ACTION AND MECHANISM- Antiallergic. Bilastine is a long-acting, selective antagonist of peripheral H1 receptors. It lacks significant antagonistic effects on muscarinic receptors and does not present significant sedative activity. It is effective in relieving the symptoms of allergic rhinoconjunctivitis, such as sneezing, rhinorrhea, nasal itching, nasal congestion, ocular itching, watering, and eye redness. It is also effective in relieving the intensity of itching and the number and size of hives in patients with chronic idiopathic urticaria, as well as the discomfort derived from hives. SPECIAL WARNINGS- Patients who are to undergo allergy testing using allergenic extracts should discontinue bilastine at least 72 hours beforehand to avoid false negatives. PATIENT ADVICE- Although bilastine does not usually cause drowsiness, drowsiness may occur in highly sensitive individuals. Be careful when driving.- Tell your doctor and/or pharmacist if you are going to undergo any allergy diagnostic testing.CONTRAINDICATIONS- Hypersensitivity to bilastine or any other component of the medicine.ADVANCED AGENo specific problems have been described in the elderly that require a dosage adjustment.EFFECTS ON DRIVINGBilastine does not appear to appreciably affect the ability to drive, although adverse reactions such as drowsiness, dizziness or headache have been reported.PREGNANCYSafety in animals: bilastine did not result in teratogenicity. Administration at maternotoxic doses resulted in increased pre- and post-implantation loss in rats and incomplete ossification of the cranial bones, sternum and limbs in rabbits. The NOAEL is > 30 DRMH.Safety in humans: Adequate and well-controlled studies are not available in humans. As a precautionary measure, it is advisable to avoid its use during pregnancy. Effects on fertility: Bilastine did not alter fertility in male or female rats (1,000 mg/kg/24 h). No specific studies have been conducted in humans. PHARMACOKINETICS Linear pharmacokinetics in the dose range of 5-220 mg, with low interindividual variability. - Absorption: rapid, with tmax 1.3 h. Its bioavailability is 61%. It does not show significant accumulation after repeated doses. The AUC is 737.4 ng h/ml. Effect of food: reduces absorption by approximately 20-30%. - Distribution: high plasma protein binding (84-90%). It is a substrate of P-gp and OATP1A2, but not of OAT1/3, OCT2 or BCRP transporters.- Metabolism: it has no appreciable metabolism.Enzyme inducing/inhibiting capacity: it does not present significant effects on cytochrome P450 isoenzymes or transporter proteins such as P-gp, BCRP, BSEP, MRP2, OATP1B1/3, OATP2B1, OAT1/3, OCT1/2 or NTCP.- Elimination: in feces (66.5%) and urine (28.3%) in the form of unchanged bilastine. The t1/2 is 14.5 h.Pharmacokinetics in special situations:- Children: in studies in children aged 4-11 years, it was shown that exposure with doses of 10 mg was equivalent to that achieved in adults with doses of 20 mg.- Elderly: although there do not appear to be significant differences with adults aged 18-35 years, the data are very limited.- Renal impairment: a clinically relevant effect is not expected because despite an increase in both AUC and t1/2, plasma levels were within the safety range of the active ingredient. The following AUC and t1/2 values were obtained: 967.4 ng h/ml and 15.1 h (CrCl 50-80 ml/min), 1,384.2 ng h/ml and 10.5 h (CrCl 30-49 ml/min) and 1,708.5 ng h/ml and 18.4 h (CrCl < 30 ml/min). Bilastine was completely excreted in 48-72 h.- Hepatic impairment: bilastine is not metabolized in the liver, so a significant effect is unlikely.INDICATIONS- Symptomatic treatment of [SEASONAL ALLERGIC RHINITIS], [PERENNIAL ALLERGIC RHINITIS] and [ALLERGIC CONJUNCTIVITIS].