Bilastine

R06A - Antihistamines for systemic use ATC R06AX29 Small molecule Natural product

JFDA label: Bilaxten 20mg

Mechanism of Action

Inverse Agonist of Histamine H1 receptor — Histamine H1 receptor inverse agonist

Target	Action	Gene / class
Histamine H1 receptor efficacy	INVERSE AGONIST	HRH1

Indications

Approved

Allergic rhinitis
Chronic spontaneous urticaria

Contraindications

Source: Lexicomp

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

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Nervous system disorders (4)

Common Central nervous system dysfunction · dizziness · drowsiness · headache

Gastrointestinal disorders (1)

Common Upper abdominal pain

Dosing

Source: Lexicomp

Seasonal allergic rhinitis, chronic spontaneous urticaria: Oral: 20 mg once daily (maximum: 20 mg/day)

Seasonal allergic rhinitis: Children ≥12 years and Adolescents: Oral: Refer to adult dosing

Refer to adult dosing.

No dosage adjustment necessary.

Warnings & Precautions

Source: Lexicomp

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. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Pregnancy & Lactation

Pregnancy

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; Wallace 2008; Zuberbier 2014)

Lactation

It is not known if bilastine is excreted in breast-milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

LactMed: monitor the infant.

Monitoring

Clinical pearl	Relief of symptoms

Chemistry & Properties

Formula	C28H37N3O3
Molecular weight	463.62 g/mol
IUPAC name	2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
CAS	202189-78-4
PubChem CID	185460
InChIKey	`ACCMWZWAEFYUGZ-UHFFFAOYSA-N`
logP	4.86 (XLogP 2.3)
Polar surface area	67.59 Å²
H-bond acceptors / donors	5 / 1
Drug-likeness (QED)	0.44
Lipinski violations	0

SMILES

CCOCCn1c(C2CCN(CCc3ccc(C(C)(C)C(=O)O)cc3)CC2)nc2ccccc21

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP3A4	Substrate	—

Receptor binding (top 1)

Target	Action	Affinity
H1 receptor (HRH1)	Antagonist	pKi 7.2

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (4)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Lesstab	Tablet 20.000 mg	20 tab	UNITED PHARM.MFG.CO.LTD(UPM)/JORDAN	5.240
Bilaxten	Tablet 20 mg	20 tab	Hikma Pharmaceuticals Co.Ltd/Jordan	6.550
Bilaxten 2.5mg Oral solution	Solution 2.5 mg/1 ml	120 ml	Hikma Pharmaceuticals Co.Ltd/Jordan	6.700
Bilaxten 10mg Oral dispersible tablets	Tablet 10 mg	30 tab	Hikma Pharmaceuticals Co.Ltd/Jordan	6.750