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تعداد آیتم قابل مشاهده باقیمانده : 3 مورد
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Rupatadine (United States: Not available): Drug information

Rupatadine (United States: Not available): Drug information
(For additional information see "Rupatadine (United States: Not available): Patient drug information" and see "Rupatadine (United States: Not available): Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: Canada
  • Rupall
Pharmacologic Category
  • Histamine H1 Antagonist;
  • Histamine H1 Antagonist, Second Generation
Dosing: Adult
Allergic rhinitis

Allergic rhinitis: Oral: 10 mg once daily (maximum: 10 mg/day).

Urticaria, chronic spontaneous

Urticaria, chronic spontaneous: Oral: Initial: 10 mg once daily; if symptom control is inadequate, may increase to 20 mg once daily (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Use is not recommended (has not been studied).

Dosing: Hepatic Impairment: Adult

Use is not recommended (has not been studied).

Dosing: Older Adult

Refer to adult dosing; use with caution.

Dosing: Pediatric

(For additional information see "Rupatadine (United States: Not available): Pediatric drug information")

Allergic rhinitis

Allergic rhinitis:

Children ≥2 to <12 years: Oral solution:

10 to ≤25 kg: Oral: 2.5 mg once daily.

>25 kg: Oral: 5 mg once daily.

Children ≥12 years and Adolescents: Tablets: Oral: 10 mg once daily.

Urticaria, chronic spontaneous

Urticaria, chronic spontaneous:

Children ≥2 to <12 years: Oral solution:

10 to ≤25 kg: Oral: 2.5 mg once daily.

>25 kg: Oral: 5 mg once daily.

Children ≥12 years and Adolescents: Tablets: Oral: 10 mg once daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

Use is not recommended (has not been studied).

Dosing: Hepatic Impairment: Pediatric

Use is not recommended (has not been studied).

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Cardiovascular: Prolonged QT interval on ECG (1%)

Central nervous system: Drowsiness (9%), headache (6%), fatigue (>5%), hypersomnia (2%)

Gastrointestinal: Gastroenteritis (>5%), odynophagia (>5%), sore throat (>5%), vomiting (5%), abdominal pain (2%), xerostomia (2%), epigastric pain (1%)

Genitourinary: Dysmenorrhea (>5%)

Infection: Cold symptoms (>5%)

Neuromuscular & skeletal: Increased creatine phosphokinase (3%)

Respiratory: Allergic conjunctivitis (>5%), allergic rhinitis (>5%), cough (>5%), flu-like symptoms (>5%), nasopharyngitis (>5%), rhinitis (>5%), tonsillitis (>5%)

>1%, postmarketing, and/or case reports: Anaphylaxis, anemia, angioedema, arthralgia, atrial fibrillation, back pain, depression, diarrhea, dizziness, dysesthesia, dyspnea, eczema, epistaxis, fever, hypersensitivity reaction, hypertension, hypoesthesia, increased appetite, increased gamma-glutamyl transferase, increased serum alkaline phosphatase, increased serum alt, increased serum ast, increased thirst, irritability, motion sickness, myalgia, myasthenia, nausea, night sweats, palpitations, sedation, skin rash, stupor, weakness, weight gain

Contraindications

Hypersensitivity to rupatadine or any component of the formulation; history of QTc prolongation and/or torsades de pointes, including congenital long QT syndromes; history of cardiac arrhythmias; concurrent use of CYP3A4 inhibitors or other QTc-prolonging drugs; rare hereditary problems of galactose intolerance, glucose-galactose malabsorption, or congenital lactase deficiency (tablets); rare hereditary problems of fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltase insufficiency (oral solution).

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Warnings/Precautions

Concerns related to adverse effects:

• Altered cardiac conduction: QTc interval prolongation and torsades de pointes (very rare) have been reported; use caution in patients at increased risk for arrhythmias, including torsades de pointes (eg, uncorrected electrolyte abnormalities). Use is contraindicated in patients with a history of QTc prolongation and/or torsades de pointes, including congenital long QT syndromes, history of cardiac arrhythmias, or taking other QTc-prolonging drugs.

• Hypersensitivity: Rare hypersensitivity reactions, including anaphylaxis, angioedema, and urticarial, have been reported.

