Monograph: |
BILASTINE
BILASTINE IS A NOVEL NEW-GENERATION ANTIHISTAMINE THAT IS HIGHLY SELECTIVE FOR THE H1 HISTAMINE RECEPTOR, HAS A RAPID ONSET AND PROLONGED DURATION OF ACTION.
PHARMACOLOGY
INDICATION
FOR SYMPTOMATIC RELIEF OF NASAL AND NON-NASAL SYMPTOMS OF SEASONAL RHINITIS IN PATIENTS 12 YEARS OF AGE AND OLDER AND FOR SYMPTOMATIC RELIEF IN CHRONIC SPONTANEOUS URTICARIA IN PATIENTS 18 YEARS OF AGE AND OLDER LABEL .
PHARMACODYNAMICS
BILASTINE IS AN ANTIALLERGENIC AND ACTS TO REDUCE ALLERGIC SYMPTOMS SUCH AS NASAL CONGESTION AND URTICARIA LABEL .
MECHANISM OF ACTION
BILASTINE IS A SELECTIVE HISTAMINE H1 RECEPTOR ANTAGONIST (KI = 64NM) LABEL . DURING ALLERGIC RESPONSE MAST CELLS UNDERGO DEGRANULATION WHICH RELEASES HISTAMINE AND OTHER SUBASTANCES. BY BINDING TO AND PREVENTING ACTIVATION OF THE H1 RECEPTOR, BILASTINE REDUCES THE DEVELOPMENT OF ALLERGIC SYMPTOMS DUE TO THE RELEASE OF HISTAMINE FROM MAST CELLS.
ADDITIONAL DATA AVAILABLE
Adverse Effects
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
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ADDITIONAL DATA AVAILABLE
Contraindications
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
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ADDITIONAL DATA AVAILABLE
Blackbox Warnings
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
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ABSORPTION
BILASTINE HAS A TMAX OF 1.13 H LABEL . THE ABSOLUTE BIOAVAILABILITY IS 61%. NO ACCUMULATION OBSERVED WITH DAILY DOSING OF 20-100 MG AFTER 14 DAYS. CMAX DECREASED BY 25 % AND 33% WHEN TAKEN WITH A LOW FAT AND HIGH FAT MEAL COMPARED TO FASTED STATE. ADMINISTRATION WITH GRAPEFRUIT JUICE DECREASED CMAX BY 30%.
VOLUME OF DISTRIBUTION
NOT AVAILABLE
PROTEIN BINDING
BILASTINE IS 84-90% BOUND TO HUMAN PLASMA PROTEINS LABEL .
METABOLISM
BILASTINE DOES NOT INTERACT WITH THE CYTOCHROME P450 SYSTEM AND DOES NOT UNDERGO SIGNIFICANT METABOLISM IN HUMANS LABEL .
ROUTE OF ELIMINATION
BILASTINE IS MAINLY EXCRETED IN THE FECES (66.5%) WITH SOME EXCRETED IN THE URINE (28.3%) LABEL . NEARLY ALL IS EXCRETED AS THE PARENT COMPOUND.
HALF LIFE
THE MEAN HALF LIFE OF ELIMINATION IS 14.5H LABEL .
CLEARANCE
BILASTINE HAS A TOTAL CLEARANCE IS 9.20 L/H AND A RENAL CLEARANCE OF 8.7 L/H LABEL .
TOXICITY
THE MOST COMMON ADVERSE EFFECTS EXPERIENCED DURING CLINICAL TRIALS WERE ABDOMINAL PAIN, DIZZINESS, HEADACHE, AND SOMNOLENCE LABEL . BILASTINE IS ASSOCIATED WITH Q/T PROLONGATION. THE NO OBSERVED ADVERSE EFFECT LEVEL OF BILASTINE IS 1200 MG/KG/DAY IN RATS AND 125 MG/KG/DAY IN DOGS .
INTERACTIONS
DRUG INTERACTIONS
DRUG INTERACTION
2,5-DIMETHOXY-4-ETHYLAMPHETAMINE 2,5-DIMETHOXY-4-ETHYLAMPHETAMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
2,5-DIMETHOXY-4-ETHYLTHIOAMPHETAMINE 2,5-DIMETHOXY-4-ETHYLTHIOAMPHETAMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
4-BROMO-2,5-DIMETHOXYAMPHETAMINE 4-BROMO-2,5-DIMETHOXYAMPHETAMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
ABEXINOSTAT THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ABEXINOSTAT.
