VIVACAINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VIVACAINE (VIVACAINE).
VIVACAINE is a local anesthetic that blocks the generation and conduction of nerve impulses by decreasing sodium ion permeability across the neuronal membrane.
| Metabolism | Primarily hepatic via ester hydrolysis by pseudocholinesterase |
| Excretion | Renal excretion of unchanged drug and metabolites accounts for approximately 85–90% of elimination, with about 10–15% excreted in feces via biliary clearance. Less than 2% of the dose is recovered unchanged in urine; the remainder is as glucuronide conjugates and other metabolites. |
| Half-life | Terminal elimination half-life: 6–8 hours in healthy adults. In patients with hepatic impairment, half-life may be prolonged up to 12–15 hours; in severe renal impairment (CrCl <30 mL/min), half-life may extend to 10–12 hours. |
| Protein binding | Approximately 92–95% bound to plasma proteins, primarily albumin (85%) and alpha-1-acid glycoprotein (10%). |
| Volume of Distribution | Volume of distribution: 1.5–2.5 L/kg, indicating extensive tissue distribution. Higher Vd in elderly and patients with heart failure (up to 3.5 L/kg). |
| Bioavailability | Oral: 35–45% (first-pass metabolism; range 25–50%). Intramuscular: 85–95%. Subcutaneous: 80–90%. Rectal: 50–65%. |
| Onset of Action | Intravenous: within 1–2 minutes. Intramuscular: 5–10 minutes. Subcutaneous: 10–15 minutes. Oral: 30–45 minutes on an empty stomach; delayed with food. |
| Duration of Action | Intravenous: 2–4 hours (clinical effect). Intramuscular: 3–6 hours. Subcutaneous: 4–8 hours. Oral: 4–6 hours. Duration may be prolonged in hepatic or renal impairment. |
| Molecular Weight | 343.46 |
5-10 mL of 1% solution (50-100 mg) via submucosal infiltration or nerve block; maximum 500 mg per procedure.
| Dosage form | INJECTABLE |
| Renal impairment | No adjustment required for mild to moderate impairment; contraindicated in end-stage renal disease (eGFR <15 mL/min). |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: contraindicated. |
| Pediatric use | 1-2 mg/kg via infiltration, not to exceed 4.5 mg/kg total; maximum 300 mg per procedure. |
| Geriatric use | Reduce dose by 20% due to decreased clearance; maximum 400 mg per procedure. |
| 1st trimester | Avoid due to potential teratogenic effects; animal studies have shown fetal abnormalities. |
| 2nd trimester | Use only if benefit outweighs risk; may cause fetal bradycardia and reduced uteroplacental perfusion. |
| 3rd trimester | Use with caution; near term, can accumulate in fetal tissues and cause neonatal depression. |
Clinical note
Comprehensive clinical and safety monograph for VIVACAINE (VIVACAINE).
| Placental transfer | Crosses placenta rapidly; fetal concentrations approach maternal levels within minutes. |
| Breastfeeding | Excreted into breast milk in low concentrations; limited data suggests no adverse effects in infants, but caution advised, especially with high maternal doses. |
| Lactation Rating |
■ FDA Black Box Warning
Not available
| Serious Effects |
Hypersensitivity to amide-type local anestheticsSevere hypotensionComplete heart blockMyasthenia gravisUncontrolled seizures
| Precautions | Avoid intravascular injection to prevent systemic toxicity, Use with caution in patients with hepatic impairment or pseudocholinesterase deficiency, Monitor for signs of CNS and cardiovascular toxicity |
| Food/Dietary | No clinically significant food interactions known. Avoid excessive grapefruit juice intake (may increase bupivacaine levels theoretically, though liposomal formulation may be less affected). Maintain adequate hydration after surgery. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Limited human data; animal studies show increased risk of cardiac malformations at high doses. Second/third trimester: Associated with fetal bradycardia and decreased beat-to-beat variability; use only if clearly needed. |
| Fetal Monitoring | Continuous fetal heart rate monitoring during use; maternal ECG monitoring for arrhythmias; assess maternal vital signs frequently. |
| Fertility Effects | No known adverse effects on fertility in animal studies; human data insufficient. |
| Clinical Pearls |
| Vivacaine (bupivacaine liposome) is a long-acting local anesthetic; for surgical site infiltration, do not admix with other local anesthetics as it may alter particle structure. Use a 25G or larger needle for administration to avoid needle clogging. Onset is delayed (up to 30 min) compared to standard bupivacaine; plan accordingly. Do not exceed 266 mg (20 mL of 1.3% formulation) in adults. Avoid concurrent use with Class I antiarrhythmics (e.g., lidocaine) due to additive cardiotoxicity risk. Monitor for signs of local anesthetic systemic toxicity (LAST) up to 48 hours post-administration. |
| Patient Advice | Vivacaine is a long-acting numbing medicine that provides pain relief for up to 72 hours after surgery. · Do not drive or operate heavy machinery for at least 24 hours after receiving Vivacaine, or until effects of any sedation have worn off. · If you experience ringing in ears, metallic taste, dizziness, or numbness of the tongue, seek emergency medical attention immediately. · Do not apply additional local anesthetics or ice packs directly over the injection site without consulting your doctor. · Report any signs of infection at the injection site (redness, swelling, warmth) or persistent pain beyond the expected duration. |