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https://www.readbyqxmd.com/read/28430384/pharmacokinetics-of-concentrated-naloxone-nasal-spray-over-first-30%C3%A2-minutes-post-dosing-analysis-of-suitability-for-opioid-overdose-reversal
#1
Gill Mundin, Rebecca McDonald, Kevin Smith, Stephen Harris, John Strang
BACKGROUND AND AIMS: Lack of non-injectable naloxone formulations has impeded widespread take-home provision for the prevention of heroin/opioid overdose deaths. For non-injectable formulations that are finally being investigated, rapid onset of action and sufficient bioavailability will be vital. We present analysis of data from a study of concentrated naloxone nasal spray formulations. Our aims are: to assess 1) pharmacokinetic properties and 2) suitability for overdose reversal in terms of naloxone absorption within 30 minutes post-dosing...
April 21, 2017: Addiction
https://www.readbyqxmd.com/read/28416993/antinociceptive-effect-of-intrathecal-sec-o-glucosylhamaudol-on-the-formalin-induced-pain-in-rats
#2
Sang Hun Kim, Hwa Song Jong, Myung Ha Yoon, Seon Hee Oh, Ki Tae Jung
BACKGROUND: The root of Peucedanum japonicum Thunb., a perennial herb found in Japan, the Philippines, China, and Korea, is used as an analgesic. In a previous study, sec-O-glucosylhamaudol (SOG) showed an analgesic effect. This study was performed to examine the antinociceptive effect of intrathecal SOG in the formalin test. METHODS: Male Sprague-Dawley rats were implanted with an intrathecal catheter. Rats were randomly treated with a vehicle and SOG (10 µg, 30 µg, 60 µg, and 100 µg) before formalin injection...
April 2017: Korean Journal of Pain
https://www.readbyqxmd.com/read/28412373/mechanistic-evaluation-of-tapentadol-in-reducing-the-pain-perception-using-in-vivo-brain-and-spinal-cord-microdialysis-in-rats
#3
Vijay Benade, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Saivishal Daripelli, Ganesh Ayyanki, Shantaveer Irappanavar, Ranjithkumar Ponnamaneni, Arunkumar Manoharan
Role of monoamine neurotransmitters in the modulation of emotional and pain processing in spinal cord and brain regions is not well known. Tapentadol, a norepinephrine reuptake inhibitor with µ-opioid receptor agonistic activity has recently been introduced for the treatment of moderate to severe pain. The objective of the present study was to examine the effects of tapentadol on modulation of monoamines in the prefrontal cortex and dorsal horn using brain microdialysis. Tapentadol was administered intraperitoneally at 4...
April 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28361412/study-of-%C3%AE-and-%C3%AE-opioid-activities-in-agents-with-various-%C3%AE%C2%BA-receptor-selectivity
#4
O Yu Grechko, R A Litvinov, A A Spasov, A I Rashchenko, D M Shtareva, V A Anisimova, V I Minkin
A putative opioid agonist RU-1205 was ineffective within in vitro model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC50=2.6×10(-7) M. In vivo experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77...
March 30, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28298770/intraperitoneal-levobupivacaine-with-or-without-clonidine-for-pain-relief-after-laparoscopic-cholecystectomy-a-randomized-double-blind-placebo-controlled-trial
#5
Nishith Govil, Parag Kumar
BACKGROUND: Irrigation of local anesthetic intraperitoneally in combination with opioids and non-opioids agents has been used to provide pain relief with varying success in laparoscopic surgeries. This randomized double blind placebo controlled study is designed to study the effect of intraperitoneal instillation of levo-bupivacaine along with clonidine for pain relief after laparascopic cholecystectomy. METHODS: 75 patients were randomized to receive 20 ml of 0...
