GANFORT EYE DROPS 3ML is a combination medicine of Timolol - a beta blocker agent used in ophthalmology.
Mechanism of Action
GANFORT consists of two active ingredients: bimatoprost and timolol maleate. These two ingredients lower intraocular pressure (IOP) through a complementary and synergistic mechanism of action, resulting in greater reductions in IOP than the individual ingredients. Ganfort quickly springs into action.
Bimatoprost is an effective agent for lowering intraocular pressure. It is a synthetic prostamide, molecularly related to prostaglandin F2α (PGF2α) and acts through the specific prostamide receptor.
Bimatoprost lowers intraocular pressure in humans by increasing drainage of aqueous humor through trabecular meshwork and uvula (via Schlemm's canals).
Timolol is a beta 1 and beta 2 adrenergic receptor blocker (non-selective), with no intrinsic sympatholytic or direct inhibitory effects on myocardial activity, and no anabolic effects. Local sensitization (membrane fixation action). Timolol lowers intraocular pressure by reducing the formation of aqueous humor.
Clinical effects
Bimatoprost lowers intraocular pressure with an IOP-lowering effect that peaks in about 12 hours; Timolol has an eye pressure lowering effect that reaches its peak in about 1-2 hours. Both bimatoprost and timolol significantly reduce intraocular pressure after the first dose.
The intraocular pressure-lowering effect of Ganfort was not less than that of adjuvant therapy with bimatoprost (once/day) and timolol (twice/day).
Some of the available literature on Ganfort suggests that evening administration may be more effective in lowering IOP than morning administration. However, the possibility of adherence should be considered when considering morning or evening doses.
Use in children
The effectiveness and safety of Ganfort in children aged 0 to 18 years has not been established.
Pharmacokinetic properties
Drug Janfort
Plasma concentrations of bimatoprost and timolol were determined in a crossover study comparing monotherapy with Ganfort in healthy subjects. Systemic absorption of each drug is minimal and is not affected by the combination in a single formulation.
In two 12-month studies evaluating systemic absorption, no drug accumulation of individual components was observed.
Bimatoprost
Bimatoprost penetrates well into the human cornea and sclera in vitro. Following ocular administration, systemic exposure to bimatoprost was very low and did not accumulate over time. After instillation of one drop of bimatoprost 0.03% once daily in both eyes for 2 weeks, peak blood concentrations were reached within 10 minutes of instillation and decreased to below the detectable limit (0.025 ng/mL) within 1.5 hours of instillation. The mean values of peak concentration (Cmax) and area under the concentration curve (AUC0-24 h) were similar between day 7 and day 14 at approximately 0.08 ng/mL and 0, respectively. .09 ng • h/ml respectively. This indicates that steady-state drug concentrations are achieved within the first week of dosing.
Bimatoprost is moderately distributed in body tissues, with a constant human volume of distribution of 0.67 l/kg. In human blood, bimatoprost is mainly in plasma. Bimatoprost is approximately 88% bound to plasma proteins.
