PLIAGLIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PLIAGLIS (PLIAGLIS).
Pliaglis is a topical local anesthetic combination of lidocaine and tetracaine. Lidocaine and tetracaine stabilize neuronal membranes by inhibiting sodium ion influx, thereby blocking initiation and conduction of nerve impulses.
| Metabolism | Lidocaine is primarily metabolized in the liver by CYP3A4 to monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Tetracaine is metabolized primarily by plasma esterases. |
| Excretion | Renal: 70% (lidocaine and metabolites); fecal: 10% (primarily unchanged); biliary: 20% (metabolites). |
| Half-life | 1.5-2 hours (lidocaine); prolonged in hepatic impairment or heart failure (up to 6-8 hours). |
| Protein binding | 65-75% bound to alpha-1-acid glycoprotein (lidocaine). |
| Volume of Distribution | 1.1-1.7 L/kg (lidocaine); increased in chronic use or disease states affecting protein binding. |
| Bioavailability | Topical: variable (30-80% depending on application site and integrity); intraoral: 55-65%; not applicable parenterally. |
| Onset of Action | Topical application: 5-10 minutes for surface anesthesia; local infiltration: 2-5 minutes. |
| Duration of Action | Topical: 30-60 minutes; local infiltration: 1-3 hours (dose-dependent). |
Lidocaine 2.5% and prilocaine 2.5% cream: Apply 1 g per 10 cm² of intact skin; cover with occlusive dressing. Maximum dose: 20 g per application for adults weighing ≥70 kg; for <70 kg, max 10 g. Frequency: Single application, minimum 1 hour before procedure, up to 5 hours.
| Dosage form | CREAM |
| Renal impairment | No specific GFR-based dose modifications; caution in severe renal impairment (CrCl <30 mL/min) due to potential accumulation of metabolites. Consider reduced application area or shorter duration. |
| Liver impairment | Child-Pugh Class C: Avoid use due to reduced clearance of lidocaine and prilocaine. Child-Pugh A or B: Use with caution; may require reduced dose or smaller application area. |
| Pediatric use | Infants and children: Apply 1 g per 10 cm²; maximum dose based on weight: <5 kg: 1 g; 5-10 kg: 2 g; 10-20 kg: 5 g; >20 kg: 10 g. Do not exceed 20 g. Contraindicated in neonates <37 weeks gestational age. |
| Geriatric use | No specific dose adjustment; use lowest effective dose. Increased risk of systemic toxicity due to age-related changes in skin permeability and drug clearance. Monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PLIAGLIS (PLIAGLIS).
| Breastfeeding | Limited data; lidocaine and prilocaine are excreted in breast milk but considered compatible with breastfeeding. M/P ratio not established. Use caution. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal studies, lidocaine (one component) produced no teratogenic effects; prilocaine (the other component) was not teratogenic in rats. Risk cannot be ruled out. Use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
There is no FDA black box warning for Pliaglis.
| Serious Effects |
["Hypersensitivity to lidocaine, tetracaine, or any component of the formulation.","Application to large areas of broken skin or open wounds.","Use in patients with known history of methemoglobinemia."]
| Precautions | ["Avoid application to broken or irritated skin.","Do not use on mucous membranes or eyes.","Monitor for signs of systemic toxicity, especially with large surface area or prolonged use.","Use with caution in patients with hepatic impairment, G6PD deficiency, or methemoglobinemia risk."] |
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| Monitor for maternal signs of lidocaine/prilocaine toxicity (e.g., CNS, cardiovascular) and fetal heart rate if used during labor. Methemoglobinemia risk in neonates with prolonged use. |
| Fertility Effects | No known adverse effects on fertility based on animal studies. |