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Rupatadine (Rupall) - Uses, Dose, Side effects, MOA, Brands

Rupatadine is an antihistamine medication used primarily for the treatment of allergies. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms like sneezing, itching, and watery eyes. Rupatadine is commonly used to relieve symptoms associated with allergic rhinitis (hay fever) and urticaria (hives). It's available in oral tablet form and is generally well-tolerated, with common side effects including drowsiness, headache, and dry mouth.

Rupatadine (Rupall) is a selective long-acting antihistamine that is used for the symptomatic treatment of patients with seasonal and perennial allergic rhinitis. It is also used in the treatment of patients with chronic urticaria. Rupatadine Uses:

Allergic rhinitis:
- It is used for the symptomatic treatment of seasonal and perennial allergic rhinitis in patients 2 years of age or older.
Chronic spontaneous urticaria:
- It is also used for the symptomatic treatment of chronic spontaneous urticaria manifesting as pruritus and hives in patients 2 years of age and older.

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Rupatadine (Rupall) Dose in Adults

Rupatadine (Rupall) Dose in the treatment of Allergic rhinitis and chronic spontaneous urticaria:

When using rupatadine to treat allergies like hay fever or hives, the typical dose is 10 milligrams taken by mouth once a day.
You shouldn't take more than 10 milligrams in a day.
This dosage is effective for both allergic rhinitis (hay fever) and chronic spontaneous urticaria (hives).

Rupatadine (Rupall) Dose in Childrens

Rupatadine (Rupall) Dose in the treatment of Allergic rhinitis and chronic spontaneous urticaria: Oral:

For children aged 2 to under 12 years:
- If the child weighs between 10 kg to 25 kg, the dose is 2.5 milligrams once daily, with a maximum of 2.5 milligrams per day.
- If the child weighs more than 25 kg, the dose is 5 milligrams once daily, with a maximum of 5 milligrams per day.
For children aged 12 years and older, and adolescents:
- They should follow the same dosing as adults.

Rupatadine (Rupall) pregnancy Risk Category: B (C)

There isn't much information about using rupatadine during pregnancy, so it's best for pregnant women to avoid taking it.
The manufacturer suggests steering clear of rupatadine if you're pregnant.

Use during breastfeeding:

Since it's not clear whether rupatadine passes into breast milk, the manufacturer advises against breastfeeding while using rupatadine.
This caution is to ensure the safety of the nursing infant.
If you're considering using rupatadine and you're breastfeeding.

Dose in Kidney Disease:

Using rupatadine in people with kidney problems isn't recommended because it hasn't been studied in this group.

Dose in Liver disease:

Using rupatadine in people with liver problems isn't recommended because it hasn't been studied in this group.

Side Effects of Rupatadine (Rupall):

Cardiovascular:
- Prolonged Q-T Interval On ECG
Central Nervous System:
- Drowsiness
- Headache
- Fatigue
- Hypersomnia
Gastrointestinal:
- Gastroenteritis
- Odynophagia
- Sore Throat
- Vomiting
- Abdominal Pain
- Xerostomia
- Epigastric Pain
Genitourinary:
- Dysmenorrhea
Infection:
- Cold Symptoms
Neuromuscular & Skeletal:
- Increased Creatine Phosphokinase
Respiratory:
- Allergic Conjunctivitis
- Allergic Rhinitis
- Cough
- Flu-Like Symptoms
- Nasopharyngitis
- Rhinitis
- Tonsillitis

Contraindications to Rupatadine (Rupall):

Rupatadine should not be used if you have a hypersensitivity to rupatadine itself or any ingredient in the medication.
It's also not suitable if you have a history of QTc prolongation or torsades de pointes, including congenital long QT syndromes, or if you've had cardiac arrhythmias.
Avoid rupatadine if you're taking medications that inhibit CYP3A4 or other drugs that can prolong QTc interval.
Additionally, individuals with rare hereditary conditions such as galactose intolerance, glucose-galactose malabsorption, Lapp lactase deficiency (for tablets), fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltase insufficiency (for oral solution) should avoid using rupatadine.

Warnings and precautions

Modified cardiac conduction

Rupatadine can affect the electrical conduction of the heart, potentially leading to QTc interval prolongation and a rare but serious heart rhythm disorder called torsades de pointes.
It's important to be cautious when using rupatadine, especially in patients who are at increased risk for arrhythmias, such as those with uncorrected electrolyte abnormalities.
Rupatadine should not be used in individuals with a history of QTc prolongation and/or torsades de pointes, including those with congenital long QT syndromes, a history of cardiac arrhythmias, or those taking other medications that prolong QTc interval.

