XARACOLL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for XARACOLL (XARACOLL).

How it works

XARACOLL (bupivacaine and meloxicam) is a fixed-dose combination product for local analgesia. Bupivacaine is an amide local anesthetic that blocks sodium ion channels, inhibiting nerve impulse conduction. Meloxicam is an NSAID that inhibits cyclooxygenase (COX) isoforms, reducing prostaglandin synthesis.

What the body does with it

Metabolism	Bupivacaine undergoes hepatic metabolism via N-dealkylation and hydroxylation mediated primarily by CYP3A4 and CYP1A2. Meloxicam is extensively metabolized in the liver by CYP2C9 and CYP3A4.
Excretion	Primarily hepatic metabolism followed by renal excretion of metabolites; approximately 70-80% eliminated in urine (metabolites), <15% unchanged in feces via biliary excretion.
Half-life	Terminal elimination half-life is approximately 2-4 hours; clinical context: methadone-like opioid, prolonged half-life in elderly, renal impairment, or hepatic impairment; requires monitoring for accumulation.
Protein binding	Approximately 80-90%; primarily bound to alpha-1-acid glycoprotein and albumin; clinically relevant: displacement interactions possible but not common.
Volume of Distribution	Approximately 1.0-2.0 L/kg; extensive tissue distribution due to lipophilicity; clinical meaning: large Vd indicates high tissue binding; minimal effect of hemodialysis; reflects rapid redistribution.
Bioavailability	Buccal: approximately 70-80%; sublingual: approximately 70-80%; intravenous: 100% (not usually route); note: buccal avoids first-pass metabolism significantly.
Onset of Action	Buccal: 15-30 minutes; sublingual: 10-20 minutes; intravenous: morphine-like rapid onset (minutes) but not applicable; primary route buccal for acute pain; onset correlates with transmucosal absorption.
Duration of Action	Buccal/sublingual: 4-6 hours for analgesia; clinical notes: longer than IV morphine due to buccal route; duration may extend in hepatic impairment; acute pain management duration sufficient for procedural pain.

Classification & Brands

Dosing & administration

Adults: Single dose of 1.3 g (two microspheres) applied intraoperatively directly to the subcutaneous tissue before wound closure.

Dosage form	IMPLANT
Renal impairment	No dose adjustment required for any degree of renal impairment.
Liver impairment	No dose adjustment required for any degree of hepatic impairment, including Child-Pugh Class C.
Pediatric use	Not approved for use in pediatric patients (safety and efficacy not established).
Geriatric use	No specific dose adjustment recommended; use standard adult dosing. Clinical studies included patients aged 65 and older with no observed differences in safety or efficacy.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for XARACOLL (XARACOLL).

Breastfeeding	Bupivacaine is excreted in breast milk in low amounts; M/P ratio approximately 0.3-0.7. Meloxicam is excreted in low levels. Use caution; monitor infant for sedation and gastrointestinal effects. Consider alternative analgesics.
Teratogenic Risk	Fetal risk cannot be ruled out. XARACOLL (bupivacaine and meloxicam) is not recommended during pregnancy. Bupivacaine crosses the placenta; meloxicam, as an NSAID, is associated with premature closure of the ductus arteriosus and oligohydramnios in the third trimester. Avoid use after 30 weeks gestation.

Warnings & precautions

■ FDA Black Box Warning

Risk of cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. Risk of serious gastrointestinal adverse events, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to bupivacaine, meloxicam, any amide local anesthetic, or any component of the product; history of asthma, urticaria, or allergic-type reactions after taking aspirin or NSAIDs; coronary artery bypass graft (CABG) surgery; advanced renal disease; in patients with known sulfite sensitivity.

Clinical Precautions

Precautions

Cardiovascular thrombotic events; gastrointestinal bleeding, ulceration, and perforation; hepatotoxicity; hypertension; heart failure; renal toxicity; anaphylactoid reactions; serious skin reactions; fetal toxicity; hematologic toxicity; pre-existing asthma; ophthalmic effects; and use in labor and delivery.

Clinical Tips & Counseling

Drug interactions

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XARACOLL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for XARACOLL (XARACOLL).

How it works

What the body does with it

Metabolism	Bupivacaine undergoes hepatic metabolism via N-dealkylation and hydroxylation mediated primarily by CYP3A4 and CYP1A2. Meloxicam is extensively metabolized in the liver by CYP2C9 and CYP3A4.
Excretion	Primarily hepatic metabolism followed by renal excretion of metabolites; approximately 70-80% eliminated in urine (metabolites), <15% unchanged in feces via biliary excretion.
Half-life	Terminal elimination half-life is approximately 2-4 hours; clinical context: methadone-like opioid, prolonged half-life in elderly, renal impairment, or hepatic impairment; requires monitoring for accumulation.
Protein binding	Approximately 80-90%; primarily bound to alpha-1-acid glycoprotein and albumin; clinically relevant: displacement interactions possible but not common.
Volume of Distribution	Approximately 1.0-2.0 L/kg; extensive tissue distribution due to lipophilicity; clinical meaning: large Vd indicates high tissue binding; minimal effect of hemodialysis; reflects rapid redistribution.
Bioavailability	Buccal: approximately 70-80%; sublingual: approximately 70-80%; intravenous: 100% (not usually route); note: buccal avoids first-pass metabolism significantly.
Onset of Action	Buccal: 15-30 minutes; sublingual: 10-20 minutes; intravenous: morphine-like rapid onset (minutes) but not applicable; primary route buccal for acute pain; onset correlates with transmucosal absorption.
Duration of Action	Buccal/sublingual: 4-6 hours for analgesia; clinical notes: longer than IV morphine due to buccal route; duration may extend in hepatic impairment; acute pain management duration sufficient for procedural pain.

Classification & Brands

Dosing & administration

Adults: Single dose of 1.3 g (two microspheres) applied intraoperatively directly to the subcutaneous tissue before wound closure.

Dosage form	IMPLANT
Renal impairment	No dose adjustment required for any degree of renal impairment.
Liver impairment	No dose adjustment required for any degree of hepatic impairment, including Child-Pugh Class C.
Pediatric use	Not approved for use in pediatric patients (safety and efficacy not established).
Geriatric use	No specific dose adjustment recommended; use standard adult dosing. Clinical studies included patients aged 65 and older with no observed differences in safety or efficacy.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for XARACOLL (XARACOLL).

Breastfeeding	Bupivacaine is excreted in breast milk in low amounts; M/P ratio approximately 0.3-0.7. Meloxicam is excreted in low levels. Use caution; monitor infant for sedation and gastrointestinal effects. Consider alternative analgesics.
Teratogenic Risk	Fetal risk cannot be ruled out. XARACOLL (bupivacaine and meloxicam) is not recommended during pregnancy. Bupivacaine crosses the placenta; meloxicam, as an NSAID, is associated with premature closure of the ductus arteriosus and oligohydramnios in the third trimester. Avoid use after 30 weeks gestation.