- Symptomatic treatment of [URTICARIA].INTERACTIONS- P-gp inhibitors. Bilastine is a substrate of P-gp and OATP1A2, so its plasma levels may increase when combined with drugs that are potent P-gp inhibitors (e.g., cyclosporine, ketoconazole, erythromycin) or OATP1A2 inhibitors (e.g., rifampicin, ritonavir, grapefruit juice). Its use should be avoided in patients with renal impairment (see Precautions; renal impairment). Do not use with grapefruit juice. BREASTFEEDING Safety in animals: Bilastine is excreted in rat milk (50% of maternal cp). Safety in humans: It is unknown whether it is excreted in milk, and the consequences this may have for the infant. It is recommended to assess the need to discontinue breastfeeding or avoid its administration based on the benefits to the mother and the risks to the child.CHILDRENSafety and efficacy in children and adolescents < 6 years or 20 kg in weight have not been evaluated, therefore it is recommended to avoid its use.The safety profile in adolescents 12 years and older was similar to that in adults.RULES FOR CORRECT ADMINISTRATION- Tablets: swallow whole with a sufficient amount of water.DOSAGE“TABLETS DOSAGE”- Adults and adolescents 12 years and older: 20 mg/24 h.- Children < 12 years: not recommended.- Elderly: no dosage adjustment is required.DOSAGE IN LIVER FAILURENo dosage adjustment is required.DOSAGE IN RENAL FAILURENo dosage adjustment is required.PRECAUTIONS- [RENAL FAILURE]. No dosage adjustment is required. However, it is advisable to avoid using bilastine with potent P-gp inhibitors (e.g., ketoconazole, erythromycin, cyclosporine, ritonavir, or diltiazem) in these patients due to the risk of increased plasma levels. Skin tests for hypersensitivity to allergen extracts. Due to their antihistamine effects, they may cause false negative results in diagnostic tests using these extracts. It is recommended to discontinue administration at least 72 hours before performing the test. ADVERSE REACTIONS Adverse reactions are described according to each frequency range, considering very common (>10%), common (1-10%), uncommon (0.1-1%), rare (0.01-0.1%), very rare (<0.01%) or of unknown frequency (cannot be estimated from the available data). “ADRs in adults and adolescents” - Infections and infestations: uncommon [HERPES SIMPLEX COLD HERPES].- Immune system disorders: frequency unknown [HYPERSENSITIVITY REACTIONS], with [ANAPHYLAXIS], [ANGIOEDEMA], [DYSPNEA], [SKIN RASHES], localized edema or local swelling and [ERYTHEMA].- Metabolism and nutrition disorders: uncommon [INCREATED APPETITE], [WEIGHT GAIN], [HYPERTRIGLYCERIDEMIA].- Psychiatric disorders: uncommon [ANXIETY].- Nervous system disorders: common [DROWSY], [HEADACHE]; uncommon [DIZZINESS], [INSOMNIA].- Ear and labyrinth disorders: uncommon [TINNITUS], [VERTIGO].- Cardiac disorders: uncommon [RIGHT BUNDLE BLOCK], [CARDIAC ARRHYTHMIA], sinus [QT PROLONGATION], other ECG abnormalities; [PALPITATIONS], [TACHYCARDIA].- Respiratory, thoracic and mediastinal disorders: uncommon [DYSPNEA], nasal discomfort, [DRY NASAL].- Gastrointestinal disorders: uncommon [ABDOMINAL PAIN], [NAUSEA], gastric discomfort, [DIARRHOEA], [DRY MOUTH], [DYSPEPSIA], [GASTRITIS].- Hepatobiliary disorders: uncommon [GGT ELEVATED], [TRANSAMINASES ELEVATED].- Skin and subcutaneous tissue disorders: uncommon [PRURITUS].- Renal and urinary disorders: uncommon [SEUM CREATININE ELEVATED].- General disorders and administration site conditions: uncommon [FATIGUE], [POLYDIPSIA], improvement of a pre-existing condition, [FEVER], [ASTHENIA].OVERDOSE Symptoms: The highest dose administered In clinical trials, the dose was 220 mg in single doses or 200 mg/24 h for 7 days in repeated doses. These patients presented an increased incidence of adverse reactions, with a frequency twice as high as after therapeutic doses. The most frequent were dizziness, headache, and nausea. No serious adverse events or significant prolongation of the QTc interval were reported. Measures to be taken: - Antidote: There is no specific antidote. - General elimination measures: None described. - Monitoring: Clinical status of the patient. - Treatment: Symptomatic