Actiq

Actiq by Cephalon is a solid formulation of fentanyl citrate on a plastic stick that dissolves slowly in the mouth for absorption across the buccal mucosa. Generically Actiq is a form of oral transmucosal fentanyl citrate (OTFC). In the UK, fentanyl is a Class A drug under the Misuse of Drugs Act 1971. In the Netherlands, Fentanyl is a List I substance of the Opium Law. In the U.S., fentanyl is a Schedule II controlled substance per the Controlled Substance Act. Other pharmaceutical preparations consisting of fentanyl are Durogesic and Duragesic (72-hour continuous-release fentanyl patches) and Fentora, a rapidly dissolving fentanyl lozenge which, like Actiq, is administered transmucosally over the buccal mucosa. OTFC is absorbed much as nicotine is absorbed when dipping tobacco is placed in one's mouth between the gum and cheek.

An Actiq lozenge contains 2 grams of sugar (8 calories). The status of a sugar-free version, called Actiq-SF, is unclear. Since the release of Fentora—an effervescent buccal fentanyl tablet for breakthrough cancer pain—Cephalon has indefinitely postponed plans to release a sugar free version of Actiq.

Fentanyl

Fentanyl (also known as fentanil, brand names Sublimaze,Actiq, Durogesic, Duragesic, Fentora, Matrifen, Haldid, Onsolis, Instanyl,Abstral, Lazanda and others) is a potent, synthetic opioid analgesic with a rapid onset and short duration of action. It is a strong agonist at the μ-opioid receptors. Historically, it has been used to treat breakthrough pain and is commonly used in pre-procedures as a pain reliever as well as an anesthetic in combination with a benzodiazepine.

Fentanyl is approximately 80 to 100 times more potent than morphine and roughly 40 to 50 times more potent than pharmaceutical grade (100% pure) heroin.

Fentanyl was first synthesized by Paul Janssen in 1960, following the medical inception of pethidine (also known as meperidine, marketed as Demerol) several years earlier. Janssen developed fentanyl by assaying analogues of the structurally related drug pethidine for opioid activity. The widespread use of fentanyl triggered the production of fentanyl citrate (the salt formed by combining fentanyl and citric acid in a 1:1 stoichiometry), which entered the clinical practice as a general anaesthetic under the trade name Sublimaze in the 1960s. Following this, many other fentanyl analogues were developed and introduced into medical practice, including sufentanil, alfentanil, remifentanil, and lofentanil.