A local anaesthetic with a moderately quick onset and medium duration of action is mepivacaine (Carbocaine).

For local anaesthetic during dental treatments  and nerve blocks, it is recommended.

Mepivacaine (Carbocaine) Uses:

• Dental anesthesia:

  • It is employed to create a local anesthetic for dental procedures in both adults and children.
  • This is done through infiltration or nerve block.

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

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    Furthermore, it is used for local or regional pain relief and anesthesia through methods such as local infiltration, peripheral nerve blocks, and central neural procedures like epidural and caudal.

  • However, the use of spinal anesthesia is not allowed.

Mepivacaine (Carbocaine) Dose in Adults:

It's crucial to understand that the dose of the drug can vary based on factors such as the specific procedure, the level of anesthesia required, the blood supply to the tissue, the duration of anesthesia needed, and the patient's overall health.

It is recommended to use the smallest dose and concentration necessary to achieve the desired effect.

Mepivacaine Dose in the Local or regional anesthesia (eg, epidural, caudal, or peripheral nerve blocks):

• The highest amount of this drug that can be given in a single procedure is 400 mg, whether given all at once or in multiple doses.

• If epinephrine is added, a dose of 500 mg is permissible.

• The maximum total amount that can be administered within a 24-hour period is 1,000 mg.

Mepivacaine Dose in the treatment of Cervical, brachial, intercostal, pudendal nerve block:

• You can use 5 to 40 mL of a 1% solution or 5 to 20 mL of a 2% solution, up to a maximum dose of 400 mg.

• Administer half of the total amount on each side to block the pudendal nerve.

Mepivacaine Dose in the treatment of Transvaginal block (paracervical plus pudendal):

•  

  It can be distributed. A total of 300 mg can be dispersed in a maximum of 30 mL (combined for both sides) of a 1% solution.

• Administer half of the total dose to each side.

Mepivacaine Dose in the treatment of Paracervical block:

• You can use up to 20 mL (total for both sides) of a 1% solution, with a maximum of 200 mg.

• Inject half of the total dose on each side.

• This is the highest dose recommended for a 90-minute procedure.

• The injection should be administered slowly, with a 5-minute interval between sides.

Mepivacaine dose in the treatment of Caudal and epidural block (preservative-free solutions only):

• You have several options:

• 15 to 30 mL of a 1% solution with a maximum dose of 300 mg,
• 10 to 25 mL of a 1.5% solution with a maximum dose of 375 mg, or
• 10 to 20 mL of a 2% solution, with a maximum dose of 400 mg.

Mepivacaine Dose in the treatment of Infiltration:

• You can use up to 40 mL of a 1% solution (maximum dose of 400 mg).

• If epinephrine is added, then up to 50 mL with a maximum dose of 500 mg is allowed.

• Alternatively, an equivalent amount of a 0.5% solution can be prepared by diluting the 1% solution with normal saline (NS) and used for large areas.

Mepivacaine dose in the treatment of Peripheral nerve block to provide a surgical level of anesthesia:

• Blockade of two or more different nerves, a nerve plexus, or very big nerves at more proximal sites constitutes a  major nerve block:

  • You can administer 30 to 50 mL of a 1.5% or 1% solution, with a maximum dosage of 500 mg.

• Minor nerve block (blockade of a single nerve [eg, ulnar or radial]):

  • You can use 5 to 20 mL of a 1% solution, with a maximum dose of up to 200 mg.

• Therapeutic block:

  • You can administer 1 to 5 mL of a 1% solution with a maximum dose of 50 mg, or 1 to 5 mL of a 2% solution with a maximum dose of 100 mg.

Mepivacaine Dose in Dental anesthesia:

• Single site in upper or lower jaw:

  • You can administer 51 mg using a 3% solution.

Mepivacaine Dose for treating Infiltration and nerve block of the entire oral cavity:

• For each appointment, the dosage should not exceed 300 mg, and the maximum dose as a 3% solution should not exceed 270 mg, up to 6.6 mg/kg.
• The manufacturer recommends the highest total dose not exceeding 400 mg.
• The specific number of dental cartridges (1.7 mL each) required for the indicated amounts of mepivacaine dental anesthetic 3% can be referred to in the provided table.

Mepivacaine (Carbocaine) Dose in Childrens:

• It's important to note that the dose varies based on the procedure, the required level of anesthesia, the blood supply to the tissue, the duration of anesthesia, and the patient's overall health.

• Choose the smallest dose and concentration needed for the desired effect.

• To prevent entering blood vessels, consider administering the anesthesia incrementally and perform a negative aspiration before each injection.

• However, even if there's no blood in the syringe, it doesn't guarantee that the injection is outside the blood vessels.

• This procedure should only be carried out under the supervision of a trained medical professional with experience in anesthesia.

Mepivacaine Dose in the Dental anesthesia:

• According to the manufacturer's labeling, for children and adolescents using a 3% solution, the maximum dose is 5-6 mg/kg, with an overall limit of 270 mg.