January 2017: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/28280516/evaluation-of-analgesic-activity-of-papaver-libanoticum-extract-in-mice-involvement-of-opioids-receptors
#6
Mohamad Ali Hijazi, Ahmed El-Mallah, Maha Aboul-Ela, Abdalla Ellakany
Papaver libanoticum is an endemic plant to Lebanese region (family Papaveraceae) that has not been investigated before. The present study aimed to explore the analgesic activity of dried ethanolic extract of Papaver libanoticum (PLE) using tail flick, hot plate, and acetic acid induced writhing models in mice. The involvement of opioid receptors in the analgesic mechanism was investigated using naloxone antagonism. Results demonstrated that PLE exhibited a potent dose dependent analgesic activity in all tested models for analgesia...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28246760/-side-effects-of-pain-therapy-sufficient-analgesia-without-unnecessary-complications
#7
F Greul, A Zimmer, W Meißner
Interventions of acute and chronic pain treatment are associated with risks. Therefore, it is important to know about treatment side effects in order to avoid unnecessary complications and therapy interruption. This knowledge, however, is not to prevent/abandon this treatment altogether. Rather, it is intended to use pain treatment interventions rationally. The following article is to deepen the knowledge of unintended effects of analgetic treatments. Moreover, it will help find an optimal pain therapy in terms of efficacy and tolerable risks as well as limitations...
February 28, 2017: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/28242230/thermal-antinociception-following-oral-administration-of-tapentadol-in-conscious-cats
#8
Graeme M Doodnaught, Marina C Evangelista, Paulo V M Steagall
OBJECTIVE: To evaluate the onset, magnitude and duration of thermal antinociception after oral administration of two doses of tapentadol in cats. STUDY DESIGN: Prospective, randomized, blinded, experimental study. ANIMALS: Six healthy adult cats weighing 4.4 ± 0.4 kg. METHODS: Skin temperature (ST) and thermal threshold (TT) were evaluated using a wireless TT device up to 12 hours after treatment. Treatments included placebo (PBO, 50 mg dextrose anhydrase orally), buprenorphine (BUP, 0...
January 7, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28223843/the-use-of-rotation-to-fentanyl-in-cancer-related-pain
#9
Delia Dima, Ciprian Tomuleasa, Ioana Frinc, Sergiu Pasca, Lorand Magdo, Ioana Berindan-Neagoe, Mihai Muresan, Cosmin Lisencu, Alexandru Irimie, Mihnea Zdrenghea
Pain is commonly diagnosed with respect to cancer and heart diseases, being a major symptom in most neoplastic diseases. Uncontrolled pain leads to a decrease in the quality of life and an increase in the morbidity of the patient. Opioids represent the best analgetic supportive therapy and are frequently used in patients suffering from cancer and experiencing a high level of pain. Opioid treatment starts with a gradual titration of the dose until the minimum effective dose and the maximum tolerated dose are determined...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28182123/long-term-safety-and-analgesic-efficacy-of-buprenorphine-buccal-film-in-patients-with-moderate-to-severe-chronic-pain-requiring-around-the-clock-opioids
#10
Martin Hale, Veronica Urdaneta, M Todd Kirby, Qinfang Xiang, Richard Rauck
BACKGROUND: This open-label, single-arm study was conducted to evaluate the long-term safety and efficacy of a novel buprenorphine formulation, buprenorphine buccal film, in the treatment of moderate-to-severe chronic pain requiring around-the-clock opioids. METHODS: The primary purpose of this study was to evaluate the long-term safety and tolerability of buprenorphine buccal film. Five hundred and six patients who completed previous studies with buprenorphine buccal film (n=445; rollover patients) or were recruited de novo for this study (n=61) were enrolled in this study...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28159539/continued-midazolam-versus-diphenhydramine-in-difficult-to-sedate-patients-a-randomized-double-blind-trial
#11
Hamita Sachar, Nipaporn Pichetshote, Kavitha Nandigam, Keta Vaidya, Loren Laine
BACKGROUND AND AIMS: Current guidelines recommend diphenhydramine in patients undergoing endoscopy who are not adequately sedated with a benzodiazepine and opioid combination. Because this practice has not been adequately assessed, we performed a randomized, double-blind trial comparing diphenhydramine with continued midazolam in such patients. METHODS: Patients undergoing elective colonoscopy with moderate sedation were eligible. Sedation was measured with the Modified Observer's Assessment of Alertness/Sedation (MOAA/S) score with adequate sedation defined as 3 on a 0- to 5-point scale...
