Travoprost is a clear, colorless to light yellow viscous liquid. It is very soluble in acetonitrile and ethanol (99.5) but practically insoluble in water.
Optical rotation [α]25 365: +52° to +58° (0.2g, ethanol (99.5), 10 mL, 100 mm).
Chemical name: Isopropyl(5Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-{(1E,3R)-3-hydroxy-4-[3-(trifluoromethyl)phenoxy]but-1-enyl}cyclopentyl)hept-5-enoate.
Molecular formula: C26H35F3O6
Molecular weight: 500.55
Strength: 0.04 mg in 1 mL.
pH: 5.0-6.0.
Osmotic pressure ratio: 0.9-1.1.
Excipients/Inactive Ingredients: Polyoxyethylene hydrogenated castor oil 40, boric acid, propylene glycol, D-sorbitol, 20% polihexanide solution, pH adjuster.
Pharmacology: Bioequivalence study: A partially shielded, parallel-group comparison study was conducted in patients with primary open-angle glaucoma or ocular hypertension. One drop/dose of TRAVOPROST OPHTHALMIC SOLUTION 0.004%W/V or a reference product (ophthalmic solution, 0.004%) was instilled in both eyes once daily for 4 weeks, and the intraocular pressure was measured. When the obtained data (Parameter: a change in the intraocular pressure from the baseline measured at 10:00 in Week 4 of the treatment phase (TRAVOPROST OPHTHALMIC SOLUTION 0.004%W/V: 22.09 ± 2.13 mmHg, Reference product (ophthalmic solution, 0.004%): 21.86 ± 2.25 mmHg) were statistically analyzed using the 95% confidence interval approach, the result was within the acceptable bioequivalent range of ±1.5 mmHg. Thus, these drugs were validated to be biologically equivalent. (See Table 1.)
Click on icon to see table/diagram/image
To be used on open-angle glaucoma and ocular hypertension.
One drop in the affected eye(s) once daily.
Precautions related to Dosage and Administration: The dosage of travoprost should not exceed once daily since it has been shown that more frequent administration may decrease the intraocular pressure lowering effect.
Patients with a history of hypersensitivity to any of the ingredients in this product.
Careful Administration: This product should be administered with special caution in the following patients: (1) Aphakic patients, pseudophakic patients with a torn posterior lens capsule. Macular edema, including cystoid macular edema and the decreased visual acuity associated with macular edema, have been reported.
(2) Patients with intraocular inflammation (iritis/uveitis). Elevated intraocular pressure (IOP) has been reported.
(3) Pregnant, parturient, nursing women. See Use in Pregnancy & Lactation.
Important Precautions: When this product is administered, the color change of the iris or eyelids may occur due to pigmentation (increased melanin); hypertrichosis around eyes may also occur. These changes progress gradually while continuously using this product and stop upon discontinuation of use. The change in eyelid color and periocular hypertrichosis may gradually disappear or subside after discontinuation. On the other hand, it has been reported that the iris color change does not disappear even discontinuation of use. In patients with a multi-colored iris, the iris color change is clearly noticeable; in patients with a mono-colored dark-brown iris (many of the Japanese people), such change has been observed as well. In particular, the treatment of one eye may cause iris color difference between the right and left eyes. With regard to these symptoms, since there is no sufficient long-term data, the patients should be regularly examined by a physician and observed closely. Patients should be fully informed of these symptoms before use. In addition, to prevent or reduce the discoloration of eyelids and periocular hypertrichosis, patients should be instructed to remove the product liquid in case of contact with the eyelids or skin by wiping off or washing the face.
Corneal epithelium disorder (superficial punctate keratitis, filamentary keratitis, corneal erosion) may occur during administration of this product. The patients should be adequately instructed to seek medical attention immediately if the subjective symptoms of eye stinging, itching, and eye pain persist.
This product should be administered with special caution in the patients with angle-closure glaucoma due to an insufficient clinical experience.
Since blurred vision may temporarily occur after administration of the product, patients should be advised to refrain from operating machinery or driving a car until the symptoms recover.
