Ebastine

Ebastine should be used with caution in patients with severe hepatic insufficiency. A dosage of 10 mg should not be exceeded in patients with severe hepatic insufficiency, since no clinical studies have been developed with a higher dose than 10 mg.

Pharmacokinetic interactions have been observed when ebastine is given with ketoconazole or itraconazole and erythromycin. These interactions resulted in increased plasma concentrations of ebastine and to a lesser extent of carebastine which were, nevertheless, not associated with any clinically significant pharmacodynamic consequences.

Pharmacokinetic interactions have been observed when ebastine is given with rifampicin. These interactions could result in lower plasma concentrations and reduced antihistamine effects.

As with other antihistamines, caution must be exercised when using ebastine in patients known to be at cardiac risk such as those with long QT syndrome, hypokalemia, treatment with any drug known to produce an increase in QT interval or inhibit CYP3A4 enzyme systems such as azole antifungals and macrolide antibiotics

There are limited amount of data from the use of ebastine in pregnant women. Animals studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferably to avoid the use of ebastine during pregnancy.

It is not known whether the active substance is excreted in human milk. High protein binding (>97%) of ebastine and its main metabolite, carebastine, suggest no excretion of drug into breast milk. As a precautionary measure, it is preferably to avoid the use of ebastine during lactation.

Fertility

There are no fertility data with ebastine in humans. Animal studies have not shown adverse effects on fertility.

In a joint analysis of placebo-controlled clinical trials conducted in 5,708 patients treated with ebastine, the adverse reactions most frequently reported were dry mouth and somnolence.

Adverse reactions reported in clinical trials in children (n=460) were similar to those observed in adults

The list below displays all ADRs that have been reported in clinical trials or from post marketing experience using the following convention: Very common (>1/10); common (>1/100 to <1/10); uncommon (>1/1,000 to <1/100); rare (>1/10,000 to <1/1,000); very rare (<1/10,000), not known (cannot be estimated from the available data).

Psychiatric disorders

Very rare: nervousness, insomnia.

Nervous system disorders

Rare: somnolence.

Very rare: diziness, hypesthesia, headache.

Gastrointestinal disorders

Rare: dry mouth.

Very rare: vomiting, abdominal pain, nausea, dyspepsia.

Hepato-biliary disorders

Very rare: abnormal liver function test.

Skin and subcutaneous tissue disorders

Very rare: urticaria, rash, dermatitis.

Reproductive system and breast disorders

Very rare: menstrual disorders.

General disorders and administration site conditions

Very rare: oedema, asthenia.