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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VIVACAINE (VIVACAINE).
| Breastfeeding | Excreted in breast milk in low amounts (M/P ratio ~0.5). Considered compatible with breastfeeding; monitor infant for bradycardia and irritability. |
| 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 |
■ FDA Black Box Warning
Not available
| Serious Effects |
["Known hypersensitivity to ester-type anesthetics","Severe hypotension","Myasthenia gravis","Third-degree heart block"]
| 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"] |
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| 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. |