bupivacaine

Absorption: Systemic absorption follows epidural administration, but amount absorbed depends on dose.

Distribution: If systemic absorption occurs, this agent is widely distributed and crosses the placenta.

Metabolism/Excretion: Small amounts that may reach systemic circulation are mostly metabolized by the liver; 6% excreted unchanged in the urine.

Half-Life: 1.5—5 hr (after epidural use); 19 hr (implant).

Time/Action Profile ⬆ ⬇

(analgesia)

ROUTE	ONSET	PEAK	DURATION
Epidural	10–30 min	Unknown	2–8 hr‡
Implant	Unknown	Unknown	Unknown

‡Duration of anesthetic block.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity; cross-sensitivity with other amide local anesthetics may occur (ropivacaine, lidocaine, mepivacaine, prilocaine);
Contains bisulfites and should be avoided in patients with known intolerance;
OB: Obstetrical paracervical block anesthesia.

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);
Concurrent use of other local anesthetics;
Hepatic impairment;
Concurrent use of anticoagulants (including low-dose heparin and low-molecular-weight heparins/heparinoids) ↑ the risk of spinal/epidural hematomas;
Hypotension or heart block;
Pedi: Infants <6 mo (↑ risk of methemoglobinemia); children <12 yr (safety not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias, bradycardia, CARDIOVASCULAR COLLAPSE, hypotension

Derm: pruritus

EENT: blurred vision, tinnitus

F and E: metabolic acidosis

GI: nausea, vomiting

GU: urinary retention

Hemat: methemoglobinemia

Local: incision site swelling/pain (implant)

Neuro: anxiety, circumoral tingling/numbness, dizziness, dysgeusia, headache, irritability, SEIZURES, tremor

Misc: fever, allergic reactions

Interactions ⬆ ⬇

Drug-drug:

Additive toxicity may occur with concurrent use of other amide local anesthetics (includinglidocaine, mepivacaine, and prilocaine).
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.
Use of solution containing epinephrine with MAO inhibitors may cause hypertension.

Route/Dosage ⬆ ⬇

Solutions containing preservatives should not be used for caudal or epidural blocks.
Epidural (Adults and Children >12 yr): 10–20 mL of 0.25% (partial to moderate block), 0.5% (moderate to complete block), or 0.75% (complete block) solution. Administer in increments of 3–5 mL allowing sufficient time to detect toxic signs/symptoms of inadvertent IV or IT administration. A test dose of 2–3 mL of 0.5% with epinephrine solution is recommended prior to epidural blocks.
Caudal block(Adults and Children >12 yr): 15–30 mL of 0.25% or 0.5% solution. A test dose of 2–3 mL of 0.5% with epinephrine solution is recommended prior to caudal blocks.
Peripheral nerve block(Adults and Children >12 yr): 5 mL of 0.25% or 0.5% solution (maximum dose = 400 mg).
Sympathetic nerve block(Adults and Children >12 yr): 20–50 mL of 0.25% solution.
Dental block(Adults and Children >12 yr): 1.8–3.6 mL per site of 0.5% with epinephrine solution.
Local infiltration(Adults and Children >12 yr): 0.25% solution infiltrated locally (maximum dose = 175 mg).
Implant(Adults ): 300 mg (three 100–mg implants) as single dose.

Availability ⬆ ⬇

(Generic available)

Solution for injection (with and without preservatives): 0.25%; 0.5%; 0.75%
Implant: 100 mg
In combination with: epinephrine 1:200,000; meloxicam (Zynrelef Kit). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Monitor for sensation during procedure and return of sensation after procedure.
Monitor BP, HR, and respiratory rate continuously while patient is receiving this medication.
Monitor for signs and symptoms of methemoglobinemia (cyanotic skin discoloration, abnormal coloration of blood) during and after implantation. Methemoglobin levels may continue to rise requiring immediate treatment with oxygen therapy, hydration, methylene blue, exchange transfusion, hyperbaric oxygen, and removal of implant, depending on symptom severity.
Systemic Toxicity: Assess for systemic toxicity (circumoral tingling and numbness, ringing in ears, metallic taste, dizziness, blurred vision, tremors, slow speech, irritability, twitching, seizures, cardiac arrhythmias). Notify health care professional if symptoms occur.
Epidural: Monitor BP, heart rate, and respiratory rate continuously while patient is receiving this medication. Mild hypotension is common because of the effect of local anesthetic block of nerve fibers on the sympathetic nervous system, causing vasodilation. Significant hypotension and bradycardia may occur, especially when rising from a prone position or following large dose increases or boluses. Treatment of unresolved hypotension may include hydration, decreasing the epidural infusion rate, and/or removal of local anesthetic from analgesic solution.
Unwanted Motor and Sensory Deficit: The goal of adding low-dose local anesthetics to epidural opioids for pain management is to provide analgesia, not to produce anesthesia. Patients should be able to ambulate if their condition allows, and epidural analgesic should not hamper this important recovery activity. However, many factors, including location of the epidural catheter, local anesthetic dose, and variability in patient response, can result in patients experiencing unwanted motor and sensory deficits. Pain is the first sensation lost, followed by temperature, touch, proprioception, and skeletal muscle tone.
- Assess for sensory deficit every shift. Ask patient to point to numb and tingling skin areas (numbness and tingling at the incision site is common and usually normal). Notify health care professional of unwanted motor and sensory deficits.
- Unwanted motor and sensory deficits often can be corrected with simple treatment. For example, a change in position may relieve temporary sensory loss in an extremity. Minor extremity muscle weakness is often treated by decreasing the epidural infusion rate and keeping the patient in bed until the weakness resolves. Sometimes removing the local anesthetic from the analgesic solution is necessary, such as when signs of local anesthetic toxicity are detected or when simple treatment of motor and sensory deficits has been unsuccessful.

Implementation ⬆ ⬇

See Route and Dosage section.
Do not confuse bupivacaine with ropivacaine.
Xaracoll: Clinicians must be experienced in bupivacaine toxicity. Oxygen, other resuscitative drugs, cardiopulmonary resuscitative equipment, and personnel resources needed for proper management of toxic reactions and related emergencies must be readily available during and following implantation.
- Place implant in surgical site dry; pre-moistening may result in premature release of bupivacaine.
- Avoid additional local anesthetic administration within 96 hr following implantation. If additional local anesthetic cannot be avoided, monitor for systemic toxicity.

Patient/Family Teaching ⬆ ⬇

Instruct patient to notify health care professional if signs or symptoms of systemic toxicity occur.
Advise patient to request assistance during ambulation until orthostatic hypotension and motor deficits are ruled out.
Advise patient treated with Xaracoll to avoid procedures requiring additional local anesthetics and to notify health care professional immediately if signs and symptoms of methemoglobinemia (pale, gray, or blue colored skin; headache; rapid heart rate; shortness of breath; lightheadedness; fatigue) occur.
Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