Travoprost

Travoprost
Clinical data
Trade names Travatan
AHFS/Drugs.com Monograph
MedlinePlus a602027
License data
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		 Topical (eye drops)
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Metabolism Activation by ester hydrolysis, deactivation by beta oxidation, OH-oxidation, double bond reduction
    Onset of action 2 hours
    Elimination half-life 1.5 hours (in aqueous fluid)
    45 minutes (terminal)
    Duration of action ≥ 24 hours
    Excretion Mainly via kidney
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    ECHA InfoCard 100.207.141 Edit this at Wikidata
    Chemical and physical data
    Formula C26H35F3O6
    Molar mass 500.548 g/mol
    3D model (JSmol)
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    Travoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a synthetic prostaglandin analog (or more specifically, an analog of prostaglandin F2α)[1][2] that works by increasing the outflow of aqueous fluid from the eyes.[3] It is also known by the brand names of Travatan and Travatan Z, manufactured by Alcon.

    Side effects

    Possible side effects are:[4]

    • blurred vision
    • eyelid redness
    • permanent darkening of eyelashes
    • eye discomfort
    • permanent darkening of the iris to brown (heterochromia)
    • burning sensation during use
    • thickening of the eyelashes
    • inflammation of the prostate gland, restricting urine flow (BPH)

    Research suggests that wiping the eye with an absorbent pad after the administration of eye drops can result in shorter eyelashes and a lesser chance of hyperpigmentation in the eyelid, compared to not wiping off excess fluid.[5]

    Pharmacology

    Mechanism of action

    Like other analogs of prostaglandin F2α such as tafluprost and latanoprost, travoprost is an ester prodrug of the free acid, which acts as an agonist at the prostaglandin F receptor, increasing outflow of aqueous fluid from the eye and thus lowering intraocular pressure.[4]

    Pharmacokinetics

    Travoprost is absorbed through the cornea, where it is hydrolysed to the free travoprost acid. Highest concentrations of the acid in the eye are reached one to two hours after application, and its half-life in the aqueous fluid is 1.5 hours. Once it reaches the bloodstream, it is quickly metabolised, so that concentrations in the system do not exceed 25 pg/ml (compared to 20 ng/ml in the eye, which is higher by nearly a factor of 1000).[4]

    Metabolites are formed by beta oxidation of the acidic chain (compare Tafluprost#Pharmacokinetics), oxidation of the OH-group in the other side chain, and reduction of the double bond next to this OH-group. Travoprost acid and its metabolites are mainly excreted via the kidney[4] with a terminal half-life of 45 minutes.[6]

    One 2.5 ml dropperette of Travatan

    References

    1. ↑ Alcon Laboratories, Inc. (September 2011). "Travatan - travoprost solution". DailyMed. Bethesda, MD: U.S. National Library of Medicine. Retrieved 2011-09-30.
    2. ↑ Alcon Laboratories, Inc. (September 2011). "Travatan Z (travoprost) solution". DailyMed. Bethesda, MD: U.S. National Library of Medicine. Retrieved 2011-09-30.
    3. ↑ AHFS Consumer Medication Information (2011-01-01). "Travoprost Ophthalmic". MedlinePlus. Bethesda, MD: U.S. National Library of Medicine. Retrieved 2011-09-30.
    4. 1 2 3 4 Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Travatan 40 Mikrogramm/ml Augentropfen.
    5. ↑ Xu L, Wang X, Wu M (2017). "Topical medication instillation techniques for glaucoma". Cochrane Database Syst Rev. 2: CD010520. doi:10.1002/14651858.CD010520.pub2. PMC 5419432. PMID 28218404.
    6. ↑ Drugs.com: Travoprost Monograph.
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