fentanyl analogs Dotaz Zobrazit nápovědu
The review describes fentanyl and its analogs as new synthetic opioids and the possibilities of their identification and determination using electrochemical methods (e.g., voltammetry, potentiometry, electrochemiluminescence) and electrochemical methods combined with various separation methods. The review also covers the analysis of new synthetic opioids, their parent compounds, and corresponding metabolites in body fluids, such as urine, blood, serum, and plasma, necessary for a fast and accurate diagnosis of intoxication. Identifying and quantifying these addictive and illicit substances and their metabolites is necessary for clinical, toxicological, and forensic purposes. As a reaction to the growing number of new synthetic opioid intoxications and increasing fatalities observed over the past ten years, we provide thorough background for developing new biosensors, screen-printed electrodes, or other point-of-care devices.
- Klíčová slova
- amperometry, fentanyl, fentanyl analogs, metabolite, oxidation, screen-printed electrode, voltammetry,
- MeSH
- fentanyl * MeSH
- opioidní analgetika * MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- fentanyl * MeSH
- opioidní analgetika * MeSH
BACKGROUND: Oromucosal fentanyl is currently used for the treatment of breakthrough pain (BTP) in opioid-treated cancer patients. Ethypharm developed a sublingual formulation of fentanyl suprabioavailable to oral transmucosal fentanyl citrate with a higher early systemic exposure and a shorter Tmax. OBJECTIVES: This study evaluated the efficacy and safety profile of fentanyl Ethypharm (FE) in relieving BTP in opioid-treated cancer patients. METHODS: Opioid-treated adult cancer patients, experiencing 1 to 4 episodes of BTP per day, were included in the study. After an open-label titration period to identify an optimal dose that would provide adequate pain relief for 2 consecutive episodes of BTP with an acceptable level of adverse events, patients were randomly assigned to a double-blind, placebo-controlled, crossover period with 1 of 13 prespecified sequences of 9 tablets (6 tablets of FE of the dose identified during the open-label titration and 3 placebo). Pain intensity and pain relief were recorded at 3, 6, 10, 15, 30, and 60 minutes after study drug administration. Adverse events were recorded. The primary end point was the sum of pain intensity differences (SPID) at 30 minutes. RESULTS: The distribution of optimal dosages of FE was as follows: 133 µg, 35.9%; 267 µg, 30.8%; 400 µg, 14.1%; 533 µg, 12.8%; and 800 μg, 6.4%. In the modified intention-to-treat population (n = 73), FE significantly improved mean (SE) SPID compared with placebo at 30 minutes (75.0 [49.8] vs 52.5 [52.8]; P < 0.0001). FE significantly improved SPID, pain intensity difference, and pain relief compared with placebo from 6 to 60 minutes' postadministration. Patients with BTP who received placebo required the use of rescue medication more often than those treated with FE (38.4% vs 17.5%; P < 0.0001). A significant improvement in pain scores (>33% and >50% reductions) was also reported for BTP treated with FE. Pain scores for patients with BTP with a neuropathic component (13 patients) were lower with FE than for those receiving placebo, but the difference was not significant. AEs were of mild or moderate severity and typical of opioid drugs. CONCLUSIONS: This newly developed galenic formulation with a higher early systemic exposure and a shorter Tmax compared with oral transmucosal fentanyl citrate makes FE a particularly suitable formulation for the management of BTP in opioid-treated cancer patients due to the very rapid onset of action. FE provided significant improvement in pain intensity of BTP compared with placebo as early as 6 minutes' postadministration with a sustained effect over 60 minutes. FE was well tolerated by patients. ClinicalTrials.gov identifier: NCT 01842893.
- Klíčová slova
- breakthrough pain, cancer pain, fentanyl citrate, sublingual tablet,
- MeSH
- aplikace sublinguální MeSH
- dospělí MeSH
- dvojitá slepá metoda MeSH
- fentanyl aplikace a dávkování škodlivé účinky terapeutické užití MeSH
- klinické křížové studie MeSH
- lidé středního věku MeSH
- lidé MeSH
- management bolesti MeSH
- management nemoci MeSH
- měření bolesti MeSH
- nádory farmakoterapie MeSH
- opioidní analgetika aplikace a dávkování škodlivé účinky terapeutické užití MeSH
- průlomová bolest farmakoterapie MeSH
- senioři MeSH
- tablety MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- klinické zkoušky MeSH
- práce podpořená grantem MeSH
- randomizované kontrolované studie MeSH
- Názvy látek
- fentanyl MeSH
- opioidní analgetika MeSH
- tablety MeSH
OBJECTIVES: To compare the analgesic potency and side effects of epidural combination trimecaine with morphine and bupivacaine with fentanyl in postoperative analgesia after a major urological surgery. METHODS: We randomised 150 consecutive patients. In the trimecain/morphine group (n = 75) trimecaine 50 mg with 4 mg morphine was given epidurally in 8 hour intervals. In the bupivacain/fentanyl group (n = 75) the infusion of 0.25 % bupivacaine and fentanyl 2 microg/ml was administered at an infusion rate of 8 ml/h. RESULTS: The postoperative pain scores were lower in the trimecain/morphine group, the difference was significant during the first 6 hours after surgery, there was also a trend toward higher postoperative SpO2 values in this group, the difference was significant 36 hours after surgery. The total sum of postoperative complications and side effects was significantly higher in the bupivacian/fentanyl group (p = 0.002). CONCLUSION: The combination of epidural trimecaine with morphine after a major urological surgery provides a superior analgesia with fewer side effects when compared to epidurally delivered bupivacaine with fentanyl (Tab. 2, Fig. 5, Ref. 17). Full Text (Free, PDF) www.bmj.sk.
