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https://www.readbyqxmd.com/read/27557472/linking-in-vitro-lipolysis-and-microsomal-metabolism-for-the-quantitative-prediction-of-oral-bioavailability-of-bcs-ii-drugs-administered-in-lipidic-formulations
#1
Paloma Benito-Gallo, Maria Marlow, Vanessa Zann, Peter Scholes, Pavel Gershkovich
Lipidic formulations (LFs) are increasingly utilized for the delivery of drugs that belong to class II of the Biopharmaceutics Classification System (BCS). The current work proposes, for the first time, the combination of in vitro lipolysis and microsomal metabolism studies for the quantitative prediction of human oral bioavailability of BCS II drugs administered in LFs. Marinol and Neoral were selected as model LFs, and their observed oral bioavailabilities (Fobserved ) were obtained from published clinical studies in humans...
October 3, 2016: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/27435265/cannabinoids-inflammation-and-fibrosis
#2
REVIEW
Robert B Zurier, Sumner H Burstein
Cannabinoids apparently act on inflammation through mechanisms different from those of agents such as nonsteroidal anti-inflammatory drugs (NSAIDs). As a class, the cannabinoids are generally free from the adverse effects associated with NSAIDs. Their clinical development thus provides a new approach to treatment of diseases characterized by acute and chronic inflammation and fibrosis. A concise survey of the anti-inflammatory actions of the phytocannabinoids Δ9 -tetrahydrocannabinol (THC), cannabidiol, cannabichromene, and cannabinol is presented...
November 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27109234/chronic-%C3%AE-9-tetrahydrocannabinol-administration-reduces-ige-b-cells-but-unlikely-enhances-pathogenic-sivmac251-infection-in-male-rhesus-macaques-of-chinese-origin
#3
Qiang Wei, Li Liu, Zhe Cong, Xiaoxian Wu, Hui Wang, Chuan Qin, Patricia Molina, Zhiwei Chen
Delta9-tetrahydrocannabinol (Δ(9)-THC) is the major psychoactive component of the cannabis plant. Δ(9)-THC has been used in the active ingredient of Marinol as an appetite stimulant for AIDS patients. Its impact on progression of HIV-1 infection, however, remains debatable. Previous studies indicated that Δ(9)-THC administration enhanced HIV-1 infection in huPBL-SCID mice but seemingly decreased early mortality in simian immunodeficiency virus (SIV) infected male Indian-derived rhesus macaques. Here, we determine the chronic effect of Δ(9)-THC administration using 0...
September 2016: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/27007804/various-acylglycerols-from-common-oils-exert-different-antitumor-activities-on-colorectal-cancer-cells
#4
Rebeca P Ramos-Bueno, María J González-Fernández, José L Guil-Guerrero
Colorectal cancer is one of the leading causes of death in Western countries; therefore, the implementation of healthy dietary habits in order to prevent its occurrence is a desirable action. We show here that both free fatty acids (FFAs) and some acylglycerols induce antitumoral actions in the colorectal cancer cell line HT-29. We tested several C18 polyunsaturated fatty acid-enriched oils (e.g., sunflower and Echium) as well as other oils, such as arachidonic acid-enriched (Arasco®) and docosahexaenoic acid-enriched (Marinol® and cod liver oil), in addition to coconut and olive oils...
2016: Nutrition and Cancer
https://www.readbyqxmd.com/read/26443472/medical-marijuana-patient-counseling-points-for-health-care-professionals-based-on-trends-in-the-medical-uses-efficacy-and-adverse-effects-of-cannabis-based-pharmaceutical-drugs
#5
REVIEW
Jayesh R Parmar, Benjamin D Forrest, Robert A Freeman
The purpose of this report is to present a review of the medical uses, efficacy, and adverse effects of the three approved cannabis-based medications and ingested marijuana. A literature review was conducted utilizing key search terms: dronabinol, nabilone, nabiximols, cannabis, marijuana, smoke, efficacy, toxicity, cancer, multiple sclerosis, nausea, vomiting, appetite, pain, glaucoma, and side effects. Abstracts of the included literature were reviewed, analyzed, and organized to identify the strength of evidence in medical use, efficacy, and adverse effects of the approved cannabis-based medications and medical marijuana...
