Fentanyl Citrate Sublingual Dosing And Stability

Fentanyl S/L:

- Use: incident pain


- Onset of action: 5-15 minutes

- Peak effect: within 20 minutes

- Duration of action: maximum 45minutes

- Supplied: 100mcg/2ml ampoules (Sublimaze®) – glass ampoules.

* Needs special authorization for Alberta Blue Cross

- Note: decreased saliva production can delay absorption of sublingual fentanyl

- If administered sublingually, the drugs have to remain there for at least 5 minutes.
- Oral bioavailability of fentanyl is negligible and therefore this medication cannot be taken orally.
- Patients are generally unable to keep more than 1.5ml to 2ml under the tongue before it dribbles into the mouth, rendering it inactive.

Counseling:

- Determine the maximum amount of liquid that can be held under the tongue using the cold water technique (pt should be able to feel cold water trickling down throat).

o Max 1.5 ml – 2ml (CHR long term care formulary)

o Max 0.5 ml – 1ml (cold water test)

- Fentanyl must remain under the tongue for at least 5 minutes to be absorbed.

o Oral bioavailability of fentanyl is negligible and therefore this medication cannot be taken orally.

- Any remaining/extra fentanyl in the amp should be drawn up to a syringe and kept in the fridge.


CHR Incident Pain Protocol*

Step 1: Fentanyl 12.5mcg (0.25ml)

Step 2: Fentanyl 25 mcg (0.5ml)

Step 3: Fentanyl 50 mcg (1ml)

Step 4: Fentanyl 100 mcg (2ml)

- Opioid naïve pt: start at Step 1.

- If the pt is opioid tolerant, then start at Step 2.

- If pt unable to tolerate the volume in a single dose then the volume may be given in 2 doses at an interval of 5-10minutes apart. (ie: 2ml – take 1ml twice 5 minutes apart).

- After 10-15 minutes, if the initial dose appears to be insufficient, then the same dose may be repeated up to 2 further doses, at 10-15 minute intervals.

- Consider moving to the next step of the protocol if the maximum number of doses (3) is required to achieve comfort. One may move to the next step of the protocol after one hour of the last dose of fentanyl.

- The Incident Pain Protocol may be used up to q1h.

Side Effects:

Drowsiness, sedation, nausea and vomiting. Respiratory depression is dose dependent, it could potentially occur with an initial fentanyl dose greater than 200mcg IV.

Stabilty:

Undiluted fentanyl citrate 50 mcg/mL was tested for stability in polypropylene syringes. The fentanyl citrate injection was filled into polypropylene syringes that were then capped off. The samples were stored for 28 days under refrigeration at 5 °C and at room temperature of 22 °C exposed to light. No change in color or clarity occurred. No loss of fentanyl citrate at either set of storage conditions occurred when evaluated using stability-indicating HPLC analysis.

*Hecq JD, Boitquin LP, Venbeckbergen DF et al. Effect of freezing, long-term storage, and microwave thawing on the stability of ketorolac tromethamine. Ann Pharmacother. 2005; 39:1654-8. [PubMed 16159993]

[Accessed Feb 10/10: Handbook on Injectable Drugs - 15th Ed. (2009)]

Pharmacy On-Call (Calgary Pharmacy) will premix syringes which are stable for 1 week.

*Calgary Health Region Long Term Care Formulary: fentanyl citrate injection.