Table 1.

Overview of pharmacological properties of fentanyl and its derivatives [3, 4, 14, 15, 52, 112, 173–180].

	Fentanyl	Sufentanil	Alfentanil	Remifentanil
Potency compared to morphine	100–300	800–1000	40–50	100–200
IV induction dose (μg/kg)	2–6	0.25–2.0	25–100	1–2
IV maintenance dose (μg/kg)	0.5–2	2.5–10	5–10	0.1–1.0
IV infusion rate (μg/kg/h)	0.5–5	0.5–1.5	30–120	0.1–1.0
Other routes of administration than IV	transdermal, transmucosal (buccal, nasal, sublingual), epidural	epidural, sublingual
Time to onset (min)	1.5	1	0.75	< 1
Time to peak effect (min)	4.5–8	2.5–5	1.5	1.5
Duration of peak effect (min)	20–30	30	15
Duration of analgesic effect (min)	60–120	100–150	30–60	5–10
Analgesic plasma concentration (ng/mL)	0.6–3.0	0.5–2.5	50–300	0.3–3
Plasma concentration associated with loss of consciousness (ng/mL)	> 20.0	> 2.5	> 400	> 4
t1/2α(min)	1.7 ± 0.1	1.4 ± 0.3	1.31 ± 0.48	1
t1/2β(min)	13.4 ± 1.6	17.7 ± 2.6	9.4 ± 2.7	6
t1/2γ(min)	219 ± 10 (120–240)	164 ± 22 (120–180)	93.7 ± 8.3 (60–120)	10–20 (6–14)
Vdc(L/kg)	0.36 ± 0.07	0.16 ± 0.02	0.12 ± 0.04	0.1
Vdss(L/kg)	4.0 ± 0.4 (3–5)	1.7 ± 0.2 (2.5–3.0)	1.0 ± 0.3 (0.4–1.0)	0.35 (0.2–0.4)
CL (mL/min/kg)	13 ± 2 (10–20)	12.7 ± 0.8 (10–15)	7.6 ± 2.4 (3–9)	40 (30–60)
Protein binding (%)	80–84	91–92.5	88.7–92.1	70
pKa	8.4	8.0	6.5	7.1
Non-ionized fraction @ pH 7.40 (%)	8.5	20	89	67
Metabolism	CYP3A	CYP3A	CYP3A	Plasma and tissue esterases
Lipid solubility (octanol/water distribution coefficient)	813–816	1727–1778	128	18
References	[14, 52, 112, 173–179]	[3, 14, 112, 173–175, 177–179]	[4, 14, 112, 173–175, 177–180]	[14, 15, 112, 173–175, 177–179]

Abbreviations: t_1/2α distribution half-life, t_1/2β redistribution half-life, t_1/2γ terminal elimination half-life, Vd_C volume of distribution of the central compartment, Vd_ss volume of distribution at steady state, CL clearance.

Italic numbers indicate information from the Summary of Product Characteristics (SPC).