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SUMMARY OF PRODUCT CHARACTERISTICS
1
NAME OF THE MEDICINAL PRODUCT
Scandonest 30 mg/ml, solution for injection
2
QUALITATIVE AND QUANTITATIVE COMPOSITION
1 ml solution for injection contains 30 mg mepivacaine hydrochloride.
Excipients with known effect: 6 mg/ml of sodium chloride, sodium hydroxide (for pH-adjustment).
For the full list of excipients, see section 6.1.
3
PHARMACEUTICAL FORM
Solution for injection.
Clear and colourless solution.
4
CLINICAL PARTICULARS
4.1
Therapeutic indications
Local anaesthesia (infiltration and nerve-block anaesthesia) in dentistry during minor procedures.
4.2
Posology and method of administration
Posology
The smallest volume of solution which will lead to an effective anaesthesia should be used. The
dosage should be tailored to the age, weight and general condition of the individual patient.
The recommended doses as well as the maximum doses not to be exceeded for adults and children are
gathered in the following table:
ADULTS
CHILDREN
20 kg child
40 kg child
Recommended
therapeutic
dose
in cartridge of 1.8 ml
1 cartridge
~¼ cartridge
~½ cartridge
in mg of mepivacaine
hydrochloride
54 mg
15 mg
30 mg
Maximum
recommended
dosage
in cartridge of 1.8 ml
5.5 cartridges
~1cartridge
~2cartridges
in mg of mepivacaine
hydrochloride
300 mg
60 mg
120 mg
The dose should be minimised for patients with liver and kidney disease. See section 5.2.
Paediatric population
Children from 4 years of age (ca.20kg body weight) and older (see section 4.3.)
Recommended therapeutic dose:
The quantity to be injected should be administrated by the age and weight of the child and the
magnitude of the operation. The average dosage is 0,75mg/kg=0.025ml of mepivacaine solution per
kg body weight.
Maximum recommended dosage:
Do not exceed the equivalent of 3 mg mepivacaine/kg (0,1ml mepivacaine/kg) of body weight.
Method of administration
Local injection (block or infiltration).
For use in dental anaesthesia only.
To avoid intravascular injection, aspiration control at least in two planes (rotation of the needle by
180°) must always be carefully undertaken, although a negative aspiration result does not safely rule
out an unintentional and unnoticed intravascular injection.
The injection rate should not exceed 1 ml per minute.
Major systemic reactions as a result of accidental intravascular injection can be avoided in most cases
by an injection technique – after aspiration slow injection of 0.1-0.2 ml and slow application of the
rest – not earlier than 30 seconds to 1 minute after.
4.3
-
Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1
Hypersensitivity to local anaesthetics of the amide type.
Patients with severe disorders of atrioventicular conduction not compensated by pace maker
Epilepsy not controlled by any treatment
Intermittent acute porphyria.
Children below 4 years of age (ca.20kg body weight).
4.4
Special warnings and precautions for use
Warnings
The patient should be made aware of the fact that the anaesthesia can increase the risk of damage to
lips, tongue, and to the mucous membrane or soft palate. Intake of food should be avoided until the
anaesthesia has worn off.
Injection of local anaesthetics must be avoided in infected areas.
Athletes should be warned that this medicinal product contains an active substance likely to induce a
positive reaction to tests undertaken in anti doping controls.
This product contains less than 1 mmol sodium (23 mg) per cartridge, i.e. it is considered as
essentially “sodium free‟.
Precautions for use
Dental local anaesthetics contain high concentrations of active substance. This means that rapid
injection under high pressure can lead to complications even after administration of small volumes
(see section 4.9). The risk is especially high in the event of inadvertent intravascular injection, since
the injected drug may transfer in a retrograde manner. Intra-arterial injection in the head and neck
region results in higher concentrations of the drug reaching the brain than in the case of intravenous
injection. Careful aspiration prior to injection is recommended to reduce the risk of intravascular
injection.
In the case of intraneural injection, there is a risk that, owing to the high pressure, the drug may
transfer in a retrograde manner along the nerve. In order to avoid intraneural injection, and to prevent
nerve damage in connection with nerve blocks, the needle should always be withdrawn slightly if
paraesthesia occurs during injection.
Care should be taken in patients with second- or third-degree AV heart block, since local anaesthetics
can depress myocardial conduction. Special vigilance is also required in the elderly and in patients
with severe or untreated hypertension, severe heart disease, severe anaemia, severe liver disease,
severely impaired renal function, circulatory insufficiency or whose general condition is impaired.
