Buy Certacaine injection 40 mg/ml + 0.005 mg/ml 2 ml ampoules 10 pcs
  • Buy Certacaine injection 40 mg/ml + 0.005 mg/ml 2 ml ampoules 10 pcs

Articaine, Epinephrine

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Clinical Pharmacology


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


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.


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.


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



Indicated for local anesthesia (infiltration and conduction anesthesia) in



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.


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


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 nameManufacturerCountryDosage 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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Articaine, Epinephrine

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.


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:


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


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.



- 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


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,


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


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.



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.


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


hypertension, should, if necessary, apply peripheral


  • Brand name: Certacain
  • Active ingredient: Articaine, Epinephrine
  • Dosage form: Injection
  • Manufacturer: Graminexx

Studies and clinical trials of Articaine, Epinephrine (Click to expand)

  1. 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
  2. Comparison of ropivacaine and articaine with epinephrine for infiltration anaesthesia in dentistry – a randomized study
  3. Clinical use of an epinephrine-reduced (1/400,000) articaine solution in short-time dental routine treatments—a multicenter study
  4. 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
  5. Articaine/epinephrine formulations
  6. Articaine and epinephrine for lower third molar extraction
  7. A comparison of anaesthetic area, pain on injection and adverse effect of lidocaine, mepivacaine and articaine with epinephrine for upper premolar extraction
  8. Comparison of 4% Articaine with 1:100,000 Epinephrine and 2% Lidocaine with 1:100,000 Epinephrine When Used as a Supplemental Anesthetic
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. Epinephrine-reduced articaine solution (1:400,000) in paediatric dentistry: a multicentre non-interventional clinical trial
  15. Efficacy and safety of intraseptal and periodontal ligament anesthesia achieved by computer-controlled articaine + epinephrine delivery: a dose-finding study
  16. 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
  17. Articaine/epinephrine
  18. Articaine/epinephrine
  19. Clinical study of hemodynamic changes comparing 4% articaine hydrochloride with 1:100,000 and 1:200,000 epinephrine
  20. 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
  21. Preliminary Comparison of Missed Blocks with 4% Articaine and 2% Lidocaine both with 1:100,000 epinephrine on Inferior Alveolar Nerve Block Injections
  22. Articaine/epinephrine
  23. Articaine/epinephrine
  24. Articaine/epinephrine

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