tafluprost

Action and Spectrum

Actions and spectrum: 

tafluprost is a prostaglandin analogue used to treat open-angle glaucoma and ocular hypertension. It reduces intraocular pressure by increasing the outflow of aqueous humor.

tafluprost binds to and activates the prostaglandin FP receptor, which is found in the ciliary muscle of the eye. This leads to relaxation of the ciliary muscle and increased outflow of aqueous humor, resulting in reduced intraocular pressure. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Conjunctival hyperemia (4-20%) 

1-10% 

Blurred vision (2%) 

Growth of eyelashes (2%) 

Cataract (3%) 

allergic conjunctivitis/Ocular pruritus (5%) 

Ocular stinging (7%)  

Post marketing Reports 

Eye disorders: uveitis/ Iritis 

Periorbital and lid changes like deepening of the eyelid with prostaglandin analogs 

Respiratory disorders: dyspnea, Exacerbation of asthma 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

tafluprost is contraindicated in patients who have hypersensitivity to the drug or any of its components. It is contraindicated in patients who have a history of macular edema, uveitis, iritis, or anterior chamber inflammation. Additionally, it is not recommended for use in patients with active intraocular inflammation, neovascular glaucoma, or angle-closure glaucoma.  

Caution: 

• Hypersensitivity: tafluprost is contraindicated in patients who are hypersensitive to it or any of its components. 
• Eye Infections: tafluprost in patients with active intraocular inflammation should be used with caution 
• Cystoid macular edema (CME): tafluprost in patients with a history of CME should be used with caution, as it can exacerbate the condition. 
• Contact lens wearers: tafluprost contains benzalkonium chloride, which can be absorbed by soft contact lenses. Contact lenses should be removed before the instillation of tafluprost and reinserted 15 minutes after instillation. 
• Pregnancy and lactation: There is insufficient data on the use of tafluprost in pregnant or lactating women. It should only be used during pregnancy if the potential benefits outweigh the risks. 
• Children: The safety and efficacy of tafluprost in children have not been established. It should only be used in children under the supervision of a physician.

Comorbidities: 

• Active intraocular inflammation 
• Macular edema 
• patients with risk factors for macular edema or pseudophakic patients,Aphakic patients with a torn posterior lens capsule, 
• Herpetic keratitis or history of herpes simplex 
• Corneal dystrophy or other corneal abnormalities 
• Uveitis 
• Cystoid macular edema 
• Patients with severe allergic reactions, including anaphylaxis, to any of the components of tafluprost 
• Patients with hepatic or renal impairment 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: C 

Lactation: safety and efficacy not established  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

tafluprost is a prostaglandin F2-alpha analog used in the treatment of glaucoma and ocular hypertension. The drug works by reducing intraocular pressure (IOP) through increased aqueous humor outflow. tafluprost binds to and activates the prostaglandin F2-alpha receptor, which leads to increased matrix metalloproteinase production, proteolysis of extracellular matrix proteins, and relaxation of ciliary muscle, resulting in increased aqueous humor outflow. tafluprost is metabolized primarily by hydrolysis via esterases to an inactive carboxylic acid metabolite, which is eliminated renally.  

Pharmacodynamics: 

tafluprost is a synthetic prostaglandin F2α analog that lowers intraocular pressure (IOP) by increasing the outflow of aqueous humor through the uveoscleral pathway. It is used in the treatment of open-angle glaucoma and ocular hypertension. The exact mechanism of action of tafluprost is not fully known, but it is believed to work by binding to the prostaglandin F2α receptor and activating the G protein-coupled receptor signaling pathway, which leads to increased outflow of aqueous humor. tafluprost also causes a reduction in the production of aqueous humor, which contributes to its IOP-lowering effects.  

Pharmacokinetics: 

Absorption 

tafluprost is administered topically to the eye and is rapidly absorbed through the cornea. 

Distribution 

tafluprost is distributed to the anterior segment of the eye. 

Metabolism 

tafluprost undergoes hydrolysis to an inactive metabolite in the cornea and plasma. 

Elimination and excretion 

tafluprost and its metabolites are primarily eliminated by renal excretion. 

Adminstartion

Administration: 

tafluprost is a prescription eye drop medication that is used to reduce intraocular pressure (IOP) in people with open-angle glaucoma or ocular hypertension. The recommended dose of tafluprost is one drop in the affected eye(s) once daily in the evening. It can be used in combination or alone with other eye drops. 

Before administering tafluprost, hands should be washed thoroughly. The patient should be instructed to tilt their head back, look up, and pull down their lower eyelid to create a small pocket. A single drop of the medication should be instilled into the pocket, and the patient should be instructed to close their eyes and apply with a gentle pressure over inner corner of the eye for 1 to 2 minutes.

They should also avoid blinking or rubbing their eyes. Contact lenses should be removed before using tafluprost and should not be reinserted for at least 15 minutes after the medication has been administered. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tafluprost 

Pronounced: [ TA-floo-prost ]  

Why do we use tafluprost ? 

tafluprost is a medication used to lower the pressure inside the eye in conditions like open-angle glaucoma and ocular hypertension. It is a prostaglandin analog, which acts by increasing the fluid outflow from the eye.

This helps to reduce intraocular pressure, which is a major risk factor for glaucoma. tafluprost is administered as eye drops and is usually used once daily in the evening.