Bilastine

Registered South African indications:

• Symptomatic treatment of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR) and idiopathic chronic urticaria (ICU)

Contraindications

Registered contraindications in South Africa & other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

South African recommendations

Caution in the following patient groups

• Pregnancy
• Breastfeeding

Coadministration with P-glycoprotein inhibitors and renal impairment

• In patients with moderate or severe renal impairment coadministration of bilastine with P-glycoprotein inhibitors, such as e.g., ketoconazole, erythromycin, cyclosporin, ritonavir or diltiazem, may increase plasmatic levels of bilastine and therefore increase the risk of adverse effects of bilastine
• Therefore, coadministration of bilastine and P-glycoprotein inhibitors should be avoided in patients with moderate or severe renal impairment

Ability to drive and use machines

• Bilastine can cause drowsiness and dizziness. Patients experiencing drowsiness or dizziness should avoid driving and use of machines

Recommendations in other jurisdictions

Caution in the following patient groups

• Pregnancy
• Breastfeeding

Paediatric precautions

• Efficacy and safety of bilastine in children under 2 years of age have not been established and there is little clinical experience in children aged 2 to 5 years, therefore bilastine should not be used in these age groups

Coadministration with P-glycoprotein inhibitors and renal impairment

• In patients with moderate or severe renal impairment coadministration of bilastine with P-glycoprotein inhibitors, such as e.g., ketoconazole, erythromycin, cyclosporin, ritonavir or diltiazem, may increase plasmatic levels of bilastine and therefore increase the risk of adverse effects of bilastine
• Therefore, coadministration of bilastine and P-glycoprotein inhibitors should be avoided in patients with moderate or severe renal impairment

Excipient precautions

• This medicine contains less than 1mmol sodium (23mg) per tablet, that is to say essentially 'sodium free'

Ability to drive and use machines

• A study performed in adults to assess the effects of bilastine on the ability to drive demonstrated that treatment with 20mg did not affect the driving performance
• However, as the individual response to the medicinal product may vary, patients should be advised not to drive or use machines until they have established their own response to bilastine

Forms avail. in SA and covered in this monograph: tab

South African registered indications and dosages

Symptomatic treatment of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR) and idiopathic chronic urticaria (ICU)

• Oral (tab): 20mg, once daily to be swallowed with water

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It is recommended to take the daily dose in one single intake. Bilastine should be taken one hour before or two hours after intake of food or fruit juice

Forms avail. in SA and covered in this monograph: tab

South African registered indications and dosages

Symptomatic treatment of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR) and idiopathic chronic urticaria (ICU)

Younger than 12 years

• Not established for use

12 years and older

• See adult dosage

Pregnancy

South African recommendations

• Caution; not recommended
• Bilastine should not be used during pregnancy
• The safety of bilastine in pregnancy has not been established. There are no or limited data on 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

Recommendations in other jurisdictions

• Caution; not recommended
• 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
• As a precautionary measure, it is preferable to avoid the use of bilastine during pregnancy

Breastfeeding

South African recommendations

• Caution; not recommended
• Bilastine should not be used during breastfeeding
• The safety of bilastine in lactation has not been established. The excretion of bilastine in human milk has not been studied
• Pharmacokinetic data in animals show excretion of bilastine in milk

Recommendations in other jurisdictions

• Caution; not recommended
• The excretion of bilastine in milk has not been studied in humans. Available pharmacokinetic data in animals have shown excretion of bilastine in milk
• A decision on whether to continue/discontinue breastfeeding or to discontinue/abstain from bilastine therapy must be made taking into account the benefit of breastfeeding for the child and the benefit of bilastine therapy for the mother

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• There are no or limited amount of clinical data. A study in rats did not indicate any negative effect on fertility

South African recommendations

• No dose adjustment recommended

  No dosage adjustment is required in patients with renal impairment because, despite the increase in AUC, the concentrations of bilastine were within the therapeutic range

Recommendations in other jurisdictions

• No dose adjustment recommended
  Studies conducted in adults in special risk groups (renally impaired patients) indicate that it is not necessary to adjust the dose of bilastine in adults

Recommendations below are applicable to South Africa and other jurisdictions

• No dose adjustment recommended
  There is no clinical experience in adult patients with hepatic impairment
  However, since bilastine is not metabolised and is eliminated as unchanged in urine and faeces, hepatic impairment is not expected to increase systemic exposure above the safety margin in adult patients
  Therefore, no dosage adjustment is required in adult patients with hepatic impairment

Recommendations below are applicable to South Africa and other jurisdictions

• No dose adjustment recommended

Adults and Adolescents

Infections and Infestations

Uncommon

• Oral herpes

Metabolism and Nutrition Disorders

Uncommon

• Increased appetite

Psychiatric Disorders

Uncommon

• Anxiety
• Insomnia

Nervous System Disorders

Common

• Somnolence
• Headache

Uncommon

• Dizziness

Ear and Labyrinth Disorders

Uncommon

• Tinnitus
• Vertigo

Cardiac Disorders

Uncommon

• Right bundle branch block
• Sinus arrhythmia
• Electrocardiogram QT prolonged
• Other ECG abnormalities

Respiratory, Thoracic and Mediastinal Disorders

Uncommon

• Dyspnoea
• Nasal discomfort
• Nasal dryness

Gastrointestinal Disorders

Uncommon

• Upper abdominal pain
• Abdominal pain
• Nausea
• Stomach discomfort
• Diarrhoea
• Dry mouth
• Dyspepsia
• Gastritis

Skin and Subcutaneous Tissue Disorders

Uncommon

• Pruritus

General Disorders and Administration Site Conditions

Uncommon

• Fatigue
• Thirst
• Improved pre-existing condition
• Pyrexia
• Asthenia

Investigations

Uncommon

• Increased gamma-glutamyltransferase
• Increased alanine aminotransferase
• Increased aspartate aminotransferase
• Increased blood creatinine
• Increased blood triglycerides increased
• Increased weight

Paediatric Population

Infections and Infestations

Common

• Rhinitis

Nervous System Disorders

Common

• Headache

Uncommon

• Dizziness
• Loss of consciousness

Eye Disorders

Common

• Allergic conjunctivitis

Uncommon

• Eye irritation

Gastrointestinal Disorders

Common

• Abdominal pain / Upper abdominal pain

Uncommon

• Diarrhoea
• Nausea
• Lip swelling

Skin and Subcutaneous Tissue Disorders

Uncommon

• Eczema
• Urticaria

General Disorders and Administration Site Conditions

Uncommon

• Fatigue

• Medicinal products that are substrates or inhibitors of OATP1A2
• Ritonavir
• Rifampicin

Other interactions

• Food
• Grapefruit juice (may also apply to other fruit juices)

Interactions that do not affect the safety profile of bilastine or the listed medicine

• Ketoconazole
• Erythromycin
• Cyclosporin

Interactions that do not the affect safety profile of bilastine

• Diltiazem

Observations

• Relief of symptoms

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 hours following single doses.