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Bupivacaine and Epinephrine (Dental)
Pronunciation
U.S. Brand Names
Generic Available
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Dosage Forms
References

Pronunciation
(byoo PIV a kane & ep i NEF rin)

U.S. Brand Names
Marcaine® with Epinephrine

Generic Available

Yes


Pharmacological Index

Local Anesthetic


Use

Dental and Medical: Local anesthesia


Pregnancy Risk Factor

C


Contraindications

Hypersensitivity to bupivacaine


Warnings/Precautions

Should be avoided in patients with uncontrolled hyperthyroidism


Adverse Reactions

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.


Drug Interactions

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


Mechanism of Action

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.


Pharmacodynamics/Kinetics

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


Usual Dosage

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.


Dietary Considerations

No data reported


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Dosage Forms

Injection: Bupivacaine hydrochloride 0.5% with epinephrine 1:200,000 (1.8 mL cartridges in boxes of 50)


References

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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