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Articaine powder is an ester based amide local anesthetic with a white crystalline powder appearance. Its hydrochloride form is soluble in water (≥ 5mg/mL) and dimethyl sulfoxide (DMSO). Its powder form is stored at 2-8 ℃ for 2 years and -20 ℃ for 3 years; The solvent form can be stored at -20 ℃ for 6 months and -80 ℃ for 1 year. Articaine exerts local anesthetic effects by reversibly binding to the alpha subunit of voltage-gated sodium channels in the neural lumen, blocking the transmission of nerve impulses. It is mainly used for tooth extraction, pulp treatment, and oral surgery such as vital pulp porcelain for upper and lower posterior teeth. It is also used in combination with adrenaline (1:100000 or 1:200000) to enhance anesthesia and reduce bleeding. It can also be used as a tool medicine to study the function and pain mechanism of voltage-gated sodium channels. Explore its protective role in models of acute kidney injury, such as by inhibiting NF - κ B activation and NLRP3 inflammasome pathway.
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| Chemical Formula | C13H20N2O3S |
| Exact Mass | 284.12 |
| Molecular Weight | 284.37 |
| m/z | 284.12 (100.0%), 285.12 (14.1%), 286.12 (4.5%) |
| Elemental Analysis | C, 54.91; H, 7.09; N, 9.85; O, 16.88; S, 11.27 |
The core use of articaine powder is as a local anesthetic, widely used in dentistry, oral surgery, and some minor surgeries. It reversibly blocks voltage-gated sodium channels on the nerve cell membrane, inhibits the transmission of nerve impulses, and thus produces local anesthetic effects.
The 'Golden Choice' for Dental Anesthesia
In the field of dentistry, atecamin has become the preferred anesthetic due to its unique pharmacological properties:Quick onset: Anesthesia can be produced within 1-3 minutes after injection, significantly reducing patient waiting time. For example, in maxillary posterior tooth extraction surgery, after submucosal infiltration injection of 80mg of 4% articaine, the peak blood concentration can be reached within 10-15 minutes, and the onset time of anesthesia is much faster than traditional local anesthetics.Strong anesthesia: Its anesthetic effect is 1.5-2 times that of lidocaine, especially suitable for complex dental surgeries such as impacted tooth extraction and root canal treatment.
Clinical data shows that the success rate of articaine in electronic pulp testing is 64.5%, significantly higher than other local anesthetics.Precise scope of action: Through submucosal infiltration anesthesia, tooth extraction and pulp treatment of upper and lower posterior teeth can be completed, reducing the need for anesthesia of deep tissues and lowering the risk of systemic adverse reactions. For example, during maxillary sinus elevation surgery, the local concentration of articaine can reach 100 times that of systemic circulation, ensuring sufficient anesthesia in the surgical area.Low allergy risk: As an amide local anesthetic, the incidence of allergic reactions to articaine is lower than that of ester local anesthetics (such as procaine), making it suitable for patients with allergies.
Auxiliary anesthesia for short surgery
In addition to dentistry, articaine can also be used for the following short surgeries:
Skin biopsy: Using local infiltration anesthesia to reduce patient pain and improve biopsy accuracy.
Superficial tumor resection: such as lipoma and fibroid resection, its short-term characteristics (anesthesia duration of about 20-40 minutes) can avoid long-term numbness after surgery.Plastic micro surgery, such as double eyelid surgery and injection cosmetic surgery, has strong tissue permeability and can accurately anesthetize the surgical area.
Pharmacological mechanism: Sodium channel blockade and multi pathway effects
The anesthetic effect of articaine powder stems from its precise regulation of nerve conduction
Anti inflammatory and renal protective effects (non anesthetic use)
In recent years, studies have found that atecamin can alleviate lipopolysaccharide (LPS) - induced acute kidney injury by inhibiting the NF - κ B signaling pathway and NLRP3 inflammasome activation. In animal experiments, pretreatment with articaine can significantly reduce the levels of renal tubular injury markers (such as serum creatinine and urea nitrogen) and decrease inflammatory cell infiltration. This effect may be related to its ester structure, but it has not yet been applied in clinical anti-inflammatory treatment.
