Tuesday, October 4, 2016

Fentanyl Lozenge




Generic Name: fentanyl citrate

Dosage Form: lozenge
FULL PRESCRIBING INFORMATION
WARNING: IMPORTANCE OF PROPER PATIENT SELECTION, DOSING AND POTENTIAL FOR ABUSE

Reports of serious adverse events, including deaths in patients treated with Oral Transmucosal Fentanyl Citrate (OTFC) have been reported. Deaths occurred as a result of improper patient selection (e.g., use in opioid non-tolerant patients) and/or improper dosing. The substitution of OTFC for any other fentanyl product may result in fatal overdose.


OTFC is indicated only for the management of breakthrough cancer pain in patients with malignancies who are already receiving and who are tolerant to around-the-clock opioid therapy for their underlying persistent cancer pain. Patients considered opioid tolerant are those who are taking around-the-clock medicine consisting of at least 60 mg of oral morphine daily, at least 25 mcg of transdermal fentanyl/hour, at least 30 mg of oral oxycodone daily, at least 8 mg of oral hydromorphone daily or an equianalgesic dose of another opioid for a week or longer.


OTFC is not indicated for use in opioid non-tolerant patients including those with only as needed (PRN) prior exposure.


Life-threatening respiratory depression could occur at any dose in opioid non-tolerant patients. Deaths have occurred in opioid non-tolerant patients.


OTFC is contraindicated in the management of acute or postoperative pain including headache/migraine.


When prescribing, do not convert patients on a mcg per mcg basis to Oral Transmucosal Fentanyl Citrate (OTFC) from other fentanyl products.


When dispensing, do not substitute an OTFC prescription for other fentanyl products. Substantial differences exist in the pharmacokinetic profile of OTFC compared to other fentanyl products that result in clinically important differences in the extent of absorption of fentanyl. As a result of these differences, the substitution of OTFC for any other fentanyl product may result in fatal overdose.


Special care must be used when dosing OTFC. If the breakthrough pain episode is not relieved 15 minutes after completion of the OTFC unit, patients may take ONLY ONE additional dose using the same strength and then must wait at least 4 hours before taking another dose [see Dosage And Administration (2.2)].


Oral Transmucosal Fentanyl Citrate (OTFC) contains fentanyl, an opioid agonist and a Schedule II controlled substance, with an abuse liability similar to other opioid analgesics. OTFC can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing OTFC in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse or diversion. Schedule II opioid substances which include morphine, oxycodone, hydromorphone, oxymorphone, and methadone have the highest potential for abuse and risk of fatal overdose due to respiratory depression. 


Patients and their caregivers must be instructed that OTFC contains a medicine in an amount which can be fatal to a child. Death has been reported in children who have accidentally ingested OTFC. All units must be kept out of the reach of children and opened units properly discarded [see Warnings and Precautions (5.3), Patient Counseling Information (17.5, 17.6), and How Supplied/Storage And Handling (16.2)].


OTFC is intended to be used only in the care of cancer patients and only by oncologists and pain specialists who are knowledgeable of and skilled in the use of Schedule II opioids to treat cancer pain.


The concomitant use of OTFC with strong and moderate cytochrome P450 3A4 inhibitors may result in an increase in fentanyl plasma concentrations, and may cause potentially fatal respiratory depression [s ee Drug Interactions (7)].




Indications and Usage for Fentanyl Lozenge


Oral Transmucosal Fentanyl Citrate (OTFC) is indicated only for the management of breakthrough cancer pain in patients 16 and older with malignancies who are already receiving and who are tolerant to around-the-clock opioid therapy for their underlying persistent cancer pain. Patients considered opioid tolerant are those who are taking around-the-clock medicine consisting of at least 60 mg of oral morphine daily, at least 25 mcg of transdermal fentanyl/hour, at least 30 mg of oral oxycodone daily, at least 8 mg of oral hydromorphone daily or an equianalgesic dose of another opioid daily for a week or longer. Patients must remain on around-the-clock opioids when taking OTFC.


