Levocabastine

• (3S, 4R ) -1 - [4- cyano-4- (4-fluorophenyl ) cyclohexyl ]-3- methyl-4- phenylpiperidine - 4-carboxylic acid
• {3S-[1(cis),3α,4β]-1-[4-Cyano-4-(4-fluorphenyl)cyclohexyl]}-3-methyl-4-phenylpiperidin-4-carbonsäure

• 79516-68-0
• 79547-78-7 (hydrochloride)

R01AC02, S01GX02

Antihistamine

H1-receptor antagonist

Hydrochloride

Attention

Hydrochloride

Template: Infobox chemical / molecular formula search available

Levocabastine is a drug from the group of H1 - antihistamines of the second generation. It is used in the form of a suspension as eye drops and nasal sprays for local symptomatic treatment of allergic diseases.

• 2.1 Mechanism of action ( pharmacodynamics )
• 2.2 Absorption and distribution in the body ( pharmacokinetics )

Clinical information

Areas of application (indications )

Levocabastine is an H1 - antihistamine, which is applied only topically. Levocabastinhaltige eye drops and nasal sprays are for the symptomatic treatment of allergic conjunctivitis, vernal conjunctivitis, including ( VKC ), or licensed for the symptomatic treatment of allergic rhinitis.

Contraindications ( contraindications)

In a known hypersensitivity to levocabastinhaltige drug whose use is contraindicated.

Interactions with other drugs

With normal use, no drug interactions are to be expected. Containing oxymetazoline nasal sprays can temporarily reduce the absorption of nasally administered levocabastine.

Use during pregnancy and lactation

An embryotoxic and teratogenic potential could not be derived from animal studies. Since only limited data from pregnant women are present, the risk of pregnancy in humans is considered to be largely unknown.

The transition from nasal or Ophtal administered levocabastine in the mother's milk is limited ( about 0.6 and 0.3 percent). The use during lactation is based on a benefit- risk assessment.

Adverse effects (side effects)

In the application of levocabastine eye drops often occur ( 1 - 10 percent), eye pain and blurred vision on. Occasionally ( 0.1 to 1 percent) occurs on an eyelid. Conjunctivitis, eye swelling, blepharitis, ocular hyperaemia, tearing, other complaints administration, angioedema, hypersensitivity, contact dermatitis, urticaria and headache are very rare (< 0.01 percent).

Very common ( <10 percent) after the application of levocabastine nasal spray headaches were observed. Frequently, nausea, fatigue, pain, sinusitis, dizziness, drowsiness, pain in the laryngopharyngeal area, epistaxis and cough occur. Occasionally, angioedema, nausea, irritation, pain, dryness administration, hypersensitivity reactions, dyspnea, nasal discomfort, nasal congestion and bronchospasm. Side effects such as tachycardia, burning, discomfort administration and Nasalödem are rare ( 0.01 to 0.1 percent).

Pharmacological properties

Mechanism of action ( pharmacodynamics )

Levocabastine is a H1-receptor antagonist with a selectivity over other histamine receptors, and amine. Furthermore binds levocabastine to the neurotensin receptor NTS2.

Uptake and distribution in the body ( pharmacokinetics )

The systemic bioavailability of levocabastine after application to the eye is from about 30 to 60 percent. With normal use, no effective blood levels are reached. After use in the nose, the systemic bioavailability is 60 to 80 percent. The plasma half-life is 35 to 40 hours. Systemic recorded levocabastine is excreted mainly in the urine.