LIDOCAINE HYDROCHLORIDE 0.2% AND 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 stabilizes neuronal membranes by inhibiting the ionic fluxes required for initiation and conduction of impulses, thereby producing local anesthesia. Dextrose 5% provides caloric support.
| Metabolism | Lidocaine is primarily metabolized in the liver by CYP1A2 and CYP3A4 to monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Dextrose is metabolized via glycolysis. |
| Excretion | Renal excretion of unchanged drug and metabolites: 10% unchanged, 90% as metabolites (primarily 4-hydroxy-2,6-xylidine and glycylxylidide). Less than 1% biliary/fecal. |
| Half-life | Terminal elimination half-life: 1.5–2 hours (prolonged to 2–3 hours in hepatic impairment; unchanged in renal impairment). |
| Protein binding | 70% bound primarily to alpha1-acid glycoprotein (AAG) and albumin; binding saturable and increased in inflammatory states. |
| Volume of Distribution | Vd: 1.1–1.7 L/kg (central compartment Vc: 0.5 L/kg; distributes rapidly to well-perfused tissues). |
| Bioavailability | Oral: 35% (extensive first-pass metabolism); Subcutaneous: 100% (complete absorption); Rectal: 30–50% (variable). IV: 100%. |
| Onset of Action | Intravenous: 45–90 seconds; Epidural: 5–15 minutes; Subcutaneous infiltration: 1–3 minutes. |
| Duration of Action | Duration: 60–120 minutes (IV bolus); 90–120 minutes (infiltration); 30–60 minutes (epidural without epinephrine). |
| Molecular Weight | 234.34 |
Intravenous administration: Initial dose of 1-1.5 mg/kg (up to 300 mg total) given at a rate not exceeding 50 mg/min. Followed by continuous infusion at 1-4 mg/min (20-50 mcg/kg/min) for arrhythmia management.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required for lidocaine; however, use with caution in severe renal impairment (GFR < 10 mL/min) due to potential accumulation of metabolites. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce loading dose by 50% and infusion rate by 50%. Child-Pugh Class C: Reduce loading dose by 75% and infusion rate by 75%. |
| Pediatric use | Weight-based dosing: Loading dose: 1-1.5 mg/kg IV (max 100 mg). Infusion: 20-50 mcg/kg/min IV. For neonates: Loading dose 0.5-1 mg/kg, infusion 10-30 mcg/kg/min. |
| Geriatric use | Reduce initial dose by 50% and monitor closely due to decreased hepatic clearance and increased risk of toxicity. Typical initial loading dose: 0.5-0.75 mg/kg IV. |
| 1st trimester | Lidocaine crosses the placenta. Limited human data; avoid in first trimester unless benefit outweighs risk. Consider alternative agents when possible. |
| 2nd trimester | Lidocaine use in second trimester is considered relatively safe at recommended doses. Monitor for maternal and fetal toxicity with high doses or prolonged infusion. |
| 3rd trimester | Lidocaine can cause neonatal CNS depression and bradycardia if administered close to delivery. Dose-dependent; use caution and avoid high doses or paracervical block. |
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 0.5-0.7. Free fraction higher in fetus due to lower protein binding. Accumulation possible with repeated dosing. |
■ FDA Black Box Warning
None
| Common Effects | ventricular arrhythmias |
| Serious Effects |
Hypersensitivity to lidocaine or amide-type anestheticsThird-degree atrioventricular block (without pacemaker)Adams-Stokes syndromeSevere sinoatrial blockUncontrolled ventricular arrhythmias (for intravenous use)
| Precautions | Risk of lidocaine toxicity (CNS and cardiac effects), Use caution in patients with hepatic impairment, heart failure, or hypovolemia, Monitor ECG and serum lidocaine levels, Avoid rapid IV administration, Contains dextrose; use with caution in patients with diabetes mellitus |
| Food/Dietary | No specific food interactions. However, as the solution contains dextrose, monitor blood glucose in diabetic patients. Grapefruit juice may theoretically increase lidocaine levels (CYP3A4 inhibition), but clinical significance is unclear. |
Loading safety data…
| Breastfeeding | Lidocaine is excreted into breast milk in small amounts (milk:plasma ratio ~0.4). At typical doses, risk to nursing infant is minimal. However, monitor infant for signs of toxicity (e.g., sedation, irritability) with high maternal doses or prolonged use. |
| Lactation Rating | L2 (Probably Compatible) |
| Teratogenic Risk | Lidocaine crosses the placenta. First trimester: No well-controlled studies; animal studies show no evidence of fetal harm. Second trimester: No specific risks identified; used for epidural anesthesia without increased malformations. Third trimester: IV lidocaine may cause fetal bradycardia; uterine artery vasoconstriction reported with high doses. Dextrose 5%: No teratogenic risk. |
| Fetal Monitoring | Monitor maternal ECG and blood pressure during IV administration. Fetal heart rate monitoring recommended during labor epidural use due to risk of fetal bradycardia. Observe for signs of local anesthetic toxicity (perioral numbness, metallic taste, seizures). |
| Fertility Effects | No adverse effects on human fertility reported in standard studies. Dextrose 5% does not affect fertility. |
| Clinical Pearls | Lidocaine hydrochloride 0.2% in D5W is primarily used as a continuous IV infusion for acute ventricular arrhythmias, especially post-MI. Monitor for CNS toxicity (tinnitus, perioral numbness) and cardiac toxicity (QRS widening, hypotension). Reduce dose in heart failure, hepatic impairment, and elderly. Therapeutic level: 1.5-5 mcg/mL. Avoid in second-degree or third-degree AV block without pacemaker. |
| Patient Advice | This medication is given into a vein to treat irregular heartbeats. · Report any ringing in ears, numbness around mouth, dizziness, or confusion immediately. · You may experience drowsiness or blurred vision; avoid driving until effects are known. · This solution contains dextrose; inform your doctor if you have diabetes. · Do not stop or adjust the infusion rate on your own. |