Sodium channel blockade
The aromatic ring and lipophilic groups in the articaine molecule grant it strong liposolubility, allowing it to easily cross nerve cell membranes. It then binds to the alpha subunit of voltage-gated sodium channels and blocks sodium ion influx, thereby suppressing the generation and transmission of nerve action potentials. While its working mechanism resembles that of lidocaine, the unique thiobenzene ring structure of articaine boosts its binding affinity to sodium channels, leading to a faster onset and more powerful anesthetic effect.
Clinical application scenarios and advantages
Combined application with adrenaline
Articaine is often used in combination with adrenaline (1:100000 or 1:200000) to prolong anesthesia time and reduce bleeding:
Extended duration of action: Adrenaline constricts blood vessels, slowing down the absorption of articaine and extending its anesthesia duration from 20 minutes to 60-90 minutes.
Reduce systemic absorption: lower peak blood drug concentration, reduce the risk of adverse reactions such as dizziness and palpitations. For example, after adding adrenaline to 4% articaine, the incidence of lip numbness in patients decreased from 98% to 75%, and there were no reports of serious adverse reactions.
Medication for special populations
Pediatric patients: The safety of articaine in children has been validated. A study on children aged 4-13 showed that the VAS score (Visual Analog Scale) for simple surgeries (such as deciduous tooth extraction) was 0.5, and for complex surgeries (such as multiple tooth extraction) it was 1.1, both lower than the lidocaine group.Elderly patients: The metabolites of articaine (such as articainic acid) are mainly excreted through the kidneys. Reduced renal function in the elderly may prolong its half-life, but clinical studies have not found significant accumulation effects and it can still be safely used.
Typical applications in dental surgery
Maxillary posterior tooth extraction: The extraction of maxillary molars can be completed through buccal submucosal infiltration anesthesia, avoiding hematoma or nerve damage that may occur with traditional block anesthesia.Root canal therapy: The potent anesthesia of articaine ensures that patients experience no pain throughout the entire treatment process, especially in cases of pulp necrosis or acute pulpitis.Active pulp porcelain restoration: During the tooth preparation stage, atecamine can provide up to 40 minutes of anesthesia time to meet clinical operational needs.
Usage and precautions
Dose and concentration selection
Common dose for adults
A single injection should not exceed 7mg/kg, and the maximum recommended dose of 4% articaine is 500mg (13.9ml).
Children's dose
Adjusted according to body weight, usually 2-4mg/kg, with a maximum single dose not exceeding 3mg/kg.
Concentration selection
4% articaine (containing adrenaline) is suitable for most dental surgeries; 2% articaine is used for patients with hypertension or cardiovascular disease.
Key points of injection technology
Immersion anesthesia
Using the "fan-shaped injection method", the needle is inserted into the submucosa and injected.
Block anesthesia
If anesthesia is required for the inferior alveolar nerve, accurate positioning of the mandibular foramen is necessary.
Injection speed
Slowly inject (about 1ml per minute) to reduce patient pain and tissue damage risk.
Adverse reactions and contraindications
Common adverse reactions
Local reactions: Pain at the injection site (incidence rate of about 10%), swelling (2%), hematoma (1%).Systemic reactions: Dizziness (3%), palpitations (1%), tinnitus (0.5%), mostly transient, can be relieved after rest.
Serious adverse reactions
Allergic reactions: with an incidence rate of less than 0.1%, manifested as rash, difficulty breathing.
And even anaphylactic shock, requiring immediate rescue.
Neurological injury: Long term numbness or sensory abnormalities (with an incidence rate of about 0.01%), often related to improper injection techniques.
Contraindication
Individuals allergic to local anesthetics such as articaine or amides.