ACEBUTOLOL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ACEBUTOLOL.
ACEPROMETAZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ACEPROMETAZINE.
ACETYLDIGOXIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ACETYLDIGOXIN.
ACRIVASTINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ACRIVASTINE IS COMBINED WITH BILASTINE.
ADENOSINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ADENOSINE.
AJMALINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN AJMALINE IS COMBINED WITH BILASTINE.
ALFUZOSIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ALFUZOSIN IS COMBINED WITH BILASTINE.
ALIMEMAZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ALIMEMAZINE IS COMBINED WITH BILASTINE.
AMANTADINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN AMANTADINE IS COMBINED WITH BILASTINE.
AMIFAMPRIDINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH AMIFAMPRIDINE.
AMIODARONE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH AMIODARONE.
AMISULPRIDE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN AMISULPRIDE IS COMBINED WITH BILASTINE.
AMITRIPTYLINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH AMITRIPTYLINE.
AMODIAQUINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN AMODIAQUINE IS COMBINED WITH BILASTINE.
AMOXAPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN AMOXAPINE IS COMBINED WITH BILASTINE.
AMPHETAMINE AMPHETAMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
ANAGRELIDE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ANAGRELIDE.
ANISODAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ANISODAMINE.
ANTAZOLINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ANTAZOLINE.
APOMORPHINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN APOMORPHINE IS COMBINED WITH BILASTINE.
ARANIDIPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ARANIDIPINE IS COMBINED WITH BILASTINE.
ARFORMOTEROL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ARFORMOTEROL IS COMBINED WITH BILASTINE.
ARIPIPRAZOLE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ARIPIPRAZOLE IS COMBINED WITH BILASTINE.
ARIPIPRAZOLE LAUROXIL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ARIPIPRAZOLE LAUROXIL.
ARSENIC TRIOXIDE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ARSENIC TRIOXIDE.
ARTEMETHER THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ARTEMETHER.
ASENAPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ASENAPINE.
ASTEMIZOLE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ASTEMIZOLE.
ATAZANAVIR THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ATAZANAVIR IS COMBINED WITH BILASTINE.
ATOMOXETINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN ATOMOXETINE IS COMBINED WITH BILASTINE.
ATROPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH ATROPINE.
AZATADINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN AZATADINE IS COMBINED WITH BILASTINE.
AZIMILIDE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH AZIMILIDE.
AZITHROMYCIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH AZITHROMYCIN.
BEDAQUILINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BEDAQUILINE.
BENCYCLANE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BENCYCLANE.
BENIDIPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BENIDIPINE.
BENZATROPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BENZATROPINE IS COMBINED WITH BILASTINE.
BENZPHETAMINE BENZPHETAMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
BENZYLPENICILLOYL POLYLYSINE BILASTINE MAY DECREASE EFFECTIVENESS OF BENZYLPENICILLOYL POLYLYSINE AS A DIAGNOSTIC AGENT.
BEPRIDIL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BEPRIDIL.
BETAHISTINE THE THERAPEUTIC EFFICACY OF BETAHISTINE CAN BE DECREASED WHEN USED IN COMBINATION WITH BILASTINE.
BETAXOLOL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BETAXOLOL.
BORTEZOMIB THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BORTEZOMIB IS COMBINED WITH BILASTINE.
BRETYLIUM THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BRETYLIUM IS COMBINED WITH BILASTINE.
BROMPHENIRAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BROMPHENIRAMINE IS COMBINED WITH BILASTINE.
BUCLIZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BUCLIZINE IS COMBINED WITH BILASTINE.
BUNAFTINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BUNAFTINE.
BUPRANOLOL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BUPRANOLOL IS COMBINED WITH BILASTINE.
BUSERELIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BUSERELIN IS COMBINED WITH BILASTINE.
BUTRIPTYLINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH BUTRIPTYLINE.
CARBINOXAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CARBINOXAMINE.
