OBJECTIVE: To compare changes in oesophageal (T-Oeso) and rectal (T-Rec) temperature in dogs during general anaesthesia and premedicated with fentanyl, medetomidine-fentanyl or acepromazine-fentanyl. STUDY DESIGN: Prospective, randomized, blind clinical study. ANIMALS: A total of 120 healthy dogs, aged 2-10 years and weighing 5-20 kg. METHODS: Dogs were randomly allocated to one of three groups. Animals of F group were premedicated with fentanyl (0.01 mg kg-1), MF group with medetomidine (0.005 mg kg-1) and fentanyl (0.01 mg kg-1) and AF group with acepromazine (0.01 mg kg-1) and fentanyl (0.01 mg kg-1). Anaesthesia was induced with propofol and maintained with isoflurane in oxygen-air mixture. Fentanyl was administered continuously (0.01 mg kg-1 hour-1). The T-Oeso, T-Rec and ambient temperatures were recorded after induction (T0) and subsequently at 10 minute intervals for 60 minutes (T10-T60). Data were analysed using anova or their non-parametric equivalents (p < 0.05). RESULTS: Median T-Oeso was significantly higher in MF group between T0-T20 compared with other groups. Median T-Oeso significantly decreased in F group from 38.0 °C (T0) to 37.4 °C (T30), 37.1 °C (T40), 36.9 °C (T50) and 36.6 °C (T60), in MF group from 38.3 °C (T0) to 37.7 °C (T30), 37.5 °C (T40), 37.2 °C (T50) and 37.1 °C (T60) and in AF group from 37.7 °C (T0) to 37.3 °C (T40), 37.2 °C (T50) and 37.1 °C (T60). The T-Rec significantly decreased in F group from 38.0 °C (T0) to 37.4 °C (T40), 37.2 °C (T50) and 36.9 °C (T60), in MF group from 38.3 °C (T0) to 37.5 °C (T50) and 37.4 °C (T60) and in AF group from 38.2 °C (T0) to 37.6 °C (T40), 37.5 °C (T50) and 37.4 °C (T60). CONCLUSIONS AND CLINICAL RELEVANCE: Premedication with fentanyl, medetomidine-fentanyl or acepromazine-fentanyl in the doses used decreased the T-Oeso and T-Rec. The T-Oeso at the beginning of anaesthesia was higher after premedication with medetomidine-fentanyl. However, this difference was not clinically significant.

• Klíčová slova
• heat loss, hypothermia, neuroleptic, opioid, temperature, α(2)-adrenoceptor agonist,
• MeSH
• acepromazin * farmakologie   aplikace a dávkování   MeSH
• anestetika intravenózní farmakologie   aplikace a dávkování   MeSH
• celková anestezie veterinární   MeSH
• ezofágus účinky léků   MeSH
• fentanyl * farmakologie   aplikace a dávkování   MeSH
• kombinace anestetik aplikace a dávkování   farmakologie   MeSH
• medetomidin * farmakologie   aplikace a dávkování   MeSH
• premedikace anestezie veterinární   MeSH
• prospektivní studie MeSH
• psi MeSH
• rektum MeSH
• tělesná teplota * účinky léků   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• psi MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• randomizované kontrolované studie veterinární MeSH
• Názvy látek
• acepromazin * MeSH
• anestetika intravenózní MeSH
• fentanyl * MeSH
• kombinace anestetik MeSH
• medetomidin * MeSH

The extended occurrence of fentanils abuse associated with the dramatic increase in opioid fatal overdoses and dependence strongly emphasizes insufficiencies in opioid addiction treatment. Recently, the growth hormone secretagogue receptor (GHS-R1A) antagonism was proposed as a promising mechanism for drug addiction therapy. However, the role of GHS-R1A and its endogenous ligand ghrelin in opioid abuse is still unclear. Therefore, the aim of our study was to clarify whether the GHS-R1A antagonist JMV2959 could reduce the fentanyl-induced conditioned place preference (CPP), the fentanyl intravenous self-administration (IVSA), and the tendency to relapse, but also whether JMV2959 could significantly influence the fentanyl-induced dopamine efflux in the nucleus accumbens (NAC) in rats, that importantly participates in opioids' reinforcing effects. Following an ongoing fentanyl self-administration, JMV2959 3 mg/kg was administered intraperitoneally 20 minutes before three consequent daily 360-minute IVSA sessions under a fixed ratio FR1, which significantly reduced the number of active lever-pressing, the number of infusions, and the fentanyl intake. Pretreatment with JMV2959 also reduced the fentanyl-seeking/relapse-like behaviour tested in rats on the 12th day of the forced abstinence period. Pretreatment with JMV2959 significantly and dose-dependently reduced the manifestation of fentanyl-CPP. The fentanyl-CPP development was reduced after the simultaneous administration of JMV2959 with fentanyl during conditioning. The JMV2959 significantly reduced the accumbens dopamine release induced by subcutaneous and intravenous fentanyl. Simultaneously, it affected the concentration of byproducts associated with dopamine metabolism in the NAC. Our findings suggest that GHS-R1A importantly participates in the rewarding/reinforcing effects of fentanyl.

