Bula do profissional da saúde - MEPISV DFL INDÚSTRIA E COMÉRCIO S/A
A eficácia do cloridrato de mepivacaína é equivalente à do cloridrato de lidocaína. MALAMED, SF. Manual de Anestesia Local. 5a. Ed. Elsevier, 2005.
Mepisv é indicado para a anestesia local em odontologia. Indicado para a produção de anestesia local por infiltração ou bloqueio, para intervenções odontológicas em geral, extrações múltiplas, próteses imediatas e procedimentos endodônticos.
Os AL tipo amida são contra-indicados a pacientes que apresentem hipertermia maligna (hiperpirexia). A insuficiência hepática é uma contra-indicação relativa à administração de anestésicos locais. Isto inclui pacientes submetidos à diálise renal e aqueles com nefrite túbulo intersticial crônica. Insuficiência hepática e cardiovascular significativas e a tireotoxicose (hipertireoidismo) são contra-indicações relativas ao uso dos AL. A hipersensibilidade aos AL do tipo amida e a quaisquer componentes presentes na composição de Mepisv é uma contra-indicação absoluta. MALAMED, SF. Manual de Anestesia Local. 5a. Ed. Elsevier, 2005.
MODO DE USAR E CUIDADOS DE CONSERVAÇÃO DEPOIS DE ABERTO
Carregue um carpule na seringa-carpule. Perfure o local a ser anestesiado. Realize aspiração antes da injeção da solução anestésica, a fim de minimizar a probabilidade de injeção intravascular. Retire a seringa, destrua a agulha e descarte o carpule após o uso, mesmo que o conteúdo não tenha sido utilizado totalmente.
POSOLOGIA
Como para todos os AL, a dose varia e depende da região a ser anestesiada, da vascularização dos tecidos, da tolerância individual e da técnica de anestesia. Deve ser administrada a menor dose necessária para produzir anestesia eficaz. A dose máxima é de 4,4 mg/Kg sem ultrapassar 300 mg (equivalente a 5 carpules para adultos saudáveis normais); a dose deve ser reduzida em pacientes clinicamente comprometidos, debilitados ou idosos. MALAMED, SF. Manual de Anestesia Local. 5a. Ed. Elsevier, 2005.
Doses máxima em carpules para pacientes saudáveis (4,4 mg de cloridrato de mepivacaína / Kg – cada carpule de 1,8 ml contém 54 mg de cloridrato de mepivacaína).
| Peso do Paciente (em Kg) | 10 | 20 | 30 | 40 | 50 | 60 | 70 | 80 | igual ou acima de 90 |
| * N° de Carpules | 0,5 | 1,5 | 2,0 | 3,0 | 4,0 | 4,5 | 5,5 | 5,5 | 5,5 |
* n° de carpules = arredondado para meio carpule
ADVERTÊNCIAS
Os carpules não devem ser autoclavados. Caso o dentista deseje realizar uma assepsia externa do carpule, deve-se aplicar um lenço umedecido com álcool isopropílico a 91% ou álcool etílico a 70% ao diafragma de borracha. Os carpules não devem ser mergulhados em álcool ou em qualquer outra solução desinfetante.
Os dentistas que utilizam anestésicos locais em seus consultórios devem conhecer o diagnóstico e tratamento de emergências que podem surgir. Assim, deve existir equipamento de reanimação, de oxigenação e fármacos de reanimação para uso imediato. Os pacientes devem ser informados sobre a possibilidade de perda temporária de sensação e função muscular após a injeção infiltrativa e de bloqueio.
Os pacientes devem ser avisados para estarem atentos enquanto estruturas como língua, lábios, mucosas e palato estiverem anestesiadas, a fim de evitar traumas nessas estruturas. A alimentação deve ser suspensa até a recuperação da função normal dessas estruturas. O prazo de validade de Mepisv é de 36 meses.
Nenhum medicamento deve ser usado após estar vencido o seu prazo de validade. Lembrar-se de que a presença de precipitação, partículas em suspensão, turvação e alteração na coloração do produto torna inconveniente seu uso. As condições sistêmicas do paciente devem ser previamente analisadas antes de qualquer intervenção odontológica a fim de se evitar efeitos adversos. Lembrar-se de que a administração de qualquer solução anestésica local deve ser feita lentamente. MALAMED, SF. Manual de Anestesia Local. 5a. Ed. Elsevier, 2005.
“Para evitar vazamento da solução durante a injeção, certifique-se da penetração da agulha no centro do diafragma de borracha durante o carregamento da seringa. Uma penetração fora do centro produz uma punção de formato oval que pode permitir o vazamento ao redor da agulha. Outras causas de vazamento e quebra incluem seringas desgastadas, seringas sem aspiração, seringas com arpão torto e seringas não projetadas para carpules de 1,8mL”.
USO EM IDOSOS, CRIANÇAS E OUTROS GRUPOS DE RISCO
Grávidas e mulheres em período de amamentação: Segundo Haas (2002) os AL usados em odontologia podem ser administrados às gestantes (o cloridrato de mepivacaína está na categoria C do FDA). Entretanto, deve-se sempre fazer a aspiração antes da injeção do anestésico a fim de evitar a injeção intra-vascular. Não se sabe se o cloridrato de mepivacaína é excretado no leite materno.
Crianças: A principal preocupação com pacientes pediátricos é a relativa facilidade de induzir uma superdose. Assim, antes da administração do AL à criança, o dentista deve determinar o peso da criança e calcular a máxima dose. Aconselha-se selecionar a solução contendo a menor concentração de AL.
Idosos: É prudente administrar uma dose de AL bem abaixo da dose máxima, visto que pacientes idosos podem apresentar algum comprometimento hepático e/ou cardiovascular. HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 n° 9, October, 2002.
Interações com medicamentos: Em geral, os depressores do SNC como narcóticos, opióides, ansiolíticos, fenotiazínicos, barbitúricos e anti-histamínicos, quando empregados em conjunto com AL, levam à potencialização das ações cardiorespiratórias dos AL. O uso conjunto de AL e drogas que compartilham uma via metabólica comum pode produzir reações adversas. Os fármacos que induzem a produção de enzimas microssomais hepáticas, como os barbitúricos, podem alterar a velocidade de metabolização dos AL com ligação amida. Assim, o aumento da indução das enzimas microssomais hepáticas, aumentará a velocidade de metabolismo do AL. HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 n° 9, October, 2002 e MALAMED, SF. Manual de Anestesia Local. 5a. Ed. Elsevier, 2005.
Interações com exames: A injeção intramuscular de cloridrato de mepivacaína pode resultar em um aumento dos níveis da creatinina fosfoquinase. Dessa forma, a determinação dessa enzima como diagnóstico da presença de infarto agudo do miocárdio, sem a separação da isoenzima, pode comprometer o resultado deste exame. POLOCAINE® DENTAL Prescribing information Dentsply Pharmaceutical, PM-CS-PI-0003 Rev.10/01.
Injectable sterile solution of Mepivacaine Hydrochloride 3% (30 mg/ml) without vasoconstrictor
ROUTE OF ADMINISTRATION
Parenteral injection, intraosseous, conjunctival and intracanal injection.
PRESENTATION
Each cartridge contains 10, 30, 50 or 100 carpules of 1.8 ml glass tubes.
PEDIATRIC AND ADULT USE
COMPOSITION
Each 1.8 ml carpule contains:
Mepivacaine Hydrochloride.........................54,0 mg
Excipients: q.s.p................................................1,8 ml
Excipients: Sodium Chloride and Water for Injection
TECHNICAL INFORMATION FOR HEALTH PROFESSIONALS
PHARMACOLOGICAL CHARACTERISTICS
Local anesthetics (LA) prevent the generation and conduction of a nervous impulse, causing loss of sensitivity without loss of consciousness. The mechanism of action is based on the theory of the specific receptor, which proposes that local anesthetics act through their direct binding to specific receptors in the sodium channel, blocking them, causing a reduction or elimination of the permeability of the channel to sodium ions, interrupting nerve conduction (non-depolarizing nerve block). LA can also act, through competitive antagonism, with calcium ions, displacing calcium ions from the sodium channel receptor, allowing the al to be connected to this receiver. The LA produce a reduction very much small practically insignificant in conductance of ions potassium. The hydrochloride mepivacaine (1-methyl-2 ,6 -pipecoloxylidida hydrochloride) is a LA of the amide type, being relatively resistant to hydrolysis. It has a PKa of 7.6 and a protein binding of 75%.
