Articaine, Epinephrine
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Clinical Pharmacology
Pharmacodynamics
The drug Tsertacain, used for local infiltration and conduction
anesthesia in dentistry, is a combination drug, in which
includes articaine (amide-type local anesthetic) and adrenaline
(epinephrine) (vasoconstrictor). Epinephrine is added to the drug
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for prolonging the action of anesthesia. Articaine has a local anesthetic
action due to blockade of potential-dependent sodium channels in the cell membrane
neurons, which leads to reversible inhibition of the conduction of impulses along the nervous
fiber and reversible loss of sensitivity.
The drug Tsertacain has a rapid effect (latency period - from 1 to 3 minutes).
The duration of anesthesia is 40 mg / ml for dosage + 0.005 mg / ml - not
less than 45 minutes, for dosages of 40 mg / ml + 0.01 mg / ml - not less than 75 minutes. Due to low
the content of epinephrine in the drug its effect on the cardiovascular system
slightly: there is almost no increase in blood pressure and
heart rate.
Children
Published studies have shown that children aged 3.5 to 16 years
the use of the drug in a dose of 5 mg / kg body weight provided sufficient
local anesthetic action during mandibular infiltration
or maxillary conduction anesthesia. The duration of anesthesia was
comparable in all age groups and depended on the amount of the drug administered.
Pharmacokinetics
Articaine is rapidly and almost immediately after administration is metabolized (by
hydrolysis) by non-specific plasma esterases in tissues and blood (90%);
the remaining 10% of the dose of articaine is metabolized by microsomal enzymes
the liver. The main metabolite of articaine formed is articaic acid -
does not have local anesthetic activity and systemic toxicity, which
allows for repeated administration of the drug.
Blood articaine concentrations in the alveolar region of the tooth after submucosal administration in
hundreds of times the concentration of articaine in the systemic circulation. Binding
Articaine with plasma proteins is approximately 95%.
Articaine is excreted through the kidneys, mainly in the form of articaic acid. After
submucosal administration, the half-life is approximately 25 minutes.
Articaine penetrates the placental barrier, practically does not stand out with the thoracic
milk
Indications
Indicated for local anesthesia (infiltration and conduction anesthesia) in
dentistry.
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For dosage of 40 mg / ml + 0.005 mg / ml: with planned interventions, such as
uncomplicated removal of one or more teeth, treatment of carious cavities and
grinding teeth before prosthetics.
Composition
1 ml of the preparation contains:
Active ingredients: 40 mg / ml + 0.005 mg / ml
Articaine hydrochloride 40.0 mg
Adrenaline tartrate
in terms of adrenaline (epinephrine) 0.005
Excipients:
Sodium Chloride 1.23 mg
Hydrochloric acid solution 5 M
or sodium hydroxide solution 3 M to pH 2.7 - 5.2
Water for injection to 1.0 ml
Articaine, Epinephrine is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Certacaine | injection | ||
Ultracaine DS | Sanofi-aventis | France | ampoules |
Ultracaine DS Forte (Sanofi-aventis | Sanofi-aventis | France | cartridge |
Ultracaine DS (Sanofi-aventis | Sanofi-aventis | France | cartridge |
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Dosage and Administration
The drug is intended for use in the oral cavity and can be administered only in
tissues where there is no inflammation.
Injection into inflamed tissue is not allowed.
The drug can not be administered intravenously.
In order to avoid accidental ingestion of the drug in the blood vessels, before
its introduction should always be carried out aspiration test (in two stages).
Major systemic reactions that may develop as a result of random
intravascular administration of the drug can be avoided by following the injection technique:
after the aspiration test, 0.1-0.2 ml of the drug is slowly injected, then, not
earlier than 20-30 seconds, slowly inject the rest of the dose. Pressure
injections should match the sensitivity of the tissue.
For anesthesia with uncomplicated removal of the teeth of the upper jaw in the absence of
inflammation is usually sufficient to create a depot of the drug in the area of the transition fold
by introducing it into the submucosa from the vestibular side (1.7 ml of the drug per
tooth). In rare cases, complete anesthesia may be required.
additional administration from 1 ml to 1.7 ml. In most cases, this allows not
carry out painful palatal injections. When deleting several near
placed teeth, it is usually possible to limit the number of injections.
For anesthesia with cuts and suturing in the palate to create the palatine
A depot requires about 0.1 ml of the drug per injection.
In the case of removal of premolars of the lower jaw, in the absence of inflammation,
do without mandibular anesthesia, as is usually sufficient
infiltration anesthesia provided by the injection of 1.7 ml per tooth. If so
by not achieving the desired effect, additional
injection of 1-1.7 ml of anesthetic into the submucosa in the region of the transitional fold of the lower
jaws from the vestibular side. If in this case it was not possible to achieve complete
anesthesia, it is necessary to conduct a conductive blockade of the mandibular nerve.
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When processing cavities and grinding teeth under the crowns, with the exception of the lower
molars, depending on the volume and duration of treatment is shown
the introduction of the drug Certacainum 40 mg / ml + 0.005 mg / ml in the transition fold region with
vestibular side in a dose of 0.5-1.7 ml per tooth.
During surgery, the drug Certacainum 40 mg / ml + 0.01 mg / ml in
Depending on the severity and duration of the intervention is dosed individually.
When performing a single medical procedure, adults can enter Articaine in a dose up to
7 mg per 1 kg of body weight. Patients were well tolerated in doses up to 500 mg.
(corresponds to 12.5 ml of solution for injection).
For pediatric patients (over 4 years old), minimal doses should be applied,
necessary to achieve adequate anesthesia, the dose of the drug Certacain
is selected depending on the age and body weight of the child, but the dose of articaine is not
should exceed 7 mg per 1 kg of body weight (0.175 ml / kg). Use of the drug in children
younger than 1 year has not been studied.
For elderly patients and all patients with severe renal and hepatic
insufficiency may create elevated plasma concentrations
Articaine. For these patients, the minimum dose required for
achieve sufficient depth of anesthesia
Adverse reactions
The frequency of side effects is presented in accordance with the classification,
recommended by the World Health Organization:
very often (≥ 1/10);
often (≥ 1/100, <1/10);
infrequently (≥ 1/1000, <1/100);
rarely (≥ 1/10000, <1/1000);
very rarely (<1/10000), including individual messages;
frequency is unknown (according to the available data, determine the frequency of occurrence
seems possible).
Nervous system disorders
Often: paresthesia, hypesthesia; headache mainly due to
composition of the drug epinephrine.
Infrequently: dizziness.
Frequency unknown: dose-dependent reactions from the central nervous system:
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agitation, nervousness, stupor, sometimes progressive to loss of consciousness, coma,
respiratory disorders, sometimes progressing to respiratory arrest, muscular
tremor, muscle twitching, sometimes progressive to generalized
seizures.
Sometimes in violation of the correct injection technique with the introduction
damage to local anesthetics in dental practice
facial nerve, which can lead to the development of facial paralysis.
Violations by the organ of vision
Frequency unknown: visual impairment (blurred vision,
mydriasis, blindness, double vision), usually reversible and occurring during or
shortly after injection of a local anesthetic.
Disorders of the gastrointestinal tract
Often: nausea, vomiting.
Violations of the heart and blood vessels
Infrequently: tachycardia, disturbance of a heart rhythm, increase in arterial pressure.
Frequency unknown: lower blood pressure, bradycardia, cardiac
failure and shock.
Immune system disorders
Frequency unknown: allergic reactions (swelling and inflammation at the injection site),
hyperemia of the skin, itching, conjunctivitis, rhinitis, angioedema (edema
upper and / or lower lips, cheeks, vocal cords swelling with a "lump in the throat",
difficulty swallowing, hives, difficulty breathing). Any of these manifestations
may progress to anaphylactic shock.
General disorders and disorders at the site of administration
Frequency unknown: occasional intravascular injection may result
zones of ischemia at the injection site, up to tissue necrosis.
Hypersensitivity to articaine or other local anesthetic
amide-type agents, epinephrine, sulfites (in particular, in patients suffering from
bronchial asthma with increased sensitivity to sulfites, as possible
acute allergic reactions with symptoms of anaphylactic shock, such as
bronchospasm), or to any other of the auxiliary components of the drug.
Contraindications due to the presence in the composition of the drug Articaine
- severe sinus dysfunction or severe conduction disorders
(for example, severe bradycardia, atrioventricular block II or III degree);
- acute decompensated heart failure;
- severe arterial hypotension.
