XYLOCAINE 5% W/ GLUCOSE 7.5%
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XYLOCAINE 5% W/ GLUCOSE 7.5% (XYLOCAINE 5% W/ GLUCOSE 7.5%).
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.
| Metabolism | Primarily metabolized in the liver via cytochrome P450 enzymes (CYP1A2 and CYP3A4) to active metabolites (e.g., monoethylglycinexylidide) and inactive metabolites. Less than 10% excreted unchanged in urine. |
| Excretion | Hepatic metabolism (90% N-dealkylation by CYP1A2/CYP3A4 to monoethylglycinexylidide and glycinexylidide); renal excretion of metabolites and parent drug (<10% unchanged); <1% biliary/fecal. |
| Half-life | 1.5-2 hours (terminal); prolonged in heart failure, hepatic disease, or elderly; neonates 3-6 hours due to immature hepatic function. |
| Protein binding | 65-75% bound to alpha-1-acid glycoprotein (AAG) and albumin. |
| Volume of Distribution | 0.5-1.0 L/kg (IV); smaller in neonates (0.3-0.5 L/kg) due to reduced adipose tissue and protein binding. |
| Bioavailability | Epidural/spinal: ~100%; oral: <35% (extensive first-pass metabolism); topical: negligible systemic absorption (unless broken skin or high-dose). |
| Onset of Action | Epidural: 5-15 min; spinal: immediate; peripheral nerve block: 4-6 min; infiltration: 2-5 min. |
| Duration of Action | Epidural/spinal: 60-90 min with epinephrine (plain: 30-60 min); peripheral block: 60-180 min depending on dose and site; infiltration: 30-60 min. |
Adult: 5-25 mL (250-1250 mg lidocaine) of 5% lidocaine with glucose 7.5% solution, administered by caudal or lumbar epidural injection, single dose. Max total dose: 1250 mg.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment for GFR; use with caution in severe renal impairment due to potential for metabolite accumulation. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid use or reduce dose by 75% with close monitoring. |
| Pediatric use | Weight-based dosing: 2-4 mg/kg of lidocaine, administered epidurally. Maximum single dose: 4 mg/kg. Not recommended for patients <12 kg body weight due to high concentration. |
| Geriatric use | Reduce dose by 20-50% due to decreased clearance and increased susceptibility to toxicity. Use lowest effective dose and monitor for neurologic and cardiovascular effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XYLOCAINE 5% W/ GLUCOSE 7.5% (XYLOCAINE 5% W/ GLUCOSE 7.5%).
| Breastfeeding | Lidocaine is excreted into breast milk in small amounts, with an estimated infant dose of 0.1-0.5% of the maternal weight-adjusted dose. M/P ratio is approximately 0.4. No adverse effects have been reported in breastfed infants. Use with caution, especially in preterm infants, and monitor for signs of lidocaine toxicity (e.g., sedation, poor feeding). |
| Teratogenic Risk | Lidocaine crosses the placenta. Fetal bradycardia and neonatal central nervous system depression may occur with high maternal serum concentrations. No teratogenicity has been reported in humans; animal studies have not demonstrated fetal harm. Use during the first trimester is generally considered safe, but avoid paracervical block in the second and third trimesters due to risk of fetal acidosis and bradycardia. |
■ FDA Black Box Warning
Risk of cardiac arrest and death when used for local anesthesia, especially in large doses or when injected intravascularly. Resuscitative equipment and trained personnel must be immediately available.
| Serious Effects |
["Hypersensitivity to lidocaine or amide-type anesthetics","Severe hypotension","Complete heart block (without pacemaker)","Intravascular injection is contraindicated"]
| Precautions | ["Avoid intravascular injection; aspirate before administration.","Caution in patients with hepatic impairment, cardiac disease, or elderly.","Risk of methemoglobinemia, especially with concomitant use of oxidizing agents.","Monitor for neurological and cardiac toxicity during administration."] |
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| Fetal Monitoring | Monitor maternal vital signs and fetal heart rate continuously during administration. Assess for signs of maternal central nervous system or cardiovascular toxicity (e.g., perioral numbness, tinnitus, seizures, hypotension). For epidural or spinal use, monitor fetal heart rate patterns (bradycardia may occur). |
| Fertility Effects | No adverse effects on fertility or reproductive performance have been observed in animal studies. There is no evidence that lidocaine impairs human fertility. |