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Risk first

Contraindications

Hypersensitivity to the active substance or excipients.
Additional absolute contraindications are indication- and product-specific — consult SmPC.

Precautions

5 WARNINGS AND PRECAUTIONS • Pigmentation: Pigmentation of the iris, periorbital tissue (eyelid), and eyelashes can occur.
Iris pigmentation likely to be permanent.
( 5.1 ) • Eyelash Changes: Gradual change to eyelashes including increased length, thickness and number of lashes.
Usually reversible.
( 5.2 ) 5.1 Pigmentation Travoprost ophthalmic solution has been reported to cause changes to pigmented tissues.
The most frequently reported changes have been increased pigmentation of the iris, periorbital tissue (eyelid), and eyelashes.
Pigmentation is expected to increase as long as travoprost is administered.
The pigmentation change is due to increased melanin content in the melanocytes rather than to an increase in the number of melanocytes.
After discontinuation of travoprost, pigmentation of the iris is likely to be permanent, while pigmentation of the periorbital tissue and eyelash changes have been reported to be reversible in some patients.
Patients who receive treatment should be informed of the possibility of increased pigmentation.
The long-term effects of increased pigmentation are not known.
Iris color change may not be noticeable for several months to years.

Point of care

Dosing

Adult

2 DOSAGE AND ADMINISTRATION The recommended dosage is one drop in the affected eye(s) once daily in the evening. Travoprost ophthalmic solution (ionic buffered solution) should not be administered more than once daily since it has been shown that more frequent administration of prostaglandin analogs may decrease the IOP lowering effect. Reduction of the IOP starts approximately 2 hours after the first administration with maximum effect reached after 12 hours. Travoprost ophthalmic solution (ionic buffered solution) may be used concomitantly with other topical ophthalmic drug products to lower IOP. If more than one topical ophthalmic drug is being used, the drugs should be administered at least 5 minutes apart. One drop in the affected eye(s) once daily in the evening. ( 2 )

Paediatric

8.4 Pediatric Use Use in pediatric patients below the age of 16 years is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use.

Renal

Review renal impairment dosing; many agents need CrCl/eGFR adjustment.

CrCl 0–120: Confirm renal dosing in product SmPC / primary label.

Hepatic

Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.

Safety

Drug interactions

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Professional use: confirm indication, dose, duration, monitoring and patient counselling points against current Kenya STG / EML and the product SmPC.
Document allergy status and key interactions.

Safety

Adverse effects

(30% to 50%) is conjunctival hyperemia.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Viatris at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The most common adverse reaction observed in controlled clinical trials with travoprost ophthalmic solution 0.004% was ocular hyperemia, which was reported in 30% to 50% of patients.
Up to 3% of patients discontinued therapy due to conjunctival hyperemia.
Ocular adverse reactions reported at an incidence of 5% to 10% in these clinical trials included decreased visual acuity, eye discomfort, foreign body sensation, pain, and pruritus.
Ocular adverse reactions reported at an incidence of 1% to 4% in clinical trials with travoprost ophthalmic solution 0.004% included abnormal vision, blepharitis, blurred vision, cataract, conjunctivitis, corneal staining, dry eye, iris discoloration, keratitis, lid margin crusting, ocular inflammation, photophobia, subconjunctival hemorrhage, and tearing.
Non-ocular adverse reactions reported at an incidence of 1% to 5% in these clinical studies were allergy, angina pectoris, anxiety, arthritis, back pain, bradycardia, bronchitis, chest pain, cold/flu syndrome, depression, dyspepsia, gastrointestinal disorder, headache, hypercholesterolemia, hypertension, hypotension, infection, pain, prostate disorder, sinusitis, urinary incontinence, and urinary tract infections. 6.2 Postmarketing Experience Additional adverse reactions have been identified during post approval use of travoprost ophthalmic solution 0.004% in clinical practice.
Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made.
The reactions, which have been chosen for inclusion due to either their seriousness, frequency of reporting, possible causal connection to travoprost, or a combination of these factors, include: arrhythmia, vomiting, epistaxis, tachycardia, and insomnia.
In postmarketing use with prostaglandin analogs, periorbital and lid changes including deepening of the eyelid sulcus have been observed.

Use

Indications

(ionic buffered solution) 0.004% is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.
Travoprost ophthalmic solution (ionic buffered solution) is a prostaglandin analog indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.

