Epinastine

Registered South African indications:

• Symptoms of seasonal allergic conjunctivitis

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to benzalkonium chloride

Contraindications registered in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients

• Pregnancy
• Breastfeeding
• Concomitant use of soft contact lenses
• Significantly damaged corneas (phosphate containing formulations)
• May impair ability to drive or operate machinery

Forms avail. in SA and covered this monograph: opd

South African registered indications and dosages

Symptoms of seasonal allergic conjunctivitis
- Short-term treatment

• Ophthalmic (opd): Instil 1 drop into affected eye(s), twice daily during the symptomatic period

There is no experience in clinical studies with the use of epinastine for more than 8 weeks, therefore its use beyond that time span is not recommended

Epinastine should not be administered while wearing contact lenses (see additional prescribing points)

To avoid contamination of the eye or eye drops do not allow the dropper tip to come into contact with any surface

If more than one topical ophthalmic medicinal product is being used, administer at least 10 minutes apart

Paeds. forms avail. in SA and covered this monograph: opd

South African registered indications and dosages

Symptoms of seasonal allergic conjunctivitis
- Short-term treatment

Younger than 12 years

• Not established for use

12 years and older

• See adult dosage

Pregnancy

• Caution
• Data on a limited number (11) of exposed pregnancies indicate no adverse effects of epinastine on pregnancy or on the health of the foetus/newborn child. To date, no other relevant epidemiological data is available
• Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonic/foetal development, parturition or postnatal development
• Caution should be exercised when prescribing to pregnant women

Breastfeeding

• Caution
• Epinastine is excreted in the breast milk of rats, but it is not known if epinastine is excreted in human milk
• Due to the lack of experience, caution should be exercised when prescribing to breastfeeding women

Fertility

• There is no adequate data from the use of epinastine on fertility in humans

Renal Impairment

• No dose adjustment recommended 
  Epinastine has not been studied in patients with renal impairment. However, no dose adjustment is considered necessary due to low systemic absorption

Hepatic Impairment

• No dose adjustment recommended
  Epinastine has not been studied in patients with hepatic impairment. The metabolism of epinastine in humans is minimal (<10%), therefore no dose adjustment is considered necessary due to low systemic absorption

Elderly

• No dose adjustment recommended
  Epinastine has not been studied in the elderly. Post-marketing safety data from the tablet formulation of epinastine hydrochloride indicates no particular safety issues for older people, thus no dose adjustment is considered necessary

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache

Respiratory Disorders

• Asthma
• Nasal irritation
• Rhinitis

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reaction
  - Symptoms or signs of eye allergy
  - Extra-ocular allergic reactions
  - Angioedema
  - Skin rash
  - Redness

Sensory Disorders

• Burning sensation in eye
• Eye irritation
• Conjunctival or ocular hyperaemia
• Eye discharge
• Eye dryness
• Eye pruritus
• Visual disturbance
• Increased lacrimation
• Eye pain
• Eye swelling
• Eyelid oedema
• Corneal calcification
• Dysgeusia

No information available (see additional prescribing points)

None routine

Contact lens special precautions

• Benzalkonium chloride may be absorbed by and discolour soft contact lenses
• Patients should be instructed to wait until 15 minutes after instillation of epinastine before inserting contact lenses
• Epinastine should not be administered while wearing contact lenses

Interaction with other medicinal products and other forms of interaction

• No interaction studies have been performed
• No interactions are anticipated in humans since systemic concentrations of epinastine are extremely low following ocular dosing
• In addition, epinastine is mainly excreted unchanged in humans indicated a low level of metabolism

Epinastine is a topically active, direct H1-receptor antagonist. Epinastine has a high binding affinity for the histamine H1-
receptor and a 400 times lower affinity for the histamine H2-receptor. Epinastine also possesses affinity for the α1-, α2-,
and the 5-HT2-receptor. It has low affinity for cholinergic, dopaminergic and a variety of other receptor sites. Epinastine
does not penetrate the blood/brain barrier and, therefore, does not induce side effects of the central nervous system, i.e.,
it is non-sedative.

Eye drops (per ml) 0.5mg

• Relestat (Allergan) originator