• In adults, a single site in the upper or lower jaw is given 51 mg, equivalent to one 1.7 mL cartridge.

• As an alternative recommendation, according to the American Academy of Pediatric Dentistry (AAPD 2015), the maximum dose is 4.4 mg/kg, with a total limit of 300 mg in any single dental session.

Mepivacaine Dose in the regional or Local anesthesia (eg, epidural, caudal, or peripheral nerve blocks):

• The manufacturer advises a maximum adult dose of 400 mg, and the highest recommended single or cumulative dose for one procedure is 5 to 6 mg/kg.

• For patients under 3 years old or weighing less than 14 kg, only concentrations less than 2% should be used.

• This is to ensure sufficient drug volume for the area and to reduce the risk of local anesthetic systemic toxicity.

Mepivacaine Pregnancy Category: C

• There have not been studies conducted on animal reproduction for mepivacaine.

• Mepivacaine has been employed for providing pain relief during childbirth (obstetrical pain relief).

Use of mepivacaine while breastfeeding

• It is currently uncertain whether mepivacaine is present in breast milk.

• Therefore, breastfeeding mothers should exercise caution when using mepivacaine.

• However, it's noted that breastfeeding infants usually remain healthy, even when their mothers receive the typical infiltration doses of mepivacaine during dental anesthetics.

Dose in Kidney Disease:

While there are no specific dose adjustments outlined in the literature, caution is advised when using the medication, suggesting that individualized care and careful monitoring may be necessary.

Mepivacaine (Carbocaine) Dose in Liver disease:

The literature does not provide specific guidance on altering the dosage.

However, individuals with severe liver disease may have difficulty metabolizing local anesthetics properly, increasing the risk of potentially harmful plasma concentrations.

Therefore, caution is recommended when administering the drug to such patients.

Side effects of Mepivacaine (Carbocaine):

The effects of mepivacaine on the central nervous system (CNS) and cardiovascular system depend on factors such as the concentration of mepivacaine in the blood, the method of administration, and the patient's physical condition.

Detrimental effects are more likely to occur during systemic injection compared to infiltration.

• Cardiovascular:

  • Ventricular arrhythmia
  • Bradycardia
  • Syncope
  • Cardiovascular depression
  • Heart block
  • Cardiovascular stimulation
  • Hypertension
  • Low cardiac output
  • Hypotension
  • Tachycardia
  • Cardiac insufficiency

• Central nervous system:

  • Persistent anesthesia
  • Chills
  • Paralysis
  • Convulsions
  • Increased body temperature
  • Excitement
  • Loss of consciousness
  • Nervousness
  • Drowsiness
  • Dizziness
  • Confusion
  • Restlessness
  • Anxiety

• Dermatologic:

  • Pruritus
  • Erythema
  • Urticaria
  • Diaphoresis

• Gastrointestinal:

  • Fecal incontinence
  • Nausea
  • Oral paresthesia (persistent; involving lips, tongue, and oral tissues)
  • Vomiting

• Genitourinary:

  • Urinary retention
  • Urinary incontinence

• Hematologic & oncologic:

  • Methemoglobinemia

• Hypersensitivity:

  • Anaphylactoid reaction
  • Angioedema
  • Hypersensitivity reaction

• Neuromuscular & skeletal:

  • Tremor
  • Chondrolysis (continuous intra-articular administration)
  • Weakness

• Ophthalmic:

  • Miosis
  • Blurred vision

• Otic:

  • Tinnitus

• Respiratory:

  • Apnea
  • Respiratory depression
  • Sneezing

Contraindications to Mepivacaine (Carbocaine):

Hypersensitivity is a serious contraindication to the use of this drug.

Warnings and precautions

• Toxicity to the CNS:

  • After each administration of local anesthetic, it's crucial to closely and continuously monitor the patient's level of consciousness.

  • If symptoms such as restlessness, anxiety, or dizziness arise, the primary approach to treatment is supportive and focused on managing the symptoms.

• Familial malignant hyperthermia

  • These symptoms could potentially indicate malignant hyperthermia. It is crucial to adhere to a standard protocol for both identifying and treating this condition.

• Infusion-related intra-articular chondrolysis

  • It is not recommended to administer continuous intra-articular injections of local anesthetics after arthroscopic or other surgical procedures.
  • Chondrolysis, which is most commonly observed in the shoulder joint, has been reported after infusion.
  • In certain cases, this may lead to the need for shoulder replacement or arthroplasty.

• Methemoglobinemia

  • Local anesthesia has been utilized to manage clinically significant cases of methemoglobinemia.

  • It is essential to treat methemoglobinemia promptly, as it can occur either immediately or several hours after exposure.

  • Individuals at a higher risk include those with glucose-6-phosphate dehydrogenase deficiencies, congenital or irreversible methemoglobinemia, cardiac issues, exposure to oxidizing agents or their byproducts, and infants younger than 6 months old.

