Generic

Rupatadine Fumarate

Indications

Rupatadine is indicated for the symptomatic treatment of Seasonal & Perennial Allergic Rhinitis and Urticaria.

Pharmacology

Rupatadine is a non-sedative antagonist of histamine H1-receptors with a lengthy half-life. It also inhibits platelet-activating factor (PAF) (PAF). Histamine and PAF both produce broncho constriction, which increases vascular permeability and serves as a mediator in the inflammatory process. Rupatadine has a better therapeutic impact than a single antihistamine because of its dual mechanism of action. Rupatadine also inhibits mast cell degranulation triggered by immunological and non-immune stimuli, as well as the release of cytokines, particularly tumor necrosis factor-alpha (TNF), in human mastocytes and monocytes.

Dosage and Administration

Adults and adolescents (over 12 years): The recommended dose is 10 mg once a day. Rupatadine may be taken with or without food.

Children aged 2 to 11 years:

For children weighing 25 kg or more: 1 teaspoonful (5 ml) of the oral solution once daily with or without food.

For children weighing equal or more than 10 kg to less than 25 kg: 1/2 teaspoonful (2.5 ml) oral solution once daily with or without food.

Interaction

When taking Rupatadine 20 mg with ketoconazole or erythromycin at the same time, systemic exposure is increased. When these drugs, as well as other inhibitors of the CYP3A4 isozyme, are used together, rupatadine should be used with caution. When used with statins, CNS depressants, or alcohol, rupatadine should be used with caution.

Grapefruit and grapefruit juice should not be eaten at the same time as Rupatadine.

Contraindications

Hypersensitivity to Rupatadine or to any of the excipients.

Side Effects

Asthenia, dizziness, and drowsiness are all common symptoms. Uncommon: Increased appetite, arthralgia, back pain, dizziness, constipation, cough, diarrhea, dry throat, epistaxis, fever, gastrointestinal discomfort, increased risk of infection, irritability, malaise, myalgia, nasal dryness, nausea, oropharyngeal pain, rash, thirst, vomiting, weight gain Palpitations, and tachycardia are uncommon.

Pregnancy & Lactation

There is no clinical data available on the exposure of Rupatadine during pregnancy. Pregnant women should therefore not use Rupatadine unless the potential benefit outweighs the potential risk for the infant. No information is available, on whether Rupatadine is excreted in the mother’s milk. Therefore, it should not be used during lactation, unless the potential benefits for the mother justify the potential risk to the infant.

Precautions & Warnings

Rupatadine should be taken with caution in patients who have a known QT interval prolongation, uncorrected hypokalemia, or persistent proarrhythmic circumstances including clinically severe bradycardia or acute myocardial ischemia. In senior people, rupatadine should be administered with caution (65 years and older). The use of Rupatadine 10 mg tablets in patients with compromised renal or liver function is currently not indicated due to a lack of clinical data.

Therapeutic Class

Non-sedating antihistamines

Storage Conditions

Store in a cool & dry place below 30°C, and protect from light & moisture. Keep out of reach of children.

Pharmaceutical Name

Aristopharma Ltd.