Polocaine 2% 1000mg/50ml Inj, 50ml
It is used to numb an area before a procedure.
Drug Class
Local Anesthetic
Pharmacologic Class
Amide-type Local Anesthetic; Sodium Channel Blocker
Pregnancy Category
Category C
FDA Approved
Jun 1960
DEA Schedule
Not Controlled
Overview
What is this medicine?
Mepivacaine is a medicine used to numb a specific area of your body to prevent pain during medical or dental procedures. It works by temporarily blocking nerve signals in the area where it's injected.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the instructions carefully. This medication is administered via injection.
Storage and Disposal
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 disposing of it.
Missed 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 determine when the medication is necessary and administer it accordingly.
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the instructions carefully. This medication is administered via injection.
Storage and Disposal
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 disposing of it.
Missed 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 determine when the medication is necessary and administer it accordingly.
Lifestyle & Tips
- Avoid eating or drinking until sensation returns to the numb area, especially in the mouth or throat, to prevent choking or biting your tongue/cheek.
- Be careful with activities that require fine motor skills or full sensation until the numbness wears off.
- Follow all post-procedure instructions from your healthcare provider.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Dosage varies significantly based on procedure, site of injection, and individual patient factors. Typically, the lowest effective dose is used.
Condition-Specific Dosing:
infiltration:
Up to 400 mg (20 mL of 2% solution) per single procedure, not to exceed 1000 mg/24 hours.
peripheralNerveBlock:
50-400 mg (2.5-20 mL of 2% solution) depending on the nerve block.
epiduralCaudalBlock:
150-300 mg (7.5-15 mL of 2% solution) for epidural; 75-150 mg (3.75-7.5 mL of 2% solution) for caudal.
dentalAnesthesia:
20-60 mg (1-3 mL of 2% solution) per injection site.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Maximum recommended dose is 5-6 mg/kg (0.25-0.3 mL/kg of 2% solution) not to exceed 400 mg in a single dose.
Adolescent:
Dosing similar to adult, based on weight and procedure, not to exceed 5-6 mg/kg or 400 mg per single dose.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, but use with caution.
Moderate:
No specific adjustment recommended, but use with caution.
Severe:
No specific adjustment recommended, but use with caution. Metabolites are renally excreted, so accumulation may occur.
Dialysis:
Consideration for accumulation of metabolites; use with caution.
Hepatic Impairment:
Mild:
Use with caution; consider lower doses.
Moderate:
Reduced doses may be necessary due to impaired metabolism. Monitor for signs of toxicity.
Severe:
Significant dose reduction is likely necessary. Contraindicated in severe hepatic disease due to risk of accumulation and toxicity.
Pharmacology
Mechanism of Action
Mepivacaine, an amide-type local anesthetic, stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of nerve impulses. It specifically blocks voltage-gated sodium channels, preventing the transient increase in permeability to sodium ions that is responsible for depolarization of the nerve membrane and subsequent action potential propagation.
Pharmacokinetics
Absorption:
Bioavailability:
Varies significantly based on site of administration (e.g., highly vascularized areas like intercostal blocks lead to faster absorption and higher peak plasma levels).
Tmax:
2-15 minutes (epidural), 10-45 minutes (peripheral nerve block), 30-60 minutes (infiltration).
FoodEffect:
Not applicable (parenteral administration).
Distribution:
Vd:
1.5 L/kg (adults), 1.1 L/kg (neonates).
ProteinBinding:
70-85% (primarily to alpha-1-acid glycoprotein).
CnssPenetration:
Yes (crosses blood-brain barrier).
Elimination:
HalfLife:
1.9 hours (adults), 3.2 hours (neonates).
Clearance:
Not readily available as a single rate, but primarily hepatic metabolism.
ExcretionRoute:
Renal (metabolites and unchanged drug).
Unchanged:
<5% (in urine).
Pharmacodynamics
OnsetOfAction:
2-7 minutes (rapid).
PeakEffect:
Varies with site of injection and concentration; generally within 15-30 minutes.
DurationOfAction:
1-3 hours (without vasoconstrictor); duration is shorter than bupivacaine but longer than lidocaine.
Safety & Warnings
BLACK BOX WARNING
Local anesthetics, including mepivacaine, can cause systemic toxicity, particularly if accidentally injected intravascularly. Severe adverse reactions, including seizures, respiratory depression, and cardiovascular collapse, can occur. Not for obstetric paracervical block due to reports of fetal bradycardia and death.
