Abstract | BACKGROUND AND OBJECTIVES: METHODS: The pharmacokinetics of sublingual sufentanil 10 and 80 µg were compared with IV sufentanil in 12 subjects in a phase 1 study. The safety and efficacy of sublingual sufentanil (5-15 µg) were evaluated in double-blind, randomized, placebo-controlled phase 2 studies in patients undergoing knee replacement surgery (n = 101) or open abdominal (ABD) surgery (n = 94). The primary efficacy measurement was the summed pain intensity difference compared with baseline over 12 hours (SPID-12). RESULTS: Sublingual sufentanil pharmacokinetics were dose proportional following single doses of 10 and 80 µg. Plasma half-time (time from peak plasma concentration to 50% of peak concentration) was 80 to 90 minutes for sublingual sufentanil compared with 15 minutes or less for IV sufentanil. In the phase 2 studies, greater SPID-12 scores (ie, lower pain intensity) compared with placebo were observed for sublingual sufentanil 15 µg in the knee replacement study (P < 0.05) and for 10 and 15 µg in the ABD study (P < 0.01). All doses of sublingual sufentanil were well tolerated, and the incidence of adverse events was similar between the sublingual sufentanil and placebo groups. CONCLUSIONS:
Sufentanil formulated as a sublingual solid dosage form provides a duration of action that allows effective analgesia for postoperative patients in a medically supervised setting.
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Authors | Harold S Minkowitz, Neil K Singla, Mark A Evashenk, Stephen S Hwang, Yu-Kun Chiang, Lawrence G Hamel, Pamela P Palmer |
Journal | Regional anesthesia and pain medicine
(Reg Anesth Pain Med)
2013 Mar-Apr
Vol. 38
Issue 2
Pg. 131-9
ISSN: 1532-8651 [Electronic] England |
PMID | 23271030
(Publication Type: Clinical Trial, Phase I, Clinical Trial, Phase II, Comparative Study, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
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Chemical References |
- Analgesics, Opioid
- Tablets
- Sufentanil
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Topics |
- Abdomen
(surgery)
- Administration, Sublingual
- Adult
- Aged
- Analgesics, Opioid
(administration & dosage, adverse effects, pharmacokinetics)
- Analysis of Variance
- Area Under Curve
- Arthroplasty, Replacement, Knee
(adverse effects)
- Biological Availability
- Female
- Half-Life
- Humans
- Infusions, Intravenous
- Least-Squares Analysis
- Male
- Metabolic Clearance Rate
- Middle Aged
- Pain Measurement
- Pain, Postoperative
(diagnosis, prevention & control)
- Sufentanil
(administration & dosage, adverse effects, pharmacokinetics)
- Tablets
- Treatment Outcome
- Young Adult
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