This product must notbe used in opioid non-tolerant patients because life-threatening respiratory depression and death could occur at any dose in patients not on chronic regimen of opioids. For this reason, OTFC is contraindicated in the management of acute or postoperative pain.


OTFC is intended to be used only in the care of cancer patients and only by oncologists and pain specialists who are knowledgeable of and skilled in the use of Schedule II opioids to treat cancer pain.



Fentanyl Lozenge Dosage and Administration


As with all opioids, the safety of patients using such products is dependent on healthcare professionals prescribing them in strict conformity with their approved labeling with respect to patient selection, dosing, and proper conditions for use.



Initial Dose


Individually titrate Oral Transmucosal Fentanyl Citrate (OTFC) to a dose that provides adequate analgesia and minimizes side effects. The initial dose of OTFC to treat episodes of breakthrough cancer pain is always 200 mcg. The OTFC unit should be consumed over 15 minutes. Patients should be prescribed an initial titration supply of six 200 mcg OTFC units, thus limiting the number of units in the home during titration. Patients should use up all units before increasing to a higher dose to prevent confusion and possible overdose.



Dose Titration


From this initial dose, closely follow patients and change the dosage level until the patient reaches a dose that provides adequate analgesia using a single OTFC dosage unit per breakthrough cancer pain episode. If signs of excessive opioid effects appear before the unit is consumed, the dosage unit should be removed from the patient’s mouth immediately, disposed of properly, and subsequent doses should be decreased. Patients should record their use of OTFC over several episodes of breakthrough cancer pain and review their experience with their physicians to determine if a dosage adjustment is warranted.


In cases where the breakthrough pain episode is not relieved 15 minutes after completion of the OTFC unit (30 minutes after the start of the unit), patients may take ONLY ONE additional dose of the same strength for that episode. Thus, patients should take a maximum of two doses of OTFC for any breakthrough pain episode.


Patients must wait at least 4 hours before treating another episode of breakthrough pain with OTFC. To reduce the risk of overdosing during titration, patients should have only one strength of OTFC available at any one time.


* Available dosage strengths include: 200, 400, 600, 800, 1200, and 1600 mcg.



Maintenance Dosing 


Once titrated to an effective dose, patients should generally use ONLY ONE Oral Transmucosal Fentanyl Citrate (OTFC) unit of the appropriate strength per breakthrough pain episode.


On those occasions when the breakthrough pain episode is not relieved 15 minutes after completion of the OTFC unit, patient may take ONLY ONE additional dose using the same strength for that episode.


Patients MUST wait at least 4 hours before treating another episode of breakthrough pain with OTFC. Once a successful dose has been found (i.e., an average episode is treated with a single unit), patients should limit consumption to four or fewer units per day.


Dosage adjustment of OTFC may be required in some patients in order to continue to provide adequate relief of breakthrough pain.


Generally, the OTFC dose should be increased only when a single administration of the current dose fails to adequately treat the breakthrough pain episode for several consecutive episodes.


If the patient experiences greater than four breakthrough pain episodes per day, the dose of the maintenance (around-the-clock) opioid used for persistent pain should be re-evaluated.



Administration of OTFC


Open the blister package with scissors immediately prior to product use. The patient should place the Oral Transmucosal Fentanyl Citrate (OTFC) unit in his or her mouth between the cheek and lower gum, occasionally moving the drug matrix from one side to the other using the handle. The OTFC unit should be sucked, not chewed. A unit dose of OTFC, if chewed and swallowed, might result in lower peak concentrations and lower bioavailability than when consumed as directed [ see Clinical Pharmacology (12.3)].


The OTFC unit should be consumed over a 15-minute period. Longer or shorter consumption times may produce less efficacy than reported in OTFC clinical trials. If signs of excessive opioid effects appear before the unit is consumed, remove the drug matrix from the patient’s mouth immediately and decrease future doses.



Discontinuation of OTFC


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.



Dosage Forms and Strengths


Each dosage unit has white to off-white color and is a solid drug matrix on a handle.

Each strength is marked on the individual solid drug matrix and the handle tag. Oral Transmucosal Fentanyl Citrate (OTFC) is available in 200 mcg, 400 mcg, 600 mcg,

800 mcg, 1200 mcg and 1600 mcg strengths [see How Supplied/Storage And Handling (16.3)].



Contraindications


OTFC is contraindicated in opioid non-tolerant patients. OTFC is contraindicated in the management of acute or postoperative pain including headache/migraine. Life-threatening respiratory depression and death could occur at any dose in opioid non-tolerant patients.


Patients considered opioid tolerant are those who are taking around-the-clock medicine consisting of at least 60 mg of oral morphine daily, at least 25 mcg of transdermal fentanyl/hour, at least 30 mg of oral oxycodone daily, at least 8 mg of oral hydromorphone daily, or an equianalgesic dose of another opioid daily for a week or longer.


OTFC is contraindicated in patients with known intolerance or hypersensitivity to any of its components or the drug fentanyl. Anaphylaxis and hypersensitivity have been reported in association with the use of OTFC.



Warnings and Precautions


See Boxed Warning - WARNING: IMPORTANCE OF PROPER PATIENT SELECTION, DOSING and POTENTIAL FOR ABUSE



Important Information Regarding Prescribing and Dispensing


When prescribing, DO NOT convert a patient to OTFC from any other fentanyl product on a mcg per mcg basis as OTFC and other fentanyl products are not equivalent on a microgram per microgram basis.


OTFC is NOT a generic version of fentanyl buccal tablets (Fentora ®). When dispensing, DO NOT substitute an OTFC prescription for fentanyl buccal tablets (Fentora®) prescription under any circumstances. Fentanyl buccal tablets (Fentora®) and OTFC are not equivalent. Substantial differences exist in the pharmacokinetic profile of OTFC compared to other fentanyl products including fentanyl buccal tablets (Fentora®) that result in clinically important differences in the rate and extent of absorption of fentanyl. As a result of these differences, the substitution of OTFC for any other fentanyl product may result in a fatal overdose.


There are no safe conversion directions available for patients on any other fentanyl products. (Note: This includes oral, transdermal, or parenteral formulations of fentanyl.) Therefore, for opioid tolerant patients, the initial dose of OTFC should always be 200 mcg. Each patient should be individually titrated to provide adequate analgesia while minimizing side effects [see Dosage And Administration (2.2)].



Respiratory Depression


As with all opioids, there is a risk of clinically significant respiratory depression in patients using Oral Transmucosal Fentanyl Citrate (OTFC). Accordingly, follow all patients for symptoms of respiratory depression. Respiratory depression may occur more readily when opioids are given in conjunction with other agents that depress respiration.



Patient/Caregiver Instructions


Patients and their caregivers must be instructed that Oral Transmucosal Fentanyl Citrate (OTFC) contains a medicine in an amount which can be fatal to a child. Death has been reported in children who have accidentally ingested OTFC. Patients and their caregivers must be instructed to keep both used and unused dosage units out of the reach of children. While all units should be disposed of immediately after use, partially consumed units represent a special risk to children. In the event that a unit is not completely consumed it must be properly disposed as soon as possible [see How Supplied/Storage And Handling, (16.1, 16.2), and Patient Counseling Information (17.1, 17.7)].


Physicians and dispensing pharmacists must specifically question patients or caregivers about the presence of children in the home (on a full time or visiting basis) and counsel them regarding the dangers to children from inadvertent exposure.


OTFC could be fatal to individuals for whom it is not prescribed and for those who are not opioid-tolerant.



