Active substanceBimatoprost + TimololBimatoprost + Timolol
Similar drugsTo uncover
  • Ganfort®
    drops d / eye 
  • Dosage form: & nbspeye drops
    Composition:

    Active substances: bimatoprost 0.3 mg / ml, timolol maleate 6.8 mg / ml (in terms of timolol 5.0 mg / ml).

    Excipients: benzalkonium chloride, citric acid monohydrate, sodium hydrogen phosphate heptahydrate, sodium chloride, hydrochloric acid, sodium hydroxide, water.

    Description:

    A clear, colorless or light yellow solution.

    Pharmacotherapeutic group:antiglaucoma agents combined (prostaglandin F2-alpha analogue synthetic + beta-blocker)
    ATX: & nbsp

    S.01.E.D.51   Timolol in combination with other drugs

    Pharmacodynamics:

    Ganfort® is a combined medicinal product that is part of it bimatoprost and timolol reduce intraocular pressure (IOP) due to the combined interaction, leading to a much more pronounced hypotensive effect in comparison with the effect of each of the components alone.

    Bimatoprost refers to synthetic proteams, the chemical structure is similar to prostaglandin F2α (PGF2α). Bimatoprost has no effect on any of the known types of prostaglandin receptors. The hypotensive effect of bimatoprost is due to increased outflow of intraocular fluid through the trabeculae and the uveoscleral pathway of the eye.

    Timolol - non-selective beta-blocker, does not have internal sympathomimetic and membrane-stabilizing activity.

    Timolol reduces IOP by reducing the formation of intraocular fluid. The exact mechanism of action is not established, it may be associated with inhibition of the synthesis of cyclic adenosine monophosphate (c-AMP) and is caused by endogenous stimulation of beta-adrenergic receptors.

    Pharmacokinetics:

    Ganforth®

    Systemic absorption of the drug is minimal, it does not differ either with combined treatment or with instillation of each component of the drug alone.

    In two studies of 12 months duration, no systemic cumulation of any of the active substances was noted.

    Bimatoprost

    In studies in vitro shown, that bimatoprost penetrates the iris and sclera. When instillating 0.03% bimatoprosta solution, 1 drop in each eye once a day for 2 weeks, the maximum concentration (CmOh) of bimatoprost in blood plasma is reached within 10 minutes after application, and within 1.5 hours its concentration in the blood plasma is reduced to the lower limit of detection (0.025 ng / ml). Mean values FROMmOh and the area under the "concentration-time" curve (AUC0-24h) bimatoprost were close on days 7 and 14, and were 0.08 ng / ml and 0.09 ng * h / ml, respectively, indicating that the equilibrium concentration of bimatoprost was reached within the first week of use.

    Bimatoprost is moderately distributed in tissues, and the systemic volume of distribution when the equilibrium concentration of the drug is reached is 0.67 l / kg. Bimatoprost is mainly in the blood plasma. The association of bimatoprost with plasma proteins is approximately 88%. Bimatoprost is oxidized, N-deleylation and glucuronation with the formation of various metabolites.

    Bimatoprost is excreted mainly by the kidneys. About 67% of the drug, injected intravenously to healthy volunteers, was excreted in the urine, and 25% - through the gastrointestinal tract (GIT). The half-life (T1/2) of bimatoprost, determined after its intravenous administration, was approximately 45 minutes; and the total ground clearance is 1.5 l / h / kg.

    In elderly patients:

    When applying bimatoprost 2 times a day, the mean AUC0-24h in elderly patients is 0.0634 ng * h / ml, which significantly exceeds the value of this parameter in healthy young people - 0.0218 ng * h / ml.

    Nevertheless, this difference is not of clinical importance, since the systemic exposure of bimatoprost in its local application in elderly patients and healthy young people remains very low. Cumulation of bimatoprost in the systemic circulation is not observed, the safety profile is not different in elderly patients and young people.

    Timolol

    In patients who underwent surgical cataract treatment, after instillation of eye drops in the form of a 0.5% solution, CmOh Timolol in the intraocular fluid after 1 h was 898 ng / ml. Some of the drug enters the systemic circulation, and is metabolized in the liver. T1/2 timolol is about 4-6 hours. A part of timolol, subjected to metabolism in the liver, is excreted through the gastrointestinal tract, and the other part and metabolites are excreted by the kidneys. Timolol to a small extent binds to blood plasma proteins.

    Indications:

    Decrease in intraocular pressure (IOP) in patients with open-angle glaucoma and intraocular hypertension with insufficient effectiveness of topical application of beta-adrenoblockers and prostaglandin analogues.