• Klíčová slova
• IVSA, addiction, CPP, dopamine, fentanyl, ghrelin antagonism,
• MeSH
• autoaplikace MeSH
• dopamin metabolismus   MeSH
• fentanyl aplikace a dávkování   škodlivé účinky   MeSH
• ghrelin metabolismus   MeSH
• glycin analogy a deriváty   farmakologie   MeSH
• intravenózní podání MeSH
• krysa rodu Rattus MeSH
• narkotika aplikace a dávkování   škodlivé účinky   MeSH
• nucleus accumbens účinky léků   MeSH
• operantní podmiňování účinky léků   MeSH
• potkani Wistar MeSH
• receptory ghrelinu antagonisté a inhibitory   MeSH
• triazoly farmakologie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• dopamin MeSH
• fentanyl MeSH
• ghrelin MeSH
• glycin MeSH
• N-(1-(4-(4-methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)-2-(1H-indol-3-yl)ethyl)-2-aminoacetamide MeSH Prohlížeč
• narkotika MeSH
• receptory ghrelinu MeSH
• triazoly 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

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

OBJECTIVE: To develop a safe and effective immobilization protocol in rhesus monkeys, which is not based on dissociative anaesthetic agent. STUDY DESIGN: Prospective, randomised, experimental trial. ANIMALS: Twenty rhesus monkeys, weighing 2.6-8.0 kg, 1-3 years of age, of both sexes. METHODS: The monkeys received 50 μg kg(-1) medetomidine, 0.25 mg kg(-1) midazolam and 5 μg kg(-1) fentanyl with 150 IU hyaluronidase intramuscularly (IM). The animals were closely observed for behavioural changes and reaction to sound stimulus. Pulse rate and oxygen saturation of haemoglobin (SpO(2) ) were monitored every 5 minutes, for 20 minutes. After this period, 250 μg kg(-1) atipamezole or a placebo was administered IM and behavioural changes were closely observed. RESULTS: Full immobilization was observed after mean 269 ± SD 116 seconds. Ten minutes after injection mean arterial oxygen saturation of haemoglobin was 94 ± 4%, but did not fall significantly further. The median pulse rate was 116 beats minute(-1) 5 minutes after the administration of the drug. This level further decreased to a median level of 108 beats minute(-1) 20 minutes after the drug's administration. The median time to recover from immobilization was significantly shorter after atipamezole administration when compared to placebo (2.7 versus 55 minutes). All animals awoke smoothly and no side effects such as vomiting or agitation were observed. CONCLUSIONS: Short term and reversible pharmacological immobilization was achieved using combination of midazolam, medetomidine, and fentanyl. CLINICAL RELEVANCE: The present study demonstrates that 20-minute pharmacological immobilization with a combination of midazolam, medetomidine, and fentanyl is feasible in rhesus monkeys with minimal effect on heart rate.