Contraindications due to the presence in the composition of the drug epinephrine
- angle-closure glaucoma;
- hyperfunction of the thyroid gland;
- paroxysmal tachycardia, tachyarrhythmia;
- recent myocardial infarction (up to 6 months);
- recently transferred coronary artery bypass surgery (up to 3 months);
- taking non-selective beta-blockers, for example, propranolol (risk
hypertensive crisis and severe bradycardia);
- pheochromocytoma;
- severe form of arterial hypertension.
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Carefully
- in patients with chronic heart failure, coronary artery disease
heart, angina, atherosclerosis, myocardial infarction in history, impaired
heart rhythm, hypertension;
- in patients with cerebrovascular disorders, history of stroke;
- in patients with chronic bronchitis, emphysema;
- in patients with diabetes mellitus (potential risk of changes in concentration
blood glucose);
- in patients with cholinesterase deficiency (use is possible only in the case of
absolutely necessary, since it is possible prolongation and a pronounced increase
drug action);
- in patients with bleeding disorders;
- in patients with severe violations of the liver and kidneys;
- in patients with marked arousal;
- in patients with epilepsy in history;
- when combined with halogen-containing agents when conducting
inhalation anesthesia
Drug interactions
Simultaneous use is contraindicated
With simultaneous use with non-cardio selective beta-blockers,
for example, propanolol, may develop hypertonic crisis and severe
bradycardia.
Simultaneous use is possible with caution.
The action of vasoconstrictors that increase blood pressure, for example,
epinephrine may be enhanced by tricyclic antidepressants or
monoamine oxidase inhibitors.
Local anesthetics enhance the effect of drugs
depressing the central nervous system. Narcotic analgesics increase
action of local anesthetics, however, increase the risk of respiratory depression.
When using the drug Tsertacain in patients taking heparin or
acetylsalicylic acid, may develop bleeding at the injection site.
With simultaneous use with cholinesterase inhibitors may slow down
metabolism of local anesthetics, resulting in possible
prolongation and pronounced enhancement of the action of Articaine.
Epinephrine can inhibit insulin release from pancreatic beta cells
glands and reduce the effects of hypoglycemic agents for oral administration.
Some means of inhalation anesthesia, such as halothane, may increase
myocardial sensitivity to catecholamines and increase the risk of developing disorders
heart rate after injection of the drug Certacain.
When processing the injection site of a local anesthetic with disinfectant solutions,
containing heavy metals, increases the risk of local reactions - edema,
soreness
Special instructions
Regional and local anesthesia should be performed by experienced professionals in
an appropriately equipped room with the availability of ready to
immediate use of equipment and preparations necessary for
monitoring of cardiac activity and resuscitation. Staff,
performing anesthesia must be qualified and trained
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performing anesthesia, must be familiar with the diagnosis and treatment of systemic
toxic reactions, adverse events, reactions and other complications.
To prevent infection (including the hepatitis virus)
make sure that new solutions are always used when taking the solution from the ampoules
sterile syringes and needles.
In order to avoid the development of adverse reactions, it is necessary to apply minimal
effective doses of the drug and before the introduction of the drug to conduct a two-step
aspiration test (see the section "Route of Administration and Doses").
When using the drug may inadvertently injuring the lips, cheeks,
mucous membrane and tongue, especially in children, due to reduced sensitivity.
The patient should be warned that food is possible only after
termination of local anesthesia and recovery of sensitivity.
The drug is intended for use in dentistry. Use for anesthesia
distal extremities is unacceptable due to the risk of ischemia due to
epinephrine content.
Impact on the ability to drive vehicles and mechanisms
The possibility of admission of the patient to the management of vehicles and mechanisms
determined by a doctor.
Overdosage
Symptoms
The most common symptoms are cardiovascular reactions.
system and nervous system, nausea, motor restlessness, clouding of consciousness
during injection, respiratory disorders, muscle twitching, convulsions, shock.
Treatment
Symptomatic treatment. When first signs of overdose appear or
side effects such as nausea, motor restlessness, turbidity
consciousness during the injection, it should be interrupted, the patient transferred to the horizontal
position, clear airway, monitor heart rate and blood pressure.
It is recommended, even if the symptoms do not seem too severe, to ensure
intravenous access. For respiratory disorders, depending on the severity, give
oxygen, in some cases, conduct artificial respiration. Central
analeptics are contraindicated. Muscle twitching or generalized cramps
removed by intravenous injection of short or ultrashort barbiturates
actions. Falling blood pressure, tachycardia or bradycardia often
are eliminated when the patient is placed in a horizontal position. With severe
circulatory disorders and shock of any genesis after stopping the injection
emergency measures are shown: ensuring the airway (oxygen
insufflation), intravenous fluids (electrolyte solution),
glucocorticosteroids. Additionally, you can enter plasma substitutes, albumin.
