Pharmacodynamics and pharmacokinetics
Articaine is a thiophene and has a local anesthetic effect. Used for conduction and infiltration anesthesia . Articaine undergoes hydrolysis in a slightly alkaline environment of tissues with the release of a base that has lipophilic properties, and therefore easily penetrates through the cell membrane into the nerve fiber.
By influencing receptors, it blocks the delivery of sodium ions into the cell and the conduction of impulses along nerve fibers. The effect of the drug is observed immediately after its administration and lasts from 1 to 3 hours. Efficiency is reduced in acidic environments.
When administered intramuscularly, Cmax is achieved within 20 to 40 minutes.
When introduced under the mucous membrane of the oral cavity, it exhibits high diffusion ability.
95% bound to plasma proteins.
Metabolized in the liver, T½ is approximately 60 – 80 minutes.
Within 6 hours, 54 - 63% is excreted by the kidneys.
Can penetrate the placental barrier (to a lesser extent than other local anesthetics); it penetrates the blood-brain barrier in small quantities. It is practically not excreted in breast milk.
Articaine during pregnancy in dentistry
Articaine is usually well tolerated at all stages of pregnancy. There is no data on the long-term effects of the drug on the neurophysiology of the newborn. Also, no teratogenic damage was observed after use of the drug in the first trimester.
There are no data from clinical studies of the penetration of Articaine into breast milk. To minimize possible risk to the baby, breastfeeding mothers may choose to express milk for approximately 4 hours after the injection. After which breastfeeding can be resumed.
Contraindications
- children under 4 years of age;
- increased sensitivity to local anesthetics of the amide group;
- paroxysmal tachycardia;
- B12 deficiency anemia (megaloblastic);
- angle-closure glaucoma;
- atrial fibrillation;
- bronchial asthma;
- chronic hypoxia.
Prescribe with caution:
- for pathologies of the central nervous system;
- with pseudocholinesterase deficiency;
- with pernicious anemia;
- with hypoxia.
Side effects
Peripheral and central nervous system:
- headache;
- dyspnea;
- visual impairment;
- apnea;
- muscle twitching;
- tremor;
- convulsions;
- diplopia;
- disturbance of consciousness.
The cardiovascular system:
- bradycardia;
- tachycardia;
- decrease in blood pressure.
Digestive system:
- nausea;
- diarrhea;
- vomit.
Allergic manifestations:
- itching;
- skin rash;
- angioedema;
- very rarely - anaphylactic shock.
Instructions for use of Articaine (Method and dosage)
The instructions for Articaine in dentistry suggest an individual dosage regimen, depending on the severity of the procedure, the time of its implementation and the patient’s tolerability of the drug.
The maximum single dose of the drug is 6 mg per kilogram of body weight.
To carry out surgical intervention, which requires more time than Articaine can provide, a combination drug is used - Articaine Inibsa Epinephrine as active ingredients . Epinephrine exhibits a vasoconstrictor effect at the site of drug administration, thereby increasing its absorption time, prolonging its effect.
Instructions for use of the drug Articaine Epinephrine in dentistry recommend the following doses of the drug.
During the procedure for removing teeth of the upper jaw without complications and inflammation - 1.7 ml of the drug per tooth, if ineffective, another 1 ml - 1.7 ml.
For a palatal incision or suture - 0.1 ml.
When grinding teeth to install crowns or prepare cavities, a vestibular injection is given in a dose of 0.5 ml - 1.7 ml for each tooth.
During the procedure for removing premolars of the lower jaw without complications, infiltration anesthesia , which acts as a conduction anesthesia.
The maximum dose in dentistry for adult patients is 7 mg per kilogram of weight. For pediatric patients over 4 years of age - 5 mg per kilogram of body weight.
What is Articaine and what is its composition?
