Bilastine (United States: Not available): Drug information

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

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)

Brand Names: Canada

Blexten

Pharmacologic Category

Histamine H₁ Antagonist;
Histamine H₁ Antagonist, Second Generation;
Piperidine Derivative

Dosing: Adult

Allergic rhinitis

Allergic rhinitis: Oral: 20 mg once daily (maximum: 20 mg/day).

Urticaria, chronic spontaneous

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).

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

No dosage adjustment necessary.

Dosing: Hepatic Impairment: Adult

No dosage adjustment necessary.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

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

Allergic rhinitis, seasonal

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

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.

Dosing: Kidney Impairment: Pediatric

Altered kidney function: Children ≥4 years weighing ≥16 kg and Adolescents: Oral: No dosage adjustment necessary.

Dosing: Hepatic Impairment: Pediatric

Children ≥4 years weighing ≥16 kg and Adolescents: Oral: No dosage adjustment necessary.

Adverse Reactions

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

1% to 10%:

Central nervous system: Drowsiness (4%), headache (4%), dizziness (1%)

Gastrointestinal: Upper abdominal pain (1%)

<1%, postmarketing, and/or case reports: Abdominal pain, abnormal T waves on ECG, acneiform eruption, anxiety, asthenia, back pain, chest discomfort, constipation, diarrhea, disturbance in attention, dry nose, dysgeusia, dyspepsia, dyspnea, ECG abnormality, epistaxis, eructation, eye pain, fatigue, fever, gastritis, hypersensitivity reaction, hypersomnia, increased appetite, increased gamma-glutamyl transferase, increased serum alanine aminotransferase, increased serum aspartate aminotransferase, increased serum bilirubin, increased serum cholesterol, increased serum triglycerides, increased thirst, insomnia, inversion T wave on ECG, jitteriness, malaise, menstrual disease (delayed), motion sickness, myalgia, myasthenia, nasal discomfort, nausea, nightmares, oral herpes simplex infection, pain, palpitations, papular rash, pharyngitis, prolonged QT interval on ECG, pruritus, right bundle branch block, sinus arrhythmia, sinus bradycardia, stomach discomfort, ST segment changes on ECG, tachycardia, throat irritation, tinnitus, urticaria, ventricular premature contractions, vertigo, vomiting, weight gain, weight loss, widened QRS complex on ECG, xerostomia

Contraindications

Hypersensitivity to bilastine or any component of the formulation; history of QT prolongation and/or torsades de pointes, including congenital long QT syndromes.

Warnings/Precautions

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.

Product Availability

Not available in the United States.

Generic Equivalent Available: US

May be product dependent

Dosage Forms: Canada

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

Tablet Disintegrating, Oral:

Blexten: 10 mg

Administration: Adult

Oral: Administer with water 1 hour before or 2 hours after intake of food or fruit juices.

Administration: Pediatric

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).

Use: Labeled Indications

Note: Not approved in the United States.

Allergic rhinitis: Relief of symptoms associated with seasonal allergic rhinitis in patients ≥4 years of age and weighing ≥16 kg.

Chronic spontaneous urticaria: Symptomatic treatment of adults with chronic spontaneous urticaria (eg, pruritus, hives) in patients ≥4 years of age and weighing ≥16 kg.

Metabolism/Transport Effects

Substrate of P-glycoprotein/ABCB1 (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

Asciminib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). 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

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

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

Elacestrant: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

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

Erdafitinib: May increase the 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

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

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

Futibatinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

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

Gilteritinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). 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 decrease the serum concentration of Bilastine. Risk C: Monitor therapy

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. 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

Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). 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

Loop Diuretics: May enhance the QTc-prolonging effect of Bilastine. Risk C: Monitor therapy

Lumacaftor and Ivacaftor: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may decrease the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). 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

Mitapivat: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). 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

Pacritinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

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

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Bilastine. Risk X: Avoid combination

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

Pretomanid: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

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

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect 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 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

Sotorasib: May increase the 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 the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

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

Taurursodiol: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

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

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.

Pregnancy Considerations

Information related to the use of bilastine in pregnancy is limited.

Antihistamines may be used for the treatment of rhinitis and urticaria in pregnant women. Although second generation antihistamines are preferred, agents other than bilastine are currently recommended (Murase 2014; Scadding 2017; Zuberbier 2018).

Breastfeeding Considerations

It is not known if bilastine is present in breast milk.

According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

Relief of symptoms

Mechanism of Action

Histamine antagonist with selective peripheral H₁ receptor antagonist affinity and no affinity for muscarinic receptors.

Pharmacokinetics (Adult Data Unless Noted)

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)

