NESACAINE-MPF
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NESACAINE-MPF (NESACAINE-MPF).
Nesacaine-MPF (chloroprocaine) is an ester-type local anesthetic that stabilizes neuronal membranes by inhibiting sodium ion influx, thereby blocking impulse conduction in nerve fibers.
| Metabolism | Hydrolyzed by plasma pseudocholinesterase (butyrylcholinesterase) to 2-chloro-4-aminobenzoic acid and diethylaminoethanol. |
| Excretion | Renal excretion of metabolites; <10% unchanged drug. Biliary/fecal elimination minor. |
| Half-life | Terminal half-life: 3-4 hours (adults); prolonged in hepatic or renal impairment. |
| Protein binding | 55-70% bound to alpha-1-acid glycoprotein and albumin. |
| Volume of Distribution | Vd: 1.3-1.5 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Not applicable; administered parenterally. Oral bioavailability negligible due to first-pass metabolism. |
| Onset of Action | Epidural: 5-15 min; Caudal: 5-10 min; Peripheral nerve block: 10-20 min. |
| Duration of Action | Epidural: 60-90 min; with epinephrine: 90-120 min. Duration is dose-dependent. |
1% solution: 2.5-30 mL (25-300 mg) subcutaneously or locally; maximum 30 mL per dose. 2% solution: 1.25-15 mL (25-300 mg) subcutaneously or locally; maximum 15 mL per dose.
| Dosage form | INJECTABLE |
| Renal impairment | No specific adjustment recommended; use with caution in severe renal impairment due to potential metabolite accumulation. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50%. Child-Pugh Class C: contraindicated. |
| Pediatric use | Weight-based: 1% solution up to 4.5 mg/kg subcutaneously or locally; 2% solution up to 4.5 mg/kg subcutaneously or locally. Maximum single dose: weight-dependent but not to exceed adult max. |
| Geriatric use | Lower doses (e.g., 50% of standard) due to increased sensitivity and reduced clearance; monitor for CNS and cardiovascular effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for NESACAINE-MPF (NESACAINE-MPF).
| Breastfeeding | Excreted in breast milk in trace amounts. M/P ratio unknown. Considered compatible with breastfeeding due to short half-life and low oral bioavailability. Monitor infant for local anesthetic toxicity. |
| Teratogenic Risk | Nesacaine-MPF (chloroprocaine) is a local anesthetic. No well-controlled studies in pregnant women. Animal studies have not shown fetal harm. Caution in first trimester. Risk of fetal bradycardia and acidosis if used in paracervical block during second trimester. Third trimester use may cause fetal heart rate changes. |
■ FDA Black Box Warning
Not for use in patients with known hypersensitivity to ester-type local anesthetics or to para-aminobenzoic acid (PABA). Avoid intravascular injection; test dose recommended before administration of full dose for epidural anesthesia.
| Serious Effects |
Hypersensitivity to ester-type local anesthetics or PABA, severe hypertension, untreated hypovolemia, coagulopathy, infection at injection site, and neurological disorders (e.g., multiple sclerosis, spinal stenosis) for neuraxial use.
| Precautions | Risk of central nervous system toxicity and cardiotoxicity with inadvertent intravascular injection or overdose. Use with caution in patients with impaired cardiovascular function, hepatic disease, or pseudocholinesterase deficiency. May cause methemoglobinemia; risk increased with concurrent use of oxidizing agents. |
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| Fetal Monitoring |
| Monitor maternal vital signs, fetal heart rate, and uterine activity. Assess for signs of systemic toxicity (e.g., CNS, cardiovascular). Epidural test dose recommended. Continuously monitor during anesthesia. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at clinical doses. |