| 词条 | Tafluprost |
| 释义 |
| IUPAC_name = Isopropyl (5Z)-7- | image = Tafluprost_structure.svg | tradename = Saflutan, Taflotan, Tapros, Zioptan | Drugs.com = {{drugs.com|MTM|tafluprost-ophthalmic}} | pregnancy_AU = | pregnancy_US = C | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Rx-only | legal_status = | routes_of_administration = Topical (eye drops) | bioavailability = | protein_bound = | metabolism = Activation by ester hydrolysis, deactivation by beta oxidation | metabolites = | onset = 2–4 hrs | elimination_half-life = | duration_of_action = ≥ 24 hrs | excretion = | CAS_number = 209860-87-7 | ATC_prefix = S01 | ATC_suffix = EE05 | ATC_supplemental = | PubChem = 6433101 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 66899 | DrugBank = DB08819 | ChEMBL = 1963683 | ChemSpiderID = 8044182 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 1O6WQ6T7G3 | KEGG = D06274 | chemical_formula = | C=25 | H=34 | F=2 | O=5 | molecular_weight = 452.531266 g/mol | smiles = CC(C)OC(=O)CCC\\C=C/CC(C(O)CC1O)C1\\C=C\\C(F)(F)COc2ccccc2 | StdInChI = 1S/C25H34F2O5/c1-18(2)32-24(30)13-9-4-3-8-12-20-21(23(29)16-22(20)28)14-15-25(26,27)17-31-19-10-6-5-7-11-19/h3,5-8,10-11,14-15,18,20-23,28-29H,4,9,12-13,16-17H2,1-2H3/b8-3-,15-14+/t20-,21-,22+,23-/m1/s1 | StdInChIKey = WSNODXPBBALQOF-VEJSHDCNSA-N }}Tafluprost (trade names Taflotan by Santen Pharmaceutical and Zioptan by Merck in the US) is a prostaglandin analogue. It is used topically (as eye drops) to control the progression of open-angle glaucoma and in the management of ocular hypertension, alone or in combination with other medication. It reduces intraocular pressure by increasing the outflow of aqueous fluid from the eyes.[2] Adverse effectsThe 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.[2][5] InteractionsNonsteroidal 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.[2]No interactions with systemic (for example, oral) drugs are expected because tafluprost does not reach relevant concentrations in the bloodstream.[2][5] PharmacologyMechanism of actionTafluprost 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.[2][5] Other PGF2α analogues with the same mechanism include latanoprost and travoprost.[2] PharmacokineticsTafluprost, 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.[2][5] 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.[5] An analogous pathway (at least up to the tetranor-metabolites) has been found for latanoprost and travoprost. {{clear left}}References1. ^1 2 3 4 5 6 7 {{cite book|title=Austria-Codex|editor=Haberfeld, H|publisher=Österreichischer Apothekerverlag|location=Vienna|year=2015|language=German}} .[1][2][3][4]2. ^1 2 3 4 5 {{cite book|title=Arzneistoff-Profile|editor1=Dinnendahl, V |editor2=Fricke, U |publisher=Govi Pharmazeutischer Verlag|location=Eschborn, Germany|date=2011|edition=25|volume=9|isbn=978-3-7741-9846-3|language=German}} 3. ^1 {{cite journal|pmid=19477946|year=2009|author1=Fukano|first1=Y|title=Disposition and metabolism of a novel prostanoid antiglaucoma medication, tafluprost, following ocular administration to rats|journal=Drug Metabolism and Disposition|volume=37|issue=8|pages=1622–34|last2=Kawazu|first2=K|doi=10.1124/dmd.108.024885}} 4. ^1 {{cite journal|pmid=21491995|year=2011|author1=Fukano|first1=Y|title=Metabolism and ocular tissue distribution of an antiglaucoma prostanoid, tafluprost, after ocular instillation to monkeys|journal=Journal of Ocular Pharmacology and Therapeutics|volume=27|issue=3|pages=251–9|last2=Kawazu|first2=K|last3=Akaishi|first3=T|last4=Bezwada|first4=P|last5=Pellinen|first5=P|doi=10.1089/jop.2010.0178}} }}{{Prostaglandins}}{{Antiglaucoma preparations and miotics}}{{Prostanoidergics}} 7 : Prostaglandins|Alcohols|Alkenes|Carboxylate esters|Isopropyl esters|Organofluorides|Phenol ethers |
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