Fentanyl systemic

Parenteral (generic, Sublimaze) 50 mcg/mL for injection Fentanyl Transdermal System (Duragesic) 12.5, 25, 50, 75, 100 mcg/h delivery Fentanyl Buccal 100, 200, 400, 600, 800 meg oral lozenge Fentanyl Actiq 200, 400, 600, 800, 1200, 1600 meg lozenge on a stick Patient Controlled Transdermal Iontophoretic Fentanyl System 40 meg per dose for delivery Hydromorphone (generic, Dilaudid)... 

Hartrick CT. Patient-controUedtransdermal iontophoretic fentanyl system as an alternative to intravenous morphine RCA review and metaanalysis. Future Neurol 2007 2(6) 621-627. 

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. 

Fentanyl transdermal is a transdermal system that is effective in the management of the severe pain associated with cancer. The transdermal system allows for a timed-release patch containing the drug fentanyl to be activated over a 72-hour period. A small number of patients may require systems applied every 48 hours. The nurse monitors for adverse effects in the same manner as for other narcotic analgesics (eg, the nurse notifies the primary health care provider if the respiratory rate is 10/min or less). 

Epidural analgesia is frequently used for lower extremity procedures and pain (e.g., knee surgery, labor pain, and some abdominal procedures). Intermittent bolus or continuous infusion of preservative-free opioids (morphine, hydromorphone, or fentanyl) and local anesthetics (bupivacaine) may be used for epidural analgesia. Opiates given by this route may cause pruritus that is relieved by naloxone. Adverse effects including respiratory depression, hypotension, and urinary retention may occur. When epidural routes are used in narcotic-dependent patients, systemic analgesics must also be used to prevent withdrawal since the opioid is not absorbed and remains in the epidural space. Doses of opioids used in epidural analgesia are 10 times less than intravenous doses, and intrathecal doses are 10 times less than epidural doses (i.e., 10 mg of IV morphine is equivalent to 1 mg epidural morphine and 0.1 mg of intrathecally administered morphine).45... 

Severe pain should be treated with an opioid such as morphine, hydromorphone, methadone, or fentanyl. Moderate pain can be treated effectively in most cases with a weak opioid such as codeine or hydrocodone, usually in combination with acetaminophen. Meperidine should be avoided owing to its relatively short analgesic effect and its toxic metabolite, normeperidine. Normeperidine may accumulate with repeated dosing and can lead to central nervous system side effects including seizures. 

Other than possibly for the insensible perspiration they absorb, transdermal patches tend to operate as thermodynamically static systems, meaning as com-positionally fixed systems, from the moment they are applied until their removal. Marketed ethanol-driven estradiol and fentanyl patches are exceptions because they meter out ethanol and drive it into the stratum corneum to propel the absorption process. Compositional steadfastness is still the rule, however, and it is this feature that bestows the zero-order delivery attribute on the ordinary transdermal patch. Drug is present within the patches in reservoir amounts whether or not the reservoir compartment is easily distinguished, for there must be enough drug to sustain delivery over the full course of patch wear. 

Figure 7.3 Correlation analysis for Fapp values across freshiy isolated animal buccal mucosa and freshly isolated human buccal mucosa of Lucifer yellow, enalaprilat, atenolol, caffeine, sumatriptan, and fentanyl. Results from internal study by Absorption Systems Company.

Figure 7.6 Cumulative receiver concentrations of fentanyl, caffeine, and atenol vs time across cultured human buccal tissue (average SD, N = 3). Results from internal study by Absorption Systems Company.

Fentanyl transdermal system Fentanyl transdermal systems contain a high concentration of the potent schedule II opioid agonist, fentanyl. Schedule II opioid substances have the highest potential for abuse and associated risk of fatal overdose due to respiratory depression. Fentanyl can be abused and is subject to criminal diversion. The high content of fentanyl in the patches may be a particular target for abuse and diversion. 

Fentanyl transdermal system is indicated for management of persistent, moderate to severe chronic pain that ... 

Fentanyl transdermal system should only be used in patients who are already receiving opioid therapy, who have demonstrated opioid tolerance, and who require a total daily dose at least equivalent to fentanyl transdermal system 25 mcg/h. 

Do not administer fentanyl transdermal system to children younger than 2 years of age. Administer to children only if they are opioid tolerant and 2 years of age or older. 

Only use in patients who are already receiving opioid therapy, who have demonstrated opioid tolerance, and who require a total daily dose at least equivalent to fentanyl transdermal system 25 meg/h. Patients who are considered opioid tolerant are those who have been taking, for a week or longer, morphine 60 mg/day or more, oral oxycodone 30 mg/day or more, oral hydromorphone 8 mg/day or more, or an equianalgesic dose of another opioid. 

Do not use this table to convert from fentanyl transdermal system to other therapies because this conversion to fentanyl is conservative. Use of this table for conversion to other analgesic therapies can overestimate the dose of the new agent. Overdosage of the new analgesic agent is possible. 

Pediatric patients initiating therapy on a fentanyl transdermal system 25 mcg/h should be opioid-tolerant and receiving oral morphine equivalents 60 mg/day or more. 

The majority of patients are adequately maintained with transdermal fentanyl administered every 72 hours. A small number of patients may require systems to be applied every 48 hours.During the initial application, patients should use short-acting analgesics for the first 24 hours as needed until analgesic efficacy with the transdermal system is attained. Thereafter, some patients still may require periodic supplemental doses of other short-acting analgesics for breakthrough pain. 

Discontinuation - Upon system removal, it takes 17 hours or more for the fentanyl serum concentration to fall by 50% after system removal. Titrate the dose of the new analgesic based on the patient s report of pain until adequate analgesia has been attained. For patients requiring discontinuation of opioids, a gradual downward titration is recommended because it is not known at what dose level the opioid may be discontinued without producing the signs and symptoms of abrupt withdrawal. 

Fentanyl transdermal therapeutic system see below see below... 

Fever/External heat Serum fentanyl concentrations may increase by approximately one third for patients with a body temperature of 40°C (104°F) because of temperature-dependent increases in fentanyl release from the transdermal system and increased skin permeability. 

Following removal of transdermal system, 17 hr are required for 50% decrease in serum fentanyl concentrations... 

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