Ultracaine Heavy

Bupivacaine Hydrochloride + Dextrose is primarily indicated for use in spinal anesthesia. Specific approved and clinically accepted indications include:

• Surgical Anesthesia via Subarachnoid Block, including:
• Cesarean section
• Urologic procedures
• Lower abdominal surgeries
• Lower limb orthopedic surgeries
• Gynecological procedures
• Pain Management (Off-label but clinically practiced):
• Management of acute surgical pain in lower body surgeries
• Postoperative pain control through intrathecal administration

This combination is particularly preferred when hyperbaric spinal anesthesia is required due to the presence of dextrose which modifies the solution’s density for controlled spread in the subarachnoid space.

Route: Intrathecal (spinal) injection only.

Adult Dosing (for spinal anesthesia):

• Usual concentration: Bupivacaine Hydrochloride 0.5% with 8% Dextrose
• Dose range: 1.5 mL to 4 mL (7.5–20 mg bupivacaine), depending on:
• Type of surgery
• Required level and duration of anesthesia
• Patient height, weight, and position

Cesarean Section:

• 1.5 mL to 2.2 mL (7.5–11 mg) intrathecally injected

Elderly or Debilitated Patients:

• Start with reduced doses due to increased sensitivity to local anesthetics.

Pediatrics:

• Not routinely recommended; spinal anesthesia in pediatric patients should only be performed by trained specialists with adjusted dosages.

Hepatic or Renal Impairment:

• No specific dose adjustment necessary, but clinical caution and monitoring advised.

Administration Notes:

• Inject slowly over 10–15 seconds after proper CSF flow is confirmed.
• Patient should be in a lateral or sitting position.
• Do not use preservatives or mix with other agents in the syringe.

Bupivacaine Hydrochloride is an amide-type local anesthetic that acts by reversibly blocking sodium ion influx through voltage-gated sodium channels in neuronal membranes. This inhibition prevents initiation and propagation of nerve impulses. The addition of dextrose makes the solution hyperbaric, allowing it to settle predictably within the spinal canal under gravity, which aids in controlling the anesthetic level. The result is effective and region-specific sensory and motor blockade suitable for surgical procedures.

• Absorption: Following intrathecal administration, absorption into systemic circulation is slow and depends on dose and vascularity of the injection site.
• Distribution: Widely distributed, particularly in highly perfused organs. Crosses placenta and blood-brain barrier.
• Protein Binding: ~95% (mainly to alpha-1 acid glycoprotein)
• Metabolism: Hepatic metabolism via CYP3A4 and CYP1A2 enzymes.
• Elimination: Primarily renal; <5% excreted unchanged.
• Half-life: Approximately 2.7 hours after spinal administration.
• Onset: 3–8 minutes (intrathecal route)
• Duration of action: 90–150 minutes depending on dose and patient positioning.

• Pregnancy: Not assigned under FDA pregnancy categories. However, widely used for spinal anesthesia in cesarean section. No teratogenicity observed in human data when administered intrathecally.
• Lactation: Minimal systemic absorption after spinal use; negligible excretion into breast milk. Considered safe during breastfeeding.

Caution is advised during early pregnancy unless benefit outweighs risk.

• Primary Class: Local Anesthetic (Amide Type)
• Subclassification: Long-acting regional anesthetic
• Formulation Role: Hyperbaric spinal anesthetic (due to dextrose)

• Known hypersensitivity to bupivacaine, dextrose, or other amide-type local anesthetics
• Severe hypotension or hypovolemia
• Septicemia or local infection at the injection site
• Spinal deformities or pre-existing neurological disease complicating administration
• Patients with bleeding disorders or receiving anticoagulant therapy (risk of spinal hematoma)
• Obstetric patients with contraindications to regional anesthesia (e.g., fetal distress requiring general anesthesia)

• Hypotension and Bradycardia: May occur due to sympathetic blockade; preload with fluids and monitor hemodynamics.
• Total Spinal Anesthesia: Accidental overdose or rapid upward spread may cause respiratory paralysis and unconsciousness.
• Neurotoxicity: Risk of cauda equina syndrome if improperly dosed.
• Delayed recovery of bladder or bowel function: Monitor in elderly.
• High-risk groups: Elderly, hepatic dysfunction, cardiac conduction disorders.

Monitor for early signs of toxicity: tinnitus, metallic taste, numbness around mouth, or seizures.

Common:

• Hypotension
• Bradycardia
• Nausea
• Urinary retention
• Pruritus (itching)

Less Common:

• Back pain
• Shivering
• Headache (post-dural puncture)

Serious/Rare:

• Total spinal block with respiratory paralysis
• Cardiac arrest (especially with high doses)
• Seizures due to systemic toxicity
• Cauda equina syndrome
• Persistent neurological deficit (extremely rare)

• Other Local Anesthetics: Additive CNS and cardiac toxicity
• Class I Antiarrhythmics (e.g., lidocaine, mexiletine): Potentiated effects
• CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir): May reduce bupivacaine metabolism, increasing toxicity risk
• CNS Depressants: Enhanced sedative effects
• MAO Inhibitors & Tricyclic Antidepressants: May increase cardiovascular effects

No significant food or alcohol interaction reported with intrathecal use, but caution advised in all CNS depressant combinations.

• Recent anesthetic guidelines continue to recommend hyperbaric bupivacaine + dextrose as a first-line spinal anesthetic in cesarean sections and lower body surgeries.
• Updated WHO and ASA protocols emphasize minimum effective dosing and recommend positioning techniques (e.g., sitting or lateral) to control block spread.
• No new contraindications or black box warnings introduced in recent revisions.

• Store below 25°C in a light-resistant container
• Do not freeze
• Keep in the original ampoule until use
• Discard any unused portion after opening
• Use only clear, particle-free solutions
• Shelf life: As indicated by manufacturer; typically 24–36 months unopened