Dosis máximas: 4,4 mg de clorhidrato de mepivacaína/kg
(Cada Carpule de 1,8 ml contiene 36 mg de clorhidrato de
mepivacaína y 0,018 mg de epinefrina)
Peso
(Kg)
10
20
30
40
50
60
70
80
90
100
N 0 Carpules MEPIADRE
1
2
3,5
4,5
6
7
8
8
8
8
Las dosis indicadas representan lo máximo sugerido para
individuos sanos, normales; para pacientes debilitados o ancianos,
deben ser menores.
7.Advertencias
La seguridad y la eficacia de los anestésicos locales dependen de la
dosificación recomendada, de la técnica correcta, de una anamnesia
previa, de las precauciones adecuadas y de la rapidez y habilidad del
profesional para intervenir en los casos de emergencia. Se debe usar la
menor dosis que permita obtener una anestesia eficaz. La
administración de dosis frecuentes de mepivacaína puede causar un
acentuado aumento en los niveles plasmáticos debido a la absorción
sistémica, al aumento de la cantidad del fármaco y sus metabolitos o a
la lenta degradación metabólica. La tolerancia puede variar de
acuerdo con el estado del paciente, ya que a pacientes debilitados, de
edad avanzada, que padecen de enfermedades graves o a niños se les
deben suministrar dosis reducidas, calculadas de acuerdo con la edad
y las condiciones físicas. Se recomienda tomar cuidados especiales en
el caso de administración frecuente a pacientes con graves trastornos
hepáticos o renales, ya que su metabolismo está afectado. También se
debe prestar atención especial al administrar anestésicos locales a
pacientes con antecedentes de sensibilidad o alergia a los
componentes de la fórmula. Pueden ocurrir serias arritmias cardíacas
si se utilizan preparaciones que contienen vasoconstrictores en
pacientes durante o después de la administración de halotano,
tricloroetileno, ciclopropano o cloroformo. Existe un pequeño riesgo
de que los vasoconstrictores causen isquemia o necrosis local en
pacientes con enfermedades vasculares periféricas. Se debe tener en
cuenta que el metabisulfito de potasio está presente en la fórmula,
sustancia que puede causar reacciones alérgicas, incluyendo síntomas
anafilácticos y que presentan riesgos fatales o episodios menos graves
de asma en algunos individuos susceptibles. Esta sensibilidad al
sulfito se observa con mayor frecuencia en individuos asmáticos que
en no asmáticos. Antes del procedimiento se le debe advertir al
paciente sobre la posibilidad de pérdida transitoria de la sensibilidad y
de la función muscular después de las infiltraciones y bloqueos
nerviosos. En pediatría o en pacientes con algún disturbio mental se
debe advertir a los responsables de la observación del paciente a fin
de evitar traumas labiales.
8. Uso en ancianos, niños y otros grupos de riesgo.
En pacientes ancianos, cuyas funciones metabólicas, renales y
hepáticas generalmente se encuentran debilitadas, se debe tener el
cuidado de administrar la menor dosis necesaria y suficiente para
proporcionar una anestesia específica y eficaz. En pacientes con
disfunción hepática y/o disfunción renal y en pacientes asmáticos,
MEPIADRE se debe administrar con cautela. Los pacientes con
hipertensión arterial, enfermedades coronarias o cardiovasculares
(principalmente si están relacionados con una secuela de fiebre
reumática aguda) deben evitar el uso de anestésicos que contienen
vasoconstrictores, como MEPIADRE . En pacientes con enfermedad
vascular periférica existe un pequeño riesgo de isquemia o necrosis
local causada por los vasoconstrictores. Todavía no se cuenta con
estudios adecuados y bien controlados en mujeres embarazadas y
además, los estudios sobre reproducción en animales no siempre
consiguen predecir la respuesta en humanos. Todavía no se dispone
de datos sobre la posible excreción de la mepivacaína a través de la
leche humana y, como muchos fármacos se excretan por esa vía, se
recomienda cuidado especial cuando se administra MEPIADRE a
mujeres lactantes. El uso en niños menores de 10 años debe obedecer
las recomendaciones del ítem Posología descrito anteriormente. Aún
no se han determinado los datos de seguridad y eficacia
correspondientes a los pacientes pediátricos menores de 3 años, por
tal motivo se recomienda que no se les administre el producto.
