BILAXTEN Bilastine 20mg Tablet 1's
RXDRUG-DR-XY43523-1pc
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Symptomatic treatment of seasonal & perennial allergic rhino-conjunctivitis & urticaria.
Dosage/Direction for Use
Adults and Adolescents ≥12 years: Allergic Rhino-conjunctivitis (SAR and PAR) and Urticaria: 20 mg (1 tablet) once daily.
Elderly: No dosage adjustments are required in elderly patients (see Pharmacodynamics and Pharmacokinetics under Actions). There is little experience in patients >65 years.
Renal Impairment: No dosage adjustment is required in patients with renal impairment (see Pharmacokinetics under Actions).
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 (see Pharmacokinetics under Actions).
Duration of Treatment: For allergic rhinitis the treatment should be limited to the period of exposure to allergens. For seasonal allergic rhinitis, treatment could be discontinued after the symptoms have resolved and reinitiated upon their reappearance. In perennial allergic rhinitis continued treatment may be proposed to the patients during the allergen exposure periods. For urticaria the duration of treatment depends on the type, duration and course of the complaints.
Administration: The tablet should be taken by oral route 1 hr before or 2 hrs after intake of food or fruit juice. It is recommended to take the daily dose in 1 single intake.
Elderly: No dosage adjustments are required in elderly patients (see Pharmacodynamics and Pharmacokinetics under Actions). There is little experience in patients >65 years.
Renal Impairment: No dosage adjustment is required in patients with renal impairment (see Pharmacokinetics under Actions).
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 (see Pharmacokinetics under Actions).
Duration of Treatment: For allergic rhinitis the treatment should be limited to the period of exposure to allergens. For seasonal allergic rhinitis, treatment could be discontinued after the symptoms have resolved and reinitiated upon their reappearance. In perennial allergic rhinitis continued treatment may be proposed to the patients during the allergen exposure periods. For urticaria the duration of treatment depends on the type, duration and course of the complaints.
Administration: The tablet should be taken by oral route 1 hr before or 2 hrs after intake of food or fruit juice. It is recommended to take the daily dose in 1 single intake.
Overdosage
Information regarding acute overdose is limited to experience from clinical trials conducted during the development of bilastine. After administration of bilastine at doses 10-11 times the therapeutic dose [220 mg (single dose); or 200 mg/day for 7 days] to healthy volunteers, frequency of treatment emergent adverse events was 2 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.
Critical evaluation of bilastine's multiple dose (100 mg x 4 days) effect on ventricular repolarization by a "thorough QT/QTc cross-over study" involving 30 healthy volunteers did not show significant QTc prolongation.
In the event of overdose, symptomatic and supportive treatment is recommended.
There is no known specific antidote to bilastine.
Critical evaluation of bilastine's multiple dose (100 mg x 4 days) effect on ventricular repolarization by a "thorough QT/QTc cross-over study" involving 30 healthy volunteers did not show significant QTc prolongation.
In the event of overdose, symptomatic and supportive treatment is recommended.
There is no known specific antidote to bilastine.
Administration
Should be taken on an empty stomach: Take 1 hr before or 2 hr after intake of food or fruit juice.
Contraindications
Hypersensitivity to bilastine or to any of the excipients of Bilaxten.
Special Precautions
In patients with moderate or severe renal impairment, co-administration of bilastine with P-gp inhibitors eg, ketoconazole, erythromycin, cyclosporine, ritonavir or diltiazem, may increase plasmatic levels of bilastine and therefore increase the risk of adverse effects of bilastine. Therefore, co-administration of bilastine and P-gp inhibitors should be avoided in patients with moderate or severe renal impairment.
Effects on the Ability to Drive or Operate Machinery: A study performed to assess the effects of bilastine on the ability to drive demonstrated that treatment with 20 mg did not affect the driving performance. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or use machines.
Impairment of Fertility: There are no or limited amount of clinical data. A study in rats did not indicate any negative effect on fertility (see Toxicology: Preclinical Safety Data under Actions).
Use in pregnancy & lactation: There are no or limited amount of data from the use of bilastine in pregnant women.
Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity, parturition or postnatal development (see Toxicology: Preclinical Safety Data under Actions). As a precautionary measure, it is preferable to avoid the use of Bilaxten during pregnancy.
It is unknown whether bilastine is excreted in human breast milk. The excretion of bilastine in milk has not been studied in animals. A decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with Bilaxten should be made taking into account the benefit of breastfeeding to the child and the benefit of bilastine therapy to the mother.
Use in children: The safety and efficacy of bilastine in children <12 years have not been established.
Effects on the Ability to Drive or Operate Machinery: A study performed to assess the effects of bilastine on the ability to drive demonstrated that treatment with 20 mg did not affect the driving performance. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or use machines.
Impairment of Fertility: There are no or limited amount of clinical data. A study in rats did not indicate any negative effect on fertility (see Toxicology: Preclinical Safety Data under Actions).
Use in pregnancy & lactation: There are no or limited amount of data from the use of bilastine in pregnant women.
Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity, parturition or postnatal development (see Toxicology: Preclinical Safety Data under Actions). As a precautionary measure, it is preferable to avoid the use of Bilaxten during pregnancy.
It is unknown whether bilastine is excreted in human breast milk. The excretion of bilastine in milk has not been studied in animals. A decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with Bilaxten should be made taking into account the benefit of breastfeeding to the child and the benefit of bilastine therapy to the mother.
Use in children: The safety and efficacy of bilastine in children <12 years have not been established.
Use In Pregnancy & Lactation
There are no or limited amount of data from the use of bilastine in pregnant women.
Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity, parturition or postnatal development (see Toxicology: Preclinical Safety Data under Actions). As a precautionary measure, it is preferable to avoid the use of Bilaxten during pregnancy.
It is unknown whether bilastine is excreted in human breast milk. The excretion of bilastine in milk has not been studied in animals. A decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with Bilaxten should be made taking into account the benefit of breastfeeding to the child and the benefit of bilastine therapy to the mother.
Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity, parturition or postnatal development (see Toxicology: Preclinical Safety Data under Actions). As a precautionary measure, it is preferable to avoid the use of Bilaxten during pregnancy.
It is unknown whether bilastine is excreted in human breast milk. The excretion of bilastine in milk has not been studied in animals. A decision on whether to continue/discontinue breastfeeding or to continue/discontinue therapy with Bilaxten should be made taking into account the benefit of breastfeeding to the child and the benefit of bilastine therapy to the mother.
Adverse Reactions
The number of adverse events experienced by patients suffering from allergic rhino-conjunctivitis or chronic idiopathic urticaria treated with bilastine 20 mg in clinical trials was comparable with patients receiving placebo (12.7% vs 12.8%).
The adverse drug reactions (ADRs) most commonly reported by patients receiving bilastine 20 mg during phase II and III clinical trials were headache, somnolence, dizziness and fatigue. These adverse events occurred with a comparable frequency in patients receiving placebo.
The adverse drug reactions (ADRs) most commonly reported by patients receiving bilastine 20 mg during phase II and III clinical trials were headache, somnolence, dizziness and fatigue. These adverse events occurred with a comparable frequency in patients receiving placebo.
Drug Interactions
Interaction with Food: Food significantly reduces the oral bioavailability of bilastine by 30%.
Interaction with Grapefruit Juice: Concomitant intake of bilastine 20 mg and grapefruit juice decreased bilastine bioavailability by 30%. This effect may also apply to other fruit juices. The degree of bioavailability decrease may vary between producers and fruits. The mechanism for this interaction is an inhibition of OATP1A2, an uptake transporter for which bilastine is a substrate (see Pharmacokinetics under Actions). Medicinal products that are substrates or inhibitors of OATP1A2 eg, ritonavir or rifampicin, may likewise have the potential to decrease plasma concentrations of bilastine.
Interaction with Ketoconazole or Erythromycin: Concomitant intake of bilastine and ketoconazole or erythromycin increased bilastine AUC 2-fold and Cmax 2-3 fold. These changes can be explained by interaction with intestinal efflux transporters, since bilastine is substrate for P-gp and not metabolized (see Pharmacokinetics under Actions).
These changes do not appear to affect the safety profile of bilastine and ketoconazole or erythromycin, respectively.
Other medicinal products that are substrates or inhibitors of P-gp eg, cyclosporine, may likewise have the potential to increase plasma concentrations of bilastine.
Interaction with Diltiazem: Concomitant intake of bilastine 20 mg and diltiazem 60 mg increased Cmax of bilastine by 50%. This effect can be explained by interaction with intestinal efflux transporters and does not appear to affect the safety profile of bilastine.
Interaction with Alcohol: The psychomotor performance after concomitant intake of alcohol and bilastine 20 mg was similar to that observed after intake of alcohol and placebo.
Interaction with Lorazepam: Concomitant intake of bilastine 20 mg and lorazepam 3 mg for 8 days did not potentiate the depressant CNS effects of lorazepam.
Incompatibilities: Not applicable.
Interaction with Grapefruit Juice: Concomitant intake of bilastine 20 mg and grapefruit juice decreased bilastine bioavailability by 30%. This effect may also apply to other fruit juices. The degree of bioavailability decrease may vary between producers and fruits. The mechanism for this interaction is an inhibition of OATP1A2, an uptake transporter for which bilastine is a substrate (see Pharmacokinetics under Actions). Medicinal products that are substrates or inhibitors of OATP1A2 eg, ritonavir or rifampicin, may likewise have the potential to decrease plasma concentrations of bilastine.
Interaction with Ketoconazole or Erythromycin: Concomitant intake of bilastine and ketoconazole or erythromycin increased bilastine AUC 2-fold and Cmax 2-3 fold. These changes can be explained by interaction with intestinal efflux transporters, since bilastine is substrate for P-gp and not metabolized (see Pharmacokinetics under Actions).
These changes do not appear to affect the safety profile of bilastine and ketoconazole or erythromycin, respectively.
Other medicinal products that are substrates or inhibitors of P-gp eg, cyclosporine, may likewise have the potential to increase plasma concentrations of bilastine.