Hypersensitivity

Rare cases of hypersensitivity reactions, including severe allergic reactions like anaphylaxis, angioedema (swelling under the skin), and urticaria (hives), have been reported with the use of rupatadine.
While these reactions are uncommon, it's essential to be aware of the possibility and seek immediate medical attention if you experience any signs or symptoms of a severe allergic reaction while taking rupatadine.

Myalgia:

Some individuals may experience muscle pain and weakness, known as myalgia, while taking rupatadine.
While this side effect is not very common, it's important to be aware of it.

Hepatic impairment

Due to a lack of sufficient studies, the use of rupatadine is not recommended for individuals with hepatic impairment, which refers to decreased liver function.

Renal impairment

Using rupatadine in individuals with renal impairment, which refers to decreased kidney function, is not recommended because it has not been studied in this group.

Rupatadine (United States: Not available): Drug Interaction

Risk Factor C (Monitor therapy)
Acetylcholinesterase Inhibitors	May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors.
Alcohol (Ethyl)	CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl).
Alizapride	May enhance the CNS depressant effect of CNS Depressants.
Amantadine	May enhance the anticholinergic effect of Anticholinergic Agents.
Amezinium	Antihistamines may enhance the stimulatory effect of Amezinium.
Amphetamines	May diminish the sedative effect of Antihistamines.
Anticholinergic Agents	May enhance the adverse/toxic effect of other Anticholinergic Agents.
Aprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Betahistine	Antihistamines may diminish the therapeutic effect of Betahistine.
Botulinum Toxin-Containing Products	May enhance the anticholinergic effect of Anticholinergic Agents.
Brexanolone	CNS Depressants may enhance the CNS depressant effect of Brexanolone.
Brimonidine (Topical)	May enhance the CNS depressant effect of CNS Depressants.
Bromopride	May enhance the CNS depressant effect of CNS Depressants.
Cannabidiol	May enhance the CNS depressant effect of CNS Depressants.
Cannabis	May enhance the CNS depressant effect of CNS Depressants.
Chloral Betaine	May enhance the adverse/toxic effect of Anticholinergic Agents.
Chlorphenesin Carbamate	May enhance the adverse/toxic effect of CNS Depressants.
Clofazimine	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CNS Depressants	May enhance the adverse/toxic effect of other CNS Depressants.
CYP3A4 Inhibitors (Moderate)	May increase the serum concentration of Rupatadine.
Dimethindene (Topical)	May enhance the CNS depressant effect of CNS Depressants.
Doxylamine	May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended.
Dronabinol	May enhance the CNS depressant effect of CNS Depressants.
Duvelisib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Erdafitinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Esketamine	May enhance the CNS depressant effect of CNS Depressants.
Fosaprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Fosnetupitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Gastrointestinal Agents (Prokinetic)	Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic).
Glucagon	Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased.
HMG-CoA Reductase Inhibitors (Statins)	Rupatadine may enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk for increased CPK and/or other muscle toxicities may be increased.
HydrOXYzine	May enhance the CNS depressant effect of CNS Depressants.
Itopride	Anticholinergic Agents may diminish the therapeutic effect of Itopride.
Kava Kava	May enhance the adverse/toxic effect of CNS Depressants.
Larotrectinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Lofexidine	May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Magnesium Sulfate	May enhance the CNS depressant effect of CNS Depressants.
MetyroSINE	CNS Depressants may enhance the sedative effect of MetyroSINE.
Mianserin	May enhance the anticholinergic effect of Anticholinergic Agents.
Minocycline	May enhance the CNS depressant effect of CNS Depressants.
Mirabegron	Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron.
Mirtazapine	CNS Depressants may enhance the CNS depressant effect of Mirtazapine.
Nabilone	May enhance the CNS depressant effect of CNS Depressants.
Netupitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Nitroglycerin	Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption.
Palbociclib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Piribedil	CNS Depressants may enhance the CNS depressant effect of Piribedil.
Pramipexole	CNS Depressants may enhance the sedative effect of Pramipexole.
Ramosetron	Anticholinergic Agents may enhance the constipating effect of Ramosetron.
ROPINIRole	CNS Depressants may enhance the sedative effect of ROPINIRole.
Rotigotine	CNS Depressants may enhance the sedative effect of Rotigotine.
Rufinamide	May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
Selective Serotonin Reuptake Inhibitors	CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced.
Simeprevir	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Tetrahydrocannabinol	May enhance the CNS depressant effect of CNS Depressants.
Tetrahydrocannabinol and Cannabidiol	May enhance the CNS depressant effect of CNS Depressants.
Thiazide and Thiazide-Like Diuretics	Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics.
Topiramate	Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate.
Trimeprazine	May enhance the CNS depressant effect of CNS Depressants.
Risk Factor D (Consider therapy modification)
Benzylpenicilloyl Polylysine	Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects.
Blonanserin	CNS Depressants may enhance the CNS depressant effect of Blonanserin.
Buprenorphine	CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants.
Chlormethiazole	May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used.
Droperidol	May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Flunitrazepam	CNS Depressants may enhance the CNS depressant effect of Flunitrazepam.
Hyaluronidase	Antihistamines may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving antihistamines (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required.
HYDROcodone	CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
Methotrimeprazine	CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established.
Opioid Agonists	CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
OxyCODONE	CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
Perampanel	May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination.
Pramlintide	May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract.
Secretin	Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin.
Sodium Oxybate	May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated.
Stiripentol	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.
Suvorexant	CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended.
Tapentadol	May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
Zolpidem	CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol.
Risk Factor X (Avoid combination)
Aclidinium	May enhance the anticholinergic effect of Anticholinergic Agents.
Azelastine (Nasal)	CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal).
Bromperidol	May enhance the CNS depressant effect of CNS Depressants.
Cimetropium	Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium.
Conivaptan	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CYP3A4 Inhibitors (Strong)	May increase the serum concentration of Rupatadine.
Eluxadoline	Anticholinergic Agents may enhance the constipating effect of Eluxadoline.
Fusidic Acid (Systemic)	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Glycopyrrolate (Oral Inhalation)	Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation).
Glycopyrronium (Topical)	May enhance the anticholinergic effect of Anticholinergic Agents.
Grapefruit Juice	May increase the serum concentration of Rupatadine.
Idelalisib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Ipratropium (Oral Inhalation)	May enhance the anticholinergic effect of Anticholinergic Agents.
Levosulpiride	Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride.
Orphenadrine	CNS Depressants may enhance the CNS depressant effect of Orphenadrine.
Oxatomide	May enhance the anticholinergic effect of Anticholinergic Agents.
Oxomemazine	May enhance the CNS depressant effect of CNS Depressants.
Paraldehyde	CNS Depressants may enhance the CNS depressant effect of Paraldehyde.
Pitolisant	Antihistamines may diminish the therapeutic effect of Pitolisant.
Potassium Chloride	Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride.
Potassium Citrate	Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate.
Revefenacin	Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin.
Thalidomide	CNS Depressants may enhance the CNS depressant effect of Thalidomide.
Tiotropium	Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium.
Umeclidinium	May enhance the anticholinergic effect of Anticholinergic Agents.