July 2016: Research in Social & Administrative Pharmacy: RSAP
https://www.readbyqxmd.com/read/26162535/a-state-of-the-art-review-of-the-management-and-treatment-of-taste-and-smell-alterations-in-adult-oncology-patients
#6
REVIEW
Trina Thorne, Karin Olson, Wendy Wismer
PURPOSE: The purpose of this review was to examine studies of interventions for the prevention and management of taste and smell alterations (TSA) experienced by adult oncology patients. METHODS: Articles published between 1993 and 2013 were identified by searching CINAHL, MEDLINE and Food Science & Technology Abstracts (FSTA) and were included if they were in English and focused on adult oncology patients. Only interventions within the scope of nursing practice were reviewed...
September 2015: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/25957748/comparing-treatment-effects-of-oral-thc-on-simulated-and-on-the-road-driving-performance-testing-the-validity-of-driving-simulator-drug-research
#7
J L Veldstra, W M Bosker, D de Waard, J G Ramaekers, K A Brookhuis
RATIONALE: The driving simulator provides a safe and controlled environment for testing driving behaviour efficiently. The question is whether it is sensitive to detect drug-induced effects. OBJECTIVE: The primary aim of the current study was to investigate the sensitivity of the driving simulator for detecting drug effects. As a case in point, we investigated the dose-related effects of oral ∆(9)-tetrahydrocannabinol (THC), i.e. dronabinol, on simulator and on-the-road driving performance in equally demanding driving tasks...
August 2015: Psychopharmacology
https://www.readbyqxmd.com/read/25666611/fatty-acid-binding-proteins-fabps-are-intracellular-carriers-for-%C3%AE-9-tetrahydrocannabinol-thc-and-cannabidiol-cbd
#8
Matthew W Elmes, Martin Kaczocha, William T Berger, KwanNok Leung, Brian P Ralph, Liqun Wang, Joseph M Sweeney, Jeremy T Miyauchi, Stella E Tsirka, Iwao Ojima, Dale G Deutsch
Δ(9)-Tetrahydrocannabinol (THC) and cannabidiol (CBD) occur naturally in marijuana (Cannabis) and may be formulated, individually or in combination in pharmaceuticals such as Marinol or Sativex. Although it is known that these hydrophobic compounds can be transported in blood by albumin or lipoproteins, the intracellular carrier has not been identified. Recent reports suggest that CBD and THC elevate the levels of the endocannabinoid anandamide (AEA) when administered to humans, suggesting that phytocannabinoids target cellular proteins involved in endocannabinoid clearance...
April 3, 2015: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/24835149/dithiolopyrrolones-biosynthesis-synthesis-and-activity-of-a-unique-class-of-disulfide-containing-antibiotics
#9
REVIEW
Bo Li, Walter J Wever, Christopher T Walsh, Albert A Bowers
Covering: up to 2014. Dithiolopyrrolone (DTP) group antibiotics were first isolated in the early half of the 20th century, but only recently has research been reawakened by insights gained from the synthesis and biosynthesis of this structurally intriguing class of molecules. DTPs are characterized by an electronically unique bicyclic structure, which contains a compact disulfide bridge between two ene-thiols. Points of diversity within the compound class occur outside of the bicyclic core, at the two amide nitrogens...
July 2014: Natural Product Reports
https://www.readbyqxmd.com/read/24691713/a-unified-strategy-for-the-synthesis-of-the-c1-c14-fragment-of-marinolic-acids-mupirocins-pseudomonic-acids-and-thiomarinols-total-synthesis-of-pseudomonic-acid-methyl-monate-c
#10
Y Sridhar, P Srihari
A flexible stereoselective approach to the common C1-C14 skeleton present in natural products of the pseudomonic acid family is described. The strategy has been extended and the total synthesis of pseudomonic acid methyl monate C was achieved. The key synthetic reactions utilized include Achmatowicz rearrangement, Johnson-Claisen rearrangement, Julia-Kocienski olefination, and Horner-Wadsworth-Emmons olefination reaction.
May 14, 2014: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/24197528/effects-of-dietary-borage-oil-enriched-in-%C3%AE-linolenic-acid-18-3-n-6-or-marine-fish-oil-enriched-in-eicosapentaenoic-acid-20-5-n-3-on-growth-mortalities-liver-histopathology-and-lipid-composition-of-juvenile-turbot-scophthalmus-maximus
#11
J G Bell, D R Tocher, F M Macdonald, J R Sargent
A marine fish oil, Marinol K (MO) and borage oil (BO) were used to formulate diets relatively rich in eicosapentaenoic acid [EPA; 20:5(n-3)] and γ-linolenic acid [GLA; 18:3(n-6)], respectively. The diets were fed to duplicate groups of juvenile turbot (Scophthalmus maximus) of initial weight 1.4 g for a period of 12 weeks. No differences were observed in final weights either between duplicate tanks or between dietary treatments. Mortalities in the MO-fed group were significantly greater than in the BO-fed group...
