GLYDO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GLYDO (GLYDO).
GLYDO (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 hepatic via CYP1A2, with minor contributions from CYP3A4; metabolites include monoethylglycinexylidide (MEGX) and glycinexylidide (GX). |
| Excretion | Renal excretion of unchanged drug accounts for approximately 10% of the dose; the remainder is metabolized in the liver to inactive metabolites that are excreted renally. Fecal elimination is negligible (<2%). |
| Half-life | Terminal elimination half-life is approximately 1.5 to 2 hours in adults with normal hepatic and renal function. In neonates, half-life is prolonged (up to 3-4 hours) due to immature hepatic metabolism. |
| Protein binding | 60-80% bound to alpha-1-acid glycoprotein (AAG); binding is concentration-dependent and decreases with high drug levels. |
| Volume of Distribution | Volume of distribution is approximately 1.1 L/kg (range 0.6-1.5 L/kg). Higher Vd in heart failure (up to 2.5 L/kg) due to increased perfusion of adipose tissue. |
| Bioavailability | Intravenous: 100%; Intramuscular: 80-90% (due to first-pass metabolism); Oral: approximately 35% (extensive first-pass metabolism, only used for prophylaxis). |
| Onset of Action | Intravenous: 1-2 minutes; Intramuscular: 5-10 minutes; Oral (as antiarrhythmic): 30-60 minutes. |
| Duration of Action | Intravenous: 10-20 minutes (single bolus) due to rapid redistribution; continuous infusion required for sustained effect. Intramuscular: 30-60 minutes. Oral: 2-4 hours. |
For anesthesia: 1-5% solution, 0.5-5 mg/kg IV or 2.5-15 mg intrathecally; for antiarrhythmic: 1-1.5 mg/kg IV bolus then 1-4 mg/min infusion.
| Dosage form | JELLY |
| Renal impairment | No specific dose adjustment required; use with caution in severe renal impairment (GFR <30 mL/min) due to accumulation of metabolites. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: reduce dose by 75% or avoid use. |
| Pediatric use | Antiarrhythmic: loading dose 1 mg/kg IV, maintenance 20-50 mcg/kg/min; local anesthesia: max 4.5 mg/kg (7 mg/kg with epinephrine). |
| Geriatric use | Reduce initial dose by 50%; monitor for toxicity; clearance may be decreased due to reduced hepatic blood flow. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GLYDO (GLYDO).
| Breastfeeding | Lidocaine is excreted into human breast milk in small amounts with a milk-to-plasma (M/P) ratio of approximately 0.4-1.1. At therapeutic maternal doses, the estimated daily infant dose via breastfeeding is less than 1% of the maternal weight-adjusted dose, which is unlikely to cause adverse effects in the nursing infant. However, caution is advised if high intravenous doses are used or if the infant is premature or has low hepatic function. |
| Teratogenic Risk | GLYDO (lidocaine HCl) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated teratogenic effects; however, there are no adequate and well-controlled studies in pregnant women. Lidocaine crosses the placenta. In the first trimester, risk cannot be excluded. During the second and third trimesters, use only if clearly needed. At term, lidocaine may cause fetal bradycardia, neonatal respiratory depression, or CNS effects due to potential for accumulation. |
■ FDA Black Box Warning
Not applicable; no FDA black box warning for lidocaine.
| Serious Effects |
["Hypersensitivity to lidocaine or any amide-type anesthetics","Severe atrioventricular block (without pacemaker)","Wolff-Parkinson-White syndrome (for IV use)","Adams-Stokes syndrome (for IV use)","Severe hepatic disease (relative contraindication for IV use)"]
| Precautions | ["Cardiotoxicity: can cause arrhythmias, hypotension, or cardiac arrest at high doses","CNS toxicity: seizures, respiratory depression, especially with rapid absorption or overdose","Anaphylactic reactions: rare but severe allergic reactions may occur","Methemoglobinemia: associated with certain formulations (e.g., benzocaine-containing products)","Hepatic impairment: decreased metabolism, increased risk of toxicity"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and level of consciousness for signs of systemic toxicity. Assess fetal heart rate pattern (continuous electronic fetal monitoring) during labor and delivery to detect fetal bradycardia or non-reassuring changes. Monitor for neonatal adverse effects such as respiratory depression, hypotonia, or seizures post-delivery if lidocaine was used near term. |
| Fertility Effects | Lidocaine has no known direct effects on fertility based on animal studies. No human data are available. Local anesthetics do not typically impact reproductive function at clinical doses. However, high systemic concentrations could theoretically interfere with sperm motility or uterine contractility, but this is not clinically relevant with standard dosing. |