bupivacaine liposomal

High Alert

Single-use infiltration to produce postsurgical local analgesia.
Interscalene brachial plexus nerve block to produce postsurgical regional analgesia.
Sciatic nerve block in the popliteal fossa to produce postsurgical regional analgesia.
Adductor canal block to produce postsurgical regional analgesia.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity; cross-sensitivity with other amide local anesthetics (ropivacaine, lidocaine, mepivacaine, prilocaine) may occur;
Use of other local anesthetics within 96 hr after administration;
OB: Obstetrical paracervical block anesthesia (may cause fetal bradycardia/death).

Use Cautiously in:

Glucose-6-phosphate dehydrogenase deficiency, history of methemoglobinemia, cardiac or pulmonary disease, or concurrent exposure to oxidizing agents (or metabolites of these agents) (↑ risk of methemoglobinemia);
Impaired cardiovascular function;
Hepatic impairment;
Renal impairment;
OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Children <6 yr (safety and effectiveness not established); infants <6 mo (↑ risk of methemoglobinemia).

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema, prolonged AV conduction, tachycardia

Derm: pruritus

GI: constipation, nausea, vomiting

Hemat: anemia, methemoglobinemia

MS: back pain, muscle spasm

Neuro: CENTRAL NERVOUS SYSTEM TOXICITY, dizziness, drowsiness, headache, insomnia

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLACTOID-LIKE REACTIONS AND LARYNGEAL EDEMA)

Interactions ⬆ ⬇

Drug-drug:

Should not be administered concurrently with local lidocaine; wait at least 20 min before infiltration with bupivacaine liposomal.
Should not be admixed with other local anesthetics.
Concurrent use of other formulations of bupivacainemay ↑ overall exposure and risk of toxicity; if administered in same syringe, the ratio of the bupivacaine dose to the bupivacaine liposomal dose should not exceed 1–2 mg; otherwise, avoid using other formulations of bupivacaine within 96 hr of bupivacaine liposomal.
Concurrent use of acetaminophen, benzocaine, bupivacaine, chloroquine, cyclophosphamide, dapsone, flutamide, hydroxyurea, ifosfamide, metoclopramide, nitrofurantoin, nitroglycerin, nitroprusside, nitrous oxide, phenobarbital, phenytoin, prilocaine, primaquine, procaine, quinine, rasburicase, ropivacaine, sulfonamides, tetracaine, and valproate may ↑ risk of methemoglobinemia; monitor closely.

Availability ⬆ ⬇

(Generic available)

Liposomal suspension for injection: 13.3 mg/mL

Route/Dosage ⬆ ⬇

Different formulations of bupivacaine are not bioequivalent and are not interchangeable.

Local Analgesia

Infiltration(Adults ): Bunionectomy: 106 mg (8 mL) given as 7 mL into osteotomy and 1 mL into SUBQ tissue; Hemorrhoidectomy: 266 mg (20 mL) diluted to a volume of 30 mL and given as six 5-mL aliquots.
Infiltration(Children ≥6 yr): 4 mg/kg (max = 266 mg).

Regional Analgesia

Interscalene brachial plexus nerve block(Adults ): 133 mg
Sciatic nerve block in popliteal fossa(Adults ): 133 mg
Adductor canal block(Adults ): 133 mg admixed with 50 mg (10 mL) of 0.5% bupivacaine HCl.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Local anesthetics inhibit initiation and conduction of sensory nerve impulses by altering the influx of sodium and efflux of potassium in neurons, slowing or stopping pain transmission. Liposome formulation prolongs the duration of action.

Therapeutic effects:

Lessened postoperative pain.

Classifications ⬆ ⬇

Therapeutic Classification: anesthetics (topical/local)

Pharmacologic Classification: amides

Pharmacokinetics ⬆ ⬇

Absorption: Depends on amount injected and vascularity of administration site. Some systemic absorption occurs, but action is primarily local.

Distribution: Widely distributed following release from liposomes; high concentrations in highly perfused organs (heart, lungs, liver, brain).

Protein Binding: 95%.

Metabolism/Excretion: Mostly metabolized by the liver; metabolites are primarily renally excreted; 6% excreted unchanged in urine.

Half-Life: Following bunionectomy: 34.1 hr; following hemorrhoidectomy: 23.8 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
infiltration	unknown	0.5–2 hr	96 hr‡

‡Pain relief lasted for 24 hr.

Patient/Family Teaching ⬆ ⬇

Inform patient that infiltration may cause temporary loss of sensation or motor activity in infiltrated area.
Rep: Instruct females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