OCTOCAINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OCTOCAINE (OCTOCAINE).
Octocaine (lidocaine) is a sodium channel blocker. It binds to and inhibits voltage-gated sodium channels in neuronal cell membranes, preventing depolarization and conduction of nerve impulses. This stabilizes the neuronal membrane and produces local anesthesia.
| Metabolism | Lidocaine is extensively metabolized in the liver via oxidative N-dealkylation by CYP1A2 and CYP3A4 to active metabolites (e.g., monoethylglycinexylidide, glycinexylidide). Approximately 90% of a dose is metabolized; less than 10% is excreted unchanged in urine. |
| Excretion | Renal (hepatic metabolism; <5% unchanged in urine). Biliary/fecal elimination of metabolites. |
| Half-life | Terminal half-life: 1.5–2.0 hours (infiltration) to 2.0–3.0 hours (epidural). Prolonged in hepatic impairment. |
| Protein binding | ~95% bound to alpha-1-acid glycoprotein and albumin. |
| Volume of Distribution | Vd: ~0.5 L/kg. Reflects moderate tissue binding and distribution. |
| Bioavailability | IV: 100%; Topical: minimal systemic absorption (~1-5% depending on site); Oral: negligible due to first-pass metabolism. |
| Onset of Action | Infiltration: 2–5 minutes; Epidural: 5–15 minutes; Topical: 1–3 minutes on mucous membranes. |
| Duration of Action | Infiltration (with epinephrine): 2–4 hours; Epidural (with epinephrine): 1.5–3 hours; Topical: 15–30 minutes. |
0.5% to 2% solution, 1-5 mL per site, not to exceed 7 mg/kg total dose, for local infiltration or nerve block. Maximum single dose: 500 mg (or 7 mg/kg) for plain solution; with epinephrine: 7 mg/kg, max 500 mg.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended; use with caution in severe renal impairment (eGFR <30 mL/min) due to risk of accumulation. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50% and monitor for toxicity; Child-Pugh C: contraindicated or use with extreme caution, maximum dose 50% of normal. |
| Pediatric use | Infants and children: 0.5% to 1% solution, maximum 4-5 mg/kg (plain) or 7 mg/kg (with epinephrine). For specific blocks, refer to weight-based nomograms; do not exceed adult doses. |
| Geriatric use | Elderly patients may have reduced clearance; use lower doses (e.g., 50-70% of standard) and titrate carefully; maximum single dose 400 mg. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OCTOCAINE (OCTOCAINE).
| Breastfeeding | OCTOCAINE is excreted into human milk in small amounts with an estimated M/P ratio of 0.2-0.4. The relative infant dose is less than 2% of the maternal weight-adjusted dose, which is unlikely to be harmful. However, due to limited data, caution is advised. Breastfeeding after regional anesthesia is considered safe; observe infant for signs of local anesthetic toxicity (e.g., drowsiness, irritability). |
| Teratogenic Risk | OCTOCAINE is a local anesthetic with no known teratogenic effects based on animal studies and limited human data. It is classified as FDA Pregnancy Category C. Trimester-specific risks: no increased risk of major malformations reported from inadvertent exposure during first trimester; second and third trimester use is not associated with fetal harm; however, avoidance during labor and delivery due to potential fetal bradycardia and CNS depression is recommended. |
■ FDA Black Box Warning
No FDA black box warning exists for lidocaine. However, systemic toxicity can occur from accidental intravascular injection or overdose, leading to cardiovascular and central nervous system effects.
| Serious Effects |
["Hypersensitivity to lidocaine or any amide-type local anesthetic","Severe hypotension or shock","Complete heart block (without pacemaker)","Severe hepatic impairment","Known history of malignant hyperthermia (relative)"]
| Precautions | ["Risk of systemic toxicity (seizures, cardiac arrhythmias) from inadvertent intravascular injection or overdose","May cause methemoglobinemia, especially with concomitant oxidant stress (e.g., prilocaine use)","Use with caution in patients with hepatic impairment (decreased metabolism)","Avoid in patients with severe shock or heart block","Allergic reactions are rare but possible"] |
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| Fetal Monitoring | Continuous fetal heart rate monitoring during labor analgesia due to risk of fetal bradycardia. Maternal monitoring includes vital signs, ECG (for cardiac arrhythmias), and signs of systemic toxicity (e.g., perioral numbness, tinnitus, metallic taste, seizures). Assess for adequate pain relief and motor block if used for regional anesthesia. |
| Fertility Effects | OCTOCAINE has no known direct effects on fertility. Animal reproductive studies did not show impaired fertility. No human data available; however, as a short-acting local anesthetic, it is unlikely to impact reproductive function when used in standard clinical doses. |