mepivacaine (Carbocaine, Polocaine, Polocaine-MPF)

Dosing and uses of Carbocaine, Polocaine (mepivacaine)

• Adult
• Pediatric

 

Adult dosage forms and strengths

injectable solution

• 1%
• 1.5%
• 2%
• 3%

 

Infiltration Anesthesia

Up to 400 mg (80 mL of 0.5% or 40 mL of 1% solution)

 

Cervical/Brachial/Intercostal or Pudendal Block

50-400 mg (5-40 mL) of 1% or 100-400 mg (5-20 mL) 2% solution

 

Postherpetic Neuropathy (Orphan)

Orphan indication sponsor

• Cinergen, LLC; 146 Medinah Drive; Blue Bell, PA 19422-3212

 

HIV-Associated Neuropathy (Orphan)

Orphan indication sponsor

• Cinergen, LLC; 146 Medinah Drive; Blue Bell, PA 19422-3212

 

Administration

Usually no more than 400 mg/dose; doses up to 550 mg has been used but rare & given no more frequently than q1.5hr; no more than 1000 mg in 24 hours

Use preservative-free preparations for spinal or epidural anesthesia

 

Other Indications & Uses

Epidural/caudal anesthesia; peripheral/sympathetic nerve block

 

Pediatric dosage forms and strengths

injectable solution

• 1%
• 1.5%
• 2%
• 3%

 

Administration

<13.6 kg: No more than 5-6 mg/kg/dose

 

Carbocaine, Polocaine (mepivacaine) adverse (side) effects

Frequency not defined

Systemic dose-related toxicity

• Underventilation/apnea ("Total or High Spinal"),
• Hypotension
• Acidosis
• Systemic diseases which alter protein production/competition of other drugs for protein binding sites

Angioneurotic edema (including laryngeal edema), syncope, depression of the myocardium, decreased cardiac output, heart block, hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmias, and possibly cardiac arrest

Excitation and/or depression, restlessness, anxiety, dizziness, tinnitus, blurred vision, tremors (possible convulsions), chills, constriction of the pupils, elevated temperature, paralysis of the of consciousness, persistent anesthesia, paresthesia, weakness, paralysis of the lower extremities/sphincter control, headache, septic meningitis, meningismus, cranial nerve palsies due to traction on nerves from of cerebrospinal fluid

Urticaria, pruritus, erythema, excessive sweating

Nausea, vomiting

Backache

Urinary retention, fecal/urinary incontinence

Sneezing, respiratory paralysis (secondary to spinal block)

Loss of perineal sensation and sexual function

Anaphylactoid-like symptomatology (including severe hypotension)

Slowing of labor; increased incidence of forceps delivery

 

Warnings

Contraindications

Hypersensitivity to mepivacaine or amide anesthetics, sensitivity to parabens

 

Cautions

Some formulations may contain sulfites

History of malignant hyperthermia

DO NOT use solutions with epinephrine in distal areas of body (eg, digit, nose, ear)

Addition of vasoconstrictor, epinephrine, will promote local hemostasis, decrease systemic absorption, and increase duration of action

Risk of chondrolysis if receiving intra-articular injection following arthroscopic or other surgical procedures

 

Pregnancy and lactation

Pregnancy category: C

Lactation: not known if excreted in breast milk

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Carbocaine, Polocaine (mepivacaine)

Half-life: 1.9-3.2 hr (adults); 8.7-9 hr (neonates)

Duration: 2-2.5 hr

Onset: 3-20 min

Protein Bound: 75%

Metabolism: liver

Metabolites: two phenols, which are excreted almost exclusively as their glucuronide conjugates, and the N-demethylated compound (2',6'-pipecoloxylidide)

Excretion: urine (principally)

 

Mechanism of action

Local anesthetics prevent generation/conduction of nerve impulses by reducing sodium permeability and increasing action potential threshold