9. Interacciones medicamentosas
Segundo estudios de P. Henry e J. Van der Driesche, del Laboratorio
de Farmacología del Centro Hospitalario de la Universidad de
Rennes, el uso de anestésicos locales asociado al 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. MEPIADRE no se debe
usar en pacientes que hagan uso de medicamentos que 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.
COMPOSITION:
Each mL of the injectable solution of MEPIADRE contains:
Mepivacaine Hydrochloride ... ................................. 20.0 mg
Epinephrine ...............................................................10.0 µg
Excipients e.f .......................................................... ...1.0 mL
Excipients: Sodium Chloride, Potassium Metabisulfite, EDTA
Disodium Salt and Water for Injection.
Content: 50 cartridges.
10.Acciones adversas a medicamentos
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; 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. La somnolencia después de la administración de mepivacaína
normalmente es la primera señal de que existe un alto nivel del
fármaco en la sangre; puede ser consecuencia de la rápida absorción.
Los tratamientos de auxilio para estas manifestaciones deben estar a
la mano del profesional para el caso de que sea necesario actuar
rápidamente. Se debe disponer para uso inmediato de equipos de
reanimación, oxígeno u otras drogas para este tipo de emergencia.
Prácticamente no se conocen casos de 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.
11. Sobredosis
Las reacciones generalizadas del SNC o las reacciones
cardiovasculares generalmente están relacionadas con altos niveles
plasmáticos por causa de una inyección intravascular accidental o
sobredosis. (Ver Advertencias y Acciones Adversas ). Las primeras
señales y síntomas de la intoxicación por mepivacaína pueden incluir
somnolencia, que puede causar 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 un masaje cardíaco externo.
- El tratamiento de auxilio de la deficiencia circulatoria puede
necesitar la administración de líquidos por vía intravenosa (suero).
12.Almacenamiento
El producto se debe conservar en su embalaje original al abrigo
de la
0
luz. Se debe evitar el calor excesivo (temperatura superior a 40 C).
El plazo de validez del producto es de 24 meses, contados a partir de la
fecha de fabricación.
VENTA BAJO PRESCRIPCIÓN MÉDICA
PRODUCTO DE USO EXCLUSIVAMENTE PROFESIONAL
MEPIADRE
mepivacaine hydrochloride + epinephrine
English
Pharmaceutical form - Injectable solution
Presentation - Box containing 5 blisters with 10 cartridges
of 1.8 mLeach
Exclusively for parenterally use by means of nerve blockade or
infiltration injection
FORADULTAND/OR PEDIATRIC USE
THE USE BY CHILDREN UNDER 3 YEARS OLD IS NOT
RECOMENDED. CHECK THE DOSAGE TABLE IN
POSOLOGY.
ASK YOUR PATIENT TO INFORM ABOUT THE
OCCURRENCE OF ANY UNDESIRABLE REACTION
AFTER THE USE OF MEPIADRE.
ASK YOUR PATIENT ABOUT OTHER DRUGS THAT HE
MIGHT BE USING.
MEPIADRE SHOULD ONLY BE USED IN PREGNANT
WOMEN AND IN NURSING MOTHERS WITH THE
GUIDANCE OF THE HEALTH CARE PROFESSIONAL IN
CHARGE.
KEEP THE PRODUCT IN ITS ORIGINAL PACKAGE .
PROTECT FROM LIGHT. AVOID EXCESSIVE
HEAT
0
(TEMPERATURES ABOVE 40 C ).
DO NOT USE THIS PRODUCT IF SHELF-LIFE HAD
EXPIRED. BEFORE USE, OBSERVE THE PRODUCT´S
ASPECT.
PARTIALLY USED CARTRIDGES SHOULD NOT BE
REUSED.
EVERY DRUG SHOULD BE KEPT OUT OF THE REACH
OF CHILDREN.
TECHNICAL INFORMATION FOR
THE HEALTH CARE PROFESSIONALS
1. Pharmacological characteristics
Mepivacaine Hydrochloride
Classification: Amide
Chemical Formula:
1-methyl-2´,6´-pipecoloxilidide
Hydrochloride.
