Dental Anesthetics: Agent Selection, Dosing and Brand Comparison

Selection of a dental anesthetic depends on four variables: the injection technique, the duration the procedure requires, the condition of the tissue, and the patient's cardiovascular status. Five injectable agents cover general practice, and the limits that govern how many cartridges can be given come from the vasoconstrictor more often than from the anesthetic itself.

The four reasons to choose a dental anesthetic

Injection technique. Infiltration and nerve block have different requirements. Articaine penetrates dense cortical bone, which makes buccal infiltration in the posterior mandible a working alternative to a block. Articaine is not recommended for the inferior alveolar nerve block because of the greater risk of nerve damage associated with its use in that technique.

Duration. Lidocaine 2% with epinephrine 1:100,000 produces three to five hours of soft tissue anesthesia. Bupivacaine 0.5% with epinephrine 1:200,000 can extend to eight hours. Plain formulations without a vasoconstrictor are shorter.

Tissue condition. Inflamed and infected tissue is acidic. Less dental anesthetic remains in the free base form that crosses the nerve membrane, which reduces the block obtained from a standard dose. A comparison of articaine and lidocaine under these conditions is available in our review of articaine and lidocaine.

Cardiovascular status. The advised maximum epinephrine dose is 0.2 mg for a healthy adult and 0.04 mg for a patient with cardiovascular disease. Below that threshold the vasoconstrictor determines the number of cartridges available for the appointment.

The five injectable agents in general practice

Lidocaine 2% with epinephrine

Lidocaine is the most widely used local anesthetic in dentistry and is treated as the reference agent for comparison. Onset is two to four minutes. Soft tissue anesthesia lasts three to five hours with epinephrine 1:100,000. Metabolism is hepatic, with approximately ten percent excreted unchanged by the kidney. Half life is around ninety minutes.

Products: Lignospan Standard (Septodont), Cook-Waite Lidocaine 2% with epinephrine 1:100,000, Septodont Lidocaine 2% with epinephrine 1:100,000, Xylocaine 2% Dental with epinephrine 1:100,000 (Dentsply Sirona), Quala Lidocaine 2% with epinephrine 1:100,000.

Articaine 4%

Articaine carries a thiophene ring in place of the benzene ring common to the other amides, and an ester side chain. Approximately ninety percent is hydrolyzed by plasma esterases to articainic acid and ten percent is metabolized hepatically. Half life is around twenty minutes.

Articaine diffuses through dense cortical bone, which supports buccal infiltration in the posterior mandible. Its efficacy against lidocaine has been assessed by systematic review and meta-analysis in irreversible pulpitis and in pediatric dentistry. Articaine is not recommended for the inferior alveolar nerve block.

Products: Septocaine 4% with epinephrine 1:100,000 (gold), Septocaine 4% with epinephrine 1:200,000 (silver), Orabloc 4% with epinephrine 1:100,000 (Pierrel).

Mepivacaine 3% plain and 2% with levonordefrin

Mepivacaine has weak vasodilator properties and can be administered without a vasoconstrictor. It is described as the dental anesthetic of choice for patients with cardiovascular disease.

Its higher pH and lower pKa allow more effective passage across the nerve membrane in acidic tissue, and it can be more successful than other agents at anesthetizing teeth with irreversible pulpitis. It is less potent than lidocaine, and the plain formulation has a shorter duration. Indications and limits are covered in our guide to mepivacaine without a vasoconstrictor.

Products: Carbocaine 3% plain, Carbocaine 2% with levonordefrin 1:20,000.

Prilocaine 4%

Prilocaine has weak vasodilator properties and is supplied plain or with felypressin. It shows lower toxicity and less vasodilation than lidocaine. Metabolism is distributed across the lungs, kidneys and liver, which reduces hepatic load. It is used in patients with unstable angina and uncontrolled severe hypertension.

Exceeding the maximum dose of prilocaine can lead to methemoglobinemia. Some clinicians avoid felypressin containing formulations in pregnancy on the theoretical grounds of labor induction from felypressin and fetal methemoglobinemia from prilocaine. Both complications are rare at the doses used in dentistry.

Products: Citanest Plain 4% (Dentsply).

Bupivacaine 0.5% with epinephrine

Onset is five to eight minutes. Soft tissue anesthesia lasts four to nine hours with epinephrine 1:200,000. Bupivacaine has high lipid solubility, strong protein binding, hepatic metabolism, and higher cardiotoxicity than the other agents listed here.

