bupivacaine liposome

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.

Pharmacokinetics ⬆ ⬇

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

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

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.

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) , procedural pain

Interactions ⬆ ⬇

Drug-drug:

Should not be administered concurrently with local lidocaine, wait at least 20 minutes before infiltration with bupivacaine liposome.
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.

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 (10 mL)

Availability ⬆ ⬇

Liposomal suspension for injection: 13.3 mg/mL

Assessment ⬆ ⬇

Assess infiltrated area for pain following administration and periodically during therapy.
Monitor cardiovascular and respiratory status (vital signs, level of consciousness) constantly following infiltration. Notify health care professional immediately if signs of cardiac toxicity (atrioventricular block, ventricular arrhythmias, cardiac arrest) occur.
Monitor for central nervous system toxicity. Notify health care professional promptly if they occur. Early signs of central nervous system toxicity include restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, twitching, depression or drowsiness.
Monitor for signs and symptoms of allergic reactions (urticaria, pruritus, erythema, angioneurotic edema, laryngeal edema, tachycardia, sneezing, nausea, vomiting, syncope, excessive sweating, elevated temperature, severe hypotension). Have resuscitative equipment available.

Implementation ⬆ ⬇

Do not confuse bupivacaine with ropivacaine.
Do not confuse with propofol. In a syringe suspension is milky white and may be mistaken for other medications. Label syringe to ensure dose is not administered IV.
Infiltration: Diluent: May be administered undiluted or diluted with 0.9% NaCl up to 0.89 mg/mL. Total dose should not exceed 266 mg (20 mL). Invert vial multiple times to resuspend particles immediately prior to withdrawal from vial. Inject with a 25 gauge or larger bore needle slowly into soft tissues of surgical site with frequent aspiration to check for blood and minimize risk of intravascular injection. Use diluted suspension within 4 hrs of preparation in a syringe. Vials are for single dose; discard unused portions. May be stored in refrigerator for up to 30 days prior to opening. Do not use if solution is discolored or has been frozen or exposed to high temperatures for extended period.
Do not administer in an area with povidone iodine until dry. If administered with other non-bupivacaine local anesthetics, administer other agents first and wait at least 20 min before infiltrating with bupivacaine liposome.

Patient/Family Teaching ⬆ ⬇

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

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