Bulas Medicamentos Alphacaine | Page 2

7. CUIDADO DE ALMACENAMIENTO Evitar calor excesivo (temperatura superior a 40°C) y proteger de la luz. El plazo de validez del producto es de 24 meses, contados a partir de la fecha de fabricación. Número de lote y fecha de fabricación y plazo de validez: ver embalaje. No use medicamento después de su plazo de validez. Guárdelo en su embalaje original. Antes de usar, observe el aspecto del producto. Todo medicamento se debe mantener fuera del alcance de los niños. 8. POSOLOGÍA Y MODO DE USAR Como ocurre con todos os anestésicos locales, la dosis varía y depende del área a ser anestesiada, de la vascularización de los tejidos, del número de segmentos nerviosos a ser bloqueados, de la tolerancia individual y de la técnica anestésica usada. Se debe usar la menor dosis necesaria y suficiente para proporcionar una anestesia específica. La dosis necesaria se debe determinar en función del estado de cada individuo. La dosis máxima sugerida por el Consejo de Terapéutica Odontológica de la Asociación Americana de Odontología y por la Convención de la USP es de 4,4 mg/kg, con o sin vasoconstrictor. Esta dosis permite, además, el uso de una cantidad significativa del fármaco para obtener una anestesia clínica profunda con un riesgo un poco menor de reacciones tóxicas (superdosificación). La dosis máxima recomendada para niños menores de 10 años, con peso y desarrollo normales, se debe determinar por medio de la fórmula pediátrica standard (ej.: Regla de Clark). La dosis máxima recomendada de epinefrina es de 0,2 mg (o el equivalente a 5,5 Carpules de ALPHACAINE 50, 8,8 Carpules de ALPHACAINE 80 o 11 Carpules de ALPHACAINE 100) para pacientes adultos sanos. La dosis máxima recomendada para los individuos sensibles a la epinefrina, como determinados pacientes ASA III o ASA IV y pacientes clínicamente hipertireóideos, es de 0,04 mg por consulta (1 Carpule de ALPHACAINE 50 1 y ½ Carpule de ALPHACAINE 80 o 2 Carpules de ALPHACAINE 100). En la infiltración oral y/o bloqueo mandibular, la dosis inicial usualmente efectiva es de 1 a 5 ml de lidocaína (½ a 2 e ½ Carpules). En niños menores de 10 años raramente se necesita administrar más que 0,9 a 1,0 ml (½ Carpule) de lidocaína por procedimiento para conseguir anestesia local para un único diente. Se recomienda aspirar durante la aplicación para evitar el riesgo de una inyección intravascular. Dosis máximas: 4,4 mg de clorhidrato de lidocaína/kg 0,2 mg de epinefrina/kg (Cada Carpule de 1,8 ml contiene 36 mg de clorhidrato de lidocaína) Peso (Kg) 0 N Carpules ALPHACAINE 50 1 (44 mg) 10 2 (88 mg) 20 3,5 (132 mg) 30 40 40 4,5 (176 mg) 6 (220 mg) 50 6 (220 mg) 60 6 (220 mg) 70 6 (220 mg) 80 6 (220 mg) 90 6 (220 mg) 100 0 0 0 N Carpules N Carpules N Carpules ALPHACAINE 80 ALPHACAINE 100 ALPHACAINE 200 1 (44 mg) 2 (88 mg) 3,5 (132 mg) 40 4,5 (176 mg) 6 (220 mg) 7 (264 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 1 (44 mg) 2 (88 mg) 3,5 (132 mg) 40 4,5 (176 mg) 6 (220 mg) 7 (264 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 1 (44 mg) 2 (88 mg) 3,5 (132 mg) 40 4,5 (176 mg) 6 (220 mg) 7 (264 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) Las dosis indicadas representan lo máximo sugerido para individuos sanos normales; para pacientes debilitados o ancianos deben ser menores. Se aconseja desinfectar la tapa del carpule que entra en contacto con la aguja con algodón embebido en alcohol al 70%. No inmergir los carpules bajo ningún concepto, cualquiera que sea la solución. Se recomienda aspirar durante la aplicación para evitar el riesgo de una inyección intravascular. Para aspirar, la aguja debe ser posicionada hasta que no ocurra ninguno retorno de sangre con la aspiración. Sin embargo, se debe observar que la ausencia de sangre en la jeringa no garantiza que se evitó la inyección intravascular y siempre se recomienda una doble aspiración. No se deben reaprovechar los Carpules parcialmente usados. 