Pharmacology

Mode of action

12.

1 Mechanism of Action Travoprost free acid… → The exact mechanism of action is unknown a…

Full mechanism text

12.1 Mechanism of Action Travoprost free acid, a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce IOP by increasing uveoscleral outflow. The exact mechanism of action is unknown at this time.

ADME

Pharmacokinetics & PD

Onset	Product-specific
Duration	Product-specific
Route	OPHTHALMIC
Elimination	of travoprost free acid from plasma was rapid and levels were generally below the limit of quantification within one hour after dosing. The terminal elimination
Half-life	of 45 minutes. There was no difference in plasma concentrations between Days 1 and 7, indicating steady-state was reached early and that there was no significant accumulation. Travoprost, an isopropyl ester prodrug, is hydrolyzed by esterases in the cornea to its biologically act...

Full PK/PD text

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Travoprost free acid, a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce IOP by increasing uveoscleral outflow. The exact mechanism of action is unknown at this time. 12.3 Pharmacokinetics Travoprost is absorbed through the cornea and is hydrolyzed to the active free acid. Data from 4 multiple dose pharmacokinetic studies (totaling 107 subjects) have shown that plasma concentrations of the free acid are below 0.01 ng/mL (the quantitation limit of the assay) in two-thirds of the subjects. In those individuals with quantifiable plasma concentrations (N = 38), the mean plasma C max was 0.018 ± 0.007 ng/mL (ranged 0.01 to 0.052 ng/mL) and was reached within 30 minutes. From these studies, travoprost is estimated to have a plasma half-life of 45 minutes. There was no difference in plasma concentrations between Days 1 and 7, indicating steady-state was reached early and that there was no significant accumulation. Travoprost, an isopropyl ester prodrug, is hydrolyzed by esterases in the cornea to its biologically active free acid. Systemically, travoprost free acid is metabolized 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 elimination of travoprost free acid from plasma was rapid and levels were generally below the limit of quantification within one hour after dosing. The terminal elimination half-life of travoprost free acid was estimated from fourteen subjects and ranged from 17 minutes to 86 minutes with the mean half-life of 45 minutes. Less than 2% of the topical ocular dose of travoprost was excreted in the urine within 4 hours as the travoprost free acid.

Kenya

Brands & prices

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Special populations

Pregnancy & lactation

Pregnancy

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies in pregnant women to inform a drug-associated risk. In animal reproduction studies, subcutaneous (SC) administration of travoprost to pregnant mice and rats throughout the period of organogenesis produced embryo-fetal lethality, spontaneous abortion, and premature delivery at potentially clinically relevant doses. Advise pregnant women of a potential risk to a fetus. Because animal reproductive studies are not always predictive of human response, travoprost should be administered during pregnancy only if the potential benefit justifies the potential risk to the fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown; however, in the U.S. general population, the estimated background risk of major birth defects is 2% to 4% and of miscarriage is 15% to 20% of clinically recognized pregnancies. Data Animal Data An embryo-fetal study was conducted in pregnant rats administered travoprost once daily by SC injection from gestation day (GD) 6 to 18, to target the period of organogenesis. At 10 mcg/kg (60 times the maximum recommended human ocular dose [MRHOD], based on estimated plasma C max ), travoprost was teratogenic in rats, evidenced by an increase in the incidence of skeletal malformations as well as external and visceral malformations, including fused sternebrae, domed head and hydrocephaly. Travoprost caused post-implantation loss at 10 mcg/kg. The no observed adverse effect level (NOAEL) for post-implantation loss was 3 mcg/kg (18 times the MRHOD, based on estimated plasma C max ). The maternal NOAEL was 10 mcg/kg. An embryo-fetal study was conducted in pregnant mice administered travoprost once daily by SC injection from GD 6 to 11, to target the period of organogenesis. At 1 mcg/kg (6 times the MRHOD, based on estimated plasma C max ), travoprost caused postimplantation loss and decreased fetal weight. The no observed adverse effect level (NOAEL) for malformations was 0.3 mcg/kg (2 times the MRHOD, based on estimated plasma C max ). The maternal NOAEL was 1 mcg/kg. Pre/postnatal studies were conducted in rats administered travoprost once daily by subcutaneous injection from GD 7 (early embryonic period) to postnatal Day 21 (end of lactation period). At doses of greater than or equal to 0.12 mcg/kg/day (0.7 times the MRHOD, based on estimated plasma C max ), adverse pregnancy outcomes (embryo-fetal lethality, abortion, and early delivery), low-birth weight and developmental delays were observed. The NOAEL for adverse pregnancy outcomes, low-birth weight and developmental delay was 0.1 mcg/kg (0.6 times the MHROD, based on estimated plasma C max ). The NOAEL for maternal toxicity was 0.72 mcg/kg (4 times the MHROD, based on estimated plasma C max ).

