MARCAINE HYDROCHLORIDE W/ EPINEPHRINE PRESERVATIVE FREE
Clinical safety rating: safe
Beta-blockers may antagonize cardiac effects and cause severe hypertension Can cause angina and arrhythmias in patients with heart disease.
Bupivacaine blocks sodium ion channels on the neuronal membrane, inhibiting depolarization and conduction of nerve impulses. Epinephrine causes local vasoconstriction, delaying absorption and prolonging anesthetic effect.
| Metabolism | Bupivacaine is primarily metabolized by the liver via N-dealkylation, hydroxylation, and conjugation, mediated by CYP3A4 and CYP1A2. Epinephrine is metabolized by COMT and MAO. |
| Excretion | Primarily hepatic metabolism via CYP3A4 and amide hydrolysis; <5% excreted unchanged in urine. Biliary excretion accounts for <2% of total elimination. |
| Half-life | Terminal half-life of bupivacaine is 2.7–4.2 hours in adults; prolonged to 8–12 hours in neonates and patients with hepatic impairment. |
| Protein binding | Approximately 95% bound, primarily to alpha-1-acid glycoprotein (AAG) and albumin. |
| Volume of Distribution | Vd: 0.7–1.5 L/kg in adults; reflects extensive tissue distribution, including rapid uptake into highly perfused organs. |
| Bioavailability | Epidural: near 100%; peripheral nerve block: 80–100%; subcutaneous: 70–80% (enhanced by epinephrine). |
| Onset of Action | Epidural: 5–15 minutes; peripheral nerve block: 15–30 minutes; local infiltration: 2–10 minutes. |
| Duration of Action | Epidural: 2–4 hours (prolonged by epinephrine to 3–6 hours); peripheral nerve block: 3–8 hours (with epinephrine: 6–12 hours); local infiltration: 1–3 hours. |
Local infiltration: up to 30 mL of 0.25% (75 mg) or 0.5% (150 mg) solution. Epidural (lumbar): 10-20 mL of 0.5% (50-100 mg) with 1:200,000 epinephrine, repeated every 1.5-3 hours as needed. Maximum single dose: 225 mg (with epinephrine 1:200,000).
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended for mild-to-moderate renal impairment. Use with caution in severe renal impairment (eGFR <30 mL/min/1.73m²) due to potential accumulation of metabolites; consider reducing dose and monitoring for toxicity. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 25-50%. Child-Pugh Class C: avoid use; if necessary, use extreme caution with 50% reduction and close monitoring. |
| Pediatric use | Dose based on weight and procedure. Maximum dose: 2-2.5 mg/kg (with epinephrine 1:200,000). Example: for caudal epidural, 1-2 mg/kg of 0.25% solution. Not recommended for children under 12 years for epidural anesthesia. |
| Geriatric use | Reduce doses by 20-30% due to decreased clearance and increased sensitivity to local anesthetics. Titrate slowly; monitor for hypotension and neurologic symptoms. Maximum single dose: 150 mg (with epinephrine 1:200,000). |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Beta-blockers may antagonize cardiac effects and cause severe hypertension Can cause angina and arrhythmias in patients with heart disease.
| FDA category | Animal |
| Breastfeeding | Bupivacaine is excreted into human breast milk in small amounts. The milk-to-plasma (M/P) ratio is approximately 0.3. The epinephrine is poorly absorbed orally and rapidly metabolized. The American Academy of Pediatrics considers the combination compatible with breastfeeding. Caution is advised in preterm or low-birth-weight infants due to potential accumulation. |
| Teratogenic Risk |
■ FDA Black Box Warning
Not for use in obstetrical paracervical block anesthesia (fetal bradycardia and death). Risk of cardiotoxicity and CNS toxicity with unintentional intravascular injection or overdose. Use only with resuscitative equipment available.
| Common Effects | cardiac arrest |
| Serious Effects |
Hypersensitivity to bupivacaine, epinephrine, or amide-type anesthetics. Severe hypotension, shock, or AV block (for epidural). Do not use in paracervical block (obstetric). Concurrent use with halogenated hydrocarbons (risk of arrhythmia). Avoid in patients with pheochromocytoma or severe peripheral vascular disease.
| Precautions | Risk of systemic toxicity (cardiac arrest, seizures) from intravascular injection or overdose; use test dose and incremental injection. Caution in hepatic impairment, severe hypertension, cardiac disease, or concurrent use of MAOIs, tricyclic antidepressants, or beta-blockers. Avoid in patients with acidosis, hypoxia, or hypotension. |
Loading safety data…
| Bupivacaine with epinephrine is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown adverse effects on fetal development at high doses. In the first trimester, risk is theoretical; however, the epinephrine component may reduce uteroplacental blood flow. In the second and third trimesters, use may cause fetal bradycardia and hypoxia due to epinephrine-induced vasoconstriction. Avoid use in paracervical block (first trimester) as it has been associated with fetal bradycardia. |
| Fetal Monitoring | Continuous electronic fetal monitoring is recommended when used for labor analgesia. Monitor maternal blood pressure and heart rate closely due to potential for hypotension and bradycardia. Assess for signs of systemic toxicity (e.g., perioral numbness, metallic taste, seizures, CNS depression). Epidural top-ups should be administered with careful aspiration to avoid intravascular injection. |
| Fertility Effects | No specific studies on fertility effects in humans. Animal studies have not reported adverse effects on fertility. However, epinephrine may theoretically impair uterine blood flow, potentially affecting implantation if used during early pregnancy. No significant impacts on male or female fertility are documented. |