Mepivacaine

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection, as hydrochloride:

Carbocaine: 1% (50 mL); 2% (50 mL) [contains methylparaben]

Polocaine: 1% (50 mL); 2% (50 mL) [contains methylparaben]

Solution, Injection, as hydrochloride [preservative free]:

Carbocaine Preservative-Free: 1% (30 mL); 1.5% (30 mL); 2% (20 mL)

Polocaine-MPF: 1% (30 mL); 1.5% (30 mL); 2% (20 mL) [methylparaben free]

Solution, Injection, as hydrochloride [dental use]:

Carbocaine: 3% (1.7 mL)

Polocaine Dental: 3% (1.7 mL)

Scandonest 3% Plain: 3% (1.7 mL)

Pharmacology

Mechanism of Action

Mepivacaine is an amide local anesthetic similar to lidocaine. Local anesthetics bind selectively to the intracellular surface of sodium channels to block influx of sodium into the axon. As a result, depolarization necessary for action potential propagation and subsequent nerve function is prevented. The block at the sodium channel is reversible. When drug diffuses away from the axon, sodium channel function is restored and nerve propagation returns.

Pharmacokinetics/Pharmacodynamics

Metabolism

Primarily hepatic via N-demethylation, hydroxylation, and glucuronidation

Excretion

Urine (90% to 95% as metabolites)

Onset of Action

Route and dose dependent: Range: 3 to 20 minutes; Dental: Upper jaw: 30 to 120 seconds; Lower jaw: 1 to 4 minutes

Duration of Action

Route and dose dependent: 2 to 2.5 hours; Dental: Upper jaw: 20 minutes; Lower jaw: 40 minutes

Half-Life Elimination

Neonates: 8.7 to 9 hours; Adults: 1.9 to 3.2 hours

Protein Binding

~75%

Use: Labeled Indications

Dental anesthesia: Production of local anesthesia for dental procedures by infiltration or nerve block in adult and pediatric patients.

Local or regional anesthesia (eg, epidural, caudal, or peripheral nerve blocks): Production of local or regional analgesia and anesthesia by local infiltration, peripheral and central neural techniques (epidural and caudal). Not for use in spinal anesthesia.

Contraindications

Hypersensitivity to mepivacaine, other amide-type local anesthetics, or any component of the formulation

Dosage and Administration

Dosing: Adult

Note: Dose varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. The smallest dose and concentration required to produce the desired effect should be used.

Local or regional anesthesia (eg, epidural, caudal, or peripheral nerve blocks):

Maximum single or total dose given for one procedure: 400 mg; 500 mg if epinephrine has been added (Barash 2009)

Maximum dose per 24 hours: 1,000 mg

Cervical, brachial, intercostal, pudendal nerve block: 5 to 40 mL of a 1% solution (maximum: 400 mg) or 5 to 20 mL of a 2% solution (maximum: 400 mg). For pudendal block, inject one-half the total dose each side.

Transvaginal block (paracervical plus pudendal): Up to 30 mL (total for both sides) of a 1% solution (maximum: 300 mg). Inject one-half the total dose each side.

Paracervical block: Up to 20 mL (total for both sides) of a 1% solution (maximum: 200 mg). Inject one-half the total dose to each side. This is the maximum recommended dose per 90-minute procedure; inject slowly with 5 minutes between sides.

Caudal and epidural block (preservative free solutions only): 15 to 30 mL of a 1% solution (maximum: 300 mg) or 10 to 25 mL of a 1.5% solution (maximum: 375 mg) or 10 to 20 mL of a 2% solution (maximum: 400 mg).

Infiltration: Up to 40 mL of a 1% solution (maximum: 400 mg); up to 50 mL if epinephrine has been added (maximum: 500 mg) (Barash 2009); an equivalent amount of a 0.5% solution (prepared by diluting the 1% solution with NS) may be used for large areas.

Peripheral nerve block to provide a surgical level of anesthesia (Miller 2010):

Major nerve block (blockade of two or more distinct nerves, a nerve plexus, or very large nerves at more proximal sites: 30 to 50 mL of a 1% or 1.5% solution (maximum: 500 mg)

Minor nerve block (blockade of a single nerve [eg, ulnar or radial]): 5 to 20 mL of a 1% solution (maximum: 200 mg)

Therapeutic block: 1 to 5 mL of 1% solution (maximum: 50 mg) or 1 to 5 mL of 2% solution (maximum: 100 mg)

Dental anesthesia:

Single site in upper or lower jaw: 51 mg as a 3% solution.

Infiltration and nerve block of entire oral cavity: 270 mg as a 3% solution, up to 6.6 mg/kg not to exceed 300 mg per appointment. Manufacturer's maximum recommended total dose: 400 mg.

The following number of dental cartridges (1.7 mL) provide the indicated amounts of mepivacaine dental anesthetic 3%. See table.

Table has been converted to the following text.

The following numbers of dental cartridges (1.7 mL) provide the indicated amounts of mepivacaine 3%.

1 Cartridge: 51 mg mepivacaine 3%

2 Cartridges: 102 mg mepivacaine 3%

3 Cartridges: 153 mg mepivacaine 3%

4 Cartridges: 204 mg mepivacaine 3%

5 Cartridges: 255 mg mepivacaine 3%

6 Cartridges: 306 mg mepivacaine 3%

7 Cartridges: 357 mg mepivacaine 3%

8 Cartridges: 408 mg mepivacaine 3%

Dosing: Geriatric

Refer to adult dosing; reduce dose consistent with age and physical status.

Dosing: Pediatric

Note: Dose varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. The smallest dose and concentration required to produce the desired effect should be used. Consider incremental administration with negative aspiration prior to each injection; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided (Mulroy 2010). Should only be administered under the supervision of a qualified physician experienced in the use of anesthetics.

