Bactil Forte Flas 20 Mg 10 Oral Lyophilized

Bactil Forte Flas (20 Mg 10 Oral Lyophilized)

Ebastine

ACTION AND MECHANISM

- [ANTIALLERGIC], [HISTAMINERGIC ANTAGONIST (H-1)]. Ebastine is a piperidine derivative that potently, competitively, reversibly and specifically blocks H1 receptors, reducing the systemic effects of histamine for a long time. It leads to vasoconstriction and decreased vascular permeability, reducing redness and edema associated with allergy. Partially mitigates symptoms associated with allergic processes such as eye redness or nasal congestion. It also produces a slight bronchodilator effect and a decrease in dermal itching. Clinical experience also seems to show that ebastine is capable of preventing the release of histamine from mast cells.

Ebastine is barely able to cross the blood-brain barrier, so it has virtually no significant sedative effects. It has great selectivity for H1 receptors, lacking important anticholinergic and antiserotonergic effects. Similarly, no effects on the heart have been found in clinical trials, using doses up to 100 mg.

PHARMACOKINETICS

- Absorption: Ebastine is rapidly absorbed from the intestine after oral administration, suffering an intense first pass effect in the liver that generates an active metabolite, carebastine. The Cmax of ebastine obtained after administering a dose of 20 mg is 2.8 ng / ml, while after administering a dose of 10 mg, a Cmax of carebastine of 80-100 ng / ml is reached at 2.6-4 hours. Antihistamine activity begins after 1-3 hours, peaks after 8-12 hours, and can be prolonged for up to 48 hours. After the interruption of a 5-day treatment, antihistamine effects were observed for 72 hours, due to the metabolites of ebastine, mainly carebastine.

Effect of food : food increases the AUC of carebastine between 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 strongly bound to plasma proteins (95%).

- Metabolism: Ebastine is intensively metabolized by the CYP3A4 isoenzyme, giving rise to the active metabolite carebastine.

- Elimination: Ebastine is eliminated mainly by hepatic metabolism. 66% of the dose appears in urine, mainly in the form of conjugated metabolites. It can also appear in small amounts in the stool (6%). The elimination half-life of carebastine is 15-19 hours.

Pharmacokinetics in special situations : no significant pharmacokinetic differences have been observed between patients older than 65 years and younger, nor between individuals with different degrees of renal or hepatic insufficiency compared to healthy patients.

INDICATIONS

- [SEASONAL ALLERGIC RHINITIS] or [PERENNIAL ALLERGIC RHINITIS], associated or not with [ALLERGIC CONJUNCTIVITIS].

- [URTICARIA CRONICA IDIOPATICA].

- [ALLERGIC CONTACT DERMATITIS].

POSOLOGY

"TABLETS DOSAGE"

- Adults: 10-20 mg / 24 h.

- Children and adolescents <18 years:

* Adolescents from 12 years old: does not require dosage adjustment.

- Elderly: does not require dosage adjustment.

Duration of treatment: until symptoms disappear.

Missed dose: skip the missed dose and administer the next dose at the usual time. Do not double the next dose.

DOSAGE IN KIDNEY INSUFFICIENCY

It does not require dosage adjustment.

DOSAGE IN LIVER INSUFFICIENCY

- Mild to moderate hepatic impairment (Child-Pugh class A): does not require dose adjustment.

- Severe hepatic impairment (Child-Pugh class C): maximum dose 10 mg / 24 h.

RULES FOR CORRECT ADMINISTRATION

- Tablets: swallow whole, with the help of a glass of liquid, preferably water.

Administration with food : can be taken with or without food.

CONTRAINDICATIONS

- Hypersensitivity to any component of the drug. There may be cross reactions with other antihistamines, so it is not recommended to use any H1 antihistamine in patients who have presented hypersensitivity to any compound in the group.

- [PORFIRIA]. H1 antihistamines have been associated with the appearance of porphyric outbreaks and are therefore not considered safe in these patients.

PRECAUTIONS

- [LIVER FAILURE]. Ebastine is extensively metabolized in the liver. In the event of liver failure, an increase in plasma concentration may occur. It is recommended not to exceed the dose of 10 mg / 24 hours in patients with severe hepatic impairment, while in those with mild or moderate impairment it is not necessary to take any measures, although it is advisable to monitor these patients (See Dosage).

- [CARDIAC ARRHYTHMIA]. Patients with cardiac risk, such as those with [BRADYCARDIA], [QT INTERVAL PROLONGATION], with [HYPOPOTASEMIA] or in treatment with drugs that affect the QT interval or that inhibit the metabolism of ebastine (See Interactions). In clinical trials, it has been shown that ebastine does not have significant effects on the heart at doses of up to 100 mg / 24 hours, but it 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 therefore could lower the seizure threshold.

- Photosensitivity. Ebastine could lead to photosensitivity phenomena, so it is recommended not to sunbathe during treatment, and protect yourself with sun filters.

- Acute allergic processes. Since ebastine may take about three hours to show pharmacological effects, its use in severe acute allergic conditions is not recommended.

PRECAUTIONS RELATING TO EXCIPIENTS

- This medicine contains aspartame as an excipient, so it should be taken into account by people affected by [PHENYLKETONURIA]. 100 mg of aspartame correspond to 56.13 mg of phenylalanine.

ADVICE TO THE PATIENT

- It is recommended to administer this medicine every day at the same time.

- The recommended dose should not be exceeded, as sedation could appear.

- It is advisable not to sunbathe during the treatment.

