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epinastine (Elestat)

 

Classes: Antihistamines, Ophthalmic

Dosing and uses of Elestat (epinastine)

 

Adult dosage forms and strengths

ophthalmic solution

  • 0.05%

 

Allergic Conjunctivitis

Instill 1 gtt in affected eye(s) q12hr; continue throughout period of exposure even in absense of symptoms

 

Pediatric dosage forms and strengths

ophthalmic solution

  • 0.05%

 

Allergic Conjunctivitis

<2 years: Safety and efficacy not established

>2 years: As adults, instill 1 gtt in affected eye(s) q12hr

 

Elestat (epinastine) adverse (side) effects

Frequency not defined

Headache

Burning sensation in eye

Folliculosis

Hyperemia

Pruritus

Nonocular infection

 

Postmarketing Reports

Increased lacrimation

 

Warnings

Contraindications

Hypersensitivity

Contact lens-related irritation

 

Cautions

Do not wear contact lenses if eyes are red; wait 10 min after epinastine to insert contacts

Keratitis may occur from inadvertent contamination of multi-dose ophthalmic solution; use caution

Not for contact lens irritation relief

Do not wear contact lenses if eye is red

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Excretion in milk unknown; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Elestat (epinastine)

Mechanism of action

Histamine H1 antagonist, inhibits vascular permeability and release of histamine and other mediators involved in allergic response; has affinity for H2 alpha1, alpha2, and 5HT2 receptors

 

Absorption

Onset: 3-5 min

Duration: 8 hr

 

Distribution

Protein Bound: 64%

 

Elimination

Half Life: 12 hr

Total Body Clearance: 56 L/hr

Excretion: Urine 55%; feces 30%