Marcaine 0.25% Inj, 50ml

Bupivacaine is an amide-type local anesthetic. It reversibly blocks the initiation and conduction of nerve impulses by decreasing the permeability of the neuronal membrane to sodium ions. This action stabilizes the membrane and inhibits depolarization, preventing the propagation of the action potential.

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 experience any of the following symptoms, contact your doctor or seek medical attention immediately:

Allergic Reaction: 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, or swelling of the mouth, face, lips, tongue, or throat.
Acidosis (Too Much Acid in the Blood): Confusion, fast breathing, fast heartbeat, irregular heartbeat, severe stomach pain, upset stomach, vomiting, excessive sleepiness, shortness of breath, or feeling extremely tired or weak.
Methemoglobinemia: Blue or gray discoloration of the lips, nails, or skin, irregular heartbeat, seizures, severe dizziness or fainting, severe headache, excessive sleepiness, feeling tired or weak, or shortness of breath. This rare condition can be life-threatening if left untreated.
Cardiovascular Issues: Fast, slow, or abnormal heartbeat, chest pain or pressure, dizziness or fainting, lightheadedness, sleepiness, confusion, or blurred vision.
Neurological Symptoms: Change in balance, restlessness, anxiety, change in speech, shakiness, twitching, ringing in the ears, trouble breathing, slow breathing, or shallow breathing, seizures, numbness or tingling in the mouth, metallic taste.
Gastrointestinal Issues: Severe stomach upset or vomiting, feeling hot or cold, nervousness, excitability, sneezing, excessive sweating.
* Spinal-Related Symptoms: Difficulty urinating, loss of bladder or bowel control, erectile dysfunction, long-lasting burning, numbness, tingling, or paralysis in the lower half of the body, backache, fever or chills, stiff neck, sensitivity to bright lights.

Other Possible Side Effects

As with any medication, you may experience side effects. While many people do not experience any side effects or only minor ones, it is essential to contact your doctor if you have any symptoms that bother you or persist. This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor.

Reporting Side Effects

You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can also provide guidance on managing side effects and offer medical advice.

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.
Certain health conditions, including:
+ Bleeding disorders
+ Abnormal heart rhythms
+ Blood infections or infections at the site where the medication will be administered
+ Low blood pressure
* If you are using or plan to use another medication similar to this one. If you are unsure, consult your doctor or pharmacist.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dosage of any medication without first consulting your doctor.

Important Warnings and Cautions

General Precautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Until the effects of this drug have worn off and you feel fully alert, avoid driving and other activities that require your full attention.

Risk of Methemoglobinemia

This medication can cause a severe blood disorder called methemoglobinemia. Your risk may be higher if you have glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. Additionally, the risk may increase when taking certain other medications or in infants under 6 months of age. If you have a history of methemoglobinemia, inform your doctor.

Special Considerations

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Not all products are suitable for children, so consult with your doctor before use. If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks with your doctor to ensure the best outcome for you and your baby.

Mouth and Throat Precautions

When using this medication for mouth-related procedures, do not eat until the numbness has worn off, as you may accidentally bite your tongue.

Spinal Administration Precautions

After spinal administration of this medication, you may experience temporary loss of feeling and motor function in the lower half of your body. Wait until these effects have resolved before attempting to get out of bed or perform other activities.

Injection Precautions (Non-Spinal)

When this medication is administered via injection (other than spinal), you may experience temporary loss of feeling and motor function at the injection site.

• Other local anesthetics (additive systemic toxicity)
• Antiarrhythmics (e.g., Class I antiarrhythmics like mexiletine, lidocaine, tocainide - increased risk of cardiac depression/toxicity)
• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir) - potential for increased bupivacaine levels and toxicity.

• Opioids (synergistic analgesic effect, but increased risk of respiratory depression when used intrathecally/epidurally)
• Sedatives/Hypnotics (additive CNS depression)
• Neuromuscular blockers (prolongation of block, though less common with bupivacaine)
• Vasoconstrictors (e.g., epinephrine - prolongs duration of action, but also increases systemic absorption of bupivacaine if not used carefully)

• Lightheadedness
• Dizziness
• Tinnitus
• Metallic taste
• Numbness of tongue/lips (circumoral numbness)
• Visual disturbances (blurred vision, diplopia)
• Tremors
• Muscle twitching
• Seizures
• Drowsiness
• Unconsciousness
• Respiratory depression/arrest
• Bradycardia
• Hypotension
• Cardiac arrhythmias
• Cardiac arrest

Category C. Use only if the potential benefit justifies the potential risk to the fetus. Bupivacaine crosses the placenta. Fetal bradycardia and other adverse effects have been reported. The 0.75% concentration is contraindicated for obstetrical epidural anesthesia due to increased risk of cardiac arrest.

L2 (Safer). Bupivacaine is excreted into breast milk in small amounts. The amount ingested by the infant is very low and unlikely to cause adverse effects. Generally considered compatible with breastfeeding.

Use with caution, especially in infants and young children, due to increased susceptibility to systemic toxicity and immature metabolic pathways. Dosing must be carefully calculated on a mg/kg basis, and maximum doses should not be exceeded. Not recommended for epidural block in children under 12 years due to higher risk of toxicity.

Use with caution. Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced renal clearance of metabolites, and altered body composition. Consider lower doses and slower administration rates. Monitor closely for adverse effects.

• Always aspirate before injection to avoid inadvertent intravascular administration, which can lead to severe systemic toxicity, including cardiac arrest.
• Bupivacaine has a relatively long duration of action compared to other local anesthetics like lidocaine.
• Cardiac toxicity is a major concern, especially with higher concentrations or accidental intravascular injection. Lipid emulsion (Intralipid) should be readily available for treatment of severe local anesthetic systemic toxicity (LAST).
• The 0.75% concentration is contraindicated for obstetrical epidural anesthesia due to increased risk of cardiac arrest.
• Onset of action is slower than lidocaine, but duration is longer.
• Monitor for signs of CNS toxicity (e.g., circumoral numbness, tinnitus, lightheadedness, seizures) and cardiovascular toxicity (e.g., bradycardia, hypotension, arrhythmias).

• Lidocaine (shorter acting, less cardiotoxic)
• Ropivacaine (similar to bupivacaine, but less cardiotoxic)
• Levobupivacaine (S-enantiomer of bupivacaine, potentially less cardiotoxic)
• Mepivacaine
• Chloroprocaine (ester-type, very short acting)

If your symptoms or health problems persist or worsen, 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 for someone else. 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 emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.