• MeSH
• analýza krevních plynů veterinární   MeSH
• časové faktory MeSH
• fentanyl * aplikace a dávkování   farmakologie   MeSH
• hypnotika a sedativa * aplikace a dávkování   farmakologie   MeSH
• imobilizace metody   veterinární   MeSH
• injekce intramuskulární veterinární   MeSH
• kombinovaná farmakoterapie veterinární   MeSH
• Macaca mulatta * MeSH
• medetomidin * aplikace a dávkování   farmakologie   MeSH
• midazolam * aplikace a dávkování   farmakologie   MeSH
• srdeční frekvence účinky léků   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• fentanyl * MeSH
• hypnotika a sedativa * MeSH
• medetomidin * MeSH
• midazolam * MeSH

THE AIM OF THE STUDY: Recently, alpha2 sympathoadrenergic drugs are used in premedication to improve the perioperative course. The aim of our study was to compare a premedication with a new alpha2 sympathoadrenergic drug and standard premedication. METHODS: After ethic committee approval and written patient consent, in a randomised, double-blinded study, combination of dexmedetomidine 1.0 microg x kg(-1) + ketamine 0.5 mg x kg(-1) + fentanyl 1.0 microg x kg(-1) + atropine 0.5 mg (group FNT), dexmedetomidine 1.0 microg x kg(-1) + ketamine 0.5 mg x kg(-1) + alfentanil 5.0 microg x kg(-1) + atropine 0.5 mg (group ALFNT), or pethidine 1.0 mg x kg(-1) + atropine 0.5 mg (group Dolsin) was administered to a deltoid muscle 15 min. before anaesthesia (GA) in patients elicited for laparoscopic cholecystectomy (LCHE). GA was performed in a standard way, ECG, NIBP, respiration rate, SpO2, onset of effect, Observers Assessment of Alertness Sedation Score (OAASS) before GA, circulatory reaction to intubation and capnoperitoneum, fentanyl consumption during GA, time to the first request for post-operative analgesia and postoperative nausea and vomiting were measured. The data were processed by Kruskal-Wallis and Fisher tests. P-value < 0.05 was considered significant. RESULTS: There were 16 patients in FNT and Dolsin and 15 patients in ALFNT with no differences in demography except for younger age in ALFNT. The main differences were in hypertension during capnoperitoneum: 0/16 FNT and 1/15 ALFNT vs. 11/16 Dolsin, both p < 0.001, per-operative fentanyl consumption: FNT 31.5 microg vs. Dolsin 165.0 microg, p < 0.001 and ALFNT 50.0 microg, p < 0.05 (ALFNT vs. Dolsin, p < 0.01) and request to the first analgesic post surgery: FNT 1.3 h. vs. Dolsin 0.45 h., p < 0.05 vs. ALFNT 0.8 h., p < 0.01. There were no differences in side effects except for bradycardia in ALFNT (p < 0.05). CONCLUSIONS: Dexmedetomidine-ketamine-fentanyl-atropine combination is superior to pethidine-atropine combination in suppressing of adverse hemodynamic effects of capnoperitoneum, decreased need for analgesia during GA and prolonged postoperative analgesia.

• MeSH
• anestetika disociativní aplikace a dávkování   MeSH
• atropin aplikace a dávkování   MeSH
• cholecystektomie laparoskopická * MeSH
• dexmedetomidin aplikace a dávkování   MeSH
• dvojitá slepá metoda MeSH
• fentanyl aplikace a dávkování   MeSH
• hemodynamika účinky léků   MeSH
• hypnotika a sedativa aplikace a dávkování   MeSH
• ketamin aplikace a dávkování   MeSH
• kombinace anestetik aplikace a dávkování   MeSH
• lidé středního věku MeSH
• lidé MeSH
• meperidin aplikace a dávkování   MeSH
• neopioidní analgetika MeSH
• opioidní analgetika aplikace a dávkování   MeSH
• pooperační bolest prevence a kontrola   MeSH
• probouzení z anestezie MeSH
• Check Tag
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• randomizované kontrolované studie MeSH
• Názvy látek
• anestetika disociativní MeSH
• atropin MeSH
• dexmedetomidin MeSH
• fentanyl MeSH
• hypnotika a sedativa MeSH
• ketamin MeSH
• kombinace anestetik MeSH
• meperidin MeSH
• neopioidní analgetika MeSH
• opioidní analgetika 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 authors describe their own experience with anaesthesia using large doses of fentanyl in patients operated on account of ischaemic heart disease and acquired valvular defects. Considerable stability of the circulation and careful monitoring of cardiorespiratory parameters along with aimed influencing of serious deviations is the basis of success of this procedure, which makes it possible to perform cardiosurgery in high risk patients. The authors try to improve the described method further by using some modern procedures.

• MeSH
• anestezie metody   MeSH
• fentanyl aplikace a dávkování   MeSH
• kardiochirurgické výkony * MeSH
• lidé MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• fentanyl MeSH