9. REACCIONES ADVERSAS Los efectos colaterales son similares a los observados con otros anestésicos locales del tipo amida. Las acciones adversas, en general, están relacionadas con la dosificación y pueden resultar de altos niveles plasmáticos causados por dosis excesiva, absorción rápida, o inyección intravascular accidental, o también pueden ser el resultado de hipersensibilidad, idiosincrasia o tolerancia reducida por parte del paciente. Pueden ocurrir efectos sobre el sistema cardiovascular y el SNC. Las manifestaciones del SNC pueden ser de excitación o depresión, como fotofobia, nerviosismo, aprensión, euforia, confusión, mareos, somnolencia, zumbidos, visión borrosa, vómitos, sensación de calor, frío, hormigueo, temblores, pérdida de la conciencia, depresión y parada respiratoria. Las manifestaciones cardiovasculares normalmente son de depresión del sistema y caracterizadas por bradicardia, hipotensión y colapso cardiovascular, que pueden conducir a una parada cardíaca. Las señales y los síntomas de una función cardiovascular deprimida comúnmente pueden ser el resultado de una reacción vasovagal pero, eventualmente, pueden ser el resultado de un efecto directo de la droga. Los tratamientos de auxilio para estas manifestaciones deben estar al alcance del profesional para el caso de ser necesaria una acción rápida. Prácticamente no existe la alergia a los anestésicos locales del tipo amida.; a pesar de que sean factibles son extremamente raras las reacciones alérgicas documentadas y reproducibles. Las manifestaciones alérgicas suaves se caracterizan por lesiones cutáneas, urticaria, edema. Las reacciones anafilácticas son sumamente raras. Las manifestaciones neurológicas, por ejemplo deficiencia neurológica persistente, asociadas al uso de anestésicos locales pueden estar relacionadas a la técnica utilizada, la dosis total de anestésico administrada, la vía de administración y las condiciones físicas del paciente. Puede ocurrir parestesia con el uso de ALPHACAINE. En casos de eventos adversos, notifique al Sistemas de Notificaciones en Vigilancia Sanitaria – NOTIVISA, disponible en www.anvisa.gov.br/hotsite/notivisa/index.htm, o para la Vigilancia Sanitaria del Estado o del Municipio. 10. SOBREDOSIS Reacciones generalizadas del SNC o reacciones cardiovasculares generalmente están relacionadas con altos niveles plasmáticos por causa de una inyección intravascular accidental o sobredosis. (Ver Advertencias y Acciones Adversas). Los primeros señales y síntomas de la intoxicación por lidocaína pueden incluir somnolencia lo que puede llevar a la pérdida de la conciencia y parada respiratoria. En estos casos se debe proceder de la siguiente manera: - Coloque al paciente en posición supina. Levántele las piernas con una inclinación de 30° a 45º sobre la horizontal. - Asegúrese de que haya pasaje de aire. Si la ventilación es inadecuada, ventile al paciente con oxígeno (si es posible). - Si el pulso está bajo (< 40) o no lo puede determinar, comience a hacerle masaje cardíaco externo. - El tratamiento de auxilio de la deficiencia circulatoria puede necesitar la administración de líquidos por vía intravenosa (suero). En caso de intoxicación llame al 0800 722 6001, si necesitar más ayuda. VENTA BAJO PRESCRIPCIÓN MÉDICA PRODUCTO DE USO EXCLUSIVAMENTE PROFESIONAL Aprobada por ANVISA en 21/05/2013. ALPHACAINE 1:50,000 / 1:80,000 / 1:100,000 / 1:200,000 Lidocaine Hydrochloride + Epinephrine ENGLISH PRESENTATIONS: - Sterile injectable solution of Lidocaine Hydrochloride 2% (20mg/mL) +Epinephine 20µg /mL packaged in glass cartridge of 1,8 mL. Each package contains 50 cartridges. - Sterile injectable solution of Lidocaine Hydrochloride 2% (20mg/mL) +Epinephine 12.5µg /mL packaged in glass cartridge of 1,8 mL. Each package contains 50 cartridges. - Sterile injectable solution of Lidocaine Hydrochloride 2% (20mg/mL) +Epinephine 10µg /mL packaged in glass cartridge of 1,8 mL. Each package contains 50 cartridges. - Sterile injectable solution of Lidocaine Hydrochloride 2% (20mg/mL) +Epinephine 5µg /mL packaged in glass cartridge of 1,8 mL. Each package contains 50 cartridges. USE ONLY IN INFILTRATION OR NERVE BLOCK VIA SUBMUCOSA AND INTRAORAL. FOR ADULT AND/OR PEDIATRIC USE COMPOSITION: Each