Fentanyl

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Abstral, Actiq, Durogesic, Effentora, Ernsdolor, Fentamed, Fentanyl, Fentaplast, Fentarichtex, Fentoron, Gelitanyl, Instanyl, Ionsys (d), Matrifen; Belgium: Durogesic, Fentanyl, Matrifen; Bulgaria: Dolforin, Durogesic, Fentanyl, Victanyl; Cyprus: Durogesic, Fentanyl, Ionsys (d), Matrifen; Czech Republic: Dolforin, Durogesic, Effentora, Fentagesic, Fentalis, Fentanyl, Instanyl, Matrifen, Tocril; Denmark: Actiq, Durogesic, Fentanyl, Haldid, Instanyl, Matrifen; Estonia: Dolforin, Durogesic, Effentora, Fentanyl, Instanyl, Lunaldin, Matrifen; Finland: Durogesic, Fentanyl, Matrifen; France: Abstral, Actiq, Durogesic, Fentanyl, Matrifen; Germany: Abstral, Actiq, Durogesic, Effentora, Fentaderm, Fentadolon, Fentaduplo, Fentamat, Fentamedica, Fentanyl, Fentapatch, Fentaquick, Fentareu, Fentavera, Instanyl, Matrifen; Greece: Abstral, Actiq, Demogyl, Dolfen, Durogesic, Fentadur, Fentanyl, Ionsys (d), Meganyl, Matrifen, Myfene; Hungary: Dolorfin, Durogesic, Fentanil, Fentanyl, Fentawin, Instanyl, Lunaldin, Matrifen, Sedaton; Ireland: Abstral, Actiq, Durogesic, Effentora, Fental Matrix, Fentanex, Fentanyl, Instanyl, Matrifen, Mytanyl, Sublimaze; Italy: Actiq, Durogesic, Fentanest, Fentanil, Fentanyl, Matrifen, Quatrofen; Latvia: Dolforin, Durogesic, Effentora, Fentanils, Fentanyl, Instanyl, Ionsys (d), Matrifen, Rapinyl; Lithuania: Dolforin, Durogesic, Effentora, Fentanilis, Fentanyl, Instanyl, Lunaldin, Matrifen, Tocril; Malta: Durogesic, Fentanyl; Netherlands: Actiq, Durogesic, Effentora, Fentanyl, Instanyl; Poland: Dolforin, Durogesic, Effentora, Fenta MX, Fentagesic, FentaHexal, Fentanyl, Fentawin, Matrifen, Rapinyl; Portugal: Abstral, Actiq, Durogesic, Effentora, Fentanest, Fentanil, Fentanilo, Instanyl, Nilfene; Romania: Dolforin, Durogesic, Effentora, Fentanyl, Instanyl, Ionsys (d); Slovakia: Adolor, Dolforin, Durogesic, Effentora, Fentasan, Fentanyl, Instanyl, Lunaldin, Matrifen, Rapinyl; Slovenia: Durogesic, Epufen, Fentanil, Fentanyl, Lefen, Matrifen, Tocril, Victanyl; Spain: Actiq, Durogesic, Fendivia, Fentanest, Fentanilo, Matrifen; Sweden: Abstral, Actiq, Durogesic, Effentora, Fentanyl, Instanyl, Ionsys (d), Matrifen, Matrimed, Nycofen, Quatrofen; UK: Abstral, Actiq, Durogesic, Effentora, Fentalis, Fentanyl, Instanyl, Matrifen, Mezolar, Osmanil, Sublimaze, Victanyl.

North America

Canada: Duragesic, Fentanyl; USA: Actiq, Duragesic, Fentora, Onsolis, Sublimaze.

Latin America

Argentina: Durogesic, Fentanilo, Fentax, Nafluvent, Sublimaze, Talnur; Brazil: Durogesic, Fentabbott, Fentanest, Fentatil, Unifental; Mexico: Durogesic, Fenodid, Fentanest, Filtaten.

Asia

Japan: Durotep, Fentanyl.

Drug combinations

Fentanyl and Droperidol

Chemistry

Fentanyl: C~22~H~28~N~2~O. Mw: 336.47. (1) Propanamide, N-phenyl-N-[1-(2-phenylethyl)-4-piperidinyl]; (2) N-(1-Phenethylpiperidin-4-yl)-N-phenylpropionamide. CAS-437-38-7 (2006).

Fentanyl Citrate: C~22~H~28~N~2~O C~6~H~8~O~7~. Mw: 528.59. N-(1-Phenethyl-4-piperidyl)propionanilide citrate (1:1). CAS-990-73-8 (1963).

Pharmacologic Category

Analgesics and Antipyretics; Opiate Agonists. (ATC-Code: N01AH01; N02AB03).

Mechanism of action

A synthetic phenylpiperidine-derivative opiate agonist. Binds with stereospecific receptors at many sites within the CNS, increases pain threshold, alters pain reception, inhibits ascending pain pathways.

Therapeutic use

Sedation, relief of pain, preoperative medication, adjunct to general or regional anesthesia. Management of persistent moderate-to-severe chronic pain. Management of breakthrough cancer pain in opioid-tolerant patients. Prevention or relief of tachypnea and postoperative emergence delirium. Adjunct in preoperative intravenous conscious sedation in patients undergoing dental surgery.

Pregnancy and lactiation implications

Fentanyl crosses the placenta and has been used safely during labor. Excreted in low concentrations into breast milk. Breast-feeding is considered acceptable following single doses to the mother (no information available when used long-term).

Unlabeled use

Contraindications

Hypersensitivity to fentanyl or any component of the formulation. Severe respiratory disease or depression including acute asthma (unless mechanically ventilated). Paralytic ileus. Patients requiring short-term therapy, management of intermittent pain. Management of acute or postoperative pain and in opioid-nontolerant patients.

Warnings and precautions

Shares the toxic potentials of opiate agonists. Opioid-nontolerant patients should not receive some formulations/strengths of fentanyl. May cause potentially life-threatening hypoventilation, respiratory depression, and/or death. Increased risk of respiratory depression in elderly or debilitated patients, and conditions associated with hypoxia or hypercapnia. Use with caution when administering to patients with bradycardia or bradyarrhythmias. Use with caution in history of drug abuse or acute alcoholism (tolerance, psychological and physical dependence may occur with prolonged use). Use with extreme caution in head injury, intracranial lesions, or elevated intracranial pressure (exaggerated elevation of intracranial pressure may occur). Use with caution in hepatic dysfunction, in renal impairment, or in pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function (critical respiratory depression may occur). Use with strong or moderate CYP3A4 inhibitors may result in increased effects and potential respiratory depression. Use with caution in the elderly (may be more sensitive to adverse effects). Injection may cause muscle rigidity; respiratory depression may persist beyond analgesic effect. Buccal tablet and lozenge preparations contain an amount of medication that can be fatal to children. Rapid I.V. infusion may result in skeletal muscle and chest wall rigidity, impaired ventilation, or respiratory distress/arrest. Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in prolonged therapy with μ-opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.

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