• Myalgia: Muscle pain and weakness have been reported.

Dosage form specific issues:

• Methyl parahydroxybenzoate: Some formulations may contain methyl parahydroxybenzoate; may cause allergic reactions (possibly delayed).

• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Zar 2007). See manufacturer's labeling.

Warnings: Additional Pediatric Considerations

Some dosage forms may contain propylene glycol; in neonates, large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).

Product Availability

Product available in various countries; not currently available in the U.S.

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Oral:

Rupall: 1 mg/mL (30 mL, 120 mL) [contains methylparaben, propylene glycol, quinoline yellow (d&c yellow #10), saccharin sodium]

Tablet, Oral:

Rupall: 10 mg [contains corn starch]

Administration: Adult

Oral: Administer with or without food. For solution, insert oral syringe (provided with packaging) into perforated stopper. Turn bottle upside down to allow syringe to fill with appropriate dose. Wash oral syringe after use.

Administration: Pediatric

Oral: May administer with or without food.

Solution: Children 2 to 11 years: Measure dose with calibrated measuring device. Insert oral syringe (provided with packaging) into perforated stopper. Wash oral syringe after use.

Tablet: Children ≥12 years and Adolescents: Doses should be taken with full glass of water.

Use: Labeled Indications

Note: Not approved in the United States.

Allergic rhinitis: Symptomatic treatment of seasonal and perennial allergic rhinitis in patients ≥2 years of age.

Chronic spontaneous urticaria: Symptomatic treatment of chronic spontaneous urticaria (eg, pruritus, hives) in patients ≥2 years of age.

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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. Risk D: Consider therapy modification

Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Betahistine may diminish the therapeutic effect of Antihistamines. Risk C: Monitor therapy

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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. Risk D: Consider therapy modification

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

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. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Rupatadine. Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Rupatadine. Risk X: Avoid combination

Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy

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. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Grapefruit Juice: May increase the serum concentration of Rupatadine. Risk X: Avoid combination

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. Risk C: Monitor therapy

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Risk C: Monitor therapy

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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. Risk C: Monitor therapy

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

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. Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification

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. Risk D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pitolisant: Antihistamines may diminish the therapeutic effect of Pitolisant. Risk X: Avoid combination

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. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

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. Risk D: Consider therapy modification

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. Risk D: Consider therapy modification

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

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 D: Consider therapy modification

Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification

Food Interactions

Grapefruit juice increases rupatadine systemic exposure 3.5-fold. Management: Avoid grapefruit juice during therapy.

Pregnancy Considerations

Information related to the use of rupatadine in pregnancy is limited; the manufacturer recommends avoiding use in pregnant women.

Breastfeeding Considerations

It is not known if rupatadine is present in breast milk; breastfeeding is not recommended by the manufacturer.

Mechanism of Action

Rupatadine is a second generation long-acting antihistamine with selective peripheral H1 antagonistic activity and platelet activating factor (PAF) antagonistic activities. At higher concentrations, rupatadine will inhibit degranulation of mast cells and release of cytokines, particularly TNF-alpha in human mast cells and monocytes.

Pharmacokinetics (Adult Data Unless Noted)

Onset: 1 to 2 hours.

Duration: Antihistaminic activity: Up to 24 hours.

Absorption: Rapid.

Distribution: Vd: 9,799 L.

Protein binding: 98.5% to 99%.

Metabolism: Undergoes oxidation, hydroxylation, and N-dealklyation mainly by CYP 3A4 and to a lesser extent by CYP2C9, CYP2C19, and CYP2D6; active metabolites include desloratadine and hydroxylated derivatives of desloratadine.

Half-life elimination:

Children: 2 to 5 years of age: 15.9 hours; 6 to 11 years of age: 12.3 hours.

Adults: 4.04 to 6.07 hours.

Adults ≥65 years of age: 8.7 hours.

Time to peak, serum: 0.75 to 1 hour.