mL of ALPHACAINE 1:50,000 injection contains: Lidocaine hydrochloride.......................................20.0 mg Epinephrine .........................................................20.0µg Excipients e.f.........................................................1.0 mL Excipients: Sodium Bisulfite, Sodium Chloride and Water for Injection. Each mL of ALPHACAINE 1:80,000 injection contains: Lidocaine hydrochloride......................................20.0 mg Epinephrine ........................................................12.5µg Excipients e.f........................................................1.0 mL Excipients: Sodium Bisulfite, Sodium Chloride and Water for Injection. Each mL of ALPHACAINE 1:100,000 injection contains: Lidocaine hydrochloride......................................20.0 mg Epinephrine ........................................................10.0µg Excipients e.f........................................................1.0 mL Excipients: Sodium Bisulfite, Sodium Chloride and Water for Injection. Each mL of ALPHACAINE 1:200,000 injection contains: Lidocaine hydrochloride......................................20.0 mg Epinephrine ..........................................................5.0µg Excipients e.f........................................................1.0 mL Excipients: Sodium Bisulfite, Sodium Chloride and Water for Injection. TECHNICAL INFORMATION FOR HEALTH CARE PROFESSIONALS 1. INDICATIONS The product is indicated for local anesthesia by nerve block or infiltration, for general dental interventions, multiple extractions, immediate dentures and endodontic and periodontal procedures simple and complex. 2. EFFICACY RESULTS Several clinical studies have been conducted in order to evaluate the ability of anesthetics to block conduction in nerve axons of the peripheral nervous system (Friedman, P.M. and others: Comparative study of the efficacy of four topical anesthetics, Dermatol Surg 25:12, 1999/Buckley, J.A.; Ciancio, S.G.; Mc Mullen, J.A.: Efficacy of epinephrine concentration in local anesthesia during periodontal surgery, J. Periodontol 55:653-657, 1984) and its efficacy in provide anesthesia when associated to several vasoconstrictor (Jacob, W.: Local anaesthesia and vasoco nstrictive additional components, Newslett Int Fed Dent Anesthesiol Soc 2(1):3, 1989/Bennett, C.R.: Monheim's local anesthesia and pain control in dental practice, ed 7, St. Louis, 1983, Mosby-Year Book). 3. PHARMACOLOGY Lidocaine Hydrochloride Classification: Amide Other names: Xylocaine Chemical formula: 2-Diethylamino 2',6-acetoxylidide hydrochloride. Potency: 2 (procaine = 1) Toxicity: 2 (in comparison with procaine) Mechanism of action: Promotes local anesthesia through the stabilization of neuronal membranes, inhibiting the ionic flux required for the onset and conduction of impulses. Absorption: Lidocaine is completely absorbed following parenteral administration and its margin of absorption depends on the site of administration and the presence or otherwise of vasoconstrictors. The link between plasma and lidocaine depends on the concentration of the drug and the linked fraction decreases in accordance with the increase of concentration. It crosses the blood-brain and placentary barriers, presumably via passive diffusion. Metabolism: It is metabolized in the liver by the microsomal fixed-functions oxidases, to monoethylglyceine and xylidide; xylidide is a local anesthetic and potentially toxic. Excretion: Via the kidneys; less than 10% unchanged, more than 80% various metabolites. Vasodilating properties: Considerably less than those of procaine; however, more than those of prilocaine or mepivacaine. Onset of action: Rapid (2 to 3 minutes). Anesthetic half-life: 1.6 hours. Topical anesthetic action: Yes (in clinically acceptable concentrations). Epinephrine Other chemical names: Adrenaline It is a sympathomimetic amine, being chemically recognized as 3,4-dihydroxi (methylamino) methyl benzilic alcohol. It acts on both á- and â-adrenergic receptors, where â effects predominate. It has been used in minimal concentrations which permit a prolonged anaesthetic effect, necessary for lengthy surgical interventions or where major bleeding occurs. 