Fentanyl Citrate (Page 7 of 7)

12.3 Pharmacokinetics

Fentanyl Citrate Injection is administered by the intravenous or intramuscular route. The pharmacokinetics of fentanyl can be described as a three-compartment model.

Distribution

Fentanyl plasma protein binding capacity decreases with increasing ionization of the drug. Alterations in pH may affect its distribution between plasma and the central nervous system. It accumulates in skeletal muscle and fat, and is released slowly into the blood. The volume of distribution for fentanyl is 4 L/kg. It has a distribution time of 1.7 minutes and redistribution time of 13 minutes.

Elimination

The terminal elimination half-life is 219 minutes.

Fentanyl, which is primarily transformed in the liver, demonstrates a high first pass clearance and releases approximately 75% of an intravenous dose in urine, mostly as metabolites with less than 10% representing the unchanged drug. Approximately 9% of the dose is recovered in the feces, primarily as metabolites.

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis

Long-term studies in animals to evaluate the carcinogenic potential of fentanyl citrate injection have not been conducted.

Mutagenesis

Studies in animals to evaluate the mutagenic potential of fentanyl have not been conducted.

Impairment of Fertility

Decreased pregnancy rates occurred in a multigenerational study in which pregnant rats were treated subcutaneously during the first 21 days of pregnancy with 160 mcg/kg to 1250 mcg/kg fentanyl (0.26 times to 2 times a human dose of 100 mcg/kg based on body surface area).

Studies in animals to characterize the effect of fentanyl on male fertility have not been conducted.

16 HOW SUPPLIED/STORAGE AND HANDLING

Fentanyl Citrate Injection, USP, equivalent to 50 mcg (0.05 mg) fentanyl base per mL, is a preservative-free solution, supplied as follows:

Unit of Sale	Total Strength/Total Volume (Concentration)
NDC 0409-1276-32 Carton of 102 mL fill in 2.5 mL Carpuject™ Single-dose cartridge with Luer Lock for the Carpuject™ Syringe System	100 mcg/2 mL(50 mcg/mL)

Carpuject™ Single-dose cartridges with Luer Lock are packaged in a Slim-Pak™ tamper detection package. Note that a needle is not included.

Instructions for Use of the Syringe Systems

Instructions for using the Carpuject™ Syringe are available with the reusable Carpuject™ Holder, List 2049-02.

Carpuject™ Single-dose cartridges are to be used ONLY with Carpuject™ Holders, List 2049-02.

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

Distributed by Hospira, Inc., Lake Forest, IL 60045 USA

LAB-0829-7.0

PRINCIPAL DISPLAY PANEL — 2 mL Cartridge Label

2 mL Single-use Carpuject™
Sterile Cartridge Unit with Luer Lock

NDC 0409-1276-03

Fentanyl Citrate Injection, USP
100 mcg Fentanyl / 2 mL
(50 mcg/mL)
CII

For Intravenous or Intramuscular Use
PROTECT FROM LIGHT.

Rx only

Distributed by Hospira, Inc., Lake Forest, IL 60045 USA

Hospira

PAA144187

LOT #####AA EXP DMMMYYYY

PRINCIPAL DISPLAY PANEL — 2 mL Cartridge Carton

NDC 0409-1276-32
Contains 10 of NDC 0409-1276-03
Rx only

2 mL Single-dose
10 Carpuject™
Sterile Cartridge Units
with Luer Lock

Needle not included

SLIM-PAK™
Tamper Detection Package

Fentanyl
Citrate
Injection,
USP
100 mcg Fentanyl / 2 mL
(50 mcg/mL)
CII

For Intravenous or
Intramuscular Use

Carpuject Cartridges are to be used ONLY with Carpuject Holders.

Hospira

FENTANYL CITRATE fentanyl citrate injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:0409-1276 Route of Administration INTRAMUSCULAR, INTRAVENOUS DEA Schedule CII

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength FENTANYL CITRATE (FENTANYL) FENTANYL 50 ug in 1 mL

Inactive Ingredients Ingredient Name Strength SODIUM HYDROXIDE

Packaging # Item Code Package Description Multilevel Packaging 1 NDC:0409-1276-32 10 CARTRIDGE in 1 CARTON contains a CARTRIDGE (0409-1276-03) 1 NDC:0409-1276-03 2 mL in 1 CARTRIDGE This package is contained within the CARTON (0409-1276-32)

Marketing Information Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date ANDA ANDA072786 07/20/2005

Labeler — Hospira, Inc. (141588017)

Establishment
Name	Address	ID/FEI	Operations
Hospira, Inc.		030606222	ANALYSIS (0409-1276), LABEL (0409-1276), MANUFACTURE (0409-1276), PACK (0409-1276)

Revised: 09/2023 Hospira, Inc.