Dental anesthesia: Children and Adolescents: 3% solution: Injection:

Manufacturer's labeling: Maximum dose: 5 to 6 mg/kg; maximum total dose: 270 mg. In adults, the dose for single site in upper or lower jaw is 51 mg (one 1.7 mL cartridge)

Alternate dosing: American Academy Pediatric Dentistry (AAPD 2015): Maximum dose: 4.4 mg/kg; maximum total dose: 300 mg in any single dental sitting

Local or regional anesthesia (eg, epidural, caudal, or peripheral nerve blocks): Maximum single or total dose given for one procedure: 5 to 6 mg/kg (maximum adult dose per manufacturer: 400 mg); only concentrations <2% should be used in patients <3 years or <14 kg to ensure adequate drug volume for area and to decrease the potential for local anesthetic systemic toxicity

Administration

Administer slowly in small incremental doses, with frequent aspirations before and during the injection to avoid intravascular injection. Use with caution when there is inflammation and/or sepsis in the region of the proposed injection.

Storage

Mepivacaine 1%, 1.5%, and 2%: Store at 20°C to 25°C (68°F to 77°F). Brief exposure up to 40°C (104°F) does not adversely affect the product. Solutions may be sterilized.

Mepivacaine 3% (dental products): Store at <25°C (77°F); do not freeze. Protect from light.

Drug Interactions

Beta-Blockers: May increase the serum concentration of Mepivacaine. Monitor therapy

Bupivacaine (Liposomal): Local Anesthetics may enhance the adverse/toxic effect of Bupivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine, but the optimal duration of dose separation for other local anesthetics is unknown Avoid combination

Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Monitor therapy

Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy

Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Monitor therapy

Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Monitor therapy

Adverse Reactions

Frequency not defined. Degree of adverse effects in the CNS and cardiovascular system is directly related to the blood levels of mepivacaine, route of administration, and physical status of the patient. The effects below are more likely to occur after systemic administration rather than infiltration.

Cardiovascular: Bradycardia, cardiac insufficiency, cardiovascular depression, cardiovascular stimulation, heart block, hypertension, hypotension, low cardiac output, syncope, tachycardia, ventricular arrhythmia

Central nervous system: Anxiety, chills, confusion, convulsions, dizziness, drowsiness, excitement, loss of consciousness, increased body temperature, nervousness, paralysis, persistent anesthesia, restlessness

Dermatologic: Diaphoresis, erythema, pruritus, urticaria

Gastrointestinal: Fecal incontinence, nausea, oral paresthesia (persistent; involving lips, tongue, and oral tissues), vomiting

Genitourinary: Urinary incontinence, urinary retention

Hematologic & oncologic: Methemoglobinemia

Hypersensitivity: Anaphylactoid reaction, angioedema, hypersensitivity reaction

Neuromuscular & skeletal: Chondrolysis (continuous intra-articular administration), tremor, weakness

Ophthalmic: Blurred vision, miosis

Otic: Tinnitus

Respiratory: Apnea, respiratory depression, sneezing

Warnings/Precautions

Concerns related to adverse effects:

• CNS toxicity: Careful and constant monitoring of the patient's state of consciousness should be done following each local anesthetic injection; at such times, restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness may be early warning signs of CNS toxicity. Treatment is primarily symptomatic and supportive.
• Familial malignant hyperthermia: May potentially trigger malignant hyperthermia; follow standard protocol for identification and treatment.
• Intra-articular infusion related chondrolysis: Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use; chondrolysis (primarily in the shoulder joint) has occurred following infusion, with some cases requiring arthroplasty or shoulder replacement.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
• Respiratory arrest: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest.
• Seizures: Convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease, including rhythm disturbances, shock, heart block, and hypotension.
• Hepatic impairment: Use with caution in patients with hepatic impairment. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at a greater risk of developing, toxic plasma concentrations.
• Renal impairment: Use with caution in patients with renal impairment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Acutely ill patients: Use with caution in acutely ill patients; reduce dose consistent with age and physical status.
• Debilitated patients: Use with caution in debilitated patients; reduce dose consistent with age and physical status.
• Elderly: Use with caution in the elderly; reduce dose consistent with age and physical status.
• Pediatric: Use with caution in children; reduce dose consistent with age and physical status.

Dosage form specific issues:

• Preservative-containing solutions: Do not use solutions containing preservatives for caudal or epidural block.

Other warnings/precautions:

• Administration: Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided. Use with caution when there is inflammation and/or sepsis in the region of the proposed injection.
• Appropriate dosing: To avoid serious adverse effects and high plasma levels, the lowest dosage resulting in effective anesthesia should be administered. Repeated doses may cause significant increases in blood levels with each repeated dose due to the possibility of accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with patient status.
• Test dose: A test dose is recommended prior to epidural administration and all reinforcing doses with continuous catheter technique.
• Trained personnel: Clinicians using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.

Monitoring Parameters

Vital signs, state of consciousness; signs of CNS toxicity

Pregnancy

Pregnancy Considerations

Animal reproduction studies have not been conducted. Mepivacaine has been used in obstetrical analgesia.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Have patient report immediately to prescriber signs of methemoglobinemia (blue or gray color of the lips, nails, or skin; abnormal heartbeat; seizures; severe dizziness or passing out; severe headache; fatigue; loss of strength and energy; or shortness of breath), change in speech, slow heartbeat, fast heartbeat, change in balance, burning or numbness feeling, agitation, anxiety, metallic taste, blurred vision, noise or ringing in the ears, tremors, twitching, lightheadedness, fatigue, confusion, depression, difficulty breathing, slow breathing, or shallow breathing (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.