Bimatoprost is a synthetic prostamide that is structurally related to prostaglandins F2α.
The action that can reduce IOP in this drug is to selectively simulate the effect of prostamides, and not to bind to prostaglandins with receptors.
The mechanism of action of the drug Bimatoprost is not precisely known, because at the present time no receptors have been found for it in the body.
The effect of a gradual decrease in IOP is the uveoscleral outflow of the intraocular fluid, as well as the increased outflow of the trabecular network passing through.
The effect of this drug begins somewhere after 4 hours immediately after administration, and reaches a maximum after only 8-12 hours. Its total duration is about 24 hours.
Bimatoprost effectively penetrates the sclera and the cornea. It is also not capable of cumulation, and after instillation it has a rather low systemic effect.
Thus, when administered once a day, its maximum concentration in the blood occurs in about 10 minutes, and decreases to the lowest sensitivity limit of laboratory methods in just 1.5 hours. With intravenous administration, the half-life is approximately 45 minutes.
Plasma proteins in general bind about 88% of Bimatoprost. The remaining amount is in absolutely free form.
Removal of the drug is carried out by the kidneys:
- up to 67% is excreted in the urine,
- 25% - with feces.
Indications for use
The effect of the drug Bimatoprost does not appear immediately, but for 1-2 months. Remember that the effect may be inconsistent, and if you stop using it, the eyelashes may return to the previous state.
In addition, in some cases there are differences in the length of old and new eyelashes, thickness, as well as the direction of growth and intensity of color.
If suddenly you forget to apply the drug at the time - this does not mean that you need to double the next dose, just plan to continue to apply the drug at the usual time.
Do not use Bimatoprost during pregnancy or breastfeeding, in the absence of data from clinical trials.
The drug Bimatoprost is recommended for use with:
- hypotrichosis (insufficient growth) of the eyelashes;
- excessive loss of eyelashes.
Mode of application
The standard dose is 1 drop once a day (in the evening) to the affected eye. A significant increase in the multiplicity of application can reduce the therapeutic effect.
In the case when the next dose is missed, the use of the drug should be continued without change, that is, 1 drop per day. In the case of simultaneous administration of Bimatoprost with any other prostaglandin analogues, it is imperative to monitor the level of IOP.
Release form, composition
Ophthalmic drops for local use. Bimatoprost 0.03% is produced in a 3 ml polyethylene bottle (the kit also has a special applicator).
The main active ingredient of this drug: bimatoprost - 0.03 mg / ml.
Additional components are:
- sodium chloride;
- benzalkonium chloride;
- disubstituted sodium hydrogen phosphate;
- distilled water,
- citric acid.
To adjust the pH, sodium hydroxide or hydrochloric acid is added. At the same time the pH level is 6.8-7.8.
Interaction with various drugs
The interaction of the drug Bimatoprost with other drugs is unlikely due to its extremely low concentration in the blood immediately after instillation into the eyes.
According to the results of preclinical studies, this drug is biotransformed in absolutely different ways, without affecting the liver enzymes that are involved in the metabolism of other drugs.
Conducting numerous studies did not show interaction with all types of β-blockers in the case of simultaneous use. However, interaction with other antiglaucoma drugs has not yet been studied.
Bimatoprost is contraindicated in the following cases:
- in childhood;
- pregnancy, as well as breastfeeding;
- in case of hypersensitivity to the drug Bimatoprost or other components of the drug.
Bimatoprost can often cause increased pigmentation of the eyelids, iris and eyelashes. Such effects may occur 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 particular severity of such manifestations depends solely on the duration of the reception. Immediately after discontinuing Bimatoprost, the pigmentation of the iris often does not return to the original, and the pigmentation of the eyelashes and eyelids can significantly decrease. The long-term effects of this effect have not yet been studied.
There are exceptions when reversal is noted when discontinuing the drug: increased growth, the number and thickness of eyelashes.
With extreme caution, this drug is prescribed to patients with a rather active inflammatory intraocular process (for example, uveitis and iritis) due to its amplification.
In addition, there are some data on the recurrence of corneal infiltrates or eye infection during the use of Bimatoprost.
In this case, the most careful control is needed for sick patients who use this drug, if there is a history of viral eye damage (for example, the herpes simplex virus).
Acceptance of the drug Bimatoprost in exceptional cases can contribute to the gradual development of so-called macular edema.
It is because of this that doctors do not recommend using this drug to patients at risk of developing one of their pathologies:
- diabetic retinopathy,
- damage to the posterior capsule due to cataract extraction,
The effect of the drug Bimatoprost has not yet been studied in the treatment of narrow-angle and angle-closure, neovascular, congenital and uveal glaucoma.
With extreme caution, Bimatoprost should be prescribed to patients with both hepatic and renal insufficiency.
The effect of the drug has also not been studied in patients with impaired respiratory function. But there is some evidence of worsening asthma, chronic lung disease and dyspnea.
This group of patients should be given this drug with extreme caution.
In the presence of any intracardiac blockade or heart failure, the safety of using the drug Bimatoprost has not yet been assessed, but in the literature there are isolated reports of hypotension, as well as the development of bradycardia against the background of its use.
In addition, it is recommended to prescribe this drug with extreme caution to patients with a fairly low heart rate, as well as low blood pressure.
Due to the presence in the composition of a substance such as benzalkonium chloride with long-term use of the drug, constant monitoring of the state of the cornea is mandatory. All this is due to the risk of developing toxic or pinpoint ulcerative keratopathy, especially in patients who use contact lenses or with dry eye syndrome.
