Actiq (Fentanyl Citrate Oral Transmucosal) - Summary

ACTIQ SUMMARY

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 radiopaque and is fracture resistant (ABS plastic) under normal conditions when used as directed.

Actiq is indicated only for the management of breakthrough cancer pain in patients with malignancies who are already receiving and who are tolerant to opioid therapy for their underlying persistent cancer pain. Patients considered opioid tolerant are those who are taking at least 60 mg morphine/day, 50 mcg transdermal fentanyl/hour, or an equianalgesic dose of another opioid for a week or longer.

Because life-threatening hypoventilation could occur at any dose in patients not taking chronic opiates, Actiq is contraindicated in the management of acute or postoperative pain. This product must not be used in opioid non-tolerant patients.

Actiq 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.

Actiq should be individually titrated to a dose that provides adequate analgesia and minimizes side effects. 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 (see DOSAGE AND ADMINISTRATION).

Patients and their caregivers must be instructed that Actiq contains a medicine in an amount that can be fatal to a child. Patients and their caregivers must be instructed to keep all units out of the reach of children and to discard opened units properly in a secured container.

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NEWS HIGHLIGHTS

Media Articles Related to Actiq (Fentanyl Oral Transmucosal)

Opiate Painkillers May Encourage Spread Of Cancer
Source: Health News from Medical News Today [2009.11.23]
New research from the US adds weight to the growing body of evidence that opiate-based painkillers like morphine, which has been used to treat postoperative and chronic cancer pain for two hundred years, encourage cancer cells to grow and spread.

62-Year-Old Man Becomes First Patient In China Implanted With Rechargeable Neurostimulator For Chronic Pain
Source: Medical Devices / Diagnostics News From Medical News Today [2009.11.19]
St. Jude Medical, Inc. (NYSE:STJ) announced that a 62-year-old man from Shenzhen, Guangdong province has become the first patient in China to be implanted with the Eon™ neurostimulator, a rechargeable device used to help manage chronic pain. Despite prior back surgeries, the patient suffered from chronic back pain for more than a decade.

CNSBio Inc. To Present Latest Clinical Trial Data For CNSB015 At Neuropathic Pain Conference In San Francisco
Source: Pain / Anesthetics News From Medical News Today [2009.11.19]
CNSBio Inc. will present recent Phase IIa proof-of-concept clinical trial data for CNSB015, an orally administered potassium channel modulator used in combination with opioids for the treatment of neuropathic pain, at the 12th International Conference on the Mechanisms and Treatment of Neuropathic Pain on November 20-21, 2009 in San Francisco, CA. Dr.

Common Pain Relief Medication May Encourage Cancer Growth
Source: Pain / Anesthetics News From Medical News Today [2009.11.19]
Although morphine has been the gold-standard treatment for postoperative and chronic cancer pain for two centuries, a growing body of evidence is showing that opiate-based painkillers can stimulate the growth and spread of cancer cells. Two new studies advance that argument and demonstrate how shielding lung cancer cells from opiates reduces cell proliferation, invasion and migration in both cell-culture and mouse models.

Transplanting People's Own Stem Cells Into Heart Lessens Pain, Improves Ability To Walk
Source: Pain / Anesthetics News From Medical News Today [2009.11.19]
The largest national stem cell study for heart disease showed the first evidence that transplanting a potent form of adult stem cells into the heart muscle of subjects with severe angina results in less pain and an improved ability to walk. The transplant subjects also experienced fewer deaths than those who didn't receive stem cells.

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Published Studies Related to Actiq (Fentanyl Oral Transmucosal)

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.

Transmucosal fentanyl vs intravenous morphine in doses proportional to basal opioid regimen for episodic-breakthrough pain. [2007.06.18]
The use of supplemental doses of opioids is commonly suggested to manage breakthrough pain. A comparative study of intravenous morphine (IV-MO) and oral transmucosal fentanyl citrate (OTFC) given in doses proportional to the basal opioid regimen was performed in 25 cancer patients receiving stable opioid doses...

Oral transmucosal fentanyl citrate versus placebo for painful dressing changes: a crossover trial. [2007.03]
CONCLUSION: Compared with placebo, OTFC improved analgesia during painful dressing changes without an increase in side-effects.

Relative bioavailability of the fentanyl effervescent buccal tablet (FEBT) 1,080 pg versus oral transmucosal fentanyl citrate 1,600 pg and dose proportionality of FEBT 270 to 1,300 microg: a single-dose, randomized, open-label, three-period study in healthy adult volunteers. [2006.05]
BACKGROUND: The fentanyl effervescent buccal tablet (FEBT) was designed to enhance the rate and extent of absorption of fentanyl through the buccal mucosa. FEBT is being investigated for the management of breakthrough pain. OBJECTIVES: The primary objective of this study was to compare the relative bioavailability of FEBT 1,080 microg with that of oral transmucosal fentanyl citrate (OTFC) 1,600 microg, and the secondary objective was to assess the dose proportionality of FEBT 270 to 1,300 microg in healthy adult volunteers... CONCLUSIONS: In this pharmacokinetic study in healthy volunteers, total systemic exposure increased in a dose-proportional manner up to FEBT 1,300 microg, whereas doses above 810 microg showed a less-than-dose-proportional increase in C(max). The results suggest that fentanyl enters the systemic circulation to a significantly greater extent (C(max) and AUC(0-Tmax')) and significantly more rapidly (T(max)) with FEBT compared with OTFC.

The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia. [2004.11]
The bioavailability of oral transmucosal fentanyl citrate (OTFC) in children is similar to that of fentanyl solution administered orally to adults. We hypothesized that administering an oral fentanyl solution to children would result in similar fentanyl plasma concentrations and pharmacokinetic variables as administering comparable doses of OTFC.

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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 São 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.

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