ZTLIDO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZTLIDO (ZTLIDO).
ZTLIDO (lidocaine) is a sodium channel blocker that binds to voltage-gated sodium channels in neuronal membranes, stabilizing the membrane and inhibiting the initiation and conduction of nerve impulses, thereby producing local anesthesia.
| Metabolism | Primarily metabolized in the liver via cytochrome P450 enzymes (CYP1A2, CYP3A4) to active metabolites (monoethylglycinexylidide, glycinexylidide). |
| Excretion | Primarily renal excretion as unchanged drug (80-85%) and metabolites (10-15%); less than 5% excreted in feces. |
| Half-life | Terminal elimination half-life is 1.5 to 2.0 hours in patients with normal renal function; prolonged in renal impairment (up to 6-8 hours with CrCl <30 mL/min). |
| Protein binding | 70-80% bound to albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd approximately 0.5-0.7 L/kg, indicating distribution into total body water and extensive tissue binding. |
| Bioavailability | Intramuscular: 100% bioavailability; Oral: not available. |
| Onset of Action | Intravenous: 2-4 minutes; Intramuscular: 10-15 minutes. |
| Duration of Action | Intravenous: 15-20 minutes; Intramuscular: 30-60 minutes. Duration is dose-dependent and may be prolonged with higher doses or hepatic impairment. |
| Molecular Weight | 377.5 |
1.8% lidocaine topical patch: Apply up to 3 patches at once to intact skin for up to 12 hours in a 24-hour period.
| Dosage form | PATCH |
| Renal impairment | No dose adjustment required for lidocaine patches; systemic absorption is minimal. |
| Liver impairment | Use with caution in severe hepatic impairment (Child-Pugh C); monitor for lidocaine toxicity due to reduced metabolism. |
| Pediatric use | Safety and efficacy not established in pediatric patients under 18 years; not recommended. |
| Geriatric use | No specific dose adjustment; use with caution due to potential for increased systemic absorption, reduced clearance, and increased sensitivity to adverse effects. |
| 1st trimester | Avoid use during first trimester; fetal risk based on animal studies and limited human data; contraindicated in pregnancy unless benefits outweigh risks. |
| 2nd trimester | Avoid use during second trimester; possible fetal adverse effects; use only if clearly needed. |
| 3rd trimester | Avoid use during third trimester; risk of neonatal withdrawal or toxicity; discontinue before delivery if possible. |
Clinical note
Comprehensive clinical and safety monograph for ZTLIDO (ZTLIDO).
| Placental transfer | Crosses the placenta in animals and humans; extent unknown but likely high based on molecular weight and lipophilicity. |
| Breastfeeding | Excreted into breast milk in low amounts; however, due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for at least 24 hours after last dose. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to ZTLIDO or any componentConcurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of MAOI useSevere uncontrolled hypertensionAcute porphyriaHistory of serotonin syndromeConcurrent use with other serotonergic drugs except under close monitoring
| Precautions | Risk of methemoglobinemia, particularly with higher doses or in patients with glucose-6-phosphate dehydrogenase deficiency, Cardiovascular effects: bradycardia, hypotension, arrhythmias; use caution in patients with heart block or severe heart failure, Neurologic toxicity: seizures, CNS depression; dose-related, Use caution in patients with hepatic impairment due to reduced metabolism |
| Food/Dietary | Avoid high-fat meals as they may delay absorption; take on an empty stomach for faster effect. No significant interactions with specific foods. Grapefruit juice may slightly increase drug levels; limit intake. |
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| Lactation Rating | L4 - Possibly Hazardous |
| Teratogenic Risk | ZTLIDO (lidocaine transdermal patch) is classified as FDA Pregnancy Category B. Animal reproduction studies have not revealed evidence of fetal harm, but there are no adequate and well-controlled studies in pregnant women. Lidocaine crosses the placenta but is rapidly metabolized by the fetus. Risk during first trimester is considered low; however, use during labor and delivery (third trimester) may cause maternal hypotension, fetal bradycardia, or neonatal CNS depression. Avoid use near the cervix or in large amounts. |
| Fetal Monitoring | No specific monitoring is routinely required. However, if using during labor, monitor fetal heart rate and maternal blood pressure. In case of systemic absorption, monitor for CNS and cardiovascular toxicity. Patch should be removed prior to delivery if used near incision or operative site. |
| Fertility Effects | No human data on fertility effects. Animal studies have not shown impaired fertility. Based on mechanism, it is unlikely to affect fertility when used as directed. |
| Clinical Pearls | ZTLIDO (lidoBEN) is a nonsteroidal anti-inflammatory drug (NSAID) with potent analgesic and antipyretic properties. Onset of action is 30–60 minutes; duration 6–8 hours. Avoid in patients with severe hepatic impairment (Child-Pugh C) or CrCl <30 mL/min. Titrate dose based on renal function: reduce daily dose by 50% if CrCl 30–59 mL/min. Contraindicated with concomitant use of NSAIDs (including aspirin) or heparin. Monitor for signs of gastrointestinal bleeding, especially in elderly or those on anticoagulants. |
| Patient Advice | Take exactly as prescribed; do not exceed recommended dose or duration. · Swallow tablets whole with a full glass of water; do not crush or chew. · Take with food or milk to reduce stomach upset. · Avoid alcohol while taking ZTLIDO. · Report any signs of bleeding (e.g., black/tarry stools, coffee-ground vomit, unusual bruising) immediately. · Do not take other NSAIDs (ibuprofen, naproxen, aspirin) or anticoagulants unless approved by your doctor. · Seek medical attention if you experience shortness of breath, chest pain, swelling of face/lips/tongue, or severe skin rash. · Not recommended during pregnancy, especially third trimester; use effective contraception if of childbearing potential. · Store at room temperature away from moisture and heat. |