LIDOCAINE HYDROCHLORIDE 0.2% 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 stabilizes the neuronal membrane by inhibiting the ionic fluxes required for initiation and conduction of impulses, resulting in local anesthetic and antiarrhythmic effects.
| Metabolism | Primarily hepatic metabolism via CYP1A2 to monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both active metabolites. |
| Excretion | Renal excretion of unchanged drug and metabolites accounts for >95% of elimination, with ~10% as unchanged lidocaine and ~90% as metabolites (primarily 4-hydroxy-2,6-xylidine, with minor contribution from monoethylglycinexylidide and glycinexylidide). Biliary/fecal excretion is minimal (<1%). |
| Half-life | Terminal elimination half-life is approximately 1.5–2 hours (mean 1.8 h) in adults with normal hepatic function; may be prolonged in patients with hepatic impairment (e.g., cirrhosis) or heart failure (up to 10 h), and in neonates (3–6 h). |
| Protein binding | 70–80% bound to alpha-1-acid glycoprotein (AAG) and, to a lesser extent, albumin. Binding is variable; decreases in conditions with low AAG (e.g., neonates) and increases in inflammatory states (elevated AAG). |
| Volume of Distribution | Volume of distribution is approximately 1.0–1.5 L/kg in adults (range 0.7–2.0 L/kg). Higher Vd in patients with heart failure (~2.5 L/kg) due to decreased tissue perfusion; lower Vd in elderly (0.5–1.0 L/kg). Indicates extensive tissue distribution (e.g., brain, heart, liver). |
| Bioavailability | Intravenous: 100%. Subcutaneous infiltration: essentially 100% (locally administered). Not administered orally due to extensive first-pass hepatic metabolism (<10% bioavailability). |
| Onset of Action | Intravenous (IV) administration: onset of antiarrhythmic effect is rapid (within 45–90 seconds). Subcutaneous infiltration: local anesthesia onset within 2–5 minutes. |
| Duration of Action | IV: antiarrhythmic effect lasts 10–20 minutes after a single bolus, necessitating continuous infusion. Subcutaneous infiltration: local anesthesia lasts 30–60 minutes, prolonged with epinephrine (up to 2 hours). |
| Molecular Weight | 234.34 |
Intravenous infusion: 1-4 mg/min (0.2% solution = 2 mg/mL) for antiarrhythmic therapy; loading dose 1-1.5 mg/kg IV bolus, then infusion. Maximum infusion rate 4 mg/min.
| Dosage form | INJECTABLE |
| Renal impairment | GFR > 10 mL/min: no adjustment. GFR ≤ 10 mL/min: reduce infusion by 50% or monitor for toxicity; prolonged half-life may require dose reduction. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 25-50%. Child-Pugh C: reduce dose by 50-75% or consider alternative; increased risk of toxicity due to reduced metabolism. |
| Pediatric use | IV bolus: 1 mg/kg loading, then infusion 20-50 mcg/kg/min (0.03-0.05 mg/kg/min). Infusion rate may be titrated to effect; maximum infusion rate 50 mcg/kg/min. |
| Geriatric use | Elderly patients (≥65 years): reduce infusion rate by 50% and monitor for CNS and cardiac toxicity; lower hepatic clearance and reduced volume of distribution necessitate caution. |
| 1st trimester | Crosses placenta; use only if clearly needed. No well-controlled studies, but animal studies have not shown fetal harm. |
| 2nd trimester | Crosses placenta; use only if clearly needed. Consider cumulative dose and duration. |
| 3rd trimester | Crosses placenta; may cause fetal bradycardia or CNS depression if high maternal levels. Use lowest effective dose and monitor fetal heart rate. |
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 is approximately 0.5–0.7. Rapid equilibration occurs; fetal levels are ~50-70% of maternal levels. |
■ FDA Black Box Warning
No FDA black box warning for lidocaine in dextrose solution.
| Common Effects | ventricular arrhythmias |
| Serious Effects |
Hypersensitivity to lidocaine or any amide-type local anestheticsSevere heart block (second- or third-degree) without pacemakerAdams-Stokes syndromeWolff-Parkinson-White syndromeUncontrolled bradycardia or hypotension
| Precautions | Continuous monitoring of ECG and vital signs required during IV administration, Risk of CNS toxicity (seizures, respiratory depression) with high doses, Caution in patients with hepatic impairment or severe heart failure, May exacerbate pre-existing arrhythmias in some patients |
| Food/Dietary | No known dietary restrictions with this intravenous medication. However, avoid excessive grapefruit juice as it may theoretically affect lidocaine metabolism via CYP1A2 and CYP3A4 inhibition, though clinical significance is minimal due to IV route. |
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| Breastfeeding |
| Lidocaine is excreted into breast milk in small amounts (milk:plasma ratio ~0.4). Not expected to cause adverse effects in nursing infants with maternal therapeutic doses. However, use caution with high doses or prolonged infusions; monitor infant for sedation or irritability. |
| Lactation Rating | L2 (Limited data - probably compatible) |
| Teratogenic Risk | Lidocaine crosses the placenta. First trimester: No well-controlled studies, but animal data show no teratogenicity at clinically relevant doses. Second/third trimester: Fetal bradycardia and CNS depression may occur with high maternal doses; use lowest effective dose. No structural malformations associated. |
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, level of consciousness, and ECG for signs of CNS or cardiac toxicity. Fetal heart rate monitoring (external) recommended during labor and delivery for signs of bradycardia. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at clinically relevant doses. |
| Clinical Pearls | Lidocaine HCl 0.2% in D5W is an antiarrhythmic (class IB) used for ventricular arrhythmias. In plastic containers, the drug may adsorb to PVC; use non-PPVC tubing. Monitor for CNS toxicity (drowsiness, confusion, seizures) and cardiac toxicity (bradycardia, hypotension). Reduce dose in heart failure, hepatic impairment, or elderly. Therapeutic serum level: 1.5-5 mcg/mL; toxicity >5 mcg/mL. Administer by IV infusion only; do not use if discolored or contains precipitate. For continuous infusion, use an infusion pump. |
| Patient Advice | This medication is given through a vein to treat irregular heartbeats. · Report any symptoms of toxicity immediately: dizziness, drowsiness, ringing in ears, blurred vision, muscle twitching, or seizures. · Tell your healthcare provider if you have liver disease, heart failure, or low blood pressure. · Do not stop the infusion suddenly without physician guidance. · Avoid alcohol while receiving this medication as it may increase side effects. · Inform your doctor of all medications you are taking, especially other heart medications. |