Articaine: Clinical Aspects and Dosage Calculation
In modern oral surgery, articaine-based drugs occupy a leading position. They are used for both infiltration and conduction anesthesia. An important clinical advantage is high hemodynamic stability: when performing infiltration anesthesia using a 4% articaine solution combined with adrenaline (at a dilution of 1:100,000), hemodynamic changes are unlikely.
To achieve stable and complete anesthesia, the standard dosage of the 4% solution (with adrenaline 1:200,000 or 1:100,000) ranges from 0.5 to 1.8 ml. If the clinical situation requires an enhanced effect, an additional administration of 1.0–1.8 ml is permitted. However, it is strictly not recommended to reduce the working solution concentration to 2–3%, as this directly leads to a decrease in the efficacy of the local anesthetic.
The maximum allowable doses of the drug are strictly regulated:
- For adult patients, the limit is 7 mg/kg of body weight.
- For children, the maximum dosage is reduced to 5 mg/kg.
Clinical recommendation: to ensure maximum patient safety in practice, no more than half (1/2) of the calculated maximum allowable dose should be used.
Prevention of Complications in Local Anesthesia
A key step in the safe administration of local anesthesia (especially during conduction anesthesia) is the aspiration test. It must be performed without fail before administering the main volume or the entire dose of the drug.
The main goal of this maneuver is to eliminate the risk of accidental intravascular administration of the solution. Direct entry of the anesthetic with a vasoconstrictor into the bloodstream can provoke an acute cardiovascular reaction: a significant increase in blood pressure (BP) and an uncontrolled increase in heart rate (pulse).
Lidocaine: Pharmacological Profile
The drug Lidocainum (chemical name: 2-diethylamino-2',6'-acetoxylidide hydrochloride) belongs to the amide group of local anesthetics and is an acetanilide derivative. In clinical practice, it is widely known under many synonyms: xicaine, xylocaine, luan, lidestin, solcaine, octocaine, baicaine, dentacaine, xylodont, xylestesin, xylonest, lignocaine, lignospan.
Lidocaine is indicated for all types of local anesthesia used in oral surgery.
Historically, lidocaine is often compared to novocaine. Compared to the latter, the amide anesthetic demonstrates a number of indisputable advantages:
- Significantly superior in anesthetic potency.
- Superior in overall duration of action.
- Substantially less frequently causes allergic reactions in patients.
Systemic Effects and Drug Interactions of Lidocaine
In addition to its primary function—nerve impulse blockade—lidocaine has a pronounced systemic effect on the body. The drug exerts a noticeable sedative effect and also affects the cardiac conduction system.
Due to its ability to suppress ectopic pacing sites in the myocardium, it possesses a powerful antiarrhythmic effect and is successfully used in medicine as an antiarrhythmic agent.
Regarding drug interactions, an important aspect is that lidocaine is fully compatible with sulfonamides, allowing them to be safely prescribed to patients in the postoperative period.
Briefly: answers to topical questions
What anesthetics are used for surface (topical) anesthesia in the oral cavity?
For surface (topical) anesthesia in the oral cavity, specialized and universal local anesthetics are used.
- Cocaine — used exclusively for surface anesthesia.
- Tetracaine — a water-soluble agent included in combination drugs (e.g., Aroma-paste).
- Benzocaine — the base for water-insoluble agents.
- Bumecaine — used exclusively for surface anesthesia.
- Pramocaine — used exclusively for surface anesthesia.
- Pyromecaine — a water-soluble agent with a high risk of rapid absorption.
- Lidocaine (Lidocainum) — used as a 10% solution (no more than 2 ml) or as part of EMLA cream.
- Trimecaine (Trimecainum) — used as a 3–5% ointment.
Combination drugs are also used, such as Aroma-paste (ethylaminobenzoate, dibucaine hydrochloride, tetracaine hydrochloride, homosulfamine).
What is the mechanism of action of local anesthetics at the cellular level?
The mechanism of action of local anesthetics at the cellular level consists of blocking voltage-gated sodium channels. As weak bases, the drugs penetrate the nerve fiber cell membrane in their non-ionized form via simple diffusion. Inside the axon, they become ionized and block sodium channels from the inner surface, binding preferentially to channels in the inactivated state. This leads to a decrease in the permeability of cell membranes to sodium and potassium ions. As a result, the influx of sodium ions is blocked, which prevents cell membrane depolarization, as well as the generation and conduction of action potentials (pain impulses).
What are the absolute contraindications to the use of articaine with adrenaline?
Absolute contraindications to the use of articaine with adrenaline (epinephrine) include the following conditions and diseases:
- Hypersensitivity — intolerance to articaine or preservatives (sulfites) included in the finished drug formulation.
- Glaucoma — specifically, the angle-closure form of the disease.
- Severe cardiac rhythm disturbances — including paroxysmal tachycardia and tachyarrhythmia.
Intravenous administration of this drug is also strictly prohibited.
Which drug groups interact with lidocaine?
Lidocaine (Lidocainum) interacts with the following drug groups:
- Sulfonamides — lidocaine is fully compatible with them. During metabolism, it does not form para-aminobenzoic acid (PABA), and therefore does not reduce the antimicrobial activity of sulfonamide drugs.
- Immunosuppressants (cyclosporine, tacrolimus, sirolimus) — when administered intravenously, lidocaine acts as an inhibitor of cytochrome P450 (CYP3A4) enzymes and P-glycoprotein. This leads to an increased concentration of immunosuppressants in the blood, which requires mandatory monitoring and adjustment of immunosuppressive therapy.
What is the technique for performing infiltration anesthesia in the maxilla?
The technique for performing infiltration anesthesia in the maxilla involves injecting the local anesthetic solution into the submucosal layer above the periosteum.
- Injection site — the transitional fold of the oral vestibule. The needle is inserted slightly superior to the projection of the root apices of the target tooth.
- Administration features — due to the porous structure of the maxillary bone, the solution easily diffuses, so there is no need to attempt subperiosteal needle insertion.
- Exceptions — during anesthesia of the first maxillary molar (zygomaticoalveolar crest region), the solution is injected near the apex of the second premolar and behind the zygomaticoalveolar crest.
Class and exam questions
What is the maximum dose of articaine for a child?
The maximum permissible dose of articaine for children is 5 mg/kg of body weight; however, clinical guidelines recommend using no more than half of this dose.
What is the main clinical advantage of lidocaine over novocaine?
Lidocaine is superior to novocaine in anesthetic potency and duration of action, and significantly less frequently causes allergic reactions.
Is it possible to dilute a 4% articaine solution to reduce toxicity?
Reducing the solution concentration to 2–3% is not recommended, as this directly leads to a decrease in the clinical effect of the local anesthetic.
What else to study on this topic
- Technique for Performing the Aspiration Test
- Conduction Anesthesia: Indications and Drug Application Features
- The Influence of Vasoconstrictor Concentration (1:100,000 and 1:200,000) on the Properties of Articaine
- Amide Local Anesthetics: Chemical Structure Features
- Mechanism of the Antiarrhythmic Action of Lidocaine
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