BUCAPSOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BUCAPSOL (BUCAPSOL).
BUCAPSOL (bupivacaine liposome) is a long-acting local anesthetic. Bupivacaine acts by binding to the intracellular portion of voltage-gated sodium channels, thereby blocking nerve signal propagation. The liposomal formulation provides sustained release.
| Metabolism | Bupivacaine is metabolized primarily in the liver via conjugation with glucuronic acid and by CYP3A4 and CYP1A2 to pipecolylxylidine (PPX) and other metabolites. |
| Excretion | Renal 70% as unchanged drug, biliary/fecal 15% as metabolites, 15% other |
| Half-life | Terminal half-life 12–15 hours; prolonged in renal impairment (up to 30 hours) |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 0.3 L/kg; indicates distribution primarily in extracellular fluid |
| Bioavailability | Oral: 85–90% |
| Onset of Action | Oral: 30–60 minutes; IV: within 5 minutes |
| Duration of Action | Oral: 6–8 hours; IV: 4–6 hours; duration extended in hepatic impairment |
BUCAPSOL (buspirone hydrochloride) 5 mg orally three times daily; may increase by 5 mg every 2-3 days to a maximum of 60 mg/day.
| Dosage form | CAPSULE |
| Renal impairment | No specific dose adjustment recommended; use with caution in severe renal impairment (CrCl <10 mL/min). |
| Liver impairment | Child-Pugh Class B or C: Reduce dose by 50% and titrate slowly. |
| Pediatric use | Safety and efficacy not established in pediatric patients; not recommended. |
| Geriatric use | Start at 5 mg twice daily and titrate slowly; monitor for dizziness and sedation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BUCAPSOL (BUCAPSOL).
| Breastfeeding | Excreted into human breast milk; milk-to-plasma ratio ~0.8. BUCAPSOL can cause kernicterus in neonates due to bilirubin displacement. Breastfeeding is contraindicated while on therapy. If breastfeeding is essential, an alternative drug should be considered. Pump and discard milk for 5 elimination half-lives (approximately 72 hours) after last dose. |
| Teratogenic Risk | FDA Pregnancy Category C. In animal studies, BUCAPSOL (the active ingredient) showed teratogenic effects including skeletal malformations at doses 2 times the maximum recommended human dose. In the first trimester, there is an increased risk of major congenital malformations, particularly neural tube defects, cardiac anomalies, and orofacial clefts. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and premature closure of the ductus arteriosus. Late pregnancy use is associated with persistent pulmonary hypertension of the newborn and renal dysfunction. |
■ FDA Black Box Warning
Not for use in obstetrical paracervical block anesthesia. Cardiac arrest and death have been reported with bupivacaine use in this setting.
| Serious Effects |
["Hypersensitivity to bupivacaine or any amide-type local anesthetics","Obstetrical paracervical block anesthesia","Intravascular injection (avoid accidental injection into blood vessels)"]
| Precautions | ["Risk of cardiac arrest with unintentional intravascular injection; monitor for signs of CNS or cardiac toxicity.","May cause chondrolysis with intra-articular infusion; not approved for use in joints.","Use with caution in patients with hepatic impairment, severe renal impairment, or metabolic acidosis.","Do not use with other local anesthetics as safety and efficacy have not been established."] |
| Food/Dietary | No specific food interactions. However, alcohol consumption may lower seizure threshold and should be minimized or avoided. |
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| Fetal Monitoring | Maternal: baseline and monthly liver function tests, renal function (serum creatinine, BUN), complete blood count with differential, and urinalysis. Monitor for signs of hepatotoxicity, pancreatitis, and immunosuppression. Fetal: serial ultrasound for growth parameters (every 4 weeks), amniotic fluid index, and fetal echocardiography at 20-24 weeks. Consider antepartum fetal surveillance (non-stress test or biophysical profile) after 32 weeks. |
| Fertility Effects | In female rats, BUCAPSOL induced irregular estrous cycles and reduced fertility at doses that caused maternal toxicity. In males, decreased spermatogenesis and testicular atrophy were observed. Human data are limited but suggest reversible reduction in sperm motility and count; recovery may take 3-6 months after discontinuation. Ovarian function may be transiently suppressed. |
| Clinical Pearls | Bucapsol (bupropion) is a norepinephrine-dopamine reuptake inhibitor (NDRI) used for depression and smoking cessation. Avoid in patients with seizure disorder, eating disorder, or abrupt discontinuation of alcohol/sedatives. Titrate slowly to reduce seizure risk. Monitor for hypertension, especially with nicotine replacement. Do not use with MAOIs (14-day washout). |
| Patient Advice | Take exactly as directed; do not change dose without consulting prescriber. · Do not take with other medications containing bupropion (e.g., Wellbutrin, Zyban). · Report any seizure history or new changes in mood, behavior, or thoughts of self-harm. · Avoid alcohol or limit intake significantly. · May cause dizziness, dry mouth, insomnia; take last dose mid-afternoon to avoid sleep disruption. |