Interaction with Diltiazem: Concomitant intake of bilastine 20 mg and diltiazem 60 mg increased Cmax of bilastine by 50%. This effect can be explained by interaction with intestinal efflux transporters and does not appear to affect the safety profile of bilastine.
Interaction with Alcohol: The psychomotor performance after concomitant intake of alcohol and bilastine 20 mg was similar to that observed after intake of alcohol and placebo.
Interaction with Lorazepam: Concomitant intake of bilastine 20 mg and lorazepam 3 mg for 8 days did not potentiate the depressant CNS effects of lorazepam.
Incompatibilities: Not applicable.
Caution For Usage
Instructions for Use and Handling: No special requirements. Any unused product or waste material should be disposed of in accordance with local requirements.
Storage
Store below 30°C.
Shelf-Life: 5 years.
Shelf-Life: 5 years.
Action
Pharmacotherapeutic Group: Antihistamines for systemic use, other antihistamines for systemic use. ATC Code: R06AX29.
Pharmacology: Pharmacodynamics: Bilastine is a non-sedating, long-acting histamine antagonist with selective peripheral H1-receptor antagonist affinity and no affinity for muscarinic receptors. Bilastine inhibited histamine-induced wheal and flare skin reactions for 24 hrs following single doses.
In clinical trials performed in adult and adolescent patients with allergic rhino-conjunctivitis (seasonal and perennial), bilastine 20 mg, administered once daily for 14-28 days, was effective in relieving symptoms eg, sneezing, nasal discharge, nasal itching, nasal congestion, ocular itching, tearing and ocular redness. Bilastine effectively controlled symptoms for 24 hrs.
In 2 clinical trials performed in patients with chronic idiopathic urticaria, bilastine 20 mg, administered once daily for 28 days was effective in relieving the itching intensity and the number and size of wheals, as well as the patients discomfort due to urticaria. Patients improved their sleep conditions and their quality of life.
No clinically relevant prolongation of QTc interval or any other cardiovascular effect has been observed in the clinical trials performed with bilastine, even at doses of 200 mg daily (10 times the clinical dose) for 7 days in 9 subjects, or even when co-administered with P-glycoprotein (P-gp) inhibitors eg, ketoconazole (24 subjects) and erythromycin (24 subjects). Additionally, a thorough QT study including 30 volunteers has been performed.
In controlled clinical trials at the recommended dose of 20 mg once daily, the central nervous system (CNS) safety profile of bilastine was similar to placebo and the incidence of somnolence was not statistically different from placebo. Bilastine at doses of up to 40 mg once daily did not affect psychomotor performance in clinical trials and driving performance in a standard driving test.
Elderly patients (≥65 years) included in phase II and III studies showed no difference in efficacy or safety with respect to younger patients.
Pharmacology: Pharmacodynamics: Bilastine is a non-sedating, long-acting histamine antagonist with selective peripheral H1-receptor antagonist affinity and no affinity for muscarinic receptors. Bilastine inhibited histamine-induced wheal and flare skin reactions for 24 hrs following single doses.
In clinical trials performed in adult and adolescent patients with allergic rhino-conjunctivitis (seasonal and perennial), bilastine 20 mg, administered once daily for 14-28 days, was effective in relieving symptoms eg, sneezing, nasal discharge, nasal itching, nasal congestion, ocular itching, tearing and ocular redness. Bilastine effectively controlled symptoms for 24 hrs.
In 2 clinical trials performed in patients with chronic idiopathic urticaria, bilastine 20 mg, administered once daily for 28 days was effective in relieving the itching intensity and the number and size of wheals, as well as the patients discomfort due to urticaria. Patients improved their sleep conditions and their quality of life.
No clinically relevant prolongation of QTc interval or any other cardiovascular effect has been observed in the clinical trials performed with bilastine, even at doses of 200 mg daily (10 times the clinical dose) for 7 days in 9 subjects, or even when co-administered with P-glycoprotein (P-gp) inhibitors eg, ketoconazole (24 subjects) and erythromycin (24 subjects). Additionally, a thorough QT study including 30 volunteers has been performed.
In controlled clinical trials at the recommended dose of 20 mg once daily, the central nervous system (CNS) safety profile of bilastine was similar to placebo and the incidence of somnolence was not statistically different from placebo. Bilastine at doses of up to 40 mg once daily did not affect psychomotor performance in clinical trials and driving performance in a standard driving test.
Elderly patients (≥65 years) included in phase II and III studies showed no difference in efficacy or safety with respect to younger patients.
MedsGo Class
Antihistamines & Antiallergics
Features
Brand
Bilaxten
Full Details
Dosage Strength
20 mg
Drug Ingredients
- Bilastine
Drug Packaging
Tablet 1's
Generic Name
Bilastine
Dosage Form
Tablet
Registration Number
DR-XY43523
Drug Classification
Prescription Drug (RX)
View all variations as list
| CODE | Dosage Strength | Drug Packaging | Availability | Price | ||
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RXDRUG-DR-XY43523-1pc
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In stock
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₱3300 |
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