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Bilaxten;
(AR) Argentina: Bilidren;
(AT) Austria: Olisir | Rhinolibre;
(AU) Australia: Allertine;
(BD) Bangladesh: Allertin | Bilamin | Bilan | Bilastin | Bilista | Biltin | Bislor | Zilas;
(BE) Belgium: Bellozal | Bilastine ab | Bilastine eg | Ilexel;
(BF) Burkina Faso: Bilaxten;
(BG) Bulgaria: Bilergia | Fortecal | Fortecal children | Fortecal for children;
(BR) Brazil: Alektos | Alektos ped | Bilastina | Bilastina ems | Bilastina neo quimica | Hisbila | Naire | Tynna;
(CH) Switzerland: Bilastin zentiva | Bilaxten;
(CI) Côte d'Ivoire: Bilaxten;
(CL) Chile: Bilidren | Blaxitec;
(CO) Colombia: Bilaxten;
(CZ) Czech Republic: Bilastine glenmark | Nestibil | Xados;
(DE) Germany: Bitosen;
(DO) Dominican Republic: Bilaxten | Blaxitec;
(EC) Ecuador: Alerin | Bilaxten;
(EE) Estonia: Bilastine zentiva | Opexa;
(EG) Egypt: Pharmabilast;
(ES) Spain: Abisax | Abrilia | Bilastina alter | Bilastina aristo | Bilastina cinfa | Bilastina Kern Pharma | Bilastina mylan | Bilastina Normon | Bilastina pensa | Bilastina ratiopharm | Bilastina sandoz | Bilastina stada | Bilastina tecnigen | Bilastina teva | Bilaxten | Ibis | Obalix;
(FI) Finland: Revitelle;
(FR) France: Bilaska | Bilastine biogaran | Bilastine eg | Bilastine teva | Bilastine viatris | Bilastine zentiva | Inorial;
(GB) United Kingdom: Ilaxten;
(GR) Greece: Bilargen | Bilaz;
(HK) Hong Kong: Labixten;
(HR) Croatia: Nixar;
(HU) Hungary: Bilastine stada | Bilastine teva | Bilergin | Lendin;
(IE) Ireland: Drynol;
(IN) India: Actv 24 | Akubliss | Allerblis | Antegy | Ata | Belatin | Belaxid | Beltas | Beltas forte | Bil1 | Bilabest | Bilacad | Bilacalm | Bilachek | Biladerm | Bilafav | Bilafem od | Bilagra | Bilahenz | Bilahist | Bilajoy | Bilambic | Bilamed | Bilamove | Bilanair | Bilanix | Bilanta | Bilaset | Bilashine | Bilashine dt | Bilast | Bilastero | Bilastibel | Bilasure | Bilatop | Bilaxta | Bilaxten | Bilazap | Bilazest | Bilazest kids | Bilazo | Bilbay | Bilkwik | Billacare | Billargic | Billasi | Bilmegh | Bilten | Bistadin | Bl 24 | Blson | Bularid l | Byloza | Cosome ar | Elbel | Histabil | Mastowell | Maxstine | Nilhist | Nohives | Prucros | Prulastin | Ubil;
(IT) Italy: Arynal | Ayrinal | Bilastina aristo | Bilastina doc | Bilastina eg | Bilastina mylan | Bilastina sandoz | Bilatina zentiva | Olisir | Robilas;
(JO) Jordan: Bilaxten | Lesstab;
(JP) Japan: Bilanoa | Bilanoa od;
(KE) Kenya: Ilaxten;
(KW) Kuwait: Bilaxten;
(LB) Lebanon: Labixten;
(LT) Lithuania: Opexa;
(LU) Luxembourg: Bellozal;
(LV) Latvia: Opexa;
(MA) Morocco: Labixten;
(MX) Mexico: Blaxitec | Labixten;
(MY) Malaysia: Bilaxten;
(NO) Norway: Zilas;
(NZ) New Zealand: Labixten;
(PE) Peru: Bilaxten;
(PH) Philippines: Bilaxten;
(PL) Poland: Adablix | Bilaflex | Bilagra | Bilant | Bilargena | Bilastine aristo | Bilaxten | Clatexo | Clatra;
(PT) Portugal: Bilastina aristo | Bilastina azevedos | Bilastina bluepharma | Bilastina ciclum | Bilastina farmoz | Bilastina pharmakern | Bilastina teva | Bilastina tolife | Bilastina zentiva | Bilaxten | Lergonix;
(PY) Paraguay: Bilaxten;
(QA) Qatar: Bilaxten;
(RO) Romania: Borenar;
(RU) Russian Federation: Nixar;
(SA) Saudi Arabia: Bilaxten;
(SE) Sweden: Bilaxten;
(SG) Singapore: Bilaxten;
(SI) Slovenia: Bilador;
(SK) Slovakia: Bilastin stada | Nestibil | Omarit;
(TH) Thailand: Bilaxten;
(TR) Turkey: Bilaxten;
(TW) Taiwan: Labixten;
(UA) Ukraine: Nixar;
(VE) Venezuela, Bolivarian Republic of: Labixten;
(VN) Viet Nam: Timbivo;
(ZA) South Africa: Ilaxten

Blexten (bilastine) [product monograph]. Mississauga, Ontario, Canada: Aralez Pharmaceuticals Canada Inc; August 2021.
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Scadding GK, Kariyawasam HH, Scadding G, et al. BSACI guideline for the diagnosis and management of allergic and non-allergic rhinitis (revised edition 2017; first edition 2007). Clin Exp Allergy. 2017;47(7):856‐889. doi:10.1111/cea.12953 [PubMed 30239057]
Weller K, Church MK, Hawro T, et al. Updosing of bilastine is effective in moderate to severe chronic spontaneous urticaria: a real-life study. Allergy. 2018;73(10):2073-2075. doi:10.1111/all.13494 [PubMed 29869790]
Zuberbier T, Aberer W, Asero R, et al. The EAACI/GA²LEN/EDF/WAO guideline for the definition, classification, diagnosis and management of urticaria. Allergy. 2018;73(7):1393‐1414. doi:10.1111/all.13397 [PubMed 29336054]

Topic 112241 Version 135.0

خرید پکیج

Bilastine (United States: Not available): Drug information