It presents a rapid onset of action (1.5 to 2 min) and a half-life time of 90 minutes for hydrochloride mepivacaine. Amide-like LA easily crosses the blood-brain barrier, placenta and enters the circulatory system of the developing fetus. The primary site of biotransformation of amide-type LA is the liver, due to micrososome mixed function oxidases. Hydroxylation and N- demethylation play important roles in the metabolism of mepivacaine hydrochloride. Excretion is renal, and about 1.0 to 16.0 % is excreted unchanged in the urine. The pH of an anesthetic solution and the pH of the tissue in which it is injected has great influence on its nerve block action. Tissue acidification reduces the effectiveness of local anesthesia. There is inadequate anesthesia when local anesthetics are injected into infected or inflamed areas. Mepivacaine hydrochloride produces only slight vasodilation. The expected duration of anesthetic action are: 20 to 40 minutes for pulp anesthesia and 2 to 3 hours for tissue anesthesia. MALAMED, SF. Manual of Local
Anesthesia. 5th Ed. Elsevier, 2005.
EFFICACY RESULTS
The efficacy of mepivacaine hydrochloride is equivalent to that of lidocaine hydrochloride. MALAMED, SF.
Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
INDICATIONS
Mepisv is indicated to the anesthesia local in dentistry. Indicated to the production of anesthesia local for infiltration or blockage, for dental interventions in general, multiple extractions, immediate prostheses and procedures endodontics.
CONTRAINDICATIONS
Amide-like LA are contraindicated to patients with malignant hyperthermia (hyperpyrexia). Liver failure is a contraindication on to administration of anesthetics local. This includes patients submitted to dialysis kidney and those with nephritis interstitial tubule chronic. Failure liver and cardiovascular significant and the thyrotoxicosis (hyperthyroidism) are contraindications relating to the use of LA. The hypersensitivity to al of the type amida and the any components gifts in composition of Mepisv is an absolute contraindication. MALAMED, SF. Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
HOW TO USE AND CARE OF STORAGE AFTER OPEN
Load a carpule into the carpule syringe. Pierce the site to be anesthetized. Perform aspiration before injection of the anesthetic solution in order to minimize the likelihood of intravascular injection. Remove the syringe, destroy the needle and discard the carpule after use, even if the contents have not been fully used
DOSAGE
As for all LA, the dose varies and depends on the region to be anesthetized, tissue vascularization, individual tolerance and anesthesia technique. The lowest dose required to produce effective anesthesia should be administered. The maximum dose is 4.4 mg/kg without exceeding 300 mg (equivalent to 5 carpules for normal healthy adults); dose should be reduced in clinically compromised, debilitated, or elderly patients. MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier, 2005.
Maximum doses in carpules for healthy patients (4.4 mg of mepivacaine hydrochloride / Kg – each 1.8 ml carpule contains 54 mg of mepivacaine hydrochloride).
| Patient Weight (in Kg) | 10 | 20 | 30 | 40 | 50 | 60 | 70 | 80 | Equal to or above 90 |
| * N° of Carpules | 0,5 | 1.5 | 2,0 | 3,0 | 4,0 | 4,5 | 5,5 | 5,5 | 5,5 |
* carpule number = rounded to half carpule
WARNINGS
Carpules should not be autoclaved. If the dentist wishes to perform an external asepsis of the carpule, a handkerchief moistened with 91% isopropyl alcohol or 70% ethyl alcohol should be applied to the rubber diaphragm. Carpule should not be dipped in alcohol or any other disinfectant solution. Dentists who use local anesthetics in their offices should know the diagnosis and treatment of emergencies that can arise. Like this must exist equipment of resuscitation of oxygenation and drugs resuscitation to use immediate. The patients should be informed about the possibility of loss temporary of feeling and function after infiltrative and blocking injection. Patients should be advised to be vigilant while structures such as tongue, lips, mucous membranes and palate are anesthetized in order to avoid trauma to these structures. The power supply should be suspended until the function is re-started normal these structures. The shelf life of Mepisv is 36 Months. No medicine must be used after its expiry date has expired. Remember that the presence of precipitation, particles in suspension, turbidity and change in color of the product makes inconvenient your use. The conditions systemic of the patient should be previously analyzed before of any intervention dental the end of if avoid effects adverse. Remember of that the administration of any solution anesthetic local should be done slowly. MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier 2005.
„To prevent leakage of the solution during injection, make sure that the needle is penetrated into the center of the rubber diaphragm while loading the syringe. A penetration outside the center produces an oval-shaped puncture that can allow leakage around the needle. Other causes of leakage and breakage include worn syringes, unaspirationd syringes, syringes with a snare harpoon, and undesigned 1.8mL carpule syringes.“
USE IN THE ELDERLY, CHILDREN AND OTHER RISK GROUPS
Pregnant women and women in breastfeeding: According to Haas (2002) LA used in dentistry can be administered to pregnant women (mepivacaine hydrochloride is in category C of the FDA). However, aspiration should always be done before injection of the anesthetic in order to avoid intravascular injection. It is not known whether mepivacaine hydrochloride is excreted in breast milk.
Children: The main concern with pediatric patients is the relative ease of inducing an overdose. Thus, before the administration of LA to the child, the dentist should determine the weight of the child and calculate the maximum dose. It is advisable to select the solution containing the lowest concentration of LA.
Elderly: It is prudent to administer a dose of AL well below the maximum dose, as elderly patients may have some hepatic and/or cardiovascular impairment. HAAS, D. An update on Local Anesthetics in Dentistry.
Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002.
DRUG INTERACTIONS
Drug interactions : In general, CNS depressants such as narcotics, opioids, anxiolytics, phenothiazinics, barbiturates and antihistamines, when employees in set with al take to potentiation of actions cardiorespiratory of LA. The use LA set and drugs that share a common metabolic pathway may produce adverse reactions.
Drugs that induce the production of hepatic microsomore enzymes, such as barbiturates, may alter the rate of metabolization of amide-linked AL. Thus, the increase of induction of enzymes micrososomes liver increase the speed of metabolism of the AL. Haas D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002 and MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier 2005.
Exam interactions: Intramuscular injection of mepivacaine hydrochloride may result in an increase in creatinine phosphokinase levels. This way the determination this enzyme as diagnosis of presence of infarction acute of the infarction without the separation may compromise the outcome of this test. POLOCAINE® DENTAL Prescribing information Dentsply Pharmaceutical, PM- CS-PI-0003 Rev.10/01.
ADVERSE DRUG REACTIONS
Adverse reactions after administration of mepivacaine hydrochloride are similar in nature to the reactions observed with other local amide-like anesthetics. These reactions are usually dose-dependent and may be the result of a high plasma concentration. The following effects are most frequently reported:
CNS: The initial clinical signs and symptoms of CNS toxicity are excitatory in nature.
With the increase in blood level of an LA above its therapeutic value, adverse reactions will be observed. The initial clinical signs and symptoms of overdose (toxicity) originate from the CNS and are of excitatory origin, such as: signs of difficult speech, chills, muscle contraction, tremors of the muscles of the face and distal extremities and symptoms of warm and flushed skin sensation, generalized delirium, dizziness, visual disturbances such as inability to focus, hearing disorder such as tinnitus, drowsiness and disorientation. Paresthesia bilateral of tongue and region perioral right sign of a reaction toxic due to high levels of LA. The excitement after the administration of an LA should serve as a warning to the clinician of an increasing blood level of LA and the possibility of a generalised tonic-clonic convulsive episode if plasma levels continue to raise.
Cardiovascular system: Myocardium: LA produces myocardial depression related to the plasma level of LA (superdose). The action of the LA reduces the excitability electric of the infarction reduces the speed of driving and reduces the force of contraction. Peripheral vascular network: LA produce peripheral vasodilation, through the relaxation of smooth muscle of blood vessel walls, resulting in a slight degree of hypotension, an increase in incoming and outgoing blood flow at the al administration site, with consequent increase in the rate of absorption of LA and decreased duration of LA action, increased bleeding in the treatment area , increased blood levels of LA and increased the possibility of superdose.
Myocardial depression associated with peripheral vasodilation results in hypotension.
System Respiratory: In Levels lower to overdose have a action relaxing direct about the muscle smooth bronchial; In overdose levels may produce respiratory arrest as a result of generalised depression of the CNS.