January 31, 2017: Gastrointestinal Endoscopy
https://www.readbyqxmd.com/read/28153523/systemic-administration-of-the-dietary-constituent-resveratrol-inhibits-the-nociceptive-jaw-opening-reflex-in-rats-via-the-endogenous-opioid-system
#12
Shota Kokuba, Shiori Takehana, Katsuo Oshima, Yoshihito Shimazu, Mamoru Takeda
The aim of the present study was to investigate whether, under in vivo conditions, systemic administration of resveratrol could attenuate the rat nociceptive jaw-opening reflex (JOR) via the endogenous opioid system. The JOR evoked by electrical stimulation of the tongue was recorded as digastric muscle electromyograms (dEMG) in pentobarbital-anesthetized rats. The amplitude of the dEMG increased significantly in proportion to the intensity of electrical stimulation (from 1× to 5 × threshold for the JOR)...
January 30, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28144724/pharmacokinetics-of-a-new-nasal-formulation-of-naloxone
#13
Ida Tylleskar, Arne Kristian Skulberg, Turid Nilsen, Sissel Skarra, Phatsawee Jansook, Ola Dale
PURPOSE: Nasal naloxone is wanted for bystander administration in opioid overdose and as a needle-free alternative for emergency medical personnel. Epidemiologic studies have indicated a therapeutic effect of bystander administration of low-concentration/high-volume formulations. The objective for this study was to describe the nasal pharmacokinetics of a new high-concentration/low-volume nasal formulation of naloxone. METHODS: This was an open, randomized triple crossover trial in healthy, human volunteers (n = 12) where two doses of nasal naloxone (0...
January 31, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28127938/an-open-label-randomized-bioavailability-study-of-alternative-methods-of-oral-administration-of-naloxegol-in-healthy-subjects
#14
Khanh Bui, Bruce Birmingham, Ulysses Diva, Bruce Berger
Naloxegol is a peripherally acting μ-opioid receptor antagonist approved as an orally administered tablet for the treatment of opioid-induced constipation. Patients with swallowing difficulties may benefit from alternative approaches to the oral administration of the whole-tablet formulation of naloxegol. This open-label, randomized, 4-period, 4-treatment, crossover, single-dose study (NCT02446171) evaluated the pharmacokinetic (PK) characteristics of crushed naloxegol 25-mg tablets (suspended in water) administered orally or by nasogastric tube and a naloxegol solution compared with the commercially available 25-mg tablet formulation in healthy volunteers...
January 27, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28093646/mechanisms-of-inhibitory-action-of-trk-130-naltalimide-a-%C3%AE-opioid-receptor-partial-agonist-on-the-micturition-reflex
#15
Morihiro Fujimura, Naoki Izumimoto, Sayoko Kanie, Ryosuke Kobayashi, Satoru Yoshikawa, Shinobu Momen, Mikito Hirakata, Toshikazu Komagata, Satoshi Okanishi, Masashi Iwata, Tadatoshi Hashimoto, Takayuki Doi, Naoki Yoshimura, Koji Kawai
PURPOSE: To clarify the mechanism of inhibitory action of TRK-130 (Naltalimide), a unique µ-opioid receptor partial agonist, on the micturition reflex. METHODS: The effect of TRK-130 on isovolumetric rhythmic bladder contractions (RBCs) was examined in guinea pigs, the effect of which was clarified by co-treatment with naloxone or in spinal cord transection. The effect of TRK-130 on urodynamic parameters was also observed in guinea pigs. In addition, the effect of TRK-130 on bladder contraction induced by peripheral stimulation of the pelvic nerve was investigated in rats...
