MARCAINE- bupivacaine hydrochloride and epinephrine bitartrate injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

BUPIVACAINE HYDROCHLORIDE ANHYDROUS (UNII: AKA908P8J1) (BUPIVACAINE - UNII:Y8335394RO), epinephrine bitartrate (UNII: 30Q7KI53AK) (epinephrine - UNII:YKH834O4BH)

Available from:

Septodont, Inc.

Administration route:

SUBMUCOSAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Marcaine® 0.5% (5 mg/mL) with epinephrine 1:200,000 injection is indicated for the production of local anesthesia for dental procedures by infiltration injection or nerve block in adults. Marcaine® 0.5% (5 mg/mL) with epinephrine 1:200,000 injection is not recommended for children. Marcaine® 0.5% (5 mg/mL) with epinephrine 1:200,000 injection, is contraindicated in patients with a known hypersensitivity to it or to any local anesthetic agent of the amide type or to other components of bupivacaine solutions.

Product summary:

Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.] Protect from light. Do not permit to freeze. Marcaine® 0.5% (5 mg/mL) with epinephrine 1:200,000 injection, (as bitartrate)–Sterile isotonic solutions containing sodium chloride. Each 1 mL contains 5 mg bupivacaine hydrochloride and 0.0091 mg epinephrine bitartrate, with 0.5 mg sodium metabisulfite, 7 mg sodium chloride, 0.001 mL monothioglycerol, and 2 mg ascorbic acid as antioxidants, 0.0017 mL 60% sodium lactate buffer, and 0.1 mg edetate calcium disodium as stabilizer. The pH of these solutions is adjusted with sodium hydroxide or hydrochloric acid. Solutions of bupivacaine that contain epinephrine should not be autoclaved and should be protected from light. Do not use the solution if its colour is pinkish or darker than slightly yellow or if it contains a precipitate. Marcaine® 0.5% (5 mg/mL) with epinephrine 1:200,000 injection (NDC 0362-0557-05) is available in cartons containing 5 blisters of 10 X 1.8 mL single-dose dental cartridges.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

MARCAINE- BUPIVACAINE HYDROCHLORIDE AND EPINEPHRINE BITARTRATE
INJECTION,
SOLUTION
SEPTODONT, INC.
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MARCAINE® 0.5% (5 MG/ML) WITH EPINEPHRINE 1:200,000 INJECTION (AS
BITARTRATE)
(BUPIVACAINE HYDROCHLORIDE AND EPINEPHRINE INJECTION, USP)
RX ONLY
THIS SOLUTION IS INTENDED FOR DENTAL USE.
DESCRIPTION
Bupivacaine hydrochloride is (±) -1-Butyl-2´, 6´-pipecoloxylidide
monohydrochloride,
monohydrate, a white crystalline powder that is freely soluble in 95
percent ethanol,
soluble in water, and slightly soluble in chloroform or acetone. It
has the following
structural formula:
MOLECULAR WEIGHT - 342.90 C
H N O • HCL • H O
Epinephrine bitartrate is
(-)-1-(3,4-Dihydroxyphenyl)-2-methylamino-ethanol (+) tartrate
(1:1) salt. It has the following structural formula:
MOLECULAR WEIGHT - 333.29 C
H NO
Bupivacaine is available in a sterile isotonic solution with
epinephrine 1:200,000 (as
bitartrate). Solutions of bupivacaine containing epinephrine may not
be autoclaved.
Bupivacaine is related chemically and pharmacologically to the
aminoacyl local
anesthetics. It is a homologue of mepivacaine and is chemically
related to lidocaine. All
three of these anesthetics contain an amide linkage between the
aromatic nucleus and
the amino or piperidine group. They differ in this respect from the
procaine-type local
anesthetics, which have an ester linkage.
CLINICAL PHARMACOLOGY
Bupivacaine stabilizes the neuronal membrane and prevents the
initiation and
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28
2
2
13
19
9
transmission of nerve impulses, thereby effecting local anesthesia.
The onset of action following dental injections is usually 2 to 10
minutes and anesthesia
may last two or three times longer than lidocaine and mepivacaine for
dental use, in
many patients up to 7 hours. The duration of anesthetic effect is
prolonged by the
addition of epinephrine 1:200,000.
It has also been noted that there is a period of analgesia that
persists after the return of
sensation, during which time the need for strong analgesic is reduced.
After injection of bupivacaine for c