Fentanyl — brand names include Sublimaze, Actiq, Durogesic, Duragesic, Fentora, Onsolis, and Instanyl — is a synthetic primary μ-opioid agonist and a potent narcotic analgesic with a short duration of action and rapid onset. Historically it has been used to treat chronic breakthrough pain and is commonly used in pre-procedures. More recently fentanyl has been used for primary pain relief in patch form.
Fentanyl is approximately 100 times more potent than morphine, with 100 micrograms of Fentanyl approximately equivalent to 10 mg of morphine and 75 mg of pethidine (meperidine) in analgesic activity. It has an LD50 of 3.1 milligrams per kilogram in rats, 0.03 milligrams per kilogram in monkeys, and an undetermined LD50 in humans.
Fentanyl was first synthesized by Dr. Paul Janssen in 1960 following the medical inception of pethedine several years earlier. Janssen developed fentanyl by assaying analogues of the structurally-related drug pethedine for its opioid activity. The widespread use of fentanyl triggered the production of fentanyl citrate (fentanyl combined with citrate at a 1:1 ratio), which entered the clinical practice as a general anaesthetic under the trade name Sublimaze in the 1960s. Following this, many other fentanyl analogs were developed and introduced into the medical practice, including Sufentanil, Alfentanil, Remifentanil, and Lofentanil.
In the mid 1990s, fentanyl saw its first widespread palliative use with the clinical introduction of the Duragesic patch, followed in the next decade by the introduction of the first quick-acting prescription formations of fentanyl for personal use, the Actiq lollipop and Fentora buccal tablets. Through the delivery method of transdermal patches, fentanyl is currently the most widely used synthetic opioid in clinical practice, with several new delivery methods currently in development.
A number of fatal fentanyl overdoses have been directly tied to the drug over the past several years. In particular, manufacturers of time-release fentanyl patches have come under scrutiny for defective products. While the fentanyl contained in the patches was safe, a malfunction of the patches caused an excessive amount of fentanyl to leak and to be absorbed by patients, resulting in life-threatening side effects and even death.
Manufacturers of fentanyl transdermal pain patches have voluntarily recalled numerous lots of their patches, and the U.S. Food and Drug Administration (FDA) has issued Public Health Advisories related to the fentanyl patch dangers. Manufacturers affected include Janssen Pharmaceutica Products, L.P.; Alza Corporation; Actavis South Atlantic, LLC; Sandoz; and Cephalon, Inc.
On June 19, 2007, a US$5.5 million jury verdict was awarded in a case against Johnson & Johnson subsidiaries Alza Corporation and Janssen Pharmaceutica Products, the manufacturers of the Duragesic fentanyl transdermal pain patch. This case, the first federal trial involving a fentanyl patch, was tried in the Federal District Court for the Southern District of Florida, West Palm Beach Division. Led by attorney Jim Orr, the Dallas, Texas-based law firm Heygood, Orr, Reyes, Pearson & Bartolomei (now Heygood, Orr & Pearson) achieved the verdict for the family of Adam Hendelson, a 28-year-old Florida man, who died while wearing a fentanyl transdermal pain patch.
On November 17, 2008, lead attorneys Jim Orr and Michael Heygood won a case against Johnson & Johnson subsidiaries Alza Corporation and Janssen Pharmaceutica Products in a Cook County Circuit Court, achieving a US$16.5 million jury verdict for the family of 38-year-old Janice DiCosolo, a mother of three who died while wearing the patch in 2004.
Numerous documents from the Dicosolo case and others have been posted in PDF format at the website DangerousDrugs.US
Further Reading
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