Gunfort, eye drops 0.3 mg+5 mg/ml 3 ml

Ganfort is a combination medication with bimatoprost and timolol decreasing intraocular pressure (IOP) through a synergistic interaction, resulting in a significantly more pronounced hypotensive effect compared to the effects of each component alone.

Bimatoprost is a synthetic prostamide with a chemical structure similar to prostaglandin F2a (PGF2a). Bimatoprost has no effect on any of the known types of prostaglandin receptors. The hypotensive effect of bimatoprost is achieved by enhancing the outflow of intraocular fluid through the trabecula and through the uveoscleral pathway of the eye.

Timolol is a non-selective beta-adrenoblocker and has no intrinsic sympathomimetic and membrane-stabilizing activity.

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

Indications

Glaucoma, Increased Intraocular Pressure

Reduction of intraocular pressure (IOP) in patients with open-angle glaucoma and intraocular hypertension when local administration of beta-adrenoblockers and prostaglandin analogues is not sufficient.

Active ingredient

Bimatoprost, Timolol

Composition

1 ml of eye drop solution contains:

Active substance

• Bimatoprost 0.3 mg.
• Timolol maleate 6.8 mg.
  • Timolol converted to 5.0 mg.

Excipients

Benzalkonium chloride,

citric acid monohydrate,

sodium hydrophosphate heptahydrate,

sodium chloride,

hydrochloric acid,

sodium hydroxide,

water.

How to take, the dosage

Recommended doses in adults (including elderly patients): 1 drop is instilled into the conjunctival sac of the affected eye once daily in the morning.

If the drug is missed once, it is administered the next day. It is not recommended to exceed the dose of 1 administration once a day. If more than 2 preparations are used, a 5-minute break between each instillation is necessary.

Special Instructions

In the same way as other ophthalmic medications, Gunfort can penetrate the systemic bloodstream.

The symptoms of heart failure should be compensated for before starting Ganforth. Regular monitoring of patients with severe heart failure and determination of heart rate is necessary. There have been reports of cardiovascular and respiratory adverse events with timolol use, including deaths due to bronchospasm in patients with bronchial asthma and, less frequently, from heart failure.

Bsta-adrenoblockers may mask symptoms of hypoglycemia, hyperthyroidism and cause worsening of the course of Prinzmetal angina, severe peripheral and central vascular disorders and arterial hypotension.
In patients with a history of atopic manifestations and severe anaphylactic reactions to various allergens doses of epinephrine (adrenaline), which are usually used to stop anaphylactic reactions, against the background of beta-adrenoblocker use may be ineffective. In patients with mild liver disease or baseline elevated liver enzyme activity of alanine aminotransferase (ALT), aspartate aminotransferase (ACT) and/or total bilirubin, bimatoprost had no effect on liver function during the 4-hour study period over 24 months.

Patients should be advised of possible eyelash growth, increased eyelid pigmentation and iris pigmentation before starting treatment, as these side effects have been established in studies of bimatoprost and Gunfort. Some of the changes may be permanent and may be accompanied by differences between the eyes if the drug was only injected in one eye. Iris pigmentation may remain permanent after withdrawal of Ganforte. After 12 months of treatment with Ganforte iris pigmentation rate was observed in 0.2% of patients. And after 12 months of treatment with bimatoprost alone in the form of eye drops 1.5%, no further increase in the frequency of this effect was observed during the therapy duration of 3 years. Increased iris pigmentation is due to increased production of melanocytes, not simply an increase in their number.

The excipient benzalkonium chloride, a component of Hanfort, may irritate the eye mucosa and change color of soft contact lenses. Contact lenses should be removed before insertion of the drug, they can be put on 15 minutes after instillation. Benzalkonium chloride may cause acute keratitis and/or toxic corneal ulceration. Therefore, the patient’s condition should be monitored during frequent or prolonged treatment with Ganforth in persons with dry eye syndrome and corneal changes.

After opening the bottle, we cannot rule out the possibility of microbial contamination of its contents, which may lead to inflammatory eye lesions. The shelf life of the drug after the first opening of the bottle is 28 days. After this time the vial should be thrown away, even if the solution has not been completely used.

It is recommended that the date of opening of the bottle be written on the carton of the drug.

Impact on driving and operating machinery

Transient visual impairment may occur after administration of the drug, so the patient should wait until full recovery of vision before starting to drive or operate machinery.

