Actiq

ACTIQ is a medication in a unique oral transmucosal delivery system (OTS?). It offers personal pain control by providing pain relief in 15 minutes (though you may not experience full relief for up to 45 minutes after finishing an ACTIQ unit). Actiq is designed to be dissolved slowly in the mouth in a manner to facilitate transmucosal absorption.

Actiq is supplied in six dosage strengths. Each unit is individually wrapped in a child-resistant, protective blister package.

Active Ingredient: Fentanyl citrate C-II

Pregnancy – Category C

Fentanyl has been shown to impair fertility and to have an embryocidal effect with an increase in resorptions in rats when given for a period of 12 to 21 days in doses of 30 mcg/kg IV or 160 mcg/kg subcutaneously.

Actiq Dose
200 mcg, 400 mcg, 600 mcg, 800 mcg, 1200 mcg, 1600 mcg

HIGHLIGHTS OF RECENT LABELING CHANGES
General considerations: Each
transmucosal unit contains about 2 g of sugar. Frequent consumption of products containing sugar may increase
the risk of dental caries, and dry mouth associated with opioid use may add to
the risk.
Patient counseling:  Diabetic
patients should be advised that each
unit contains about 2 g of sugar. To ensure appropriate oral hygiene, all
patients should be told to consult their dentist.

Manufacturer: Cephalon
Manufacturer’s website: www.cephalon.com
Product website: www.actiq.com


Indications/Dosage/Administration

Breakthrough cancer pain in patients with malignancies who are already
receiving and who are tolerant to opioid therapy for their underlying persistent
cancer pain:
200 µg to start; thereafter, closely follow patient
and change dosage level until patient reaches a dose providing adequate
analgesia using a single dosage unit per breakthrough cancer pain episode.
Redosing within a single episode: Until appropriate dose is reached,
patients may need to use an additional unit during a single episode. Start
redosing 15 min after previous unit has been completed (30 min after start
of previous unit. While patient is in titration phase and consuming units
that might be subtherapeutic individually, patient should take to more
than two units for each individual cancer breakthrough pain episode.

Patients considered to be opioid tolerant are taking at least 60
mg/day of morphine, 50 µg/h of transdermal fentanyl, or an equianalgesic
dose of another opioid for at least 1 wk.

Initial prescription: Prescribe an initial titration supply of
six 200-µg units to limit the number of units in the home during
titration; patient should use all units before increasing to a higher dose.

Increasing dose: If more than one unit
is needed per episode during treatment of several consecutive breakthrough
cancer pain episodes, consider an increase in dose. At each new dose during
titration, prescribe six units of the titration dose. Evaluate each
new dose over several episodes of breakthrough cancer pain (generally 1-2
days) to determine whether new dose provides adequate efficacy with acceptable
adverse events. Incidence of side effects is likely to be greater during
initial titration period.

Administration: Immediately before use, open foil package with
scissors. Place unit between cheek and lower gum, occasionally moving drug
matrix from one side to another using handle. Unit should not be chewed;
if chewed or swallowed, lower peak concentration and bioavailability may
occur. Advise patient to consume unit over 15 min; longer or shorter
consumption time may lead to lesser efficacy.

Titration of dosage: Individually titrate to a dose providing
adequate analgesia and minimal side effects. If signs of excessive opioid
effects appear before unit is consumed, remove dosage unit from patient’s
mouth immediately, dispose of unit properly, and decrease subsequent doses.
Patients should record their use of drug over several episodes of breakthrough
cancer pain and review their experience with their physicians.

Maximum daily dose: Once successful dose has been found, limit
consumption to four or less units/day. If consumption increases above this
level, reevaluate dose of long-acting opioid used for persistent cancer
pain.

Dosage adjustment: Dosage adjustment of both fentanyl and the
maintenance opioid analgesic may be needed to continue to provide adequate
relief of breakthrough cancer pain (see "Increasing
dose
," above). Consider increasing around-the-clock opioid dose
used for persistent cancer pain in patients who have over four breakthrough
cancer pain episodes daily.

Disposal of units: Advise patients to dispose of completely used
and partially used units. After complete consumption of unit and total
dissolution of matrix, throw handle away in a trash container out of reach
of children. If any drug matrix remains on handle, place handle under hot
running tap water until all of the drug matrix is dissolved, and then dispose
as above. Dispose of handles in the child-resistant container at least
once daily. If patient does not consume the entire unit and remaining drug
cannot be dissolved immediately as above, temporarily store the unit in
the provided child-resistant container until proper disposal is possible.
To dispose of unused units, remove unit from pouch using scissors, hold
unit by handle over the toilet bowl, cut off drug matrix end using wire-cutting
pliers so that it falls into the toilet, and dispose of handle in a place
out of reach of children; then flush toilet twice after 5 units have been
cut and deposited into the toilet. Do not flush entire units, handles,
foil pouches, or carton. If caregivers need more information, instruct
them to call 800/615-0187.

Discontinuation of therapy: A gradual downward titration is recommended
for patients discontinuing opioid therapy; it is not known at what dose
level the opioid may be discontinued without producing signs and symptoms
of abrupt withdrawal.


Patient Monitoring

Patient instructions: Question patients or caregivers of the
presence of children in the home on a full-time or visiting basis. Advise
patients and caregivers that this dosage form contains a medicine in an
amount that could be fatal to a child; partially consumed units pose a
particular risk. Instruct patients and caregivers to keep all units out
of the reach of children, and to discard opened units properly in a secured
container. Supply patients and providers with the Actiq Welcome Kit, which
contains educational materials, safe storage containers, and a patient
safety video; give patients the opportunity to discuss the video. For more
information on these materials, call 800/615-0187. Advise patients to consult
their dentist to ensure appropriate oral hygiene. Inform diabetics that each
unit contains about 2 g of sugar.


