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.
Contraindications of Rupatadine
- 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
- Fatigue
- Dry mouth
- Headache
- Drowsiness
- Dizziness
- Weakness
- dry mouth, sore throat, cough;
- muscle pain;
- drowsiness, tired feeling;
- nausea, diarrhea; or
- headache.
- fast, pounding, or uneven heartbeat;
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
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.
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