septocaine- Articaine hydrochloride and epinephrine bitartrate injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Articaine Hydrochloride (UNII: QS9014Q792) (articaine - UNII:D3SQ406G9X), Epinephrine bitartrate (UNII: 30Q7KI53AK) (epinephrine - UNII:YKH834O4BH)

Available from:

SEPTODONT, Inc.

INN (International Name):

Articaine hydrochloride and epinephrine bitartrate

Pharmaceutical form:

INJECTION, SOLUTION

Composition:

40 mg in 1 mL

Administration route:

SUBCUTANEOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Septocaine® is indicated for local, infiltrative, or conductive anesthesia in both simple and complex dental and periodontal procedures. Septocaine® is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type, or in patients with known hypersensitivity to sodium metabisulfite.

Product summary:

Septocaine® (articaine HCl 4% with epinephrine 1:100,000 Injection) is available in 1.7 mL glass cartridges, in boxes or cans of 50 cartridges. The product is formulated with a 15% overage of epinephrine. NDC 12862-1050-1 Can of 50 cartridges NDC 12862-1050-2 Box of 50 cartridges Store at 25°C (77°F) with brief excursions permitted between 15° and 30°C (59°F-86°F) (see USP controlled room temperature). Protect from light.

Summary of Product characteristics

SEPTOCAINE- ARTICAINE HYDROCHLORIDE AND EPINEPHRINE BITARTRATE
INJECTION, SOLUTION
SEPTODONT, INC.
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SEPTOCAINE
(ARTICAINE HYDROCHLORIDE 4% (40 MG/ML)
WITH EPINEPHRINE 1:100,000 INJECTION)
FOR INFILTRATION AND NERVE BLOCK ANESTHESIA
DESCRIPTION
Septocaine
injection is a sterile, aqueous solution that contains articaine HCl
4% (40mg/mL) with
epinephrine bitartrate in a 1:100,000 strength. Articaine HCl is a
local anesthetic, which is chemically
designated as
4-methyl-3-[2-(propylamino)-propionamido]-2-thiophene-carboxylic acid,
methyl ester
hydrochloride and is a racemic mixture. Articaine HCl has a molecular
weight of 320.84 and the
molecular and structural formulae are displayed below :
Articaine HCl has a partition coefficient in n-octanol/ Soerensen
buffer (pH : 7.35) of 17 and a pKa of
7.8.
Epinephrine bitartrate,
(-)-1-(3,4-Dihydroxyphenyl)-2-methylamino-ethanol (+) tartrate (1:1)
salt, is a
vasoconstrictor that is added to articaine HCl in a concentration of
1:100,000 as the free base. It has a
molecular weight of 333.3. The molecular and structural formulae are
displayed below:
Septocaine
contains articaine HCl (40mg/mL), epinephrine as bitartrate
(1:100,000), sodium chloride
(1.6 mg/mL), and sodium metabisulfite (0.5 mg/mL). The product is
formulated with a 15% overage of
epinephrine. The pH is adjusted to 5.0 with sodium hydroxide.
®
®
®
CLINICAL PHARMACOLOGY
PHARMACOKINETICS
Absorption
Following dental injection by the submucosal route of an articaine
solution containing 1:200,000
epinephrine, articaine reaches peak blood concentration about 25
minutes after a single dose injection
and 48 minutes after three doses. Peak plasma levels of articaine
achieved after 68 and 204 mg doses
are 385 and 900 ng/mL, respectively.
Distribution
Approximately 60 to 80% of articaine HCl is bound to human serum
albumin and γ-globulins at 37°C in
vitro.
Metabolism
Articaine HCl is rapidly metabolized by plasma carboxyesterase to its
primary metabolite, articainic
acid, which is inactive. In vitro studies sho