ACTIQ (fentanyl citrate) oral transmucosal lozenge is a solid formulation of fentanyl, an opioid agonist, 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.
Fentanyl citrate, USP is N-(1-Phenethyl-4-piperidyl) propionanilide citrate (1:1). Fentanyl is a highly lipophilic compound (octanol-water partition coefficient at pH 7.4 is 816:1) that is freely soluble in organic solvents and sparingly soluble in water (1:40). The molecular weight of the free base is 336.5 (the citrate salt is 528.6). The pKa of the tertiary nitrogens are 7.3 and 8.4. The compound has the following structural formula:
Hydrated dextrates, citric acid, dibasic sodium phosphate, artificial berry flavor, magnesium stearate, and edible glue (modified food starch and confectioner’s sugar).
ACTIQ 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-theclock opioid therapy for their underlying persistent cancer pain.
Patients considered opioid tolerant are those who are taking, for one week or longer, around-the-clock medicine consisting of at least 60 mg of oral morphine per day, at least 25 mcg of transdermal fentanyl per hour, at least 30 mg of oral oxycodone per day, at least 8 mg of oral hydromorphone per day, at least 25 mg oral oxymorphone per day, at least 60 mg of oral hydrocodone per day, or an equianalgesic dose of another opioid . Patients must remain on around-the-clock opioids when taking ACTIQ.
Limitations Of Use
- Not for use in opioid non-tolerant patients.
- Not for use in the management of acute or postoperative pain, including headache/migraine and dental pain [see CONTRAINDICATIONS].
- 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.
DOSAGE AND ADMINISTRATION
Important Dosage And Administration Instructions
- Healthcare professionals who prescribe ACTIQ on an outpatient basis must enroll in the TIRF REMS Access program and comply with the requirements of the REMS to ensure safe use of ACTIQ [see WARNINGS AND PRECAUTIONS].
- Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals [see WARNINGS AND PRECAUTIONS].
- It is important to minimize the number of strengths available to patients at any time to prevent confusion and possible overdose.
- Initiate the dosing regimen for each patient individually, taking into account the patient’s severity of pain, patient response, prior analgesic treatment experience, and risk factors for addiction, abuse, and misuse [see WARNINGS AND PRECAUTIONS].
- Monitor patients closely for respiratory depression, especially within the first 24-72 hours of initiating therapy and following dosage increases with ACTIQ and adjust the dosage accordingly [see WARNINGS AND PRECAUTIONS].
- Instruct patients and caregivers to take steps to store ACTIQ securely and to properly dispose of unused ACTIQ as soon as no longer needed [see WARNINGS AND PRECAUTIONS, Patient Counseling Information].
- Other TIRF formulations and ACTIQ are not equivalent. DO NOT substitute an ACTIQ prescription for any other TIRF formulation under any circumstances. Do not convert patients on a mcg per mcg basis from any other fentanyl product to ACTIQ [see WARNINGS AND PRECAUTIONS].
Individually titrate ACTIQ to a dose that provides adequate analgesia and minimizes side effects. The initial dose of ACTIQ to treat episodes of breakthrough cancer pain is always 200 mcg. The ACTIQ unit should be consumed over 15 minutes. Patients should be prescribed an initial titration supply of six 200 mcg ACTIQ 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.
- In cases where the breakthrough pain episode is not relieved after 15 minutes after completion of the ACTIQ unit (30 minutes after the start of the unit), patients may take ONLY ONE additional dose using the same strength for that episode. Thus patients should take a maximum of two doses of ACTIQ for any episode of breakthrough pain.
- Patients MUST wait at least 4 hours before treating another episode of breakthrough pain with ACTIQ.
From an initial dose, closely follow patients and change the dosage strength until the patient reaches a dose that provides adequate analgesia using a single ACTIQ 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 patientâ€™s mouth immediately, disposed of properly, and subsequent doses should be decreased. Patients should record their use of ACTIQ 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 ACTIQ 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 ACTIQ for any breakthrough pain episode.
Patients must wait at least 4 hours before treating another episode of breakthrough pain with ACTIQ. To reduce the risk of overdosing during titration, patients should have only one strength of ACTIQ available at any one time.
- Once titrated to an effective dose, patients should generally use ONLY ONE ACTIQ 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 ACTIQ 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 ACTIQ. 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 ACTIQ may be required in some patients in order to continue to provide adequate relief of breakthrough pain.
