; 1/10)
• Uncommon (≥ 1/1000 to < 1/100)
• Rare (≥ 1/10,000 to <1/1,000)
The frequencies of adverse reactions reported in patients treated with rupatadine 10 mg tablets during clinical trials were as follows:
• Infections and infestations
- Uncommon : Pharyngitis, Rhinitis
• Metabolism and nutrition disorders
- Uncommon : Increased appetite
• Nervous system disorders:
- Common : Somnolence, Headache, Dizziness
- Uncommon : Disturbance in attention
• Cardiac disorders
- Rare: tachycardia and palpitations*
• Respiratory, thoracic, and mediastinal disorders
- Uncommon : Epistaxis, Nasal dryness, Cough, Dry throat, Oropharyngeal pain
• Gastrointestinal disorders
- Common : Dry mouth
- Uncommon : Nausea, Abdominal pain upper, Diarrhoea, Dyspepsia, Vomiting, Abdominal pain, Constipation
• Skin and subcutaneous tissue disorders
- Uncommon : Rash
• Musculoskeletal, connective tissues, and bone disorders
- Uncommon : Back pain, Arthralgia, Myalgia
• General Disorders and administration site condition
- Common : Fatigue, Asthenia
- Uncommon: Thirst, Malaise, Pyrexia, Irritability
• Investigations
- Uncommon : Blood creatine phosphokinase increased, Alanine aminotransferase increased, Aspartate aminotransferase increased, Liver function test abnormal, Weight increased
* tachycardia and palpitations have been reported in post-marketing experience with rupatadine 10 mg tablets.
4.9 Overdose
No case of overdose has been reported. In a clinical safety study rupatadine at daily dose of 100 mg during 6 days was well tolerated. The most common adverse reaction was somnolence. If accidental ingestion of very high doses occurs symptomatic treatment together with the required supportive measures should be given.
5. Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: other antihistamines for systemic use, ATC code: R06A X28.
Rupatadine is a second generation antihistamine, long-acting histamine antagonist, with selective peripheral H1-receptor antagonist activity. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug.
In vitro studies with rupatadine at high concentration have shown an inhibition of the degranulation of mast cells induced by immunological and non-immunological stimuli as well as the release of cytokines, particularly of the TNFα in human mast cells and monocytes. The clinical relevance of the observed experimental data remains to be confirmed.
Chronic idiopathic urticaria was studied as a clinical model for urticarial conditions, since the underlying pathophysiology is similar, regardless of etiology, and because chronic patients can be more easily recruited prospectively. Since histamine release is a causal factor in all urticarial diseases, rupatadine is expected to be effective in providing symptomatic relief for other urticarial conditions, in addition to chronic idiopathic urticaria, as advised in clinical guidelines.
Clinical trials in volunteers (n= 375) and patients (n=2650) with allergic rhinitis and chronic idiopathic urticaria did not show significant effect on the electrocardiogram when rupatadine was administered at doses ranging from 2 mg to 100 mg.
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