The risk of using the drug during pregnancy according to the FDA is category C. In an animal study, it was found that the drug Bimatoprost has a strong teratogenic effect in the case of increasing doses that far exceed the maximum for the human body.
No adequate research has been conducted on women. The possibility of excretion of the drug, as well as its metabolites into the milk of a nursing mother, was also not studied, but this fact was established in experiments on animals.
Because of this, the appointment of this drug is possible only when the resulting effect for the mother will exceed the risk of developing any side effects for the child.
In humans, at the moment, Bimatoprost has not revealed any effects on fertility. In addition, the drug did not have any carcinogenic or mutagenic effect in the conducted experiments on animals.
Not evaluated and the safety of using Bimatoprost in children under 18 years of age.
Short-term blurred vision or other visual disturbances are also possible. In case of their occurrence, it is required to refrain from driving auto transport.
The most common and most frequent side effect is conjunctival hyperemia (in 15-40% of cases).
By the third year of use of the drug, it progressively begins to decrease almost to complete disappearance.
Approximately 0.5-3% of patients consider this a reason to stop taking the drug. Quite frequent side effects are severe itching and growth of eyelashes (approximately 15-40%).
In 1-10% of all cases, side effects such as:
- dryness, pain, burning and irritation in the eye,
- some visual impairment,
- constant foreign body sensation in the eye,
- pigmentation of the entire perimacular region,
- superficial point keratitis,
- darkening of eyelashes,
- periorbital erythema,
- allergic conjunctivitis,
- discharge from the eye,
- increased pigmentation of the iris,
- conjunctival edema,
- wrong hair growth.
In rare cases, iritis is possible (intraocular inflammation).
Of all the systemic side effects, most often (approximately 10%) are infection and cold of the upper respiratory tract. There are also exceptions when patients complain of elevated liver enzymes, headache, and asthenic conditions.
Terms and conditions of storage
Stored at a temperature of 2-25 °C, always in a place protected from children.
Eye Care: 5 Common Mistakes
Try not to rub your eyes, although this brings a slight relief: you can easily bring the infection, because your hands are not as clean as it may seem at first glance.
Eye care is a rather serious topic, because vision is one of the most important sense organs. Eyes are necessary for us to live, although there are people who are deprived of the ability to perceive the world through sight.
Many people with complete blindness have been able to adapt to this circumstance. Such people often have more developed other senses.
But most of us would like to maintain our vision in good condition, because it is our eyes that greatly contribute to our physical and intellectual development.
The problem is that our eyes, like other organs, are constantly exposed to various negative factors. Therefore, inadequate eye care can lead to the development of various diseases.
Each of us needs to take care of our eyes and not make mistakes that at first glance do not seem serious, but can harm them. What are these mistakes?
Do not use sunglasses
The use of sunglasses has become a necessary habit to protect our vision.
They protect our eyes from the negative effects of ultraviolet rays. The sun increases the risk of developing cataracts, corneal burns and damage to the conjunctiva.
The effect of ultraviolet rays accumulates over the years: in other words, the negative effects of exposure to the sun can manifest themselves only after a few years.
Therefore, it is important not to neglect wearing sunglasses and choose high quality lenses.
Sleep with contact lenses
Some types of contact lenses do not inconvenience if a person falls asleep in them.
But most lenses are not designed for sleep. When we do not remove the lenses at night, the cornea does not receive the required amount of oxygen, which can lead to its swelling and the appearance of ulcers.
Also, such a habit can provoke the appearance of viral and bacterial infections, because if we do not sterilize contact lenses every day, various microorganisms appear on their surface.
Therefore, even if you use multi-day contact lenses, sleep with them is not recommended. Such a habit significantly increases the risk of eye diseases.
It is best to use the most breathable lenses and pay sufficient attention to their disinfection.
Rub your eyes
The habit of rubbing your eyes over time can lead to unpleasant consequences.
When we burn our eyes, we often have three of their hands. Although this brings relief, such a habit is not at all useful. It can cause eye inflammation and allergies.
Do not forget that our hands are not as clean as it may seem at first glance. On the surface of our fingers and palms there are many harmful microorganisms, which, getting into the eyes, find a favorable environment for reproduction.
Spend a lot of time in front of the screen.
Nowadays, many people tend to spend a lot of time with tablets and smartphones. This trend is directly related to the growth of eye diseases in recent years.
Our eyes are not designed for constant light exposure of these devices, especially when they are located at close range.
Because of such a pastime, we experience visual stress, which is why we have blurred eyes and headaches.
The impact of such light leads to a change in the structure of tissues and increases the risk of developing various diseases.
For their prevention, it is recommended to limit the use of such devices and perform daily visual gymnastics.
Sleep with makeup
The common habit of not removing makeup before bedtime not only hurts our skin, but also adversely affects the health of our eyes.
Chemicals contained in cosmetics, cause skin problems and acne, and also irritate our eyes and cause the appearance of barley.
Pencil, eyeliner and mascara prevent the supply of skin cells with oxygen, which is why our eyes become inflamed and bags and edema appear under them.
It should also be noted that it is not recommended to apply eyeliner to the inner edge of the eyelids, because this is where the Meibomian glands are located, producing a lacrimal secret.
As you can see, if you do not want to have problems with your eyes, these habits are best avoided, no matter how harmless they may seem at first glance.
It is also recommended to be monitored regularly by an oculist. This will help in time to detect problems.