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). Fentanyl is a Schedule II controlled substance per the Controlled Substance Act. Other pharmaceutical preparations consisting of fentanyl are 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 like how nicotine is absorbed when dip is placed in one's mouth between the gum and cheek.

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Administration

Nearly 80 times stronger than morphine^[1], Actiq is intended for opiate-tolerant individuals and is effective in treating cancer breakthrough pain. However, it is often prescribed for "off-label uses", i.e. not for cancer patients, such as bone injuries, migraines, severe back pain, neuropathy, arthritis, and other situations of moderate to severe chronic, non-malignant pain. ^[1], ^[2], ^[3]

The Actiq dosage unit is a white, berry-flavored lozenge 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 tract. 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. This is why the drug is far less potent if consumed orally compared to transmucosally.

Dosing

Actiq is available in 6 dosages, measured in micrograms: 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

Actiq, like all opioids, has a potential for abuse and can be habit forming. Actiq should not be taken with alcohol. Although Actiq was only approved by the FDA for treatment of intractable pain in cancer patients, it has been estimated that in the first half of 2006 approximately 90-99% of the 187,076 Actiq prescriptions filled in the U.S. were for "off-label uses", i.e. not for cancer patients.^[1], ^[2] Actiq was reported to be one of many legally prescribed addictive medications found in Anna Nicole Smith's room when she died.^[1]

As with all opioids, there have also been reports of illicit use on the street, where it is known as "perc-a-pop", and sells for $20-$25 each.^[4] The attorneys-general of Connecticut and Pennsylvania have launched investigations into its diversion from the legitimate pharmaceutical market, including Cephalon's "sales and promotional practices for Provigil, Actiq and Gabitril".^[4] In order to curb misuse, many health insurers have begun to require precertification and/or quantity limits for Actiq prescriptions. ^[5],^[6],^[7]

An Actiq lozenge contains 2 grams of sugar ^[8] (8 calories), making weight gain and tooth decay a conceivable concern for patients who consume many Actiqs per day.^[3] Diabetics also need to take Actiq's sugar content into account. A sugar-free version, called Actiq-SF, is in development, and should be available beginning first quarter 2007. Side effects include the normal side effects found with this class of narcotic analgesic plus constipation and dry mouth. Other side effects include rash, sweating, hot flashes, and dizziness.

Generic Alternatives

Beginning late September, 2006, a generic version of Actiq has been available, made by Barr Pharmaceuticals. Cephalon 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. Because Actiq is extremely expensive, the generic OTFC just hitting the market will likely make the drug more accessible.

References