Allergic reactions: They are characterized by skin lesions, hives, edema, or anaphylactic reactions.
Psychogenic reactions: Events triggered by anxiety are among the most common adverse reactions associated with LA. They can be manifested for several symptoms as syncope hyperventilation nausea vomiting changes us beats heart and pressure blood
Paraesthesias: Prolonged anesthesia or paresthesia of the tongue and lips are known to be risks of surgical procedures such as extractions, although they can occur after procedures non-surgical. Many these reactions are transitional and disappear within of 8 weeks, although some reactions may be permanent.
HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002 and MALAMED, SF. Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
Injectable sterile solution of Mepivacaine Hydrochloride 3% (30 mg/ml) without vasoconstrictor
ROUTE OF ADMINISTRATION
Parenteral injection, intraosseous, conjunctival and intracanal injection.
PRESENTATION
Each cartridge contains 10, 30, 50 or 100 carpules of 1.8 ml glass tubes.
PEDIATRIC AND ADULT USE
COMPOSITION
Each 1.8 ml carpule contains:
Mepivacaine Hydrochloride.........................54,0 mg
Excipients: q.s.p................................................1,8 ml
Excipients: Sodium Chloride and Water for Injection
TECHNICAL INFORMATION FOR HEALTH PROFESSIONALS
PHARMACOLOGICAL CHARACTERISTICS
Local anesthetics (LA) prevent the generation and conduction of a nervous impulse, causing loss of sensitivity without loss of consciousness. The mechanism of action is based on the theory of the specific receptor, which proposes that local anesthetics act through their direct binding to specific receptors in the sodium channel, blocking them, causing a reduction or elimination of the permeability of the channel to sodium ions, interrupting nerve conduction (non-depolarizing nerve block). LA can also act, through competitive antagonism, with calcium ions, displacing calcium ions from the sodium channel receptor, allowing the al to be connected to this receiver. The LA produce a reduction very much small practically insignificant in conductance of ions potassium. The hydrochloride mepivacaine (1-methyl-2 ,6 -pipecoloxylidida hydrochloride) is a LA of the amide type, being relatively resistant to hydrolysis. It has a PKa of 7.6 and a protein binding of 75%.
It presents a rapid onset of action (1.5 to 2 min) and a half-life time of 90 minutes for hydrochloride mepivacaine. Amide-like LA easily crosses the blood-brain barrier, placenta and enters the circulatory system of the developing fetus. The primary site of biotransformation of amide-type LA is the liver, due to micrososome mixed function oxidases. Hydroxylation and N- demethylation play important roles in the metabolism of mepivacaine hydrochloride. Excretion is renal, and about 1.0 to 16.0 % is excreted unchanged in the urine. The pH of an anesthetic solution and the pH of the tissue in which it is injected has great influence on its nerve block action. Tissue acidification reduces the effectiveness of local anesthesia. There is inadequate anesthesia when local anesthetics are injected into infected or inflamed areas. Mepivacaine hydrochloride produces only slight vasodilation. The expected duration of anesthetic action are: 20 to 40 minutes for pulp anesthesia and 2 to 3 hours for tissue anesthesia. MALAMED, SF. Manual of Local
Anesthesia. 5th Ed. Elsevier, 2005.
EFFICACY RESULTS
The efficacy of mepivacaine hydrochloride is equivalent to that of lidocaine hydrochloride. MALAMED, SF.
Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
INDICATIONS
Mepisv is indicated to the anesthesia local in dentistry. Indicated to the production of anesthesia local for infiltration or blockage, for dental interventions in general, multiple extractions, immediate prostheses and procedures endodontics.
CONTRAINDICATIONS
Amide-like LA are contraindicated to patients with malignant hyperthermia (hyperpyrexia). Liver failure is a contraindication on to administration of anesthetics local. This includes patients submitted to dialysis kidney and those with nephritis interstitial tubule chronic. Failure liver and cardiovascular significant and the thyrotoxicosis (hyperthyroidism) are contraindications relating to the use of LA. The hypersensitivity to al of the type amida and the any components gifts in composition of Mepisv is an absolute contraindication. MALAMED, SF. Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
HOW TO USE AND CARE OF STORAGE AFTER OPEN
Load a carpule into the carpule syringe. Pierce the site to be anesthetized. Perform aspiration before injection of the anesthetic solution in order to minimize the likelihood of intravascular injection. Remove the syringe, destroy the needle and discard the carpule after use, even if the contents have not been fully used
DOSAGE
As for all LA, the dose varies and depends on the region to be anesthetized, tissue vascularization, individual tolerance and anesthesia technique. The lowest dose required to produce effective anesthesia should be administered. The maximum dose is 4.4 mg/kg without exceeding 300 mg (equivalent to 5 carpules for normal healthy adults); dose should be reduced in clinically compromised, debilitated, or elderly patients. MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier, 2005.
Maximum doses in carpules for healthy patients (4.4 mg of mepivacaine hydrochloride / Kg – each 1.8 ml carpule contains 54 mg of mepivacaine hydrochloride).
| Patient Weight (in Kg) | 10 | 20 | 30 | 40 | 50 | 60 | 70 | 80 | Equal to or above 90 |
| * N° of Carpules | 0,5 | 1.5 | 2,0 | 3,0 | 4,0 | 4,5 | 5,5 | 5,5 | 5,5 |
* carpule number = rounded to half carpule
WARNINGS
Carpules should not be autoclaved. If the dentist wishes to perform an external asepsis of the carpule, a handkerchief moistened with 91% isopropyl alcohol or 70% ethyl alcohol should be applied to the rubber diaphragm. Carpule should not be dipped in alcohol or any other disinfectant solution. Dentists who use local anesthetics in their offices should know the diagnosis and treatment of emergencies that can arise. Like this must exist equipment of resuscitation of oxygenation and drugs resuscitation to use immediate. The patients should be informed about the possibility of loss temporary of feeling and function after infiltrative and blocking injection. Patients should be advised to be vigilant while structures such as tongue, lips, mucous membranes and palate are anesthetized in order to avoid trauma to these structures. The power supply should be suspended until the function is re-started normal these structures. The shelf life of Mepisv is 36 Months. No medicine must be used after its expiry date has expired. Remember that the presence of precipitation, particles in suspension, turbidity and change in color of the product makes inconvenient your use. The conditions systemic of the patient should be previously analyzed before of any intervention dental the end of if avoid effects adverse. Remember of that the administration of any solution anesthetic local should be done slowly. MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier 2005.
„To prevent leakage of the solution during injection, make sure that the needle is penetrated into the center of the rubber diaphragm while loading the syringe. A penetration outside the center produces an oval-shaped puncture that can allow leakage around the needle. Other causes of leakage and breakage include worn syringes, unaspirationd syringes, syringes with a snare harpoon, and undesigned 1.8mL carpule syringes.“
USE IN THE ELDERLY, CHILDREN AND OTHER RISK GROUPS
Pregnant women and women in breastfeeding: According to Haas (2002) LA used in dentistry can be administered to pregnant women (mepivacaine hydrochloride is in category C of the FDA). However, aspiration should always be done before injection of the anesthetic in order to avoid intravascular injection. It is not known whether mepivacaine hydrochloride is excreted in breast milk.
Children: The main concern with pediatric patients is the relative ease of inducing an overdose. Thus, before the administration of LA to the child, the dentist should determine the weight of the child and calculate the maximum dose. It is advisable to select the solution containing the lowest concentration of LA.
Elderly: It is prudent to administer a dose of AL well below the maximum dose, as elderly patients may have some hepatic and/or cardiovascular impairment. HAAS, D. An update on Local Anesthetics in Dentistry.
Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002.
DRUG INTERACTIONS
Drug interactions : In general, CNS depressants such as narcotics, opioids, anxiolytics, phenothiazinics, barbiturates and antihistamines, when employees in set with al take to potentiation of actions cardiorespiratory of LA. The use LA set and drugs that share a common metabolic pathway may produce adverse reactions.
Drugs that induce the production of hepatic microsomore enzymes, such as barbiturates, may alter the rate of metabolization of amide-linked AL. Thus, the increase of induction of enzymes micrososomes liver increase the speed of metabolism of the AL. Haas D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002 and MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier 2005.
Exam interactions: Intramuscular injection of mepivacaine hydrochloride may result in an increase in creatinine phosphokinase levels. This way the determination this enzyme as diagnosis of presence of infarction acute of the infarction without the separation may compromise the outcome of this test. POLOCAINE® DENTAL Prescribing information Dentsply Pharmaceutical, PM- CS-PI-0003 Rev.10/01.
ADVERSE DRUG REACTIONS
Adverse reactions after administration of mepivacaine hydrochloride are similar in nature to the reactions observed with other local amide-like anesthetics. These reactions are usually dose-dependent and may be the result of a high plasma concentration. The following effects are most frequently reported:
CNS: The initial clinical signs and symptoms of CNS toxicity are excitatory in nature.
With the increase in blood level of an LA above its therapeutic value, adverse reactions will be observed. The initial clinical signs and symptoms of overdose (toxicity) originate from the CNS and are of excitatory origin, such as: signs of difficult speech, chills, muscle contraction, tremors of the muscles of the face and distal extremities and symptoms of warm and flushed skin sensation, generalized delirium, dizziness, visual disturbances such as inability to focus, hearing disorder such as tinnitus, drowsiness and disorientation. Paresthesia bilateral of tongue and region perioral right sign of a reaction toxic due to high levels of LA. The excitement after the administration of an LA should serve as a warning to the clinician of an increasing blood level of LA and the possibility of a generalised tonic-clonic convulsive episode if plasma levels continue to raise.
Cardiovascular system: Myocardium: LA produces myocardial depression related to the plasma level of LA (superdose). The action of the LA reduces the excitability electric of the infarction reduces the speed of driving and reduces the force of contraction. Peripheral vascular network: LA produce peripheral vasodilation, through the relaxation of smooth muscle of blood vessel walls, resulting in a slight degree of hypotension, an increase in incoming and outgoing blood flow at the al administration site, with consequent increase in the rate of absorption of LA and decreased duration of LA action, increased bleeding in the treatment area , increased blood levels of LA and increased the possibility of superdose.
Myocardial depression associated with peripheral vasodilation results in hypotension.
System Respiratory: In Levels lower to overdose have a action relaxing direct about the muscle smooth bronchial; In overdose levels may produce respiratory arrest as a result of generalised depression of the CNS.
Allergic reactions: They are characterized by skin lesions, hives, edema, or anaphylactic reactions.
Psychogenic reactions: Events triggered by anxiety are among the most common adverse reactions associated with LA. They can be manifested for several symptoms as syncope hyperventilation nausea vomiting changes us beats heart and pressure blood
Paraesthesias: Prolonged anesthesia or paresthesia of the tongue and lips are known to be risks of surgical procedures such as extractions, although they can occur after procedures non-surgical. Many these reactions are transitional and disappear within of 8 weeks, although some reactions may be permanent.
HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002 and MALAMED, SF. Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
SUPERDOSE
LA-related emergencies are usually a consequence of high plasma concentrations. Thus, the best approach is prevention, accompanied by monitoring of cardiorespiratory vital signs and patient awareness after each injection of LA. At any sign of alteration, it is advisable to administer oxygen. The first measure in seizure control is to maintain the patient's oxygenation level. If the seizure persists, an ultra-fast-acting barbiturico or intravenous benzodiazepine should be administered. The professional should be familiar with these anticonvulsant drugs prior to the use of LA. Auxiliary treatment may be necessary to control cardiovascular depression, such as intravenous administration of fluids and vasopressors. If not treated immediately, both convulsion and depression cardiovascular can result in hypoxia bradycardia arrhythmias and stop heart. Case occur stop heart standard cardiopulmonary resuscitation procedure should be established.
Dialysis no presents value in treatment of toxicity acute of the hydrochloride of mepivacaine. In mice female the DL50 intravenous mepivacaine hydrochloride is 33 mg/kg and subcutaneous DL50 is 258 mg/kg.
POLOCAINE® DENTAL prescribing information. Dentsply Pharmaceutical, PM-CS-PI-0003 Rev.10/01.
In cases of adverse events, notify by VigiMed system, available on the Anvisa Portal.
STORAGE
Store at room temperatura from 15°C to 30 °C and away from light.
Lot number, date of manufacture and expiration date: See packaging.
PROFESSIONAL USE
EVERY MEDICINE MUST BE KEPT OUT OF THE REACH OF CHILDREN
LEGAL SAYINGS
MS Register: 1.0177.0030
Responsible Pharmacist :
Renata Caroline Magalhães – CRF-RJ 21674
Manufactured and Packaged by:
Injectable sterile solution of Mepivacaine Hydrochloride 3% (30 mg/ml) without vasoconstrictor
Parenteral injection, intraosseous, conjunctival and intracanal injection.
Each cartridge contains 10, 30, 50 or 100 carpules of 1.8 ml glass tubes.
PEDIATRIC AND ADULT USE
Each 1.8 ml carpule contains:
Mepivacaine Hydrochloride.........................54,0 mg
Excipients: q.s.p................................................1,8 ml
Excipients: Sodium Chloride and Water for Injection
TECHNICAL INFORMATION FOR HEALTH PROFESSIONALS
Local anesthetics (LA) prevent the generation and conduction of a nervous impulse, causing loss of sensitivity without loss of consciousness. The mechanism of action is based on the theory of the specific receptor, which proposes that local anesthetics act through their direct binding to specific receptors in the sodium channel, blocking them, causing a reduction or elimination of the permeability of the channel to sodium ions, interrupting nerve conduction (non-depolarizing nerve block). LA can also act, through competitive antagonism, with calcium ions, displacing calcium ions from the sodium channel receptor, allowing the al to be connected to this receiver. The LA produce a reduction very much small practically insignificant in conductance of ions potassium. The hydrochloride mepivacaine (1-methyl-2 ,6 -pipecoloxylidida hydrochloride) is a LA of the amide type, being relatively resistant to hydrolysis. It has a PKa of 7.6 and a protein binding of 75%.
It presents a rapid onset of action (1.5 to 2 min) and a half-life time of 90 minutes for hydrochloride mepivacaine. Amide-like LA easily crosses the blood-brain barrier, placenta and enters the circulatory system of the developing fetus. The primary site of biotransformation of amide-type LA is the liver, due to micrososome mixed function oxidases. Hydroxylation and N- demethylation play important roles in the metabolism of mepivacaine hydrochloride. Excretion is renal, and about 1.0 to 16.0 % is excreted unchanged in the urine. The pH of an anesthetic solution and the pH of the tissue in which it is injected has great influence on its nerve block action. Tissue acidification reduces the effectiveness of local anesthesia. There is inadequate anesthesia when local anesthetics are injected into infected or inflamed areas. Mepivacaine hydrochloride produces only slight vasodilation. The expected duration of anesthetic action are: 20 to 40 minutes for pulp anesthesia and 2 to 3 hours for tissue anesthesia. MALAMED, SF. Manual of Local
Anesthesia. 5th Ed. Elsevier, 2005.
The efficacy of mepivacaine hydrochloride is equivalent to that of lidocaine hydrochloride. MALAMED, SF.
Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
Mepisv is indicated to the anesthesia local in dentistry. Indicated to the production of anesthesia local for infiltration or blockage, for dental interventions in general, multiple extractions, immediate prostheses and procedures endodontics.
Amide-like LA are contraindicated to patients with malignant hyperthermia (hyperpyrexia). Liver failure is a contraindication on to administration of anesthetics local. This includes patients submitted to dialysis kidney and those with nephritis interstitial tubule chronic. Failure liver and cardiovascular significant and the thyrotoxicosis (hyperthyroidism) are contraindications relating to the use of LA. The hypersensitivity to al of the type amida and the any components gifts in composition of Mepisv is an absolute contraindication. MALAMED, SF. Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
Load a carpule into the carpule syringe. Pierce the site to be anesthetized. Perform aspiration before injection of the anesthetic solution in order to minimize the likelihood of intravascular injection. Remove the syringe, destroy the needle and discard the carpule after use, even if the contents have not been fully used
As for all LA, the dose varies and depends on the region to be anesthetized, tissue vascularization, individual tolerance and anesthesia technique. The lowest dose required to produce effective anesthesia should be administered. The maximum dose is 4.4 mg/kg without exceeding 300 mg (equivalent to 5 carpules for normal healthy adults); dose should be reduced in clinically compromised, debilitated, or elderly patients. MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier, 2005.
