Version July 2025
Allergic rhinitis, seasonal:
Children ≥4 to 11 years weighing ≥16 kg: Oral: 10 mg once daily.
Children ≥12 years and Adolescents: Oral: 20 mg once daily.
Urticaria, chronic spontaneous: Note: Considered first-line therapy for management of chronic urticaria; if response inadequate after 2 to 4 weeks of therapy or symptoms intolerable, consider increasing the dose of bilastine (as age and weight permit) as second-line treatment rather than changing therapy (Ref).
Children ≥4 to 11 years weighing ≥16 kg: Oral: 10 mg once daily.
Children ≥12 years and Adolescents: Oral: 20 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.
Altered kidney function: Children ≥4 years weighing ≥16 kg and Adolescents: Oral: No dosage adjustment necessary.
Children ≥4 years weighing ≥16 kg and Adolescents: Oral: No dosage adjustment necessary.
(For additional information see "Bilastine (United States: Not available): Drug information")
Allergic rhinitis: Oral: 20 mg once daily (maximum: 20 mg/day).
Urticaria, chronic spontaneous: Oral: Initial: 20 mg once daily. If symptom control is inadequate after 2 weeks, may increase to 40 mg once daily; if symptoms remain uncontrolled after an additional 2 weeks, may increase to 80 mg once daily (Ref). 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.
No dosage adjustment necessary.
No dosage adjustment necessary.
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%:
Gastrointestinal: Upper abdominal pain (1%)
Nervous system: Dizziness (1%), drowsiness (4%), headache (children, adolescents, adults: 2% to 4%)
<1%:
Cardiovascular: Chest discomfort, ECG abnormality (including abnormal T waves on ECG, inversion T wave on ECG, prolonged QT interval on ECG, ST segment changes on ECG, widened QRS complex on ECG), premature ventricular contractions, right bundle branch block, sinoatrial nodal rhythm disorder, sinus bradycardia, syncope (children)
Dermatologic: Acneiform eruption, eczema (children), papular rash, pruritus, urticaria (children, adolescents, adults)
Endocrine & metabolic: Increased thirst, menstrual disease (delayed)
Gastrointestinal: Abdominal pain, constipation, diarrhea (children, adolescents, adults), dysgeusia, dyspepsia, eructation, gastritis, increased appetite, motion sickness, nausea (children, adolescents, adults), oral herpes simplex infection, stomach discomfort, vomiting, xerostomia (including dry tongue)
Hematologic & oncologic: Anemia
Hypersensitivity: Swelling of lips (children)
Nervous system: Anxiety, asthenia, disturbance in attention, fatigue (children, adolescents, adults), hypersomnia, insomnia, jitteriness, loss of consciousness (children), malaise, myasthenia, nightmares, pain, vertigo
Neuromuscular & skeletal: Back pain, myalgia
Ophthalmic: Eye irritation (children), eye pain
Otic: Tinnitus
Respiratory: Dry nose, dyspnea, epistaxis, nasal discomfort, pharyngitis, throat irritation
Miscellaneous: Fever
Frequency not defined:
Endocrine & metabolic: Hypercholesterolemia, increased serum triglycerides, weight gain, weight loss
Hepatic: Increased gamma-glutamyl transferase, increased serum alanine aminotransferase, increased serum aspartate aminotransferase, increased serum bilirubin
Postmarketing (any population):
Cardiovascular: Palpitations, tachycardia
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis, angioedema)
Hypersensitivity to bilastine or any component of the formulation; history of QT prolongation and/or torsades de pointes, including congenital long QT syndromes.
Disease-related concerns:
• QT interval prolongation: QTc interval prolongation has been reported with use; use is contraindicated in patients with a history of QT prolongation and/or Torsade de pointes, including congenital long QT syndromes. Use caution in patients with a history of cardiac arrhythmia, significant bradycardia, a family history of sudden cardiac death, electrolyte abnormalities (eg, hypokalemia, hypomagnesemia), or with concomitant use of other QTc-prolonging drugs.
Not available in the United States.
No
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Oral:
Blexten: 2.5 mg/mL (120 mL) [contains methylparaben, propylparaben]
Tablet, Oral:
Blexten: 20 mg
Generic: 20 mg
Tablet Disintegrating, Oral:
Blexten: 10 mg
Oral: Administer with water 1 hour before or 2 hours after intake of food or fruit juices.