4. CONTRAINDICATIONS ALPHACAINE is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type or to any other substance present in formula and in patients receiving drugs known to produce blood pressure alterations, as MAO inhibitors, tricyclic antidepressants and phenothiazines. 5. WARNINGS AND PRECAUTIONS The safety and efficacy of local anesthetics depend on the recommended dosage, the correct technique employed, the previous anamnesis, the appropriate precautions taken and the fastness and qualification of the health care professional during emergencies. It should be used the lowest doses that are able to provide efficient anesthesia. The administration of frequent doses of lidocaine may cause a sharp increase of levels in the blood with each additional dose, due to the increase of the drug, its metabolites or to slow metabolic breakdown. Tolerance may vary depending on the patient's state, those debilitated by old age or serious illnesses or children should be given reduced doses, calculated in accordance with their age and physical condition. Special care is recommended in frequent application in patients with serious kidney or liver problems due to their inability to normally metabolize the anesthetic drug, thereby being subject to the risk of toxic concentrations in the plasma. Special care should be taken in the administration of local anesthetics in patients with known drug sensitivities or allergies to any of the substances in the formula. Patients with hypertension, coronary or cardiovascular problems (particularly related to sequela of acute rheumatic fever), must avoid the use of anesthetics containing vasoconstrictors as ALPHACAINE. In patients with peripheral vascular disease, there is a little potential risk that vasoconstrictors cause ischemic injury or local necrosis. The presence of Sodium Bisulfite in the formula must be taken into account when treating patients who are susceptible to asthma. Parents should be advised, as well as people liable for patients with mental disturbance, to observe them, in order to avoid possible inadvertent trauma to the lips. This product is not to be used if the solution is yellowish or with particles. In elderly patients, in who the metabolic, renal and hepatic functions are usually diminished, care must be taken in terms of administering the smallest necessary dose that is enough for providing a specific kind of anesthesia. Care should be taken in the use of ALPHACAINE in patients with liver or kidney problems and in patients susceptible to asthma. The use in children under 10 years old should follow the recommendations described in Dosage. There aren't available adequate and well-controlled studies in pregnant and breastfeeding women so ALPHACAINE must be used, in this risk group, carefully and under professional supervision. There is no data available on the possible excretion of lidocaine in human milk and as many drugs are excreted in this way, it is recommended special caution when this product is administered to mothers during the breastfeeding period. 6. DRUG INTERACTIONS According to studies undertaken by P. Henry and J. Van der Driessche of the pharmacology laboratory of the Rennes University Hospital Center, the use of local anesthetic associated with the consumption of alcohol and/or tranquilizing medication directly interferes in the efficiency of the anesthetic, potentially increasing or decreasing its time of action and potency. ALPHACAINE should not be used in patients in treatment with drugs known to affect blood pressure, as monoamine oxidase inhibitors, tricyclic antidepressants or phenothiazines. Serious cardiac arrhythmia may occur if preparations containing vasoconstrictors are used in patients during or after the administration of halotane, trichloroethylene, cyclopropane or chloroform. Concurrent administration of vasopressor drugs and ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents. 7. STORAGE CONDITIONS Excessive heat (temperature above 40°C) must be avoided, protect from light. The expiry date of this produc t is equivalent to 24 months after manufacturing date. Batch number and manufacturing and expiry date: see product box. Do not use medicine with expiry date. Store in its original package. Before use, observe the medicine aspect. Every drug should be kept out of the reach of children. 