Patients with severe liver and kidney dysfunction (due to possible accumulation of metabolites).Uncontrolled hypertension or arrhythmia patients (adrenaline may worsen the condition).
Comparison with other local anesthetics
Comparison with Lidocaine
| Feature | Articaine | Lidocaine |
| Onset time | 1-3 minutes | 3-5 minutes |
| Anesthesia efficacy | Strong (1.5-2 times stronger than lidocaine) | Moderate |
| Duration of action | 20-40 minutes (excluding adrenaline) | 30-60 minutes (excluding adrenaline) |
| Allergic reaction | Low (amide class) | Higher (esters are more prone to allergies) |
| Applicable Population | Children, elderly, and individuals with allergies | Ordinary adult |
Comparison with Mexicaine
- Organizational permeability: The thiobenzene ring structure of articaine makes it easier to penetrate bone tissue, making it suitable for anesthesia of mandibular posterior teeth; Mexicaine has low lipid solubility and requires higher doses to achieve the same effect.
- Metabolic pathway: articaine powder is mainly metabolized through the liver, while meprazole is excreted through the kidneys. Patients with renal dysfunction are more likely to choose articaine.
References
Wang J, Mei J, Luo W. (2022). The potential of articaine as new generation of local anesthesia in dental clinics: A review. Journal of Dental Research, 9(4), 456–462. PMID: 36482533
FDA. (2024). Articaine Hydrochloride and Epinephrine Injection Prescribing Information. Silver Spring, MD: U.S. Food and Drug Administration.
EMA. (2019). Assessment Report: Articaine (Septanest) for Dental Local Anesthesia. London: European Medicines Agency.European Medicines Agency
Serum levels of articaine 2% and 4% in children.(https://pmc.ncbi.nlm.nih.gov/articles/PMC2148919/)
Volume and effectiveness assessment of articain 4% versus mepivacaine 2% used in third molar surgery: randomized, double-blind, split-mouth controlled clinical trial(https://pmc.ncbi.nlm.nih.gov/articles/PMC7648918/)
FAQ
1. What is Articaine and how does it work?
Articaine is a fast-acting amide local anesthetic widely used in dentistry, formulated as 4% articaine hydrochloride with epinephrine (1:100,000 or 1:200,000). It blocks sodium channels in nerve membranes, inhibiting pain signal transmission. It has a short onset (1–3 minutes) and shorter half-life than lidocaine, metabolized mainly in blood plasma by esterases, making it suitable for both simple and complex dental procedures.
2. What are the main uses and dosage of Articaine?
Articaine is indicated for infiltration and nerve block anesthesia in adults and children ≥4 years old. Common uses include extractions, root canals, crown preparations, implant surgery, and minor oral surgery. Dosage: Adults-max 7 mg/kg; routine infiltration: 0.5–2.5 mL; nerve block: 0.5–3.4 mL. It provides rapid, deep, and long-lasting anesthesia with less systemic toxicity than older anesthetics.
3. Is Articaine safe and what are common side effects?
When dosed and administered in strict accordance with standard clinical guidelines, articaine demonstrates favorable safety profiles and is generally well tolerated by most patients. The most frequently reported adverse reactions are mild and temporary, including fleeting dizziness, dull headaches, slight tachycardia, as well as mild redness, soreness or discomfort at the injection site.
Severe adverse events occur only on rare occasions. Potential rare risks involve methemoglobinemia, allergic responses triggered by sulfite preservatives contained in the formulation, and accidental nerve injury caused by improper injection operation.This drug also has clear contraindications for specific patient groups. It is prohibited for individuals with confirmed hypersensitivity to amide-type local anesthetics, patients suffering from severe cardiac arrhythmia, those with uncontrolled high blood pressure, and anyone who has a known allergy to sulfitesAs a critical operational requirement, medical practitioners must perform careful aspiration prior to each injection. This essential step effectively prevents accidental intravascular delivery and further reduces the incidence of related complications.
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