Version May 2024
Note: Bupivacaine (liposomal) is not bioequivalent to bupivacaine hydrochloride; dosing conversion from bupivacaine hydrochloride to bupivacaine (liposomal) or vice versa is not possible.
Analgesia, postsurgical:
Local anesthesia: Infiltration: Single dose: Dose is based on size of surgical site, volume required to cover the area, and individual patient factors (maximum dose: 266 mg [20 mL]). General dosage guidance for bunionectomy and hemorrhoidectomy provided below:
Bunionectomy: 7 mL of undiluted bupivacaine (liposomal) infiltrated into the tissues surrounding the osteotomy and 1 mL of undiluted bupivacaine (liposomal) infiltrated into the subcutaneous tissue of the surgical site (total dose = 106 mg [8 mL])
Hemorrhoidectomy: 30 mL of diluted bupivacaine (liposomal) (20 mL diluted with 10 mL NS) divided and infiltrated as 6 injections of 5 mL each (total dose = 266 mg [20 mL]) around the anal sphincter.
Regional analgesia:
Adductor canal block: Single dose: Total knee arthroplasty: 133 mg (10 mL).
Interscalene brachial plexus nerve block: Single dose: Total shoulder arthroplasty or rotator cuff repair: 133 mg (10 mL).
Sciatic nerve block in the popliteal fossa: Single dose: Bunionectomy: 133 mg (10 mL).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer’s labeling; renal impairment may reduce bupivacaine elimination increasing systemic exposure and the risk of adverse effects or toxicities; use with caution.
There are no dosage adjustments provided in the manufacturer’s labeling; use with caution; severe impairment may reduce bupivacaine metabolism increasing systemic exposure and the risk of adverse effects or toxicities.
Refer to adult dosing.
(For additional information see "Liposomal bupivacaine: Pediatric drug information")
Note: Bupivacaine (liposomal) is not bioequivalent to bupivacaine hydrochloride; dosing conversion from bupivacaine hydrochloride to bupivacaine (liposomal) or vice versa is not possible.
Local analgesia:
Children ≥6 years and Adolescents <18 years: Local infiltration: 4 mg/kg administered once; maximum dose: 266 mg/dose (20 mL).
Adolescents ≥18 years: Local infiltration: Single dose: Dose is based on size of surgical site, volume required to cover the area, and individual patient factors; maximum dose: 266 mg/dose (20 mL).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; renal impairment may reduce bupivacaine elimination, increasing systemic exposure and the risk of adverse effects or toxicities; use with caution and monitor closely.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution and monitor closely; severe impairment may reduce bupivacaine metabolism, increasing systemic exposure and the risk of adverse effects or toxicities.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Gastrointestinal: Constipation (2% to 22%), nausea (2% to 40%), vomiting (28%)
Nervous system: Motor dysfunction (12% to 21%)
Miscellaneous: Fever (2% to 23%)
1% to 10%:
Cardiovascular: Atrial fibrillation (<2%), bradycardia (1% to 2%), cardiac arrhythmia (<2%), deep vein thrombosis (<2%), edema (<2%), first degree atrioventricular block (<2%), hypertension (<10%), hypotension (7%), left bundle branch block (<2%), orthostatic hypotension (<2%), oxygen saturation decreased (<2%), palpitations (<2%), peripheral edema (2% to 3%), presyncope (<2%), prolonged QT interval on ECG (<2%), right bundle branch block (<2%), sinus bradycardia (<2%), sinus tachycardia (2% to 3%), supraventricular extrasystole (<2%), syncope (2%), tachycardia (3% to 4%), ventricular premature contractions (<2%), ventricular tachycardia (<2%)
Dermatologic: Cellulitis (<2%), diaphoresis (<2%), erythema of skin (<2%), hyperhidrosis (5%), increased wound secretion (<2%), pallor (<2%), pruritic rash (<2%), pruritus (3%), skin blister (<2%), skin rash (<2%), urticaria (<2%)
