Table 1.

Key pharmacokinetic parameters for approved formulations of fentanyl for breakthrough pain²²,²⁸–³⁰,³²,³³

Agent	Available strengths	Absolute bioavailability	Fraction absorbed transmucosally	Tmax	Cmax	AUC0–infa	t½
Oral transmucosal fentanyl citrate (ACTIQ®)28,b	200 μg 400 μg 600 μg 800 μg 1200 μg 1600 μg	50% compared to intravenous fentanyl	25% though buccal mucosa	20–40 minutes (range 20–80 minutes) for doses from 200 μg to 1600 μg	0.39–2.51 ng/mL for doses from 200 μg to 1600 μg	102 ng-minute/mL for 200 μg to 1026 ng-minute/mL for 1600 μg (AUC0–1440)	193–386 minutes for doses from 200 μg to 1600 μg (mean)
Fentanyl buccal tablets (FENTORA®)22	100 μg 200 μg 300 μg 400 μg 600 μg 800 μg	65%	48% though buccal mucosa	35–45 minutes (range 20–181 minutes) for doses from 100 μg to 800 μg	0.25–1.59 ng/mL for doses from 100 μg to 800 μg	0.98–9.05 ng-hour/mL for doses from 100 μg to 800 μg	2.63–11.70 hours for doses from 100 μg to 800 μg
Fentanyl buccal soluble film (ONSOLIS®)29	200 μg 400 μg 600 μg 800 μg 1200 μg	71%	51% though buccal mucosa	60 minutes (range 45–240 minutes) for 800 μg dose	0.38–2.19 ng/mL for doses from 200 μg to 1200 μg	3.46–20.43 ng-hour/mL for doses from 200 μg to 1200 μg	~14 hours (terminal t½)
Sublingual fentanyl tablet (ABSTRAL®)30	100 μg 200 μg 300 μg 400 μg 600 μg 800 μg	54%	N/A	30–60 minutes (range 16–240 minutes) for doses from 100 μg to 800 μg	0.187–1.42 ng/mL for doses from 100 μg to 800 μg	0.974–8.95 ng-hour/mL for doses from 100 μg to 800 μg	5.02–10.1 hours for doses from 100 μg to 800 μg
Sublingual fentanyl spray (SUBSYS™)31	100 μg 200 μg 400 μg 600 μg 800 μg	76%	N/A	0.69–1.25 hours (range 0.08–4.00 hours) for doses from 100 μg to 800 μg	0.20–1.61 ng/mL for doses from 100 μg to 800 μg	1.25–10.38 ng-hour/mL for doses from 100 μg to 800 μg	5.25–11.99 hours for doses from 100 μg to 800 μg
Intranasal fentanyl spray (Instanyl®)32	50 μg 100 μg 200 μg	89%	Not relevant	12–15 minutes for doses from 50 μg to 200 μg	0.35–1.2 ng/mL for doses from 50 μg to 200 μg	N/A	Elimination t½ 3–4 hours
Fentanyl pectin nasal spray (Lazanda®)33	100 μg 400 μg (enabling dosing at 100 μg, 200 μg, 400 μg, and 800 μg)	N/A PI states that bioavailability is 20% higher than oral transmucosal fentanyl citrate	N/A	0.33–0.35 hours for doses from 100 μg to 800 μg	351.5–2844.0 pg/mL for doses from 100 μg to 800 μg	2460.5–17,272 ng-hour/mL for doses from 100 μg to 800 μg	15–24.9 hours for doses from 100 μg to 800 μg

Notes: ^aUnless otherwise stated; ^bparameters based on arterial sampling.

Abbreviations: AUC_{0_Inf}, area under the plasma concentration-time curve from time zero to infinity; C_max, maximum plasma drug concentration; N/A, not available; PI, prescribing information; t_½, half-life; T_max, time taken to reach C_max