- MeSH
- anestetika lokální * aplikace a dávkování MeSH
- bupivakain aplikace a dávkování MeSH
- epidurální analgezie * MeSH
- fentanyl aplikace a dávkování MeSH
- fixní kombinace léků MeSH
- lidé středního věku MeSH
- lidé MeSH
- měření bolesti MeSH
- morfin aplikace a dávkování MeSH
- opioidní analgetika * aplikace a dávkování MeSH
- pooperační bolest prevence a kontrola MeSH
- trimekain aplikace a dávkování MeSH
- urologické chirurgické výkony * MeSH
- Check Tag
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- randomizované kontrolované studie MeSH
- srovnávací studie MeSH
- Názvy látek
- anestetika lokální * MeSH
- bupivakain MeSH
- fentanyl MeSH
- fixní kombinace léků MeSH
- morfin MeSH
- opioidní analgetika * MeSH
- trimekain MeSH
The article presents the first Polish case of fatal single-substance poisoning with cyclopropylfentanyl, a representative of fentanyl derivatives, whose victim was a 37-year-old man. This opioid was detected in biological material collected during medicolegal autopsy and in the syringe found near the deceased. Blood and urine samples were analyzed using liquid chromatography with mass spectrometry. The concentration of cyclopropylfentanyl was 24 ng/mL in blood and 73 ng/mL in urine.
- Klíčová slova
- cyclopropylfentanyl, fentanyl analogs, new psychoactive substances (NPS), opioids,
- MeSH
- dospělí MeSH
- fentanyl analogy a deriváty MeSH
- lidé MeSH
- opioidní analgetika * MeSH
- tandemová hmotnostní spektrometrie * MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- mužské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- kazuistiky MeSH
- Geografické názvy
- Polsko MeSH
- Názvy látek
- cyclopropylfentanyl MeSH Prohlížeč
- fentanyl MeSH
- opioidní analgetika * MeSH
Breakthrough cancer pain has been defined as a transitory increase in pain intensity that occurs despite relatively stable and adequately controlled background pain. More than half of cancer patients with chronic pain suffer by some form of breakthrough cancer pain. The management of breakthrough cancer pain is comprehensive and includes pharmacological and nonpharmacological approaches. The principal treatment strategies are optimization of regular analgesic medication combined with effective rescues medication. The new transmucosal forms of fentanyl represent an important improvement in our treatment options.
- MeSH
- aplikace bukální MeSH
- fentanyl aplikace a dávkování terapeutické užití MeSH
- lidé MeSH
- management bolesti MeSH
- měření bolesti MeSH
- nádory komplikace farmakoterapie MeSH
- opioidní analgetika terapeutické užití MeSH
- průlomová bolest farmakoterapie etiologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- fentanyl MeSH
- opioidní analgetika MeSH
BACKGROUND: Intravenous patient-controlled analgesia (IV PCA) using opiods is an accepted method for delivering postoperative analgesia. The aim of this study was to compare fentanyl and tramadol with IV PCA after spinal anesthesia (SA) and general anesthesia (GA) following cesarean section (C/S). METHODS: Ninety women were randomly assigned to three groups (n=30). Group 1 was treated with IV fentanyl PCA after SA. Groups 2 and 3 were treated with IV fentanyl PCA and IV tramadol PCA after GA. Outcome measures were recorded for the first 24 h post-anesthesia. RESULTS: PCA use was significantly lower after SA (P<0.05). Eighteen patients in the SA Group and 27 patients and 24 patients from the GA groups required additional opioid. Opioid consumption and patient satisfaction were similar for groups after GA (P>0.05). 638.4 ± 179.1 μg fentanyl was consumed by patients of Group 2, 356.3 ± 87.0 μg fentanyl and 559.5 ± 207.0 mg tramadol was consumed by Group 1 and Group 3 respectively. There was no significant difference in the overall severity and incidence of nausea, drowsiness or pruritus. CONCLUSION: Our study shows that analgesic consumption and post-operative pain scores after SA in C/S decreased, without increase in adverse reactions.
- MeSH
- celková anestezie MeSH
- císařský řez * MeSH
- dospělí MeSH
- fentanyl aplikace a dávkování MeSH
- lidé MeSH
- měření bolesti MeSH
- opioidní analgetika aplikace a dávkování MeSH
- pacientem kontrolovaná analgezie * MeSH
- pooperační bolest farmakoterapie MeSH
- porodnická anestezie * MeSH
- spinální anestezie MeSH
- těhotenství MeSH
- tramadol aplikace a dávkování MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- randomizované kontrolované studie MeSH
- srovnávací studie MeSH
- Názvy látek
- fentanyl MeSH
- opioidní analgetika MeSH
- tramadol MeSH