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Rupatadine; Uses, Dosage, Side Effects, Interactions

Rupatadine is a dual histamine H1 receptor and platelet activating factor receptor antagonist that is used for symptomatic relief in seasonal and perennial rhinitis as well as chronic spontaneous urticaria. It was approved for marketing in Canada under the tradename Rupall and comes in tablet formulation for adult use and liquid formulation for pediatric use.

Rupatadine is a second-generation tricyclic H1-antihistamine.

Mechanism of action of Rupatadine

Rupatadine is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist. During allergic response mast, cells undergo degranulation, releasing histamine and other substances. Histamine acts on H1 receptors to produce symptoms of nasal blockage, rhinorrhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorrhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatadine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms. Rupatadine possesses anti-allergic properties such as the inhibition of the degranulation of mast cells induced by immunological and non-immunological stimuli, and inhibition of the release of cytokines, particularly of the tumor necrosis factors (TNF) in human mast cells and monocytes.

Indications of Rupatadine

Allergic Rhinitis
Hives
Pruritis
Asthma
Allergic intraocular inflammatory diseases
Atopic eczema
Inflammatory dermatoses
Pruritis
Allergic symptoms like urticaria,
Rhinorrhea,
Sneezing and itching
Skin itching
Itching of the skin
Itching skin
Runny nose
Sneezing
Itchy eyes
For the symptomatic relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and perennial allergic rhinitis in patients 2 years of age and older. Also used for the symptomatic relief of chronic spontaneous urticaria in patients 2 years of age and older.

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Contraindications of Rupatadine

Hypersensitivity to Rupatadine is a contraindication. In addition, Rupatadine should not be used if you have the following conditions:

Children below the age of twelve years
Don’t drink alcohol
Hypersensitivity
Stomach Cancer
Porphyria
Liver Problems
Kidney disease with the reduction in kidney function
Allergies to Histamine H2 Inhibitors

Dosages of Rupatadine

Oral
Allergic rhinitis, Chronic idiopathic urticaria
Adult: 10 mg once daily.

Side Effects of Rupatadine

The most common

More common

headache
fast, pounding, or uneven heartbeat;
fever, flu symptoms;
seizure (convulsions); or
jaundice (yellowing of the skin or eyes).
dry mouth, sore throat, cough;
muscle pain;
drowsiness, tired feeling;
nausea,
fever, flu symptoms;
seizure (convulsions); or
jaundice (yellowing of the skin or eyes).

Less common

Dizziness
dry mouth
dysmenorrhea, such as difficult or painful menstruation
dyspepsia, such as acid or sour stomach, belching, heartburn, indigestion, stomach discomfort , upset or pain,
fatigue, such as, unusual tiredness or weakness
myalgias, such as joint pain, swollen joints, muscle aching or cramping, muscle pains or stiffness, difficulty in moving
pharyngitis, such as body aches or pain, congestion, cough, dryness or soreness of throat, fever, hoarseness, runny nose, tender swollen glands in neck, trouble in swallowing, voice changes.
somnolence, such as, sleepiness or unusual drowsiness
nausea

Drug Interactions of Rupatadine

Rupatadine may interact with following drugs,supplements & may change the efficacy of drugs

antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
diltiazem
domperidone
macrolide antibiotics (e.g., clarithromycin, erythromycin)
mifepristone
other antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
sotalol
“statin” anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
zopiclone

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Pregnancy and Lactation of Rupatadine

Pregnancy category B

Pregnancy

There are a limited amount of data from the use of rupatadine in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development (see section 5.3). As a precautionary measure, it is preferable to avoid the use of rupatadine during pregnancy.

Lactation

Rupatadine is excreted in animal milk. It is unknown whether rupatadine is excreted into breast milk. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from rupatadine therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.