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
+ Abnormal heartbeat
+ Severe stomach pain, upset stomach, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling very 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
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling 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 stomach upset or vomiting
+ Feeling hot or cold
+ Sneezing
+ Excessive sweating
Additional Side Effects (Epidural Use)
If you are receiving this medication via epidural, you may also experience:
Erectile dysfunction
Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
Loss of bladder or bowel control
Urination difficulties
Headache
Backache
Fever or chills
Stiff neck
Sensitivity to light
Other Side Effects
As with any medication, you may experience side effects that are not severe but still bothersome. If you have any side effects that concern you or do not go away, contact your doctor for advice. Not all possible side effects are listed here. If you have questions or concerns about side effects, you can:
Contact your doctor for medical advice
Report side effects to the FDA at 1-800-332-1088
Report side effects online at https://www.fda.gov/medwatch
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
+ Abnormal heartbeat
+ Severe stomach pain, upset stomach, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling very 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
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling 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 stomach upset or vomiting
+ Feeling hot or cold
+ Sneezing
+ Excessive sweating
Additional Side Effects (Epidural Use)
If you are receiving this medication via epidural, you may also experience:
Erectile dysfunction
Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
Loss of bladder or bowel control
Urination difficulties
Headache
Backache
Fever or chills
Stiff neck
Sensitivity to light
Other Side Effects
As with any medication, you may experience side effects that are not severe but still bothersome. If you have any side effects that concern you or do not go away, contact your doctor for advice. Not all possible side effects are listed here. If you have questions or concerns about side effects, you can:
Contact your doctor for medical advice
Report side effects to the FDA at 1-800-332-1088
Report side effects online at https://www.fda.gov/medwatch
Seek Immediate Medical Attention If You Experience:
- Dizziness or lightheadedness
- Ringing in the ears (tinnitus)
- Numbness or tingling around the mouth (perioral numbness)
- Metallic taste in the mouth
- Blurred vision or double vision
- Tremors or muscle twitching
- Feeling anxious or restless
- Difficulty breathing
- Slow or irregular heartbeat
- Feeling faint or unusually tired
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.
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 they may affect the safety and efficacy of this medication.
To ensure your safety, it is crucial to:
Discuss all your medications and health problems with your doctor and pharmacist to verify that it is safe to take this medication in conjunction with your other treatments.
* Avoid starting, stopping, or changing the dose of any medication without first consulting your doctor. This precaution will help prevent potential interactions and adverse effects.
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.
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 they may affect the safety and efficacy of this medication.
To ensure your safety, it is crucial to:
Discuss all your medications and health problems with your doctor and pharmacist to verify that it is safe to take this medication in conjunction with your other treatments.
* Avoid starting, stopping, or changing the dose of any medication without first consulting your doctor. This precaution will help prevent potential interactions and adverse effects.
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, that you are using this drug.
Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with medications 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 (65 and older): Use this medication with caution, as you may be more susceptible to side effects.
Pregnancy and Breastfeeding
If you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Mouth and Numbing Effects
- 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 sensation returns.
Epidural Administration
After receiving this medication via epidural, you may experience temporary loss of sensation and motor function in the lower half of your body. Do not attempt to get out of bed or engage in any activities until your feeling and motor function have returned to normal.
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are using this drug.
Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with medications 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 (65 and older): Use this medication with caution, as you may be more susceptible to side effects.
Pregnancy and Breastfeeding
If you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Mouth and Numbing Effects
- 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 sensation returns.
Epidural Administration
After receiving this medication via epidural, you may experience temporary loss of sensation and motor function in the lower half of your body. Do not attempt to get out of bed or engage in any activities until your feeling and motor function have returned to normal.
Overdose Information
Overdose Symptoms:
- Severe dizziness or lightheadedness
- Seizures
- Unconsciousness
- Respiratory arrest (stopping breathing)
- Cardiac arrest (heart stops beating)
What to Do:
If you experience any severe symptoms after receiving this injection, seek immediate medical attention. Call 911 or your local emergency number. For general poison control, call 1-800-222-1222.
Drug Interactions
Major Interactions
- Other local anesthetics (additive systemic toxicity)
- Antiarrhythmics (e.g., Class I antiarrhythmics like tocainide, mexiletine; additive cardiac effects, increased risk of toxicity)
Moderate Interactions
- Opioids (increased risk of respiratory depression when used in epidural/spinal anesthesia)
- Sedatives/Hypnotics (additive CNS depression)
- Neuromuscular blockers (may prolong or enhance effect of depolarizing agents like succinylcholine, though less direct interaction than with ester-type LAs)
- Vasopressors (if mepivacaine formulation contains epinephrine, increased risk of hypertension and arrhythmias)
Monitoring
Baseline Monitoring
Patient history and physical examination
Rationale: To identify pre-existing conditions (e.g., cardiac, hepatic, renal disease, allergies) that may influence drug safety or efficacy.
Timing: Prior to administration.
Vital signs (heart rate, blood pressure, respiratory rate)
Rationale: To establish baseline and detect early signs of systemic toxicity or adverse reactions.
Timing: Prior to administration.
Allergy assessment
Rationale: To prevent hypersensitivity reactions.
Timing: Prior to administration.
Routine Monitoring
Vital signs (heart rate, blood pressure, respiratory rate)
Frequency: Continuously during and immediately after administration, then periodically as clinically indicated.
Target: Within patient's normal physiological range.
Action Threshold: Significant deviations (e.g., bradycardia, hypotension, hypertension, tachypnea, bradypnea) warrant immediate intervention.
Neurological status (CNS toxicity)
Frequency: Continuously during and immediately after administration, then periodically.
Target: Absence of symptoms like lightheadedness, dizziness, tinnitus, perioral numbness, metallic taste, blurred vision, tremors, muscle twitching, seizures.
Action Threshold: Any new or worsening CNS symptoms require immediate assessment and management (e.g., stopping injection, administering anticonvulsants).
Cardiovascular status (cardiac toxicity)
Frequency: Continuously during and immediately after administration, then periodically.
Target: Stable cardiac rhythm and function.
Action Threshold: Arrhythmias (e.g., bradycardia, ventricular fibrillation), hypotension, or cardiac arrest require immediate advanced cardiac life support.
Pain assessment
Frequency: During and after procedure.
Target: Adequate pain control.
Action Threshold: Inadequate analgesia may indicate improper injection technique or insufficient dose.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Perioral numbness
- Metallic taste
- Blurred vision
- Tremors
- Muscle twitching
- Seizures
- Drowsiness
- Unconsciousness
- Respiratory depression
- Bradycardia
- Hypotension
- Arrhythmias
- Cardiac arrest
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Not recommended for obstetric paracervical block due to risk of fetal bradycardia and death.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally avoided unless clearly needed.
Second Trimester:
Use with caution, lowest effective dose.
Third Trimester:
Use with caution, especially near term. Contraindicated for paracervical block.
Lactation
Mepivacaine is excreted in breast milk in small amounts. Generally considered compatible with breastfeeding, but caution is advised. Monitor infant for drowsiness or feeding difficulties.
Infant Risk:
Low risk of adverse effects, but observe for unusual drowsiness or changes in feeding patterns.
Pediatric Use
Dose carefully by weight (mg/kg) to avoid systemic toxicity. Children may be more susceptible to systemic toxicity. Not recommended for use in children under 3 years of age for certain procedures due to lack of data.
Geriatric Use
Reduced doses may be necessary due to decreased hepatic function, reduced renal clearance of metabolites, and increased sensitivity to systemic toxicity. Monitor closely for adverse effects.
Clinical Information
Clinical Pearls
- Mepivacaine is an amide-type local anesthetic, known for its rapid onset and intermediate duration of action.
- 2% mepivacaine provides a more profound and longer-lasting block than 1% mepivacaine.
- Plain mepivacaine (without epinephrine) is preferred in areas where vasoconstriction is undesirable (e.g., digits, penis, nose, ears) due to the risk of ischemia.
- Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to rapid systemic toxicity.
- Systemic toxicity primarily affects the CNS and cardiovascular system. Early signs of CNS toxicity (e.g., perioral numbness, tinnitus, lightheadedness) should prompt immediate cessation of injection and supportive care.
- Not recommended for intravenous regional anesthesia (Bier block) due to high risk of systemic toxicity if tourniquet fails.
- The maximum recommended dose should never be exceeded, and the lowest effective dose should always be used.
Alternative Therapies
- Lidocaine (another amide-type local anesthetic, similar onset, shorter duration)
- Bupivacaine (amide-type, slower onset, longer duration, higher cardiotoxicity risk)
- Ropivacaine (amide-type, similar to bupivacaine but less cardiotoxic)
- Articaine (amide-type, often used in dentistry, rapid onset, intermediate duration)
- Procaine (ester-type local anesthetic, shorter duration, higher allergy risk)
Cost & Coverage
Average Cost:
$10 - $50 per 50mL vial (2%)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (often covered under medical benefit for procedures)
General Drug Facts
If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed to someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.
Proper disposal of unused or expired medications is crucial. Do not dispose of them by flushing down the toilet or pouring down the drain unless specifically instructed to do so. If you are unsure about the correct disposal method, consult your pharmacist for advice. Many communities have drug take-back programs, which your pharmacist can help you locate.
Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.
Proper disposal of unused or expired medications is crucial. Do not dispose of them by flushing down the toilet or pouring down the drain unless specifically instructed to do so. If you are unsure about the correct disposal method, consult your pharmacist for advice. Many communities have drug take-back programs, which your pharmacist can help you locate.
Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.