CARIPORIDE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CARIPORIDE IS COMBINED WITH BILASTINE.
CELIPROLOL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CELIPROLOL IS COMBINED WITH BILASTINE.
CERITINIB THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CERITINIB.
CETIRIZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CETIRIZINE IS COMBINED WITH BILASTINE.
CHLORCYCLIZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CHLORCYCLIZINE IS COMBINED WITH BILASTINE.
CHLOROQUINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CHLOROQUINE.
CHLORPHENIRAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CHLORPHENIRAMINE.
CHLORPHENTERMINE CHLORPHENTERMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
CHLORPROMAZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CHLORPROMAZINE.
CHLORPROTHIXENE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CHLORPROTHIXENE IS COMBINED WITH BILASTINE.
CIBENZOLINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CIBENZOLINE.
CICLETANINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CICLETANINE.
CILOSTAZOL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CILOSTAZOL IS COMBINED WITH BILASTINE.
CINNARIZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CINNARIZINE.
CINOXACIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CINOXACIN.
CIPROFLOXACIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CIPROFLOXACIN.
CISAPRIDE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CISAPRIDE.
CITALOPRAM THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CITALOPRAM.
CLARITHROMYCIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CLARITHROMYCIN.
CLEMASTINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CLEMASTINE.
CLOMIPRAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CLOMIPRAMINE.
CLOZAPINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CLOZAPINE.
COCAINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH COCAINE.
COUMAPHOS THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN COUMAPHOS IS COMBINED WITH BILASTINE.
CRIZOTINIB THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CRIZOTINIB.
CUDC-101 THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CUDC-101.
CUDC-907 THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH CUDC-907.
CYCLIZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CYCLIZINE IS COMBINED WITH BILASTINE.
CYPROHEPTADINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN CYPROHEPTADINE IS COMBINED WITH BILASTINE.
DABRAFENIB THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN DABRAFENIB IS COMBINED WITH BILASTINE.
DASATINIB THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN DASATINIB IS COMBINED WITH BILASTINE.
DEGARELIX THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN DEGARELIX IS COMBINED WITH BILASTINE.
DELAFLOXACIN THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH DELAFLOXACIN.
DELAMANID BILASTINE MAY INCREASE THE QTC-PROLONGING ACTIVITIES OF DELAMANID.
DEOXYEPINEPHRINE THE THERAPEUTIC EFFICACY OF DEOXYEPINEPHRINE CAN BE INCREASED WHEN USED IN COMBINATION WITH BILASTINE.
DESFLURANE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN DESFLURANE IS COMBINED WITH BILASTINE.
DESIPRAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN DESIPRAMINE IS COMBINED WITH BILASTINE.
DESLORATADINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH DESLORATADINE.
DEUTETRABENAZINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH DEUTETRABENAZINE.
DEXBROMPHENIRAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN DEXBROMPHENIRAMINE IS COMBINED WITH BILASTINE.
DEXCHLORPHENIRAMINE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH DEXCHLORPHENIRAMINE.
DEXCHLORPHENIRAMINE MALEATE THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH DEXCHLORPHENIRAMINE MALEATE.
DEXTROAMPHETAMINE DEXTROAMPHETAMINE MAY DECREASE THE SEDATIVE AND STIMULATORY ACTIVITIES OF BILASTINE.
DEXVERAPAMIL THE RISK OR SEVERITY OF QTC PROLONGATION CAN BE INCREASED WHEN BILASTINE IS COMBINED WITH DEXVERAPAMIL.
ADDITIONAL DATA AVAILABLE
路 EXTENDED DESCRIPTION
Extended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
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路 SEVERITY
Severity
A severity rating for each drug interaction, from minor to major.
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路 EVIDENCE LEVEL
Evidence Level
A rating for the strength of the evidence supporting each drug interaction.
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路 ACTION
Action
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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FOOD INTERACTIONS
路 AVOID GRAPEFRUIT PRODUCTS. AVOID OTHER FRUIT JUICE AS WELL FOR OPTIMAL ABSORPTION.
路 TAKE ON AN EMPTY STOMACH. TAKE AT LEAST TWO HOURS BEFORE OR ONE HOUR AFTER EATING
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