FENTANYL TRANSDERMAL SYSTEM. Full Prescribing Information. FOR USE IN OPIOID- TOLERANT PATIENTS ONLYFENTANYL TRANSDERMAL SYSTEM - fentanyl patch, extended release Mallinckrodt Inc.- -- -- -- -- -FENTANYL TRANSDERMAL SYSTEM2. CII Full Prescribing Information Rx only FOR USE IN OPIOID- TOLERANT PATIENTS ONLYFentanyl transdermal system contains a high concentration of a potent Schedule II opioid agonist, fentanyl. Schedule II opioid substances which include fentanyl, hydromorphone, methadone, morphine, oxycodone, and oxymorphone 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 (fentanyl transdermal system) may be a particular target for abuse and diversion. Fentanyl transdermal system is indicated for management of persistent, moderate to severe chronic pain that: requires continuous, around- the- clock opioid administration for an extended period of time, andcannot be managed by other means such as non- steroidal analgesics, opioid combination products, or immediate- release opioids. 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 2. Patients who are considered opioid- tolerant are those who have been taking, for a week or longer, at least 6. Because serious or life- threatening hypoventilation could occur, fentanyl transdermal system is contraindicated: in patients who are not opioid- tolerantin the management of acute pain or in patients who require opioid analgesia for a short period of timein the management of post- operative pain, including use after out- patient or day surgeries (e. Patients receiving fentanyl transdermal system and any CYP3. A4 inhibitor should be carefully monitored for an extended period of time and dosage adjustments should be made if warranted (see CLINICAL PHARMACOLOGY, Drug Interactions; WARNINGS; PRECAUTIONS and DOSAGE AND ADMINISTRATION for further information).
The safety of fentanyl transdermal system has not been established in children under 2 years of age. Fentanyl transdermal system should be administered to children only if they are opioid- tolerant and 2 years of age or older (see PRECAUTIONS, Pediatric Use). Use in non- opioid tolerant patients may lead to fatal respiratory depression. Overestimating the fentanyl transdermal system dose when converting patients from another opioid medication can result in fatal overdose with the first dose (see DOSAGE AND ADMINISTRATION, Initial Fentanyl Transdermal System Dose Selection). Due to the mean half- life of approximately 1. Fentanyl transdermal system can be abused in a manner similar to other opioid agonists, legal or illicit. This risk should be considered when administering, prescribing, or dispensing fentanyl transdermal system in situations where the healthcare professional is concerned about increased risk of misuse, abuse or diversion. Persons at increased risk for opioid abuse include those with a personal or family history of substance abuse (including drug or alcohol abuse or addiction) or mental illness (e. Patients should be assessed for their clinical risks for opioid abuse or addiction prior to being prescribed opioids. All patients receiving opioids should be routinely monitored for signs of misuse, abuse and addiction. Patients at increased risk of opioid abuse may still be appropriately treated with modified- release opioid formulations; however, these patients will require intensive monitoring for signs of misuse, abuse, or addiction. Osmanil 100mcg/hr transdermal patches. Fentanyl Transdermal System. NDC Number: 60505-7009-02. Pack Size (Form): 5 PATCH (POUCH) TE Rating: AB. Fentanyl transdermal systems are intended for transdermal use (on intact skin) only. Do not use a fentanyl transdermal system if the pouch seal is broken or the patch is cut, damaged, or changed in any way. Avoid exposing the fentanyl transdermal system application site and surrounding area to direct external heat sources, such as heating pads or electric blankets, heat or tanning lamps, saunas, hot tubs, and heated water beds, while wearing the system. Avoid taking hot baths or sunbathing. There is a potential for temperature- dependent increases in fentanyl released from the system resulting in possible overdose and death. Patients wearing fentanyl transdermal systems who develop fever or increased core body temperature due to strenuous exertion should be monitored for opioid side effects and the fentanyl transdermal system dose should be adjusted if necessary. DESCRIPTIONFentanyl transdermal system is a transdermal system providing continuous systemic delivery of fentanyl, a potent opioid analgesic, for 7. The chemical name is N- Phenyl- N- (1- (2- phenylethyl)- 4- piperidinyl) propanamide. The structural formula is: The molecular weight of fentanyl base is 3. C2. 2H2. 8N2. O. The n- octanol: water partition coefficient is 8. The p. Ka is 8. 4. System Components and Structure. The amount of fentanyl released from each system per hour is proportional to the surface area (2. The composition per unit area of all system sizes is identical. Dose*(mcg/hr)Size(cm. Fentanyl Content(mg)2. Fentanyl transdermal system is a rectangular transparent unit comprising a protective liner and four functional layers. Proceeding from the outer surface toward the surface adhering to skin, these layers are: a backing layer of PET foil; a drug containing layer of fentanyl and dipropylene glycol with hydroxypropyl cellulose; an ethylene vinyl- acetate copolymer membrane that controls the rate of fentanyl delivery to the skin surface; anda silicone adhesive. Before use, a protective liner covering the adhesive layer is removed and discarded. The active component of the system is fentanyl. The remaining components are pharmacologically inactive: dipropylene glycol, hydroxypropyl cellulose, ethylene vinyl- acetate copolymer, silicone adhesives between polyester backings, silicone fluid. CLINICAL PHARMACOLOGYPharmacology. Fentanyl is an opioid analgesic. Fentanyl interacts predominately with the opioid mu- receptor. These mu- binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, fentanyl exerts its principal pharmacologic effects on the central nervous system. In addition to analgesia, alterations in mood, euphoria, dysphoria, and drowsiness commonly occur. Fentanyl depresses the respiratory centers, depresses the cough reflex, and constricts the pupils. Analgesic blood concentrations of fentanyl may cause nausea and vomiting directly by stimulating the chemoreceptor trigger zone, but nausea and vomiting are significantly more common in ambulatory than in recumbent patients, as is postural syncope. Opioids increase the tone and decrease the propulsive contractions of the smooth muscle of the gastrointestinal tract. The resultant prolongation in gastrointestinal transit time may be responsible for the constipating effect of fentanyl. Because opioids may increase biliary tract pressure, some patients with biliary colic may experience worsening rather than relief of pain. While opioids generally increase the tone of urinary tract smooth muscle, the net effect tends to be variable, in some cases producing urinary urgency, in others, difficulty in urination. At therapeutic dosages, fentanyl usually does not exert major effects on the cardiovascular system. However, some patients may exhibit orthostatic hypotension and fainting. Histamine assays and skin wheal testing in clinical studies indicate that clinically significant histamine release rarely occurs with fentanyl administration. Clinical assays show no clinically significant histamine release in dosages up to 5. Pharmacokinetics (see graph and tables)Fentanyl transdermal system is a drug- in- adhesive matrix designed formulation. Fentanyl is released from the matrix at a nearly constant amount per unit time. The concentration gradient existing between the matrix and the lower concentration in the skin drives drug release. Fentanyl moves in the direction of the lower concentration at a rate determined by the copolymer release membrane and the diffusion of fentanyl through the skin layers. While the actual rate of fentanyl delivery to the skin varies over the 7. While there is variation in dose delivered among patients, the nominal flux of the systems (2. Following fentanyl transdermal system application, the skin under the system absorbs fentanyl, and a depot of fentanyl concentrates in the upper skin layers. Fentanyl then becomes available to the systemic circulation. Serum fentanyl concentrations increase gradually following initial fentanyl transdermal system application, generally leveling off between 1. Peak serum concentrations of fentanyl generally occurred between 2. Table A). Serum fentanyl concentrations achieved are proportional to the fentanyl transdermal system delivery rate. With continuous use, serum fentanyl concentrations continue to rise for the first two system applications. By the end of the second 7. Patients reach and maintain a steady- state serum concentration that is determined by individual variation in skin permeability and body clearance of fentanyl. After system removal, serum fentanyl concentrations decline gradually, falling about 5. Continued absorption of fentanyl from the skin accounts for a slower disappearance of the drug from the serum than is seen after an IV infusion, where the apparent half- life is approximately 7 (range 3 to 1. Alterations in p. H may affect its distribution between plasma and the central nervous system. Fentanyl accumulates in the skeletal muscle and fat and is released slowly into the blood. The average volume of distribution for fentanyl is 6 L/kg (range 3 to 8; N=8). Fentanyl is metabolized primarily via human cytochrome P4. A4 isoenzyme system.
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