- Efficacy and Tolerability of Co-Administering Full µ-Opioid Receptor Agonists with Buprenorphine and Mixed Opioid Agonists. [Journal Article]
- DRDrug Res (Stuttg) 2016 Dec 07
- Overlapping buprenorphine, opioid, and benzodiazepine prescriptions among Veterans dually enrolled in VA and Medicare Part D. [Journal Article]
- SASubst Abus 2016 Dec 07; :0
- CONCLUSIONS: Many buprenorphine recipients receive overlapping prescriptions for opioids and benzodiazepines from a different health care system than the one in which their buprenorphine was filled. These findings highlight a previously undocumented safety risk for Veterans dually enrolled in VA and Medicare.
- Intravenous Use of Intranasal Naloxone: A Case of Overdose Reversal. [Journal Article]
- SASubst Abus 2016 Dec 07; :0
- CONCLUSIONS: This is the first known published case of a community-distributed naloxone nasal spray being used intravenously by a lay person (bystander). The case emphasizes the efficacy of naloxone in overdose reversal, and also the need for education or instructions on naloxone use by others (not just the user). Finally it highlights the risk of overdose in those entering treatment, seeking intoxication one last time.
- Inhibition of Glucuronidation and Oxidative Metabolism of Buprenorphine Using GRAS Compounds or Dietary Constituents/Supplements: In Vitro Proof of Concept. [Journal Article]
- BDBiopharm Drug Dispos 2016 Dec 07
- The present study investigated the potential of generally recognized as safe compounds or dietary substances to inhibit the presystemic metabolism of buprenorphine and increase its oral bioavailabili...
The present study investigated the potential of generally recognized as safe compounds or dietary substances to inhibit the presystemic metabolism of buprenorphine and increase its oral bioavailability. Using IVIVE, the buprenorphine extraction ratios in intestine and liver were predicted as 96% and 71%, respectively. In addition, the relative fraction of buprenorphine metabolized by oxidation and glucuronidation in these two organs was estimated using pooled human intestinal and liver microsomes. In both organs, oxidation appeared to be the major metabolic pathway with a six and four fold higher intrinsic clearance than glucuronidation in intestine and liver, respectively. The oral bioavailability of buprenorphine was predicted to be 1.16%. Inhibition of 75% and 50% of intestinal and hepatic presystemic metabolism would result in Foral of 49%, which is comparable to the bioavailability of sublingual buprenorphine. In human liver microsomes, chrysin, curcumin, ginger extract, hesperitin, magnolol, quercetin and silybin inhibited ≥50% glucuronidation whereas chrysin, curcumin, ginger extract, 6-gingerol, pterostilbene, resveratrol and silybin exhibited ≥30% inhibition of oxidation. In human intestinal microsomes, curcumin, ginger extract, α-mangostin, quercetin and silybin inhibited ≥50% glucuronidation while chrysin, ginger extract, α-mangostin, pterostilbene and resveratrol exhibited ≥30% inhibition of oxidation. These results demonstrate the feasibility of our proposed approach of using generally recognized as safe or dietary compounds to inhibit the presystemic metabolism of BUP and thus improve its oral bioavailability. An oral buprenorphine formulation containing these inhibitors or their combinations has promising potential to replace sublingual buprenorphine.
- Comparison of Abuse, Suspected Suicidal Intent, and Fatalities related to the 7-day Buprenorphine Transdermal Patch versus other Opioid Analgesics in the National Poison Data System. [Journal Article]
- PMPostgrad Med 2016 Dec 06
- CONCLUSIONS: This post-marketing evaluation of BTDS indicates infrequent poison center calls for intentional abuse and suspected suicidal intent events, suggesting lower rates of these risks with BTDS compared to other ER/LA opioids.
- Primary Care-Based Models for the Treatment of Opioid Use Disorder: A Scoping Review. [Journal Article]
- AIMAnn Intern Med 2016 Dec 06
- Greater integration of medication-assisted treatment (MAT) for opioid use disorder (OUD) in U.S. primary care settings would expand access to treatment for this condition. Models for integrating MAT ...
Greater integration of medication-assisted treatment (MAT) for opioid use disorder (OUD) in U.S. primary care settings would expand access to treatment for this condition. Models for integrating MAT into primary care vary in structure. This article summarizes findings of a technical report for the Agency for Healthcare Research and Quality describing MAT models of care for OUD, based on a literature review and interviews with key informants in the field. The report describes 12 representative models of care for integrating MAT into primary care settings that could be considered for adaptation across diverse health care settings. Common components of existing care models include pharmacotherapy with buprenorphine or naltrexone, provider and community education, coordination and integration of OUD treatment with other medical and psychological needs, and psychosocial services and interventions. Models vary in how each component is implemented. Decisions about adopting MAT models of care should be individualized to address the unique milieu of each implementation setting.