General Considerations

Hypersensitivity: Contraindicated in patients hypersensitive
to fentanyl or any component.

Inappropriate uses: Because of risk of life-threatening hypoventilation
at any dose in patients not taking chronic opiates, drug is contraindicated
in managing acute or postoperative pain. Risk of respiratory depression
begins at fentanyl plasma levels of 2 ng/mL in opioid nontolerant individuals;
do not use in opioid nontolerant patients.

Respiratory depression: Clinically significant hypoventilation
may occur; carefully observe patients for symptoms of respiratory depression.
Hypoventilation may occur more readily when opioids are given with other
respiratory depressants. Titrate with caution in patients with chronic
obstructive pulmonary disease or preexisting medical conditions that may
predispose to hypoventilation; normal analgesic doses of opioids may further
decrease respiratory drive to point of respiratory failure.

Ambulatory patients: Caution patients not to engage in potentially
hazardous activities requiring full mental alertness.

Sugar content/dental caries: Each unit contains about 2 g of sugar.
Frequent consumption of products containing sugar may increase risk of dental
caries, and dry mouth associated with opioid use may add to risk.

Renal or hepatic impairment: Use caution because of importance
of the liver and kidney in the metabolism and excretion of drugs and effects
on plasma binding proteins.

Advanced age: Elderly patients are twice as sensitive to effects
of fentanyl as are younger patients. Use caution.

Adverse reactions: Side effects seen are typical of opioids;
adverse events frequently will stop or decrease in intensity with continued
use, as patient is properly titrated. Manage side effects accordingly.

Dependence: Physical dependence usually does not occur until
after several weeks of continued opioid usage; tolerance initially is manifested
by shortened duration of analgesic effect and decreased intensity of analgesia.

Head injuries, increased intracranial pressure: Use extreme caution
in patients who may be particularly susceptible to intracranial effects
of CO2 retention (eg, those with increased intracranial
pressure, impaired consciousness). Opioids may obscure clinical course
of patients with head injury; use only if clinically warranted.

Cardiac disease: Use caution in patients with bradyarrhythmias;
drug may produce bradycardia.

Pregnancy: Use only if expected benefits justify potential fetal
risks (Pregnancy Category C).

Labor and delivery: Not indicated for analgesia during labor
and delivery.

Breast-feeding: Do not use in nursing mothers.

Pediatric use: Appropriate dosing and safety in opioid tolerant
children under 16 yr of age with breakthrough cancer pain not established.


Adverse Reactions
Frequent reactions (incidence of 1% or more) are printed
in italics. Reactions were reported in 254 patients taking any dose
tested. All patients also were taking concomitant opioids, such as sustained-release
morphine or transdermal fentanyl, for persistent cancer pain.

Cardiovascular: Migraine (1% or more); deep
thrombophlebitis, hypertension, and hypotension (< 1%).

Dermatologic: Pruritus, rash, and sweating (2%); alopecia
and exfoliative dermatitis (< 1%).

Digestive: Nausea (23%), vomiting (12%), constipation (4%);
diarrhea, dyspnea, and flatulence (1% or more);
anorexia, eructation,
esophageal stenosis, fecal impaction, gum hemorrhage, mouth ulceration,
and oral moniliasis (< 1%).

Genitourinary: Vaginal hemorrhage, dysuria, hematuria, urinary
incontinence, and urinary tract infection (< 1%).

Neurologic: Dizziness and somnolence (17%), asthenia (9%),
headache (6%), confusion (4%), anxiety (3%), abnormal gait, dry mouth,
nervousness, and vasodilatation (2%), hallucinations, insomnia, abnormal
thinking, vertigo, and hypesthesia (1% or more);
abnormal dreams, urinary
retention, agitation, amnesia, emotional lability, euphoria, incoordination,
decreased libido, neuropathy, paresthesia, and speech disorder (< 1%).

Respiratory: Dyspnea (4%); pharyngitis, increased cough (1%
or more);
hemoptysis, pleural effusion, rhinitis, asthma, hiccup, pneumonia,
respiratory insufficiency, and increased sputum (< 1%).

Miscellaneous: Accidental injury and abnormal vision (2%);
pain, fever, abdominal pain, chills, back pain, chest pain, infection,
peripheral edema, and dehydration (1% or more)
; flu syndrome, abscess,
bone pain, anemia, leukopenia, edema, hypercalcemia, weight loss, myalgia,
pathological fracture, myasthenia, and taste perversion (< 1%).


Drug Interactions

CNS depressants, including alcohol; sedatives, hypnotics, general
anesthetics, phenothiazines, tranquilizers, skeletal muscle relaxants,
sedating antihistamines, other opioids:
Increased CNS depression. Hypoventilation,
hypotension, and profound sedation may occur.

Potent inhibitors of cytochrome P450 3A4 isoform (eg, ketoconazole,
erythromycin, and certain protease inhibitors [eg, ritonavir]):
Increased
or prolonged CNS depression. Hypoventilation, hypotension, and profound
sedation may occur. Monitor patients for a change in opioid effects and
adjust dose, if warranted.

MAO inhibitors: Not recommended for use in patients who
have received MAO inhibitors within 14 days, since severe and unpredictable
potentiation by MAO inhibitors reported with use of opioids.


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