Maximum doses in carpules for healthy patients (4.4 mg of mepivacaine hydrochloride / Kg – each 1.8 ml carpule contains 54 mg of mepivacaine hydrochloride).
| Patient Weight (in Kg) | 10 | 20 | 30 | 40 | 50 | 60 | 70 | 80 | Equal to or above 90 |
| * N° of Carpules | 0,5 | 1.5 | 2,0 | 3,0 | 4,0 | 4,5 | 5,5 | 5,5 | 5,5 |
* carpule number = rounded to half carpule
Carpules should not be autoclaved. If the dentist wishes to perform an external asepsis of the carpule, a handkerchief moistened with 91% isopropyl alcohol or 70% ethyl alcohol should be applied to the rubber diaphragm. Carpule should not be dipped in alcohol or any other disinfectant solution. Dentists who use local anesthetics in their offices should know the diagnosis and treatment of emergencies that can arise. Like this must exist equipment of resuscitation of oxygenation and drugs resuscitation to use immediate. The patients should be informed about the possibility of loss temporary of feeling and function after infiltrative and blocking injection. Patients should be advised to be vigilant while structures such as tongue, lips, mucous membranes and palate are anesthetized in order to avoid trauma to these structures. The power supply should be suspended until the function is re-started normal these structures. The shelf life of Mepisv is 36 Months. No medicine must be used after its expiry date has expired. Remember that the presence of precipitation, particles in suspension, turbidity and change in color of the product makes inconvenient your use. The conditions systemic of the patient should be previously analyzed before of any intervention dental the end of if avoid effects adverse. Remember of that the administration of any solution anesthetic local should be done slowly. MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier 2005.
„To prevent leakage of the solution during injection, make sure that the needle is penetrated into the center of the rubber diaphragm while loading the syringe. A penetration outside the center produces an oval-shaped puncture that can allow leakage around the needle. Other causes of leakage and breakage include worn syringes, unaspirationd syringes, syringes with a snare harpoon, and undesigned 1.8mL carpule syringes.“
Pregnant women and women in breastfeeding: According to Haas (2002) LA used in dentistry can be administered to pregnant women (mepivacaine hydrochloride is in category C of the FDA). However, aspiration should always be done before injection of the anesthetic in order to avoid intravascular injection. It is not known whether mepivacaine hydrochloride is excreted in breast milk.
Children: The main concern with pediatric patients is the relative ease of inducing an overdose. Thus, before the administration of LA to the child, the dentist should determine the weight of the child and calculate the maximum dose. It is advisable to select the solution containing the lowest concentration of LA.
Elderly: It is prudent to administer a dose of AL well below the maximum dose, as elderly patients may have some hepatic and/or cardiovascular impairment. HAAS, D. An update on Local Anesthetics in Dentistry.
Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002.
Drug interactions : In general, CNS depressants such as narcotics, opioids, anxiolytics, phenothiazinics, barbiturates and antihistamines, when employees in set with al take to potentiation of actions cardiorespiratory of LA. The use LA set and drugs that share a common metabolic pathway may produce adverse reactions.
Drugs that induce the production of hepatic microsomore enzymes, such as barbiturates, may alter the rate of metabolization of amide-linked AL. Thus, the increase of induction of enzymes micrososomes liver increase the speed of metabolism of the AL. Haas D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002 and MALAMED, SF. Manual de Anestesia Local 5a ed. Elsevier 2005.
Exam interactions: Intramuscular injection of mepivacaine hydrochloride may result in an increase in creatinine phosphokinase levels. This way the determination this enzyme as diagnosis of presence of infarction acute of the infarction without the separation may compromise the outcome of this test. POLOCAINE® DENTAL Prescribing information Dentsply Pharmaceutical, PM- CS-PI-0003 Rev.10/01.
Adverse reactions after administration of mepivacaine hydrochloride are similar in nature to the reactions observed with other local amide-like anesthetics. These reactions are usually dose-dependent and may be the result of a high plasma concentration. The following effects are most frequently reported:
CNS: The initial clinical signs and symptoms of CNS toxicity are excitatory in nature.
With the increase in blood level of an LA above its therapeutic value, adverse reactions will be observed. The initial clinical signs and symptoms of overdose (toxicity) originate from the CNS and are of excitatory origin, such as: signs of difficult speech, chills, muscle contraction, tremors of the muscles of the face and distal extremities and symptoms of warm and flushed skin sensation, generalized delirium, dizziness, visual disturbances such as inability to focus, hearing disorder such as tinnitus, drowsiness and disorientation. Paresthesia bilateral of tongue and region perioral right sign of a reaction toxic due to high levels of LA. The excitement after the administration of an LA should serve as a warning to the clinician of an increasing blood level of LA and the possibility of a generalised tonic-clonic convulsive episode if plasma levels continue to raise.
Cardiovascular system: Myocardium: LA produces myocardial depression related to the plasma level of LA (superdose). The action of the LA reduces the excitability electric of the infarction reduces the speed of driving and reduces the force of contraction. Peripheral vascular network: LA produce peripheral vasodilation, through the relaxation of smooth muscle of blood vessel walls, resulting in a slight degree of hypotension, an increase in incoming and outgoing blood flow at the al administration site, with consequent increase in the rate of absorption of LA and decreased duration of LA action, increased bleeding in the treatment area , increased blood levels of LA and increased the possibility of superdose.
Myocardial depression associated with peripheral vasodilation results in hypotension.
System Respiratory: In Levels lower to overdose have a action relaxing direct about the muscle smooth bronchial; In overdose levels may produce respiratory arrest as a result of generalised depression of the CNS.
Allergic reactions: They are characterized by skin lesions, hives, edema, or anaphylactic reactions.
Psychogenic reactions: Events triggered by anxiety are among the most common adverse reactions associated with LA. They can be manifested for several symptoms as syncope hyperventilation nausea vomiting changes us beats heart and pressure blood
Paraesthesias: Prolonged anesthesia or paresthesia of the tongue and lips are known to be risks of surgical procedures such as extractions, although they can occur after procedures non-surgical. Many these reactions are transitional and disappear within of 8 weeks, although some reactions may be permanent.
HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, October, 2002 and MALAMED, SF. Manual of Local Anesthesia. 5th Ed. Elsevier, 2005.
SUPERDOSE
LA-related emergencies are usually a consequence of high plasma concentrations. Thus, the best approach is prevention, accompanied by monitoring of cardiorespiratory vital signs and patient awareness after each injection of LA. At any sign of alteration, it is advisable to administer oxygen. The first measure in seizure control is to maintain the patient's oxygenation level. If the seizure persists, an ultra-fast-acting barbiturico or intravenous benzodiazepine should be administered. The professional should be familiar with these anticonvulsant drugs prior to the use of LA. Auxiliary treatment may be necessary to control cardiovascular depression, such as intravenous administration of fluids and vasopressors. If not treated immediately, both convulsion and depression cardiovascular can result in hypoxia bradycardia arrhythmias and stop heart. Case occur stop heart standard cardiopulmonary resuscitation procedure should be established.
Dialysis no presents value in treatment of toxicity acute of the hydrochloride of mepivacaine. In mice female the DL50 intravenous mepivacaine hydrochloride is 33 mg/kg and subcutaneous DL50 is 258 mg/kg.
POLOCAINE® DENTAL prescribing information. Dentsply Pharmaceutical, PM-CS-PI-0003 Rev.10/01.
In cases of adverse events, notify by VigiMed system, available on the Anvisa Portal.
STORAGE
Store at room temperatura from 15°C to 30 °C and away from light.
Lot number, date of manufacture and expiration date: See packaging.
PROFESSIONAL USE
EVERY MEDICINE MUST BE KEPT OUT OF THE REACH OF CHILDREN
LEGAL SAYINGS
MS Register: 1.0177.0030
Responsible Pharmacist :
Renata Caroline Magalhães – CRF-RJ 21674
Manufactured and Packaged by:
DFL Indústria e Comércio S.A
Estrada do Guerenguê, 2059 – Rio de Janeiro – RJ, Brasil
Postal Code: 22713–002
CNPJ: 33.112.665/0001–46
Brazilian Industry
SAC: 0800 602 68 80 – Fax: 55–21–3342–4009
–
SALE UNDER MEDICAL PRESCRIPTION.
