Marcaine 0.75% Inj, 10ml

Bupivacaine, an amide-type local anesthetic, 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.

Serious Side Effects: Seek Medical Help Immediately

Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:

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
Abnormal heart rhythms, including fast, slow, or irregular heartbeat
Chest pain or pressure
Dizziness or fainting
Feeling lightheaded, sleepy, confused, or experiencing blurred vision
Balance problems
Restlessness
Anxiety
Changes in speech
Shakiness
Twitching
Ringing in the ears
Breathing difficulties, including slow or shallow breathing
Seizures
Numbness or tingling in the mouth
Metallic taste
Severe nausea or vomiting
Feeling extremely hot or cold
Feeling nervous and excitable
Sneezing
Excessive sweating
Spinal-related side effects, such as:
+ Difficulty urinating
+ Loss of bladder or bowel control
+ Erectile dysfunction
+ Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
+ Back pain
+ Fever or chills
+ Stiff neck
+ Sensitivity to bright lights

Other Side Effects

Like all medications, this drug can cause side effects, although not everyone will experience them. If you have any side effects that bother you or do not go away, contact your doctor for advice. Some common side effects may include:

Mild allergic reactions
Gastrointestinal symptoms
Fatigue
Headache
* Dizziness

Reporting Side Effects

If you experience any side effects, you can report them to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. You can also contact your doctor for medical advice about side effects.

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. Describe the allergic reaction you experienced, including the symptoms that occurred.
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 dose 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

Drugs like this one have been associated with a severe blood condition called methemoglobinemia. Your risk may be increased if you have glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. Additionally, the risk may be higher 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, planning to become pregnant, or breastfeeding, discuss the benefits and risks with your doctor to ensure the best outcome for you and your baby.

Mouth and Dental Considerations

While your mouth feels numb, avoid eating to prevent accidentally biting your tongue.

Spinal Administration

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

Injection (Non-Spinal)

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

• Intravenous regional anesthesia (Bier block) - due to high risk of systemic toxicity and cardiac arrest.
• Obstetrical paracervical block anesthesia (due to fetal bradycardia/death risk).
• 0.75% concentration for obstetrical epidural anesthesia (due to risk of refractory cardiac arrest).

• Other local anesthetics (e.g., lidocaine, ropivacaine): Additive systemic toxicity (CNS and cardiovascular).
• Class I antiarrhythmics (e.g., mexiletine, tocainide): Additive cardiac effects, increased risk of myocardial depression and arrhythmias.
• Antiarrhythmics (e.g., amiodarone, verapamil): May potentiate cardiac effects of bupivacaine.

• CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir): May increase bupivacaine plasma concentrations, though metabolism by CYP3A4 is minor.
• CNS depressants (e.g., opioids, benzodiazepines, sedatives): Additive CNS depression.
• Neuromuscular blocking agents: May prolong or enhance the effect of neuromuscular blockers.

• Not available

• Lightheadedness
• Dizziness
• Tinnitus (ringing in ears)
• Perioral numbness or tingling
• Metallic taste
• Blurred vision
• Tremors or muscle twitching
• Slurred speech
• Anxiety or restlessness
• Drowsiness
• Seizures
• Hypotension
• Bradycardia
• Arrhythmias
• Chest pain
• Shortness of breath

Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. The 0.75% concentration is contraindicated for obstetrical epidural anesthesia due to the risk of refractory cardiac arrest. Not for obstetrical paracervical block anesthesia due to risk of fetal bradycardia and death.

L3 (Moderately safe). Bupivacaine is excreted into breast milk in small amounts. Generally considered compatible with breastfeeding when used as a single dose for anesthesia. Monitor infant for drowsiness or feeding difficulties.

Use with extreme caution. Pediatric patients, especially infants and neonates, are more susceptible to systemic toxicity due to differences in pharmacokinetics (e.g., lower protein binding, immature hepatic metabolism). Lower concentrations (0.25%, 0.5%) and doses (max 2.5 mg/kg) are typically used. The 0.75% concentration is generally not recommended for pediatric use.

Geriatric patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced protein binding, and increased sensitivity. Reduced doses and careful monitoring are recommended. Start with lower doses and titrate slowly.

• Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to rapid systemic toxicity.
• Use the lowest effective concentration and dose to achieve the desired effect and minimize the risk of systemic toxicity.
• The 0.75% concentration carries a higher risk of cardiac toxicity and is specifically contraindicated for obstetrical epidural anesthesia and intravenous regional anesthesia (Bier block).
• Resuscitation equipment, including lipid emulsion therapy (Intralipid), should be immediately available whenever bupivacaine is administered, especially for high-risk procedures or doses.
• Monitor patients closely for signs of local anesthetic systemic toxicity (LAST), which can manifest as CNS symptoms (e.g., perioral numbness, tinnitus, seizures) or cardiovascular symptoms (e.g., hypotension, bradycardia, arrhythmias, cardiac arrest).
• The addition of epinephrine prolongs the duration of action and reduces systemic absorption, but also carries its own risks (e.g., vasoconstriction, cardiac effects).

• Lidocaine (shorter duration)
• Ropivacaine (less cardiotoxic than bupivacaine at equipotent doses)
• Levobupivacaine (less cardiotoxic than bupivacaine)
• Chloroprocaine (ester-type, very short duration)
• General anesthesia
• Regional anesthesia techniques using other agents

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. Additionally, some medications may come with a separate 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 it occurred.