8. DOSAGE AND HOW TO USE As occurs with all local anesthetics, dosages vary and depend on the area to be anesthetized, the vascularity of tissues, the number of nerve segments to be blocked, the individual tolerance and the technique of anesthesia. The least volume of injection that results in effective local anesthesia should be administered. The necessary dosage must be determined on an individual basis. The maximum dosage suggested by the Council on Dental Therapeutics of the American Dental Association and the USP Convention is 4.4 mg/kg for lidocaine with or without a vasoconstrictor additive. This dose still allows for a significant volume of drug to be used to achieve profound clinical anesthesia with a somewhat diminished risk of development of toxic (overdose) reactions. For children of less than ten years who have a normal lean body mass and normal body development, the maximum dose may be determined by the application of one of the standard pediatric drug formulas (e.g., Clark's rule). The maximum recommended dosage of epinephrine is 0.2 mg (or the equivalent to 5.5 cartridges of ALPHACAINE 50, 8.8 cartridges of ALPHACAINE 80 or 11 cartridges of ALPHACAINE 100) for healthy adult patients. The maximum recommended dosage for epinephrine-sensitive patients, such as ASA III and ASA IV and clinically hyperthyroid patients, is 0.04 mg of epinephrine (1 cartridge of ALPHACAINE 50, 1and ½ cartridge of ALPHACAINE 80 or 2 cartridges of ALPHACAINE 100) per appointment. In oral infiltration and/or mandibular block, initial dosages of 1.0-5.0 ml of lidocaine (1/2 to 21/2 cartridges of ALPHACAINE) are usually effective. In children under 10 years of age it is rarely necessary to administer more than one-half cartridge of ALPHACAINE (0.9 to 1.0 ml of lidocaine) per procedure, to achieve local anesthesia for a procedure involving a single tooth. During administration, it is recommended to perform a slight aspiration in order to avoid the risks of intravenous injection. Maximum dose: 4.4 mg of lidocaine hydrochloride/kg and 0.2 mg of epinephrine/kg (Each 1.8 ml cartridge contains 36 mg of lidocaine hydrochloride) Weight Number of (Kg) ALPHACAINE 50 Cartridges 1 (44 mg) 10 2 (88 mg) 20 3,5 (132 mg) 30 40 40 4,5 (176 mg) 6 (220 mg) 50 6 (220 mg) 60 6 (220 mg) 70 6 (220 mg) 80 6 (220 mg) 90 6 (220 mg) 100 Number of Number of Number of ALPHACAINE 80 ALPHACAINE 100 ALPHACAINE 200 Cartridges Cartridges Cartridges 1 (44 mg) 2 (88 mg) 3,5 (132 mg) 40 4,5 (176 mg) 6 (220 mg) 7 (264 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 1 (44 mg) 2 (88 mg) 3,5 (132 mg) 40 4,5 (176 mg) 6 (220 mg) 7 (264 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 1 (44 mg) 2 (88 mg) 3,5 (132 mg) 40 4,5 (176 mg) 6 (220 mg) 7 (264 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) 8 (300 mg) Doses indicated are the maximum suggested for normal healthy individuals: they should be decreased for debilitated or elderly patients. It is recommended that chemical disinfection of the cartridge cap be accomplished by wiping it thoroughly with a pledget of cotton that has been moistened with 70% ethyl alcohol just prior to use. Immersion is not recommended. During administration, it is recommended to perform a slight aspiration in order to avoid the risks of an undesirable intra-vascular injection. However, it should be noted that the absence of blood in the syringe does not guarantee that intravascular injection was avoided and a double aspiration is always recommended. Cartridges partially used should not be reused. 9. ADVERSE REACTIONS Side effects following lidocaine administration are similar to those observed in other amide-based anesthetics. Adverse reactions are normally the result of high plasma levels caused by excessive dosage, rapid absorption or unintentional intra-vascular injection, or may result from hypersensitivity, idiosyncrasy, or reduced tolerance on the part of the patient. Effects involving cardiovascular and central nervous systems may occur. Reactions in the CNS are exciting and/or depressing and may be characterized by photo-phobia, irritability, apprehension, euphoria, confusion, dizziness, drowsiness, ringing in the ears, blurred vision, vomiting, burning sensation, cold or numbness, loss of consciousness, respiratory depression and arrest. Cardiovascular reactions are normally depressive and characterized by bradycardia, hypertension and cardiovascular collapse, which may lead to cardiac arrest. Signs and symptoms of a depressed cardiovascular system are commonly the result of a vasovagal reaction but may also be the result of a direct effect of the drug. The health care professional should have support treatments for these reactions available within easy reach so as to effect a rapid response if, and when, necessary. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use. Allergy to amide local anesthetics is virtually nonexistent; true, documented and reproducible allergic reactions are extremely rare, though possible. Mild allergic reactions may include cutaneous lesions, itchiness and edema. Anaphylactic reactions are extremely rare. Neurological reactions, as persistent neurological deficiency, associated with the use of local anesthetics may be related to the technique used, the total dose of anesthetic administered, the route of administration and the patient's physical condition. Paresthesia may occur using ALPHACAINE. In case of adverse events, notify the Health Surveillance Notifications System – NOTIVISA, available at www.anvisa.gov.br/hotsite/notivisa/index.htm, or the Health Surveillance of State or City. 10. OVERDOSE Generalized reactions in the central nervous system or cardiovascular reactions are generally related to high plasmatic levels due to accidental intravenous injection or overdose (See Warnings and Adverse R eactions). The first signs and symptoms of lidocaine overdose may be drowsiness, leading to a loss of consciousness and respiratory arrest. In such cases, the following procedure should be followed: - Place the patient in the supine position. Raise the legs 30-45 above horizontal level. - The passage of air must be ensured. If the ventilation is inadequate, ventilate the patient with oxygen if possible. - If the pulse is weak (<40) or non-determinable, initiate external cardiac massage. - Support treatment of circulatory deficiency may require the intravenous administration of parenteral solutions (saline). In case of poisoning call 0800 722 6001, if you need further informations. SALES UNDER MEDICAL PRESCRIPTION FOR PROFESSIONAL USE ONLY Approved by ANVISA in 21/05/2013. Fabricado e distribuído por/ Fabricado y distribuido por/ Manufactured and distributed by: Estrada do Guerenguê, 2059 - Rio de Janeiro/RJ - Brasil CEP: 22713-002 CNPJ : 33.112.665/0001-46 Indústria Brasileira/Industria Brasileña/Made in Brazil SAC: 0800 602 68 80 Fax: 55 (21) 3342-4009 www.dfl.com.br - [email protected] Farmacêutico Responsável/Farmacéutico Responsable/ Pharmacist in Charge: Evaldo Rodrigues de Oliveira CRF-RJ N°: 2897 MS N°: 101770016 consumo de alcohol y de medicamentos tranquilizantes interfiere directamente en la eficiencia del anestésico ya sea aumentando o disminuyendo su tiempo de acción o afectando su potencia. ALPHACAINE no se debe usar en pacientes que hagan uso de medicamentos provocan alteraciones de la presión arterial como inhibidores de la monoaminooxidase (MAO), antidepresivos tricíclicos y fenotiacinas. Pueden ocurrir serias arritmias cardíacas si se emplean preparaciones con vasoconstrictores durante o después de la administración de halotano, tricloroetileno, ciclopropano o cloroformo. La administración simultánea de fármacos vasopresores y de drogas oxitócicas del tipo ergot puede causar hipertensión severa persistente o accidentes vasculares cerebrales. Rev. 12