Potency: 2 (procaine = 1; lidocaine = 2).
Toxicity: 1.5 to 2 (procaine = 1; lidocaine = 2).
Absorption: The absorption of mepivacaine is complete following
parenteral administration, its rate of absorption depending upon
various factors, such as the site of injection and the presence or
absence of a vasoconstrictor agent.
Action Mechanism: Mepivacaine hydrochloride stabilizes the
neuronal membrane by inhibiting the ionic flow that is necessary to
the start and conduction of the impulses, causing a local anesthetic
effect.
Metabolism: Mepivacaine, because of its amide structure, is not
detoxified by the circulating plasma esterases. The liver is the
principal site of metabolism, which occurs through the action of
microsomal fixed-function oxidases, with over 50 per cent of the
administered dose being excreted into the bile as metabolites.
Hydroxylation and N-demethylation play important roles in the
metabolism of mepivacaine.
Excretion: Mepivacaine hydrochloride is excre ted via the kidneys,
with approximately 1 to 16% of anesthetic dose excreted unchanged.
Most of the anaesthetic and its metabolites are eliminated within 30
hours.
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
alpha and beta-adrenergic receptors, where beta 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.
2. Efficacy Results
Clinical trials have been evaluated and testified the capacity of the
anesthetics to block the conduction in the axons of the peripheral
nervous system (Friedman PM 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/Covino BG: Clinical
Pharmacology of local anesthetic agents . In Cousins MJ,
Bridenbaugh PO, editors
: Neural blockade in clinical anesthesia and
nd
management of pain , 2 ed, Philadelphia, 1988, JB Lippincott) and its
efficacy in provide anesthesia when associated to several
vasoconstrictor (Jacob, W.: Local anaesthesia and vasoconstrictive
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. Indications
The use of MEPIADRE is indicated for local anesthesia by nerve
blockade or infiltration, for general procedures, multiple extractions,
immediate prosthesis and endodontic procedures. MEPIADRE
onset of action is rapid (30 to 2 minutes in the upper jaw and 1 to 4
minutes in the lower jaw). Pulpal anesthesia of aproximately 60
minutes´ duration and soft tissue anesthesia of 3 to 5 hours are to be
expected. Epinephrine is included with the anaesthetic in order to
achieve a deeper and more prolonged anesthesia, by localizing the
solution at the site of the injection and intensifying and prolonging the
anaesthetic effect and decreasing the rate at which the anaesthetic
drug enters the systemic circulation. The presence of a
vasoconstrictor also decreases surgical hemorrhage in the immediate
area of injection.
4. Contraindications
MEPIADRE 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. Caution should be exercised
when MEPIADRE is used in pregnant or nursing mothers or in
asthmatic patients (See Warnings ).
5.Administration and storage conditions after opening cartridge
This product is intended exclusively for professional use. The
recommended specific techniques and procedures of local anesthesia
in the oral cavity should be used. MEPIADRE should be kept in its
original package, protected from light and excessive heat
(temperatures above 40°C). Partially used cartridges should not be
reused. 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 intravascular injection. If blood is aspirated, the
needle must be repositioned until no return of blood can be elicited by
aspiration. Note, however, that the absence of blood in the syringe
does not assure that intravascular injection will be avoided and a
double aspiration is always recommended. Local anaesthetic
procedures should be used with caution when there is inflammation
and/or sepsis in the region of the proposed injection. MEPIADRE
should not be injected repeatedly at the same site because reduced
blood flow and increased oxygen consumption in the affected tissues
may cause tissue anoxia, delay healing, edema or necrosis at the
injection site.
6. Dosage
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 dose recommended by Stanley
F. Malamed in his
th
book “Manual of Local Anesthesia, 5 edition”, is 4.4 mg/kg,
without exceeding 300 mg (the equivalent to 8 cartridges of
MEPIADRE), for adults or children.
The maximum dose recommended for children with less than 10
years, with normal lean body mass and normal body development,
should be determined by the application of one of the standard
pediatric drug formulas (e.g., Clark's rule).
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 (2 cartridges of MEPIADRE ) per
appointment.
For routine work, 1 cartridge of MEPIADRE is usually enough.
