ACTIQ
Clinical safety rating
cautionComprehensive clinical and safety monograph for ACTIQ (ACTIQ).
Opioid agonist; binds to mu-opioid receptors in the CNS, altering pain perception and response.
| Metabolism | Primarily hepatic via CYP3A4 to inactive metabolites (norfentanyl, despropionylfentanyl, hydroxyfentanyl) and other metabolites; <7% excreted unchanged in urine. |
| Excretion | Primarily renal as metabolites (about 75% as metabolites, <10% unchanged). Fecal excretion accounts for <9%. Biliary excretion is minor. |
| Half-life | Terminal half-life 0.83–2 hours (mean 1.3 h) in adults; note that context: transmucosal absorption leads to rapid onset but short duration; half-life is not correlated with clinical effect due to oral transmucosal route and rapid redistribution. |
| Protein binding | Fentanyl is 80–85% bound to plasma proteins (primarily albumin and α1-acid glycoprotein). |
| Volume of Distribution | Approximately 4 L/kg (range 3–6 L/kg); large Vd indicates extensive tissue distribution and redistribution contributing to short duration. |
| Bioavailability | Oral transmucosal: 50% (range 47–54%) relative to IV; variable and enhanced by rapid absorption through buccal mucosa. |
| Onset of Action | Transmucosal: 5–15 minutes (analgesic effect); peak effect at 20–30 minutes. |
| Duration of Action | Analgesic duration 2–4 hours (dose-dependent; shorter with lower doses and longer with higher doses). Clinical note: duration may be shorter in opioid-tolerant patients. |
| Molecular Weight | 336.47 |
| Action Class | Disease Modifying Anti-Rheumatoid Drugs (DMARDs)- Non biologics |
| Brand Substitutes | HQ 200mg Tablet, Rumawill 200mg Tablet, ZY-Q 200 Tablet, Rarex 200mg Tablet |
200 mcg transmucosally, titrated upward as needed; initial dose for opioid-tolerant patients is 200 mcg, with additional doses possible after 15 minutes if needed. Maximum 4 doses per episode. At least 4 hours between episodes.
| Dosage form | TROCHE/LOZENGE |
| Renal impairment | No specific GFR-based dose adjustment recommended; use with caution in severe renal impairment (CrCl < 30 mL/min) and consider dose reduction due to potential accumulation. |
| Liver impairment | Child-Pugh Class A/B: No adjustment. Child-Pugh Class C: Reduce initial dose to 100 mcg and titrate slowly; monitor closely for prolonged effects. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established in patients under 16 years. |
| Geriatric use | Initiate at 100 mcg transmucosally; titrate slowly due to increased sensitivity and risk of respiratory depression. Monitor for adverse effects. |
| 1st trimester | Insufficient human data; animal studies suggest potential harm; use only if benefit outweighs risk. |
| 2nd trimester | Limited data; risk of fetal dependence and withdrawal; avoid unless clearly needed. |
| 3rd trimester | Risk of neonatal respiratory depression, withdrawal syndrome; avoid prolonged use or high doses near term. |
Clinical note
Comprehensive clinical and safety monograph for ACTIQ (ACTIQ).
| Placental transfer | Fentanyl crosses the placenta readily; can cause fetal dependence and neonatal abstinence syndrome with chronic use. |
| Breastfeeding | Fentanyl passes into breast milk in small amounts. With short-term maternal use, effects on infant are minimal, but monitor for sedation and respiratory depression. With chronic use, potential for infant withdrawal. Avoid breastfeeding if mother is on high doses or prolonged therapy. |
| Lactation Rating | L3 (Moderately Safe) for short-term use; L4 (Possibly Hazardous) for chronic or high-dose use. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: limited human data; animal studies show increased resorptions and fetal growth restriction. Second/third trimester: chronic use may cause neonatal opioid withdrawal syndrome; avoid use during labor due to risk of neonatal respiratory depression. |
| Fetal Monitoring | Monitor maternal respiratory rate, sedation, and bowel function. Fetal monitoring for signs of opioid withdrawal in chronic use; during third trimester, assess fetal growth and amniotic fluid volume. |
| Fertility Effects | Opioids may impair fertility in both sexes. In males, potential for decreased libido and erectile dysfunction; in females, possible menstrual irregularities due to altered hypothalamic-pituitary-gonadal axis. |
■ FDA Black Box Warning
Risk of respiratory depression, addiction, abuse, and misuse; accidental ingestion can be fatal; concomitant use with benzodiazepines or CNS depressants may cause profound sedation, respiratory depression, coma, and death; not for use in opioid non-tolerant patients; risk of neonatal opioid withdrawal syndrome with prolonged use during pregnancy; serious, life-threatening, or fatal respiratory depression may occur even at recommended doses.
| Serious Effects |
Significant respiratory depressionAcute or severe bronchial asthmaKnown or suspected gastrointestinal obstructionConcurrent use of MAO inhibitors or within 14 daysHypersensitivity to fentanyl or any component
| Precautions | Risk of respiratory depression; addiction, abuse, and misuse; interactions with CNS depressants; serotonin syndrome; adrenal insufficiency; severe hypotension; seizures; withdrawal; use in patients with head injuries, increased intracranial pressure, biliary tract disease, pancreatitis; risk of choking with lozenge; oral mucosal irritation; dental caries; hypokalemia; hyponatremia; use in elderly, cachectic, or debilitated patients. |
| Food/Dietary | No significant food interactions. Grapefruit juice may increase fentanyl levels, but specific studies with ACTIQ are lacking. Avoid alcohol, as it may increase sedation and respiratory depression risk. |
| Clinical Pearls | ACTIQ is a transmucosal immediate-release fentanyl formulation indicated for breakthrough cancer pain in opioid-tolerant patients. Initiate with the lowest strength (200 mcg) and titrate upward. Avoid use in opioid-naive patients due to risk of fatal respiratory depression. Place the unit between cheek and lower gum, not sublingually. Instruct patient not to bite or suck the unit. Monitor for sedation and respiratory depression. Multiple units may be used per episode if needed, but wait at least 4 hours before next episode. Dispose of partially used units by flushing down toilet. |
| Patient Advice | Only use ACTIQ if you are already taking regular around-the-clock opioid pain medicine and are tolerant to opioids. · Do not use ACTIQ for short-term pain like after surgery, headache, or dental pain. · Place the unit in your cheek pouch, not under your tongue. Do not chew or suck it. · If you need more than 4 units per day, contact your doctor as your dose may need adjustment. · Store ACTIQ in a safe place away from children, as accidental ingestion can be fatal. · Dispose of unused or partially used units by flushing them down the toilet. |
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