Bupivacaine Hydrochloride + Dextrose

Introduction

Bupivacaine Hydrochloride + Dextrose is a combination medication used primarily as a spinal anesthetic. Bupivacaine is a long-acting local anesthetic that works by blocking nerve impulses to provide pain relief, while Dextrose acts as an osmotic agent to create a hyperbaric solution that facilitates the desired spread of the anesthetic in the cerebrospinal fluid (CSF) during spinal anesthesia.

Uses

This combination is primarily used for:

Spinal anesthesia during surgeries, such as lower abdominal, orthopedic, and urologic procedures.
Relief from labor pain in obstetric procedures (e.g., cesarean section).

Brand Name	Bupivacaine Hydrochloride + Dextrose
Type
Weight
Generic	Bupivacaine Hydrochloride + Dextrose
Manufacturer
Available in	English বাংলা

Mechanism of Action

Bupivacaine Hydrochloride: Bupivacaine works by inhibiting the influx of sodium ions through voltage-gated sodium channels in the neuronal cell membrane, thereby blocking the generation and conduction of nerve impulses. This action leads to loss of sensation in the targeted area.
Dextrose: The addition of Dextrose creates a hyperbaric solution, which helps ensure that the anesthetic stays localized to a specific area of the spinal cord, leading to more controlled and predictable anesthesia.

How Long Does It Take to Work?

The onset of spinal anesthesia with Bupivacaine Hydrochloride + Dextrose occurs within 5 to 10 minutes following administration. The duration of anesthesia can last between 90 and 180 minutes, depending on the dose and patient factors.

Absorption

Bupivacaine is administered intrathecally (into the spinal canal) and rapidly absorbed into the cerebrospinal fluid. The hyperbaric nature of the solution (due to Dextrose) controls its spread within the subarachnoid space.

Route of Elimination

Bupivacaine is metabolized primarily in the liver by cytochrome P450 enzymes and is excreted in the urine, with less than 5% excreted unchanged. Dextrose is metabolized in the body through glycolysis and is eventually converted into carbon dioxide and water.

Dosage

The following dosage recommendations should be regarded as a guide for use in the average adult:

Spinal anesthesia for surgery: 2-4 ml (10-20 mg Bupivacaine hydrochloride) The patient's physical status and concomitant medication should be considered when deciding the dose, and the lowest dose required for adequate anesthesia should be used. Duration varies with dose, while segmental spread may be difficult to predict, especially with the isobaric (plain) solution. The dose should be reduced in the elderly and in patients in the late stages of pregnancy.

Pediatrics: Bupivacaine may be used in children. One of the differences between small children and adults is a relatively high CSF volume in infants and neonates, requiring a relatively larger dose/kg to produce the same level of block as compared to adults.

<5 kg: 0.40-0.50 mg/kg
5 to 15 kg: 0.30-0.40 mg/kg
15 to 40 kg: 0.25-0.30 mg/kg

The dose depends on the type and duration of the procedure:

Spinal anesthesia for surgery: Typical doses range from 7.5 mg to 15 mg of Bupivacaine, depending on the type of surgery and the patient's characteristics.
Obstetric use (e.g., cesarean section): Doses may range from 10 mg to 12.5 mg intrathecally.

Dose adjustments should be made based on the patient's body weight, medical condition, and response to the anesthetic.

Administration

The combination is administered as a single injection into the subarachnoid space (intrathecal injection) by a trained healthcare professional. It is usually given at the L2-L3, L3-L4, or L4-L5 level of the spine.

Side Effects

Common side effects include:

Hypotension
Nausea and vomiting
Headache (post-dural puncture headache)
Back pain
Shivering

Serious side effects may include:

Cardiac arrest (in rare cases)
Severe hypotension
Respiratory depression
Neurotoxicity

Toxicity

Toxic effects of Bupivacaine include central nervous system toxicity (e.g., seizures, confusion, or drowsiness) and cardiovascular toxicity (e.g., arrhythmias or cardiac arrest). Dextrose is generally well-tolerated, but overdose may lead to hyperglycemia. In case of Bupivacaine toxicity, supportive measures like oxygen, intravenous fluids, and, in severe cases, lipid emulsion therapy can be used.

Precautions

Should be used with caution in patients with cardiovascular disease, as Bupivacaine can cause severe hypotension or bradycardia.
Monitor for signs of central nervous system toxicity, particularly in elderly patients or those with hepatic impairment.
Not recommended for use in patients with coagulopathy or infections at the site of injection.

Interaction

Other local anesthetics: Co-administration with other local anesthetics increases the risk of systemic toxicity.
Beta-blockers: May enhance the hypotensive effects of Bupivacaine.
Antiarrhythmic drugs (e.g., amiodarone): Concurrent use may increase the risk of cardiotoxicity.

Disease Interaction

Patients with cardiovascular disease may be at increased risk for bradycardia and hypotension.
Patients with liver disease may have impaired metabolism of Bupivacaine, leading to toxicity.
Not recommended in patients with neurological diseases, as it may exacerbate symptoms.

Drug Interaction

Potential drug interactions include:

Opioids: Co-administration may enhance the analgesic effects but also increases the risk of respiratory depression.
Monoamine oxidase inhibitors (MAOIs): Increased risk of hypotension.

Food Interactions

No significant food interactions are reported with Bupivacaine and Dextrose.

Pregnancy Use

Bupivacaine is classified as a Category C drug for pregnancy, meaning animal studies have shown adverse effects, but there are no well-controlled human studies. It should be used only if the potential benefits justify the risks to the fetus. It is commonly used during cesarean sections with careful monitoring.

Lactation Use

Bupivacaine is excreted in breast milk in very small amounts. It is considered compatible with breastfeeding when used at low doses, such as those used in spinal anesthesia.

Acute Overdose

Acute overdose of Bupivacaine may lead to CNS and cardiovascular toxicity, including seizures, coma, hypotension, and cardiac arrest. Immediate treatment includes supportive measures, such as airway management, oxygenation, and intravenous fluids. Lipid emulsion therapy is recommended in cases of severe toxicity.

Contraindication

This combination drug is contraindicated in patients with:

Hypersensitivity to Bupivacaine, Dextrose, or other local anesthetics of the amide type.
Severe shock or heart block.
Severe coagulation disorders or infection at the injection site.

Use Direction

Administered only by healthcare professionals via intrathecal injection. The patient should be positioned appropriately, and the dose should be administered slowly and carefully into the subarachnoid space. The patient's vital signs, including heart rate and blood pressure, should be continuously monitored during the procedure.

Storage Conditions

Store at controlled room temperature, 20°C to 25°C (68°F to 77°F). Protect from light and freezing. Keep in a secure location out of the reach of children.

Volume of Distribution

Bupivacaine has a moderate volume of distribution of approximately 72 liters, indicating distribution into tissues. The distribution of Dextrose is widespread throughout body fluids.

Half Life

Bupivacaine has a half-life of approximately 2.7 to 3.5 hours after intrathecal administration. Dextrose is rapidly metabolized and does not contribute significantly to systemic effects after administration.

Clearance

The clearance of Bupivacaine is primarily hepatic, with a clearance rate of around 0.47 L/min. Dextrose is metabolized into water and carbon dioxide and is cleared through normal metabolic processes.

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