Package leaflet code_14275 Rev 01
This package leaflet has been updated in accordance with Standard package leaflet approved by Anvisa in 2018/02/02
History of Change of the Package Leaflet
| Electronic submission data | Data of the petition/notification amending package leaflet | Data on changes in leaflets | |||||||
| Date of Expedient | No. expedient | Subject | Date of Expedient | No. Expedient | Subject | Date of Approval | Package leaflet items | Versions (VP/VPS) | Presentations Related 23 |
| 06/06/2018 | 0451876/18–4 | 1808 – SIMILAR -Notificação da Alteração de Texto de Bula | N.A. | N.A. | N.A. | N.A. | LEGAL SAYINGS | VPS | – 30 MG/ML SOL INJ CT BL TRANS X 10 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 30 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 50 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 100 CARP VD TRANS X 1,8 ML |
| 30/10/2018 | 1041539/18–4 | 1808 – SIMILAR -Notificação da Alteração de Texto de Bula | N.A. | N.A. | N.A. | N.A. | LEGAL SAYINGS | VPS | – 30 MG/ML SOL INJ CT BL TRANS X 10 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 30 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 50 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 100 CARP VD TRANS X 1,8 ML |
| 03/05/2019 | 0395313/19–1 | 1808 – SIMILAR -Notificação da Alteração de Texto de Bula | N.A. | N.A. | N.A. | N.A. | LEGAL SAYINGS | VPS | – 30 MG/ML SOL INJ CT BL TRANS X 10 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 30 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 50 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 100 CARP VD TRANS X 1,8 ML |
| 15/01/2020 | 0144293/20–7 | 1808 – SIMILAR -Notificação da Alteração de Texto de Bula | N.A. | N.A. | N.A. | N.A. | LEGAL SAYINGS | VPS | – 30 MG/ML SOL INJ CT BL TRANS X 10 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 30 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 50 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 100 CARP VD TRANS X 1,8 ML |
| 14/09/2020 | 3124901/20–9 | 10457 – SIMILAR – Inclusão Inicial de Texto de Bula -publicação no Bulário RDC 60/12 | N.A. | N.A. | N.A. | N.A. | Initial insertion of package leaflet text | VP | – 30 MG/ML SOL INJ CT BL TRANS X 10 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 30 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 50 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 100 CARP VD TRANS X 1,8 ML |
| 10/03/2021 | The expedient will be generated at the end of the petition | 10450 – SIMILAR – Notificação de Alteração de Texto de Bula – RDC 60/12 | N.A. | N.A. | N.A. | N.A. | PRESENTATION | VP/VPS | – 30 MG/ML SOL INJ CT BL TRANS X 10 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 30 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 50 CARP VD TRANS X 1,8 ML – 30 MG/ML SOL INJ CT BL TRANS X 100 CARP VD TRANS X 1,8 ML |
MEPISV
DFL Indústria e Comércio S.A
Solución de inyección estéril
Clorhidrato de mepivacaína 3%
MODELO DE PROSPECTO PARA EL PROFESIONAL DE LA SALUD
FORMA FARMACÊUTICA
Solución estéril inyectable de clorhidrato de mepivacaína 3% (30 mg/ml) sin vasoconstrictor
RUTA DE ADMINISTRACIÓN
Inyección parenteral, inyección intraosseosa, conjuntival e intracanal.
PRESENTACIÓN
Cada cartucho contiene 10, 30, 50 o 100 ampollas de vidrio de 1,8 ml.
USO PEDIÁTRICO Y ADULTO
COMPOSICIÓN
Cada ampolla de 1,8 ml contiene:
Clorhidrato de mepivacaína.......................54,0 mg
Excipientes: q.s.p........................................1,8 ml
Excipientes: Cloruro de sodio y agua para inyectable
INFORMACIÓN TÉCNICA PARA PROFESIONALES DE LA SALUD
CARACTERÍSTICAS FARMACOLÓGICAS
Los anestésicos locales (AL) previenen la generación y conducción de un impulso nervioso, causando la pérdida de sensibilidad sin pérdida de conciencia. El mecanismo de acción se basa en la teoría del receptor específico, que propone que los anestésicos locales actúen a través de su unión directa a receptores específicos en el canal de sodio, bloqueándolos, causando una reducción o eliminación de la permeabilidad del canal a iones de sodio, interrumpiendo la conducción nerviosa (bloque nervioso no despolarizante). Los AL también pueden actuar, através del antagonismo competitivo, con iones de calcio, desplazando los iones de calcio del receptor del canal de sodio, permitiendo la unión del AL a este receptor. Los AL producem una reducción mucho pequeno prácticamente insignificante en conductancia de iones potasio. El clorhidrato de mepivacaína (1-metil-2’,6’- clorhidrato de pipecoloxylidida) es un AL del tipo amida, siendo relativamente resistente a la hidrólisis. Tiene un PKa de 7,6 y una conexión proteica de 75%.
Presenta un rápido inicio de acción (1,5 a 2 min) y un tiempo de vida media de 90 minutos para clorhidrato de mepivacaína. Los LA de tipo amida atraviesan fácilmente la barrera hematoencefálica, la placenta y entran en el sistema circulatorio del feto en desarrollo. El sitio principal de biotransformación de los AL de tipo amida es el hígado, debido a las oxidasas microsomales de función mixta. La hidroxilación y la N -desmetilación desempenan un papel importante en el metabolismo del clorhidrato de mepivacaína. La excreción es renal, y alrededor de 1,0 a 16,0 % se excreta sin cambios en la orina. El pH de una solución anestésica y el pH del tejido en el que se inyecta tienen una gran influencia en su acción del bloqueo nervioso. La acidificación tisular reduce la eficacia de la anestesia local. Hay anestesia inadecuada cuando los anestésicos locales se inyectan en áreas infectadas o inflamadas. El clorhidrato de mepivacaína produce sólo vasodilatación leve. La duración esperada de la acción anestésica es: 20 a 40 minutos para la anestesia
de pulpa y 2 a 3 horas para la anestesia tisular. MALAMED, SF. Manual de Anestesia Local. 5o Ed.
Elsevier, 2005.
RESULTADOS DE EFICACIA
La eficacia del clorhidrato de mepivacaína es equivalente a la del clorhidrato de lidocaína. MALAMED, SF. Manual de Anestesia Local. 5o Ed. Elsevier, 2005.
INDICACIONES
Mepisv es indicado para el anestesia local en odontología. indicado para el producción de anestesia local para infiltración o bloqueo, para intervenciones dentales en general, extracciones múltiples, prótesis inmediatas y procedimientos endodoncia.
CONTRAINDICACIONES
Los AL de tipo amida están contraindicados en pacientes con hipertermia maligna (hiperpirexia). La insuficiencia hepática es una contraindicación para la administración de anestésicos locales. Esto incluye a pacientes sometidos a diálisis renal y aquellos con nefritis crónica del túbulo intersticial. La insuficiencia hepática y cardiovascular significativa y la tirotoxicosis (hipertiroidismo) son contraindicaciones relacionadas con el uso de AL. La hipersensibilidad a los AL de tipo amida y a cualquier componente presente en la composición de Mepisv es una contraindicación absoluta. MALAMED, SF. Manual de anestesia local. 5a ed. Elsevier, 2005.
CÓMO USAR Y CUIDAR EL ALMACENAMIENTO DESPUÉS DE ABRIR
Coloque una ampolla en la jeringa-carpule. Perfore el área a anestesiar. Realice la aspiración antes de la inyección de la solución anestésica para minimizar la probabilidad de una inyección intravascular. Retire la jeringa, destruya la aguja y deseche la ampolla después de su uso, incluso si el contenido no se ha agotado.
POSOLOGÍA
Como para todos los AL, la dosis varía y depende de la región a anestesiar, vascularización tisular, tolerancia individual y técnica de anestesia. Debe administrarse la dosis más baja necesaria para producir una anestesia eficaz. La dosis máxima es de 4,4 mg/kg sin exceder 300 mg (equivalente a 5 ampollas para adultos sanos normales); la dosis debe reducirse en pacientes clínicamente comprometidos, debilitados o de edad avanzada. MALAMED, SF. Manual de anestesia local. 5to. Ed. Elsevier, 2005.