Monitoring Parameters:

None mentioned.

How to administer Rupatadine (Rupall)?

How to Take Rupatadine Orally

Administration: Rupatadine can be taken with or without food.
For Solution:
- Insert the oral syringe provided with the packaging into the perforated stopper of the solution bottle.
- Turn the bottle upside down to allow the syringe to fill with the appropriate dose.
- Wash the oral syringe after each use to maintain cleanliness and hygiene.

Mechanism of action of Rupatadine (Rupall):

Antihistamine Activity: Rupatadine belongs to the second generation of antihistamines. It selectively blocks H1 receptors in the peripheral nervous system.
Platelet Activating Factor (PAF) Antagonism: Additionally, rupatadine acts as an antagonist to Platelet Activating Factor (PAF), which is involved in inflammatory processes.
Inhibition of Mast Cell Degranulation: At higher concentrations, rupatadine can inhibit the degranulation of mast cells. This means it helps prevent the release of histamine and other inflammatory substances from these cells.
Suppression of Cytokines: Rupatadine also suppresses the release of cytokines, particularly TNF-alpha, from human mast cells and monocytes. TNF-alpha is a pro-inflammatory cytokine involved in various allergic reactions and inflammatory processes.

Onset of Action:

Rupatadine typically starts working within 1 to 2 hours after administration.

Duration of Action:

Its antihistaminic activity can last for up to 24 hours.

Absorption:

Rupatadine is rapidly absorbed into the bloodstream after administration.

Distribution:

It has a large volume of distribution (V : 9,799 L), meaning it spreads throughout the body's tissues.

Protein Binding:

Rupatadine is highly bound to proteins in the bloodstream, with 98.5% to 99% bound.

Metabolism:

The drug undergoes metabolism primarily by enzymes such as CYP3A4, with lesser contributions from CYP2C9, CYP2C19, and CYP2D6. Active metabolites include desloratadine and hydroxylated derivatives of desloratadine.

Half-life: The elimination half-life varies with age:

Children aged 2 to 5 years: 15.9 hours
Children aged 6 to 11 years: 12.3 hours
Adults: 4.04 to 6.07 hours
Elderly: 8.7 hours

Time to Peak Serum Concentration:

Rupatadine reaches its peak concentration in the bloodstream within 0.75 to 1 hour after administration.

Excretion:

The drug is primarily excreted in the urine (34.6%) and to a lesser extent in the feces (60.9%). Only a negligible amount of unchanged drug is excreted.

International Brand Names of Rupatadine: