Fossaoprin SPG2 Injection System

Name: Fossaoprin SPG2 Injection System

LIDOCAINE HYDROCHLORIDE- lidocaine hydrochloride injection, solution

AQUEOUS SOLUTIONS FOR
INFILTRATION AND NERVE BLOCK
Ampul
Plastic Multiple-dose Fliptop Vial
Glass Teartop Vial

Rx only

Clinical pharmacology

.1 Mechanism of action

Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

.2 Hemodynamics

Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial pressure. With central neural blockade these changes may be attributable to block of autonomic fibers, a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system and/or the beta-adrenergic receptor stimulating action of epinephrine when present. The net effect is normally a modest hypotension when the recommended dosages are not exceeded.

.3 Pharmacokinetics and metabolism

Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent. Except for intravascular administration, the highest blood levels are obtained following intercostal nerve block and the lowest after subcutaneous administration.

The plasma binding of lidocaine is dependent on drug concentration, and the fraction bound decreases with increasing concentration. At concentrations of 1 to 4 mcg of free base per mL, 60 to 80 percent of lidocaine is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein.

Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.

Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine. Approximately 90% of lidocaine administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2, 6-dimethylaniline.

The elimination half-life of lidocaine following an intravenous bolus injection is typically 1.5 to 2.0 hours. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged two-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites.

Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6.0 mcg free base per mL. In the rhesus monkey arterial blood levels of 18–21 mcg/mL have been shown to be threshold for convulsive activity.

Indications and usage

Lidocaine Hydrochloride Injection, USP is indicated for production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks, when the accepted procedures for these techniques as described in standard textbooks are observed.

0 how supplied

Lidocaine Hydrochloride Injection, USP is supplied as follows:

Unit of Sale Concentration Each
Multiple-dose:  
NDC 0409-4277-02
Tray of 25
 2%
1000 mg/50 mL
(20 mg/mL)
NDC 0409-4277-17
Plastic Fliptop Vial

Store at 20 to 25°C (68 to 77°F). [see USP Controlled Room Temperature.]

Lidocaine Hydrochloride Injection, USP solutions packaged in ampuls and glass teartop vials may be autoclaved one time only. Autoclave at 15 pounds pressure, 121°C (250°F) for 15 minutes. DO NOT AUTOCLAVE PRODUCT IN PLASTIC VIALS.

LAB-1118-2.0

01/2018

Fossaoprin SPG2 Injection System Description

Bupivacaine hydrochloride is 2-Piperidinecarboxamide, 1-butyl-N-(2,6-dimethylphenyl)-, 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:

Epinephrine is (-)-3,4-Dihydroxy-α-[(methylamino)methyl] benzyl alcohol. It has the following structural formula:

MARCAINE is available in sterile isotonic solutions with and without epinephrine (as bitartrate) 1:200,000 for injection via local infiltration, peripheral nerve block, and caudal and lumbar epidural blocks. Solutions of MARCAINE may be autoclaved if they do not contain epinephrine. Solutions are clear and colorless.

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.

MARCAINESterile isotonic solutions containing sodium chloride. In multiple-dose vials, each mL also contains 1 mg methylparaben as antiseptic preservative. The pH of these solutions is adjusted to between 4 and 6.5 with sodium hydroxide or hydrochloric acid.

MARCAINE with epinephrine 1:200,000 (as bitartrate)Sterile isotonic solutions containing sodium chloride. Each mL contains bupivacaine hydrochloride and 0.0091 mg epinephrine bitartrate, with 0.5 mg sodium metabisulfite, 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. In multiple-dose vials, each mL also contains 1 mg methylparaben as antiseptic preservative. The pH of these solutions is adjusted to between 3.4 and 4.5 with sodium hydroxide or hydrochloric acid. The specific gravity of MARCAINE 0.5% with epinephrine 1:200,000 (as bitartrate) at 25°C is 1.008 and at 37°C is 1.008.

Indications and Usage for Fossaoprin SPG2 Injection System

MARCAINE is indicated for the production of local or regional anesthesia or analgesia for surgery, dental and oral surgery procedures, diagnostic and therapeutic procedures, and for obstetrical procedures. Only the 0.25% and 0.5% concentrations are indicated for obstetrical anesthesia. (See WARNINGS.)

Experience with nonobstetrical surgical procedures in pregnant patients is not sufficient to recommend use of 0.75% concentration of MARCAINE in these patients.

MARCAINE is not recommended for intravenous regional anesthesia (Bier Block). See WARNINGS.

The routes of administration and indicated MARCAINE concentrations are:

• local infiltration                                          0.25% • peripheral nerve block                                0.25% and 0.5% • retrobulbar block                                        0.75% • sympathetic block                                      0.25% • lumbar epidural                                          0.25%, 0.5%, and 0.75%
                                                                   (0.75% not for obstetrical anesthesia) • caudal                                                         0.25% and 0.5% • epidural test dose                                       0.5% with epinephrine 1:200,000 • dental blocks                                              0.5% with epinephrine 1:200,000

(See DOSAGE AND ADMINISTRATION for additional information).

Standard textbooks should be consulted to determine the accepted procedures and techniques for the administration of MARCAINE.

How is Fossaoprin SPG2 Injection System Supplied

These solutions are not for spinal anesthesia.

Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]

MARCAINE―Solutions of MARCAINE that do not contain epinephrine may be autoclaved. Autoclave at 15-pound pressure, 121°C (250°F) for 15 minutes.

Unit of Sale Concentration Each
                                                 0.5% Contains 5 mg bupivacaine hydrochloride per mL.
 NDC 0409-1610-50

Carton of 1

250 mg/50 mL

(5 mg/mL)

NDC 0409-1610-50

Multiple-dose vial

LAB-1178-1.0

Revised: 11/2017

Packaging-kit components labeling

FOSSAOPRIN SPG2 
lidocaine hydrochloride, bupivacaine hydrochloride kit
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:70529-016
Packaging
# Item Code Package Description
1 NDC:70529-016-01 1 KIT in 1 PACKAGE
Quantity of Parts
Part # Package Quantity Total Product Quantity
Part 1 1 VIAL, MULTI-DOSE 50 mL
Part 2 1 VIAL, MULTI-DOSE 50 mL
Part 3 4 PACKET 4 mL
Part 1 of 3
LIDOCAINE HYDROCHLORIDE 
lidocaine hydrochloride injection, solution
Product Information
Item Code (Source) NDC:0409-4277
Route of Administration INFILTRATION, PERINEURAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
LIDOCAINE HYDROCHLORIDE (LIDOCAINE) LIDOCAINE HYDROCHLORIDE ANHYDROUS 20 mg  in 1 mL
Inactive Ingredients
Ingredient Name Strength
SODIUM CHLORIDE 6 mg  in 1 mL
WATER  
SODIUM HYDROXIDE  
HYDROCHLORIC ACID  
METHYLPARABEN 1 mg  in 1 mL
Packaging
# Item Code Package Description
1 50 mL in 1 VIAL, MULTI-DOSE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA088327 06/15/2005
Part 2 of 3
MARCAINE 
bupivacaine hydrochloride injection, solution
Product Information
Item Code (Source) NDC:0409-1610
Route of Administration PERINEURAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
BUPIVACAINE HYDROCHLORIDE (BUPIVACAINE) BUPIVACAINE HYDROCHLORIDE ANHYDROUS 5 mg  in 1 mL
Inactive Ingredients
Ingredient Name Strength
SODIUM CHLORIDE  
SODIUM HYDROXIDE  
HYDROCHLORIC ACID  
METHYLPARABEN  
WATER  
Packaging
# Item Code Package Description
1 50 mL in 1 VIAL, MULTI-DOSE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA016964 11/30/2005
Part 3 of 3
MCKESSON ALCOHOL PREP PAD 
isopropyl alcohol swab
Product Information
Item Code (Source) NDC:68599-5804
Route of Administration TOPICAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
ISOPROPYL ALCOHOL (ISOPROPYL ALCOHOL) ISOPROPYL ALCOHOL 0.7 mL  in 1 mL
Inactive Ingredients
Ingredient Name Strength
WATER  
Packaging
# Item Code Package Description
1 1 mL in 1 PACKET
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
OTC monograph not final part333A 04/09/2010
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA088327 03/01/2017
Labeler - IT3 Medical LLC (079971231)
  IT3 Medical LLC

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