Levocabastine

Levocabastine is an active ingredient for the treatment of allergies. It belongs to the group of 2nd generation antihistamines and is mainly used in eye drops and nasal sprays. Levocabastine can be used to treat allergic conjunctivitis or as a nasal spray for hay fever. It is usually present in medicines as levocabastine hydrochloride and is insoluble in water.

Levocabastine acts as a selective competitive antagonist at histamine-1 receptors. This means that it displaces histamine, the substance that normally binds to histamine-1 receptors. In this context, selective means that the active substance only binds to this one receptor. The displacement of the actual substrate (agonist) is called competitive. The competitive antagonist, in this case levocabastine, attempts to displace the actual agonist, in this case histamine, by binding more strongly to the receptor. Histamine is an endogenous messenger substance (mediator) and is mainly released by mast cells in allergies. The excessive release of histamine leads to a series of reactions in the body, which are responsible for the typical symptoms of an allergy, among other things. However, it is important to note that the symptoms only occur when there is an excessive release of histamine and that the respective allergen is responsible for this. An allergy is an overreaction of the immune system to harmless substances, which can be very different.

Levocabastine is converted (metabolized) by the liver and excreted in the urine by the kidneys. Absorption (uptake into the bloodstream) occurs rapidly and mainly through the mucous membranes. The bioavailability, i.e. the percentage of the active ingredient available in the blood, is 30-60% when used as eye drops and 60-80% when used in the nose. The half-life, i.e. the time the body needs to excrete half of the active ingredient, is around 35-40 hours. This favors an effect that can last up to 12 hours.

Always take Levocabastine exactly as described in the package leaflet or as advised by your doctor.

Adults:

The usual recommended dose is 0.1 mg twice daily per nostril or 0.015 mg twice daily per eye.

The recommended dose can be increased up to 4 times a day.

Children & adolescents from 8 years of age:

The usual recommended dose is 0.1 mg per nostril 2x daily or 0.015 mg per eye 2x daily .

The recommended dose can be increased up to 4 times a day.

The following side effects may occur:

Very common:

• Irritation of the eyes
• Headache

Frequent:

• Sinusitis
• Dizziness
• Somnolence
• Pain in the throat and larynx
• Nosebleeds
• Cough
• Nausea
• tiredness
• eye pain
• blurred vision
• Discomfort at the site of administration (eyes)

Occasional:

• Hypersensitivity
• Swelling of the eyelid
• Cardiac arrhythmia (palpitations)
• shortness of breath
• Nasal discomfort
• blocked nose
• bronchospasm
• malaise
• Irritation, pain and dryness at the site of administration (nose)

Rarely:

• rapid heart rate (tachycardia)
• Nasal swelling
• Burning and discomfort at the site of administration (nose)

Very rare:

• Painful swelling of the skin and mucous membrane
• Conjunctivitis (inflammation of the conjunctiva)
• Eye swelling
• Inflammation of the eyelids (blepharitis)
• Increased accumulation of blood in the eye (ocular hyperemia)
• watery eyes
• contact dermatitis
• hives
• Reactions at the site of administration (eyes)

Frequency unknown:

• Allergic shock (anaphylaxis)
• palpitations

Interactions may occur if the following medicines are taken at the same time:

• with oxymetazoline, the absorption of levocabastine may be reduced

Levocabastine must NOT be taken in the following cases:

• in case of allergy to Levocabastine
• in children under 8 years of age

Levocabastine should only be taken from the age of 8. From the age of 65, the breakdown of levocabastine may take longer.

Levocabastine should only be used during pregnancy after careful risk-benefit assessment by a doctor. In animal studies, toxic effects in the unborn baby were only observed with an overdose of 1250 times the recommended dose.

During breastfeeding, levocabastine should only be taken after consulting a doctor, as it passes into breast milk. However, there is a lack of further data on its use during breastfeeding.