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Indications

High Alert

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Exercise Extreme Caution in:

Adv. Reactions/Side Effects

CV: hypotension.

Endo: adrenal insufficiency.

GI: constipation, nausea, vomiting, abdominal pain, anorexia, dry mouth.

Neuro: dizziness, drowsiness, headache, confusion, depression, fatigue, hallucinations, headache, insomnia, weakness.

Resp: dyspnea, RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), physical dependence, psychological dependence.

Interactions

Drug-Drug:

Drug-Natural Products:

Drug-Food:

Availability

(Generic available)

Route/Dosage

Transmucosal products are not equivalent on a mcg-to-mcg basis.

US Brand Names

Fentanyl (Buccal Tablet): Fentora

Fentanyl (Oral Transmucosal Lozenge): Actiq

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: opioid analgesics

Pharmacologic Classification: opioid agonists

Pharmacokinetics

Absorption: Buccal tablet: 65% absorbed from buccal mucosa; 50% is absorbed transmucosally, remainder is swallowed and is absorbed slowly from the GI tract. Buccal absorption is enhanced by an effervescent reaction in the dose form; Transmucosal lozenge: Initial rapid absorption (25%) from buccal mucosa is followed by more prolonged absorption (25%) from GI tract (combined bioavailability 50%).

Distribution: Readily crosses the placenta and enters breast milk.

Metabolism/Excretion: Mostly metabolized in the liver and intestinal mucosa via the CYP3A4 isoenzyme; inactive metabolites are excreted in urine; <7% excreted unchanged in urine.

Half-life: Buccal tablet: 2.6–11.7 hr (↑ with dose); Transmucosal lozenge: 7 hr.

Contr. Subst. Schedule

Schedule II (C-II)

Time/Action Profile

(↓ pain)

ROUTEONSETPEAKDURATION
Buccal tablet15 min40–60 min60 min
Transmucosal lozengerapid15–30 minseveral hr

Patient/Family Teaching

Pronunciation

FEN-ta-nil

Code

NDC Code*