- Generally, the ACTIQ 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 ACTIQ
Open the blister package with scissors immediately prior to product use. The patient should place the ACTIQ 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 ACTIQ unit should be sucked, not chewed. A unit dose of ACTIQ, if chewed and swallowed, might result in lower peak concentrations and lower bioavailability than when consumed as directed [see CLINICAL PHARMACOLOGY].
The ACTIQ unit should be consumed over a 15-minute period. Longer or shorter consumption times may produce less efficacy than reported in ACTIQ clinical trials. If signs of excessive opioid effects appear before the unit is consumed, remove the drug matrix from the patientâ€™s mouth immediately and decrease future doses.
Discontinuation Of ACTIQ
When opioid therapy is no longer required, consider discontinuing ACTIQ along with a gradual downward tapering (titration) of other opioids to minimize possible withdrawal effects. In patients who continue to take their chronic opioid therapy for persistent pain but no longer require treatment for breakthrough pain, ACTIQ therapy can usually be discontinued immediately. [see Drug Abuse And Dependence]
Disposal Of ACTIQ
After consumption of the unit is complete and the matrix is totally dissolved, throw away the handle in a trash container that is out of the reach of children.
- If any of the drug matrix remains on the handle, place the handle under hot running tap water until all of the drug matrix is dissolved, and then dispose of the handle in a place that is out of the reach of children.
- Dispose of handles in the child-resistant container (as described in steps 1 and 2) at least once a day.
If the temporary storage bottle provided as part of the ACTIQ Child Safety Kit is available, partially consumed units may be stored in the specially provided child-resistant container out of the reach of children until proper disposal is possible.
Unopened units remaining from a prescription must be properly disposed as soon as they are no longer needed.
To dispose of the unused ACTIQ units:
- Remove the ACTIQ unit from its blister package using scissors, and hold ACTIQ by its handle over the toilet bowl.
- Using wire-cutting pliers cut off the drug matrix end so that it falls into the toilet.
- Dispose of the handle in a place that is out of the reach of children.
- Repeat steps 1, 2, and 3 for each ACTIQ unit. Flush the toilet twice after 5 units have been cut and deposited into the toilet.
Do not flush the entire ACTIQ units, ACTIQ handles, blister packages, or cartons down the toilet. Dispose of the handle where children cannot reach it.
In the event that a caregiver requires additional assistance in disposing of excess unusable units that remain in the home after a patient has expired, instruct them to call the toll-free number for Teva Pharmaceuticals (1-888-483-8279) or seek assistance from their local DEA office.
Dosage Forms And Strengths
Solid oral transmucosal lozenge: 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. ACTIQ is available in 200 mcg, 400 mcg, 600 mcg, 800 mcg, 1200 mcg and 1600 mcg strengths [see HOW SUPPLIED/Storage And Handling].
Storage And Handling
ACTIQ is supplied in six dosage strengths. Each unit is individually wrapped in a child-resistant, protective blister package. These blister packages are packed 30 per shelf carton for use when patients have been titrated to the appropriate dose.
Each dosage unit has a white to off-white color. Each individual solid drug matrix is marked with “ACTIQ” and the strength of the unit (“200”, “400”, “600”, “800”, “1200”, or “1600”). The dosage strength is also marked on the handle tag, the blister package and the carton. See blister package and carton for product information.
|Dosage Strength (fentanyl base)||Carton/Blister Package Color||NDC Number|
|200 mcg||Gray||NDC 63459-502-30|
|400 mcg||Blue||NDC 63459-504-30|
|600 mcg||Orange||NDC 63459-506-30|
|800 mcg||Purple||NDC 63459-508-30|
|1200 mcg||Green||NDC 63459-512-30|
|1600 mcg||Burgundy||NDC 63459-516-30|
Note: Colors are a secondary aid in product identification. Please be sure to confirm the printed dosage before dispensing.
Store at 20-25°C (68-77°F) with excursions permitted between 15° and 30°C (59° to 86°F) until ready to use. (See USP Controlled Room Temperature.) Protect ACTIQ from freezing and moisture. Do not use if the blister package has been opened.
Store ACTIQ securely and dispose of properly [see PATIENT INFORMATION].
Distributed By: Teva Pharmaceuticals USA, Inc., North Wales, PA 19454. Revised: Oct 2019