October 1995: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/23421098/-marihuana-and-cannobinoids-as-medicaments
#12
REVIEW
Marek Tkaczyk, Ewa Florek, Wojciech Piekoszewski
Biological activity of cannabinoids is caused by binding to two cannabinoid receptors CB1 and CB2. Psychoactive is not only tetrahydrocannabinol (THC) but also: cannabidiol, cannabigerol or cannabichromen. Formerly, the usefulness of hemp was assessed in the relation to temporary appeasement of the symptoms of some ailments as nausea or vomiting. Present discoveries indicates that cannabis-based drugs has shown ability to alleviate of autoimmunological disorders such as: Multiple sclerosis (MS), Rheumatoid arthritis (RA) or inflammatory bowel disease...
2012: Przegla̧d Lekarski
https://www.readbyqxmd.com/read/23287502/acyl-migration-evaluation-in-monoacylglycerols-from-echium-plantagineum-seed-oil-and-marinol
#13
Miguel Ángel Rincón Cervera, Elena Venegas Venegas, Rebeca Ramos Bueno, Ignacio Rodríguez García, José Luis Guil-Guerrero
Production of 2-monoacylglycerols (2-MAGs) by selective hydrolysis of the triacylglycerols (TAGs) of Echium plantagineum seed oil and Marinol and further purification was carried out. Three purification methods, including silica gel column chromatography, liquid-liquid extraction and low-temperature crystallization were assayed. Partial acyl migration during the purification step is always observed. Acyl migration rates were similar both for the column chromatography and for the liquid-liquid extraction methods, and resulted in 1-MAG/2-MAG ratios higher than 1...
May 2013: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/23108552/targeting-the-endocannabinoid-system-with-cannabinoid-receptor-agonists-pharmacological-strategies-and-therapeutic-possibilities
#14
REVIEW
Roger G Pertwee
Human tissues express cannabinoid CB(1) and CB(2) receptors that can be activated by endogenously released 'endocannabinoids' or exogenously administered compounds in a manner that reduces the symptoms or opposes the underlying causes of several disorders in need of effective therapy. Three medicines that activate cannabinoid CB(1)/CB(2) receptors are now in the clinic: Cesamet (nabilone), Marinol (dronabinol; Δ(9)-tetrahydrocannabinol (Δ(9)-THC)) and Sativex (Δ(9)-THC with cannabidiol). These can be prescribed for the amelioration of chemotherapy-induced nausea and vomiting (Cesamet and Marinol), stimulation of appetite (Marinol) and symptomatic relief of cancer pain and/or management of neuropathic pain and spasticity in adults with multiple sclerosis (Sativex)...
December 5, 2012: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/22573509/-cannabinoid-drugs-for-neurological-diseases-what-is-behind
#15
REVIEW
Javier Fernández-Ruiz
In recent years progress has been made in the development of pharmaceuticals based on the plant Cannabis sativa or on synthetic molecules with a similar action. Some of these pharmaceuticals, such as the mouth spray Sativex, have recently been approved for the treatment of spasticity in multiple sclerosis, but they are not the first and others, such as Marinol or Cesamet for the treatment of vomiting and nausea, and anorexia-cachexia syndrome, had already been approved. This incipient clinical use of cannabinoid drugs confirms something that was already known from fairly ancient times up to practically the last century, which is the potential use of this plant for medicinal applications - something which was brought to a standstill by the abusive use of preparations of the plant for recreational purposes...
May 16, 2012: Revista de Neurologia
https://www.readbyqxmd.com/read/22280340/cannabinoids-novel-medicines-for-the-treatment-of-huntington-s-disease
#16
REVIEW
Onintza Sagredo, M Ruth Pazos, Sara Valdeolivas, Javier Fernandez-Ruiz
Cannabinoid pharmacology has experienced a notable increase in the last 3 decades which is allowing the development of novel cannabinoid-based medicines for the treatment of different human pathologies, for example, Cesamet® (nabilone) or Marinol® (synthetic Δ9-tetrahydrocannabinol for oral administration) that were approved in 80s for the treatment of nausea and vomiting associated with chemotherapy treatment in cancer patients and in 90s for anorexiacachexia associated with AIDS therapy. Recently, the british company GW Pharmaceuticals plc has developed an oromucosal spray called Sativex®, which is constituted by an equimolecular combination of Δ9-tetrahydrocannabinol- and cannabidiol- enriched botanical extracts...
