Levocabastine
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| Non-proprietary name | Levocabastine | |||||||||||||||
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| Molecular formula | C 26 H 29 FN 2 O 2 | |||||||||||||||
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| Mechanism of action |
H 1 receptor antagonist |
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| Molar mass | 420.5 g · mol -1 | |||||||||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||
Levocabastine is a drug selected from the group of H 1 - antihistamines of the second generation. It is used in the form of a suspension as eye drops and nasal spray for the local symptomatic treatment of allergic diseases.
Clinical information
Application areas (indications)
Levocabastine is an H 1 antihistamine that is only used topically. Eye drops and nasal sprays containing levocabastine are approved for the symptomatic treatment of allergic conjunctivitis , including vernalis conjunctivitis (spring catarrh), and for the symptomatic treatment of allergic rhinitis .
Contraindications (contraindications)
If there is a known hypersensitivity to medicinal products containing levocabastine, their use is contraindicated .
Drug interactions
When used as intended, hardly any interactions with other drugs are to be expected. Nasal sprays containing oxymetazoline may temporarily reduce the uptake of nasal levocabastine.
Use during pregnancy and breastfeeding
An embryotoxic or teratogenic potential could not be derived from animal experiments. With limited data from pregnant women, the risk of pregnancy in humans is largely unknown.
The transfer of nasal or ophthalmic levocabastine into breast milk is limited (about 0.6 and 0.3 percent, respectively). Use during breastfeeding is based on a risk-benefit analysis.
Adverse effects (side effects)
Eye pain and blurred vision are common (1 to 10 percent) when using levocabastine eye drops. Occasionally (0.1-1 percent) eyelid edema occurs. Conjunctivitis, eye swelling, blepharitis, ocular hyperaemia, watery eyes, other administration site symptoms, angioedema, hypersensitivity, contact dermatitis, urticaria, and headache are very rare (<0.01 percent).
Headache has been observed very commonly (<10 percent) after using levocabastine nasal sprays. Often, nausea, tiredness, pain, sinusitis, drowsiness, drowsiness, pain in the pharynx and larynx, epistaxis and coughing occur. Occasionally, angioedema, malaise, irritation, pain, application site dryness, hypersensitivity reactions, dyspnoea, nasal discomfort, nasal congestion, and bronchospasm occur. Side effects such as tachycardia, burning sensation, discomfort at the application site, and nasal edema are rare (0.01-0.1 percent).
Pharmacological properties
Mechanism of action (pharmacodynamics)
Levocabastine is an H 1 receptor antagonist with selectivity over other histamine and amine receptors. Furthermore, levocabastine binds to the neurotensin receptor NTS 2 .
Absorption and distribution in the body (pharmacokinetics)
The systemic bioavailability of levocabastine after application to the eye is around 30 to 60 percent. If used as intended, no effective blood levels are achieved. After use in the nose, the systemic bioavailability is 60 to 80 percent. The plasma half-life is 35 to 40 hours. Systemically absorbed levocabastine is mainly excreted in the urine .
Trade names
Livocab (D); Livostin (A, CH); Levoreact (I)
