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Pronunciation |
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(byoo
PIV a kane & ep i NEF
rin) |
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U.S. Brand
Names |
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Marcaine® with
Epinephrine |
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Generic
Available |
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Yes |
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Pharmacological Index |
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Local Anesthetic |
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Use |
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Dental and Medical: Local anesthesia |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to bupivacaine |
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Warnings/Precautions |
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Should be avoided in patients with uncontrolled
hyperthyroidism |
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Adverse
Reactions |
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Degree of adverse effects in the central nervous system and cardiovascular
system are directly related to the blood levels of bupivacaine
Central nervous system: High blood levels result in anxiety, restlessness,
disorientation, confusion, dizziness, tremors and seizures. This is followed by
depression of CNS resulting in somnolence, unconsciousness and possible
respiratory arrest. Nausea and vomiting may also occur. In some cases, symptoms
of CNS stimulation may be absent and the primary CNS effects are somnolence and
unconsciousness.
Hypersensitivity reactions: Extremely rare, but may be manifest as
dermatologic reactions and edema at injection site. Asthmatic syndromes have
occurred. Patients may exhibit hypersensitivity to bisulfites contained in local
anesthetic solution to prevent oxidation of epinephrine. In general, patients
reacting to bisulfites have a history of asthma and their airways are
hyper-reactive to asthmatic syndrome.
Psychogenic reactions: It is common to misinterpret psychogenic responses to
local anesthetic injection as an allergic reaction. Intraoral injections are
perceived by many patients as a stressful procedure in dentistry. Common
symptoms to this stress are sweating, palpitations, hyperventilation,
generalized pallor and a fainting feeling. |
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Drug
Interactions |
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Due to epinephrine component: With tricyclic antidepressants or MAO
inhibitors could result in increased pressor response; with nonselective
beta-blockers (ie, propranolol) could result in serious hypertension and reflex
bradycardia |
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Mechanism of
Action |
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Local anesthetics bind selectively to the intracellular surface of sodium
channels to block influx of sodium into the axon. As a result, depolarization
necessary for action potential propagation and subsequent nerve function is
prevented. The block at the sodium channel is reversible. When drug diffuses
away from the axon, sodium channel function is restored and nerve propagation
returns. |
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Pharmacodynamics/Kinetics |
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Onset of action: Infiltration and nerve block: 2-20 minutes
Duration:
Infiltration: 60 minutes
Nerve block: 5-7 hours
Serum half-life: 1.5-5.5 hours/adult |
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Usual Dosage |
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Children <10 years: Dosage has not been established
Children >10 years and Adults: Infiltration and nerve block in maxillary
and mandibular area: 9 mg (1.8 mL) of bupivacaine as a 0.5% solution with
epinephrine 1:200,000 per injection site. A second dose may be administered if
necessary to produce adequate anesthesia after allowing up to 10 minutes for
onset. Up to a maximum of 90 mg of bupivacaine hydrochloride per dental
appointment. The effective anesthetic dose varies with procedure, intensity of
anesthesia needed, duration of anesthesia required, and physical condition of
the patient; always use the lowest effective dose along with careful aspiration.
The following numbers of dental carpules (1.8 mL) provide the indicated
amounts of bupivacaine hydrochloride 0.5% and vasoconstrictor (epinephrine
1:200,000):
1 cartridge = 9 mg bupivacaine and 0.009 mg epinephrine
2 cartridges = 18 mg bupivacaine and 0.018 mg epinephrine
3 cartridges = 27 mg bupivacaine and 0.027 mg epinephrine
4 cartridges = 36 mg bupivacaine and 0.036 mg epinephrine
5 cartridges = 45 mg bupivacaine and 0.045 mg epinephrine
6 cartridges = 54 mg bupivacaine and 0.054 mg epinephrine
7 cartridges = 63 mg bupivacaine and 0.063 mg epinephrine
8 cartridges = 72 mg bupivacaine and 0.072 mg epinephrine
9 cartridges = 81 mg bupivacaine and 0.081 mg epinephrine
10 cartridges = 90 mg bupivacaine and 0.090 mg epinephrine
Note: Adult and children doses of bupivacaine hydrochloride with
epinephrine cited from USP Dispensing Information (USP DI), 17th ed, The United
States Pharmacopeial Convention, Inc, Rockville, MD, 1997, 134.
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Dietary
Considerations |
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No data reported |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Dosage Forms |
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Injection: Bupivacaine hydrochloride 0.5% with epinephrine 1:200,000 (1.8 mL
cartridges in boxes of 50) |
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References |
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Ayoub ST and Coleman AE, "A Review of Local Anesthetics," Gen Dent,
1992, 40(4):285-7, 289-90.
Jastak JT and Yagiela JA,
"Vasoconstrictors and Local Anesthesia: A Review and Rationale for Use," J Am
Dent Assoc, 1983, 107(4):623-30.
MacKenzie TA and Young ER, "Local Anesthetic Update," Anesth Prog,
1993, 40(2):29-34.
Wynn RL, "Epinephrine Interactions With Beta-Blockers," Gen Dent,
1994, 42(1):16, 18.
Yagiela JA, "Local Anesthetics," Anesth Prog, 1991, 38(4-5):128-41.
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