Version July 2025
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).
(For additional information see "Rupatadine (United States: Not available): Drug information")
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; although current guidelines state that antihistamine doses may be increased up to 4 times the standard dose (eg, 40 mg/day), there is limited evidence for greater efficacy with this dose of rupatadine. Periodically reevaluate necessity for continued treatment (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).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adolescents and adults, unless otherwise noted.
1% to 10%:
Cardiovascular: Prolonged QT interval on ECG (1%)
Gastrointestinal: Abdominal pain (2%), epigastric pain (1%), vomiting (1% ), xerostomia (2%)
Nervous system: Drowsiness (9%), headache (6%), hypersomnia (2%)
Neuromuscular & skeletal: Increased creatine phosphokinase in blood specimen (3%)
<1% (children, adolescents, adults):
Cardiovascular: Palpitations
Dermatologic: Eczema, night sweats, skin rash
Endocrine & metabolic: Increased thirst, weight gain
Gastrointestinal: Diarrhea, increased appetite, motion sickness, nausea
Hematologic & oncologic: Anemia
Hepatic: Increased gamma-glutamyl transferase, increased serum alanine aminotransferase, increased serum alkaline phosphatase, increased serum aspartate aminotransferase
Nervous system: Asthenia, depression, dizziness, dysesthesia, fatigue, hypoesthesia, irritability, sedated state, stupor
Neuromuscular & skeletal: Myalgia
Miscellaneous: Fever
Postmarketing (any population):
Cardiovascular: Atrial fibrillation, hypertension, syncope, tachycardia
Dermatologic: Fixed drug eruption (Fidan 2011), urticaria
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis, angioedema)
Nervous system: Myasthenia, vertigo
Neuromuscular & skeletal: Arthralgia, back pain, rhabdomyolysis
Respiratory: Cough, dyspnea, epistaxis
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).
• 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, as fumarate:
Rupall: 10 mg [contains corn starch]
Generic: 10 mg
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.
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.
Store at 15°C to 30°C (59°F to 86°F). Protect tablets from light.
Note: Not approved in the United States.
Canadian labeling: Symptomatic treatment of seasonal and perennial allergic rhinitis (indicated for use in patients ≥2 years of age); symptomatic treatment of chronic spontaneous urticaria (eg, pruritus, hives) (indicated for use in patients ≥2 years of age).
Substrate of CYP3A4 (Major with inhibitors), CYP3A4 (Minor with inducers); 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.
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
Amezinium: Antihistamines may increase stimulatory effects of Amezinium. Risk C: Monitor
Benzylpenicilloyl Polylysine: Coadministration of Antihistamines and Benzylpenicilloyl Polylysine may alter diagnostic results. 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 decrease therapeutic effects of Betahistine. Betahistine may decrease therapeutic effects of Antihistamines. Risk C: Monitor
Certoparin: Antihistamines may increase therapeutic effects of Certoparin. Risk C: Monitor
Clofazimine: May increase serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor
CYP3A4 Inhibitors (Moderate): May increase serum concentration of Rupatadine. Risk C: Monitor
CYP3A4 Inhibitors (Strong): May increase serum concentration of Rupatadine. Risk X: Avoid
Fusidic Acid (Systemic): May increase 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 serum concentration of Rupatadine. Risk X: Avoid
HMG-CoA Reductase Inhibitors (Statins): Rupatadine may increase adverse/toxic effects of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk for increased CPK and/or other muscle toxicities may be increased. Risk C: Monitor
Hyaluronidase: Antihistamines may decrease therapeutic effects of Hyaluronidase. Risk C: Monitor
Pitolisant: Antihistamines may decrease therapeutic effects of Pitolisant. Risk X: Avoid
Grapefruit juice increases rupatadine systemic exposure 3.5-fold. Management: Avoid grapefruit juice during therapy.
Algorithms are available for the treatment of acute rhinitis and urticaria. When treatment with a second-generation oral antihistamine is recommended, agents other than rupatadine are preferred for use during pregnancy (AAAAI/ACAAI [Dykewicz 2020], EAACI [Zuberbier 2022]).
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).
