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Actiq (Fentanyl Citrate Oral Transmucosal) - Summary




Fatal respiratory depression has occurred in patients treated with ACTIQ, including following use in opioid non-tolerant patients and improper dosing. The substitution of ACTIQ for any other fentanyl product may result in fatal overdose.

Due to the risk of respiratory depression, ACTIQ is contraindicated in the management of acute or postoperative pain including headache/migraine and in opioid non-tolerant patients. [see Contraindications]

Death has been reported in children who have accidentally ingested ACTIQ. ACTIQ must be kept out of reach of children. [see Patient Counseling Information and How Supplied/Storage and Handling (16.1)

The concomitant use of ACTIQ with CYP3A4 inhibitors may result in an increase in fentanyl plasma concentrations, and may cause potentially fatal respiratory depression [see Drug Interactions] .


Substantial differences exist in the pharmacokinetic profile of ACTIQ compared to other fentanyl products that result in clinically important differences in the extent of absorption of fentanyl that could result in fatal overdose.


- When prescribing, do not convert patients on a mcg per mcg basis from any other fentanyl products to ACTIQ. [see Dosage and Administration ( 2.1)]

- When dispensing, do not substitute an ACTIQ prescription for other fentanyl products.


ACTIQ contains fentanyl, an opioid agonist and a Schedule II controlled substance, with an abuse liability similar to other opioid analgesics.

ACTIQ can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing ACTIQ in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse or diversion.

Because of the risk for misuse, abuse, addiction, and overdose, ACTIQ is available only through a restricted program required by the Food and Drug Administration, called a Risk Evaluation and Mitigation Strategy (REMS). Under the Transmucosal Immediate Release Fentanyl (TIRF) REMS Access program, outpatients, healthcare professionals who prescribe to outpatients, pharmacies, and distributors must enroll in the program. [see Warnings and Precautions] Further information is available at www.TIRFREMSAccess.com or by calling 1-866-822-1483.



ACTIQ (oral transmucosal fentanyl citrate) is a solid formulation of fentanyl citrate, a potent opioid analgesic, intended for oral transmucosal administration. ACTIQ is formulated as a white to off-white solid drug matrix on a handle that is fracture resistant (ABS plastic) under normal conditions when used as directed. ACTIQ is designed to be dissolved slowly in the mouth to facilitate transmucosal absorption. The handle allows the ACTIQ unit to be removed from the mouth if signs of excessive opioid effects appear during administration.

ACTIQ (oral transmucosal fentanyl citrate) is indicated for the management of breakthrough pain in cancer patients 16 years of age and older 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, at least 25 mg oral oxymorphone daily, or an equianalgesic dose of another opioid daily for a week or longer. Patients must remain on around-the-clock opioids when taking ACTIQ.

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

ACTIQ is intended to be used only in the care of opioid-tolerant 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.

Limitations of Use:

As a part of the TIRF REMS Access program, ACTIQ may be dispensed only to outpatients enrolled in the program [see Warnings and Precautions] . For inpatient administration of ACTIQ (e.g., hospitals, hospices, and long-term care facilities that prescribe for inpatient use), patient and prescriber enrollment is not required.

See all Actiq indications & dosage >>


Media Articles Related to Actiq (Fentanyl Oral Transmucosal)

Lidocaine Eases Pain, Improves Sex in Breast Cancer Patients
Source: Medscape Hematology-Oncology Headlines [2015.07.31]
Topical lidocaine makes intercourse more comfortable in postmenopausal breast cancer patients with severe dyspareunia.
Medscape Medical News

Vaginal Pain
Source: MedicineNet Itch Specialty [2015.07.31]
Title: Vaginal Pain
Category: Diseases and Conditions
Created: 4/17/2009 12:00:00 AM
Last Editorial Review: 7/31/2015 12:00:00 AM

Health Tip: Easing Neck Pain at Night
Source: MedicineNet Neck Pain Specialty [2015.07.31]
Title: Health Tip: Easing Neck Pain at Night
Category: Health News
Created: 7/31/2015 12:00:00 AM
Last Editorial Review: 7/31/2015 12:00:00 AM

Knee Replacement May Ease Pain for Rheumatoid Arthritis Patients
Source: MedicineNet Osteoarthritis Specialty [2015.07.31]
Title: Knee Replacement May Ease Pain for Rheumatoid Arthritis Patients
Category: Health News
Created: 7/30/2015 12:00:00 AM
Last Editorial Review: 7/31/2015 12:00:00 AM

Persistent severe back pain could signify rare spine infection: new IDSA guideline
Source: Bones / Orthopedics News From Medical News Today [2015.07.30]
Patients with back pain that doesn't go away despite therapy may have a spine infection that could lead to paralysis or death if not diagnosed and treated correctly, note the first U.S.

more news >>

Published Studies Related to Actiq (Fentanyl Oral Transmucosal)

Fentanyl pectin nasal spray: in breakthrough pain in opioid-tolerant adults with cancer. [2011.06.01]
Fentanyl pectin nasal spray (PecFent(R)) uses a novel pectin-based delivery system that turns from an aqueous solution into a gel when applied to mucosal surfaces... Fentanyl pectin nasal spray 100-800 mug was generally well tolerated and was not associated with nasal tolerability problems.