Mepivacaine use requires:
Consultation to assess medical history and ongoing concomitant medications
To perform a test injection of 5 to 10% of the dose in case of allergic risk
To perform the injection slowly with careful repetitive aspiration to avoid inadvertent
intravascular injection
To talk to the patient
To have at disposal the appropriate resuscitating equipment (in particular a source of oxygen) as
well as anti-convulsant medicines (benzodiazepines or barbiturates) myorelaxants, atropine
and vasopressors or adrenaline for a severe allergic or anaphylactic reaction
Monitoring should be increased in patients with blood coagulation disorders or under anticoagulants
(monitoring of the INR).
4.5
Interaction with other medicinal products and other forms of interaction
Care must be exercised when co-administering mepivacaine with drugs that are similar in structure to
local anaesthetics (i.e. class IB antiarrhythmic drugs), since the toxic effects are additive.
Long or permanent treatment with antiarrhythmic drugs, psychopharmaceuticals, or anticonvulsant
drugs, and alcohol consumption, could reduce sensitivity to anaesthetics. Increase the anaesthetic dose
should be enough or just wait longer for the effect, before the intervention.
Special dosage attention should be taken, with a simultaneous use of CNS depressors, which could
cause additive effects.
Local anaesthetics might release heavy metal ions from some type of disinfectant solutions. Before
the anaesthetic administration, special measures should be taken when these types of disinfectants are
used. These released ions could cause local irritation, swelling and oedema.
Heparin, nonsteroidal anti-inflammatory drugs or plasma substitutes (dextrane) administration could
increase bleeding tendency after local anaesthetic injection.
4.6
Pregnancy and lactation
Pregnancy
Data on a limited number of exposed pregnancies indicate no adverse effects of mepivacaine on
pregnancy or on the health of the foetus/ new-born child. To date, no other relevant epidemiological
data are available. The potential risk for humans is unknown.
Breastfeeding
Mepivacaine is excreted in breast milk. However, at therapeutic doses of Scandonest no effects on the
suckling child are anticipated. Scandonest can be used during breast- feeding.
4.7
Effects on ability to drive and use machines
Scandonest has minor influence on the ability to drive and use machines.
4.8
Undesirable effects
Adverse effects, strictly attributed to the local anaesthetic, occur in less than 1/1000 patients treated
with local anaesthetics. However, physiological effects from nerve block are common, but these vary
markedly depending on what type of block is administered. The effects of relative overdose (e.g. in
connection with inadvertent intravascular injection) or absolute overdose can be serious and must be
taken into consideration (see also section 4.9).
Rare
(<1/1000)
Nervous system disorders.: Unconsciousness and seizures (in the event of absolute or
relative overdose)
Neurological effects (e.g. sensation of numbness, residual paraesthesia and other
sensory disturbances) have been observed. It has not been established for certain to
what extent these symptoms are dependent on technical factors (e.g. intraneural
injection) or on the anaesthetic.
Cardiac disorders: Myocardial depression and cardiac arrest (in patients with
absolute or relative overdose).
Immune system disorders: Allergic reactions (rash; erythema; pruritus; oedema of
tongue, mouth, lips, or throat; urticaria, angiooedema) and, in the most serious cases,
anaphylactic shock. Methaemoglobinemia.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It
allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare
professionals are asked to report any suspected adverse reactions via the national reporting system
listed in
[To be completed nationally]
4.9
Overdose
Toxicity:
Undesirable toxic effects may appear with 5-6 mg/l or higher plasma levels, and convulsions could
appear with 10 mg/l or higher. These excessive plasma levels could be caused by accidental
intravascular injection or due to abnormal patient’s condition.
Limited experience of overdose. Intravenous administration of 300 mg to an 8-year old (approx. 25
kg) gave rise to seizures.
Symptoms:
Relative overdose occurs if a local anaesthetic is inadvertently injected intravascularly (for example if
a small artery in the upper half of the body is accidentally punctured and the compound reaches the
brain via injection in a retrograde direction). CNS symptoms will occur in such a case, possibly
accompanied by seizures, even after a dose that would otherwise not be regarded as toxic. Absolute
overdose is characterised principally by the occurrence of central-nervous-system and cardiovascular
adverse effects.
CNS toxicity occurs gradually, with symptoms and reactions of progressively increasing severity.
Initially, symptoms include agitation, a feeling of intoxication, a sensation of numbness in the lips and
tongue, paraesthesias around the mouth, dizziness, vision and hearing disturbances, and buzzing in the
ears. If these effects are observed while the injection is in progress, they are a warning signal and the
injection should be stopped immediately. Articulatory difficulties, muscle stiffness and twitching are
more serious symptoms and precede generalised seizures. These symptoms must not be misinterpreted
as neurotic behaviour. Unconsciousness and grand mal seizures may follow and persist for a few
seconds up to several minutes. Oxygen deficit and hypercapnia occur rapidly during the seizures
owing to increased muscle activity and insufficient ventilation. Respiratory arrest may even occur in
severe cases. Acidosis exacerbates the toxic effects of local anaesthetics.