    Contraindications:

    - Hypersensitivity to the components of the drug;

    - a syndrome of increased reactivity of the respiratory tract, including bronchial asthma in the acute stage and previous episodes in history, severe chronic obstructive pulmonary disease (COPD);

    - sinus bradycardia, syndrome of sinus node weakness, sinoauric blockade, atrioventricular blockade of II and III degree without implanted artificial pacemaker, clinically significant heart failure, cardiogenic shock;

    - age to 18 years.

    Carefully:

    - Dysfunction of the liver and kidneys (the drug is not sufficiently studied in this category of patients);

    - in patients with risk factors for edema of the macula (for example, with aphakia, pseudophakia, rupture of the posterior capsule of the lens, as well as intraocular surgery, retinal vein occlusion, inflammatory diseases of the eyes and diabetic retinopathy);

    - in patients with active intraocular inflammation (eg, uveitis), since inflammation can increase;

    - in patients with chronic obstructive pulmonary disease (COPD) of mild and moderate degree, and only in those cases when the expected benefit exceeds possible risk;

    - in patients with atrioventricular blockade I degree due to negative effects on the time of intracardiac conduction;

    - in patients with corneal diseases, since it can induce dry eye syndrome;

    - in patients with diabetes mellitus (unstable flow) and impaired glucose tolerance, because the Ganfort® beta-blocker included in the preparation timolol can mask signs of hypoglycemia;

    - in patients with inflammatory changes in the eyes, neovascular, inflammatory, occlusive glaucoma, congenital glaucoma or narrow-angle glaucoma (no data on efficacy and safety).

    Pregnancy and lactation:

    Adequate data on the use of a fixed combination Bimatoprost / timolol in pregnant women are absent. Ganfort® in pregnancy should be used only when the expected The benefit to the mother exceeds the potential risk to the fetus. Adequate and strictly controlled studies of the drug Ganfort® in pregnant women were not conducted. In animal studies, data on reproductive toxicity were obtained at high doses of bimatoprost.

    Epidemiological studies have not revealed congenital malformations of the fetus,but found the risk of delayed intrauterine development of the fetus when ingesting drugs group of beta-blockers. In those cases when patients took the beta-blocker until the time of delivery, the neonates had clinical symptoms characteristic of this group of drugs (for example, bradycardia, hypotension, respiratory distress syndrome and hypoglycemia). In the case of using the drug Ganfort® up to delivery, it is necessary to monitor the condition of the newborn during the first days of life.

    In animal studies, the reproductive toxicity of timolol is shown in use of doses, significantly exceeding those prescribed in clinical practice. Therefore, Ganfort® is not recommended for use during pregnancy, except in special cases necessity.

    Beta-blockers penetrate into breast milk. However, with the use of timolol in the form of eye drops in therapeutic doses, the development of clinical symptoms in children is unlikely because of the lack of a sufficient amount of the drug in breast milk.

    It is not known whether the bimatoprost in human milk, but it is established,that it is contained in the milk of lactating rats. Ganfort® should not be used in women during breast-feeding.

    Dosing and Administration:

    Recommended doses in adults (including elderly patients)

    One drop is dug into the conjunctival sac of the affected eye once a day 1 in the morning.

    If the administration of the drug is missed once, the drug is administered the next day. Do not exceed the dose - 1 injection once a day.

    If more than 2 drugs are used, it is necessary to take a 5-minute break between each instillation.

    Side effects:

    The frequency of side effects detected during the studies was evaluated as follows: very often (> 1/10), often (> 1/100, <1/10); infrequently (> 1/1000, <1/100).

    In clinical studies of the drug Ganfort®, the following side effects were identified:

    From the central nervous system: often - headache, dizziness.

    From the side of the organ of vision: very often - congestion hyperemia, eyelash growth; often - superficial keratitis, corneal erosion, burning sensation, itching, burning pain in the eyes, foreign body sensation, dry eye mucosa, redness of the eyelids,pain in the eyes, photophobia, discharge from the eyes, impaired vision, itchy eyelid skin, decreased visual acuity, blepharitis, eyelid edema, irritation of the eye mucosa, epiphora; infrequently - iridocyclitis, edema of the conjunctiva, tenderness of the eyelids, asthenopia, trichiasis, hyperpigmentation of the iris, deepening of the fold of the eyelid, refraction of the eyelid; frequency unknown -cystoid macular edema.

    From the respiratory system: often - rhinitis; infrequently - dyspnea; frequency unknown - bronchospasm (mainly in patients with existing bronchospastic disease).

    From the skin and subcutaneous fat; often - skin pigmentation lawsuit, hirsutism, periocular hyperpigmentation skin.

    Other side effects that were observed with the use of one of the components of the drug and potentially possible during the period of treatment with Ganfort®:

    Bimatoprost

    Infectious and parasitic diseases: infectious disease (catarrhal symptoms and symptoms of upper respiratory tract infection).

