the refrigerator, and slightly heat the other. Then soak two small pieces of cotton in a heated infusion and place them on closed eyes. After 10 minutes, make a cold compress. Alternately apply to the eyes a compress from hot or cold broth (each for 7-10 minutes).
The parsley leaf mask works effectively against bags under the eyes. Finely chop the fresh green leaves and apply them on the swollen skin. Then cover your eyes with wet cotton swabs and leave the mask for 15-20 minutes.
It is best to fight eyelid swelling with a potato mask. Take the washed, but not peeled raw potatoes and rub it on a fine grater. Then 2 tsp of the resulting puree mix with 2 tsp of flour and 1 tbsp. a spoon of milk. Then put a mask on the eyelids and hold it for 15-20 minutes.
Well improves blood circulation around the eyes mask of coriander, cucumber and sour cream. Take 2 teaspoons of chopped coriander and cucumber and stir them in 1 tbsp. spoon sour cream. Apply the mask on the eyelids and skin around the eyes for about 15 minutes. Then rinse your face with cool water and apply a moisturizer on your eyes.
Eyes really need vitamins.
In addition, the eyes need certain vitamins, thanks to which the vision remains sharp for a long time, and fatigue recedes. The most famous of them are riboflavin, thiamine, ascorbic acid (vitamin C), carotene (vitamin A), as well as folic acid, pyridoxine, vitamins PP and B12.
If you get enough of these vitamins, vision problems will not occur, and the performance will always be normal. The risk of developing eye diseases - for example, cataracts, glaucoma, will also significantly decrease; if the disease is already there, then its development will slow, and the symptoms may begin to decrease.
How to provide our eyes with everything necessary to cope with the loads and see well? First of all, you need to follow the diet, and prepare food so that the vitamins are not destroyed.
For example, vitamin C and riboflavin (vitamin B2) are destroyed by boiling, so it is better to look for other ways to prepare the products in which they are contained. Special vitamin complexes, as well as vitamin drops prescribed by ophthalmologists, will also help preserve eyesight and eye health.
Eye Care Masks
A mask with parsley and sour cream helps to remove swelling and reduce the "bags" under the eyes. Grind parsley (1 tsp) and mix it with sour cream (2 tsp). Apply the mixture on the eyelids for 20 minutes, then rinse with cool water.
Dry and fading eyelid skin will help revive oil compresses. Soak gauze wipes with olive oil, and place on closed eyes for 10 minutes. Remove the remaining oil moistened in warm tea with a cotton swab.
Compresses from infusions of herbs relieve fatigue and inflammation from the eyes. Prepare an infusion of lime blossom, calendula flowers, chamomile or cornflower. Brew the grass, as usual tea - 1 tsp. a glass of boiling water, and leave for half an hour. Compresses are best done in the morning and evening, for 5-10 minutes.
The mask of cucumber, sour cream and coriander improves blood circulation in the skin around the eyes and eliminates bruises. It is necessary to take 1 tsp. finely chopped cucumber and coriander, and mix them with 1 tbsp. sour cream. Apply the mixture for 15 minutes on the skin around the eyes. Rinse with cool water.
Another mask with an oil solution of vitamin E will help reduce the amount of wrinkles that have already appeared. Here you need to mix it (1 tablespoon) with the same amount of cocoa butter and sea buckthorn. The mixture of oils is applied with a rather thick layer around the eyes, and in the zone of the crow's feet they are fixed with pieces of parchment paper. The oil mask is held for up to 15 minutes, then get wet with a napkin. Rinse is not necessary - the mask is done at night, but not later than 1.5 hours before bedtime. If you make this mask 2-3 times a week, the wrinkles will become noticeable much less.
