Actiq
Encyclopedia
Cephalon
Cephalon, Inc. is a U.S. biopharmaceutical company co-founded in 1987 by Dr. Frank Baldino, Jr., a pharmacologist and former scientist with the DuPont Company, who served as the company's chairman and chief executive officer until his death in December 2010...
, 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
Misuse of Drugs Act 1971
The Misuse of Drugs Act 1971 is an Act of Parliament which represents UK action in line with treaty commitments under the Single Convention on Narcotic Drugs, the Convention on Psychotropic Substances, and the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic...
. In the Netherlands, Fentanyl is a List I substance of the Opium Law. In the US, Fentanyl is a Schedule II controlled substance per the Controlled Substance Act. Other pharmaceutical preparations consisting of fentanyl are Durogesic and Duragesic
Duragesic
Duragesic and Durogesic are trade names of fentanyl transdermal therapeutic systems, and are used for relief of moderate to severe pain. Since Duragesic/Durogesic release Fentanyl, a potent opioid, slowly through the skin, one patch may provide 72 hours of pain relief...
(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
Nicotine
Nicotine is an alkaloid found in the nightshade family of plants that constitutes approximately 0.6–3.0% of the dry weight of tobacco, with biosynthesis taking place in the roots and accumulation occurring in the leaves...
is absorbed when dipping tobacco
Dipping tobacco
Dipping tobacco, traditionally referred to as moist snuff, is a type of finely ground or shredded, moistened smokeless tobacco product. It is commonly and idiomatically known by various terms – most often as dip and sometimes rub or chew...
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
Sugar
Sugar is a class of edible crystalline carbohydrates, mainly sucrose, lactose, and fructose, characterized by a sweet flavor.Sucrose in its refined form primarily comes from sugar cane and sugar beet...
-free version, called Actiq-SF, is unclear. Since the release of Fentora—an effervescent buccal fentanyl tablet for breakthrough cancer pain
Cancer pain
Pain is a symptom frequently associated with cancer. Cancer can cause pain by irritating or damaging nerves, by stimulating nociceptors , or by releasing chemicals that make nociceptors respond to normally non-painful stimuli. Cancer pain may be caused by the tumor itself or by medical...
—Cephalon has indefinitely postponed plans to release a sugar free version of Actiq.
Administration
Around 80 times more potent than morphineMorphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
, Actiq is intended for opiate
Opiate
In medicine, the term opiate describes any of the narcotic opioid alkaloids found as natural products in the opium poppy plant.-Overview:Opiates are so named because they are constituents or derivatives of constituents found in opium, which is processed from the latex sap of the opium poppy,...
-tolerant individuals and is effective in treating cancer breakthrough pain. However, it is often prescribed for "off-label use
Off-label use
Off-label use is the practice of prescribing pharmaceuticals for an unapproved indication or in an unapproved age group, unapproved dose or unapproved form of administration...
s", i.e. not for cancer patients, such as bone
Bone
Bones are rigid organs that constitute part of the endoskeleton of vertebrates. They support, and protect the various organs of the body, produce red and white blood cells and store minerals. Bone tissue is a type of dense connective tissue...
injuries, migraine
Migraine
Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
s, severe back pain
Back pain
Back pain is pain felt in the back that usually originates from the muscles, nerves, bones, joints or other structures in the spine.The pain can often be divided into neck pain, upper back pain, lower back pain or tailbone pain...
, cluster headache
Headache
A headache or cephalalgia is pain anywhere in the region of the head or neck. It can be a symptom of a number of different conditions of the head and neck. The brain tissue itself is not sensitive to pain because it lacks pain receptors. Rather, the pain is caused by disturbance of the...
s, neuropathy, arthritis
Arthritis
Arthritis is a form of joint disorder that involves inflammation of one or more joints....
, and other situations of moderate to severe chronic, non-malignant
Malignant
Malignancy is the tendency of a medical condition, especially tumors, to become progressively worse and to potentially result in death. Malignancy in cancers is characterized by anaplasia, invasiveness, and metastasis...
pain.
