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Grapefruit-drug interactions

Jingjing Yu, Zhu Zhou, Jessica Tay-Sontheimer, René H Levy, Isabelle Ragueneau-Majlessi
In recent years, an increasing number of clinical drug-drug interactions (DDIs) have been attributed to inhibition of intestinal organic anion transporting polypeptides (OATPs); however, only a few of these DDI results were reflected in drug labels. This review aims to provide a thorough analysis of intestinal OATP-mediated pharmacokinetic-based DDIs, using both in vitro and clinical investigations, highlighting the main mechanistic findings and discussing their clinical relevance. On the basis of pharmacogenetic and clinical DDI results, a total of 12 drugs were identified as possible clinical substrates of OATP2B1 and/or OATP1A2...
April 13, 2017: Journal of Pharmaceutical Sciences
Yushi Kashihara, Ichiro Ieiri, Takashi Yoshikado, Maeda Kazuya, Masato Fukae, Miyuki Kimura, Takeshi Hirota, Shunji Matsuki, Shin Irie, Noritomo Izumi, Hiroyuki Kusuhara, Yuichi Sugiyama
The aims of this study were (1) to investigate the effects of atorvastatin (10 mg, therapeutic dose) and grapefruit juice (GFJ), inhibitors of OATP2B1, on the pharmacokinetics of substrates for OATP2B1 and BCRP under oral small-dosing conditions (300 μg sulfasalazine, 250 μg rosuvastatin, 300 μg glibenclamide, 1200 μg celiprolol, and 600 μg sumatriptan), and (2) to evaluate the contribution of SLCO2B1*3 and ABCG2 c.421C>A polymorphisms to the pharmacokinetics of the five test drugs in 23 healthy volunteers...
March 17, 2017: Journal of Pharmaceutical Sciences
Magdalena Cholewka-Stafińska, Renata Polaniak, Marek Kardas, Mateusz Grajek, Elżbieta Grochowska-Niedworok
Oral medication (tablets, capsules, suspensions, liquids, etc.) are frequently used in therapy. This may arise due to the fact that oral medication patient can take at home and it reduce the stress associated with taking the drug. On the Polish pharmaceutical market can be observed more frequent registration to trading anticancer drugs in oral form. Is also growing interest about drug interactions with food, but they are still less accented than drug-drug interactions. The results of pharmacokinetic studies on the interaction of drugs used in antineoplastic therapy with food are particularly important because of the characteristics of cancer patients, and a growing number of people suffering from cancer and which may have a problem...
January 23, 2017: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
Emily J Johnson, Christina S Won, Kathleen Köck, Mary F Paine
Natural products, including botanical dietary supplements and exotic drinks, represent an ever-increasing share of the health-care market. The parallel ever-increasing popularity of self-medicating with natural products increases the likelihood of co-consumption with conventional drugs, raising concerns for unwanted natural product-drug interactions. Assessing the drug interaction liability of natural products is challenging due to the complex and variable chemical composition inherent to these products, necessitating a streamlined preclinical testing approach to prioritize precipitant individual constituents for further investigation...
April 2017: Biopharmaceutics & Drug Disposition
Dan Liu, Jie Wu, Hongbo Xie, Mingyi Liu, Isaiah Takau, Hong Zhang, Yuqing Xiong, Chunhua Xia
Hesperetin (HET) and naringenin (NGR) are flavanones found in citrus (oranges and grapefruit) and Aurantii Fructus Immaturus. The present study aims to investigate the inhibition potential of HET and NGR derivatives towards one of the most important phase II drug-metabolizing enzymes-uridine diphosphate (UDP)-glucuronosyltransferases (UGTs). We used trifluoperazine as a probe substrate to test UGT1A4 activity, and recombinant UGT-catalyzed 4-methylumbelliferone glucuronidation was used as a probe reaction for other UGT isoforms...
2016: Biological & Pharmaceutical Bulletin
Dirk Theile, Nicolas Hohmann, Dominik Kiemel, Giuseppe Gattuso, Davide Barreca, Gerd Mikus, Walter Emil Haefeli, Vedat Schwenger, Johanna Weiss
Adverse drug interactions due to grapefruit juice are well known prompting warnings even in drug labels. Similar issues have not been reported for clementines and available data is scarce, despite of genetic descent. We observed substantially increased tacrolimus trough concentrations in a renal transplant patient consuming high clementine amounts and, thus, scrutinised the effects of clementine juice on drug metabolism and drug transporters in vitro and compared it to the effects of mandarin and grapefruit juice...
