Fentanyl availability

CBS News.com (2002) Russia IDs Theater Gas Fentanyl (available at http //www.cbsnews.com/stories/ 2002/10/3 l/world/main527614.shtml). 

Adverse events there is a greater risk of abuse of both fentanyl buccal tablets and fentanyl lozenges since they are both taken orally. Fentanyl oralet has been shown to have variabihty in fentanyl availability because of variation in patient mouth surface area, and the percentage of medication that is absorbed through oral mucosa versus the percentage swallowed. 

Despite the limitations imposed by the physiology of the skin, several marketed controUed release transdermal dmg dehvery systems are available in the United States for example, scopolamine [51-34-3] for the treatment of motion sickness, nitroglycerin [55-63-0] for angina, estradiol [50-28-2] for the rehef of postmenopausal symptoms and osteoporosis, clonidine [4205-90-7] for the treatment of hypertension, fentanyl [437-38-7] as an analgesic, and nicotine [54-11-5] as an aid to smoking cessation. These systems are designed to dehver dmg for periods of one to seven days. 

Sufentanil, fentanyl, remifentanil, alfentanil, and morphine sulfate should be administered only by those specifically trained in the use of IV and epidural anesthetics Oxygen, resusdtative, and intubation equipment should be readily available. 

A patient is prescribed fentanyl (Sublimaze) 50 meg IM 30 minutes before surgery. The nurse has available a vial with a dosage strength of 0.05 mg/1 mL. The nurse calculates the dosage and administers. ... 

The answer is c. (Hardman, pp 543—544. Katzang, p 2533) Fentanyl is a chemical relative of meperidine that is nearly 100 times more potent than morphine. The duration of action, usually between 30 and 60 min after parenteral administration, is shorter than that of meperidine. Fentanyl citrate is only available for parenteral administration intramuscularly and intravenously. Tran sbuc cal ( lollipop ) and transdermal patches avoid first-pass metabolism of fentanyl. 

Fentanyl was introduced to the United States in 1968 by the Janssen Pharmaceutical Company and marketed under the trade name Sublimaze. Its primary purpose was for use as an intravenous anesthetic and analgesic. It is 100 times more potent than morphine in reducing pain, and its duration of action is only 30 minutes (compared to morphine, which lasts several hours). Over the years, fentanyl has proved to be an extremely useful drug, and to date, it is still widely used for surgeries, childbirth, pain associated with cancer and other diseases, and the treatment of trauma-related injuries. Although fentanyl solutions are often given intravenously, pill forms of the drug are also available. 

Over the years it has been interesting to note that many compounded products eventually become commercially available products. Recent examples might include fentanyl lozenges, minoxidil topical solution, nystatin lozenges, clindamycin topical solution, tetracaine-adrenalin-cocaine (TAG) solution, dihydroergotamine mesylate nasal spray, buprenorphine nasal spray, buffered hypertonic saline solution, and erythromycin topical solution as well as numerous other dermatological and pediatric oral liquids and some... 

Voltarol is a brand-name preparation for diclofenac (NSAID) and modified-release tablets are available in 75 mg and 100 mg strength. Nu-seals is a proprietary preparation of enteric-coated aspirin 75 mg. Fentanyl, co-codamol and Suboxone (buprenorphine and naloxone) consist of opioid drugs. 

Fentanyl Slow onset and recovery naloxone reversal available Opioid used in balanced anesthesia and conscious sedation produces marked analgesia... 

If disturbances of gastrointestinal function prevent the use of oral sustained-release morphine, the fentanyl transdermal system (fentanyl patch) can be used over long periods. Furthermore, buccal transmucosal fentanyl can be used for short episodes of breakthrough pain (see Alternative Routes of Administration). Administration of strong opioids by nasal insufflation has been shown to be efficacious, and nasal preparations are now available in some countries. Approval of such formulations in the USA is growing. In addition, stimulant drugs such as the amphetamines have been shown to enhance the analgesic actions of the opioids and thus may be very useful adjuncts in the patient with chronic pain. 

The transdermal system provides continuous systemic delivery of fentanyl for 72 h. The amount of drug released from the system per hour is proportional to the surface area. Following application of the patch to the skin, a depot of fentanyl concentrates in the upper skin layers. This is then available to the systemic circulation. There is an initial rise in blood fentanyl concentration after application followed by a leveling off that occurs 12 to 24 h later. Peak blood concentrations occur between 24 and 72 h after application. The skin does not appear to metabolize fentanyl when delivered transdermally. 

For each drug, the prevalence of abuse was partly attributable to its absolute availability — for example, the over-the-counter status of dextromethorphan (DXM) or the expansion of fentanyl and butorphanol from inpatient to outpatient use. But the pattern of abuse for each drug was distinctive and probably could not have been predicted from the available experimental abuse-liability data. 

Earlier in the chapter, we pointed out that the relationship between drug availability and abuse may wax and wane over time. In the case of fentanyl, this can be seen in the differing results of... 

Table 8.3 shows a selective timeline of the evaluation, abuse, and regulation of DXM, a nonnarcotic cough suppressant with activity at sigma and PCP receptors. Unlike butorphanol and fentanyl, it has never been scheduled in the Controlled Substances Act, and it is available without a prescription in various over-the-counter formulations. 

Fentanyl is also available in a patch form (much like a nicotine patch used for smoking cessation) that can also be used for long-term treatment. This form of administration is referred to as transdermal fentanyl and is sold under the trade name Duregasic. The fentanyl is absorbed directly into the skin from the patch and enters the bloodstream, which carries it to the mu receptors. This form of administration appears much easier than it... 

Illegal use of fentanyl in the United States is linked to the availability of heroin. The majority of the users of the designer analogs of fentanyl prefer heroin and will use it instead when available. Due to the United States War on Drugs, the availability of fentanyl substitutes is being limited. 

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