Dosis máximas en ampollas para pacientes sanos (4,4 mg de clorhidrato de mepivacaína / Kg – cada 1,8 ml de ampolla contiene 54 mg de clorhidrato de mepivacaína).
| Peso del paciente (en Kg) | 10 | 20 | 30 | 40 | 50 | 60 | 70 | 80 | Igual a o superior 90 |
| * No de Ampollas | 0,5 | 1.5 | 2,0 | 3,0 | 4,0 | 4,5 | 5,5 | 5,5 | 5,5 |
* número de ampolla – redondeado a media ampolla
ADVERTENCIAS
Los carpules no deben esterilizarse en autoclave. Si el dentista desea realizar una asepsia externa de la ampolla se debe aplicar un tejido humedecido con alcohol isopropílico al 91% o alcohol etílico al 70% al diafragma de goma. Las ampollas no deben sumergirse en alcohol ni en ninguna otra solución desinfectante. Los dentistas que utilizan anestésicos locales en sus consultorios deben estar al tanto del diagnóstico y tratamiento de las emergencias que puedan surgir. Por lo tanto, debe haber equipo de reanimación, equipo de oxigenación y medicamentos de reanimación para uso inmediato. Se debe informar a los pacientes sobre la posibilidad de pérdida temporal de la sensibilidad y función muscular después de la inyección infiltrativa y bloqueante.
Se debe aconsejar a los pacientes que estén atentos mientras que las estructuras como la lengua, los labios, las membranas mucosas y el paladar se anestesian para evitar traumatismos en estas estructuras. La fuente de alimentación debe suspenderse hasta que se vuelva a iniciar la función normal estos estructuras. El vida útil de Mepisv és 36 meses. Ningún medicamento debe usarse después de su fecha de vencimiento. Recuerde que la presencia de precipitación, partículas en suspensión, turbidez y cambios en el color del producto hace que su uso sea inconveniente. El condiciones sistémica dela paciente debe ser previamente analizado antes de cualquier intervención dental el final de si evitar efectos adversos. Recuerda que la administración de cualquier solución anestésico local debe hacerse lentamente. MALAMED, SF. Manual de Anestesia Local. 5a ed. Elsevier 2005.
„Para evitar fugas de la solución durante la inyección, asegúrese de que la aguja esté penetrada en el centro del diafragma de goma mientras carga la jeringa. Una penetración fuera del centro produce una punción de forma ovalada que puede permitir fugas alrededor de la aguja. Otras causas de fugas y roturas incluyen jeringas desgastadas, jeringas sin aspiración, jeringas con arpón de caja y jeringas no disenadas para ampollas de 1,8 ml.“
USO EN ANCIANOS, NINOS Y OTROS GRUPOS DE RIESGO
Mujeres embarazadas y mujeres en la lactancia materna: Según Haas (2002) los AL utilizado en odontología se puede administrar a mujeres embarazadas (clorhidrato de mepivacaína está en la categoría C de la FDA). Sin embargo, la aspiración siempre debe hacerse antes de la inyección del anestésico para evitar la inyección intravascular. Se desconoce si el clorhidrato de mepivacaína se excreta en la leche materna.
Ninos: La principal preocupación con los pacientes pediátricos es la relativa facilidad de inducir una sobredosis. Por lo tanto, antes de la administración de AL al nino, el dentista debe determinar el peso del nino y calcular la dosis máxima. Es aconsejable seleccionar la solución que contenga la concentración más baja de AL.
Ancianos: Es prudente administrar una dosis de AL muy por debajo de la dosis máxima, ya que los pacientes de edad avanzada pueden tener alguna insuficiencia hepática y/o cardiovascular. HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, octubre de 2002.
INTERACCIONES MEDICAMENTOSAS
Interacciones con medicamentos: En general, depresores del SNC como narcóticos, opioides, ansiolíticos, fenotietiazinas, barbitúricos y antihistamínicos, cuando empleados en establecer con AL tomar para potenciación de acciones cardiorespiratoria de AL. El uso conjunto de AL y fármacos que comparten una vía metabólica común puede producir reacciones adversas. Los medicamentos que inducen la producción de enzimas microsomales hepáticas, como los barbitúricos, pueden alterar la tasa de metabolismo de AL ligada a la amida. Por lo tanto, aumentar la inducción de enzimas hepáticas microsomales aumentará la tasa de metabolismo de AL. HAAS D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, octubre de 2002 y MALAMED, SF. Manual de anestesia local. 5a ed. Elsevier 2005.
Interacciones de examen: La inyección intramuscular de clorhidrato de mepivacaína puede provocar un aumento en los niveles de creatina fosfoquinasa. Por tanto, la determinación de esta enzima como el diagnóstico de la presencia de infarto agudo de miocardio, sin la separación de la isoenzima, puede comprometer el resultado de este examen. POLOCAÍNA® DENTAL Prescribing information Dentsply Pharmaceutical, PM- CS-PI-0003 Rev.10/01.
REACCIONES ADVERSAS A LOS MEDICAMENTOS
Las reacciones adversas después de la administración de clorhidrato de mepivacaína son similares en naturaleza a las reacciones observadas con otros anestésicos locales similares a la amida. Estas reacciones generalmente dependen de la dosis y pueden ser el resultado de una alta concentración plasmática. Los siguientes efectos son los más frecuentes:
SNC: Los signos y síntomas clínicos iniciales de la toxicidad del SNC son de naturaleza excitatoria.
Con el aumento en el nivel de sangre de una AL por encima de su valor terapéutico, se observarán reacciones adversas. Los signos y síntomas clínicos iniciales de sobredosis (toxicidad) se originan en el SNC y son de origen excitatorio, tales como: signos de dificultad del habla, escalofríos, contracción muscular, temblores de los músculos de la cara y las extremidades distales y síntomas de sensación cutánea cálida y enrojecida, delirio generalizado, mareos, alteraciones visuales como la incapacidad para enfocarse, trastorno auditivo como titus, somnolencia y disiente.
Paresthesia bilateral de lengua y región perioral correcto firmar de un reacción nocivo pendiente para alto niveles de AL. La excitación después de la administración de un AL debe servir como una advertencia para el médico de un aumento del nivel sanguíneo del AL y de la posibilidad de un episodio convulsivo tónico-clónico generalizado si los niveles plasmáticos continúan aumentando.
Sistema cardiovascular: Miocardio: los AL producen una depresión del miocardio relacionada con el nivel plasmático de AL (sobredosis). La acción de AL reduce la excitabilidad eléctrica del miocardio, reduce la velocidad de conducción y reduce la fuerza de contracción. Rede vascular periférica: los AL producen vasodilatación periférica, al relajar el músculo liso de las paredes de los vasos sanguíneos, lo que da como
resultado un grado leve de hipotensión, un aumento del flujo sanguíneo dentro y fuera del lugar de administración del AL, con el consiguiente aumento de la velocidad de absorción. de AL y disminución de la duración de acción de AL, aumento del sangrado en el área de tratamiento, aumento de los niveles sanguíneos de AL y aumento de la posibilidad de sobredosis.
La depresión miocárdica asociada con vasodilatación periférica produce hipotensión
Sistema Respiratorio: En niveles inferior para sobredosis tienes una acción relajante directa acerca de el músculo liso bronquial; En los niveles de sobredosis pueden producir paro respiratorio como resultado de la depresión generalizada de la CNS.
Reacciones alérgicas: Se caracterizan por lesiones cutáneas, urticaria, edema o reacciones anafilácticas.
Reacciones psicogénicas: Los eventos desencadenados por la ansiedad se encuentran entre las reacciones adversas más comunes asociadas con LA. Pueden manifestarse por diversos síntomas como síncope, hiperventilación, náuseas, vómitos, cambios en la frecuencia cardíaca y la presión arterial.
Paraestesias: Se sabe que la anestesia prolongada o la parestesia de la lengua y los labios son riesgos de procedimientos quirúrgicos como extracciones, aunque pueden ocurrir después procedimientos no quirúrgico. Muchas de estas reacciones son transitorias y desaparecen dentro de 8 semanas, aunque algunas reacciones pueden ser permanente. HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, octubre de 2002 y MALAMED, SF. Manual de anestesia local. 5a ed. Elsevier, 2005.
Store at room temperatura from 15°C to 30 °C and away from light.
Lot number, date of manufacture and expiration date: See packaging.
PROFESSIONAL USE
EVERY MEDICINE MUST BE KEPT OUT OF THE REACH OF CHILDREN
Solución estéril inyectable de clorhidrato de mepivacaína 3% (30 mg/ml) sin vasoconstrictor
Inyección parenteral, inyección intraosseosa, conjuntival e intracanal.