Articaine is an amide anesthetic intended for local, infiltrative or conductive anesthesia for both simple and complex dental procedures. A local anesthetic blocks the generation and conduction of nerve impulses, presumably by increasing the threshold of electrical excitation in the nerve, slowing the propagation of the nerve impulse, and decreasing the rate of rise of the action potential.
The uniqueness of Articaine as a member of the amide family is that it contains an ester group and a thiophene instead of a benzene ring. The thiophene ring increases the lipid solubility of articaine, facilitating more efficient diffusion of the anesthetic across the lipid membrane of nerve cells into surrounding tissues. Articaine is widely used in dentistry due to its safety during short procedures that require rapid onset of anesthesia.
The onset of action of the drug Articaine is:
- from 1.5 to 1.8 min. with infiltration of the upper jaw;
- from 1.5 to 3.6 min. with block anesthesia of the lower jaw.
Articaine pulp anesthesia lasts from 30 to 120 minutes. Anesthesia of soft tissues with the drug lasts ~ 2.25 hours for infiltration of the upper jaw, 4 hours for blockade of the lower jaw.
The drug is produced in the form of an injection solution - a transparent, colorless or yellowish liquid. For retail sale to pharmacy chains, Articaine is supplied in ampoules made of colorless chemically pure glass, enclosed in blister packs and/or cardboard packs.
Composition of articaine in dentistry:
- active agent - articaine hydrochloride;
- Excipients: sodium chloride (to make the solution isotonic) and distilled water.
1 ml of solution contains 40 mg of active agent.
In odonto-dental anesthesia, articaine is used alone or in combination with epinephrine (adrenaline). Epinephrine, diluted to 1:100,000 or 1:200,000 and added to the solution, slows down the passage of articaine into the general bloodstream and thus ensures long-term maintenance of the concentration of the active substance in the tissues, allowing a small hemorrhagic surgical field to be obtained.
It is possible to replace Articaine with synonyms with the same active substance, such as:
- Artikain-Binergy;
- Ultracaine;
- Artikain-DF;
- Articaine with Epinephrine.
The decision to use analogues is made by the attending physician, taking into account the individual characteristics of the patient.
Overdose
, dizziness, loss of consciousness, motor agitation, decreased blood pressure, bradycardia, and tachycardia occur
If the first symptoms of an overdose are detected during the drug administration procedure, it is necessary to interrupt the injection, place the patient in a horizontal position, monitor the airway, and monitor blood pressure and heart rate.
In case of apnea and shortness of breath , oxygen is indicated, if necessary, endotracheal intubation and artificial ventilation.
For convulsions, slow intravenous administration of short-acting barbiturates with parallel inhalation of oxygen is recommended, under hemodynamic control.
In case of serious circulatory disorders and shock , an intravenous infusion of plasma substitutes and electrolytes , glucocorticoids and albumin are administered.
With increasing bradycardia and vascular collapse, an intravenous injection of Epinephrine (0.1 mg) is prescribed with slow administration. If necessary, continue to administer Epinephrine as an infusion under the control of blood pressure and heart rate.
Indications
In commonly used concentrations, the drug in question does not have surface anesthetic activity, but when administered by injection, its effect is superior to other drugs of the same group (Lidocaine, Mepivacaine). Therefore, the main indication for the use of Articaine is local anesthesia of a conduction or infiltrative type.
Articaine with adrenaline is used for pain relief during traumatic dental procedures in the form of the following types of local anesthesia:
- infiltration (impregnation of tissues of the surgical field);
- conduction (introduction of a substance along the nerve);
- intraligamentary (intraligamentous);
- intraseptal (intraseptal - the substance is injected into the septum of the bone between the sockets of the teeth);
- intrapulpal (injection of anesthetic into the dental pulp).
It is also used for:
- uncomplicated removal of one or more teeth;
- preparation of carious cavities and teeth before prosthetics.
Articaine in combination with epinephrine has found use in the following concentrations:
- 1:200000;
- 1:100000.