Gastrointestinal: Dysgeusia (7%), hiccups (1% to 2%), oral hypoesthesia (3% to 4%)
Genitourinary: Dysuria (<2%), urinary incontinence (<2%), urinary retention (8%)
Hematologic & oncologic: Anemia (6%, including acute posthemorrhagic anemia), hematoma (<2%), leukocytosis (<2%)
Hepatic: Increased liver enzymes (4%), increased serum alanine aminotransferase (1%), increased serum aspartate aminotransferase (3%)
Hypersensitivity: Fixed drug eruption (<2%), hypersensitivity reaction (<2%)
Infection: Fungal infection (2%)
Nervous system: Agitation (<2%), anxiety (3%), chills (<2%), confusion (5%), delirium (<2%), depression (<2%), dizziness (6%; includes postural dizziness), drowsiness (2% to 5%), fatigue (5%), feeling hot (2%), headache (4% to 8%), hyperthermia (<2%), hypoesthesia (2% to 4%), impaired mobility (decreased: 2%), insomnia (2% to 10%), lethargy (1%), myasthenia (<2%), pain (<2%), paresthesia (<2%), restlessness (<2%), sedated state (<2%), sensation disorder (sensory loss: 2%), sensation of cold (3%)
Neuromuscular & skeletal: Arthralgia (<2%), asthenia (<2%), back pain (<10%), joint swelling (<2%), laryngospasm (<2%), muscle spasm (<10%), muscle twitching (8%), musculoskeletal pain (<2%), neck pain (<2%), tremor (<2%)
Ophthalmic: Blurred vision (<2%), decreased visual acuity (<2%)
Otic: Auditory impairment (<2%), tinnitus (<2%)
Renal: Increased serum creatinine (2%)
Respiratory: Apnea (<2%), atelectasis (<2%), cough (<2%), dyspnea (<2%), hypoxia (1% to 2%), pneumonia (<2%), pulmonary infection (<2%), pulmonary infiltrates (<2%), respiratory depression (<2%), respiratory failure (<2%)
Postmarketing: Nervous system: Paralysis, seizure
Obstetrical paracervical block anesthesia
Concerns related to adverse effects:
• CNS effects: CNS effects (including excitation and/or depression) may occur, possibly leading to convulsions, unconsciousness, and/or respiratory arrest; may be related to total dose administered, route of administration, and physical status of patient; monitor for CNS-related changes or alterations in consciousness after each injection. Additionally, use of local anesthetics have been associated with neurologic effects following infiltration of soft tissue (persistent anesthesia, paresthesia weakness, paralysis), which may be irreversible.
• CNS toxicity: Careful and constant monitoring of the patient's state of consciousness should be done following each local anesthetic injection; at such times, restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, twitching, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness may be early warning signs of CNS toxicity. Sensory and/or motor loss is temporary and varies and may last up to 5 days.
• Cardiovascular toxicity: Serious and fatal cardiovascular system reactions (eg, decreased cardiac output and arterial blood pressure, atrioventricular block, ventricular arrhythmias, cardiac arrest) may occur with toxic concentrations.
• Hypersensitivity reactions: Allergic-type reactions (eg, angioneurotic edema [including laryngeal edema], dizziness, elevated temperature, excessive sweating, nausea, syncope, tachycardia, pruritus, erythema, sneezing, urticaria, vomiting) and possibly anaphylactoid-like symptoms (including severe hypotension) have been reported (rare); cross-sensitivity among amide-type local anesthetics has been reported.
• Intra-articular infusion related chondrolysis: Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use; chondrolysis (primarily in the shoulder joint) has occurred following infusion, with some cases requiring arthroplasty or shoulder replacement.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
• Respiratory arrest: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest.
• Seizures: Convulsions due to systemic toxicity leading to cardiac arrest have been reported with local anesthetics.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease; patients with impaired cardiovascular function are less able to compensate for functional changes associated with AV conduction prolongation produced by bupivacaine.
• Hepatic impairment: Use with caution in patients with hepatic impairment; patients with severe impairment may be at greater risk for toxicity.
• Renal impairment: Use with caution in patients with renal impairment; may be at greater risk for toxicity.
Other warnings/precautions:
• Appropriate use: Avoid intravascular, epidural, intrathecal, and intra-articular nerve block injections. Not indicated for preincisional or preprocedural locoregional anesthetic techniques that require deep and complete sensory block. Do not administer other local anesthetics or other formulations of bupivacaine within 96 hours following bupivacaine (liposomal) administration. Aspiration should be performed frequently prior to and during administration; the needle should be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided.
• Product interchangeability: Bupivacaine hydrochloride is not bioequivalent to bupivacaine (liposomal); dosing conversion from bupivacaine hydrochloride to bupivacaine (liposomal) and vice versa is not possible.
• Trained personnel: Clinicians using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Suspension, Injection:
Exparel: 1.3% (10 mL, 20 mL)
No
Suspension (Exparel Injection)
1.3% (per mL): $27.32
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Do not heat or autoclave prior to administration. Administer undiluted or diluted. Inject slowly (1 to 2 mL per injection) into the surgical site using a ≥25-gauge needle with frequent aspiration prior to and during administration; do not filter. Do not administer epidurally, intrathecally, intravascularly, or intra-articularly. Do not allow bupivacaine (liposomal) to come into contact with antiseptics (eg, povidone iodine) in solution; when a topical antiseptic is applied, allow site to dry prior to injection.
Non–bupivacaine-based local anesthetics may cause an immediate release of bupivacaine (liposomal) if administered together locally; therefore, bupivacaine should be administered no sooner than 20 minutes after injection of lidocaine. Do not administer other local anesthetics or other formulations of bupivacaine within 96 hours following bupivacaine (liposomal) administration; bupivacaine hydrochloride may be administered simultaneously in the same syringe or injected immediately before bupivacaine (liposomal) as long as the milligram ratio of bupivacaine hydrochloride to bupivacaine (liposomal) does not exceed 1:2.
Adductor canal block: Manufacturer's labeling recommends mixing 10 mL (133 mg) of bupivacaine (liposomal) with 10 mL (50 mg) of 0.5% bupivacaine (total volume: 20 mL).
Parenteral: Local infiltration: Administer undiluted or diluted. Inject slowly (1 to 2 mL per injection) into the surgical site using a ≥25-gauge needle with frequent aspiration prior to and during administration; do not filter. Do not administer epidurally, intrathecally, intravascularly, or intra-articularly. Do not allow bupivacaine (liposomal) to come into contact with antiseptics (eg, povidone-iodine) in solution; when a topical antiseptic is applied, allow site to dry prior to injection.
Nonbupivacaine-based local anesthetics may cause an immediate release of bupivacaine (liposomal) if administered together locally; therefore, bupivacaine (liposomal) should be administered no sooner than 20 minutes after injection of lidocaine. Do not administer other local anesthetics or other formulations of bupivacaine within 96 hours following bupivacaine (liposomal) administration; bupivacaine hydrochloride may be administered simultaneously in the same syringe or injected immediately before bupivacaine (liposomal) as long as the milligram ratio of bupivacaine hydrochloride to bupivacaine (liposomal) does not exceed 1:2.
Analgesia, postsurgical: Single-dose infiltration to produce postsurgical local analgesia in patients ≥6 years of age; interscalene brachial plexus nerve block to produce postsurgical regional analgesia in adults; sciatic nerve block in the popliteal fossa to produce postsurgical regional analgesia in adults; adductor canal block to produce postsurgical regional analgesia in adults.
Limitations of use: Safety and efficacy when used to produce postsurgical regional analgesia via other nerve blocks have not been established.