Cada cartucho contiene 10, 30, 50 o 100 ampollas de vidrio de 1,8 ml.
USO PEDIÁTRICO Y ADULTO
Cada ampolla de 1,8 ml contiene:
Clorhidrato de mepivacaína.......................54,0 mg
Excipientes: q.s.p........................................1,8 ml
Excipientes: Cloruro de sodio y agua para inyectable
INFORMACIÓN TÉCNICA PARA PROFESIONALES DE LA SALUD
Cada ampolla de 1,8 ml contiene:
Clorhidrato de mepivacaína.......................54,0 mg
Excipientes: q.s.p........................................1,8 ml
Excipientes: Cloruro de sodio y agua para inyectable
INFORMACIÓN TÉCNICA PARA PROFESIONALES DE LA SALUD
La eficacia del clorhidrato de mepivacaína es equivalente a la del clorhidrato de lidocaína. MALAMED, SF. Manual de Anestesia Local. 5o Ed. Elsevier, 2005.
Mepisv es indicado para el anestesia local en odontología. indicado para el producción de anestesia local para infiltración o bloqueo, para intervenciones dentales en general, extracciones múltiples, prótesis inmediatas y procedimientos endodoncia.
Los AL de tipo amida están contraindicados en pacientes con hipertermia maligna (hiperpirexia). La insuficiencia hepática es una contraindicación para la administración de anestésicos locales. Esto incluye a pacientes sometidos a diálisis renal y aquellos con nefritis crónica del túbulo intersticial. La insuficiencia hepática y cardiovascular significativa y la tirotoxicosis (hipertiroidismo) son contraindicaciones relacionadas con el uso de AL. La hipersensibilidad a los AL de tipo amida y a cualquier componente presente en la composición de Mepisv es una contraindicación absoluta. MALAMED, SF. Manual de anestesia local. 5a ed. Elsevier, 2005.
Coloque una ampolla en la jeringa-carpule. Perfore el área a anestesiar. Realice la aspiración antes de la inyección de la solución anestésica para minimizar la probabilidad de una inyección intravascular. Retire la jeringa, destruya la aguja y deseche la ampolla después de su uso, incluso si el contenido no se ha agotado.
Como para todos los AL, la dosis varía y depende de la región a anestesiar, vascularización tisular, tolerancia individual y técnica de anestesia. Debe administrarse la dosis más baja necesaria para producir una anestesia eficaz. La dosis máxima es de 4,4 mg/kg sin exceder 300 mg (equivalente a 5 ampollas para adultos sanos normales); la dosis debe reducirse en pacientes clínicamente comprometidos, debilitados o de edad avanzada. MALAMED, SF. Manual de anestesia local. 5to. Ed. Elsevier, 2005.
Dosis máximas en ampollas para pacientes sanos (4,4 mg de clorhidrato de mepivacaína / Kg – cada 1,8 ml de ampolla contiene 54 mg de clorhidrato de mepivacaína).
| Peso del paciente (en Kg) | 10 | 20 | 30 | 40 | 50 | 60 | 70 | 80 | Igual a o superior 90 |
| * No de Ampollas | 0,5 | 1.5 | 2,0 | 3,0 | 4,0 | 4,5 | 5,5 | 5,5 | 5,5 |
* número de ampolla – redondeado a media ampolla
Los carpules no deben esterilizarse en autoclave. Si el dentista desea realizar una asepsia externa de la ampolla se debe aplicar un tejido humedecido con alcohol isopropílico al 91% o alcohol etílico al 70% al diafragma de goma. Las ampollas no deben sumergirse en alcohol ni en ninguna otra solución desinfectante. Los dentistas que utilizan anestésicos locales en sus consultorios deben estar al tanto del diagnóstico y tratamiento de las emergencias que puedan surgir. Por lo tanto, debe haber equipo de reanimación, equipo de oxigenación y medicamentos de reanimación para uso inmediato. Se debe informar a los pacientes sobre la posibilidad de pérdida temporal de la sensibilidad y función muscular después de la inyección infiltrativa y bloqueante.
Se debe aconsejar a los pacientes que estén atentos mientras que las estructuras como la lengua, los labios, las membranas mucosas y el paladar se anestesian para evitar traumatismos en estas estructuras. La fuente de alimentación debe suspenderse hasta que se vuelva a iniciar la función normal estos estructuras. El vida útil de Mepisv és 36 meses. Ningún medicamento debe usarse después de su fecha de vencimiento. Recuerde que la presencia de precipitación, partículas en suspensión, turbidez y cambios en el color del producto hace que su uso sea inconveniente. El condiciones sistémica dela paciente debe ser previamente analizado antes de cualquier intervención dental el final de si evitar efectos adversos. Recuerda que la administración de cualquier solución anestésico local debe hacerse lentamente. MALAMED, SF. Manual de Anestesia Local. 5a ed. Elsevier 2005.
„Para evitar fugas de la solución durante la inyección, asegúrese de que la aguja esté penetrada en el centro del diafragma de goma mientras carga la jeringa. Una penetración fuera del centro produce una punción de forma ovalada que puede permitir fugas alrededor de la aguja. Otras causas de fugas y roturas incluyen jeringas desgastadas, jeringas sin aspiración, jeringas con arpón de caja y jeringas no disenadas para ampollas de 1,8 ml.“
Mujeres embarazadas y mujeres en la lactancia materna: Según Haas (2002) los AL utilizado en odontología se puede administrar a mujeres embarazadas (clorhidrato de mepivacaína está en la categoría C de la FDA). Sin embargo, la aspiración siempre debe hacerse antes de la inyección del anestésico para evitar la inyección intravascular. Se desconoce si el clorhidrato de mepivacaína se excreta en la leche materna.
Ninos: La principal preocupación con los pacientes pediátricos es la relativa facilidad de inducir una sobredosis. Por lo tanto, antes de la administración de AL al nino, el dentista debe determinar el peso del nino y calcular la dosis máxima. Es aconsejable seleccionar la solución que contenga la concentración más baja de AL.
Ancianos: Es prudente administrar una dosis de AL muy por debajo de la dosis máxima, ya que los pacientes de edad avanzada pueden tener alguna insuficiencia hepática y/o cardiovascular. HAAS, D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, octubre de 2002.
Interacciones con medicamentos: En general, depresores del SNC como narcóticos, opioides, ansiolíticos, fenotietiazinas, barbitúricos y antihistamínicos, cuando empleados en establecer con AL tomar para potenciación de acciones cardiorespiratoria de AL. El uso conjunto de AL y fármacos que comparten una vía metabólica común puede producir reacciones adversas. Los medicamentos que inducen la producción de enzimas microsomales hepáticas, como los barbitúricos, pueden alterar la tasa de metabolismo de AL ligada a la amida. Por lo tanto, aumentar la inducción de enzimas hepáticas microsomales aumentará la tasa de metabolismo de AL. HAAS D. An update on Local Anesthetics in Dentistry. Journal of the Canadian Dental Association, v. 68 No. 9, octubre de 2002 y MALAMED, SF. Manual de anestesia local. 5a ed. Elsevier 2005.
Interacciones de examen: La inyección intramuscular de clorhidrato de mepivacaína puede provocar un aumento en los niveles de creatina fosfoquinasa. Por tanto, la determinación de esta enzima como el diagnóstico de la presencia de infarto agudo de miocardio, sin la separación de la isoenzima, puede comprometer el resultado de este examen. POLOCAÍNA® DENTAL Prescribing information Dentsply Pharmaceutical, PM- CS-PI-0003 Rev.10/01.
Almacenar a temperatura ambiente entre 15°C y 30°C. Proteger de la luz.
Número de lote, fecha de fabricación y fecha de vencimiento: Ver embalaje.
USO PROFESIONAL
TODOS LOS MEDICAMENTOS DEBEN MANTENERSE FUERA DEL ALCANCE DE LOS
NINOS
MS: 1.0177.0030
Farmacéutico Responsable :
Renata Caroline Magalhães – CRF-RJ 21674
Estrada do Guerenguá, 2059 – Río de Janeiro – RJ, Brasil
Código postal: 22713–002
CNPJ: 33.112.665/0001–46
Industria brasilena
SAC: 0800 602 68 80 – Fax: 55–21–3342–4009
–