With a threatening circulatory disorder and increasing bradycardia, it is administered from
0.25 ml to 1 ml epinephrine. An intravenous injection of epinephrine should be made.
slowly under the control of heart rate and blood pressure.
A single dose of intravenous injection of epinephrine should not exceed 0.1 mg, in
Further, if necessary, epinephrine can be administered dropwise (rate of infusion
through dropper is adjusted depending on the pulse rate and blood pressure).
Severe forms of tachycardia and tachyarrhythmias can be eliminated by using
antiarrhythmic drugs, but do not use non-selective beta
adrenergic blockers. Oxygen supply and blood circulation control are needed in
anyway. With an increase in blood pressure in patients suffering
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hypertension, should, if necessary, apply peripheral
vasodilators
- Brand name: Certacain
- Active ingredient: Articaine, Epinephrine
- Dosage form: Injection
- Manufacturer: Graminexx
Studies and clinical trials of Articaine, Epinephrine (Click to expand)
- Comparative investigations on the efficacy of articaine 4% (epinephrine 1:200,000) and articaine 2% (epinephrine 1:200,000) in local infiltration anaesthesia in dentistry—a randomised double-blind study
- Comparison of ropivacaine and articaine with epinephrine for infiltration anaesthesia in dentistry – a randomized study
- Clinical use of an epinephrine-reduced (1/400,000) articaine solution in short-time dental routine treatments—a multicenter study
- Epinephrine Concentration (1:100,000 or 1:200,000) Does Not Affect the Clinical Efficacy of 4% Articaine for Lower Third Molar Removal: A Double-Blind, Randomized, Crossover Study
- Articaine/epinephrine formulations
- Articaine and epinephrine for lower third molar extraction
- A comparison of anaesthetic area, pain on injection and adverse effect of lidocaine, mepivacaine and articaine with epinephrine for upper premolar extraction
- Comparison of 4% Articaine with 1:100,000 Epinephrine and 2% Lidocaine with 1:100,000 Epinephrine When Used as a Supplemental Anesthetic
- Anesthetic Efficacy of 4% Articaine with 1:100,000 Epinephrine versus 4% Articaine with 1:200,000 Epinephrine as a Primary Buccal Infiltration in the Mandibular First Molar
- Anesthetic Efficacy of 1.8 mL versus 3.6 mL of 4% Articaine with 1:100,000 Epinephrine as a Primary Buccal Infiltration of the Mandibular First Molar
- A Comparison of the Efficacy of 4% Articaine with 1:100,000 Epinephrine and 2% Lidocaine with 1:80,000 Epinephrine in Achieving Pulpal Anesthesia in Maxillary Teeth with Irreversible Pulpitis
- A comparison of the clinical anesthetic efficacy of 4% articaine and 0.5% bupivacaine (both with 1:200,000 epinephrine) for lower third molar removal
- Comparison of 4% articaine with epinephrine (1:100,000) and without epinephrine in inferior alveolar block for tooth extraction: double-blind randomized clinical trial of anesthetic efficacy
- Epinephrine-reduced articaine solution (1:400,000) in paediatric dentistry: a multicentre non-interventional clinical trial
- Efficacy and safety of intraseptal and periodontal ligament anesthesia achieved by computer-controlled articaine + epinephrine delivery: a dose-finding study
- Hemostatic and Anesthetic Efficacy of 4% Articaine HCl With 1:200,000 Epinephrine and 4% Articaine HCl With 1:100,000 Epinephrine When Administered Intraorally for Periodontal Surgery
- Articaine/epinephrine
- Articaine/epinephrine
- Clinical study of hemodynamic changes comparing 4% articaine hydrochloride with 1:100,000 and 1:200,000 epinephrine
- Articaine (4%) with epinephrine (1:100,000 or 1:200,000) in intraosseous injections in symptomatic irreversible pulpitis of mandibular molars: anesthetic efficacy and cardiovascular effects
- Preliminary Comparison of Missed Blocks with 4% Articaine and 2% Lidocaine both with 1:100,000 epinephrine on Inferior Alveolar Nerve Block Injections
- Articaine/epinephrine
- Articaine/epinephrine
- Articaine/epinephrine