    From the side of the organ of vision: allergic conjunctivitis, cataract, darkening of eyelashes, blepharospasm, retinal hemorrhage, uveitis, periorbital erythema, blurred vision.

    From the cardiovascular system: increase in blood pressure.

    General violations and changes in the place of introduction: asthenia, peripheral edema.

    From the gastrointestinal tract: nausea.

    Laboratory indicators: changes in the activity of liver enzymes.

    Timolol

    From the immune system: systemic allergic reactions, including Quincke's edema, hives, focal and multiple rashes, itching, anaphylaxis.

    From the side of metabolism and nutrition: hypoglycemia.

    Mental disorders: insomnia, depression, nightmarish dreams, memory loss.

    From the central nervous system: syncope, acute impairment of cerebral circulation, increased symptoms of myasthenia gravis gravis, paresthesia, ischemia of the brain.

    From the side of the organ of vision: decreased sensitivity of the cornea, diplopia, ptosis, detachment of the choroid (after operative treatment of glaucoma), keratitis, blurring of vision.

    From the organ of hearing and the vestibular apparatus: noise in ears.

    From the cardiovascular system: atrioventricular blockade, cardiac arrest, heart rhythm disturbances, loss of consciousness, bradycardia, cardiac insufficiency, congestive heart failure; decline arterial pressure, pain in a difficult cage, cerebrovascular accident, intermittent claudication, Raynaud's syndrome, cold extremities, palpitations, swelling.

    From the respiratory system: bronchospasm (mainly in limes with episodes of bronchospasm in the anamnesis), dyspnea, cough.

    From the gastrointestinal tract: perversion of taste, nausea, diarrhea, indigestion, dryness of the oral mucosa, abdominal pain, vomiting.

    From the skin and subcutaneous fat: alopecia, psoriasis-like rashes, exacerbation of psoriasis, skin rash.

    From the side of the musculoskeletal system and connective tissue: systemic lupus erythematosus, pain in the muscles.

    From the urinary system: Peyronie's disease.

    From the reproductive system and the breast: sexual dysfunction, decreased libido.

    Others: asthenia / utomlavailability.

    Overdose:

    No cases of overdose of Ganfort® were reported; When administered in the form of eye drops, an overdose is unlikely.

    Bimatoprost

    When unintentionally taking Ganfor® inside, the following information can be helpful: There were no symptoms of toxic effects of bimatoprost in doses up to 100 mg / kg / day during a 2-week oral administration in an experiment in rats and mice.The dose applied in the study, expressed in mg / m2, exceeds by 70 times the possible dose of bimatoprost with accidental ingestion of the contents of the bottle of the drug Ganfort® with a child weighing 10 kg.

    Timolol

    When an overdose of timolol, the following symptoms can occur: bradycardia, lowering of blood pressure, bronchospasm, headache, dizziness, dyspnea, cardiac arrest. In studies it is shown that timolol is not completely excreted by hemodialysis.

    If an overdose occurs, symptomatic therapy is necessary.

    Interaction:

    Special studies on the study of drug interaction fixed combination Bimatoprost / timolol was not performed.

    Possible potentiation of effects of joint application ophthalmic solutions of beta-blockers and in-blockers of "slow" calcium channels, guanethidine, beta-adrenoblockers, parasympathomimetics, antiarrhythmic drugs (including amiodarone) and cardiac glycosides, which was manifested by a decrease in blood pressure and / or pronounced bradycardia.

    Potential effects of beta-blocker systemic effects (eg, heart rate reduction, depression) have been reported with the simultaneous use of timolol with CYP2D6 inhibitors (quinidine, fluoxetine, paroxetine).

    Periodically reported cases of mydriasis with the simultaneous use of ophthalmic beta-blockers and adrenaline (epinephrine).

    Patients using Ganfort® with other prostaglandin analogues should be monitored to monitor the change intraocular pressure.

    Very rarely reported cases of calcification of the cornea when combined with phosphate-containing eye drops in some patients with significant damage cornea.

    Special instructions:

    Just like other ophthalmic drugs, Ganfort® can enter the systemic circulation. Due to the presence of timolol, the beta-adrenergic component, various types of adverse reactions (from the cardiovascular and respiratory system), as with systemic beta-blockers, can be observed. Frequency of occurrence of undesirable reactions with local administration of the drug is lower than with systemic administration.

    The cardiovascular system

    Symptoms of the heart Deficiencies should be compensated before the use of the Ganfort® drug. It is necessary to regularly monitor the condition of patients with severe heart failure, determination of heart rate.

    Beta-adrenoblockers can mask symptoms hypoglycemia, hyperthyroidism and cause a deterioration in the course of Prinzmetal angina, severe peripheral and central vascular disorders, as well as arterial hypotension.

