Allergic rhinitis: Oral: 10 mg once daily (maximum: 10 mg/day).
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.
Use is not recommended (has not been studied).
Use is not recommended (has not been studied).
Refer to adult dosing; use with caution.
(For additional information see "Rupatadine (United States: Not available): Pediatric drug information")
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:
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.
Use is not recommended (has not been studied).
Use is not recommended (has not been studied).
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
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.
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.
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 available in various countries; not currently available in the U.S.
Yes
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]
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.
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.
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.
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
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 drug interactions program by clicking on the “Launch drug interactions program” link above.
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
Amezinium: Antihistamines may enhance the stimulatory effect of Amezinium. 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
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: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. 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
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
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
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). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider therapy modification
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
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
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
Loxapine: CNS Depressants may enhance the CNS depressant effect of Loxapine. Risk D: Consider therapy modification
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
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination
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
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
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy
Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
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
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
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
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
Grapefruit juice increases rupatadine systemic exposure 3.5-fold. Management: Avoid grapefruit juice during therapy.
Information related to the use of rupatadine in pregnancy is limited; the manufacturer recommends avoiding use in pregnant women.
It is not known if rupatadine is present in breast milk; breastfeeding is not recommended by the manufacturer.
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.
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).
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