LIDOCAINE HYDROCHLORIDE 0.4% IN DEXTROSE 5% IN PLASTIC CONTAINER
Clinical safety rating: safe
Beta-blockers may increase the risk of lidocaine toxicity Can cause CNS toxicity (seizures) and cardiovascular collapse.
Lidocaine is a sodium channel blocker that inhibits depolarization of cardiac myocytes and nerve axons by binding to voltage-gated sodium channels and stabilizing the neuronal membrane, thereby preventing the propagation of action potentials.
| Metabolism | Primarily hepatic metabolism via cytochrome P450 (CYP1A2 and CYP3A4) to active metabolites (monoethylglycinexylidide [MEGX] and glycinexylidide [GX]), which may contribute to toxicity. Less than 10% excreted unchanged in urine. |
| Excretion | Renal excretion of unchanged drug and metabolites; <10% unchanged in urine, >90% as metabolites (primarily monoethylglycinexylidide and glycinexylidide). Biliary/fecal elimination minimal (<1%). |
| Half-life | Terminal elimination half-life approximately 1.5-2 hours after bolus, prolonged to 2-4 hours in heart failure or hepatic impairment; continuous infusion may show context-sensitive half-life. |
| Protein binding | Approximately 60-80% bound primarily to alpha-1-acid glycoprotein (AAG), with less binding to albumin; binding is concentration-dependent and decreased in acute phase reactions. |
| Volume of Distribution | Steady-state volume of distribution (Vdss) approximately 0.9-1.3 L/kg in healthy adults; increased in heart failure and cirrhosis, decreased in elderly; reflects extensive tissue binding. |
| Bioavailability | Oral: low and erratic (<35%) due to extensive first-pass hepatic metabolism; parenteral routes (IV, epidural, spinal, peripheral nerve): 100% bioavailability. |
| Onset of Action | Intravenous: rapid (45-90 seconds); epidural: 5-15 minutes; peripheral nerve block: 4-20 minutes depending on site and concentration. |
| Duration of Action | Intravenous bolus: 10-20 minutes (anesthetic effect) due to rapid redistribution; epidural: 60-90 minutes (with epinephrine up to 120 minutes); peripheral nerve block: 30-120 minutes; continuous infusion requires dose adjustment. |
| Molecular Weight | 270.8 |
Intravenous infusion: 1-4 mg/min (20-50 mcg/kg/min) for cardiac arrhythmias. Bolus: 1-1.5 mg/kg IV, then infusion.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment; monitor for toxicity in severe impairment. |
| Liver impairment | Child-Pugh A and B: Reduce dose by 50%; Child-Pugh C: Reduce by 75% or avoid. |
| Pediatric use | Bolus: 1-1.5 mg/kg IV, repeat 0.5-1 mg/kg after 5-10 min if needed. Infusion: 20-50 mcg/kg/min. |
| Geriatric use | Reduce dose by 50% due to decreased clearance; monitor for CNS toxicity. |
| 1st trimester | Lidocaine crosses the placenta. Animal studies have not demonstrated fetal harm. No well-controlled human studies in first trimester. Use only if clearly needed. |
| 2nd trimester | Lidocaine use in second trimester is generally considered safe when indicated. Monitor for maternal toxicity which may affect fetus. |
| 3rd trimester | Lidocaine can accumulate in fetal tissues with high fetal exposure. May cause fetal bradycardia or CNS depression if high maternal levels. Use lowest effective dose for shortest duration. |
Clinical note
Beta-blockers may increase the risk of lidocaine toxicity Can cause CNS toxicity (seizures) and cardiovascular collapse.
| FDA category | Animal |
| Placental transfer | Lidocaine crosses the placenta by passive diffusion. Fetal/maternal ratio ranges from 0.5 to 0.7. Fetal elimination is slower due to immature hepatic metabolism. |
■ FDA Black Box Warning
Lidocaine should not be used for the treatment of atrial fibrillation or atrial flutter with a rapid ventricular rate, as it may increase the ventricular rate.
| Common Effects | ventricular arrhythmias |
| Serious Effects |
Known hypersensitivity to lidocaine or amide-type local anestheticsSevere heart block (second or third degree) without pacemakerAdams-Stokes syndromeWolff-Parkinson-White syndrome (when used intravenously for arrhythmia)Severe hypotension or cardiogenic shock (when used as antiarrhythmic)Hyperbaric preparations (lidocaine in dextrose) contraindicated for spinal anesthesia in patients with spinal deformities or infection at injection site
| Precautions | Risk of central nervous system toxicity (seizures, respiratory depression) at high doses; cardiac toxicity (bradycardia, hypotension, cardiac arrest) in patients with heart failure or liver disease; caution in patients with severe hepatic impairment, heart failure, or renal impairment; dose adjustment required in elderly and patients with low cardiac output; monitor ECG and vital signs during infusion. |
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| Breastfeeding | Lidocaine is excreted into breast milk in small amounts (milk:plasma ratio ~0.4). Oral bioavailability in infant is low. Consider risk of infant exposure if high maternal doses or prolonged infusion. Use with caution. |
| Lactation Rating | L2 (Probably Compatible) |
| Teratogenic Risk | Lidocaine is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal harm, but no adequate controlled studies in pregnant women exist. In the first trimester, lidocaine crosses the placenta; however, no teratogenic effects have been consistently reported. During the second and third trimesters, lidocaine can cause fetal bradycardia and central nervous system depression if high maternal serum levels occur, particularly with repeated large doses. Paracervical block anesthesia in the second trimester has been associated with fetal bradycardia and acidosis. |
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and ECG for signs of lidocaine toxicity (e.g., hypotension, arrhythmias). Fetal heart rate monitoring is recommended when lidocaine is used for regional anesthesia during labor and delivery, especially with paracervical block, due to risk of fetal bradycardia. Assess for signs of CNS toxicity in mother (drowsiness, confusion, seizures). |
| Fertility Effects | Lidocaine has no known direct effects on human fertility. Animal studies have not shown impaired fertility at clinically relevant doses. No specific data on effects on gamete function or conception rates. |
| Food/Dietary | No known food interactions specific to lidocaine; however, the dextrose component may affect blood glucose levels in diabetic patients. Monitor blood glucose closely. |
| Clinical Pearls | Lidocaine hydrochloride 0.4% in dextrose 5% is typically used for continuous intravenous infusion for ventricular arrhythmias. It is contraindicated in patients with severe heart block or Adams-Stokes syndrome. Reduce dose in patients with hepatic impairment or heart failure. Monitor for CNS toxicity (e.g., seizures, confusion) and cardiac effects (e.g., bradycardia, hypotension). Do not use solutions containing preservatives for epidural or spinal anesthesia. |
| Patient Advice | This medication is given intravenously to treat abnormal heart rhythms. · Report any dizziness, confusion, ringing in ears, or twitching immediately. · Avoid sudden position changes to prevent dizziness from low blood pressure. · Do not stop this medication abruptly without consulting your doctor. |