    Patients with severe peripheral disorders blood circulation (eg, severe forms of Raynaud's disease or Raynaud's syndrome), the drug should be used with caution.

    Respiratory system

    When using timolol, there were reports of side effects from the respiratory organs, including deaths due to bronchospasm in patients bronchial asthma, and also less often - from heart failure.

    Other beta-blockers

    Timolol may affect intraocular pressure or increase the effect of systemic beta-blockers in patients already receiving a systemic beta-blocker.

    A thorough observation of such patients.Also, the use of two local beta-blockers is not recommended.

    Anaphylactic reactions

    In patients with atopic manifestations in the history and severe anaphylactic reactions to various allergens, the doses of epinephrine (adrenaline), which are commonly used for relief of anaphylactic reactions, against the background of the use of beta-blockers may be ineffective.

    Choroidal detachment

    There have been reports of cases of choroidal detachment with the use of therapy that reduces the flow of intraocular fluid (eg, timolol, acetazolamide) after filtration surgery.

    Surgical anesthesia

    Ophthalmic preparations with β-blocking action can suppress systemic effects of β-agonists, for example, adrenaline. It is necessary to warn the anesthesia doctor about the use of a patientthymolol.

    Liver

    In patients with liver disease of the lung, or initially increased activity of liver enzymes - alanine aminotransferase (ALT), aspartate aminotransferase (ACT) and / or total bilirubin, bimatoprost had no effect on liver function during the study period lasting more than 24 months. Data on unwanted reactions due to influence timolol on liver function are absent.

    Body of sight

    Before starting treatment of patients information on the possible growth of eyelashes, increased pigmentation of the skin of the eyelids and pigmentation of the iris of the eyes, since these side effects are established in the course of studies of bimatoprost and the preparation Ganfort®. Some changes may be permanent and may be accompanied by the appearance of a difference between the eyes, if the instillations of the drug were carried out only in one eye. After the cannabis preparation is canceled, the pigmentation of the iris may remain constant. After 12 months of treatment with Ganfort®, the iris and pigmentation pigmentation frequency was noted in 0.2% of patients. And after 12 months of treatment, only bimatoprostom in the form of eye drops 1.5%, further increase in the frequency of this effect was not observed during therapy duration of 3 years. The increase in pigmentation of the iris is due to the increased production of melanocytes, and not simply by the increase in their number. The duration of the development of the effect of enhancing the pigmentation of the iris is unknown.The change in the color of the iris seen in the application of bimatoprost may not be expressed in the period from several months to several years. The use of the drug has no effect on nevi or pigment deposition on the iris of the eye. It was reported that the pigmentation of the periorbital region in some patients is reversible. Perhaps a change in refraction (due to the abolition of therapy with mystical means in individual cases).

    Leather

    It is possible to grow hair on those parts of the skin that are accidentally applied to the drug. It is important to apply the drug Ganfort® strictly in accordance with the instructions for medical use and to prevent the drug Ganfort® on the skin.

    Excipients

    Excipient Benzalkonium chloride, which is part of the preparation Ganfort®, can cause irritation of the mucous membrane of the eyes and change the color of soft contact lenses. Contact lenses must be removed before the drug is administered, they can be dressed 15 minutes after instillation. Benzalkonium chloride can cause acute keratitis and / or toxic corneal ulcer.In this regard, it is necessary to monitor the condition of the patient with frequent or prolonged treatment Ganfort® in individuals with dry eye syndrome and corneal changes.

    After opening the vial, it is impossible to exclude the possibility of microbial contamination of its contents, which can lead to inflammatory lesions of the eyes.

    The shelf life of the drug after the first opening of the bottle is 28 days. After the specified time, the vial should be discarded, even if the solution is not completely used.

    It is recommended to record the date of opening the vial on a cardboard packet of the drug.

    Effect on the ability to drive transp. cf. and fur:

    There may be a transient visual impairment after the administration of the drug, so the patient must wait until the vision is fully restored before proceeding to driving the car or controlling the mechanisms.

    Form release / dosage:Eye drops, 0.3 mg / ml + 5 mg / ml.
    Packaging:

    To 3.0 ml of the drug in a dropper bottle of white low-density polyethylene with a capacity of 5 ml with a screw cap made of impact-resistant polystyrene, which is sealed with a polymer film.

    For 1 or 3 vials, along with the instructions for use are placed in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007278/10
    Date of registration:28.07.2010
    The owner of the registration certificate:Allergen Pharmaceuticals AirlandAllergen Pharmaceuticals Airland Ireland
    Manufacturer: & nbsp
    Representation: & nbspAllergen of CIS SARL. LtdAllergen of CIS SARL. LtdRussia
    Information update date: & nbsp22.11.2015
    Illustrated instructions
      Instructions
      Up