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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)

The Opioid Crisis and Need for Compassion in Pain Management
Source: Medscape Anesthesiology Headlines [2017.09.28]
In this commentary, the author expresses concern that the response to the public health crisis of opioid addiction is creating a growing crisis of inadequate pain management.
American Journal of Public Health

CVS to Restrict Opioid Painkiller Prescription Amounts
Source: MedicineNet Drug Abuse Specialty [2017.09.25]
Title: CVS to Restrict Opioid Painkiller Prescription Amounts
Category: Health News
Created: 9/22/2017 12:00:00 AM
Last Editorial Review: 9/25/2017 12:00:00 AM

Stomach Pain Quiz: Nausea & Other Causes
Source: MedicineNet Anal Fissure Specialty [2017.09.19]
Title: Stomach Pain Quiz: Nausea & Other Causes
Category: MedicineNet Quiz
Created: 1/20/2011 12:00:00 AM
Last Editorial Review: 9/19/2017 5:59:56 PM

Back Pain Quiz: Test Your Back Pain IQ
Source: MedicineNet Ankylosing Spondylitis Specialty [2017.09.19]
Title: Back Pain Quiz: Test Your Back Pain IQ
Category: MedicineNet Quiz
Created: 6/16/2011 3:41:00 PM
Last Editorial Review: 9/19/2017 6:39:04 PM

Pain Quiz: Test Your IQ of Pain
Source: MedicineNet Constipation Specialty [2017.09.19]
Title: Pain Quiz: Test Your IQ of Pain
Category: MedicineNet Quiz
Created: 7/14/2011 3:53:00 PM
Last Editorial Review: 9/19/2017 6:41:41 PM

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)

Procedural Pain Treatment With Transmucosal Sublingual Fentanyl Tablet in Colonoscopy Patients [Recruiting]
Colonoscopy is generally considered an invasive procedure that causes remarkable pain to the patient. The pain associated with the procedure is not caused by the insertion of the scope but from inflating of the colon in order to do the inspection. It has been shown that colonoscopy can be performed successfully without sedation (Leung, 2010), but many patients feel discomfort during the procedure. Factors predicting a painful colonoscopy are female-gender, degree of patient nervousness and the technical difficulty of the colonoscopy (Ylinen et al. 2009). Also age under 40, previous abdominal surgery and use of sedation are associated with painful colonoscopy ( Seip et al. 2009). Most often sedation and/or analgesia are achieved by administering a benzodiazepine or a combination of a benzodiazepine and an opioid (Fanti et al. 2009, Maskelar et al. 2009,), dexmedetomidine (Dere et al. 2009) or by using non-pharmacologic methods (Amer-Cuenca et al. 2011). Tramadol as monotherapy did not significantly decrease pain intensity or endoscopist's evaluation of colonoscopy (Grossi et al. 2004). Currently, intravenous midazolam is the drug used most commonly to introduce some sedation for colonoscopy. Intravenous sedation definitely increases the cost of procedure; drug administration, need for pulse oximetry monitoring and the need for follow-up after the procedure make colonoscopy sometimes expensive and troublesome. It has also been shown, that low-dose midazolam neither relieves discomfort nor makes patients forget it (Elphick et al. 2009). Fentanyl is a short-acting opioid widely used in anesthesia management. Transmucosal sublingual formulation of fentanyl has been developed to further improve the management of pain. When administered as a sublingual fast-dissolving tablet (Abstral®) that is placed under the tongue, the effects is fast and predictable. Its active ingredient is absorbed by the body through the mucous membrane. After administration of buccal fentanyl maximum plasma drug concentration was measured after 25 minutes (Darwish et al. 2011). Plasma fentanyl concentrations versus time following buccal and sublingual administration are very similar (Darwish et al. 2008). Abstral® sublingual tablets should be administered directly under the tongue at the deepest part. Sublingual administration is an easy and non-invasive method of pain treatment for the patient coming to colonoscopy done as an office based procedure. Other advantages compared to invasive methods are improved comfort of patients and no need for intravenous access because of pain relief. Before, it has been used in the management of breakthrough pain in cancer patients. Sublingual fentanyl is shown to be effective and well-tolerated for the treatment of breakthrough cancer pain (Uberall et al. 2011). The use of transmucosal tablet for colonoscopy patients is a quite new approach.

Fentanyl Effect on Blood Pressure in Elderly Patients After Induction of General Anesthesia [Recruiting]
Hypotension is frequently encountered after induction of general anesthesia. It can be pronounced in elderly patients and can require administration of vasopressor agents including ephedrine and phenylephrine. Intraoperative hypotension, especially prolonged episodes, can contribute to an increase in morbidity and mortality in the postoperative period as suggested by some former studies. The investigators hypothesize that fentanyl can contribute to the decrease in blood pressure (BP) that is seen after induction of general anesthesia in older patients. This hypotension may be due to fentanyl blocking effect on the sympathetic nervous system. This study will be the first one to examine the effect of fentanyl administration on blood pressure in elderly patients with induction of general anesthesia prior to the start of surgery. If the study shows that fentanyl contributes to hypotension during this period, it may lead to a change in practice and better patient outcomes and mortality rates.

Remifentanil vs Fentanyl During Cardiac Surgery and Chronic Thoracic Pain [Recruiting]
This study will investigate the influence of intra-operative use of remifentanil versus fentanyl on the percentage of patients with chronic thoracic after cardiac surgery via sternotomy. Secondary quantitative sensory testing is performed to determine thermal and electrical detection and pain threshold and the difference in pain variability scoring. Postoperative pain scores, analgesic use, genetic variances and costs are measured.

Pharmacokinetic Study of Fentanyl 400 µg Sublingual Spray, Actiq 400 µg Transmucosally, and Fentanyl Citrate Injection 100 µg Intravenously (iv) [Completed]
The objective of this study was to compare the rate of absorption and bioavailability of fentanyl 400 g sublingual spray, Actiq 400 g transmucosally, and fentanyl citrate injection 100 g intravenously.

Bioequivalence of a Test Troche Formulation of Fentanyl Citrate (400 Mcg) Compared to Actiq 400 Mcg, Cephalon, Inc. [Completed]
The purpose of this study was to evaluate the oral bioequivalence of the Mallinckrodt test fentanyl citrate oral transmucosal 400 mcg troche compared to Actiq 400 mcg (Cephalon, Inc.) under fasting conditions.

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: 2017-09-28

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