Other Precautions: High frequency of occurring deepening of the eyelid sulcus has been reported in many studies.
Use in the Elderly: In general, elderly patients often have decreased physiological functions; therefore, this product should be administered with caution.
Use in Children: The safety of this product has not been established in low birth-weight infants, neonates, infants, and children (no sufficient clinical data).
Pregnant women: This product should be used in pregnant women or women who may be pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment. [The safety of administration during pregnancy has not been established. In animal studies, teratogenicity was observed when 10 μg/kg per day (250 times the clinical dose*) was intravenously administered to pregnant rats. And, an increase in post implantation losses and a decrease in fetal viability were observed when 1 μg/kg per day (25 times the clinical dose*) was subcutaneously administered to pregnant mice as well as when 10 μg/kg per day (250 times the clinical dose*) was intravenously administered to pregnant rats. In pregnant rabbits, moreover, death of whole embryos/fetuses was observed when 0.1 μg/kg per day (2.5 times the clinical dose*) was intravenously administered or 0.003% ophthalmic solution (equivalent to 10 times the clinical dose a t a dose per body weight) was administered. When 0.12 μg/kg per day (3 times the clinical dose*) or a higher dose was subcutaneously administered to pregnant/lactating rats from Day 7 of pregnancy to Day 21 of lactation, adverse effects (such as increased postnatal mortality, inhibition of neonatal body weight gain, delayed eye opening) were observed in the development and differentiation of offspring. In an experiment conducted by using isolated uterus of rats, dose-dependent uterine contraction occurred in a manner at the concentration (0.3 nmol/L) approximately 6 times higher than the maximum plasma concentration of this product (0.025 ng/mL=0.05 nmol/L) observed in healthy Japanese adults.]
*) Comparison with the dose (0.04 μg/kg per day) calculated assuming that the body weight of the patient is 50 kg, and 1 drop (25 μL) each of 0.004% travoprost solution is instilled in both eyes at a time.
Nursing mothers: Administration of this product should be avoided in breastfeeding mothers. If the use of this product is unavoidable, the patient should discontinue breastfeeding. [An animal study (rat: subcutaneous administration) has shown that the drug is excreted in breast milk.]
Drug-use results surveys to determine the frequency of adverse reactions have not been conducted for this product. Therefore, the frequency of adverse reactions is not known.
Clinically Significant Adverse Reactions: (Frequency unknown)
Iris pigmentation: Since iris pigmentation may occur, patients should be examined regularly. If iris pigmentation occurs, use of this product may be discontinued according to patient's clinical condition.
Other Adverse Reactions: If any of the following symptoms or abnormalities is observed appropriate measures including discontinuation of treatment should be implemented. (See Table 2.)
Click on icon to see table/diagram/image
Precautions Concerning Use: Route of administration: Ophthalmic use only.
Administration: Patients should be instructed to follow the directions as follows: 1) Be careful not to directly touch the eye with the dropper tip while instilling the product.
2) Principally keep the patient in a supine position while instillation, open the eyelid of the affected eye wide, instill this product into the conjunctival sac, close the eyelids for 1 to 5 minutes, and apply gentle pressure to the lacrimal sac before opening the eye.
3) If this product is used with other ophthalmic solution, they should be administered at least 5 minutes apart.
4) If the solution exceeds to the eyelid skin during instilling the product, remove the product by completely wiping off or washing the face.
Precautions for Handling: Stability study: The long-term stability study (25°C, 60% RH, 2 years) of TRAVOPROST OPHTHALMIC SOLUTION 0.004%W/V in the finished package form demonstrated that this product remains stable for 2 years under the usual distribution conditions in the market.
To be stored below 25 °C. Tight container.
Shelf life: 2 years.
S01EE04 - travoprost ; Belongs to the class of prostaglandin analogues. Used in the treatment of glaucoma.
Travoprost Ophthalmic Solution 0.004% w/v eye drops
2.5 mL x 1's
Sign Out
Click on icon to see table/diagram/image
Click on icon to see table/diagram/image
