Overview
11 DESCRIPTION Fentanyl Citrate Injection, USP, is an opioid agonist, available as a sterile, non-pyrogenic solution containing fentanyl citrate as the active pharmaceutical ingredient, for intravenous or intramuscular administration. Fentanyl citrate is chemically identified as N -(1-Phenethyl-4-piperidyl)propionanilide citrate (1:1) with the following structural formula: C 22 H 28 N 2 O • C 6 H...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Fentanyl Citrate Injection is an opioid agonist, whose principal actions of therapeutic value are analgesia and sedation. 12.2 Pharmacodynamics Effects on the Central Nervous System Fentanyl produces respiratory depression by direct action on brain stem respiratory centers. The respiratory depression involves a reduction in the responsiveness of the brain stem respiratory centers to both increases in carbon dioxide tension and electrical stimulation. Fentanyl causes miosis, even in total darkness. Pinpoint pupils are a sign of opioid overdose but are not pathognomonic (e.g., pontine lesions of hemorrhagic or ischemic origins may produce similar findings). Marked mydriasis rather than miosis may be seen due to hypoxia in overdose situations.
Indications
- 1 INDICATIONS AND USAGE Fentanyl Citrate Injection is indicated for: • analgesic action of short duration during the anesthetic periods, premedication, induction and maintenance, and in the immediate postoperative period (recovery room) as the need arises. • use as a narcotic analgesic supplement in general or regional anesthesia. • administration with a neuroleptic as an anesthetic premedication, for the induction of anesthesia and as an adjunct in the maintenance of general and regional anesthesia.
Common Doses
- 50 mcg
- 100 mcg
- 2 mcg
- 3 mcg
Dosage
2 DOSAGE AND ADMINISTRATION • Fentanyl Citrate Injection should be administered only by persons specifically trained in the use of intravenous anesthetics and management of the respiratory effects of potent opioids. • Ensure that an opioid antagonist, resuscitative and intubation equipment, and oxygen are readily available ( 2.1 ). • Individualize dosing based on the factors such as age, body weight, physical status, underlying pathological condition, use of other drugs, type of anesthesia to be used, and the surgical procedure involved. ( 2.
Black Box Warning
WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF FENTANYL CITRATE INJECTION Addiction, Abuse, and Misuse Because the use of Fentanyl Citrate Injection exposes patients and other users to the risks of opioid addiction, abuse and misuse, which can lead to overdose and death, assess each patient’s risk prior to prescribing and reassess all patients regularly for the development of these behaviors and conditions [see Warnings and Precautions ( 5.1 )].
Contraindications
- 4 CONTRAINDICATIONS Fentanyl Citrate Injection is contraindicated in patients with: • Hypersensitivity to fentanyl (e.g., anaphylaxis) [See Adverse Reactions ( 6 )] • Hypersensitivity to fentanyl ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following serious adverse reactions are described, or described in greater detail, in other sections: • Addiction, Abuse, and Misuse [see Warnings and Precautions ( 5.1 )] • Life-Threatening Respiratory Depression [see Warnings and Precautions ( 5.2 )] • Interactions with Benzodiazepines and Other CNS Depressants [see Warnings and Precautions ( 5.3 )] • Severe Cardiovascular Depression [see Warnings and Precautions ( 5.6 )] • Opioid-Induced Hyperalgesia and Allodynia [see Warnings and Precautions ( 5.7 )] • Serotonin Syndrome [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS Table 2 includes clinically significant drug interactions with Fentanyl Citrate Injection. Table 2: Clinically Significant Drug Interactions with Fentanyl Citrate Injection Inhibitors of CYP3A4 Clinical Impact: The concomitant use of Fentanyl Citrate Injection and CYP3A4 inhibitors can increase the plasma concentration of fentanyl, resulting in increased or prolonged opioid effects, particularly when an inhibitor is added after a stable dose of Fentanyl Citrate Injection is achieved [see Warnings and Precautions ( 5.4 )] .