Usage
- Tafluprost is prescribed for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.
- Pharmacological Classification: Prostaglandin analog, antiglaucoma agent.
- Mechanism of Action: Tafluprost, specifically its active metabolite tafluprost acid, increases uveoscleral outflow of aqueous humor, thereby reducing IOP.
Alternate Names
- Tafluprost acid (active metabolite)
- Brand Names: Zioptan, Saflutan, Taflotan
How It Works
- Pharmacodynamics: Tafluprost acid is a highly potent and selective agonist of the human prostanoid FP receptor. Its primary action is to increase uveoscleral outflow of aqueous humor.
- Pharmacokinetics: Tafluprost is administered as an ophthalmic solution. After instillation, it is hydrolyzed to tafluprost acid, its biologically active form. Tafluprost acid reaches peak plasma concentrations within 10 minutes of administration. Systemic concentrations are extremely low. Elimination is primarily through hepatic metabolism and renal excretion. The half-life of tafluprost acid is about 2 hours.
- Mode of Action: Tafluprost acid binds to and activates FP receptors in the ciliary muscle and trabecular meshwork, stimulating matrix metalloproteinases, which then facilitate aqueous humor outflow through the uveoscleral pathway.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: FP receptor agonist.
- Elimination Pathways: Hepatic metabolism, renal excretion.
Dosage
Standard Dosage
Adults:
- One drop in the affected eye(s) once daily in the evening.
Children:
- Use is not recommended in children under 18 years of age due to a lack of safety and efficacy data. Safety concerns exist regarding increased pigmentation following long-term use.
Special Cases:
- Elderly Patients: No dosage adjustment necessary.
- Patients with Renal Impairment: Use with caution. Not extensively studied in this population.
- Patients with Hepatic Dysfunction: Use with caution. Not extensively studied in this population.
- Patients with Comorbid Conditions: Use with caution in patients with active intraocular inflammation (e.g., iritis/uveitis), aphakia, pseudophakia with a torn posterior lens capsule, macular edema risk, or a history of bronchial asthma.
Clinical Use Cases
Tafluprost is not specifically indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its primary use is for chronic management of open-angle glaucoma or ocular hypertension.
Dosage Adjustments
Dose adjustments may be necessary in patients with renal or hepatic impairment, though specific recommendations are limited due to insufficient data in these patient populations.
Side Effects
Common Side Effects
- Conjunctival hyperemia (eye redness)
- Eye itching, stinging, burning, or dryness
- Blurred vision
- Increased eyelash length, thickness, and number
- Changes in eye, eyelash, or eyelid color (increased pigmentation)
- Foreign body sensation in the eye
- Increased tearing
Rare but Serious Side Effects
- Iritis/Uveitis
- Macular edema
- Allergic reactions (including skin rash, itching or hives, swelling of the face, lips, or tongue)
- Retinal detachment
Long-Term Effects
- Permanent changes in iris color (increased brown pigmentation)
Adverse Drug Reactions (ADR)
- Severe allergic reactions (anaphylaxis)
Contraindications
- Hypersensitivity to tafluprost or any component of the formulation.
Drug Interactions
- No clinically significant drug interactions are anticipated due to low systemic concentrations of tafluprost acid. However, concomitant use with other prostaglandin analogs may reduce IOP-lowering effectiveness. Separate administration of multiple ophthalmic medications by at least 5 minutes.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown some reproductive toxicity, but there are no adequate and well-controlled studies in pregnant women. Women of childbearing potential should use effective contraception.
- Breastfeeding: Tafluprost and/or its metabolites are excreted in rat milk. It is unknown whether tafluprost is excreted in human milk. Exercise caution when administering to nursing women.
Drug Profile Summary
- Mechanism of Action: FP receptor agonist, increasing uveoscleral outflow of aqueous humor.
- Side Effects: Conjunctival hyperemia, eye irritation, changes in iris/eyelid/eyelash color, blurred vision.
- Contraindications: Hypersensitivity to tafluprost.
- Drug Interactions: Limited data, potential reduced effect with other prostaglandin analogs.
- Pregnancy & Breastfeeding: Use with caution, potential fetal risk, unknown excretion in human milk.
- Dosage: One drop in affected eye(s) once daily in the evening.
- Monitoring Parameters: Intraocular pressure, pigmentation changes in the eye, eyelash changes, visual acuity.
Popular Combinations
- Timolol: May provide additional IOP-lowering effects when used adjunctively.
Precautions
- General Precautions: Use with caution in patients with active intraocular inflammation, aphakia/pseudophakia, and risk of macular edema.
- Specific Populations: As above.
- Lifestyle Considerations: May cause transient blurred vision, affecting ability to drive or operate machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Tafluprost?
A: One drop in the affected eye(s) once daily in the evening for adults. Not recommended for children under 18.
Q2: How does Tafluprost work?
A: It primarily increases uveoscleral outflow of aqueous humor, which lowers intraocular pressure.
Q3: What are the most common side effects?
A: Eye redness, irritation (stinging, burning, itching), changes in eye color, increased eyelash growth, blurred vision.
Q4: Are there any serious side effects?
A: Yes, although rare, serious side effects include iritis/uveitis, macular edema, and severe allergic reactions.
Q5: Can Tafluprost be used during pregnancy?
A: Only if the potential benefit outweighs the potential risk to the fetus. Consult with a specialist.
Q6: Can Tafluprost be used while breastfeeding?
A: Caution is advised. It is unknown if it’s excreted in human milk. Discuss risks and benefits with a doctor.
Q7: Can I use other eye drops with Tafluprost?
A: Yes, but administer them at least 5 minutes apart.
Q8: Is it safe to drive after using Tafluprost?
A: Tafluprost may cause transient blurred vision. Avoid driving or operating machinery until vision clears.
Q9: Is the iris color change permanent?
A: Yes, the increased brown pigmentation of the iris is likely permanent.
Q10: How should Tafluprost be stored?
A: Store unopened single-use containers in the foil pouch in a refrigerator. Once opened, store at room temperature for up to 28 days and discard any remaining solution after use.
