Mepivacaine

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Mepivacaine
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]

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Black Box Warning

Black Box warning
See full prescribing information for complete Boxed Warning.
* These solutions are not intended for spinal anesthesia or dental use

Overview

Mepivacaine is a local anesthetic that is FDA approved for the {{{indicationType}}} of epidural anesthesia, epidural block, injection of anesthetic agent into brachial plexus, injection of anesthetic agent into pudendal nerve, local anesthesia, local anesthesia, by infiltration, local anesthetic intercostal nerve block. local anesthetic nerve block, transvaginal, local anesthetic nerve block in cervical region. pain management, paracervical block anesthesia, regional anesthesia. There is a Black Box Warning for this drug as shown here. Common adverse reactions include cardiovascular: bradyarrhythmia, cardiac arrest, fetal bradycardia, with paracervical block, heart block, hypotension, ventricular arrhythmia, immunologic: bacterial meningitis, septic, immune hypersensitivity reaction (rare ), musculoskeletal: chondrolysis of articular cartilage, neurologic: cranial nerve disorder, seizure, respiratory: respiratory arrest.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

  • Dosage varies with anesthetic procedure, area to be anesthetized, vascularity of tissues, number of neuronal segments to be blocked, depth of anesthesia and degree of muscle relaxation required, and duration of anesthesia required.
Epidural anesthesia, epidural block
  • 15 to 30 mL (150 to 300 mg) of 1% solution.
  • 10 to 25 mL (150 to 375 mg) of 1.5% solution.
  • 10 to 20 mL (200 to 400 mg) of 2% solution
Injection of anesthetic agent into brachial plexus
  • 5 to 40 mL (50 to 400 mg) of 1% solution
  • 5 to 20 mL (100 to 400 mg) of 2% solution
  • 5 to 40 mL (50 to 400 mg) of 1% solution; one-half of total dose injected into each side
Injection of anesthetic agent into pudendal nerve
  • 5 to 20 mL (100 to 400 mg) of 2% solution; one-half of total dose injected into each side
Local anesthesia
  • Doses vary with anesthetic procedure, MAX single adult dose is 400 mg
  • Local anesthesia, by infiltration
  • 0.5% or 1% solution; MAX dose 400 mg
  • Local anesthetic intercostal nerve block
  • 5 to 40 mL (50 to 400 mg) of 1% solution
  • 5 to 20 mL (100 to 400 mg) of 2% solution
  • Local anesthetic nerve block, Transvaginal
  • Max 30 mL (300 mg) of 1% solution; one-half of total dose injected into each side
  • Local anesthetic nerve block in cervical region
  • 5 to 40 mL (50 to 400 mg) of 1% solution
  • 5 to 20 mL (100 to 400 mg) of 2% solution
Pain management: therapeutic block
  • 1 to 5 mL (10 to 50 mg) of 1% solution
  • 1 to 5 mL (20 to 100 mg) of 2% solution
Paracervical block anesthesia
  • Max 20 mL (200 mg) of 1% solution every 90 min; one half of total dose injected each side; inject slowly, with 5 min between sides
Regional anesthesia
  • Doses vary with anesthetic procedure, MAX single adult dose is 400 mg

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information about Off-Label Guideline-Supported Use of Mepivacaine in adult patients.

Non–Guideline-Supported Use

There is limited information about Off-Label Non–Guideline-Supported Use of Mepivacaine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Epidural anesthesia, epidural block
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Injection of anesthetic agent into brachial plexus
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Injection of anesthetic agent into pudendal nerve
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Local anesthesia
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Local anesthesia, by infiltration
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Local anesthetic intercostal nerve block
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Local anesthetic nerve block, Transvaginal
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Local anesthetic nerve block in cervical region
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Pain management
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Paracervical block anesthesia
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%
Regional anesthesia
  • Dose not to exceed 5-6 mg/kg
  • Age under 3 yr, weight less than 30 pounds use concentrations of 0.5-1.5%

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information about Off-Label Guideline-Supported Use of Mepivacaine in pediatric patients.

Non–Guideline-Supported Use

There is limited information about Off-Label Non–Guideline-Supported Use of Mepivacaine in pediatric patients.

Contraindications

  • Mepivacaine is contraindicated in patients with a known hypersensitivity to it or to any local anesthetic agent of the amide-type or to other components of solutions of Mepivacaine.

Warnings

Black Box warning
See full prescribing information for complete Boxed Warning.
* These solutions are not intended for spinal anesthesia or dental use
  • Local anesthetics should only be employed by clinicians who are well versed in diagnosis and management of dose-related toxicity and other acute emergencies which might arise from the block to be employed, and then only after insuring the immediate availability of oxygen, other resuscitative drugs, cardiopulmonary resuscitative equipment, and the personnel resources needed for proper management of toxic reactions and related emergencies. (see also adverse reactions and precautions.) delay in proper management of dose-related toxicity, underventilation from any cause, and/or altered sensitivity may lead to the development of acidosis, cardiac arrest and, possibly, death.
  • Local anesthetic solutions containing antimicrobial preservatives (i.e., those supplied in multiple-dose vials) should not be used for epidural or caudal anesthesia because safety has not been established with regard to intrathecal injection, either intentionally or inadvertently, of such preservatives.
  • Intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions. The majority of reported cases of chondrolysis have involved the shoulder joint; cases of gleno-humeral chondrolysis have been described in pediatric and adult patients following intra-articular infusions of local anesthetics with and without epinephrine for periods of 48 to 72 hours. There is insufficient information to determine whether shorter infusion periods are not associated with these findings. The time of onset of symptoms, such as joint pain, stiffness and loss of motion can be variable, but may begin as early as the 2nd month after surgery. Currently, there is no effective treatment for chondrolysis; patients who experienced chondrolysis have required additional diagnostic and therapeutic procedures and some required arthroplasty or shoulder replacement.
  • It is essential that aspiration for blood or cerebrospinal fluid (where applicable) be done prior to injecting any local anesthetic, both the original dose and all subsequent doses, to avoid intravascular or subarachnoid injection. However, a negative aspiration does not ensure against an intravascular or subarachnoid injection.
  • Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics.
  • Mepivacaine with epinephrine or other vasopressors should not be used concomitantly with ergot-type oxytocic drugs, because a severe persistent hypertension may occur. Likewise, solutions of Mepivacaine containing a vasoconstrictor, such as epinephrine, should be used with extreme caution in patients receiving monoamine oxidase inhibitors (MAOI) or antidepressants of the triptyline or imipramine types, because severe prolonged hypertension may result.
  • Local anesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection.
  • Mixing or the prior or intercurrent use of any local anesthetic with Mepivacaine cannot be recommended because of insufficient data on the clinical use of such mixtures.

Adverse Reactions

Clinical Trials Experience

  • Reactions to Mepivacaine are characteristic of those associated with other amide-type local anesthetics. A major cause of adverse reactions to this group of drugs is excessive plasma levels, which may be due to overdosage, inadvertent intravascular injection, or slow metabolic degradation.
Systemic
  • The most commonly encountered acute adverse experiences which demand immediate counter-measures are related to the central nervous system and the cardiovascular system. These adverse experiences are generally dose related and due to high plasma levels which may result from overdosage, rapid absorption from the injection site, diminished tolerance, or from unintentional intravascular injection of the local anesthetic solution. In addition to systemic dose-related toxicity, unintentional subarachnoid injection of drug during the intended performance of caudal or lumbar epidural block or nerve blocks near the vertebral column (especially in the head and neck region) may result in underventilation or apnea (“Total or High Spinal”). Also, hypotension due to loss of sympathetic tone and respiratory paralysis or underventilation due to cephalad extension of the motor level of anesthesia may occur. This may lead to secondary cardiac arrest if untreated. Factors influencing plasma protein binding, such as acidosis, systemic diseases which alter protein production, or competition of other drugs for protein binding sites, may diminish individual tolerance.
Central Nervous System Reactions
  • These are characterized by excitation and/or depression. Restlessness, anxiety, dizziness, tinnitus, blurred vision, or tremors may occur, possibly proceeding to convulsions. However, excitement may be transient or absent, with depression being the first manifestation of an adverse reaction. This may quickly be followed by drowsiness merging into unconsciousness and respiratory arrest. Other central nervous system effects may be nausea, vomiting, chills, and constriction of the pupils.
  • The incidence of convulsions associated with the use of local anesthetics varies with the procedure used and the total dose administered. In a survey of studies of epidural anesthesia, overt toxicity progressing to convulsions occurred in approximately 0.1% of local anesthetic administrations.
Cardiovascular Reactions
  • High doses or, inadvertent intravascular injection, may lead to high plasma levels and related depression of the myocardium, decreased cardiac output, heart block, hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmias, and possibly cardiac arrest. (See Warnings, Precautions, and Overdosage sections.)
Allergic
  • Allergic-type reactions are rare and may occur as a result of sensitivity to the local anesthetic or to other formulation ingredients, such as the antimicrobial preservative methylparaben, contained in multiple-dose vials. These reactions are characterized by signs such as urticaria, pruritus, erythema, angioneurotic edema (including laryngeal edema), tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly, anaphylactoid-like symptomatology (including severe hypotension). Cross sensitivity among members of the amide-type local anesthetic group has been reported. The usefulness of screening for sensitivity has not been definitely established.
Neurologic
  • The incidences of adverse neurologic reactions associated with the use of local anesthetics may be related to the total dose of local anesthetic administered and are also dependent upon the particular drug used, the route of administration, and the physical status of the patient. Many of these effects may be related to local anesthetic techniques, with or without a contribution from the drug.
  • In the practice of caudal or lumbar epidural block, occasional unintentional penetration of the subarachnoid space by the catheter or needle may occur. Subsequent adverse effects may depend partially on the amount of drug administered intrathecally and the physiological and physical effects of a dural puncture. A high spinal is characterized by paralysis of the legs, loss of consciousness, respiratory paralysis, and bradycardia.
  • Neurologic effects following epidural or caudal anesthesia may include spinal block of varying magnitude (including high or total spinal block); hypotension secondary to spinal block; urinary retention; fecal and urinary incontinence; loss of perineal sensation and sexual function; persistent anesthesia, paresthesia, weakness, paralysis of the lower extremities, and loss of sphincter control all of which may have slow, incomplete, or no recovery; headache; backache; septic meningitis; meningismus; slowing of labor; increased incidence of forceps delivery; cranial nerve palsies due to traction on nerves from loss of cerebrospinal fluid.
  • Neurologic effects following other procedures or routes of administration may include persistent anesthesia, paresthesia, weakness, paralysis, all of which may have slow, incomplete, or no recovery.

Postmarketing Experience

There is limited information regarding Mepivacaine Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Mepivacaine Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C

  • Animal reproduction studies have not been conducted with mepivacaine. There are no adequate and well-controlled studies in pregnant women of the effect of mepivacaine on the developing fetus. Mepivacaine hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. This does not preclude the use of Mepivacaine at term for obstetrical anesthesia or analgesia. (See Labor and Delivery.)
  • Mepivacaine has been used for obstetrical analgesia by the epidural, caudal, and paracervical routes without evidence of adverse effects on the fetus when no more than the maximum safe dosages are used and strict adherence to technique is followed.


Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Mepivacaine in women who are pregnant.

Labor and Delivery

  • Local anesthetics rapidly cross the placenta, and when used for epidural, paracervical, caudal, or pudendal block anesthesia, can cause varying degrees of maternal, fetal, and neonatal toxicity. (See Pharmacokinetics-Clinical Pharmacology.) The incidence and degree of toxicity depend upon the procedure performed, the type and amount of drug used, and the technique of drug administration. Adverse reactions in the parturient, fetus, and neonate involve alterations of the central nervous system, peripheral vascular tone, and cardiac function.
  • Maternal hypotension has resulted from regional anesthesia. Local anesthetics produce vasodilation by blocking sympathetic nerves. Elevating the patient’s legs and positioning her on her left side will help prevent decreases in blood pressure. The fetal heart rate also should be monitored continuously and electronic fetal monitoring is highly advisable.
  • Epidural, paracervical, caudal, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts. In one study, paracervical block anesthesia was associated with a decrease in the mean duration of first stage labor and facilitation of cervical dilation. Epidural anesthesia has been reported to prolong the second stage of labor by removing the parturient’s reflex urge to bear down or by interfering with motor function. The use of obstetrical anesthesia may increase the need for forceps assistance.
  • The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life. The long-term significance of these observations is unknown.
  • Fetal bradycardia may occur in 20 to 30 percent of patients receiving paracervical block anesthesia with the amide-type local anesthetics and may be associated with fetal acidosis. Fetal heart rate should always be monitored during paracervical anesthesia. Added risk appears to be present in prematurity, postmaturity, toxemia of pregnancy, and fetal distress. The physician should weigh the possible advantages against dangers when considering paracervical block in these conditions. Careful adherence to recommended dosage is of the utmost importance in obstetrical paracervical block. Failure to achieve adequate analgesia with recommended doses should arouse suspicion of intravascular or fetal intracranial injection.
  • Cases compatible with unintended fetal intracranial injection of local anesthetic solution have been reported following intended paracervical or pudendal block or both. Babies so affected present with unexplained neonatal depression at birth which correlates with high local anesthetic serum levels and usually manifest seizures within six hours. Prompt use of supportive measures combined with forced urinary excretion of the local anesthetic has been used successfully to manage this complication.
  • Case reports of maternal convulsions and cardiovascular collapse following use of some local anesthetics for paracervical block in early pregnancy (as anesthesia for elective abortion) suggest that systemic absorption under these circumstances may be rapid. The recommended maximum dose of the local anesthetic should not be exceeded. Injection should be made slowly and with frequent aspiration. Allow a five-minute interval between sides.
  • It is extremely important to avoid aortocaval compression by the gravid uterus during administration of regional block to parturients. To do this, the patient must be maintained in the left lateral decubitus position or a blanket roll or sandbag may be placed beneath the right hip and the gravid uterus displaced to the left.

Nursing Mothers

  • It is not known whether local anesthetic drugs are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when local anesthetics are administered to a nursing woman.

Pediatric Use

  • Guidelines for the administration of mepivacaine to pediatric patients are presented in Dosage And Administration.

Geriatic Use

  • Clinical studies and other reported clinical experience indicates that use of the drug in elderly patients requires a decreased dosage, (see Clinical Pharmacology, Precautions, General, and Dosage and Administration).
  • Mepivacaine and mepivacaine metabolites are known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

Gender

There is no FDA guidance on the use of Mepivacaine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Mepivacaine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Mepivacaine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Mepivacaine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Mepivacaine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Mepivacaine in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding drug administration of Mepivacaine in the drug label.

Monitoring

There is limited information regarding drug monitoring of Mepivacaine in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Mepivacaine in the drug label.

Overdosage

  • Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics or to unintended subarachnoid injection of local anesthetic solution. (See Adverse reactions, Warnings, and Precautions.)
Management of Local Anesthetic Emergencies
  • The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient’s state of consciousness after each local anesthetic injection. At the first sign of change, oxygen should be administered.
  • The first step in the management of systemic toxic reactions, as well as underventilation or apnea due to unintentional subarachnoid injection of drug solution, consists of immediate attention to the establishment and maintenance of a patent airway and effective assisted or controlled ventilation with 100% oxygen with a delivery system capable of permitting immediate positive airway pressure by mask. This may prevent convulsions if they have not already occurred.
  • If necessary, use drugs to control the convulsions. A 50 mg to 100 mg bolus IV injection of succinylcholine will paralyze the patient without depressing the central nervous or cardiovascular systems and facilitate ventilation. A bolus IV dose of 5 mg to 10 mg of diazepam or 50 mg to 100 mg of thiopental will permit ventilation and counteract central nervous system stimulation, but these drugs also depress central nervous system, respiratory, and cardiac function, add to postictal depression and may result in apnea. Intravenous barbiturates, anticonvulsant agents, or muscle relaxants should only be administered by those familiar with their use. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be evaluated. Supportive treatment of circulatory depression may require administration of intravenous fluids, and when appropriate, a vasopressor dictated by the clinical situation (such as ephedrine or epinephrine to enhance myocardial contractile force).
  • Endotracheal intubation, employing drugs and techniques familiar to the clinician may be indicated after initial administration of oxygen by mask, if difficulty is encountered in the maintenance of a patent airway or if prolonged ventilatory support (assisted or controlled) is indicated.
  • Recent clinical data from patients experiencing local anesthetic induced convulsions demonstrated rapid development of hypoxia, hypercarbia, and acidosis within a minute of the onset of convulsions. These observations suggest that oxygen consumption and carbon dioxide production are greatly increased during local anesthetic convulsions and emphasize the importance of immediate and effective ventilation with oxygen which may avoid cardiac arrest.
  • If not treated immediately, convulsions with simultaneous hypoxia, hypercarbia, and acidosis, plus myocardial depression from the direct effects of the local anesthetic may result in cardiac arrhythmias, bradycardia, asystole, ventricular fibrillation, or cardiac arrest. Respiratory abnormalities, including apnea, may occur. Underventilation or apnea due to unintentional subarachnoid injection of local anesthetic solution may produce these same signs and also lead to cardiac arrest if ventilatory support is not instituted. If cardiac arrest should occur, standard cardiopulmonary resuscitative measures should be instituted and maintained for a prolonged period if necessary. Recovery has been reported after prolonged resuscitative efforts.
  • The supine position is dangerous in pregnant women at term because of aortocaval compression by the gravid uterus. Therefore during treatment of systemic toxicity, maternal hypotension, or fetal bradycardia following regional block, the parturient should be maintained in the left lateral decubitus position if possible, or manual displacement of the uterus off the great vessels be accomplished.
  • The mean seizure dosage of mepivacaine in rhesus monkeys was found to be 18.8 mg/kg with mean arterial plasma concentration of 24.4 mcg/mL. The intravenous and subcutaneous LD50 in mice is 23 mg/kg to 35 mg/kg and 280 mg/kg respectively.

Pharmacology

Mepivacaine Wiki1.png
Mepivacaine
Systematic (IUPAC) name
(RS)-N-(2,6-dimethylphenyl)- 1-methyl-piperidine-2-carboxamide
Identifiers
CAS number 96-88-8
ATC code N01BB03
PubChem 4062
DrugBank DB00961
Chemical data
Formula C15H22N2O 
Mol. mass 246.348 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ?
Metabolism ?
Half life ?
Excretion ?
Therapeutic considerations
Pregnancy cat.

C, use w/ caution, may cause fetal bradycardia

Legal status
Routes ?

Mechanism of Action

  • Local anesthetics block the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers.
  • Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone.

Structure

  • Mepivacaine hydrochloride is 2-Piperidinecarboxamide, N-(2,6-dimethylphenyl)-1-methyl, monohydrochloride and has the following structural formula:
This image is provided by the National Library of Medicine.
  • It is a white crystalline odorless powder, soluble in water, but very resistant to both acid and alkaline hydrolysis.
  • Mepivacaine is a local anesthetic available as sterile isotonic solutions (clear, colorless) in concentrations of 1%, 1.5%, and 2% for injection via local infiltration, peripheral nerve block, and caudal and lumbar epidural blocks.
  • Mepivacaine hydrochloride is related chemically and pharmacologically to the amide-type local anesthetics. It contains an amide linkage between the aromatic nucleus and the amino group.
This image is provided by the National Library of Medicine.
  • In Water for Injection.
  • The pH of the solution is adjusted between 4.5 and 6.8 with sodium hydroxide or hydrochloric acid.

Pharmacodynamics

  • Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block and ultimately to cardiac arrest. In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure.
  • Following systemic absorption, local anesthetics can produce central nervous system stimulation, depression, or both. Apparent central stimulation is manifested as restlessness, tremors, and shivering, progressing to convulsions, followed by depression and coma progressing ultimately to respiratory arrest. However, the local anesthetics have a primary depressant effect on the medulla and on higher centers. The depressed stage may occur without a prior excited stage.
  • A clinical study using 15 mL of 2% epidural mepivacaine at the T 9-10 interspace in 62 patients, 20-79 years of age, demonstrated a 40% decrease in the amount of mepivacaine required to block a given number of dermatomes in the elderly (60-79 years, N=13) as compared to young adults 20-39 years).
  • Another study using 10 mL of 2% lumbar epidural mepivacaine in 161 patients, 19-75 years of age, demonstrated a strong inverse relationship between patient age and the number of dermatomes blocked per cc of mepivacaine injected.

Pharmacokinetics

  • The rate of systemic absorption of local anesthetics is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic solution. A dilute concentration of epinephrine (1:200,000 or 5 mcg/mL) usually reduces the rate of absorption and plasma concentration of Mepivacaine, however, it has been reported that vasoconstrictors do not significantly prolong anesthesia with Mepivacaine.
  • Onset of anesthesia with Mepivacaine is rapid, the time of onset for sensory block ranging from about 3 to 20 minutes depending upon such factors as the anesthetic technique, the type of block, the concentration of the solution, and the individual patient. The degree of motor blockade produced is dependent on the concentration of the solution. A 0.5% solution will be effective in small superficial nerve blocks while the 1% concentration will block sensory and sympathetic conduction without loss of motor function. The 1.5% solution will provide extensive and often complete motor block and the 2% concentration of Mepivacaine will produce complete sensory and motor block of any nerve group.
  • The duration of anesthesia also varies depending upon the technique and type of block, the concentration, and the individual. Mepivacaine will normally provide anesthesia which is adequate for 2 to 2 1/2 hours of surgery.
  • Local anesthetics are bound to plasma proteins in varying degrees. Generally, the lower the plasma concentration of drug, the higher the percentage of drug bound to plasma.
  • Local anesthetics appear to cross the placenta by passive diffusion. The rate and degree of diffusion is governed by the degree of plasma protein binding, the degree of ionization, and the degree of lipid solubility. Fetal/maternal ratios of local anesthetics appear to be inversely related to the degree of plasma protein binding, because only the free, unbound drug is available for placental transfer. Mepivacaine is approximately 75% bound to plasma proteins. The extent of placental transfer is also determined by the degree of ionization and lipid solubility of the drug. Lipid soluble, nonionized drugs readily enter the fetal blood from the maternal circulation.
  • Depending upon the route of administration, local anesthetics are distributed to some extent to all body tissues, with high concentrations found in highly perfused organs such as the liver, lungs, heart, and brain.
  • Various pharmacokinetic parameters of the local anesthetics can be significantly altered by the presence of hepatic or renal disease, addition of epinephrine, factors affecting urinary pH, renal blood flow, the route of drug administration, and the age of the patient. The half-life of Mepivacaine in adults is 1.9 to 3.2 hours and in neonates 8.7 to 9 hours.
  • Mepivacaine, because of its amide structure, is not detoxified by the circulating plasma esterases. It is rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine. The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites. Most of the metabolized mepivacaine is probably resorbed in the intestine and then excreted into the urine since only a small percentage is found in the feces. The principal route of excretion is via the kidney. Most of the anesthetic and its metabolites are eliminated within 30 hours. It has been shown that hydroxylation and N-demethylation, which are detoxification reactions, play important roles in the metabolism of the anesthetic. Three metabolites of mepivacaine have been identified from human adults: two phenols, which are excreted almost exclusively as their glucuronide conjugates, and the N-demethylated compound (2′ 6′-pipecoloxylidide).
  • Mepivacaine does not ordinarily produce irritation or tissue damage, and does not cause methemoglobinemia when administered in recommended doses and concentrations.

Nonclinical Toxicology

There is limited information regarding Mepivacaine Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Mepivacaine Clinical Studies in the drug label.

How Supplied

  • Single-dose vials and multiple-dose vials of Mepivacaine may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of Mepivacaine may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.
  • These solutions are not intended for spinal anesthesia or dental use
This image is provided by the National Library of Medicine.

Storage

  • Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]
Revised: November, 2009

Images

Drug Images

Package and Label Display Panel

MEPIVACAINE label.png
This image of the FDA label is provided by the National Library of Medicine.

Patient Counseling Information

There is limited information regarding Mepivacaine Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Mepivacaine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Mepivacaine Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Mepivacaine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.



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