The Fentanyl Story

Stanley, Theodore H.

doi:10.1016/j.jpain.2014.08.010

Cited by 259 publications

(251 citation statements)

References 36 publications

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“…The oral mucosa are easily accessible, more permeable than skin, and more richly supplied with blood, presenting an attractive route for drug delivery and allowing for lipophilic opioids to bypass first-pass metabolism. Fentanyl, a completely synthetic mu receptor-stimulating opioid, is one of the most lipophilic opioid analgesics, with a potency 100 times that of morphine 55 . Its lipophilicity enables rapid diffusion across the blood-brain barrier, and therefore diffusion into central nervous system structures.…”

Section: Contemporary Approaches To the Management Of Btcp With Rapidmentioning

confidence: 99%

“…Fentanyl also quickly crosses cellular barriers, providing broad tissue distribution and rapid onset of action. The potency, lipophilicity, and clinical efficacy of fentanyl have made it the object of intense interest for a variety of transmucosal applications 55 . Because both its onset of action and its peak plasma concentration depend on the dose and method of delivery, achievement of analgesia occurs within 1-2 minutes after intravenous administration, 10-15 minutes after buccal transmucosal delivery, and 14 hours after transdermal application.…”

Section: Contemporary Approaches To the Management Of Btcp With Rapidmentioning

confidence: 99%

“…Oral transmucosal fentanyl citrate was one of the first transmucosal drug formulations, developed as a fentanyl-impregnated lozenge on a stick 55 . One quarter of the fentanyl in this formulation is absorbed rapidly through the buccal mucosa, and another 25% of the total dose is absorbed through the gastrointestinal tract after it has been swallowed 57 .…”

Section: Contemporary Approaches To the Management Of Btcp With Rapidmentioning

confidence: 99%

“…Currently, two new transmucosal fentanyl products, administered sublingually (Abstral: Sentynl Therapeutics, Solana Beach, CA, U.S.A.) or buccally (Fentora: Cephalon, Malvern, PA, U.S.A.), are approved by Health Canada 55 . The dosing and titration process required with the new products often presents challenges for both the patient and the health care provider, because the initially chosen dose is often inadequate to control the pain and rescue medication has to be taken.…”

Section: Management Of Btcp: Canadian Perspectivementioning

confidence: 99%

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Canadian Recommendations for the Management of Breakthrough Cancer Pain

et al. 2016

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Breakthrough cancer pain (btcp) represents an important element in the spectrum of cancer pain management. Because most btcp episodes peak in intensity within a few minutes, speed of medication onset is crucial for proper control. In Canada, several current provincial guidelines for the management of cancer pain include a brief discussion about the treatment of btcp; however, there are no uniform national recommendations for the management of btcp. That lack, accompanied by unequal access to pain medication across the country, contributes to both regional and provincial variability in the management of btcp.Currently, immediate-release oral opioids are the treatment of choice for btcp. This approach might not always offer optimal speed for onset of action and duration to match the rapid nature of an episode of btcp. Novel transmucosal fentanyl formulations might be more appropriate for some types of btcp, but limited access to such drugs hinders their use. In addition, the recognition of btcp and its proper assessment, which are crucial steps toward appropriate treatment selection, remain challenging for many health care professionals.To facilitate appropriate management of btcp, a group of prominent Canadian specialists in palliative care, oncology, and anesthesiology convened to develop a set of recommendations and suggestions to assist Canadian health care providers in the treatment of btcp and the alleviation of the suffering and discomfort experienced by adult cancer patients.

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Section: Contemporary Approaches To the Management Of Btcp With Rapidmentioning

confidence: 99%

Section: Contemporary Approaches To the Management Of Btcp With Rapidmentioning

confidence: 99%

Section: Contemporary Approaches To the Management Of Btcp With Rapidmentioning

confidence: 99%

Section: Management Of Btcp: Canadian Perspectivementioning

confidence: 99%

See 2 more Smart Citations

Canadian Recommendations for the Management of Breakthrough Cancer Pain

et al. 2016

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“…Fentanyl, which is the most frequently used analgesic, exhibits minimal cardiovascular effects and does not increase plasma histamine levels (3). Due to its relatively short onset of action and duration of effect, fentanyl is a convenient and widely available drug used in clinical practice (4).…”

Section: Introductionmentioning

confidence: 99%

Fentanyl inhibits the progression of human gastric carcinoma MGC-803 cells by modulating NF-κB-dependent gene expression in vivo

Guan

et al. 2016

Oncology Letters

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Abstract.Fentanyl is widely used to treat acute and chronic pain. Previous in vitro studies by the present authors demonstrated that fentanyl inhibits the progression of the MGC-803 human gastric carcinoma cell line by affecting apoptosis-related genes, including nuclear factor-kappa B (NF-κB) and phosphatase and tensin homolog. In the present study, the effects of fentanyl on NF-κB-dependent gene expression were investigated in vivo. Nude mice were inoculated with an MGC-803 cell suspension, and mice that developed subcutaneous tumors measuring >1.0x1.0 cm were selected for study. Mice were administered intraperitoneal injections of fentanyl (0.05 mg/kg, group F1; 0.1 mg/kg, group F2; 0.2 mg/kg, group F3; and 0.4 mg/kg, group F4) for 14 consecutive days. Non-fentanyl-treated mice (group C) and normal saline-treated mice (group N) served as the control groups. Tumor growth was monitored by calculating the time-shift of the growth curve. Morphological changes were also observed using microscopy. The expression of NF-κB, B-cell lymphoma-2 (Bcl-2), B-cell associated X protein (Bax), vascular endothelial growth factor-A (VEGF-A) and matrix metalloproteinase-9 (MMP-9) in the subcutaneous tumor tissue was also analyzed by reverse transcription-polymerase chain reaction and western blot analysis, and confirmed using immunohistochemistry. The relative tumor volumes of groups F1, F2, F3 and F4 were significantly reduced compared with groups C and N. Furthermore, subcutaneous tumor cells exhibited nuclear swelling, chromatin condensation, reduced chromatin and nuclear fragmentation in the F1, F2, F3 and F4 groups. The number of NF-κB + , Bcl-2 + , VEGF-A + and MMP-9 + subcutaneous tumor cells was reduced, whereas the number of Bax + cells was increased in the F1, F2, F3 and F4 groups. Additionally, in these groups, tumor expression of NF-κB, Bcl-2, VEGF-A and MMP-9 transcripts and proteins was downregulated, while Bax messenger RNA and protein expression levels were upregulated. The results revealed that fentanyl inhibits the growth of subcutaneous human gastric carcinoma tumors in mice. Therefore, it could be hypothesized that this antineoplastic activity may result from the inhibition of NF-κB activation, suppression of downstream VEGF-A and MMP-9 expression, and normalization of the pro-apoptotic Bax/Bcl-2 ratio. IntroductionAt present, gastric carcinoma is the fourth most common human neoplasm and the second most common cause of carcinoma-associated mortality worldwide, accounting for 986,600 novel cases and 738,000 mortalities annually (1). The incidence and mortality rates of this disease are higher in China than in other Asian countries (1). The molecular pathogenesis of gastric carcinoma has been investigated extensively with the aim of developing more effective therapeutic strategies for this type of tumor (2). Thus, there is an urgent requirement for the development of strategies to prevent and treat this disease.Fentanyl, which is the most frequently used analgesic, exhibits minimal cardiovascular effects and d...

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Forensic Applications of Gas Chromatography – Vacuum Ultraviolet Spectroscopy Paired with Mass Spectrometry

Schonert¹

2022

Leading Edge Techniques in Forensic Trace Evidence Analysis

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The Fentanyl Story

Cited by 259 publications

References 36 publications

Canadian Recommendations for the Management of Breakthrough Cancer Pain

Canadian Recommendations for the Management of Breakthrough Cancer Pain

Fentanyl inhibits the progression of human gastric carcinoma MGC-803 cells by modulating NF-κB-dependent gene expression in vivo

Forensic Applications of Gas Chromatography – Vacuum Ultraviolet Spectroscopy Paired with Mass Spectrometry

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