- Osteotomy models - the current status on pain scoring and management in small rodents. [Journal Article]
- LALab Anim 2016; 50(6):433-441
- Fracture healing is a complex regeneration process which produces new bone tissue without scar formation. However, fracture healing disorders occur in approximately 10% of human patients and cause se...
Fracture healing is a complex regeneration process which produces new bone tissue without scar formation. However, fracture healing disorders occur in approximately 10% of human patients and cause severe pain and reduced quality of life. Recently, the development of more standardized, sophisticated and commercially available osteosynthesis techniques reflecting clinical approaches has increased the use of small rodents such as rats and mice in bone healing research dramatically. Nevertheless, there is no standard for pain assessment, especially in these species, and consequently limited information regarding the welfare aspects of osteotomy models. Moreover, the selection of analgesics is restricted for osteotomy models since non-steroidal anti-inflammatory drugs (NSAIDs) are known to affect the initial, inflammatory phase of bone healing. Therefore, opioids such as buprenorphine and tramadol are often used. However, dosage data in the literature are varied. Within this review, we clarify the background of osteotomy models, explain the current status and challenges of animal welfare assessment, and provide an example score sheet including model specific parameters. Furthermore, we summarize current refinement options and present a brief outlook on further 3R research.
- Analgesia in clinically relevant rodent models of sepsis. [Journal Article]
- LALab Anim 2016; 50(6):418-426
- Postoperative analgesia in rodent sepsis models has been considerably neglected in the past. However, intentions to model clinical practice, increasing awareness of animal ethics, efforts to apply th...
Postoperative analgesia in rodent sepsis models has been considerably neglected in the past. However, intentions to model clinical practice, increasing awareness of animal ethics, efforts to apply the 3Rs (replacement, reduction, refinement), and stricter legislation argue for a change in this respect. In this review, we describe different concepts of analgesia in rodent models of sepsis focusing on opioid agonists as well as non-opioid analgesics. Advantages and pitfalls in study design and side-effects are discussed. Score sheets should be used to adapt analgesia or to terminate experiments using humane endpoints. Further research is needed to differentiate behavioral changes caused by sepsis and pain or as a consequence of analgesia. Information on the efficacy of analgesia in sepsis models is scarce. Hence, studies are needed to identify the best ways to reduce suffering of research animals and thereby optimize the clinically relevant rodent models of sepsis.
- Effect of Nerolidol and/or Levulinic Acid on the Thermotropic Behavior of Lipid Lamellar Structures in the Stratum Corneum. [Journal Article]
- CPChem Pharm Bull (Tokyo) 2016; 64(12):1692-1697
- Permeation enhancers are required to deliver drugs through the skin efficiently and maintain effective blood concentrations. Studies of the barrier function of the stratum corneum using l-menthol, a ...
Permeation enhancers are required to deliver drugs through the skin efficiently and maintain effective blood concentrations. Studies of the barrier function of the stratum corneum using l-menthol, a monocyclic monoterpene widely used in medicines and foods, have revealed an interaction between characteristic intercellular lipid structures in the stratum corneum and permeation enhancers. The variety of permeation enhancers that can be used to contribute to transdermal delivery systems beyond l-menthol is increasing. In this study, we focused on nerolidol and levulinic acid and investigated their influence on stratum corneum lipid structures. Nerolidol, a sesquiterpene, has been reported to enhance the permeation of various drugs. Levulinic acid is reported to enhance the permeability of buprenorphine and is used as a component of the buprenorphine(®) patch. Synchrotron X-ray diffraction and attenuated total reflectance Fourier transform IR spectroscopy measurements revealed that nerolidol disturbs the rigidly arranged lipid structure and increases lipid fluidity. Levulinic acid had a smaller effect on stratum corneum lipid structures, but did increase lipid fluidity when co-administered with nerolidol or heat. We found that nerolidol has an effect on stratum corneum lipids similar to that of l-menthol, and levulinic acid had an effect similar to that of oleic acid.
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- Prescription drug abuse - A timely update. [Journal Article]
- AFAust Fam Physician 2016; 45(12):862-866
- CONCLUSIONS: Data from the Coroners Court of Victoria list the main drugs that contributed to drug-related deaths in 2009-15. Analysis of the data reveals that pharmaceutical drugs contributed to 80% of overdose deaths; benzodiazepines and opioids were the main drug groups involved. Strategies for reducing and managing prescription drug abuse in primary care settings are outlined in this article, including references to published evidence-based clinical guidelines from The Royal Australian College of General Practitioners (RACGP). The safety profile of buprenorphine/ naloxone over methadone is noted and raised as a consideration for clinicians when assessing a patient for opioid replacement therapy.