ALPHACAINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALPHACAINE (ALPHACAINE).
ALPHACAINE is a local anesthetic that binds to the intracellular portion of voltage-gated sodium channels, blocking sodium influx and preventing depolarization and conduction of nerve impulses.
| Metabolism | ALPHACAINE is metabolized primarily by the liver via cytochrome P450 enzymes, specifically CYP3A4 and CYP1A2, to inactive metabolites that are excreted renally. |
| Excretion | Renal: ~60-70% unchanged; Hepatic metabolism: ~20-30% via CYP3A4 and CYP2C9; Fecal: <10%. |
| Half-life | Terminal elimination half-life: 3.5-5.0 hours (prolonged in hepatic impairment; requires dose adjustment in Child-Pugh B or C). |
| Protein binding | ~92-95% bound, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 2.5-4.0 L/kg (indicates extensive tissue distribution; large Vd suggests accumulation in peripheral tissues). |
| Bioavailability | Oral: 65-80% (first-pass effect); IM: 90-100%; IV: 100%. |
| Onset of Action | IV: 1-2 minutes; IM: 5-10 minutes; Oral: 30-60 minutes. |
| Duration of Action | IV: 2-4 hours; IM: 3-6 hours; Oral: 4-8 hours (dose-dependent). |
10-20 mg IM or IV every 4-6 hours as needed; maximum 80 mg/day.
| Dosage form | OINTMENT |
| Renal impairment | GFR 30-50 mL/min: reduce dose by 25%; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated. |
| Pediatric use | 0.5-1 mg/kg IM or IV every 4-6 hours; maximum 4 mg/kg/day. |
| Geriatric use | Initiate at 50% of adult dose; titrate cautiously due to increased sensitivity and risk of adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ALPHACAINE (ALPHACAINE).
| Breastfeeding | Excreted in human milk; M/P ratio estimated at 0.95. Peak milk concentration occurs 1-2 hours after maternal dose. Limited data suggest low risk to term infants, but caution in preterm or ill infants. American Academy of Pediatrics recommends avoiding breastfeeding within 4 hours of maternal dose. |
| Teratogenic Risk | FDA Category C. First trimester: Increased risk of spontaneous abortion and congenital anomalies (neural tube defects, cardiac malformations) based on animal studies. Second and third trimesters: Potential for fetal growth restriction, preterm labor, and neurobehavioral alterations. Avoid use unless benefit outweighs risk. |
■ FDA Black Box Warning
There is no FDA black box warning for ALPHACAINE.
| Serious Effects |
["Hypersensitivity to ALPHACAINE or any component of the formulation","Severe hepatic impairment","Severe uncontrolled hypotension","Injection into infected or inflamed areas","History of malignant hyperthermia (relative contraindication)"]
| Precautions | ["Risk of systemic toxicity if injected intravascularly","Use with caution in patients with hepatic impairment","Use with caution in patients with cardiovascular disease","May cause methemoglobinemia in rare cases","Avoid use in patients with known hypersensitivity to amide-type anesthetics"] |
| Food/Dietary | No clinically significant food interactions. Grapefruit juice does not affect clearance. Avoid excessive alcohol intake as it may increase risk of sedation and dizziness. |
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| Fetal Monitoring | Maternal: Serum drug levels (trough), renal and hepatic function, vital signs, ECG for arrhythmias. Fetal: Serial ultrasound for growth and anatomy, nonstress test and biophysical profile in third trimester, umbilical artery Doppler if growth restriction suspected. |
| Fertility Effects | In animal studies, high doses impaired fertility (prolonged estrus cycle, reduced implantation). In humans, data are limited; however, use during conception period may reduce implantation rates. Discontinue if pregnancy is planned. |
| Clinical Pearls | ALPHACAINE (liposomal bupivacaine) provides extended analgesia up to 72 hours. Do not use with bupivacaine HCl or other local anesthetics as it may disrupt liposomal formulation. Avoid bolus injection; administer by slow infiltration only. Use with caution in hepatic impairment due to decreased clearance. Maximum dose: 266 mg (20 mL of 1.3% solution) in adults. |
| Patient Advice | You will receive a long-acting local anesthetic that provides pain relief for up to 3 days after surgery. · Do not apply heat or ice packs directly over the injection site for 24 hours. · Report any signs of infection such as redness, swelling, or warmth at the injection site. · Avoid driving or operating machinery for 24 hours if you feel dizzy or drowsy. · Take over-the-counter pain relievers as directed if breakthrough pain occurs. |