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Travoprost
0.004%
Timolol
0.5%
Tovaxo T is indicated for the treatment of Glaucoma & ocular hypertension
Travoprost free acid is a highly selective FP prostanoid receptor agonist that has been shown to reduce IOP by increasing uveoscleral and conventional outflow. Reduction of IOP starts within approximately two hours after administration, and the maximum effect is reached after 12 hours. Significant lowering of IOP can be maintained for periods exceeding 24 hours with a single dose. Repeated observations over a period of one year indicate that the IOP- lowering effect of travoprost is well maintained. Timolol maleate is a beta1 and beta2 (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anaesthetic (membrane-stabilizing) activity. The precise mechanism of the ocular hypotensive action of timolol is not definitively established. Tonography and fluorophotometry studies in man suggest that its predominant action is related to reduced aqueous humour formation.
Travoprost Absorption Travoprost is an ester prodrug. It is absorbed through the cornea where the isopropyl ester is hydrolysed to the active free acid. Studies in rabbits have shown peak concentrations of 20 ng/mL of the free acid in aqueous humour one to two hours after topical dosing. Aqueous humour concentrations declined with a half-life of approximately 1.5 hours. Distribution Following topical ocular administration to healthy volunteers, low systemic exposure to active free acid was demonstrated. Peak active free acid plasma concentrations of 25 pg/mL or less were observed between 10 and 30 minutes post-dose. Thereafter, plasma levels declined rapidly to below the 10 pg/mL assay quantitation limit before 1 hour post-administration. Due to the low plasma concentrations and rapid elimination following topical dosing, the elimination half-life of active free acid in man could not be determined. Biotransformation Metabolism is the major route of elimination of both travoprost and the active free acid. The systemic metabolic pathways parallel those of endogenous prostaglandin F2α which are characterised by reduction of the 13-14 double bond, oxidation of the 15-hydroxyl and β-oxidative cleavages of the upper side chain. Elimination Travoprost free acid and its metabolites are mainly excreted by the kidneys.Travoprost has been studied in patients with mild to severe hepatic impairment and in patients with mild to severe renal impairment (creatinine clearance as low as 14 ml/min). No dosage adjustment is necessary in these patients. Timolol Absorption The onset of reduction in intra-ocular pressure can be detected within one-half hour after a single dose. The maximum effect occurs in one or two hours; significant lowering of IOP can be maintained for as long as 24 hours with a single dose. In some cases, a decreased therapeutic effect has been observed in long-term treatment.
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