Detail

Tafluprost

Description

Name: Tafluprost
Type: small molecule
Groups: approved
Indication: Tafluprost is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Accession Number: DB08819 ( DB08819)
Description: A prostaglandin analogue ester prodrug used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension. Chemically, tafluprost is a fluorinated analog of prostaglandin F2-alpha. Tafluprost was approved for use in the U.S. on February 10, 2012.
Structure:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Saflutansolution4.5 mcgophthalmic01-01-1970Canada
Zioptansolution/ drops.0045 mg/.3mLophthalmic26-11-2014US
Zioptansolution.0045 mg/.3mLophthalmic10-02-2012US

Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
ZioptanTafluprost
ZioptanTafluprost
SaflutanTafluprost

Categories
  • Prostaglandins, Synthetic
  • Ophthalmics

Pharmacology

Indication: Tafluprost is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Pharmacodynamics: Not Available
Mechanism of action: Tafluprost acid is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Studies in animals and humans suggest that the main mechanism of action is increased uveoscleral outflow.
Absorption: Following instillation, tafluprost is absorbed through the cornea and is hydrolyzed to the biologically active acid metabolite, tafluprost acid. Tafluprost is an ester which makes the drug lipophillic enough to be quickly absorbed through. When administered to the eye, the peak plasma concentration (Cmax) and time to peak plasma concentration (Tmax) of tafluprost acid in healthy subjects was 26 pg/mL and 10 minutes respectively. a AUC, tafluprost acid = 394 pg*min/mL - 432 pg*min/mL.
Volume of distribution:
    The highest concentration of tafluprost acid was found in the cornea and conjunctiva.

Protein binding: Not Available
Metabolism: Not Available
Route of elimination: Mean plasma tafluprost acid concentrations were below the limit of quantification of the bioanalytical assay (10 pg/mL) at 30 minutes following topical ocular administration of tafluprost 0.0015% ophthalmic solution. In male rats, it was observed that tafluprost was excreted into the feces.
Half life: Not Available
Clearance: Not Available
Toxicity: Most common ocular adverse reaction is conjunctival hyperemia (range 4% – 20%).
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Not Available

Packagers:
  • Not Available

Dosage forms
FormRouteStrength
Solutionophthalmic4.5 mcg
Solutionophthalmic.0045 mg/.3mL
Solution/ dropsophthalmic.0045 mg/.3mL

Prices
Unit descriptionCostUnit

Patents
CountryPatent NumberApprovedExpires (estimated)
5886035United States2012-02-102017-12-18

Interactions

Drug Interactions
DrugInteraction
InfliximabThe therapeutic efficacy of Tafluprost can be decreased when used in combination with Infliximab.

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Alkyl aryl ethers
  • Alkyl fluorides
  • Carbonyl compounds
  • Carboxylic acid esters
  • Cyclic alcohols and derivatives
  • Cyclopentanols
  • Fatty acid esters
  • Hydrocarbon derivatives
  • Monocarboxylic acids and derivatives
  • Organofluorides
  • Phenol ethers

substituent:
  • Alcohol
  • Alkyl aryl ether
  • Alkyl fluoride
  • Alkyl halide
  • Aromatic homomonocyclic compound
  • Benzenoid
  • Carbonyl group
  • Carboxylic acid derivative
  • Carboxylic acid ester
  • Cyclic alcohol
  • Cyclopentanol
  • Ether
  • Fatty acid ester
  • Hydrocarbon derivative
  • Monocarboxylic acid or derivatives
  • Monocyclic benzene moiety
  • Organofluoride
  • Organohalogen compound
  • Organooxygen compound
  • Phenol ether
  • Prostaglandin skeleton
  • Secondary alcohol

References

Synthesis Reference: Not Available
General Reference: # Papadia M, Bagnis A, Scotto R, Traverso CE: Tafluprost for glaucoma. Expert Opin Pharmacother. 2011 Oct;12(15):2393-401. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21916788 # Pantcheva MB, Seibold LK, Awadallah NS, Kahook MY: Tafluprost: a novel prostaglandin analog for treatment of glaucoma. Adv Ther. 2011 Sep;28(9):707-15. Epub 2011 Aug 18. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21858491 # Takagi Y, Nakajima T, Shimazaki A, Kageyama M, Matsugi T, Matsumura Y, Gabelt BT, Kaufman PL, Hara H: Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug. Exp Eye Res. 2004 Apr;78(4):767-76. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15037111 # Fukano Y, Kawazu K: Disposition and metabolism of a novel prostanoid antiglaucoma medication, tafluprost, following ocular administration to rats. Drug Metab Dispos. 2009 Aug;37(8):1622-34. doi: 10.1124/dmd.108.024885. Epub 2009 May 28. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19477946
External Links:
ResourceLink
RxListhttp://www.rxlist.com/zioptan-drug.htm
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/vir1605.shtml
Drugs.comhttp://www.drugs.com/zioptan.html

ATC Codes:
  • Array

AHFS Codes:
  • 52:40.28

MSDS: Download
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