A documented approach is to administer lidocaine for onset and follow with a bupivacaine top up for duration. Extended soft tissue anesthesia carries a risk of self inflicted lip and cheek trauma in children.

Products: Marcaine 0.5% with epinephrine 1:200,000.

Dosing and the importance of planning your restocks

Maximum doses under current labeling

Current FDA labeling for lidocaine 2% with epinephrine sets a maximum of 3.2 mg per pound with an absolute maximum of 500 mg per appointment. Earlier figures of 2 mg per pound and 300 mg absolute remain in circulation and appear in older reference material.

Articaine 4% carries the same 3.2 mg per pound figure. Current labeling establishes no absolute maximum. Product inserts issued through 2010 listed 500 mg, equivalent to approximately seven cartridges.

Bupivacaine 0.5% with epinephrine has an absolute maximum of 90 mg. No milligram per pound figure is established in the United States. Canadian recommendations give 0.9 mg per pound.

Epinephrine limits

The advised maximum epinephrine dose is 0.2 mg per appointment for a healthy adult and 0.04 mg for a patient with cardiovascular disease.

For a 150 pound patient, the lidocaine content of lidocaine 2% with epinephrine 1:100,000 permits approximately thirteen cartridges. The epinephrine content reduces the figure to eleven. For articaine 4% with epinephrine 1:100,000, where labeling sets no absolute maximum for the anesthetic, the eleven cartridge figure derives entirely from epinephrine content.

Epinephrine increases heart rate, cardiac output and peripheral vasodilation. In medically compromised patients these effects carry potential for hypertensive crisis, myocardial infarction or arrhythmia. Cardiovascular response to vasoconstrictor containing local anesthesia during extraction has been studied in coronary patients.

Stock implications

A practice carrying only epinephrine containing cartridges reaches the same 0.04 mg limit on every cardiac patient and the same eleven cartridge figure on every extended appointment. Plain mepivacaine and plain prilocaine remove that constraint. Stocking articaine at both 1:100,000 and 1:200,000 lowers epinephrine load per cartridge where volume is required and hemostasis is not.

Cartridge volume: 1.7, 1.8 and 2.2 mL

Reference material calculates on 1.8 mL or 2.2 mL cartridges. Septocaine, Orabloc and Quala lidocaine cartridges sold in the United States are labeled 1.7 mL.

At 4% concentration a 1.7 mL cartridge contains 68 mg of articaine and a 1.8 mL cartridge contains 72 mg. At 2% concentration a 1.7 mL cartridge contains 34 mg of lidocaine and a 1.8 mL cartridge contains 36 mg. Cartridge counts calculated from a source using a different volume will not match the product in use.

Conditions requiring dose reduction

Advanced liver disease extends the half life of amide anesthetics. Lower doses should be considered in renal impairment. Articaine is partially exempt because approximately ninety percent of its metabolism occurs in plasma rather than the liver.

Early signs of systemic toxicity are visual and sensory disturbance and seizures. Progression involves reduced consciousness, coma and respiratory failure, with tachyarrhythmia or bradyarrhythmia through to cardiac arrest.

Where the maximum dose is defined

The applicable figure is the one stated on the product insert for the specific dental anesthetic, concentration and vasoconstrictor ratio in use. Concentrations, vasoconstrictor content and cartridge volumes differ between products, and labeling has been revised. Each product page in our catalogue links to the corresponding manufacturer documentation.

The best anesthetic brands and products

Septodont

Septodont supplies the widest range: Septocaine 4% with epinephrine 1:100,000 and 1:200,000, Lignospan Standard lidocaine 2%, Cook-Waite lidocaine 2% with epinephrine 1:100,000, and Septoject needles. Septocaine 4% with epinephrine 1:100,000 is the most widely stocked dental anesthetic cartridge among practices purchasing through our platform.

Pierrel

Orabloc is articaine hydrochloride 4% with epinephrine 1:100,000, the same molecule at the same concentration and vasoconstrictor ratio as Septocaine gold. The two are pharmacologically equivalent. Differences between them are price, cartridge presentation and supply availability.

Dentsply Sirona

Xylocaine 2% Dental with epinephrine 1:100,000 covers lidocaine. Citanest Plain 4% is the prilocaine cartridge and the option where no vasoconstrictor is required and hepatic metabolism is a consideration. Oraqix 2.5% periodontal gel is also supplied by Dentsply.

Generic cartridges

Quala supplies lidocaine 2% with epinephrine 1:100,000 in 1.7 mL cartridges at lower unit cost than the branded equivalents, at the same concentration and vasoconstrictor ratio.

