|Trade names||Saflutan, Taflotan, Tapros, Zioptan, others|
|Drug class||Prostaglandin analogue|
|Main uses||Open-angle glaucoma, ocular hypertension|
|Side effects||Eye redness, itchiness, eyelash growth, blurry vision|
|Topical (eye drops)|
|Onset of action||2–4 hrs|
|Duration of action||≥ 24 hrs|
|AHFS/Drugs.com||Multum Consumer Information|
|Metabolism||Activation by ester hydrolysis, deactivation by beta oxidation|
|Chemical and physical data|
|Molar mass||452.539 g·mol−1|
|3D model (JSmol)|
Tafluprost, sold under the brand name Zioptan among others, is a medication used to treat open-angle glaucoma and ocular hypertension. It is used as an eye drop. It may be used alone or with other medications.
Common side effects include eye redness, itchiness, eyelash growth, and blurry vision. Other side effects may include iritis and macular edema. It is a prostaglandin analogue which is believed to work by increasing the outflow of aqueous fluid from the eye.
Tafluprost was approved for medical use in the United States in 2012 and Canada in 2014. In the United States it costs about 150 USD per month as of 2021. In Canada it was less cost effective as compared to bimatoprost in 2020.
It is used as one drop once per day of a 0.0015% solution.
The most common side effect is conjunctival hyperemia, which occurs in 4 to 20% of patients. Less common side effects include stinging of the eyes, headache, and respiratory infections. Rare side effects are dyspnoea (breathing difficulties), worsening of asthma, and macular oedema.
Nonsteroidal anti-inflammatory drugs (NSAIDs) can either reduce or increase the effect of tafluprost. Timolol eye drops, a common kind of glaucoma medication, does not negatively interact with this drug.
Mechanism of action
Tafluprost is a prodrug of the active substance, tafluprost acid, a structural and functional analogue of prostaglandin F2α (PGF2α). Tafluprost acid is a selective agonist at the prostaglandin F receptor, increasing outflow of aqueous fluid from the eyes and thus lowering intraocular pressure.
Tafluprost, as a lipophilic ester, easily penetrates the cornea and is then activated to the carboxylic 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.
Tafluprost acid is inactivated by beta oxidation to 1,2-dinortafluprost acid, 1,2,3,4-tetranortafluprost acid, and its lactone, which are subsequently glucuronidated or hydroxylated. The cytochrome P450 liver enzymes play no role in the metabolism.
An analogous pathway (at least up to the tetranor-metabolites) has been found for latanoprost and travoprost.
- "Tafluprost Monograph for Professionals". Drugs.com. Retrieved 20 September 2021.
- Canada, Health (2 July 2014). "Notice: Prescription Drug List (PDL): Multiple additions". www.canada.ca. Retrieved 20 September 2021.
- "Tafluprost Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 20 September 2021.
- "Prostaglandin Analogues for Ophthalmic Use: A Review of Comparative Clinical Effectiveness, Cost-Effectiveness, and Guidelines | CADTH". www.cadth.ca. Retrieved 20 September 2021.
- Tafluprost Professional Drug Facts.
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- 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. PMID 21491995.