The Actiq dosage unit is a white, berry-flavored lozenge
Lozenge
A lozenge , often referred to as a diamond, is a form of rhombus. The definition of lozenge is not strictly fixed, and it is sometimes used simply as a synonym for rhombus. Most often, though, lozenge refers to a thin rhombus—a rhombus with acute angles of 45°...
on a stick which is swabbed on the buccal mucosa, between cheek and gum to release the fentanyl quickly into the bloodstream. It is most effective when the lozenge is consumed in exactly 15 minutes, as the balance of the drug absorbed through the cheeks and the amount swallowed is maintained.
Absorption
Normally 25% of the drug is absorbed via the buccal mucosa directly into the bloodstream while the remaining 75% is swallowed and then slowly absorbed in the gastrointestinal tractGastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
. Two-thirds of the swallowed Actiq (or 50% of the total dose) is metabolized by the liver and becomes unavailable for any pain relief function, leaving only around 33% of the ingested fentanyl available for pain relief. This is why the drug is far less potent if consumed orally compared to transmucosally.
Dosing
Actiq is available in 6 dosages, measured in microgramMicrogram
In the metric system, a microgram is a unit of mass equal to one millionth of a gram , or 1/1000 of a milligram. It is one of the smallest units of mass commonly used...
s: 200, 400, 600, 800, 1200, & 1600 mcg. Each dosage strength has its own color box and plastic handle:
Actiq 200 mcg—gray
Actiq 400 mcg—blue
Actiq 600 mcg—orange
Actiq 800 mcg—purple
Actiq 1200 mcg—green
Actiq 1600 mcg—burgundy
Side effects
Side effects typical to other opioids can be expected. Common side effects include sedationSedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
, nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
, constipation
Constipation
Constipation refers to bowel movements that are infrequent or hard to pass. Constipation is a common cause of painful defecation...
, tolerance, and respiratory depression.
Recreational use
As with all opioids, there have also been reports of illicit use on the street, where it is (incorrectly) known as "morphine lollipops", and in the US as "perc-a-pop", and sells for between $5–25, depending on its dose. The attorneys-general of ConnecticutConnecticut
Connecticut is a state in the New England region of the northeastern United States. It is bordered by Rhode Island to the east, Massachusetts to the north, and the state of New York to the west and the south .Connecticut is named for the Connecticut River, the major U.S. river that approximately...
and Pennsylvania
Pennsylvania
The Commonwealth of Pennsylvania is a U.S. state that is located in the Northeastern and Mid-Atlantic regions of the United States. The state borders Delaware and Maryland to the south, West Virginia to the southwest, Ohio to the west, New York and Ontario, Canada, to the north, and New Jersey to...
have launched investigations into its diversion from the legitimate pharmaceutical market, including Cephalon's "sales and promotional practices for Provigil, Actiq and Gabitril". In order to curb misuse, many health insurers have begun to require precertification and/or quantity limits
Managed care
...intended to reduce unnecessary health care costs through a variety of mechanisms, including: economic incentives for physicians and patients to select less costly forms of care; programs for reviewing the medical necessity of specific services; increased beneficiary cost sharing; controls on...
for Actiq prescriptions.
Generic alternatives
Beginning late September, 2006, a generic version of Actiq has been available, made by Barr PharmaceuticalsBarr Pharmaceuticals
Barr Pharmaceuticals was a global specialty pharmaceutical company that operated in more than 30 countries worldwide. Barr were engaged in the development, manufacture and marketing of generic and proprietary pharmaceuticals, biopharmaceuticals and active pharmaceutical ingredients.-History:Barr...
. Cephalon
Cephalon
Cephalon, Inc. is a U.S. biopharmaceutical company co-founded in 1987 by Dr. Frank Baldino, Jr., a pharmacologist and former scientist with the DuPont Company, who served as the company's chairman and chief executive officer until his death in December 2010...
has begun marketing its own version of generic Actiq to compete in the generic OTFC market. The generic versions of Actiq, simply called "oral transmucosal fentanyl citrate," are packaged just like name brand Actiq, and there is no difference in appearance, active and inactive ingredients, or function as compared to the name brand Actiq.