SPECIAL WARNINGS

- Due to the antiallergic effects of this medicine, it could give false negatives in dermal tests of hypersensitivity to antigenic extracts. It is recommended to suspend the administration of this medicine 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 who receive ebastine together with erythromycin, ketoconazole or antiarrhythmic drugs, due to the risk of prolongation of the QTc interval.

INTERACTIONS

No drug interactions have been observed with ebastine. The use of ebastine together with alcohol has not been shown to increase sedation. However, due to the risk of photosensitivity reactions due to the consumption of H1 antihistamines, ebastine could 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 the enzymatic inhibition of CYP3A4 by macrolides or azole antifungals, or to the effects on the heart of these drugs themselves. Extreme caution is recommended in patients receiving ebastine together with any of these drugs.

PREGNANCY

Safety in pregnant women: There have not been adequate and well-controlled studies 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 infants, although there are insufficient clinical data to demonstrate this. The use of this medicine is only accepted in the absence of safer therapeutic alternatives.

Effects on fertility: no foetotoxic or teratogenic effects of ebastine have been found in animal studies

LACTATION

It is unknown whether ebastine is excreted in milk, but other antihistamines do. Due to the risk of adverse reactions in the infant, it is recommended to discontinue breastfeeding or to avoid the administration of this drug.

KIDS

Safety and efficacy have not been evaluated in children under 2 years of age, so it is recommended to avoid its use.

Doses of 10 and 20 mg are not indicated in children between 2-12 years of age, so it is recommended for them to use the oral solution, adjusting the dose according to age.

SENIORS

There have not been enough studies in patients over 65 years of age to demonstrate the safety and efficacy of ebastine. In the elderly, the appearance of a physiological decrease in liver function is more frequent, and even the presence of insufficiency. Therefore, the elderly are more sensitive to the adverse effects of antihistamines. Antihistamines can be used in patients over 65 years of age, but caution should be exercised. If the side effects persist or are severe, it is advisable to stop the treatment.

EFFECTS ON DRIVING

Although in clinical trials ebastine has not resulted in sedation at a dose of 30 mg / 24 hours, post-marketing use has shown the appearance of cases of light sedation, so it is recommended to avoid operating dangerous machinery, including cars, until they have reasonable certainty that drug treatment does not adversely affect.

ADVERSE REACTIONS

The side effects of ebastine are usually mild and transient, and are usually dose related. Non-sedating antihistamines generally have the same side effects as sedatives, but with a much lower incidence. Especially, sedation and anticholinergic effects do not appear or do so very rarely, as long as 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:

- Immune system disorders: [HYPERSENSITIVITY REACTIONS] may appear after systemic administration of antihistamines.

- Metabolism and nutrition disorders: frequency little known [APPETITE GAIN], [WEIGHT GAIN]

- Nervous system disorders: mild [HEADACHE] or [Drowsiness] is common. Some cases of [DIZZINESS], [DISORIENTATION], [ATAXIA], [MYASTENIA], [VERTIGO], [HYPOESTHESIA], [DYSGEUSIA] [ASTENIA] are also described. As with other antihistamines, specific cases of paradoxical [EXCITABILITY] could occur, especially in young children, with insomnia and nervousness, [SHAKING], [IRRITABILITY], [EUPHORIA], [DELUSION], palpitations and even [SEIZURES].

- Psychiatric disorders: [INSOMNIA], [NERVIOSISM].

- Cardiovascular disorders. On specific occasions, [TACHYCARDIA], [PALPITATIONS] and others [CARDIAC ARRHYTHMIA] such as [EXTRASISTOLE] or [HEART BLOCK] may occur. [HYPOTENSION] or [ARTERIAL HYPERTENSION] has also been described. Cases of mild [QT INTERVAL PROLONGATION] have been reported in certain patients, such as those receiving erythromycin or ketoconazole, and at high doses.

- Respiratory, thoracic and mediastinal disorders Some cases of [EPISTAXIS] and [SINUSITIS] have been described.

- Gastrointestinal disorders: the appearance of [DRYING OF THE MOUTH] is rare. [NAUSEA], [VOMITING], [CONSTIPATION], [DIARRHEA] or [EPIGASTRIC PAIN] have also been described.

- Hepatobiliary disorders: some cases of [HEPATITIS], [CHOLESTASIS], [INCREASED TRANSAMINASES], [INCREASED ALKALINE PHOSPHATASE] and [HYPERBILIRUBINEMIA] have been reported

- Skin and subcutaneous tissue disorders: [PHOTOSENSITIVITY REACTIONS] may appear after intense exposure to sunlight, [DERMATITIS], [URTICARIA], [PRURITO], [EXANTEMATIC ERUPTIONS] and [ERYTHEMA].

- Reproductive system and breast disorders: cases of [DYSMENORRHEA] have been observed.

- Hematological disorders. Rarely, [HEMOLYTIC ANEMIA], [AGRANULOCYTOSIS], [LEUCOPENIA], [THROMBOCYTOPENIA] or [PANCITOPENIA] may appear.

- Eye disorders: rarely [GLAUCOMA] and [VISION DISORDERS] may appear as [BLURRED VISION] or [DIPLOPIA].

- General disorders and administration site conditions: some cases of [EDEMA] and [ASTENIA] have been reported

OVERDOSE

Symptoms: There is little data on ebastine poisoning. In a clinical trial in which a dose of up to 100 mg of ebastine was administered, no adverse reactions were observed.

Treatment: there is no specific antidote. Treatment will consist of the usual measures designed to favor the elimination of the drug. Symptomatic and supportive treatment is recommended, monitoring vital functions and the ECG.

Bactil Forte Flas 20 Mg 10 Oral Lyophilized Leaflet