ACTION AND MECHANISM - [ANTIALLERGIC], [HISTAMINERGIC ANTAGONIST (H-1)]. Ebastine is a piperidine derivative that potent, competitive, reversible, and specific blocks H1 receptors, thereby decreasing the systemic effects of histamine over a prolonged period. It causes vasoconstriction and decreased vascular permeability, reducing the redness and edema associated with allergies. It partially mitigates symptoms associated with allergic processes such as eye redness or nasal congestion. It also has a mild bronchodilator effect and a reduction in skin itching. Clinical experience also seems to show that ebastine is able to prevent the release of histamine from mast cells. Ebastine is barely able to cross the blood-brain barrier, so it has practically no significant sedative effects. It has high selectivity for H1 receptors, lacking significant anticholinergic and antiserotonergic effects. Likewise, no effects on the heart have been found in clinical trials using doses of up to 100 mg. SPECIAL WARNINGS - Due to the anti-allergic effects of this medicine, it may cause false negatives in skin tests for hypersensitivity to antigenic extracts. It is recommended that administration of this medicine be discontinued at least 72 hours before the test. - It is recommended to monitor cardiac function and the electrocardiogram in patients with heart disease or in those receiving ebastine together with erythromycin, ketoconazole or antiarrhythmic drugs, due to the risk of prolongation of the QTc interval. ELDERLY PEOPLE Not enough studies have been conducted in patients over 65 years of age to demonstrate the safety and efficacy of ebastine. The appearance of a physiological decrease in liver function, and even the presence of insufficiency, is more frequent in the elderly. Therefore, the elderly are more sensitive to the adverse effects of antihistamines. Antihistamines can be used in patients over 65 years of age, but extreme caution should be exercised. If side effects persist or are severe, it is advisable to discontinue treatment. PATIENT ADVICE - It is recommended to administer this medication at the same time every day. - The recommended dose should not be exceeded, as sedation may occur. - It is advisable not to sunbathe during treatment. CONTRAINDICATIONS - Hypersensitivity to any component of the medication. Cross-reactions with other antihistamines may occur, so the use of any H1 antihistamine is not recommended in patients who have previously shown hypersensitivity to any compound in this group. - [PORPHYRIA]. H1 antihistamines have been associated with the onset of porphyritic flares, so they are not considered safe in these patients. EFFECTS ON DRIVING Although ebastine did not cause sedation in clinical trials at doses of 30 mg/24 hours, post-marketing use has shown the occurrence of cases of light sedation, so it is recommended to avoid driving dangerous machinery, including automobiles, until there is reasonable certainty that pharmacological treatment does not adversely affect the patient. PREGNANCY No fetotoxic or teratogenic effects of ebastine have been verified in animal studies. Adequate and well-controlled studies have not been conducted in humans. There are reports of a possible association between the use of antihistamines in general during the last two weeks of pregnancy and an increased risk of retrolental fibroplasia in premature children, although there are insufficient clinical data to demonstrate this. The use of this medicine is only accepted in the absence of safer therapeutic alternatives.PHARMACOKINETICSOral route:- Absorption: Ebastine is rapidly absorbed from the intestine after oral administration, undergoing an intense first-pass effect in the liver that generates an active metabolite, carebastine. The Cmax of ebastine obtained after administering a 20 mg dose is 2.8 ng/ml, while after administering a 10 mg dose, a Cmax of carebastine of 80-100 ng/ml is reached in 2.6-4 hours. Antihistamine activity begins after 1-3 hours, is maximum at 8-12 hours and can last for up to 48 hours. After discontinuation of a 5-day treatment, antihistaminic effects were observed for 72 hours, due to the metabolites of ebastine, primarily carebastine. Food: Food increases the AUC of carebastine by 1.5-2 times, although this increase does not modify the Tmax. Administration of ebastine with food does not significantly modify its clinical effect. - Distribution: Ebastine and carebastine are highly bound to plasma proteins (95%). - Metabolism: Ebastine is extensively metabolized by the CYP3A4 isoenzyme, giving rise to the active metabolite carebastine. - Elimination: Ebastine is primarily eliminated by hepatic metabolism. 66% of the dose appears in urine, mainly in the form of conjugated metabolites. It may also appear in small amounts in the feces (6%). The elimination half-life of carebastine is 15-19 hours. No significant pharmacokinetic differences have been observed between patients over 65 years of age and younger patients, or between individuals with different degrees of renal or hepatic impairment compared to healthy patients. INDICATIONS - [SEASONAL ALLERGIC RHINITIS] or [PERENNIAL ALLERGIC RHINITIS], with or without association with [ALLERGIC CONJUNCTIVITIS]. INTERACTIONS No drug interactions have been observed with ebastine. The use of ebastine with alcohol has not been shown to increase sedation. However, due to the risk of photosensitivity reactions due to the use of H1 antihistamines, ebastine may potentiate the photosensitizing effects of other drugs. - Erythromycin, ketoconazole. There have been some cases of slight prolongation of the