Bupivacaine may be confused with mepivacaine, ropivacaine
Bupivacaine liposomal may be confused with conventional bupivacaine
Bupivacaine liposomal may be confused with propofol due to similar white, milky appearance.
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
Substrate of CYP1A2 (minor), CYP2C19 (minor), CYP2D6 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
BUPivacaine: May enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Bupivacaine may be administered immediately before, or administered in the same admixture syringe as liposomal bupivacaine as long as the ratio of the milligram dose of bupivacaine to liposomal bupivacaine does not exceed 1:2. Risk D: Consider therapy modification
Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Risk C: Monitor therapy
Lidocaine (Systemic): May enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with lidocaine. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine. Lidocaine may be administered 96 hours or more after liposomal bupivacaine administration. Risk D: Consider therapy modification
Local Anesthetics: May enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics, but may be administered 20 minutes or more after lidocaine. Avoid all local anesthetics within 96 hours after administration of liposomal bupivacaine. Risk X: Avoid combination
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy
Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy
Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Risk C: Monitor therapy
Bupivacaine crosses the placenta.
Following use of the nonliposomal formulation, small amounts of bupivacaine can be found in the maternal plasma, potentially causing varying degrees of maternal, fetal, and neonatal toxicity involving the CNS, peripheral vascular tone, and cardiac function.
Liposomal bupivacaine is approved for postsurgical local analgesia; studies have evaluated its use for intra-incisional blocks at the time of cesarean delivery to decrease postoperative pain (Parikh 2019; Prabhu 2018). Use of bupivacaine in obstetrical paracervical block anesthesia is contraindicated (may cause fetal bradycardia and death).
Bupivacaine and its active metabolite are present in breast milk.
In order to evaluate breast milk concentrations of liposomal bupivacaine, a prospective cohort study was conducted in 30 women 18 to 40 years of age undergoing elective cesarean delivery between 37- and 42-weeks gestation. They received a bilateral transversus abdominis plane block under ultrasound guidance within 30 minutes of delivery using bupivacaine 52 mg and liposomal bupivacaine 266 mg.
Maternal serum and breast milk were sampled over 96 hours. Bupivacaine was not present in milk samples collected prior to the transversus abdominis plane block. Peak concentrations of bupivacaine in breast milk occurred at 6 hours and were almost undetectable by 96 hours. Peak breast milk concentrations were 36% of the maternal plasma concentrations. Authors of the study calculated the relative infant dose to be <1% of the weight-adjusted maternal dose over the 96-hour dosing interval (<10% is considered compatible with breastfeeding). Adverse events (related or unrelated) were transient tachypnea noted in two neonates. There were no clinically significant adverse events in any of the neonates within the follow-up period of 14 days (Mustafa 2020).
According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Cardiovascular and respiratory (adequacy of ventilation) vital signs, state of consciousness; signs of CNS toxicity, pain relief.
Blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.
Onset: Rapid (Hu 2013)
Duration: Local: Up to 72 hours (Hu 2013); Systemic: Plasma levels can persist for 96 hours after local administration, 120 hours after interscalene brachial plexus nerve block, and 168 hours after adductor canal block or sciatic nerve block in the popliteal fossa.
Absorption: Systemic absorption varies; dependent on dose, route of administration, and vascularity of administration site
Protein binding: 95%
Metabolism: Hepatic via conjugation; major metabolite pipecoloxylidine (PPX; inactive)
Half-life elimination: 13 to 34 hours (Hu 2013)
Time to peak, plasma: Within 1 hour (initial peak); 12 to 36 hours (second peak) (Hu 2013)
Excretion: Urine (~6% unchanged)
Altered kidney function: Renal impairment may reduce bupivacaine elimination increasing systemic exposure.
Hepatic function impairment: Severe impairment may reduce bupivacaine metabolism increasing systemic exposure.
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