Actiq

— THERAPEUTIC CATEGORIES —
  • Narcotic analgesics
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Actiq Generic Name & Formulations

    Legal Class

    CII

    General Description

    Fentanyl (as citrate) 200mcg, 400mcg, 600mcg, 800mcg, 1200mcg, 1600mcg; units for oral transmucosal administration; berry-flavored.

    Pharmacological Class

    Opioid agonist.

    How Supplied

    Lozenge units—30

    Manufacturer

    Teva Pharmaceuticals

    Generic Availability

    YES

    Mechanism of Action

    Fentanyl is an opioid agonist whose principal therapeutic action is analgesia.

    Actiq Indications

    Indications

    Breakthrough pain, in opioid-tolerant patients already receiving and who are tolerant to continuous opioid therapy for underlying persistent cancer pain. Opioid-tolerant patients are those taking oral morphine ≥60mg/day, transdermal fentanyl ≥25mcg/hr, oral oxycodone ≥30mg/day, oral hydromorphone ≥8mg/day, oral oxymorphone ≥25mg/day, oral hydrocodone ≥60mg/day, or equianalgesic dose of another opioid for ≥1 week.

    Actiq Dosage and Administration

    Adult

    Do not substitute with other fentanyl products; not equivalent to other fentanyl products on a mcg to mcg basis. Use lowest effective dose for shortest duration. ≥16yrs: Place unit between cheek and lower gum, occasionally switching sides. Suck (do not chew) over 15mins; if excessive opioid effects occur, remove unit and reduce next dose. Initially one 200mcg unit. Titrate, evaluating dose over several episodes of pain, until a single unit provides adequate analgesia. If re-dosing for one pain episode is needed, start second unit 15mins after first unit is finished; max 2 units/episode. Wait at least 4hrs before treating another episode. Prescribe 6 units during titration. After a successful dose is determined: max 4 units/day. Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).

    Children

    <16yrs: not established.

    Actiq Contraindications

    Contraindications

    Opioid non-tolerant patients. Significant respiratory depression. Acute or post-op pain (including headache/migraine, dental pain, or ER). Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus.

    Actiq Boxed Warnings

    Boxed Warning

    Serious and life-threatening risks from use of Actiq: Addiction, abuse, and misuse; Life threatening respiratory depression; Accidental ingestion; Risks from concomitant use of CYP3A4 inhibitors/inducers, benzodiazepines, or other CNS depressants; Risk of medication errors; REMS program; Neonatal opioid withdrawal syndrome.

    Actiq Warnings/Precautions

    Warnings/Precautions

    Assess the potential need for access to naloxone when initiating and renewing therapy. Consider prescribing naloxone based on risk factors for overdose (eg, history of opioid use disorder, prior opioid overdose, household members or other close contacts at risk for accidental ingestion or overdose). Life-threatening respiratory depression; monitor within first 24–72hrs of initiating therapy and following dose increases. Accidental exposure may cause fatal overdose (esp. in children). Opioid-induced hyperalgesia (OIH) and allodynia; consider dose reduction of current opioid or opioid rotation if OIH is suspected. Sleep-related breathing disorders (including central sleep apnea (CSA), sleep-related hypoxemia); consider dose reduction if CSA develops. COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Abuse potential (monitor). Adrenal insufficiency. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Bradyarrhythmias. Drug abusers. Renal or hepatic impairment. Reevaluate periodically. Avoid abrupt cessation. Elderly. Cachectic. Debilitated. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery, nursing mothers: not recommended.

    REMS

    YES

    Actiq Pharmacokinetics

    Distribution

    Mean volume of distribution at steady-state: 4 L/kg. Plasma protein bound: 80–85%.

    Metabolism

    Hepatic (CYP3A4). 

    Elimination

    Primarily (>90%) eliminated by biotransformation; renal (<7%), fecal (~1%). Half-life: ~7 hours. Total plasma clearance: 0.5 L/hr/kg (range: 0.3–0.7 L/hr/kg).

    Actiq Interactions

    Interactions

    Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor closely; consider prescribing naloxone if concomitant use is warranted. During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, cyclobenzaprine, metaxalone, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid concomitant mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and/or precipitate withdrawal symptoms. Potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors, grapefruit juice). Antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics; monitor. Paralytic ileus may occur with anticholinergics.

    Actiq Adverse Reactions

    Adverse Reactions

    Nausea, dizziness, somnolence, vomiting, asthenia, headache, dyspnea, constipation, anxiety, confusion, depression, rash, insomnia; respiratory depression, severe hypotension, syncope, OIH and allodynia.

    Actiq Clinical Trials

    See Literature

    Actiq Note

    Notes

    Available by restricted distribution program. Call (866) 822-1483 or visit www.tirfremsaccess.com to enroll.

    Actiq Patient Counseling

    See Literature

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