Travoprost

500.55

500.55

201-001-2

WJ68R08KX9

C47766

S01EE04|S01ED51|S - Sensory organs

2937500000

96.2

4.1

ethanol solution

1.245±0.06 g/cm3(Predicted)

584.8±50.0 °C(Predicted)

17 °C

1.545

H2O: >16 mg/ml at 25.0°C

−20°C

D20 +14.6° (c = 1.0 in methylene chloride)

UN 1170 3/PG 2

1

11-36/37/38

16-26-36-7

F,Xi

P201, P202, P260, P261, P263, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, P501

H302

|Warning|H302 (13.33%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P263, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 16 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

No cases of overdose have been reported for travoprost. A topical overdose is not likely to occur or to be associated with toxicity. A topical overdose of travoprost may be flushed from the eye(s) with lukewarm water. Treatment of a suspected oral ingestion is symptomatic and supportive. Travoprost has harmful pharmacological effects on pregnancy and/or the fetus/new-born child. Travoprost should not be used during pregnancy unless clearly necessary. The medication subsequently must not be used in women of childbearing age/potential unless adequate contraceptive measures are in place. It is unknown whether travoprost from the eye drops is excreted in human breast milk. Animal studies have shown excretion of travoprost and metabolites in breast milk. The use of travoprost by breast-feeding mothers is not recommended. There are no data on the effects of TRAVATAN on human fertility. Animal studies showed no effect of travoprost on fertility at doses more than 250 times the maximum recommended human ocular dose. Use in patients below the age of 16 years is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use. No overall clinical differences in safety or effectiveness have been observed between elderly and other adult patients. 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) [L514. No dosage adjustment is necessary for these patients.

The binding of travoprost free acid to plasma proteins is moderate at 80% and linear over a 10,000-fold concentration range (0.10 - 100 ng/mL).

Travoprost ophthalmic solution is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Travoprost is also currently indicated for the decrease of elevated intraocular pressure in paediatric patients aged 2 months to < 18 years with ocular hypertension or paediatric glaucoma.|FDA Label|Decrease of elevated intraocular pressure in adult patients with ocular hypertension or open-angle glaucoma (see section 5.1). Decrease of elevated intraocular pressure in paediatric patients aged 3 years to < 18 years with ocular hypertension or paediatric glaucoma.|Decrease of intraocular pressure (IOP) in adult patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to topical beta-blockers or prostaglandin analogues.|Decrease of elevated intraocular pressure in adult patients with ocular hypertension or open-angle glaucoma (see section 5.1).Decrease of elevated intraocular pressure in paediatric patients aged 2 months to < 18 years with ocular hypertension or paediatric glaucoma (see section 5.1).|Treatment of glaucoma|Treatment of glaucoma, Treatment of ocular hypertension

Travoprost, an isopropyl ester prodrug, is a synthetic prostaglandin F2 alpha analog that is rapidly hydrolyzed by esterases in the cornea to its biologically active free acid. The travoprost free acid is potent and highly selective for the FP prostanoid receptor.

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

Travoprost is systemically absorbed through the cornea. In humans, peak plasma concentrations of travoprost free acid were low (25 pg/mL or less) and occurred within 30 minutes following topical ocular administration of one drop of 0.004% travoprost ophthalmic solution.|Less than 2% of the topical ocular dose of travoprost was excreted in the urine within 4 hours as the travoprost free acid. Moreover, elimination from plasma is rapid, resulting in concentrations below the limit of quantitation (< 10 pg/mL) by one hour. Furthermore, in rats, 95% of a subcutaneous radiolabeled dose was eliminated within 24 hours. The major route of elimination was via the bile (61%) with the remainder excreted by the kidneys.|Given the data currently available, it has been recorded that travoprost free acid is moderately distributed into body tissues with a volume of distribution of 2.6 L/kg in rats.|Data regarding the clearance of travoprost is not readily available or accessible.

Travoprost, an isopropyl ester prodrug, is hydrolyzed by esterases in the cornea to its biologically active free acid. Systemically, travoprost free acid is rapidly and extensively metabolized in the kidney, liver, and lung to inactive metabolites via beta-oxidation of the α(carboxylic acid) chain to give the 1,2-dinor and 1,2,3,4-tetranor analogs, via oxidation of the 15-hydroxyl moiety, as well as via reduction of the 13,14 double bond.

The terminal elimination half-life of travoprost free acid is determined to be approximately 45 minutes, although studies demonstrated half-life values that ranged from 17 to 86 minutes.

Travoprost, a prostaglandin F2α analogue, is a highly selective full agonist which has a high affinity for the prostaglandin FP receptor, and facilitates reductions in intraocular pressure by increasing the outflow of aqueous humour via trabecular meshwork and uveoscleral pathways. Reduction of the intraocular pressure in man starts about 2 hours after administration and maximum effect is reached after 12 hours. Significant lowering of intraocular pressure can be maintained for periods exceeding 24 hours with a single dose.

(((1R)-(1alpha(Z),2beta(1E,3R*),3alpha,5alpha))-7-(3,5-dihydroxy-2-(3-hydroxy-4-(3-trifluoromethyl)phenoxy)-1-butenyl)cyclopentyl)-5-heptenoic acid, 1-methylethyl ester

Human drugs -> Izba -> EMA Drug Category|Ophthalmologicals, Antiglaucoma preparations and miotics -> Human pharmacotherapeutic group|Human drugs -> DuoTrav -> EMA Drug Category|Ophthalmologicals -> Human pharmacotherapeutic group|Human drugs -> Travatan -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients