Fentanyl Oralet

Fentanyl Oralet only as anesthetic premedication Actiq only as management of breakthrough cancer pain Chronic pain... 

An additional opioid preparation that may be considered for patients who cannot tolerate oral analgesics but continue to experience brief episodes of severe pain is the fentanyl oralet (Actiq ). Fentanyl oralet releases between 100-400 pg of fentanyl within 15 minutes with high bioavailability. While not approved for acute pain management, this preparation is eflfec-... 

Generic Names fentanyl oralet, fentanyl buccal tablet... 

Fentanyl oralet (ACTIQ) is formulated as a sohd formulation of fentanyl, and is designed to be dissolved slowly in the mouth to facihtate transmucosal absorption (Figure 27.2). Fentanyl buccal tablets have a higher bioavailability of fentanyl than fentanyl oralet so they are not equivalent on a pg per pg basis. 

Metabolic pathways fentanyl buccal tablets have an absolute bioavailability of 65% following oral administration, compared to an absolute bioavailability of 50% following oral administration of fentanyl oralet. The difference is mainly due to the fact that 50% of the total dose administered of fentanyl buccal tablet is absorbed transmucosally vs. 25% of fentanyl oralet. The remaining half of the total dose of fentanyl buccal tablets and 75% of the total dose of fentanyl oralet is swallowed and undergoes more prolonged absorption from the gastrointestinal tract. About 1/3 of this amount (25% of the total dose) escapes hepatic and intestinal first-pass elimination and becomes systemically available. Therefore, a unit... 

Fentanyl buccal tablets and fentanyl oralet are both indicated for the management of breakthrough pain in patients with cancer and who are already receiving and who are tolerant to opioid therapy for their underlying continual cancer pain. 

Absolute fentanyl buccal tablets and fentanyl oralets are contraindicated in patients with known severe allergic reaction to fentanyl. 

Relative they are contraindicated in the management of acute or post-operative pain. They are not indicated for use in opioid non-tolerant patients. The safety and efficacy of fentanyl buccal tablets and fentanyl oralet have not been establidied in pediatric patients below the age of 16 years. They ould be used cautiously in patients with a history ofbradyarrhthymias, or with evidence of increased intracranial pressure or impaired consciousness, or with history of chronic obstructive pulmonary disease, or preexisting medical conditions predisposing them to respiratory depression. 

Management of breakthrough cancer pain with Actiq (fentanyl oralet)... 

When comparing the two, the buccal tablets have some potential advantages over fentanyl oralets. The buccal tablet formulation is more discreet than the oralet lollipop . Also the enhanced oral mucosal absorption allows for faster onset of pain relief (5-10 minutes) versus the oralet (10-20 minutes). Differences between the two preparations are outlined in Table 27.1. 

Drug interactions since fentanyl is metabolized mainly via the human cytochrome P450 3A4 isoenzyme system (CYP3A4) possible interactions may occur when fentanyl buccal tablet or fentanyl oralet is given along with medications that affect CYP3A4 activity. 

Also both fentanyl buccal tablets and fentanyl oralet should not be given to patients who have also taken an MAO inhibitor within 14 days, because MAO inhibitors have been reported to unpredictably potentiate fentanyl. 

Adverse events there is a greater risk of abuse of both fentanyl buccal tablets and fentanyl lozenges since they are both taken orally. Fentanyl oralet has been shown to have variabihty in fentanyl availability because of variation in patient mouth surface area, and the percentage of medication that is absorbed through oral mucosa versus the percentage swallowed. 

The most common adverse events seen with fentanyl buccal tablets and fentanyl lozenges are typical of opioid side effects. The most serious adverse reactions with all opiods include respiratory depression, circulatory depression, hypotension, and shock. Other common opioid side effects include nausea, vomiting, fatigue, dizziness, drowsiness, constipation, and headache. Dental caries has been reported with the use of fentanyl oralet. A minor adverse event with fentanyl buccal tablets is mouth ulcer. 

Fentanyl Oralet (Actiq ) can be a useful adjunct in children with cancer pain or other chronic pain. Don t call it a lollipop. 

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