The use of a local anesthetic with a higher content of adrenaline (1:100,000) significantly increases the risk of adverse reactions in patients with periodontal tissue pathology, as well as during injection into the palate.
Interaction
Local anesthetics enhance the effects of drugs that depress the central nervous system.
When Articaine is administered to patients receiving Acetylsalicylic acid or Heparin , the risk of local bleeding increases.
Narcotic analgesics potentiate the effect of local anesthetics and can lead to respiratory depression.
When used in combination with muscle relaxants , their effect may be prolonged and enhanced.
When prescribed together with antimyasthenic drugs, Articaine exhibits antagonism in relation to the effect on the skeletal muscles, especially when using high doses (correction of myasthenia gravis ).
Cholinesterase inhibitors may slow down the metabolism of Articaine.
Vasoconstrictors increase and enhance the effect of Articaine.
Articaine in pediatric dentistry
The pharmacodynamics of local anesthetics in children is comparable to that in adults. In pediatric dental practice, extreme caution must be exercised when using amide local anesthetics as lower intrinsic clearance or decreased serum protein binding may easily lead to an increased risk of toxic reactions. The route of administration is one of the main safety factors when using local anesthetics in neonates and children.
Anesthesia in dentistry with the drug Articaine , carried out using intraosseous injection, is effective in achieving deep anesthesia of teeth affected by MIG with hypersensitivity associated with chronic inflammation of the pulp in children.
In pediatric dentistry, it is recommended to use Articaine 2% due to the lower Cmax and shorter half-life of the drug.
special instructions
In case of chronic hypoxia, pseudocholinesterase deficiency, central nervous system diseases, vegetative-vascular dystonia, pernicious anemia, Articaine can be used only according to strict indications and with extreme caution.
The drug can be prescribed in combination with glucose and Epinephrine.
When used in dentistry, it is recommended to eat only after complete restoration of sensitivity.
Analogs
Level 4 ATX code matches:
Markain
Scandonest
Emla
Naropin
Versatis
Lidocaine
Ubistezin
Ultracaine D-S Forte
Ultracaine D-S
Ultracaine
- Lidocaine;
- Ultracaine;
- Bupivacaine;
- Marcain;
- Mepivacaine , etc.
Reviews about Articaine
In dentistry, provided that the dentist and the patient comply with all recommendations and contraindications for use, the drug Articaine is highly effective and has no side effects.
Before use, the patient must immediately inform the doctor about all chronic and acute diseases occurring at the current time or observed in the past. In turn, the doctor must do an allergy test to avoid severe adverse reactions.
General information, release form
Articaine was first synthesized in 1969, and its widespread use began in 1976. Nowadays, medications based on Articaine are produced by many pharmaceutical companies.
Basic requirements for local anesthetics:
- significant depth of penetration of the product;
- long duration of action;
- high degree of security.
These parameters are influenced by:
- activity of the anesthetic used;
- peripheral vascular tone.
The drug Articaine does not contain a special preservative - paraben, which most often causes hypersensitivity reactions. Contains a minimal amount of the antioxidant adrenaline (metabisulfite).
The stability of the local anesthetic is achieved through high quality glass, rubber components of the carpule, and high activity of the active substance.
It is insoluble in aqueous media, so it is used in the form of a salt, which is water soluble. For the main effects to manifest, its destruction in tissues is required with the formation of fat-soluble substances that are able to penetrate the lipid membrane of the nerve ending. It undergoes changes in tissue structures quite quickly, so the analgesic effect is noted within 1-2 minutes.
Articaine has a slight ability to expand the lumen of blood vessels, so it is advisable to use it with epinephrine (adrenaline). It quickly penetrates into soft tissues, as well as into bone structures, which ensures a rapid onset of effect, as a result of which it is widely used in therapeutic, surgical, and orthopedic interventions in dentistry.
Available in the form of cartridges and solutions for injection in ampoules. Packed in cardboard boxes.
