Fentanyl Citrate (11 brand names, 6 dosage forms, 8 routes)
Available dosage forms: INJECTABLE, TABLET, FILM, TROCHE/LOZENGE, SOLUTION, SPRAY, METERED.
Routes of administration: INJECTION, BUCCAL, SUBLINGUAL, BUCCAL, TRANSMUCOSAL, INTRAVENOUS, ORAL, NASAL, SUBLINGUAL.
Brand Names
- ABSTRAL
- ACTIQ
- FENTANYL
- FENTANYL CITRATE
- FENTANYL CITRATE AND DROPERIDOL
- FENTANYL CITRATE PRESERVATIVE FREE
- FENTORA
- INNOVAR
- LAZANDA
- ONSOLIS
- SUBLIMAZE PRESERVATIVE FREE
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 an opioid 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. •use as an anesthetic agent with oxygen in selected high-risk patients, such as those undergoing open heart surgery or certain complicated neurological or orthopedic procedures.
Contraindications
Fentanyl Citrate Injection is contraindicated in patients with: •Hypersensitivity to fentanyl (e.g., anaphylaxis) [see Adverse Reactions (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 or 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 (5.8)] •Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.11) ] •Seizures [see Warnings and Precautions (5.12) ] The following adverse reactions associated with the use of fentanyl were identified in clinical studies or postmarketing reports. Because some of these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. As with other opioid agonists, the most common serious adverse reactions reported to occur with fentanyl are respiratory depression, apnea, rigidity, and bradycardia; if these remain untreated, respiratory arrest, circulatory depression or cardiac arrest could occur. Other adverse reactions that have been reported are hypertension, hypotension, dizziness, blurred vision, nausea, emesis, diaphoresis, pruritus, urticarial, laryngospasm, and anaphylaxis. It has been reported that secondary rebound respiratory depression may occasionally occur postoperatively. When a tranquilizer is used with fentanyl, the following adverse reactions can occur: chills and/or shivering, restlessness, and postoperative hallucinatory episodes (sometimes associated with transient periods of mental depression); extrapyramidal symptoms (dystonia, akathisia, and oculogyric crisis) have been observed up to 24 hours postoperatively. When they occur, extrapyramidal symptoms can usually be cont
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) ]. After stopping a CYP3A4 inhibitor, as the effects of the inhibitor decline, the fentanyl plasma concentration will decrease [see Clinical Pharmacology (12.3)], resulting in decreased opioid efficacy or a withdrawal syndrome in patients who had developed physical dependence to fentanyl. Intervention: If concomitant use is necessary, consider dosage reduction of Fentanyl Citrate Injection until stable drug effects are achieved [see Dosage and Administration (2)]. Monitor patients for respiratory depression and sedation at frequent intervals. If a CYP3A4 inhibitor is discontinued, consider increasing the Fentanyl Citrate Injection dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal. Examples: Macrolide antibiotics (e.g., erythromycin), azole-antifungal agents (e.g., ketoconazole), protease inhibitors (e.g., ritonavir), grapefruit juice. CYP3A4 Inducers Clinical Impact: The concomitant use of Fentanyl Citrate Injection and CYP3A4 inducers can decrease the plasma concentration of fentanyl [see Clinical Pharmacology (12.3)], resulting in decreased efficacy or onset of a withdrawal syndrome in patients who have developed physical dependence to fentanyl [see Warnings and Precautions (5.4) ]. After stopping a CYP3A4 inducer, as the effects of the inducer decline, the fentanyl plasma concentration will increase [see Clinical Pharmacology (12.3)], which could increase or prolong both the therapeutic effects and adverse reactio
Mechanism of Action
Fentanyl is an opioid agonist whose principal actions of therapeutic value are analgesic and sedation.