Rupatadina
Rupatadina Uses, Dosage, Side Effects, Food Interaction and all others data.
Rupatadina is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H1 receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies.
Rupatadina 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.
Rupatadina is an anti allergenic and acts to reduce allergic symptoms like urticaria, rhinorrhea, sneezing and itching .
| Trade Name | Rupatadina |
| Generic | Rupatadine |
| Rupatadine Other Names | Rupatadina, Rupatadine |
| Type | |
| Formula | C26H26ClN3 |
| Weight | Average: 415.97 Monoisotopic: 415.1815255 |
| Protein binding | Rupatidine is 98.5-99.0% bound to human plasma proteins . |
| Groups | Approved |
| Therapeutic Class | Non-sedating antihistamines |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Rupatadina is used for the symptomatic treatment of seasonal & perennial allergic rhinitis and urticaria.
Rupatadina is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Pruritus, Urticaria
How Rupatadina works
Rupatadina 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, rhinorhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatidine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms.
Dosage
Rupatadina dosage
Rupatadina Tablet: The recommended dosage is 10 mg once daily, with or without food.
Rupatadina Oral Solution (Children aged 2 to 11 year):
- Children weighing 25 kg or more: 1 teaspoonful (5 ml) of oral solution once daily with or without food.
- 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.
Side Effects
The most common undesirable effects occurs somnolence, headache and fatigue. Other common undesirable effects include dizziness, asthenia and increase appetite.
Precaution
Administration of a dose of 10 mg daily of Rupatadina has not shown significant effects on the function of the central nervous system as seen in specific studies done for psychomotor function. Nevetheless, the patient should take precaution in driving or managing machines. The administration of rupatadine with grape fruit juice is not recommended.
Interaction
CYP3A4 inhibitors like Erythromycin & Ketoconazole inhibits both the presystemic and systemic metabolism of Rupatadina. Due to this potential interaction, it is not recommended to use Rupatadina in combination with Ketoconazole, macrolides or any other inhibitors of CYP3A4. Co administration of Rupatadina and CNS depressants or alcohol may increase CNS depressant effect.
Food Interaction
- Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of rupatadine.
- Take with or without food.
Volume of Distribution
The apparent volume of distribution is 9799 L .
Elimination Route
Rupatidine is rapidly absorbed with a Tmax of 1 h . Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.
Half Life
The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients .
Clearance
Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients .
Pregnancy & Breastfeeding use
Pregnancy category B2 (by TGA, Australia). There is no clinical data available on the exposure of Rupatadina during pregnancy. Pregnant women should therefore not use Rupatadina, unless the potential benefit outweighs the potential risk for the fetus. No information is available, whether Rupatadina 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.
Contraindication
Hypersensitivity to Rupatadina or to any of the excipients.
Special Warning
Elderly: Rupatadina should be used with caution in elderly. No information is available that indicates the requirement of any dose adjustment in this population.
Children: Neither the safety nor the efficacy of Rupatadina has been established in patients less than 12 years of age.
Patients with renal or hepatic insufficiency: Use of Rupatadina is not recommended in patients with renal or hepatic insufficiency. As no relevant clinical data is available.
Innovators Monograph
You find simplified version here Rupatadina
Rupatadina contains Rupatadine see full prescribing information from innovator Rupatadina Monograph, Rupatadina MSDS, Rupatadina FDA label
FAQ
What is Rupatadina used for?
Rupatadina is also used to relieve the symptoms associated with urticaria such as itching and hives (localised skin redness and swelling).
How safe is Rupatadina?
Rupatadina has been found to be effective and safe Iin a variety of randomized clinical trials both in both seasonal and perennial allergic rhinitis, as well as inbut also chronic urticaria Rupatadine has been found as effective and safe.
How does Rupatadina work?
Rupatadina works by blocking the action of one of the body's natural chemicals known as histamine.
What are the common side effects of Rupatadina?
Common side effects of Rupatadina are Sleepiness, headache, dizziness, dry mouth, sensation of weakness and fatigue.
Is Rupatadina safe during pregnancy?
Rupatadina is preferable to avoid the use of rupatadine during pregnancy.
Is Rupatadina safe during breastfeeding?
Rupatadina is excreted in animal milk. It is unknown whether Rupatadina is excreted into breast milk. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from Rupatadina therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.
Can I drink alcohol with Rupatadina?
Drink of alcohol is not recommended during treatment with this medicine due to the increased risk of severe adverse effects.
How long does it take for Rupatadina to work?
Rupatadina usually starts working within 2 hours and lasts for 24 hours.
How long does Rupatadina stay in my system?
The mean elimination half-life of Rupatadina in elderly and young volunteers was 8.7 hours and 5.9 hours respectively.
Is Rupatadina a sedative?
Rupatadina is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H1 receptor antagonist activity.
Does Rupatadina make I sleepy?
This drug may make you drowsy.Talk to your doctor about using Rupatadina safely.
Can I drive after taking Rupatadina?
At the recommended dosage, Rupatadina is not expected to influence your ability to drive or use machinery.
Is Rupatadina an anti inflammatory?
Rupatadina has a dual anti inflammatory effect by blocking both histamine H1 and PAF receptors.
Can I take Rupatadina for a long time?
Rupatadina 10 and 20mg once-daily doses were well tolerated in long-term use.
How long can you take Rupatadina?
All patients received Rupatadina 10 mg/day and were allowed to continue their normal concomitant medication for all conditions, other than rhinitis, for up to 6 or 12 months.
Is Rupatadina a mast cell stabilizer?
Rupatadina can inhibit histamine and cytokine secretion from human mast cells in response to allergic, immune and neuropeptide triggers.
What happens if I miss a dose?
If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.
How effective is Rupatadina for kindney?
The safety and effectiveness of Rupatadina have not been established for people with reduced kidney function. Rupatadina is not recommended for people with reduced kidney function.
How effective is Rupatadina for liver?
The safety and effectiveness of Rupatadina have not been established for people with reduced liver function. Rupatadina is not recommended for people with reduced liver function.
