Epinastine (Elestat) is a second-generation antihistamine and a mast cell stabilizer that is used in the treatment of allergic eye disease.

Epinastine (Elestat) Uses:

• It is used in the treatment of allergic conjunctivitis.

Epinastine (Elestat) Dose in Adults

Epinastine (Elestat) Dose in allergic conjunctivitis:

• Ophthalmic:
  • Instill one drop in each eye two times a day.
  • The treatment should be continued throughout the period of exposure even when the symptoms have resolved.

Epinastine (Elestat) Dose in Childrens

Epinastine (Elestat) Dose in allergic conjunctivitis in children:

• Children ≥2 years and Adolescents:

  • Ophthalmic:
    • Instill one drop in each eye two times a day.
    • The treatment should be continued throughout the period of exposure even if the symptoms have resolved.

Pregnancy Risk Factor C

• Pregnant women have not been tested for the drug.
• However, teratogenic effects in animal reproduction have not been demonstrated.

Use epinastine while breastfeeding

• It is unknown if the drug will be excreted into breastmilk.
• It is recommended that you use it with caution if you are breastfeeding.

Epinastine (Elestat) Dose in Kidney disease:

• In the manufacturer's labeling, an adjustment in the dose has not been provided.
• However, dosage adjustment is not required because of minimal systemic absorption.

Epinastine (Elestat) Dose in Liver disease:

• In the manufacturer's labeling, an adjustment in the dose has not been provided.
• However, dosage adjustment is not required because of minimal systemic absorption.

Side Effects of Epinastine (Elestat):

• Central nervous system:

  • Headache

• Infection:

  • Infection

• Ophthalmic:

  • Burning sensation of eyes
  • Eye pruritus
  • Follicular conjunctivitis
  • Ocular hyperemia

• Respiratory:

  • Cough
  • Pharyngitis
  • Rhinitis
  • Sinusitis

Contraindications to Epinastine (Elestat):

The manufacturer's labeling does not contain any contraindications.

Warnings and precautions

• Bacterial Keratitis

  • Inadvertent contamination may lead to bacterial keratitis.

Monitoring Parameters:

None mentioned in the manufacturer's labeling. Monitor the response to treatment.

How to administer Epinastine (Elestat)?

• The drug is intended for ophthalmic use only.
• Patients should be advised to avoid touching the tip of the dropper with the eyes or other surfaces.
• Prior to drug administration, remove contact lenses.
• Reinsert contact lenses after about 10 minutes. Avoid wearing contact lenses if the eyes are red.

Mechanism of action of Epinastine (Elestat):

• It acts as a selective antagonist of the H-1 receptor. 
• It blocks the release of histamine by mast cells.
• It is also a good candidate for the H-2 alpha-1 and alpha-2 receptors, as well as the 5-HT-2 receptors.

The onset of action:

• 3-5 minutes

Duration:

• 8 hours

Absorption:

• Low systemic absorption following topical application

Distribution:

• Does not cross the blood-brain barrier

Protein binding:

• 64%

Metabolism:

• <10% metabolized

Half-life elimination:

• 12 hours

Excretion: IV:

• Urine (55%);
• feces (30%)

International Brand Names of Epinastine:

• Elestat
• Alesion
• Alket
• Allerginon
• Alpatin
• Aresten
• Atergit
• Elestat
• Epigen
• Epinast
• Flurinol
• Furinol
• Karmastin
• Optest
• Purivist
• Relestat
• Statergic
• Talerc

Epinastine Brand Names in Pakistan:

• No Brands Available in Pakistan.