RAVOCAINE AND NOVOCAIN W/ LEVOPHED
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RAVOCAINE AND NOVOCAIN W/ LEVOPHED (RAVOCAINE AND NOVOCAIN W/ LEVOPHED).
Stabilizes neuronal membranes by blocking sodium channels, inhibiting initiation and conduction of nerve impulses. Levophed (norepinephrine) is an alpha-adrenergic agonist causing vasoconstriction.
| Metabolism | Procaine: Hydrolyzed by plasma pseudocholinesterase to para-aminobenzoic acid and diethylaminoethanol. Norepinephrine: Metabolized by monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT). |
| Excretion | Renal excretion of unchanged drug and metabolites: procaine <2% unchanged, >80% as para-aminobenzoic acid (PABA) and diethylaminoethanol (DEAE); levonordefrin (Levophed) undergoes hepatic metabolism and renal excretion of metabolites, <5% unchanged. |
| Half-life | Procaine: terminal elimination half-life approximately 40 seconds (rapid plasma hydrolysis); levonordefrin: elimination half-life about 5-10 minutes, clinically brief vasoconstrictor effect. |
| Protein binding | Procaine: approximately 5.8% bound to plasma proteins (mainly albumin); levonordefrin: binding not clinically significant. |
| Volume of Distribution | Procaine: Vd approximately 0.7-1.0 L/kg, reflecting rapid distribution into total body water; levonordefrin: Vd not well characterized, likely limited to extracellular space. |
| Bioavailability | Procaine: negligible oral bioavailability due to extensive first-pass hepatic hydrolysis; intramuscular or subcutaneous: 100% systemic absorption; levonordefrin: oral bioavailability low (<20%) due to extensive hepatic metabolism; parenteral administration yields 100% bioavailability. |
| Onset of Action | Infiltration or nerve block: 2-5 minutes; topical application: minimal systemic absorption, local anesthesia onset 2-5 minutes with sufficient concentration. |
| Duration of Action | Infiltration or nerve block without levonordefrin: 30-60 minutes; with levonordefrin: 60-90 minutes due to vasoconstriction prolonging local retention. |
Dental infiltration: 1-2 mL of 2% lidocaine with 1:100,000 epinephrine (max 7 mg/kg or 500 mg total). For NOVOCAIN (procaine) with LEVOPHED (levonordefrin): 1-2 mL of 2% procaine with 1:20,000 levonordefrin, max 600 mg procaine per session.
| Dosage form | INJECTABLE |
| Renal impairment | No specific adjustment required for procaine or levonordefrin as they are metabolized in plasma and liver. Use caution in severe renal impairment (GFR <30 mL/min) due to potential accumulation of metabolites (PABA). |
| Liver impairment | Child-Pugh A and B: No adjustment; Child-Pugh C: Reduce dose by 50% and monitor for toxicity due to reduced hepatic metabolism. |
| Pediatric use | Weight-based dosing: Lidocaine max 4.5 mg/kg (with epinephrine 1:100,000) or 7 mg/kg without epinephrine. Procaine with levonordefrin: 5-6 mg/kg procaine, max 300 mg per dose. Not recommended under 3 years of age. |
| Geriatric use | Reduce dose by 20-30% due to decreased hepatic blood flow and metabolism. Use lowest effective volume, especially in patients with cardiovascular disease. Monitor for prolonged effects and CNS toxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAVOCAINE AND NOVOCAIN W/ LEVOPHED (RAVOCAINE AND NOVOCAIN W/ LEVOPHED).
| Breastfeeding | Lidocaine: M/P ratio ~0.4, minimal excretion; procaine: rapidly metabolized, negligible excretion; levonordefrin: unknown M/P ratio but likely minimal due to short half-life. Generally safe with benefits outweighing risks. |
| Teratogenic Risk | First trimester: No well-controlled studies; lidocaine and procaine cross placenta; theoretical risk of fetal bradycardia from levonordefrin (Levophed) at high doses. Second and third trimesters: Use caution; may reduce uterine blood flow and cause fetal hypoxia due to vasoconstriction from levonordefrin. Avoid paracervical block in obstetrics due to risk of fetal bradycardia. |
■ FDA Black Box Warning
Risk of methemoglobinemia: Use with caution in patients with glucose-6-phosphate dehydrogenase deficiency or other conditions predisposing to methemoglobinemia. Monitor for signs of methemoglobinemia, especially with large doses or repeated use.
| Serious Effects |
Hypersensitivity to procaine, norepinephrine, or any components. Severe hypotension, cardiogenic shock, or hypovolemia (unless as life-saving measure). Patients receiving MAO inhibitors or tricyclic antidepressants due to risk of hypertensive crisis.
| Precautions | Avoid intravenous injection; may cause cardiotoxicity, CNS depression, or allergic reactions. Use with caution in patients with cardiovascular disease, hyperthyroidism, or hypertension. Monitor for signs of toxicity, especially with large doses. Contains sulfites; may cause allergic reactions in susceptible individuals. |
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| Fetal Monitoring | Maternal: Heart rate, blood pressure, respiratory rate, ECG for arrhythmias; fetal: heart rate monitoring during prolonged use or high doses. Observe for signs of local anesthetic systemic toxicity (LAST). |
| Fertility Effects | No known adverse effects on fertility in animal studies; limited human data. Local anesthetics and vasoconstrictors are not associated with impaired fertility. |