Septocaine

S

Generic Name: Articaine Hydrochloride
Class: Local Anesthetics
Chemical Name: 4-Methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiopenecarboxylic acid methyl ester monohydrochloride
Molecular Formula: C13H20N2O3S•HCl
CAS Number: 23964-57-0

Introduction

Intermediate-acting local anesthetic (amide type).1 2 3 4

Uses for Septocaine Dental Anesthesia

Local, infiltrative, or regional (i.e., nerve block) anesthesia in simple and complex dental and periodontal procedures.1 8

Anesthetic activity comparable to that of lidocaine, mepivacaine, and prilocaine.2 4 7

Septocaine Dosage and Administration General

Determine dosage based on type and extent of surgical procedure, depth of anesthesia, degree of muscular relaxation, and condition of the patient.1 Use smallest dose required to produce the desired effect.1

For pediatric patients, determine dosage based on age, weight, physical condition of the patient, and type and extent of surgical procedure.1

Administration Submucosal Injection

For solution and drug compatibility information, see Compatibility under Stability.

Administer by submucosal infiltration or by nerve block.1

Aspirate prior to administration to guard against intravascular injection.1

For chemical disinfection of the cartridge unit, use isopropyl (rubbing) alcohol (91%) or ethyl alcohol (70%).1 Do not use brands that are not of USP grade, since these preparations may contain denaturants that may be injurious to rubber.1

Dosage

Available as fixed combination containing articaine hydrochloride and epinephrine bitartrate; dosage expressed in terms of articaine hydrochloride.1

Pediatric Patients Dental Anesthesia Submucosal Injection

Children ?4 years of age: Use lower dosages than those suggested for healthy adults (see Adults under Dosage and Administration).1

Simple procedures: 0.76–5.65 mg/kg used in clinical trials.1

Complex procedures: 0.37–7.48 mg/kg used in clinical trials.1

Approximately 13% of pediatric patients in clinical trials required additional injections for complete anesthesia.1

Adults Dental Anesthesia Submucosal Injection

Usual dosage range: 20–204 mg.1

Recommended Dosages (as articaine hydrochloride 4% with epinephrine 1:100,000) for Dental Anesthesia in Healthy Adults1

Procedure

Volume of Injection (mL)

Total Dose of Articaine Hydrochloride (mg)

Infiltration

0.5–2.5

20–100

Nerve block

0.5–3.4

20–136

Oral surgery

1–5.1

40–204

Prescribing Limits Pediatric Patients Dental Anesthesia Submucosal Injection

Maximum 7 mg/kg (0.175 mL/kg).1

Adults Dental Anesthesia Submucosal Injection

Maximum 7 mg/kg (0.175 mL/kg).1

Special Populations Hepatic Impairment

Reduce dosage in patients with hepatic disease.1

Geriatric Patients

Reduce dosage in patients ?65 years of age.1

Patients 65–74 Years of Age

Simple procedures: 0.43–4.76 mg/kg used in clinical trials.1

Complex procedures: 1.05–4.27 mg/kg used in clinical trials.1

Approximately 6% of patients in clinical trials required additional injections for complete anesthesia.1

Patients ?75 Years of Age

Simple procedures: 0.78–4.76 mg/kg used in clinical trials.1

Complex procedures: 1.12–2.17 mg/kg used in clinical trials.1

None of the patients in clinical trials required additional injections for complete anesthesia.1

Other Populations

Reduce dosage in patients with cardiac disease, debilitated patients, and patients with acute illnesses.1

Cautions for Septocaine Contraindications

Known hypersensitivity to local anesthetics of the amide type or to sodium metabisulfite.1 4

Warnings/Precautions Warnings Epinephrine Administration

Injection contains epinephrine, which may cause tissue necrosis or systemic toxicity.1 Consider usual precautions associated with epinephrine administration.1

Accidental Intravascular Injection

Accidental intravascular injection may result in confusion, seizures, CNS or cardiorespiratory depression, coma, and/or respiratory arrest.1

Aspirate prior to administration to guard against intravascular injection.1

Should be used only by clinicians who are sufficiently knowledgeable in the diagnosis and management of dose-related toxicity and other acute emergencies that might arise.1 Resuscitative equipment and drugs must be available for immediate use.1

Sensitivity Reactions Sulfite Sensitivity

Articaine injection contains sodium metabisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals.1

General Precautions CNS Effects

Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse CNS effects (e.g., restlessness, anxiety, tinnitus, lightheadedness, dizziness, disorientation, excitement, blurred vision, tremors, depression, drowsiness).1 3

Carefully monitor level of consciousness after each local anesthetic injection.1

Cardiovascular Effects

Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse cardiovascular effects (e.g., reduced myocardial contractility, peripheral vasodilation, depressed cardiac conduction and excitability).1 Possible atrioventricular block, ventricular arrhythmia, cardiac arrest, and, rarely, death.1 Carefully monitor cardiovascular and respiratory vital signs after each local anesthetic injection.1

Cardiac arrhythmias may occur in patients receiving potent general anesthetics; use with caution in such patients.1

Articaine hydrochloride injection contains epinephrine; risk of exaggerated vasoconstrictor response in patients with hypertension or peripheral vascular disease.1 Risk of ischemic injury or necrosis.1