April 1, 2012: Recent Patents on CNS Drug Discovery
https://www.readbyqxmd.com/read/21671456/a-randomized-double-blind-placebo-controlled-crossover-study-to-evaluate-the-subjective-abuse-potential-and-cognitive-effects-of-nabiximols-oromucosal-spray-in-subjects-with-a-history-of-recreational-cannabis-use
#17
RANDOMIZED CONTROLLED TRIAL
Kerri Alexandra Schoedel, Nancy Chen, Annie Hilliard, Linda White, Colin Stott, Ethan Russo, Stephen Wright, Geoffrey Guy, Myroslava K Romach, Edward M Sellers
OBJECTIVE: This study aimed to evaluate the abuse potential and cognitive effects of nabiximols (Sativex, GW Pharma Ltd. Salisbury, UK), an oromucosal spray primarily containing delta‐9‐tetrahydrocannabinol (THC) and cannabidiol (CBD). METHODS: This was a single‐dose, randomized, double‐blind, crossover study comparing nabiximols (4, 8, and 16 consecutive sprays: 10.8, 21.6, and 43.2 mg THC, respectively) with dronabinol 20 and 40 mg (synthetic THC: Marinol, Solvay Pharmaceuticals, Brussels, Belgium) and matching placebos in 23 recreational cannabis users...
April 2011: Human Psychopharmacology
https://www.readbyqxmd.com/read/21454026/thcva-a-a-new-additional-marker-for-illegal-cannabis-consumption
#18
Lars Radünz, Folker Westphal, Edmund Maser, Gertrud Rochholz
The aim of the present investigations was to find markers for differentiating between the consumption of illegal cannabis products and legal medication containing fully synthetic Δ9-tetrahydrocannabinol (Δ9-THC), e.g., Marinol capsules. Δ9-Tetrahydrocannabinolic acid A (Δ9-THCA-A) and Δ9-tetrahydrocannabivarinic acid A (Δ9-THCVA-A) were taken into consideration for analysis, because these substances are the precursors of Δ9-THC and Δ9-tetrahydrocannabivarin (Δ9-THCV) in plant material of Cannabis sativa and are not contained in medical THC formulations...
February 10, 2012: Forensic Science International
https://www.readbyqxmd.com/read/21343383/delta-9-tetrahydrocannabinol-may-palliate-altered-chemosensory-perception-in-cancer-patients-results-of-a-randomized-double-blind-placebo-controlled-pilot-trial
#19
RANDOMIZED CONTROLLED TRIAL
T D Brisbois, I H de Kock, S M Watanabe, M Mirhosseini, D C Lamoureux, M Chasen, N MacDonald, V E Baracos, W V Wismer
BACKGROUND: A pilot study (NCT00316563) to determine if delta-9-tetrahydrocannabinol (THC) can improve taste and smell (chemosensory) perception as well as appetite, caloric intake, and quality of life (QOL) for cancer patients with chemosensory alterations. PATIENTS AND METHODS: Adult advanced cancer patients, with poor appetite and chemosensory alterations, were recruited from two sites and randomized in a double-blinded manner to receive either THC (2.5 mg, Marinol(®); Solvay Pharma Inc...
September 2011: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/20530732/disposition-of-cannabinoids-in-oral-fluid-after-controlled-around-the-clock-oral-thc-administration
#20
Garry Milman, Allan J Barnes, David M Schwope, Eugene W Schwilke, William D Darwin, Robert S Goodwin, Deanna L Kelly, David A Gorelick, Marilyn A Huestis
BACKGROUND: Oral fluid, a promising alternative matrix for drug monitoring in clinical and forensic investigations, offers noninvasive sample collection under direct observation. Cannabinoid distribution into oral fluid is complex and incompletely characterized due to the lack of controlled drug administration studies. METHODS: To characterize cannabinoid disposition in oral fluid, we administered around-the-clock oral Delta(9)-tetrahydrocannabinol (THC) (Marinol) doses to 10 participants with current daily cannabis use...
August 2010: Clinical Chemistry
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