RAVOCAINE AND NOVOCAIN W/ NEO-COBEFRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RAVOCAINE AND NOVOCAIN W/ NEO-COBEFRIN (RAVOCAINE AND NOVOCAIN W/ NEO-COBEFRIN).
Ravocaine (propoxycaine) and Novocain (procaine) are ester-type local anesthetics that block voltage-gated sodium channels, inhibiting nerve impulse conduction. Neo-Cobefrin (levonordefrin) is a vasoconstrictor that acts on alpha-adrenergic receptors, causing local vasoconstriction to prolong anesthesia.
| Metabolism | Primarily hydrolyzed by plasma pseudocholinesterase (butyrylcholinesterase) to para-aminobenzoic acid (PABA) and diethylaminoethanol. |
| Excretion | Renal excretion of metabolites (>90% as para-aminobenzoic acid and other conjugates); <10% unchanged |
| Half-life | Procaine: 40–84 seconds (plasma ester hydrolysis); 2-(diethylamino)ethanol metabolite: 2–4 hours; Levonordefrin: ~2 hours |
| Protein binding | Procaine: ~5.8% (primarily albumin); Levonordefrin: minimal binding |
| Volume of Distribution | Procaine: 0.7–1.0 L/kg (rapid distribution); Levonordefrin: ~0.5 L/kg |
| Bioavailability | Oral: negligible (first-pass hydrolysis); Intravenous: 100% (not used); Infiltration/nerve block: essentially 100% at site |
| Onset of Action | Infiltration: 2–5 minutes; Nerve block: 5–15 minutes; Epidural: 10–15 minutes |
| Duration of Action | Infiltration: 30–60 minutes (with levonordefrin: 60–90 minutes); Nerve block: 30–90 minutes; Dental use: 60–120 minutes (due to vasoconstrictor) |
Local infiltration or nerve block: 1-7 mL of 2% solution (20 mg/mL lidocaine equivalent) with epinephrine 1:100,000, maximum dose 7 mg/kg (actual lidocaine) or 500 mg per procedure, not to exceed 3.5 mg/kg plain or 7 mg/kg with epinephrine in adults.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment is needed for impaired renal function as local anesthetics are hepatically metabolized. However, monitor for accumulation of metabolites in severe renal impairment (GFR <30 mL/min). |
| Liver impairment | Severe hepatic impairment (Child-Pugh Class C): Reduce dose by 50% and monitor for toxicity. Moderate impairment (Child-Pugh B): Use with caution, consider reducing dose. Mild impairment (Child-Pugh A): No adjustment required. |
| Pediatric use | Weight-based: 1-2 mg/kg actual lidocaine per injection site, maximum 4.5 mg/kg (with epinephrine) total dose, not to exceed 4 mg/kg plain. Individual doses should be adjusted based on age, weight, and procedure. |
| Geriatric use | Elderly patients may require lower doses due to decreased clearance, reduced hepatic blood flow, and increased sensitivity. Start at the low end of the dosing range and titrate carefully to effect. Maximum dose 5-7 mg/kg with epinephrine, not to exceed 400 mg per procedure. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAVOCAINE AND NOVOCAIN W/ NEO-COBEFRIN (RAVOCAINE AND NOVOCAIN W/ NEO-COBEFRIN).
| Breastfeeding | Lidocaine and procaine are excreted in breast milk in low amounts. M/P ratio: lidocaine ~1.0; procaine unknown. Risk to infant is minimal with standard doses. Monitor infant for drowsiness or irritability. |
| Teratogenic Risk | Lidocaine (Ravocaine) and procaine (Novocain) are classified as FDA Pregnancy Category B. Animal studies have not shown fetal harm; however, no adequate human studies exist. Epinephrine (Neo-Cobefrin) may reduce uterine blood flow; use caution in 2nd and 3rd trimesters. Avoid in 1st trimester unless necessary. |
■ FDA Black Box Warning
Not available
| Serious Effects |
["Hypersensitivity to ester-type local anesthetics or PABA derivatives.","Severe hypotension or shock.","Current use of monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants (TCAs) due to risk of hypertensive crisis with levonordefrin."]
| Precautions | ["Risk of methemoglobinemia, especially with high doses or in patients with glucose-6-phosphate dehydrogenase deficiency.","Avoid intravascular injection to prevent systemic toxicity.","Use caution in patients with cardiovascular disease, as vasoconstrictors may increase heart rate and blood pressure."] |
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| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and ECG for arrhythmias. Fetal heart rate monitoring recommended if high doses used or if signs of toxicity. Assess for maternal seizures or CNS depression. |
| Fertility Effects | No known adverse effects on fertility in humans. Animal studies show no impairment. |