Tafluprost
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| Clinical data | |
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| Trade names | Saflutan, Taflotan, Zioptan |
| AHFS/Drugs | Multum Consumer Information |
| Routes of administration | Topicaleye drops |
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| Pharmacokineticdata | |
| Metabolism | Activation by esterhydrolysis,deactivation bybeta oxidation |
| Onset of action | 2–4 hrs |
| Duration of action | ≥ 24 hrs |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.207.745 |
| Chemical and physical data | |
| Formula | C25H34F2O5 |
| Molar mass | 452.539g·mol−1 |
| 3D model (JSmol) | |
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Tafluprost(trade namesTaflotanbySanten Pharmaceutical,Zioptanby Merck in the US andSaflutanby Mundipharma in Australia) is aprostaglandin analogue.It is used topically (aseye drops) to control the progression ofopen-angle glaucomaand in the management ofocular hypertension,alone or in combination with other medication. It reducesintraocular pressureby increasing the outflow ofaqueous fluidfrom the eyes.[2][3]
Adverse effects
[edit]The most common side effect isconjunctival hyperemia,which occurs in 4 to 20% of patients. Less common side effects include stinging of the eyes, headache, andrespiratory infections.Rare side effects aredyspnoea(breathing difficulties), worsening ofasthma,andmacular oedema.[2][3][4]
Interactions
[edit]Nonsteroidal anti-inflammatory drugs(NSAIDs) can either reduce or increase the effect of tafluprost.[2]Timololeye drops, a common kind of glaucoma medication, does not negatively interact with this drug.[3]
No interactions with systemic (for example, oral) drugs are expected because tafluprost does not reach relevant concentrations in the bloodstream.[3][4]
Pharmacology
[edit]Mechanism of action
[edit]Tafluprost is aprodrugof the active substance, tafluprost acid, astructuralandfunctional analogueofprostaglandin F2α(PGF2α). Tafluprost acid is a selectiveagonistat theprostaglandin F receptor,increasing outflow of aqueous fluid from the eyes and thus lowering intraocular pressure.[3][4]
Other PGF2αanalogues with the same mechanism includelatanoprostandtravoprost.[3]
Pharmacokinetics
[edit]Tafluprost, as alipophilicester,easily penetrates thecorneaand is then activated to thecarboxylic acid,tafluprost acid. Onset of action is 2 to 4 hours after application, the maximal effect is reached after 12 hours, and ocular pressure remains lowered for at least 24 hours.[3][4]
Tafluprost acid is inactivated bybeta oxidationto 1,2-dinortafluprost acid, 1,2,3,4-tetranortafluprost acid, and itslactone,which are subsequentlyglucuronidatedorhydroxylated.Thecytochrome P450liver enzymes play no role in the metabolism.[4]
An analogous pathway (at least up to the tetranor-metabolites) has been found for latanoprost and travoprost.
References
[edit]- ^"Product monograph"(PDF).hres.ca.Retrieved6 April2024.
- ^abcTafluprostProfessional Drug Facts.
- ^abcdefgHaberfeld H, ed. (2015).Austria-Codex(in German). Vienna: Österreichischer Apothekerverlag.
- ^abcdeDinnendahl V, Fricke U, eds. (2011).Arzneistoff-Profile(in German). Vol. 9 (25 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag.ISBN978-3-7741-9846-3.
- ^Fukano Y, Kawazu K (August 2009). "Disposition and metabolism of a novel prostanoid antiglaucoma medication, tafluprost, following ocular administration to rats".Drug Metabolism and Disposition.37(8): 1622–34.doi:10.1124/dmd.108.024885.PMID19477946.S2CID12425702.
- ^Fukano Y, Kawazu K, Akaishi T, Bezwada P, Pellinen P (June 2011). "Metabolism and ocular tissue distribution of an antiglaucoma prostanoid, tafluprost, after ocular instillation to monkeys".Journal of Ocular Pharmacology and Therapeutics.27(3): 251–9.doi:10.1089/jop.2010.0178.PMID21491995.