Additive CNS Depressant Effects


The concomitant use of OTFC with other CNS depressants, including other opioids, sedatives or hypnotics, general anesthetics, phenothiazines, tranquilizers, skeletal muscle relaxants, sedating antihistamines, and alcoholic beverages may produce increased depressant effects (e.g., respiratory depression, hypotension, and profound sedation). Concomitant use with potent inhibitors of cytochrome P450 3A4 isoform (e.g., erythromycin, ketoconazole, and certain protease inhibitors) may increase fentanyl levels, resulting in increased depressant effects [ see Drug Interactions (7)].


Patients on concomitant CNS depressants must be monitored for a change in opioid effects. Consideration should be given to adjusting the dose of OTFC if warranted.



Effects on Ability to Drive and Use Machines


Opioid analgesics impair the mental and/or physical ability required for the performance of potentially dangerous tasks (e.g., driving a car or operating machinery). Warn patients taking OTFC of these dangers and counsel them accordingly.



Chronic Pulmonary Disease


Because potent opioids can cause respiratory depression, titrate OTFC with caution in patients with chronic obstructive pulmonary disease or preexisting medical conditions predisposing them to respiratory depression. In such patients, even normal therapeutic doses of OTFC may further decrease respiratory drive to the point of respiratory failure.



Head Injuries and Increased Intracranial Pressure


Administer OTFC with extreme caution in patients who may be particularly susceptible to the intracranial effects of CO 2 retention such as those with evidence of increased intracranial pressure or impaired consciousness. Opioids may obscure the clinical course of a patient with a head injury and should be used only if clinically warranted.



Cardiac Disease


Intravenous fentanyl may produce bradycardia. Therefore, use OTFC with caution in patients with bradyarrhythmias.



MAO Inhibitors


OTFC is not recommended for use in patients who have received MAO inhibitors within 14 days, because severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics. 



Adverse Reactions



Clinical Studies Experience


The safety of Oral Transmucosal Fentanyl Citrate (OTFC) has been evaluated in 257 opioid-tolerant chronic cancer pain patients. The duration of OTFC use varied during the open-label study. Some patients were followed for over 21 months. The average duration of therapy in the open-label study was 129 days.


The adverse reactions seen with OTFC are typical opioid side effects. Frequently, these adverse reactions will cease or decrease in intensity with continued use of OTFC, as the patient is titrated to the proper dose. Expect opioid side effects and manage them accordingly.


The most serious adverse reactions associated with all opioids including OTFC are respiratory depression (potentially leading to apnea or respiratory arrest), circulatory depression, hypotension, and shock. Follow all patients for symptoms of respiratory depression.


Because the clinical trials of OTFC were designed to evaluate safety and efficacy in treating breakthrough cancer pain, all patients were also taking concomitant opioids, such as sustained-release morphine or transdermal fentanyl, for their persistent cancer pain. The adverse event data presented here reflect the actual percentage of patients experiencing each adverse effect among patients who received OTFC for breakthrough cancer pain along with a concomitant opioid for persistent cancer pain. There has been no attempt to correct for concomitant use of other opioids, duration of OTFC therapy, or cancer-related symptoms. Adverse reactions are included regardless of causality or severity.


Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.


Three short-term clinical trials with similar titration schemes were conducted in 257 patients with malignancy and breakthrough cancer pain. Data are available for 254 of these patients. The goal of titration in these trials was to find the dose of OTFC that provided adequate analgesia with acceptable side effects (successful dose). Patients were titrated from a low dose to a successful dose in a manner similar to current titration dosing guidelines. Table 1 lists, by dose groups, adverse reactions with an overall frequency of 1% or greater that occurred during titration and are commonly associated with opioid administration or are of particular clinical interest. The ability to assign a dose-response relationship to these adverse reactions is limited by the titration schemes used in these studies. Adverse reactions are listed in descending order of frequency within each body system.



























































































































































































Table 1. Percent of Patients with Specific Adverse Events Commonly Associated with Opioid Administration or of Particular Clinical Interest Which Occurred During Titration (Events in 1% or More of Patients)

*

Any Dose = A patient who experienced the same adverse event at multiple doses was only counted once

Dose GroupPercentage of Patients Reporting Event
200-

600 mcg (n=230)
800-

1400 mcg (n=138)


1600 mcg (n=54)


> 1600 mcg (n=41)
Any Dose(n=254)* 
Body As A Whole
Asthenia64079
Headache34656
Accidental Injury11402
Digestive
Nausea1415112223
Vomiting7661512
Constipation14204
Nervous
Dizziness101661517
Somnolence99112017
Confusion16204
Anxiety30203
Abnormal Gait01402
Dry Mouth11202
Nervousness11002
Vasodilatation20202
Hallucinations01221
Insomnia01201
Thinking Abnormal01201
Vertigo10001
Respiratory
Dyspnea23654
Skin
Pruritus10052
Rash11022
Sweating11222
Special Senses
Abnormal Vision10202

The following adverse reactions not reflected in Table 1 occurred during titration with an overall frequency of 1% or greater and are listed in descending order of frequency within each body system.


Body as a Whole: Pain, fever, abdominal pain, chills, back pain, chest pain, infection


Cardiovascular: Migraine


Digestive: Diarrhea, dyspepsia, flatulence


Metabolic and Nutritional: Peripheral edema, dehydration


Nervous: Hypesthesia


Respiratory: Pharyngitis, cough increased


The following reactions occurred during titration with an overall frequency of less than 1% and are listed in descending order of frequency within each body system.


Body as a Whole: Flu syndrome, abscess, bone pain


Cardiovascular: Deep thrombophlebitis, hypertension, hypotension


Digestive: Anorexia, eructation, esophageal stenosis, fecal impaction, gum hemorrhage, mouth ulceration, oral moniliasis


Hemic and Lymphatic: Anemia, leukopenia


Metabolic and Nutritional: Edema, hypercalcemia, weight loss


Musculoskeletal: Myalgia, pathological fracture, myasthenia


Nervous: Abnormal dreams, urinary retention, agitation, amnesia, emotional lability, euphoria, incoordination, libido decreased, neuropathy, paresthesia, speech disorder


Respiratory: Hemoptysis, pleural effusion, rhinitis, asthma, hiccup, pneumonia, respiratory insufficiency, sputum increased


Skin and Appendages: Alopecia, exfoliative dermatitis


Special Senses: Taste perversion


Urogenital: Vaginal hemorrhage, dysuria, hematuria, urinary incontinence, urinary tract infection


A long-term extension study was conducted in 156 patients with malignancy and breakthrough cancer pain who were treated for an average of 129 days. Data are available for 152 of these patients. Table 2 lists by dose groups, adverse reactions with an overall frequency of 1% or greater that occurred during the long-term extension study and are commonly associated with opioid administration or are of particular clinical interest. Adverse reactions are listed in descending order of frequency within each body system.





























































































































































































































































 Table 2. Percent of Patients with Adverse Events Commonly Associated with Opioid Administration or of Particular Clinical Interest Which Occurred During Long Term Treatment (Events in 1% or More of Patients)

*

Any Dose = A patient who experienced the same adverse event at multiple doses was only counted once

Dose GroupPercentage of Patients Reporting Event
200-

600 mcg (n=98)
800-

1400 mcg (n=83)


1600 mcg (n=53)


>1600 mcg (n=27)
Any Dose(n=152)* 
Body As A Whole
Asthenia2530171538
Headache121713420
Accidental Injury46479
Hypertonia22203
Digestive
Nausea3136252645
Vomiting212815731
Constipation141113420
Intestinal Obstruction02403
Cardiovascular
Hypertension11001
Nervous
Dizziness12109016
Anxiety988715
Somnolence8138715
Confusion2513710
Depression94279
Insomnia51847
Abnormal Gait51004
Dry Mouth31244
Nervousness22043
Stupor41003
Vasodilatation11403
Thinking Abnormal21002
Abnormal Dreams11001
Convulsion01201
Myoclonus00401
Tremor01201
Vertigo00401
Respiratory
Dyspnea15168722
Skin
Rash35848
Sweating32204
Pruritus20202
Special Senses
Abnormal Vision22003
Urogenital
Urinary Retention12002

 The following reactions not reflected in Table 2 occurred with an overall frequency of 1% or greater in the long-term extension study and are listed in descending order of frequency within each body system.


Body as a Whole: Pain, fever, back pain, abdominal pain, chest pain, flu syndrome, chills, infection, abdomen enlarged, bone pain, ascites, sepsis, neck pain, viral infection, fungal infection, cachexia, cellulitis, malaise, pelvic pain


Cardiovascular: Deep thrombophlebitis, migraine, palpitation, vascular disorder


Digestive: Diarrhea, anorexia, dyspepsia, dysphagia, oral moniliasis, mouth ulceration, rectal disorder, stomatitis, flatulence, gastrointestinal hemorrhage, gingivitis, jaundice, periodontal abscess, eructation, glossitis, rectal hemorrhage


Hemic and Lymphatic: Anemia, leukopenia, thrombocytopenia, ecchymosis, lymphadenopathy, lymphedema, pancytopenia


Metabolic and Nutritional: Peripheral edema, edema, dehydration, weight loss, hyperglycemia, hypokalemia, hypercalcemia, hypomagnesemia


Musculoskeletal: Myalgia, pathological fracture, joint disorder, leg cramps, arthralgia, bone disorder


Nervous: Hypesthesia, paresthesia, hypokinesia, neuropathy, speech disorder


Respiratory: Cough increased, pharyngitis, pneumonia, rhinitis, sinusitis, bronchitis, epistaxis, asthma, hemoptysis, sputum increased


Skin and Appendages: Skin ulcer, alopecia


Special Senses: Tinnitus, conjunctivitis, ear disorder, taste perversion


Urogenital: Urinary tract infection, urinary incontinence, breast pain, dysuria, hematuria, scrotal edema, hydronephrosis, kidney failure, urinary urgency, urination impaired, breast neoplasm, vaginal hemorrhage, vaginitis


The following reactions occurred with a frequency of less than 1% in the long-term extension study and are listed in descending order of frequency within each body system.


Body as a Whole: Allergic reaction, cyst, face edema, flank pain, granuloma, bacterial infection, injection site pain, mucous membrane disorder, neck rigidity


Cardiovascular: Angina pectoris, hemorrhage, hypotension, peripheral vascular disorder, postural hypotension, tachycardia


Digestive: Cheilitis, esophagitis, fecal incontinence, gastroenteritis, gastrointestinal disorder, gum hemorrhage, hemorrhage of colon, hepatorenal syndrome, liver tenderness, tooth caries, tooth disorder


Hemic and Lymphatic: Bleeding time increased


Metabolic and Nutritional: Acidosis, generalized edema, hypocalcemia, hypoglycemia, hyponatremia, hypoproteinemia, thirst


Musculoskeletal: Arthritis, muscle atrophy, myopathy, synovitis, tendon disorder


Nervous: Acute brain syndrome, agitation, cerebral ischemia, facial paralysis, foot drop, hallucinations, hemiplegia, miosis, subdural hematoma


Respiratory: Hiccup, hyperventilation, lung disorder, pneumothorax, respiratory failure, voice alteration


Skin and Appendages: Herpes zoster, maculopapular rash, skin discoloration, urticaria, vesiculobullous rash


Special Senses: Ear pain, eye hemorrhage, lacrimation disorder, partial permanent deafness, partial transitory deafness


Urogenital: Kidney pain, nocturia, oliguria, polyuria, pyelonephritis



Post-Marketing Experience


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