Oral dispersible tablet: Place on tongue to allow tablet to dissolve so it can be easily swallowed. May also disperse in water prior to administration.
Oral solution: Administer with an accurate measuring device (dosing cup provided); do not use a household teaspoon (overdosage may occur).
Oral: Administer with water 1 hour before or 2 hours after intake of food or fruit juices.
Store at 15°C to 30°C (59°F to 86°F).
Note: Not approved in the United States.
Canadian labeling: Relief of symptoms (nasal and non-nasal) associated with seasonal allergic rhinitis (indicated for patients ≥4 years of age and weighing ≥16 kg); symptomatic treatment of chronic spontaneous urticaria (eg, pruritus, hives) (indicated for patients ≥4 years of age and weighing ≥16 kg).
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (pediatric liquid medications requiring measurement) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (chemotherapeutic agent, parenteral and oral; contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care and Community/Ambulatory Care Settings).
Substrate of P-glycoprotein (Major with inhibitors), P-glycoprotein (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
Asciminib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). 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
Elacestrant: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Erdafitinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: If coadministration with these narrow therapeutic index/sensitive P-gp substrates is unavoidable, separate erdafitinib administration by at least 6 hours before or after administration of these P-gp substrates. Risk D: Consider Therapy Modification
Futibatinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Gilteritinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Grapefruit Juice: May decrease serum concentration of Bilastine. Risk C: Monitor
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may increase QTc-prolonging effects of Haloperidol. Risk C: Monitor
Hyaluronidase: Antihistamines may decrease therapeutic effects of Hyaluronidase. Risk C: Monitor
Lasmiditan: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Levacetylleucine: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Lonafarnib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors). Risk C: Monitor
Loop Diuretics: May increase QTc-prolonging effects of Bilastine. Risk C: Monitor
Lumacaftor and Ivacaftor: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may decrease serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Risk C: Monitor
Mitapivat: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
P-glycoprotein/ABCB1 Inhibitors: May increase serum concentration of Bilastine. Risk X: Avoid
Pacritinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Pitolisant: Antihistamines may decrease therapeutic effects of Pitolisant. Risk X: Avoid
Pretomanid: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Primaquine: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may increase QTc-prolonging effects of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor
Sotorasib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: Consider avoiding use of sotorasib and narrow therapeutic index/sensitive P-gp substrates. If combined use is unavoidable, monitor for increased toxicities of the substrate and consider a decrease in the substrate dosage. Risk D: Consider Therapy Modification
Sparsentan: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Taurursodiol: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid
Venetoclax: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: Avoid concomitant use of venetoclax and oral p-glycoprotein (P-gp) substrates if possible. If combined use is unavoidable, administer the P-gp substrate at least 6 hours before venetoclax to minimize the potential for an interaction. Risk D: Consider Therapy Modification
Vimseltinib: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors). Management: Avoid concomitant use of vimseltinib and P-gp substrates when possible. If combined, administer vimseltinib at least 4 hours before the P-gp substrate. Risk D: Consider Therapy Modification
Xanomeline: May increase serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor
Food: Decreases bioavailability by 33%. Management: Administer 1 hour before or 2 hours after intake of food.
Grapefruit juice: Decreases bioavailability by 30%. This effect may also apply to other fruit juices. Management: Administer 1 hour before or 2 hours after intake of grapefruit juice or other fruit juices.
Outcome data related to the use of bilastine in pregnancy are limited. Based on the limitations of available data, second-generation antihistamines are considered acceptable for use during pregnancy, with preference given to agents with more study (EAACI [Zuberbier 2022]).
Algorithms are available for the treatment of acute rhinitis and urticaria. When treatment with a second-generation oral antihistamine is recommended, agents other than bilastine are preferred for use during pregnancy (AAAAI/ACAAI [Dykewicz 2020], BAD [Sabroe 2022], EAACI [Zuberbier 2022]).
Histamine antagonist with selective peripheral H1 receptor antagonist affinity and no affinity for muscarinic receptors.
Onset: 1 hour
Duration: 26 hours
Absorption: Rapid
Protein binding: 84% to 90%
Metabolism: Minimal (~5% of dose)
Bioavailability: ~61%
Half-life elimination: ~14.5 hours
Time to peak: 1.13 hours
Excretion: Feces (67%, as unchanged bilastine); Urine (28%, as unchanged bilastine)