Recovery is dependent on metabolism of the local anaesthetic and distribution away from the central
nervous system. This occurs rapidly providing very large amounts of the drug are not injected.
In general, cardiovascular effects imply a more serious situation. A fall in blood pressure,
bradycardia, arrhythmia and cardiac arrest can occur as a result of high systemic concentrations of
local anaesthetics. These effects are usually preceded by signs of CNS toxicity unless the patient has
received general anaesthesia or is heavily sedated with such compounds as benzodiazepines or
barbiturates. It should be noted, however, that central blocks themselves often give rise to a
sympathetic block, resulting in a fall in blood pressure and, possibly, bradycardia.
Treatment:
If signs of acute systemic toxicity appear, administration of local anaesthetics should be stopped
immediately. Treatment must aim to quickly stop the seizures and also to maintain good oxygenation
and circulation. Oxygen is always given, together with controlled ventilation (if required). Diazepam
is given in the event of seizures. Patients with asystole are given cardiac massage. It is also important
that acidosis should be treated, if present.
5
PHARMACOLOGICAL PROPERTIES
5.1
Pharmacodynamic properties
Pharmacotherapeutic group: Nervous System / Local Anaesthetics / Anaesthetics, local / Amides
Local
ATC code: N01BB03
Scandonest contains mepivacaine, which is an amide local anaesthetic. Mepivacaine reversibly blocks
nerve impulses owing to its effects on ionic transport across the cell membrane. Mepivacaine has a
rapid onset, high frequency of anesthesia and low toxicity. When peripheral nerve block is performed,
mepivacaine’s effect occurs within 2-4 minutes. The duration of effect is determined by the degree of
vascularity and diffusion to the blood vessels.
Scandonest produces rapid anaesthesia which lasts 20-30 minutes when administered by infiltration
and 1-2 hours in the case of conduction anaesthesia. Owing to the lack of vasoconstriction, it is
possible to keep the pH of the solution close to neutral.
5.2
Pharmacokinetic properties
The absorption of local anaesthetics is dependent on physico-chemical properties (e.g. lipid
solubility), pharmacological properties (e.g. the vasodilating effect) and also on the vascularity of the
injection site.
The bioavailability is 100% at the action site.
The maximum plasma level of mepivacaine is achieved approximately after 30- 60 minutes.
The plasma protein binding of mepivacaine is 60-78% (principally with alpha-glycoprotein acid).
Mepivacaine distribution covers all body tissues. Liver, lungs, heart and brain achieves maximum
mepivacaine levels. Mepivacaine cross placental barrier by simple diffusion. Relation maternal: fetal
plasma levels is 0.4-0.8.
The plasma half-life is 2-3 hours for adults and 9 hours for newborns. Clearance of amides is
dependent on hepatic blood flow. The plasma half-life is prolonged if the patient is suffering from
liver disease and/or uraemia.
Metabolism principally occurs through oxidation in the liver. The metabolites are principally
eliminated via the bile and 99% are glucuronidated. The metabolites are then reabsorbed and
eliminated via the urine. The pH of the urine influences the elimination of the metabolites.
In adults, only 3–5% of the mepivacaine is eliminated in an unchanged form and in newborns, approx.
40%.
5.3
Preclinical safety data
Studies performed in animals showed that mepivacaine was well tolerated.
Mutagenicity studies showed that mepivacaine is devoid of mutagenic effect in a reverse mutation
assay in bacteria (Ames test) and in the micronucleus test in mouse.
As for any other amide type local anaesthetic, the active substance, in high doses, may induce toxic
reactions on the central nervous and the cardiovascular systems (see section 4.8. Undesirable effects).
6
PHARMACEUTICAL PARTICULARS
6.1
List of excipients
Sodium chloride,
Sodium hydroxide (for pH-adjustment),
Water for injections.
6.2
Incompatibilities
In the absence of compatibility studies, this medicinal product must not be mixed with other
medicinal products.
6.3
Shelf life
3 years.
6.4
Special precautions for storage
Do not store above 25°C.
6.5
Nature and contents of container
Glass cartridges of 1.8 ml, sealed with rubber stoppers.
Pack size:
50 x 1.8 ml
6.6
Special precautions for disposal and other handling
The cartridges are intended for single use.
Any unused medicinal product or waste material should be disposed of in accordance with local
requirements.
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MARKETING AUTHORISATION HOLDER
[To be completed nationally]
8
MARKETING AUTHORISATION NUMBER
[To be completed nationally]
9
DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
1999-11-19/ 2009-11-19
10
DATE OF REVISION OF THE TEXT
2015-02-18