A working dental anesthetic formulary for a general practice: lidocaine 2% with epinephrine 1:100,000, articaine 4% with epinephrine 1:100,000, one plain agent without a vasoconstrictor, and a long acting agent where surgical procedures are performed.

When anesthesia fails, and what to change

Infected and inflamed tissue

Acidic tissue shifts the dental anesthetic towards the ionized form, which does not cross the nerve membrane. Mepivacaine has a higher pH and lower pKa than the alternatives and crosses more effectively under these conditions. Articaine and lidocaine have been compared directly in irreversible pulpitis by systematic review and meta-analysis.

The inferior alveolar nerve block

Articaine is not recommended for this technique because of the greater associated risk of nerve damage. Buccal infiltration in the posterior mandible, where articaine penetrates cortical bone, is the alternative approach.

Repeat administration

Additional cartridges of the same solution increase the total dose without changing the pharmacological condition that caused the failure, and the total dose is limited by epinephrine content. Changing agent, changing technique, or supplementing with an intraligamentary or intraosseous injection addresses the mechanism.

Beyond the cartridge: topicals, needles and delivery

Topical anesthetics

Benzocaine is supplied at 6% to 20%. The 20% formulation acts within about thirty seconds and reaches adequate depth at two to three minutes. Lidocaine topicals are supplied as 2% to 5% gels and 10% sprays, with onset at one to two minutes and adequate effect after approximately three minutes.

Needles

Gauge affects deflection and aspiration reliability. Length follows the technique rather than the patient. Septoject 30 gauge short, J Morita 30 gauge short 21 mm and Monoject 30 gauge short are the most frequently reordered options on our platform.

Syringes

Aspirating syringes have a finite service life and degrade through repeated sterilization cycles. A harpoon that no longer engages the cartridge stopper prevents reliable aspiration, which is a clinical requirement before deposition of any dental anesthetic.

Non-injectable options

Oraqix 2.5% periodontal gel is delivered subgingivally and is indicated for scaling and root planing. It removes the injection from non surgical periodontal therapy.

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Articaine cartridges

Septocaine 4% with epinephrine 1:100,000, box of 50. Septocaine 4% with epinephrine 1:200,000, box of 50. Orabloc articaine 4% with epinephrine 1:100,000.

Lidocaine cartridges

Lignospan Standard lidocaine 2%. Cook-Waite lidocaine 2% with epinephrine 1:100,000, box of 50. Septodont lidocaine 2% with epinephrine 1:100,000. Xylocaine 2% Dental with epinephrine 1:100,000. Quala lidocaine 2% with epinephrine 1:100,000, 1.7 mL, box of 50.

Cartridges without epinephrine

Citanest Plain 4% prilocaine, box of 50.

Non-injectable

Oraqix periodontal gel 2.5%, pack of 20.

Needles and delivery

Septoject plastic hub needles, 30 gauge short, 100 per pack. J Morita 30 gauge short 21 mm, box of 100. Monoject plastic hub needle, 30 gauge short.

Frequently asked questions

Which local anesthetics do dentists use?

Lidocaine 2%, articaine 4%, mepivacaine 3% plain or 2% with levonordefrin, prilocaine 4%, and bupivacaine 0.5%. Lidocaine is the most widely used dental anesthetic.

Is articaine stronger than lidocaine?

Articaine is supplied at 4% against lidocaine at 2%, so a cartridge of equal volume contains twice the anesthetic mass. Its performance in infiltration is attributed to diffusion through dense cortical bone.

Is Septocaine the same as Orabloc?

Both are articaine hydrochloride 4% with epinephrine 1:100,000 and are pharmacologically equivalent.

Do you always need epinephrine?

No. Mepivacaine and prilocaine have weak vasodilator properties and are supplied in plain formulations for patients where a vasoconstrictor is contraindicated.

Which dental anesthetic for a patient with cardiovascular disease?

Mepivacaine is described as the anesthetic of choice because it can be given without a vasoconstrictor. The advised maximum epinephrine dose in these patients is 0.04 mg against 0.2 mg for a healthy adult.

Why does the anesthetic fail on an infected tooth?

Acidic tissue reduces the proportion of dental anesthetic in the free base form that crosses the nerve membrane. Mepivacaine's higher pH and lower pKa make it more effective in these conditions.

What is the difference between 1:100,000 and 1:200,000 epinephrine?

The 1:200,000 formulation contains half the vasoconstrictor per milliliter. It produces less hemostasis and allows a higher cartridge count before the epinephrine limit is reached.