DEMEROL (Page 7 of 10)
12.3 Pharmacokinetics
Elimination
The half-life of meperidine is 2 to 5 hours, and the half-life of normeperidine is 15 to 30 hours.
Metabolism
Meperidine is metabolized through biotransformation. In vitro data show meperidine is metabolized to normeperidine in liver mainly by CYP3A4 and CYP2B6.
Hepatic Impairment
The elimination half-life is 3 to 8 hours in healthy volunteers and is 1.3 to 2 times greater in post-operative or cirrhotic patients.
Excretion
Meperidine and normeperidine are excreted by kidneys.
Age
In clinical studies reported in the literature, changes in several pharmacokinetic parameters with increasing age have been observed. The initial volume of distribution and steady-state volume of distribution may be higher in elderly patients than in younger patients. The free fraction of meperidine in plasma may be higher in patients over 45 years of age than in younger patients.
Drug Interactions Studies
Phenytoin: The hepatic metabolism of meperidine may be enhanced by phenytoin. Concomitant administration resulted in reduced half-life and bioavailability with increased clearance of meperidine in healthy subjects; however, blood concentrations of normeperidine were increased [see Drug Interactions (7)].
Ritonavir: Plasma concentrations of the active metabolite normeperidine may be increased by ritonavir [see Drug Interactions (7)].
Acyclovir: Plasma concentrations of meperidine and its metabolite, normeperidine, may be increased by acyclovir [see Drug Interactions (7)].
Cimetidine: Cimetidine reduced the clearance and volume of distribution of meperidine and also the formation of the metabolite, normeperidine, in healthy subjects [see Drug Interactions (7)].
13 NONCLINICAL TOXICOLOGY
13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility
Carcinogenesis
Long-term studies in animals to evaluate the carcinogenic potential of meperidine have not been conducted.
Mutagenesis
Studies in animals to evaluate the mutagenic potential of meperidine have not been conducted.
Impairment of Fertility
Studies to determine the effect of meperidine on fertility have not been conducted.
16 HOW SUPPLIED/STORAGE AND HANDLING
For Parenteral Use
DEMEROL (meperidine hydrochloride injection), for subcutaneous, intramuscular, and intravenous use, is clear and colorless, and available as follows:
| Unit of Sale | Concentration (per total volume) |
|---|---|
| NDC 0409-1181-30 Carton of 130 mL fill in 30 mL Multiple-dose Vial | 1,500 mg/30 mL(50 mg/mL) |
| NDC 0409-1176-30 Carton of 101 mL fill in 2.5 mL Carpuject Single-dose cartridge with Luer Lock | 25 mg/mL |
| NDC 0409-1178-30 Carton of 101 mL fill in 2.5 mL Carpuject Single-dose cartridge with Luer Lock | 50 mg/mL |
| NDC 0409-1179-30 Carton of 101 mL fill in 2.5 mL Carpuject Single-dose cartridge with Luer Lock | 75 mg/mL |
| NDC 0409-1180-69 Carton of 101 mL fill in 2.5 mL Carpuject Single-dose cartridge with Luer Lock | 100 mg/mL |
| NDC 0409-1362-01 Clamshell of 101 mL fill in 1.5 mL NexJect™ Single-dosePrefilled Syringe with Luer Lock | 25 mg/mL |
| NDC 0409-1418-01 Clamshell of 101 mL fill in 1.5 mL NexJect™ Single-dosePrefilled Syringe with Luer Lock | 50 mg/mL |
| NDC 0409-2033-01 Clamshell of 101 mL fill in 1.5 mL NexJect™ Single-dosePrefilled Syringe with Luer Lock | 75 mg/mL |
| NDC 0409-1377-01 Clamshell of 101 mL fill in 1.5 mL NexJect™ Single-dosePrefilled Syringe with Luer Lock | 100 mg/mL |
Carpuject Single-dose cartridge are packaged in a Slim-Pak tamper detection package. Note that a needle is not included.
Carpuject and NexJectTM Single-dose products: Discard unused portion.
Multiple-dose vials: Discard unused portion after 28 days.
Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C to 30°C (59°F to 86°F). [See USP controlled room temperature.]
17 PATIENT COUNSELING INFORMATION
Serotonin Syndrome
Inform patients that opioids could cause a rare but potentially life-threatening condition resulting from concomitant administration of serotonergic drugs. Warn patients of the symptoms of serotonin syndrome and to seek medical attention right away if symptoms develop. Instruct patients to inform their health care provider if they are taking, or plan to take serotonergic medications [see Warnings and Precautions (5.7), Drug Interactions (7)].
Constipation
Advise patients of the potential for severe constipation, including management instructions and when to seek medical attention [see Adverse Reactions (6), Clinical Pharmacology (12.1)].
Distributed by Hospira, Inc., Lake Forest, IL 60045 USA
LAB-0846-7.0
INSTRUCTIONS FOR USE
To Use NexJect™ Syringe
NOTE: To prevent needlestick injuries, needles and blunt cannulas should not be recapped, purposely bent, or broken by hand.
Distributed by Hospira, Inc., Lake Forest, IL 60045 USA
LAB-1387-1.0
Revised: 9/2020
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