Mepivacaine and levonordefrin is a combination product of a local anesthetic and vasoconstrictor drugs used as a local anesthetic in dental procedures. Levonordefrin is one-sixth as potent as norepinephrine.

Mepivacaine and levonordefrin Uses:

• Dental anesthesia:

  • It is used as a local anesthetic for dental procedures by infiltration or nerve block in adult and pediatric patients.

Mepivacaine and levonordefrin Dose in Adults:

Note: Dosage varies according to the anesthetic procedure, amount of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of the patient. It is advised to use the lowest effective dose along with careful aspiration.

Mepivacaine and levonordefrin Dose in the Dental anesthesia, infiltration, or conduction block:

• Usual dose: Mepivacaine 34 mg (1.7 mL) per site or mepivacaine 180 mg (9 mL) for the entire oral cavity
• Maximum cumulative mepivacaine dose: 6.6 mg/kg or 400 mg (whichever is less) during any single dental sitting

Mepivacaine and levonordefrin Dose in Children:

Note: Dosage varies alongside the anesthetic procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of the patient.

• It is advised here to use the lowest effective dose along with careful aspiration.

Mepivacaine and levonordefrin Dose in the Dental anesthesia, infiltration, or conduction block:

• Children and Adolescents:

  • The maximum dosage must be carefully calculated on the basis of the patient's weight.
  • The manufacturer suggests a maximum mepivacaine dose of 6.6 mg/kg, which need not exceed 180 mg as a 2% solution.
  • The American Academy of Pediatric Dentistry (AAPD) proposed a maximum mepivacaine dose of 4.4 mg/kg or a maximum total dose of 300 mg in any single dental sitting (AAPD 2015).

Pregnancy Risk Factor C

• This combination is not suitable for animal reproduction studies.

Use of levonordefrin and mepivacaine during lactation

• Breast milk may contain mepivacaine and levonordefrin, but it isn't yet clear.
• According to the manufacturer, caution is exercised when administering mepivacaine/levonordefrin to breastfeeding women.
• Breastfeeding mothers are not advised to take mepivacaine and levonordefrin as they are known to have no effect on infants.

Dose in Kidney Disease:

In this regard, there are no dosage adjustments provided in the manufacturer's labeling.

Mepivacaine and levonordefrin Dose in Liver disease:

• There are no dosage adjustments provided in the manufacturer's labeling, though use with caution.
• However, patients with severe hepatic disease, as having an inability to metabolize local anesthetics normally, are more vulnerable to developing toxic plasma concentrations.

• The degree of severe effects in the CNS and cardiovascular system is directly linked to the blood levels of mepivacaine.
• The effects mentioned below are more likely to occur after systemic administration rather than infiltration. Also, see mepivacaine.

Side effects of Mepivacaine and levonordefrin

• Central nervous system:

  • Disorientation
  • Dizziness
  • Drowsiness
  • Excitement
  • Loss of consciousness
  • Nervousness
  • Seizure

• Hypersensitivity:

  • Hypersensitivity reaction

• Neuromuscular & skeletal:

  • Tremor

• Ophthalmic:

  • Blurred vision

Contraindications to Mepivacaine and levonordefrin:

Hypersensitivity to levonordefrin, mepivacaine, and local anesthetics amide-type as well as any component of the formulation

Warnings and precautions

• CNS toxicity:

  • Monitor the patient's consciousness carefully after each local anesthetic injection.
  • Any signs such as restlessness, anxiety or dizziness, blurred sight, blurred vision, tremors, and depression may indicate CNS toxicity.
  • However, the majority of treatment is supportive and symptomatic.

• Methemoglobinemia:

  • This has been reported using local anesthetics. Patients with clinically significant methemoglobinemia should be treated immediately.
  • The onset of anesthesia may occur immediately or over time (hours).
  • Patients with glucose-6-phosphate hydroxygenase deficiency or congenital or irreversible methemoglobinemia, pulmonary compromise, exposures to oxidizing agents and their metabolites, and infants under 6 months old are more at risk. cyanosis, headaches, rapid pulse, shortness or light-headedness, fatigue, and/or rapid heartbeat.

• Respiratory arrest

  • Rare cases of sudden respiratory arrest have been reported by local anesthetics.

• Seizures:

  • Convulsions that can cause cardiac arrest and systemic toxicities have been reported, possibly following an unintentional intravascular injectable.

• Cardiovascular disease

  • Patients with arteriosclerotic and cerebral vascular disease, hypertension, heart block, cerebral vascular impairment, heart block, hypertension, and/or ischemic heart disease should be treated with caution.

• Diabetes:

  • Patients with diabetes should be cautious.

• Hepatic impairment

  • Patients with hepatic impairment should be more cautious when using it.

• Hyperthyroidism:

  • Patients with hyperthyroidism should take extra care when using it.

• Renal impairment

  • Patients with impaired renal function should be careful.

Mepivacaine and levonordefrin: Drug Interaction

Monitoring parameters:

None mentioned.

How to administer Mepivacaine and levonordefrin?

• Must be administered gradually, with frequent aspirations before and during the injection to avoid intravascular injection.
• In case of inflammation and/or sepsis in the region of the proposed use it carefully.

Mechanism of action of Mepivacaine and levonordefrin:

Mepivacaine

• Local anesthetics are able to bind to specific areas of the intracellular sodium channels' surface to prevent sodium influx into the axon.
• Depolarization, which is essential for action potential propagation as well as subsequent nerve function, is therefore prevented.
• The sodium channel block can turn in the other direction. When the drug is diffused away from the axon, sodium channel function can be restored. Nerve propagation returns to normal.

Levonordefrin:

• The mepivacaine anesthetic effects by causing vasoconstriction (alpha-adrenergic receptor antagonist) to the vasculature around the nerve axons lasts for a longer time.
• This stopped mepivacaine from being absorbed by the nerves, resulting in longer retention of the axon.

The onset of action:

• Upper jaw: 30 to 120 seconds
• Lower jaw: 1 to 4 minutes

Duration:

• Upper jaw: 1 to 2.5 hours
• Lower jaw: 2.5 to 5.5 hours

Protein binding:

• Mepivacaine: ~75%

Metabolism:

• Mepivacaine: Primarily hepatic via N-demethylation, hydroxylation, and glucuronidation

Excretion:

• Mepivacaine: Urine (90% to 95% as metabolites)

International Brands of Mepivacaine and levonordefrin:

• Carbocaine 2% with Neo-Cobefrin
• Polocaine Dental
• Scandonest 2% L
• Polocaine 2% and Levonordefrin 1:20,000

Mepivacaine and levonordefrin Brands Names in Pakistan:

No Brands are Available in Pakistan yet.