Pharmacokinetics and relative bioavailability of fentanyl pectin nasal spray 100 - 800 microg in healthy volunteers. [2010.12]
CONCLUSIONS: FPNS has a shorter tmax, higher Cmax and greater bioavailability than OTFC and is well tolerated. The dose proportionality of Cmax and AUC0-1 was demonstrated. It is concluded that the pharmacokinetic profile of FPNS suggests this product is suitable for clinical investigation in breakthrough pain in cancer patients.

Pharmacokinetic comparisons of three nasal fentanyl formulations; pectin, chitosan and chitosan-poloxamer 188. [2010.02]
CONCLUSIONS: All nasal formulations demonstrated significantly increased systemic exposure and reduced times to peak plasma values compared with OTFC. The FPNS formulation exhibited the most favorable nasal and general tolerability profiles. It appears suitable for further investigation in breakthrough cancer pain management.

Oral transmucosal fentanyl citrate: a novel analgesic agent for use in retinal photocoagulation. [2009.11]
PURPOSE: To evaluate the analgesic effect of 200 microg oral transmucosal fentanyl citrate during peripheral retinal scatter photocoagulation and to determine the side effect profile... CONCLUSION: OTFC at a dosage of 200 microg is an effective and convenient analgesic for use in peripheral retinal scatter photocoagulation. We found this agent to be well tolerated in the outpatient setting. However, a larger study would be required to ascertain safety across a larger population of opiate-naive patients.

A randomized clinical trial of oral transmucosal fentanyl citrate versus intravenous morphine sulfate for initial control of pain in children with extremity injuries. [2007.08]
BACKGROUND: Extremity injury is a common condition that requires pain management in an emergency department. In pediatric patients, the most frequently used method of pain control is intravenous (IV) morphine sulfate. Oral transmucosal fentanyl citrate (OTFC) is a potential alternative to morphine, which may obviate the need to place an IV before addressing pain. OBJECTIVE: To compare OTFC with IV morphine for sedation and analgesia during initial evaluation of children with deformity of an extremity and suspected fracture... CONCLUSIONS: The use of OTFC can provide improved pain control when compared with IV morphine. The pain reduction starts 30 minutes after initiation of medication, and the effect is seen as far as 75 minutes after the initiation of analgesic medication. The study size was too small to make any statements concerning adverse effects; thus, further studies with larger sample sizes are needed to determine the use of OTFC.

more studies >>

Clinical Trials Related to Actiq (Fentanyl Oral Transmucosal)

Staccato Fentanyl Pharmacokinetics in Healthy Volunteers [Completed]
The Phase I clinical trial in approximately 50 healthy volunteers will be conducted at a single clinical center in two stages. Stage 1 is an open-label, cross-over comparison of a single dose of Staccato Fentanyl and an equivalent dose of intravenous (IV) fentanyl. Stage 2 is a randomized, doubleblind, placebo-controlled dose escalation of Staccato Fentanyl, evaluating multiple doses of fentanyl. The three primary aims of the Phase I clinical trial are to evaluate the pharmacokinetics (PK) and absolute bioavailability for Fentanyl, compare the Staccato Fentanyl PK profile to the IV fentanyl PK profile, and examine the tolerability and safety of Staccato Fentanyl in a non-opioid-tolerant, healthy volunteer population.

Analgesic Effect and Plasma Concentration of Epidural Versus Intravenous Fentanyl [Completed]
CONTEXT AND OBJECTIVE: Controversies exist regarding the site of action of Fentanyl after epidural injection. The objective of this investigation was to compare the analgesic effect of epidural and intravenous Fentanyl for lower limb orthopedic surgeries.

DESIGN AND SETTING: A randomized and double-blind study was performed in Hospital So Paulo.

METHODS: 29 patients were divided into two groups. During the postoperative period, in the presence of pain, group 1 (n = 14) patients received 5 mL of a 100 mcg Fentanyl solution in saline without preservative by the epidural route and 2 mL saline intravenously. Group 2 (n = 15) patients received 5 mL saline by the epidural route and 2 mL (100 mcg) Fentanyl intravenously. Analgesic supplementation consisted of 40 mg intravenous Tenoxicam and 5 mL epidural 0. 25% bupivacaine (if pain relief was not achieved with Tenoxicam). Pain intensity was evaluated by numerical scale and plasma concentrations of Fentanyl were measured simultaneously.

Study of the Effect of Clinical Procedures on Drug Delivery of Mylan Fentanyl Transdermal System 25 µg/hr and Duragesic 25 µg/hr [Terminated]
The objective of this study was to investigate the effect of clinical procedures on the drug delivery of Fentanyl Transdermal Systems, 25 mcg/h manufactured for Mylan Pharmaceuticals Inc. by Mylan Technologies Inc., and Duragesic, 25 mcg/h manufactured for Janssen Pharmaceutica by ALZA Corporation.

Bioequivalence and Wear Study of Mylan Fentanyl Transdermal System 25 µg/h and Mylan Fentanyl Transdermal System [Completed]
The objective of this study was to investigate the effect of three different types of occlusive overlays on the drug delivery of Fentanyl Transdermal Systems, 25 mcg/h manufactured for Mylan Pharmaceuticals Inc. by Mylan Technologies Inc., and Duragesic, 25 mcg/h manufactured for Janssen Pharmaceutica by ALZA Corporation. The acute irritation of each type of overlay worn with each fentanyl treatment was also assessed after patch removal.

Evaluate the Efficacy and Safety of ACTIQ in Patients With Cancer and Breakthrough Pain [Completed]
The primary objective of the study is to determine whether a test titration regimen of ACTIQ treatment will reduce the number of inadequately managed episodes of breakthrough pain for an individual patient by attaining a successful dose of ACTIQ treatment more quickly. The successful ACTIQ dose provides a satisfactory combination of efficacy and tolerability after a single administration, as assessed by the patient.

more trials >>

Reports of Suspected Actiq (Fentanyl Oral Transmucosal) Side Effects

OFF Label USE (78)Drug Prescribing Error (43)Pain (40)Dental Caries (24)Malaise (17)Vomiting (16)Drug Dependence (16)Nausea (15)Withdrawal Syndrome (14)Tooth Disorder (14)more >>


Based on a total of 1 ratings/reviews, Actiq has an overall score of 1. The effectiveness score is 10 and the side effect score is 4. The scores are on ten point scale: 10 - best, 1 - worst.

Actiq review by 40 year old female patient

Overall rating:  
Effectiveness:   Highly Effective
Side effects:   Severe Side Effects
Treatment Info
Condition / reason:   chronic pain
Dosage & duration:   1200 mg x 8 a day taken 2 years for the period of 2 years
Other conditions:   Interstitial Cystitis, Fibromyalgia
Other drugs taken:   Cymbalta, Oxycontin
Reported Results
Benefits:   Without question, Actiq is an extremely effective drug if you are in chronic severe pain and have no responsibilities. Actiq relaxes the body and the brain becomes numb and able to handle ongoing pain effectively. It is fast acting in the subcutaneous, "lollipop" form and within minutes you are comfortable. The flavor is also quite pleasant.
Side effects:   Actiq, when taken as directed, induces a feeling of numbness. and slurred speech is common. Thinking becomes confused and it is not unusual to fall asleep in mid-sentence. Actiq slows breathing and causes extreme tiredness. Actiq are highly addictive and it is literally impossible to stop taking them without a medical detoxification. Actiq delivered in subcutaneous form causes the teeth to rot after extended use of more than 6 months.
Comments:   Actiq should only be taken by individuals who are in severe, chronic pain where tolerance to the drug will not become problematic. It needs to be closely monitored and locked away out of reach of children or any adult who may have problems with addiction. My chronic pain condition was followed by a Pain Center at a reputable hospital. The use of opioids were used only after all other treatments for my condition had failed. Unfortunately, once Actiq was introduced to me, my medical problems worsened, although my pain was under control. I was unable to function responsibly, began dealing with symptoms of withdrawal whenever I didn't take it, which at times became worse than my actual pain and discomfort. I became more of a patient to my family and on a side note, at age 40 lost 4 molars due to the ingredients present in the "lollipops" I was taking. I had no choice but to be hospitalized for an inpatient medical detox in order to safely get this horrible drug out of my body. Fortunately my husband and I were fortunate enought to have the money to go through this detox program. I have no memory of 2 years of my life, thanks to an ignorant, negligent doctor and the drug, Actiq. Believe it or not, my painful conditions are now completely under control now, and I am able to care for my husband and children, and work! After my experience with Actiq I no longer believe in the use of pharmaceutical products as a whole, and owe my good health to diet, exercise and several natural supplements. I have never felt better in my life!

See all Actiq reviews / ratings >>

Page last updated: 2015-07-31

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