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bupivacaine (Marcaine, Sensorcaine, Exparel)
Tradenames: Marcaine, Sensorcaine.
Indications:
1) local anesthesia
- labor pain
- postoperative pain
2) used in "blocks" for anesthesia & analgesia
a) sympathetic block
b) caudal or epidural block
c) retrobulbar block
d) liposomal bupivacaine (Exparel) FDA-approved for post-operative nerve block after shoulder surgery [5]
3) spinal anesthesthia associated with cesarean section [4]
Contraindications:
1) use with caution in patients with liver disease
2) do not use in children < 12 years of age
3) do not use for spinal anesthesia in children < 18 years of age
Dosage:
1) caudal block (with or without epinephrine)
a) adults: 15-30 mL of 0.25% or 0.5%
b) children: 1-3.7 mg/kg
2) epidural block (other than caudal block)
a) adults: 10-20 mL of 0.25% or 0.5%
b) children: 1.25 mg/kg/dose
3) peripheral nerve block:
a) 5 mL dose of 0.25% or 0.5% (12.5-25 mg)
b) maximum:
1] 2.5 mg/kg (without epinephrine)
2] 3 mg/kg (with epinephrine)
3] up to 400 mg/day
4) sympathetic nerve block
- 25-50 mL of 0.25% solution without epinephrine
Injection: 0.25%, 0.5%, 0.75% with or without epinephrine.
Pharmacokinetics:
1) onset of action 2-15 minutes depending upon site of injection
2) duration 3-7 hours (longer acting local anesthetic than lidocaine)
3) highly protein bound (low transfer across placenta)
4) co-administration of epinephrine prolongs the action & localizes the anesthesia
5) small amount (6%) excreted in urine
Adverse effects:
1) not common (1-10%, dose-related) [3]
- cardiac arrest*, hypotension, bradycardia, palpitations, seizures*, restlessness, anxiety, dizziness, weakness, nausea/vomiting, blurred vision, tinnitus, apnea
2) other [2]
- confusion
- bradycardia
- drowsiness
- paresthesias
- agitation
- tremors
- psychosis
- visual disturbances
- respiratory depression
- urticaria
- allergic reactions
- sulfite reactions in sulfite-containing preparations
* cardiac arrest & convulsions associated with high plasma concentrations after inadvertant intravascular administration
Mechanism of action:
1) amide-type local anesthetic
2) reversibly blocks nerve conduction in all nerve fibers (sensory, motor & autonomic fibers)
3) decreases permeability of nerves to Na+
4) increases threshold of excitability
5) prevents propagation of action potential
6) autonomic activity lost 1st, followed by sensory & motor function
Specific
levobupivacaine (Chirocaine)
General
local anesthetic
Properties
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 1.5-5 HOURS
therapeutic-range 1-4 UG/ML
toxic-range >8 8G/ML
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Deprecated Reference
- Gever J.
Exparel Gets OK for Expanded Indication.
Now approved as nerve block for post-op pain after shoulder
surgery
MedPage Today. April 06, 2018
Component-of
betamethasone/bupivacaine/isopropanol/povidone iodine
bupivacaine/citrate/sufentanil
bupivacaine/dexamethasone/isopropanol/povidone iodine
bupivacaine/epinephrine
bupivacaine/epinephrine/fentanyl
bupivacaine/fentanyl
bupivacaine/h2o/isopropanol/lidocaine/methylprednisolone/povidone iodine/sodium chloride
bupivacaine/hydromorphone
bupivacaine/isopropanol/lidocaine/methylprednisolone/povidone iodine
bupivacaine/isopropanol/lidocaine/povidone iodine
bupivacaine/lidocaine
bupivacaine/lidocaine/povidone iodine
bupivacaine/lidocaine/povidone iodine/triamcinolone
bupivacaine/meloxicam
bupivacaine/sufentanil