Contraindications

• high sensitivity to the drug components;
• airway hyperresponsiveness syndrome, including acute bronchial asthma and history of episodes, severe chronic obstructive pulmonary disease (COPD);
• Sinus bradycardia, grade II and III atrioventricular block, clinically significant heart failure, cardiogenic shock.

With caution: liver and renal function disorders (the drug has not been adequately studied in this category of patients). In patients with risk factors for macular edema (e.g., aphakia, pseudophakia, lens rupture).

In patients with diabetes mellitus (unstable course) and impaired glucose tolerance because the beta-adreno-blocker timolol contained in Ganfort may mask the signs of hypoglycemia. In patients with ocular inflammatory changes, neovascular, inflammatory, closed-angle glaucoma, congenital glaucoma, or narrow-angle glaucoma (no data on efficacy or safety studies).

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Side effects

The incidence of side effects identified in the studies was rated as follows: very common (>1/10), common (>1/100,1/1000,

The following side effects were identified in the clinical studies of Ganforth:

Central nervous system: infrequent – headache;

Visually: very common – conjunctival hyperemia, eyelash growth; common – superficial keratitis, corneal erosion, burning sensation, itching, burning pain in eyes, foreign body sensation, dry mucous membrane of eyes, redness of eyelids, pain in eyes, photophobia, discharge from eyes, visual disturbance, itching of eyelid skin; infrequent – iridocyclitis, irritation of ocular mucosa, conjunctival edema, blepharitis, epiphora, swollen eyelids, painful eyelids, decreased visual acuity, asthenopia, trichiasis; frequency unknown: Cystoid macular edema.

Respiratory system: infrequent – rhinitis;

Skin and subcutaneous fat: frequent – pigmentation of eyelid skin; infrequent – hirsutism.

Other side effects that have been observed with one of the components of the drug and are potentially possible during treatment with Ganforth:

Bimatoprost

Cardiovascular system: increased blood pressure.

General disorders and changes at the site of administration: asthenia, peripheral edema.

An organ of vision: allergic conjunctivitis, cataracts, darkening of eyelashes, increased iris pigmentation, blepharospasm, eyelid retraction, retinal hemorrhage, uveitis.

Laboratory findings: changes in liver enzyme activity.

Timolol

Mental disorders: insomnia, nightmares, decreased libido.

Central nervous system disorders: myasthenia gravis, paresthesia, cerebral ischemia.

As to the organ of vision: decreased corneal sensitivity, diplopia, ptosis, retinal detachment (after surgical treatment), changes in refraction (due to cancellation of therapy with myotic agents in some cases), keratitis.

Hearing and vestibular system disorders: tinnitus.

Cardiovascular system disorders: heart block, cardiac arrest, heart rhythm disorders, loss of consciousness, bradycardia, heart failure, congestive heart failure; decreased blood pressure, pain in the chest, cerebral circulation disorders, intermittent claudication, Raynaud’s syndrome, cold extremities, palpitation.

Respiratory system: bronchospasm (mainly in patients with a history of bronchospasm episodes), dyspnea, cough.

Gastro-intestinal tract: nausea, diarrhea, dyspepsia, dry oral mucosa.

Skin and subcutaneous fatty tissue: alopecia, psoriasis-like rashes, exacerbation of psoriasis.

Musculoskeletal and connective tissue disorders: systemic lupus erythematosus.

Urinary system disorders: Peyronie’s disease.

Others: swelling, chest pain, fatigue.

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Overdose

No cases of overdose have been reported with Ganforth; when administered as eye drops, overdose is unlikely.

Bimatoprost

Inadvertent oral administration of Ganfort may be helpful: No symptoms of toxic effects of bimatoprost at doses up to 100 mg/kg/day were observed in a 2-week oral administration experiment in rats and mice. The dose used in the study, expressed in mg/m, was 70 times greater than the possible dose of bimatoprost when the contents of a bottle of Ganforte were accidentally ingested by a child weighing 10 kg.

Timolol

The following symptoms may occur with timolol overdose: bradycardia, decreased blood pressure, bronchospasm, headache, dizziness, shortness of breath, cardiac arrest. Studies have shown that timolol is not completely excreted by hemodialysis. If overdose occurs, symptomatic therapy is necessary.

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Pregnancy use

Ganfort is contraindicated in children under 18 years of age, pregnant women and during lactation.

Similarities

Tizoptan