QTc interval, of about 10 msec. It is unknown whether this effect is due to CYP3A4 enzyme inhibition by macrolides or azole antifungals, or to the cardiac effects of these drugs themselves. Extreme caution is recommended in patients receiving ebastine concomitantly with any of these drugs. BREASTFEEDING It is unknown whether ebastine is excreted in milk, but other antihistamines are. Due to the risk of adverse reactions in infants, it is recommended to stop breastfeeding or avoid the administration of this medicine. CHILDREN Safety and efficacy in children under 2 years of age have not been evaluated, therefore it is recommended to avoid its use. The 10 and 20 mg doses are not indicated for children between 2 and 12 years of age, therefore it is recommended to use the oral solution, adjusting the dose according to their age. GUIDELINES FOR CORRECT ADMINISTRATION - Tablets: Swallow the tablets whole, with the aid of a glass of liquid, preferably water. DOSAGE Tablets: - Adults, oral: 10-20 mg/24 h. - Children and adolescents under 18 years of age, oral: * Adolescents from 12 years of age: no dosage adjustment is required. DOSAGE IN LIVER FAILURE - Mild to moderate liver failure (Child-Pugh class A): no dosage adjustment is required. - Insufficiency Severe hepatic impairment (Child-Pugh class C): maximum dose 10 mg/24 h. DOSAGE IN RENAL FAILURE No dosage adjustment is required. PRECAUTIONS - [LIVER FAILURE]. Ebastine is extensively metabolized in the liver. In cases of liver failure, an increase in plasma concentration may occur. It is recommended not to exceed a dose of 10 mg/24 hours in patients with severe hepatic impairment, while in those with mild or moderate impairment no measures are necessary, although it is advisable to monitor these patients (See Dosage). - [CARDIAC ARRHYTHMIA]. Patients at cardiac risk, such as those with [BRADYCARDIA], [QT PROLONGATION], with [HYPOKALAEMIA] or under treatment with drugs that affect the QT interval or inhibit the metabolism of ebastine (See Interactions). In clinical trials, ebastine has been shown to have no significant effects on the heart at doses of up to 100 mg/24 hours, but this cannot be ruled out, so it is recommended to monitor cardiac function in these patients.- [EPILEPSY]. Caution should be exercised in epileptic patients, since antihistamines have occasionally been associated with paradoxical hyperexcitability reactions, even at therapeutic doses, and may therefore lower the seizure threshold.- Photosensitivity. Ebastine may cause photosensitivity, so it is recommended not to expose yourself to the sun during treatment and to protect yourself with sunscreen.- Acute allergic conditions. Because ebastine may take around three hours to produce pharmacological effects, its use is not recommended in severe acute allergic conditions. PRECAUTIONS RELATED TO EXCIPIENTS- This medicine contains lactose. Patients with hereditary [LACTOSE INTOLERANCE] or galactose intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicine. ADVERSE REACTIONS The side effects of ebastine are usually mild and transient, and are usually dose-related. Non-sedating antihistamines generally cause the same side effects as sedatives, but with a much lower incidence. In particular, sedation and anticholinergic effects do not appear or do so very rarely, provided they are not used at doses higher than those recommended. In clinical trials with 2,100 patients, ebastine caused adverse reactions in only 3.7% more patients than placebo. The most common adverse reactions are: - Digestive. [DRY MOUTH] is rare. Cases of [NAUSEA], [VOMITING], [CONSTIPATION], [DIARRHEA] or [EPIGASTRIC PAIN] have also been reported.- Neurological/psychological. Occasionally, [HEADACHE] or mild [DROWSY] may occur. Some cases of [DISORIENTATION], [PSYCHOMOTOR LISORDINATION], [MYASTHENIA], [VERTIGO], [ASTHENIA] have also been described. As with other antihistamines, isolated cases of paradoxical [EXCITABILITY] may occur, especially in young children, with [INSOMNIA], [NERVOUSNESS], [TREMOR], [IRRITABILITY], [EUPHORIA], [DELIRIUM], palpitations and even [CONVULSIONS].- Cardiovascular. Occasionally, [TACHYCARDIA], [PALPITATIONS] and other [CARDIAC ARRHYTHMIA] such as [EXTRASYSTOLE] or [HEART BLOCK] may occur. [HYPOTENSION] or [ARTERIAL HYPERTENSION] have also been described. Cases of mild [QT INTERVAL PROLONGATION] have been reported in certain patients, such as those undergoing treatment with erythromycin or ketoconazole, even at high doses.- Genitourinary. Cases of [DYSMENORRHEA] have been observed.- Respiratory. Some cases of [EPISTAXIS] and [SINUSITIS] have been reported.- Hematological. Rarely, [HEMOLYTIC ANEMIA], [AGRANULOCYTOSIS], [LEUKOPENIA], [THROMBOPENIA] or [PANCYTOPENIA] may appear.- Ocular. [GLAUCOMA] and [VISION DISTURBANCES] such as [BLURRED VISION] or [DIPLOPIA] may rarely occur.- Allergic/dermatological. [HYPERSENSITIVITY REACTIONS] may occur after systemic administration of antihistamines. [PHOTOSENSITIVITY REACTIONS] may also occur after intense exposure to sunlight, with [DERMATITIS], [PRURITUS], [EXANTHEMA] and [ERYTHEMA].OVERDOSE Symptoms: There are few data on poisoning with ebastine. No adverse reactions were observed in a clinical trial in which doses of up to 100 mg of ebastine were administered. Treatment: There is no specific antidote. Treatment will consist of standard measures to promote elimination of the drug. Symptomatic and supportive treatment is recommended, monitoring vital functions and the ECG. COMPOSITION EBASTRINE: 10 MILLIGRAMS LACTOSE (EXCIPIENT): 88.5 MILLIGRAMS - MONOHYDRATE CORN STARCH (EXCIPIENT): 0 - PREGELATINIZED