Bicahis 20

Bilastine.

Each tablet contains Bilastine 20 mg.

Pharmacology: Pharmacodynamics: Histamine antagonist with selective peripheral H₁ receptor antagonist affinity and no affinity for muscarinic receptors.
Pharmacokinetics: Onset of action: 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).

Symptomatic treatment of allergic rhino-conjunctivitis (seasonal and perennial) and urticaria in adults and adolescents ( ≥ 12 years of age).

Oral: Administer with water 1 hour before or 2 hours after intake of food or fruit juices.
Adult and Geriatric: Oral: 20 mg once daily (maximum: 20 mg/day).
Children ≥ 12 years and Adolescents: Oral: 20 mg once daily (maximum: 20 mg/day).
Renal impairment: No dosage adjustment necessary.
Hepatic impairment: There is no clinical experience in patients with hepatic impairment. Since bilastine is not metabolized and renal clearance is its major elimination route, hepatic impairment is not expected to increase systemic exposure above the safety margin. Therefore, no dosage adjustment is required in patients with hepatic impairment.
Paediatric population: There is no relevant use of bilastine in children aged 0 to 2 years in the indications allergic rhino-conjunctivitis and urticaria. The safety and efficacy in children below 12 years have not yet been established.

OVERDOSE AND TREATMENT: Overdose data are limited.
After administration of bilastine at dose 10-11 times the therapeutic dose to healthy volunteers frequency of treatment emergent adverse events was two times higher than with placebo. The adverse reactions most frequently reported were dizziness, headache and nausea. No serious adverse events and no significant prolongation in the QTc interval were reported.
Symptomatic and supportive treatment is recommended.

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

(Based on the notification of the Ministry of Public Health): 1. This medicine may cause drowsiness therefore should not drive or operate machinery or working at a risk of falling from a high place.
2. Should not drink alcohol or anything that is mixed with alcohol while using this medicine.
3. Caution in children aged under 1 year, first trimester pregnant women and lactation.

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.
In patient with moderate or severe renal impairment coadministration of bilastine with P-glycoprotein inhibitors, such as e.g. ketoconazole, erythromycin, cyclosporine, ritonavir or diltiazem, may increase plasma levels of bilastine and therefore increase the risk of adverse reactions of bilastine. Therefore, coadministration of bilastine and P-glycoprotein inhibitors should be avoided in patients with moderate or severe renal impairment (bilastine is substrate for P-glycoprotein).

Information related to the use of bilastine in pregnancy is limited. For the safety, avoid using in pregnant women.
It is not known if bilastine is excreted in breastmilk.
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.

1% to 10%: Central nervous system: Drowsiness (4%), Headache (4%), Dizziness (1%).
Gastrointestinal: Upper abdominal pain (1%).
<1%: 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.

Avoid concomitant use: Avoid concomitant use of bilastine with any of the following: Aclidinium, Azelastine (nasal), Cimetropium, Eluxadoline, Glucagon, Glycopyrrolate (oral inhalation), Ipratropium (oral inhalation), Levosulpiride, Nitroglycerin, Orphenadrine, Oxatomide, Oxomemazine, Paraldehyde, Potassium chloride, Thalidomide, Tiotropium, Umeclidinium.
Increased effect/Toxicity: Bilastine may increase the levels/effects of: Abobotulinumtoxin A, Alcohol (Ethyl), Analgesics (Opioid), Anticholinergic agents, Azelastine (Nasal), Blonanserin, Buprenorphine, Cimetropium, CNS Depressants, Eluxadoline, Flunitrazepam, Glucagon, Glycopyrrolate (Oral Inhalation), Hydrocodone, Methotrimeprazine, Metyrosine, Mirabegron, Mirtazapine, Onabotulinumtoxin A, Orphenadrine, Oxycodone, Paraldehyde, Piribedil, Potassium chloride, Pramipexole, Ramosetron, Rimabotulinumtoxin B, Ropinirole, Rotigotine; Selective Serotonin Reuptake Inhibitors, Suvorexant, Thalidomide, Thiazide and Thiazide-Like Diuretics, Tiotropium, Topiramate, Zolpidem.
The levels/effects of bilastine may be increased by: Aclidinium; Brimonidine (Topical); Canabis; Chloral Betaine; Chlormethiazole; Chlorphenesin Carbamate; Dimethindene (Topical); Doxylamine; Dronabinol; Droperidol; Hydroxyzine; Ipratropium (Oral inhalation) Kava Kava; Lofexidine; Lumacaftor, Magnesium sulfate, Methotrimeprazine; Mianserin; Minocycline; Nabione; Oxatomide; Oxomemazine; Perampanel; P-glycoprotein/ABCB1 Inhibitors; Pramlintide; Ranolazine; Rufinamide; Sodium oxybate; Tapentadol: Tetrahydrocannabinol; Trimeprazine; Umeclidinium.
Decreased effect: Bilastine may decrease the levels/effects of: Acetylcholinesterase inhibitors; Benzylpenicilloyl Polylysine; Betahistine; Gastrointestinal agents (Prokinetic); Hyaluronidase, Itopride, Levosulpiride; Nitroglycerin; Secretin.
The levels/effects of bilastine may be decreased by: Acetylcholinesterase inhibitor; Amphetamines; Grape fruit juice; Lumacaftor; P-glycoprotein/ABCB1 inducers.
Other drug-drug interaction: Interaction with ketoconazole or erythromycin: Concomitant intake of bilastine and ketoconazole or erythromycin increased bilastine AUC 2-fold and C_max 2-3 fold. These changes do not appear to affect the safety profile.
Interaction with diltiazem: Concomitant intake of bilastine and diltiazem increased C_max of bilastine by 50% and does not appear to affect the safety profile.
Food interaction: 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.

Store below 30°C.

Antihistamines & Antiallergics

R06AX29 - bilastine ; Belongs to the class of other antihistamines for systemic use.

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