• Respiratory arrest

  • Local anesthetics are not typically used to treat respiratory arrest.
  • In cases of respiratory arrest, immediate medical attention and interventions such as cardiopulmonary resuscitation (CPR) are crucial.
  • Local anesthetics are primarily used to induce loss of sensation in a specific area of the body and are not designed to address respiratory issues.
  • Respiratory arrest requires prompt and appropriate emergency medical care.

• Seizures

  • Accidental intravascular injections of local anesthetics can potentially lead to convulsions resembling cardiac arrest.

  • It's important to exercise caution during administration to minimize the risk of unintended injection into blood vessels, as such occurrences can have serious consequences.

  • Immediate recognition and appropriate management are essential in case of complications.

• Cardiovascular disease

  • Patients with cardiovascular disease, especially those with rhythm disturbances, a history of shocks, heart block, or hypotension, should exercise caution when considering the use of certain medications or procedures, including those involving local anesthetics.
  • Special attention and consultation with a healthcare professional may be needed to ensure the safety and appropriate management of these patients.

• Hepatic impairment

  • Individuals with severe hepatic (liver) disorders may be at a higher risk of producing harmful plasma concentrations of local anesthetics.

  • This is because their ability to metabolize these substances may be impaired or abnormal.

  • Caution is advised when using local anesthetics in individuals with severe hepatic disorders to minimize the risk of adverse effects.

• Renal impairment

  • Patients with impaired renal (kidney) function should exercise caution when using certain medications, including local anesthetics.

  • Impaired renal function can affect the clearance of drugs from the body, potentially leading to higher concentrations and an increased risk of adverse effects.

  • It is important for healthcare professionals to adjust dosages and closely monitor patients with impaired renal function to ensure the safe and effective use of medications.

Mepivacaine: Drug Interaction

Monitoring parameters:

• Vital signs.
• State of consciousness.
• Signs of CNS toxicity

How to administer Mepivacaine (Carbocaine)?

• To prevent intravascular injection, it's recommended to administer the injection slowly in small, incremental doses.

• Frequent aspirations before and during the injection can help ensure that the injection is not accidentally delivered into a blood vessel.

• Additionally, when there is infection and inflammation in the area where the injection is intended, caution should be exercised.

• It's important to consider the condition of the site and, if necessary, consult with a healthcare professional to determine the most appropriate course of action.

Mechanism of action of Mepivacaine (Carbocaine):

• Mepivacaine, a local anesthetic similar to lidocaine, belongs to the amide class.

• Local anesthetics, including mepivacaine, work by binding to specific areas on intracellular sodium channels.

• This binding prevents the influx of sodium ions into the nerve axon, thereby preventing depolarization.

• Depolarization is crucial for the propagation of action potentials and subsequent nerve function.

• The effect of mepivacaine is reversible. Once the medication diffuses away from the axon, sodium channel function is restored, allowing nerve transmission to resume.

• This mechanism allows for the temporary and reversible numbing of the targeted area.

The onset of action (route and dose-dependent):

• The onset duration of mepivacaine anesthesia can vary:

• Generally, it ranges from 3 to 20 minutes.
• Specifically for dental procedures:
  • In the upper jaw, the onset time is approximately 30 to 120 seconds.
  • In the lower jaw, the onset time is approximately 1 to 4 minutes.

Duration (route and dose-dependent):

• The duration of mepivacaine anesthesia can last between 2 to 2.5 hours.

• For dental procedures, the duration is typically:

• In the upper jaw: around 20 minutes.
• In the lower jaw: around 40 minutes.

Protein binding:

• About 75% of the drug sticks to proteins in the blood.

• This can affect how the drug moves around the body and how well it works.

Metabolism:

• Mostly, the liver is the main organ where the drug undergoes changes.

• These changes include N-demethylation, hydroxylation, and glucuronidation.

Half-life elimination:

• The time it takes for the drug to be eliminated from the body is different for neonates (8.7 to 9 hours) compared to adults (1.9 to 3.2 hours).
• Neonates take a longer time to eliminate the drug compared to adults.

Excretion:

• The elimination of the drug primarily occurs through the kidneys, with 90% to 95% of it being excreted as metabolites.

International Brand Names of Mepivacaine:

• Carbocaine
• Carbocaine Preservative-Free
• Polocaine; Polocaine Dental
• Polocaine-MPF
• Scandonest 3% Plain
• Carbocain
• Carbocain Dental
• Carbocaina
• Carbocaine Dental
• Carbocaine HCl
• Isocaine
• Isocaine 3%
• Lentocaine
• Meaverin
• Mepecaine
• Mepicaton
• Mepicaton 3%
• Mepidont
• Mepifrin
• Mepigobbi
• Mepivastesin
• Mevan
• Scandicain
• Scandicaine
• Scandinibsa
• Scandonest
• Scandonest Plain
• Scandonest Sans Vasoconstricteur

Mepivacaine Brand Names in Pakistan: