Polocaine 1% Solution

Manufacturer FRESENIUS KABI USA Active Ingredient Mepivacaine(me PIV a kane) Pronunciation me-PIV-a-kane
It is used to numb an area before a procedure.
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Drug Class
Local Anesthetic
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Pharmacologic Class
Amide-type Local Anesthetic
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Pregnancy Category
Category C
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FDA Approved
Jun 1960
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Mepivacaine is a medicine used to numb a specific area of your body, like a tooth or a small area of skin, to prevent pain during medical or dental procedures. It works by temporarily blocking nerve signals in that area.
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How to Use This Medicine

Taking Your Medication

To use this medication correctly, follow your doctor's instructions and read all the information provided to you. It is essential to follow the instructions carefully. This medication is administered via injection.

Storing and Disposing of Your Medication

Since this injection is given in a healthcare setting, you will not need to store it at home. A healthcare professional will administer the medication, and you will not be responsible for storing or disposing of it.

Missing a Dose

This medication is given as needed in a healthcare setting, so you will not need to worry about missing a dose. The healthcare professional will administer the medication according to your specific needs.
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Lifestyle & Tips

  • Avoid eating or drinking until the numbness completely wears off, especially if the mouth or throat area is numbed, to prevent choking or biting your tongue/cheek.
  • Be careful not to injure the numbed area, as you won't feel pain if it's damaged.
  • Follow any specific post-procedure instructions given by your healthcare provider.

Dosing & Administration

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Adult Dosing

Standard Dose: Highly variable based on procedure, site, and patient factors. For Polocaine 1% (10 mg/mL) Solution, typical doses range from 50 mg to 400 mg (5 mL to 40 mL).
Dose Range: 50 - 400 mg

Condition-Specific Dosing:

infiltration: Up to 40 mL (400 mg) of 1% solution.
peripheral nerve block: 5-20 mL (50-200 mg) of 1% solution.
epidural block: 15-20 mL (150-200 mg) of 1% solution (not typically 1% for epidural, usually 1.5% or 2%).
dental (Polocaine 2% with Levonordefrin): 1-3.6 mL (20-72 mg) of 2% solution. Max 6.6 mg/kg or 400 mg total.
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Pediatric Dosing

Neonatal: Not established for routine use. Use with extreme caution, reduced doses.
Infant: Not established for routine use. Use with extreme caution, reduced doses.
Child: Maximum recommended dose is 5-6 mg/kg (0.5-0.6 mL/kg of 1% solution) not to exceed 400 mg total. Dosing must be individualized based on age, weight, and physical status.
Adolescent: Similar to adult dosing, but consider weight and physical status. Max 5-6 mg/kg or 400 mg total.
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment required for single doses.
Moderate: No specific dose adjustment required for single doses. Caution with repeated doses due to potential accumulation of metabolites.
Severe: No specific dose adjustment required for single doses. Caution with repeated doses due to potential accumulation of metabolites.
Dialysis: Mepivacaine is not significantly removed by hemodialysis. Caution with repeated doses.

Hepatic Impairment:

Mild: No specific dose adjustment required for single doses.
Moderate: Use with caution. Consider reduced doses, especially with repeated administration, due to impaired metabolism.
Severe: Use with caution. Significant dose reduction may be necessary due to impaired metabolism and increased risk of systemic toxicity.

Pharmacology

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Mechanism of Action

Mepivacaine, an amide-type local anesthetic, reversibly blocks the initiation and conduction of nerve impulses by decreasing the permeability of the nerve cell membrane to sodium ions. This action stabilizes the neuronal membrane, preventing the generation and propagation of action potentials, thereby producing local anesthesia.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable for local administration; systemic absorption varies based on site of injection, vascularity, and presence of vasoconstrictor. Rapidly absorbed from injection sites.
Tmax: Variable, typically 5-15 minutes for peak plasma levels after nerve block, depending on site.
FoodEffect: Not applicable (parenteral administration).

Distribution:

Vd: Approximately 0.8 L/kg
ProteinBinding: Approximately 70-80% (primarily to alpha-1-acid glycoprotein)
CnssPenetration: Yes, readily crosses the blood-brain barrier and placenta.

Elimination:

HalfLife: Approximately 1.9 hours (adults); longer in neonates and patients with hepatic impairment.
Clearance: Approximately 0.9 L/min
ExcretionRoute: Renal (less than 10% as unchanged drug, remainder as metabolites).
Unchanged: Less than 10%
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Pharmacodynamics

OnsetOfAction: Rapid, typically 3-5 minutes.
PeakEffect: 5-15 minutes.
DurationOfAction: Moderate, 45-90 minutes (without vasoconstrictor); up to 3 hours with vasoconstrictor (though Polocaine 1% is plain).

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of acidosis (too much acid in the blood), such as:
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Irregular heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Signs of methemoglobinemia, a rare but potentially life-threatening condition, such as:
+ Blue or gray discoloration of the lips, nails, or skin
+ Irregular heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects, including:
+ Abnormal heartbeat (fast, slow, or irregular)
+ Restlessness
+ Anxiety
+ Changes in speech
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Numbness or tingling in the mouth
+ Metallic taste
+ Dizziness or fainting
+ Ringing in the ears
+ Shakiness
+ Twitching
+ Seizures
+ Depression
+ Breathing difficulties, slow breathing, or shallow breathing
+ Feeling nervous and excitable
+ Severe nausea or vomiting
+ Feeling hot or cold
+ Sneezing
+ Excessive sweating

Additional Side Effects (Epidural Use)

If you are using this medication via epidural administration, you may also experience:

Erectile dysfunction
Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
Loss of bowel or bladder control
Urination difficulties
Headache
Backache
Fever or chills
Stiff neck
Sensitivity to bright lights

Other Side Effects

As with any medication, you may experience side effects that are not severe but still bothersome. If you notice any of the following symptoms, contact your doctor:

Mild side effects that do not go away or bother you
* Any new or worsening symptoms

Remember, this is not an exhaustive list of potential side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Dizziness or lightheadedness
  • Ringing in the ears (tinnitus)
  • Numbness or tingling around the mouth (perioral numbness)
  • Unusual taste in the mouth (metallic taste)
  • Blurred vision or double vision
  • Tremors or muscle twitching
  • Feeling anxious or restless
  • Feeling unusually sleepy or drowsy
  • Difficulty breathing
  • Slow or irregular heartbeat
  • Feeling faint or dizzy when standing up
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor identify potential interactions between this medication and other substances.
* Any existing health problems, as this medication may interact with certain conditions.

To ensure your safety, it is crucial to verify that this medication can be taken with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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Precautions & Cautions

Important Warnings and Cautions

When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment.

Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with drugs like this one. Your risk may be increased if you have:
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency
- Heart problems
- Lung problems
- Are taking certain other medications
- Are an infant younger than 6 months of age
If you have a history of methemoglobinemia, notify your doctor.

Special Considerations
- Children: This medication should be used with caution in children, as the risk of side effects may be higher in some pediatric patients.
- Older Adults: If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
- Pregnancy and Breastfeeding: Inform your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. You and your doctor will need to discuss the potential benefits and risks to you and your baby.

Mouth and Numbing Precautions
- Eating: Avoid eating while your mouth feels numb, as you may accidentally bite your tongue.
- Numbness: Until the numbing effects of this medication have worn off and you feel fully alert, refrain from driving and other activities that require your full attention.
- Protecting the Treated Area: If you are discharged before the numbness has resolved, take precautions to protect the treated area from injury until you have regained normal sensation.

Epidural Administration
After receiving this medication via epidural administration, you may experience temporary loss of feeling and motor function in the lower half of your body. Until these effects have resolved and you have regained normal sensation and mobility, do not attempt to get out of bed or engage in any activities that may put you at risk.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Seizures
  • Unconsciousness
  • Respiratory arrest (stopping breathing)
  • Severe low blood pressure
  • Slow heart rate (bradycardia)
  • Cardiac arrest

What to Do:

If you experience any severe symptoms after receiving mepivacaine, seek immediate medical attention. For general overdose concerns, call emergency services (e.g., 911 in the US) or Poison Control (1-800-222-1222).

Drug Interactions

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Contraindicated Interactions

  • None absolute for mepivacaine itself, but caution with known hypersensitivity to amide-type local anesthetics.
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Major Interactions

  • Antiarrhythmics (Class I, e.g., Lidocaine, Tocainide, Mexiletine): Additive cardiac effects, increased risk of toxicity.
  • Other Local Anesthetics: Additive systemic toxicity if administered concurrently or sequentially.
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Moderate Interactions

  • Beta-blockers (e.g., Propranolol): May reduce hepatic blood flow, potentially decreasing mepivacaine clearance and increasing plasma levels.
  • Cimetidine: May inhibit hepatic metabolism of mepivacaine, increasing plasma levels.
  • Cholinesterase Inhibitors (e.g., Neostigmine, Pyridostigmine): May prolong neuromuscular blockade if mepivacaine is used in conjunction with neuromuscular blockers (though not a direct interaction with mepivacaine itself).
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Minor Interactions

  • Sedatives/Hypnotics/Opioids: Additive CNS depression if significant systemic absorption occurs.

Monitoring

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Baseline Monitoring

Allergy history

Rationale: To identify hypersensitivity to amide-type local anesthetics.

Timing: Prior to administration.

Vital Signs (HR, BP, RR)

Rationale: To establish baseline and detect early signs of systemic toxicity.

Timing: Prior to administration.

Patient's physical status (ASA classification)

Rationale: To assess overall health and risk for complications.

Timing: Prior to administration.

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Routine Monitoring

Vital Signs (HR, BP, RR)

Frequency: Every 5-15 minutes during and immediately after injection, then as clinically indicated.

Target: Within patient's normal limits.

Action Threshold: Significant deviations (e.g., bradycardia, hypotension, hypertension, tachypnea) or signs of CNS toxicity.

Level of consciousness/Neurological status

Frequency: Continuously during and immediately after injection.

Target: Alert and oriented.

Action Threshold: Dizziness, lightheadedness, tinnitus, perioral numbness, confusion, tremors, seizures.

Injection site for signs of local reaction

Frequency: Immediately after injection and periodically.

Target: Minimal swelling, redness.

Action Threshold: Excessive swelling, pain, signs of infection, or nerve injury.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus
  • Perioral numbness
  • Metallic taste
  • Blurred vision
  • Tremors
  • Muscle twitching
  • Seizures
  • Drowsiness
  • Unconsciousness
  • Respiratory depression
  • Bradycardia
  • Hypotension
  • Cardiac arrest

Special Patient Groups

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Pregnancy

Mepivacaine is Pregnancy Category C. Animal studies have shown adverse effects on the fetus at high doses. It crosses the placenta. Use only if the potential benefit justifies the potential risk to the fetus. Avoid paracervical block in obstetrics due to risk of fetal bradycardia and death.

Trimester-Specific Risks:

First Trimester: Limited data. Avoid if possible, or use lowest effective dose.
Second Trimester: Generally considered safer than first or third, but still Category C. Use with caution.
Third Trimester: Increased risk of fetal bradycardia and death, especially with paracervical block. Use with extreme caution and only when clearly indicated.
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Lactation

Mepivacaine is excreted into breast milk in small amounts (L3 - Moderately Safe). The amount ingested by the infant is generally considered too small to cause adverse effects. Caution is advised, especially with repeated doses or in premature infants.

Infant Risk: Low risk of adverse effects for the breastfed infant with single doses. Monitor infant for drowsiness or feeding difficulties.
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Pediatric Use

Dosing must be carefully calculated based on weight (mg/kg) and age. Children, especially younger ones, may be more susceptible to systemic toxicity. Use the lowest effective dose and monitor closely for signs of toxicity.

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Geriatric Use

Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced renal clearance of metabolites, and altered body composition. Consider reduced doses and monitor closely for adverse effects. Pre-existing cardiovascular disease may increase risk of cardiac complications.

Clinical Information

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Clinical Pearls

  • Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to systemic toxicity.
  • The addition of a vasoconstrictor (e.g., epinephrine) prolongs the duration of action and reduces systemic absorption, but Polocaine 1% is plain (without vasoconstrictor).
  • Mepivacaine has a slightly faster onset and shorter duration than lidocaine when used without a vasoconstrictor.
  • Systemic toxicity primarily affects the CNS (excitation followed by depression) and cardiovascular system (myocardial depression, vasodilation, arrhythmias).
  • Lipid emulsion therapy (lipid rescue) is an antidote for severe local anesthetic systemic toxicity (LAST).
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Alternative Therapies

  • Lidocaine (Xylocaine)
  • Bupivacaine (Marcaine, Sensorcaine)
  • Prilocaine (Citanest)
  • Articaine (Septocaine)
  • Ropivacaine (Naropin)
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Cost & Coverage

Average Cost: $10 - $50 per 50 mL vial (1% solution) per 50 mL vial
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans when administered in a clinical setting for a medical procedure.
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General Drug Facts

If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly; do not flush them down the toilet or pour them down the drain unless instructed to do so by a healthcare professional. If you are unsure about the correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek medical attention. Be prepared to provide information about the medication taken, the amount, and the time of ingestion.