LIDOCAINE HYDROCHLORIDE 0.8% 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 an amide-type local anesthetic that stabilizes the neuronal membrane by inhibiting sodium ion channels, thereby blocking the initiation and conduction of nerve impulses. It also has antiarrhythmic properties by decreasing automaticity in Purkinje fibers and suppressing ventricular arrhythmias.
| Metabolism | Lidocaine undergoes extensive hepatic metabolism primarily via CYP1A2 and CYP3A4 to active metabolites (monoethylglycinexylidide, MEGX; glycinexylidide, GX) which have antiarrhythmic and convulsant activity. Dextrose is metabolized via glycolysis and the Krebs cycle. |
| Excretion | Renal (metabolites: 4-hydroxyxylidine, glycylxylidide, monoethylglycinexylidide; <10% unchanged). Biliary/fecal negligible. |
| Half-life | Terminal elimination half-life: 1.5-2 hours (adults); prolonged in heart failure (up to 5-8 hours) or hepatic impairment (up to 10-15 hours). Clinically, context indicates redistribution half-life ~8 minutes. |
| Protein binding | 70% bound primarily to alpha-1-acid glycoprotein (AAG); binding saturable and decreased in acidosis. |
| Volume of Distribution | Vd: 1.1-1.5 L/kg (total); rapid distribution to highly perfused tissues (brain, heart, liver, kidneys). Clinically indicates large tissue reservoir. |
| Bioavailability | Intravenous: 100%. Oral: <35% (extensive first-pass metabolism). Intramuscular: 100% (bioequivalent to IV). Epidural: 70-80% (systemic absorption). |
| Onset of Action | Intravenous: 45-90 seconds (anesthetic/antiarrhythmic). Epidural: 5-15 minutes. Subcutaneous infiltration: 1-3 minutes. |
| Duration of Action | Intravenous: 10-20 minutes (antiarrhythmic); epidural: 60-90 minutes; subcutaneous infiltration: 30-120 minutes (with epinephrine). |
| Molecular Weight | 270.8 |
Intrathecal administration for spinal anesthesia: 50-100 mg (1.5-2 mL of 5% solution) as a single dose. For continuous epidural or peripheral nerve block, 0.8% solution with dextrose 5% is not typically used; refer to 1-2% lidocaine without dextrose for continuous infusion.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment. Lidocaine is extensively hepatically metabolized; <10% excreted unchanged in urine. GFR-based modifications are not necessary. |
| Liver impairment | Severe hepatic impairment (Child-Pugh class C): reduce dose by 50% and monitor for toxicity. Moderate impairment (Child-Pugh class B): consider 25% dose reduction. Mild impairment (Child-Pugh class A): no adjustment needed. |
| Pediatric use | Not approved for pediatric use; alternative formulations or agents recommended. If used off-label, dose based on weight: 0.5-1 mg/kg for spinal anesthesia, maximum 100 mg. Must be administered by experienced provider. |
| Geriatric use | Elderly patients (≥65 years) may require reduced doses due to decreased clearance and increased sensitivity. Use lower effective dose (e.g., 25-50 mg spinal), titrate slowly, and monitor for hypotension and bradycardia. |
| 1st trimester | Lidocaine crosses the placenta; animal studies have not demonstrated teratogenic effects, but human data are limited. Use only if clearly needed. |
| 2nd trimester | Similar to T1; no known fetal risk in human studies, but caution advised. Use only if benefit outweighs risk. |
| 3rd trimester | Lidocaine can cause fetal bradycardia and CNS depression if high doses are used near term. Avoid use during labor and delivery unless necessary. |
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 readily crosses the placenta via passive diffusion; equilibrium is reached between maternal and fetal compartments. |
■ FDA Black Box Warning
There is no black box warning for lidocaine hydrochloride 0.8% and dextrose 5% in plastic container.
| Common Effects | ventricular arrhythmias |
| Serious Effects |
Hypersensitivity to lidocaine or any amide-type local anestheticThird-degree atrioventricular block (without pacemaker)Severe hypotension or cardiogenic shockAdams-Stokes syndromeKnown hypersensitivity to parabens (if formulation contains parabens)
| Precautions | May cause severe hypotension and bradycardia, especially in patients with hypovolemia or heart block., Risk of central nervous system toxicity including seizures, especially with high doses or rapid absorption., Cardiotoxicity may occur with high plasma concentrations., Use caution in patients with hepatic impairment, heart failure, or elderly patients due to reduced clearance., Contains dextrose; use with caution in patients with diabetes or glucose intolerance., Avoid use in patients with myasthenia gravis (can exacerbate weakness). |
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| Breastfeeding |
| Lidocaine is excreted into breast milk in small amounts, typically less than 10% of the maternal dose. Risk to nursing infant is minimal, especially with local administration. Monitor infant for excessive sedation or arrhythmias if high doses used. |
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | First trimester: No evidence of teratogenicity in humans; lidocaine crosses placenta but not associated with major malformations. Second trimester: Low risk; use only if clearly needed. Third trimester: Potential for neonatal CNS depression and bradycardia if high maternal serum levels; epidural use may cause fetal bradycardia. Avoid in fetal distress or uteroplacental insufficiency. |
| Fetal Monitoring | Monitor maternal vital signs, ECG, and CNS status for toxicity. Continuous fetal heart rate monitoring during epidural or systemic administration; assess for signs of fetal bradycardia or distress. Monitor neonatal heart rate and respiratory status if administered near delivery. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at clinically relevant doses. |
| Food/Dietary | No significant food interactions. The solution is administered via injection; dietary restrictions are not applicable. |
| Clinical Pearls | Lidocaine hydrochloride 0.8% and dextrose 5% is a hyperbaric solution used for spinal anesthesia. The baricity (1.029-1.031 at 20°C) ensures predictable spread in cerebrospinal fluid. Administer with patient in lateral or sitting position; position changes can alter block height. Use for lower abdominal, pelvic, perineal, and lower extremity procedures. Contraindicated in patients with complete heart block, severe hypotension, or hypersensitivity to amide anesthetics. Rapid injection can cause high spinal block; monitor for respiratory compromise. Epinephrine may prolong duration but is not included in this preparation. |
| Patient Advice | You will receive an injection into your lower back to numb the lower half of your body. · You may feel warm, tingling, or numb in your legs and lower belly after the injection. · You will not be able to feel pain in the numbed area during your procedure. · Do not drive or operate machinery for at least 24 hours after the procedure. · Report any headache, difficulty breathing, or new back pain to your doctor immediately. · Avoid strenuous activity until the numbness fully wears off. |