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Epinastine: Drug information

Epinastine: Drug information
(For additional information see "Epinastine: Patient drug information" and see "Epinastine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Histamine H1 Antagonist;
  • Histamine H1 Antagonist, Second Generation
Dosing: Adult
Allergic conjunctivitis

Allergic conjunctivitis: Ophthalmic: Instill 1 drop into each eye twice daily. Continue throughout period of exposure, even in the absence of symptoms.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Epinastine: Pediatric drug information")

Allergic conjunctivitis

Allergic conjunctivitis: Children ≥2 years and Adolescents: Ophthalmic: Instill 1 drop into each eye twice daily; continue throughout period of exposure, even in the absence of symptoms.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely necessary due to low systemic absorption.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely necessary due to low systemic absorption.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

Frequency not always defined.

1% to 10%:

Central nervous system: Headache (1% to 3%)

Infection: Infection (10%; defined as cold symptoms and upper respiratory tract infection)

Ophthalmic: Burning sensation of eyes, eye pruritus, follicular conjunctivitis, ocular hyperemia

Respiratory: Cough (1% to 3%), pharyngitis (1% to 3%), rhinitis (1% to 3%), sinusitis (1% to 3%)

<1%, postmarketing, and/or case reports: Increased lacrimation

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.

Special populations:

• Contact lens wearers: Contains benzalkonium chloride which may be absorbed by contact lenses; remove contact lenses prior to use and wait 10 minutes before reinserting.

Other warnings/precautions:

• Appropriate use: For topical ophthalmic use only. Not for the treatment of contact lens irritation; do not wear contact lenses if eye is red.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as hydrochloride:

Generic: 0.05% (5 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Epinastine HCl Ophthalmic)

0.05% (per mL): $20.52 - $21.40

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

For ophthalmic use only; avoid touching tip of applicator to eye or other surfaces. Contact lenses should be removed prior to application, may be reinserted after 10 minutes. Do not wear contact lenses if eyes are red.

Administration: Pediatric

For ophthalmic use only; avoid touching tip of applicator to eye or other surfaces. Contact lenses should be removed prior to application; may be reinserted after 10 minutes. Do not wear contact lenses if eyes are red.

Use: Labeled Indications

Allergic conjunctivitis: Prevention of itching of the eye associated with allergic conjunctivitis.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Breastfeeding Considerations

It is not known if epinastine is excreted in breast milk. The manufacturer recommends that caution be exercised when administering epinastine to nursing women.

Mechanism of Action

Selective H1-receptor antagonist; inhibits release of histamine from the mast cell; also has affinity for the H2, alpha1, alpha2, and the 5-HT2 receptors

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: 3 to 5 minutes.

Duration: 8 hours.

Absorption: Low systemic absorption following topical application.

Distribution: Does not cross blood-brain barrier.

Protein binding: 64%.

Metabolism: <10% metabolized.

Half-life elimination: Terminal: ~12 hours.

Excretion: IV: Urine (~55% as unchanged drug); feces (~30%).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Relestat;
  • (AR) Argentina: Epioftal;
  • (AT) Austria: Relestat;
  • (BD) Bangladesh: Alastine | Alpatin | Epinast | Relestat;
  • (BE) Belgium: Relestat;
  • (BR) Brazil: Epenac | Relestat;
  • (CL) Chile: Relestat;
  • (CO) Colombia: Atergit | Epinoft | Relestat;
  • (CZ) Czech Republic: Purivist;
  • (DO) Dominican Republic: Relestat;
  • (EC) Ecuador: Atergit | Epioftal;
  • (EG) Egypt: Optest | Pharmastin | Relestat | Statergic;
  • (ES) Spain: Relestat;
  • (FI) Finland: Relestat;
  • (FR) France: Purivist;
  • (GB) United Kingdom: Relestat;
  • (GR) Greece: Relestat;
  • (HK) Hong Kong: Relestat;
  • (IE) Ireland: Relestat;
  • (IN) India: Epina | Epitane | Estina | Relestat;
  • (IT) Italy: Relestat;
  • (JO) Jordan: Apistat;
  • (JP) Japan: Alesion;
  • (KE) Kenya: Relestat;
  • (KR) Korea, Republic of: Alesion | Epinatine | Relestat;
  • (KW) Kuwait: Relestat;
  • (LB) Lebanon: Relestat;
  • (LU) Luxembourg: Relestat;
  • (MX) Mexico: Alket | Econ | Elestat;
  • (MY) Malaysia: Relestat;
  • (PE) Peru: Relenastine | Relestat;
  • (PH) Philippines: Relestat;
  • (PL) Poland: Relestat;
  • (PR) Puerto Rico: Elestat | Epinastine HCL;
  • (PT) Portugal: Relestat;
  • (PY) Paraguay: Atergit;
  • (RU) Russian Federation: Epinepta;
  • (SA) Saudi Arabia: Relestat;
  • (SE) Sweden: Relestat;
  • (SG) Singapore: Relestat;
  • (TH) Thailand: Relestat;
  • (TW) Taiwan: Relestat;
  • (VE) Venezuela, Bolivarian Republic of: Talerc;
  • (ZA) South Africa: Relestat;
  • (ZW) Zimbabwe: Relestat
  1. Epinastine [prescribing information]. Berlin, CT: Breckenridge Pharmaceutical Inc; April 2020.
Topic 8601 Version 163.0

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