Excretion: Urine (34.6%; negligible amount as unchanged drug); Feces (60.9%; negligible amount as unchanged drug) (Rupatadine UK Summary of Product Characteristics 2016).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Rupafin;
  • (AR) Argentina: Rupafin;
  • (AT) Austria: Rupafin;
  • (BD) Bangladesh: Dipa | Duvent | Minista | Paftrol | Rosela | Rufast | Rufecta | Runar | Rupa | Rupa aid | Rupaday | Rupadin | Rupafen | Rupaler | Rupamine | Rupanex | Rupastar | Rupatid | Rupatrol | Rupenta | Rupex | Rupin | Rupoma | Stark;
  • (BE) Belgium: Rupatadine eg | Rupatadine teva | Rupatadine uriach | Rupatall;
  • (BF) Burkina Faso: Rinialer;
  • (BG) Bulgaria: Rupafin;
  • (BR) Brazil: Rupafin;
  • (CI) Côte d'Ivoire: Rinialer;
  • (CL) Chile: Reax | Rexanel | Rupafin | Rupax;
  • (CN) China: Lu su;
  • (CO) Colombia: Rupafin;
  • (CZ) Czech Republic: Tamalis;
  • (DE) Germany: Rupafin | Rupatadin al | Rupatadine bluefish | Urtimed;
  • (DO) Dominican Republic: Rupatadina calox | Rupax | Senardin;
  • (EC) Ecuador: Rupafin;
  • (EE) Estonia: Rupafin;
  • (EG) Egypt: Alergoliber | Darupax | Elirupalin | Healthtadine | Hisatrup | Rupatoclear;
  • (ES) Spain: Alergoliber | Rinialer | Rupafin | Rupatadina aurovitas | Rupatadina bluefish | Rupatadina cinfa | Rupatadina kern pharma | Rupatadina Mabo | Rupatadina normon | Rupatadina ratiopharm | Rupatadina stada | Rupatadina teva;
  • (FI) Finland: Pafinur;
  • (FR) France: Rupatadine arrow | Rupatadine biogaran | Rupatadine eg | Rupatadine mylan | Rupatadine zentiva | Wystamm;
  • (GB) United Kingdom: Rupafin | Rupatadine;
  • (GR) Greece: Rupafin;
  • (HU) Hungary: Tamalis;
  • (IN) India: Ralif | Ralzal | Rup al | Rupahist | Rupameg | Rupanex | Rupin | Ryten | Rz | Xure;
  • (IT) Italy: Pafinur | Rupafin | Rupatadina aurobindo | Rupatadina doc Generici | Rupatadina eg | Rupatadina mylan pharma | Rupatadina teva;
  • (JP) Japan: Rupafin;
  • (KE) Kenya: Rupafin | Rupahist | Rupanase junior | Zealargy;
  • (KR) Korea, Republic of: Rupafin;
  • (KW) Kuwait: Rupafin;
  • (LB) Lebanon: Rupatadine biogaran;
  • (LT) Lithuania: Rupafin;
  • (LU) Luxembourg: Rupatall;
  • (LV) Latvia: Rupafin;
  • (MX) Mexico: Repafet;
  • (NL) Netherlands: Rupafin | Rupatadine cf | Rupatadine teva;
  • (NO) Norway: Rupafin | Urtimed;
  • (PE) Peru: Megatadina | Rinepan | Rupafin;
  • (PH) Philippines: Rupafin;
  • (PL) Poland: Alerprof | Rupafin | Rupatadine bluefish | Rupatadine Genoptim | Rupiron | Rupoclar | Rupurix;
  • (PT) Portugal: Rinialer | Rupatadina bluefish | Rupatadina cinfa | Rupatadina farmoz | Rupatadina generis | Rupatadina mylan | Rupatadina ratiopharm;
  • (QA) Qatar: Rupa | Rupafin;
  • (RO) Romania: Tamalis;
  • (RU) Russian Federation: Rupafin;
  • (SA) Saudi Arabia: Pafinur;
  • (SE) Sweden: Pafinur;
  • (SG) Singapore: Rupafin;
  • (SI) Slovenia: Rupafin;
  • (SK) Slovakia: Rupafin | Rupastad | Rupatadin vivax | Rupatadine mylan;
  • (TH) Thailand: Rupafin;
  • (TR) Turkey: Anthix | Ripatrin | Rupafin | Rupatek;
  • (UA) Ukraine: Blis;
  • (UG) Uganda: Zealargy;
  • (ZA) South Africa: Rupahist | Rupanase | Rupanase junior | Zealargy
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Topic 112988 Version 128.0

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