April 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/28092649/new-onset-depression-following-stable-slow-and-rapid-rate-of-prescription-opioid-dose-escalation
#16
Joanne Salas, Jeffrey F Scherrer, Frank David Schneider, Mark D Sullivan, Kathleen K Bucholz, Thomas Burroughs, Laurel A Copeland, Brian K Ahmedani, Patrick J Lustman
Recent studies suggest that longer durations of opioid use, independent of maximum morphine equivalent dose (MED) achieved, is associated with increased risk of new-onset depression (NOD). Conversely, other studies, not accounting for duration, found that higher MED increased probability of depressive symptoms. To determine whether rate of MED increase is associated with NOD, a retrospective cohort analysis of Veterans Health Administration data (2000-2012) was conducted. Eligible patients were new, chronic (>90 days) opioid users, aged 18 to 80, and without depression diagnoses for 2 years before start of follow-up (n = 7051)...
February 2017: Pain
https://www.readbyqxmd.com/read/28054242/anti-nociceptive-and-anti-inflammatory-actions-of-sulforaphane-in-chronic-constriction-injury-induced-neuropathic-pain-mice
#17
Cheng Wang, Congpin Wang
Neuropathic pain is still considered as incurable disease as current therapies are not ideal in terms of efficacy and tolerability. It is imperative to search for novel drugs to obtain better treatments. Sulforaphane (SFN), a derivative of glucoraphanin present in cruciferous vegetables, exhibits therapeutic effects on inflammation-related diseases. Since inflammation plays an important role in regulating chronic pain, in the present study, we investigated anti-nociceptive effects of SFN and its underlying mechanisms in a neuropathic pain mouse model, sciatic nerve chronic constriction injury (CCI)...
February 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28053591/potentially-inappropriate-medications-prescribed-for-elderly-patients-through-family-physicians
#18
Abdulaziz Al Odhayani, Ayla Tourkmani, Mohammed Alshehri, Hala Alqahtani, Adel Mishriky
The elderly population is increasing throughout the globe, resulting in higher healthcare costs. Potential inappropriate medication (PIM) prescriptions are a major health problem affecting the elderly persons. Due to limited studies in PIM use in primary care and home healthcare in Saudi Arabia, we aim to examine the extent of PIM prescription for and use by elderly patients. This study was carried out with 798 elderly patients, arbitrarily selected from Prince Sultan Medical Military City through the patient register...
January 2017: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/28035588/clinical-pharmacokinetics-and-pharmacodynamics-of-naloxegol-a-peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonist
#19
REVIEW
Khanh Bui, Diansong Zhou, Hongmei Xu, Eike Floettmann, Nidal Al-Huniti
Naloxegol is a peripherally acting µ-opioid receptor antagonist approved for use as an orally administered tablet (therapeutic doses of 12.5 and 25 mg) for the treatment of opioid-induced constipation. Over a wide dose range (i.e. single supratherapeutic doses up to 1000 mg in healthy volunteers), the pharmacokinetic properties of naloxegol appear to be time- and dose-independent. Naloxegol is rapidly absorbed, with mean time to maximum plasma concentration of <2 h. Following once-daily administration, steady state is achieved within 2-3 days and minimal accumulation is observed...
December 29, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27784231/effect-of-oral-methadone-on-ecg-characteristics-and-endocrine-hormonal-changes-and-their-inter-relationship
#20
Shokoufeh Bonakdaran, Mahdi Hassan Zadeh Daloee, Ali Akhoondpoor Manteghi, Mina Akbarirad, Abdollah Firoozi, Fatemeh Akbarirad
INTRODUCTION: Methadone is the most common opioid in use for opioid substitution therapy. The Relation of methadone and electrocardiographic findings is nearly well known while the relationship between its electrocardiographic indexes and hormonal changes are not well recognized. OBJECTIVE: To evaluate the hormonal changes in patients who are taking methadone maintenance treatment (MMT) and its effects on electrocardiographic indexes, in comparison with healthy control groups...
October 26, 2016: Endocrine, Metabolic & Immune Disorders Drug Targets
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