ABSTRACT
OBJECTIVE: To assess the use of an electronic knowledge resource to document continuing education activities and reveal educational needs of practicing pharmacists. METHODS: Over a 38-week period, 67 e-mails were sent to 6,500 Canadian Pharmacists Association (CPhA) members. Each e-mail contained a link to an e-Therapeutics+ Highlight, a factual excerpt of selected content from an online drug and therapeutic knowledge resource. Participants were then prompted to complete a pop-up questionnaire. RESULTS: Members completed 4,140 questionnaires. Participants attributed the information they learned in the Highlights to practice improvements (50.4%), learning (57.0%), and motivation to learn more (57.4%). CONCLUSIONS: Reading Highlight excerpts and completing Web-based questionnaires is an effective method of continuing education that could be easily documented and tracked, making it an effective tool for use with e-portfolios.
Subject(s)
Education, Pharmacy, Continuing/methods , Needs Assessment , Pharmacists/psychology , Surveys and Questionnaires , Canada , Educational Measurement , Health Knowledge, Attitudes, Practice , Humans , Internet , MotivationABSTRACT
In this study, we used an in vitro Caco-2 cell monolayer model to evaluate aqueous extracts of commercial-source goldenseal (Hydrastis canadensis) and milk thistle (Silybum marianum) capsule formulations, their marker phytochemicals (berberine and silibinin, respectively), as well as dillapiol, vinblastine, and the HIV protease inhibitor saquinavir for their ability to modulate CYP3A4 and ABCB1 expression after short-term exposure (48 h). Both upregulation and downregulation of CYP3A4 expression was observed with extracts of varying concentrations of the two natural health products (NHPs). CYP3A4 was highly responsive in our system, showing a strong dose-dependent modulation by the CYP3A4 inhibitor dillapiol (upregulation) and the milk thistle flavonolignan silibinin (downregulation). ABCB1 was largely unresponsive in this cellular model and appears to be of little value as a biomarker under our experimental conditions. Therefore, the modulation of CYP3A4 gene expression can serve as an important marker for the in vitro assessment of NHP-drug interactions.
Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1/biosynthesis , Cytochrome P-450 Enzyme System/biosynthesis , Hydrastis , Silybum marianum , ATP Binding Cassette Transporter, Subfamily B , Allyl Compounds , Antineoplastic Agents, Phytogenic/pharmacology , Caco-2 Cells , Capsules , Chromatography, High Pressure Liquid , Cytochrome P-450 CYP3A , Dioxoles/pharmacology , HIV Protease Inhibitors/pharmacology , Humans , Plant Extracts/administration & dosage , Plant Extracts/pharmacology , Reverse Transcriptase Polymerase Chain Reaction , Saquinavir/pharmacology , Vinblastine/pharmacologyABSTRACT
A 70% ethanol extract of California poppy (Eschscholzia californica) was able to bind to 5-HT(1A) and 5-HT(7) receptors at 100 mug/mL. The subsequent isolation procedure yielded the known alkaloids californidine (1), escholtzine (2), N-methyllaurotetanine (3), caryachine (4), and O-methylcaryachine (5), along with a new pavine alkaloid, 6S,12S-neocaryachine-7-O-methyl ether N-metho salt (7). The structure of 7 was determined by spectroscopic data interpretation, while the absolute stereochemistry was determined by means of circular dichroism. From the results obtained from the radioligand-binding assay of the pure compounds, including the commercially available protopine (6), it was evident that the activity on the 5-HT(1A) receptor was at least partly due to the presence of the aporphine alkaloid 3, which showed the highest inhibition of [(3)H]8-hydroxy-2-(di-N-propylamino)tetralin ([(3)H]8-OH-DPAT) binding with an EC(50) value of 155 nM and a K(i) of 85 nM.
Subject(s)
8-Hydroxy-2-(di-n-propylamino)tetralin/pharmacology , Alkaloids , Eschscholzia/chemistry , Receptor, Serotonin, 5-HT1A/drug effects , Serotonin Receptor Agonists/pharmacology , Alkaloids/chemistry , Alkaloids/isolation & purification , Alkaloids/pharmacology , Benzylisoquinolines/chemistry , Benzylisoquinolines/isolation & purification , Benzylisoquinolines/pharmacology , Dioxoles/chemistry , Dioxoles/isolation & purification , Dioxoles/pharmacology , Humans , Molecular StructureABSTRACT
PURPOSE: Traditional Chinese medicines (TCM) are believed by many to be safe and used for self-medication without supervision. Although the risk appears to be low, certain TCM have been associated with a number of serious adverse reactions. A preliminary study was undertaken with 12 products using a human cytochrome P450 (CYP450) isozyme assay to determine if these products could affect human drug metabolism. METHODS: Aliquots of samples were analyzed directly or as extracts for their potential to affect CYP450 2C9, 2C19, 2D6, and 3A4 mediated-metabolism of marker substrates using an in vitro fluorometric microtiter plate assay. RESULTS: One product was found to be a Chinese Proprietary Medicine (CPM). Most aqueous extracts inhibited CYP450 mediated-metabolism of at least 3 isozymes (ranging from 25-100%). All liquid samples markedly inhibited the metabolism of all 4 isozymes. De le ke chuan kang and Rensheng dao were the strongest CYP450 inhibitors. CONCLUSIONS: Our in vitro findings demonstrate that TCM can inhibit CYP450 2C9, 2C19, 2D6 and 3A4 mediated-metabolism. TCM need to be examined further under clinical settings to determine if potential interactions will occur that affect the safety and efficacy of conventional therapeutic products.