Lactation

16 years is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use. ( 8.4 ) 8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies in pregnant women to inform a drug-associated risk. In animal reproduction studies, subcutaneous (SC) administration of travoprost to pregnant mice and rats throughout the period of organogenesis produced embryo-fetal lethality, spontaneous abortion, and premature delivery at potentially clinically relevant doses. Advise pregnant women of a potential risk to a fetus. Because animal reproductive studies are not always predictive of human response, travoprost should be administered during pregnancy only if the potential benefit justifies the potential risk to the fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown; however, in the U.S. general population, the estimated background risk of major birth defects is 2% to 4% and of miscarriage is 15% to 20% of clinically recognized pregnancies. Data Animal Data An embryo-fetal study was conducted in pregnant rats administered travoprost once daily by SC injection from gestation day (GD) 6 to 18, to target the period of organogenesis. At 10 mcg/kg (60 times the maximum recommended human ocular dose [MRHOD], based on estimated plasma C max ), travoprost was teratogenic in rats, evidenced by an increase in the incidence of skeletal malformations as well as external and visceral malformations, including fused sternebrae, domed head and hydrocephaly. Travoprost caused post-implantation loss at 10 mcg/kg. The no observed adverse effect level (NOAEL) for post-implantation loss was 3 mcg/kg (18 times the MRHOD, based on estimated plasma C max ). The maternal NOAEL was 10 mcg/kg. An embryo-fetal study was conducted in pregnant mice administered travoprost once daily by SC injection from GD 6 to 11, to target the period of organogenesis. At 1 mcg/kg (6 times the MRHOD, based on estimated plasma C max ), travoprost caused postimplantation loss and decreased fetal weight. The no observed adverse effect level (NOAEL) for malformations was 0.3 mcg/kg (2 times the MRHOD, based on estimated plasma C max ). The maternal NOAEL was 1 mcg/kg. Pre/postnatal studies were conducted in rats administered travoprost once daily by subcutaneous injection from GD 7 (early embryonic period) to postnatal Day 21 (end of lactation period). At doses of greater than or equal to 0.12 mcg/kg/day (0.7 times the MRHOD, based on estimated plasma C max ), adverse pregnancy outcomes (embryo-fetal lethality, abortion, and early delivery), low-birth weight and developmental delays were observed. The NOAEL for adverse pregnancy outcomes, low-birth weight and developmental delay was 0.1 mcg/kg (0.6 times the MHROD, based on estimated plasma C max ). The NOAEL for maternal toxicity was 0.72 mcg/kg (4 times the MHROD, based on estimated plasma C max ). 8.2 Lactation Risk Summary There are no data on the effects of travoprost on the breastfed child or milk production. It is not known if travoprost is present in human milk following ophthalmic administration. A study in lactating rats demonstrated that radio-labeled travoprost and/or its metabolites were excreted in milk following subcutaneous administration. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for travoprost ophthalmic solution 0.004% and any potential adverse effects on the breast-fed child from travoprost ophthalmic solution 0.004%. 8.4 Pediatric Use Use in pediatric patients below the age of 16 years is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use. 8.5 Geriatric Use No overall clinical differences in safety or effectiveness have been observed between elderly and other adult patients. 8.6 Hepatic and Renal Impairment Travoprost ophthalmic solution 0.004% has been studied in patients with hepatic impairment and also in patients with renal impairment. No clinically relevant changes in hematology, blood chemistry, or urinalysis laboratory data were observed in these patients.

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Sources & disclaimer

Source: Local active-ingredient clinical extract; FDA drug label via OpenFDA/DailyMed; Professional class pharmacology (Therapeutic agent (verify pharmacological class))

Open source link

Clinical review date not recorded.

Decision support only — not a substitute for clinical judgment, product SmPC, or Kenya STG/EML.