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 mepivacaine hydrochloride/kg
(Each 1.8 mL cartridge contains 36 mg of
mepivacaine hydrochloride + 0.018 mg of epinephrine)
Weight
(Kg)
10
20
30
40
50
60
70
80
90
100
Number of Cartridges
of MEPIADRE
1
2
3.5
4.5
6
7
8
8
8
8
Doses indicated are the maximum suggested for normal healthy
individuals: they should be decreased for debilitated or elderly
patients.
7. Warnings
The safety and efficacy of local anesthetics depend on the
recommended dosage, the correct technique, on a previously done
anamnesis, on the adequate precautions and on the quickness and skill
of the Professional in the intervention of emergency cases. The low est
dose that results in effective anesthesia should be used. The frequent
administration of the product may cause a rise in the plasmatic levels
due to the slow metabolic degradation. The tolerance may vary
according to the patient's state, children since weakened patients,
with advanced age and serious disease patients must have reduced
dosages administered, according to their age and physical conditions.
Special care is recommended for frequent administration in patients
with liver or kidney disturbances, since the metabolism in these
patients will be compromised. Special attention should be taken in the
administration of local anesthetics to patients with a history of
sensitivity or allergy to the components of the formula. Serious
cardiac arrhythmia may occur if preparations containing
vasoconstrictors are used in patients during or after the administration
of halotane, trichloroethylene, cyclopropane or chloroform. In
patients with peripheral vascular disease, there is a little potential risk
that vasoconstrictors cause ischemic injury or local necrosis. The
presence of Sodium Metabisulfite in the formula must be taken into
account when treating patients who are susceptible to asthma. This
sensitivity to sulfite is more commonly observed in asthmatic
individuals rather than in non-asthmatics. The patient must be
previously informed of the possibility of temporary loss of sensitivity
and muscle function, after infiltrations and nerve blocks. 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.
8. Use in elderly, children and other risk groups
In elderly patients, in whom the metabolic, renal and hepatic
functions are usually decreased, 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 MEPIADRE in patients with liver or kidney problems and in
patients susceptible to asthma. Patients with hypertension, coronary
or cardiovascular problems (particularly related to sequela of acute
rheumatic fever), must avoid the use of anesthetics containing
vasoconstrictors as MEPIADRE . In patients with peripheral
vascular disease, there is a little potential risk that vasoconstrictors
cause ischemic injury or local necrosis. There are no adequate and
well-controlled studies in pregnant women and animal reproduction
studies are not always predictive of human response. It is not known
whether mepivacaine is excreted in human milk and, because many
drugs are excreted this way, caution should be exercised when
MEPIADRE is administered to nursing mothers.
The use in children under 10 years old should follow the
recommendations described previously in Dosage. Safety and
effectiveness in pediatric patients below 4 years have not been
established, therefore the use of this drug in these patients is not
recommended.
9. 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. MEPIADRE 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.
10.Adverse reactions
Side effects following MEPIADRE 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 intravascular 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.
Drowsiness following the administration of mepivacaine is usually
an early sign of a high blood level of the drug and may occur as a
consequence of rapid absorption. 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.
11. 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
Ad verse Reactions ). The first signs and symptoms of mepivacaine
intoxication can include sleepiness, which can lead to the loss of
conscience and respiratory arrest. In these cases the following
procedures must be performed:
- Place the patient in supine position. Elevate the legs 30° to 45° above
the horizontal.
- The airway must be assured. If ventilation is inadequate, ventilate
the patient with oxygen, if possible.
- If the pulse is low (< 40) or non determinable, begin external heart
massage.
- Support treatment for circulatory impairment can request the
administration of parenteral solutions (serum).
12. Storage conditions
This product should be kept in its original package
and protected from
0
light. Excessive heat (temperatures above 40 C ) must be avoided.
The expiry date of this product is equivalent to 24 months after
manufacturing date.
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: 33112665/0001-46
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:
o
Evaldo Rodrigues de Oliveira CRF - RJ N 2897
o
ANVISA/MS N : 101770022
Número do lote, data de fabricação e prazo de validade:
Vide cartucho.
Número do lote, fecha de fabricación y validez (mes/año):
Ver el cartucho.
Lot #, manufacturing date and expire date: See product box.
Rev. 04