Use with caution in patients with heart block or other cardiovascular disease.1

Specific Populations Pregnancy

Category C.1

Lactation

Not known whether articaine or its metabolites are distributed into milk.1 4 Caution advised if used in nursing women.1

Pediatric Use

Safety and efficacy not established in children <4 years of age.1 4

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.1

Hepatic Impairment

Not studied in patients with hepatic impairment.1 Use with caution in patients with severe hepatic impairment.1

Common Adverse Effects

Pain,1 2 4 7 headache,1 2 4 7 facial edema,1 2 4 gingivitis,1 2 4 paresthesia,1 2 4 infection.1 2 4

Interactions for Septocaine

Approximately 5–10% of available articaine is metabolized by CYP enzymes.1 3

Specific Drugs

Drug

Interaction

Comments

Anesthetics, general

Possible cardiac arrhythmias when articaine is administered during or following administration of potent general anesthetics1

Use with caution1

Antidepressants, tricyclics

Possible severe, prolonged hypertension due to epinephrine component1

Avoid concomitant use;1 if must be used concomitantly, careful monitoring is required1

Butyrophenones

Possible reduction or reversal of pressor effect of epinephrine1

Avoid concomitant use;1 if must be used concomitantly, careful monitoring is required 1

MAO inhibitors

Possible severe, prolonged hypertension due to epinephrine component1

Avoid concomitant use;1 if must be used concomitantly, careful monitoring is required1

Phenothiazines

Possible reduction or reversal of pressor effect of epinephrine1

Avoid concomitant use;1 if must be used concomitantly, careful monitoring is required1

Septocaine Pharmacokinetics Absorption Bioavailability

Peak plasma concentrations achieved approximately 25 minutes following single dose and 48 minutes following 3 doses.1

Onset

1–6 minutes following submucosal injection.1 Average onset of anesthesia following articaine administration appears to be similar to that of prilocaine5 6 8 but slightly faster than that of other local anesthetics (e.g., lidocaine).3 5 8

Duration

Complete anesthesia lasts approximately 1 hour.1

Distribution Plasma Protein Binding

Approximately 60–80% (albumin and ?-globulins).1

Elimination Metabolism

Systemically absorbed articaine is rapidly metabolized by plasma carboxyesterase to articainic acid (inactive);1 approximately 5–10% of available articaine is metabolized to articainic acid by CYP enzymes.1 3

Elimination Route

Excreted principally in urine as inactive metabolites and small amounts (2%) of unchanged drug;1 4 approximately 53–57% of administered dose excreted within 24 hours following submucosal administration.1

Half-life

Approximately 1.8 hours.1

Stability Storage Parenteral Injection

25°C (may be exposed to 15–30°C).1 Protect from light.1

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

May be incompatible with strong oxidizing agents.a

ActionsActions

Local anesthetics block the generation and conduction of nerve impulses by increasing the threshold for electrical excitation, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.1

Formulated with epinephrine to decrease articaine's rate and extent of systemic absorption and to prolong its duration of action.1 4

Has intermediate duration of action (approximately 1 hour).1 2 3 4

Advice to Patients

Prior to administration, advise patients of the possibility of temporary loss of sensation and muscle function following infiltration and nerve block injections.1

Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease).1

Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1

Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Articaine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection

4% with Epinephrine Bitartrate 1:100,000 (of epinephrine)

Septocaine (with sodium metabisulfite)

Septodont

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2004. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Septodont, Inc. Septocaine (articaine hydrochloride 4% with epinephrine 1:100,000) injection prescribing information. New Castle, DE; 2000 Apr.

2. Malamed SF, Gagnon S, Leblanc D. Efficacy of articaine: a new amide local anesthetic. J Am Dent Assoc. 2000; 131:635-42. [IDIS 448169] [PubMed 10832257]

3. Oertel R, Rahn R, Kirch W. Clinical pharmacokinetics of articaine. Clin Pharmacokinet. 1997; 33:417-25. [PubMed 9435991]

4. Malamed SF, Gagnon S, Leblanc D. Articaine hydrochloride: a study of the safety of a new amide local anesthetic. J Am Dent Assoc. 2001; 132:177-85. [IDIS 466889] [PubMed 11217590]

5. Simon MAM, Gielen MJM, Alberink N et al. Intravenous regional anesthesia with 0.5% articaine, 0.5% lidocaine, or 0.5% prilocaine. Reg Anesth. 1997; 22:29-34. [PubMed 9010944]

6. Pitkanen MT, Xu M, Haasio J et al. Comparison of 0.5% articaine and 0.5% prilocaine in intravenous regional anesthesia of the arm: a cross-over study in volunteers. Reg Anesth Pain. 1999; 24:131-5.

7. Malamed SF, Gagnon S, Leblanc D et al. A comparison between articaine HCl and lidocaine HCl in pediatric dental patients. Pediatr Dent. 2000; 22:307-11. [PubMed 10969438]

8. Septodont Inc., New Castle, DE: Personal communication.

a. Septodont, Inc. Septocaine (articaine hydrochloride) injection material safety data sheet. New Castle, DE; 2002 Jul.

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Septocaine

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