January 15, 2017: European Journal of Pharmaceutical Sciences
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Danuta Owczarek
Background Overactive bladder syndrome is a condition where one or more of the symptoms such as pollakiuria, urgent need to urinate, nocturia and urinary incontinence is observed. Its prevalence ranges between 7 and 27 % in men and 9-43 % in women. The role of a pharmacist is to educate the patient on medications administration scheme, and drug interactions with particular food or food components. Aim of the review To assess a potential impact of food and fruit juice on the pharmacokinetic and therapeutic effects of medications used in treating overactive bladder syndrome...
December 2016: International Journal of Clinical Pharmacy
D G Bailey
WHAT IS KNOWN AND OBJECTIVE: Grapefruit juice interacts with a number of drugs. This commentary provides feedback on a previously proposed approach for predicting clinically relevant interactions with grapefruit juice based on the average inherent oral bioavailability (F) and magnitude of increase in bioavailability with other CYP3A inhibitors of the drug. COMMENT: Additional factors such as variability of the magnitude of the pharmacokinetic interaction among individuals, product monograph cautionary statements and vulnerability of the patient population should be considered...
October 6, 2016: Journal of Clinical Pharmacy and Therapeutics
Stéphane Mouly, Célia Lloret-Linares, Pierre-Olivier Sellier, Damien Sene, J-F Bergmann
An interaction of drug with food, herbs, and dietary supplements is usually the consequence of a physical, chemical or physiologic relationship between a drug and a product consumed as food, nutritional supplement or over-the-counter medicinal plant. The current educational review aims at reminding to the prescribing physicians that the most clinically relevant drug-food interactions may not be strictly limited to those with grapefruit juice and with the Saint John's Wort herbal extract and may be responsible for changes in drug plasma concentrations, which in turn decrease efficacy or led to sometimes life-threatening toxicity...
September 28, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Paweł Paśko, Tomasz Rodacki, Renata Domagała-Rodacka, Danuta Owczarek
Benign prostatic hyperplasia (BPH) is the most common disease in elderly men. BPH symptoms include frequent urination, urgent tenesmus and urination at night, a weak and interrupted urine flow and a sense of incomplete emptying of the bladder. Alpha- 1 adrenergic receptor antagonists and 5 α-reductase inhibitors form the most important groups of medications employed in BPH. Appropriately managed BPH patients shall be subject to counselling on interactions between agents belonging to these groups, and on particular components of the food they have...
October 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Marina Kawaguchi-Suzuki, Negar Nasiri-Kenari, Jonathan Shuster, Fred G Gmitter, Paul Cancalon, Felipe de Oliveria, Jennifer Kight, Eileen M Handberg, Carl J Pepine, Reginald F Frye, Rhonda M Cooper-DeHoff
The objectives of this study were to investigate the effect of grapefruit juice low in furanocoumarins on CYP3A activity and to summarize previous findings of enzyme inhibition measured by the metabolism of midazolam after intake of grapefruit juice. Twelve healthy volunteers participated in a prospective, randomized, double-blinded, 3-way crossover clinical study to determine the effect of regular grapefruit juice (RGJ) and a novel, low-furanocoumarin hybrid grapefruit juice (HGJ) on the metabolism of oral midazolam, used as a probe for in vivo CYP3A activity, compared with water as a control...
March 2017: Journal of Clinical Pharmacology
Roberto Collado-Borrell, Vicente Escudero-Vilaplana, Rosa Romero-Jiménez, Irene Iglesias-Peinado, Ana Herranz-Alonso, María Sanjurjo-Sáez
OBJECTIVE: To review interactions between oral antineoplastic agents (OAAs) for the treatment of solid and hematological tumors and common food and medicinal plants. MATERIALS AND METHODS: All potential interactions between OAAs, medicinal plants and food were reviewed. OAAs were considered to be drugs for oral administration that have direct antitumor activity and were approved by the European Medicines Agency in April 2015. We performed the literature search in Pubmed(®) considering only medicinal plants and food...
November 2016: Journal of Cancer Research and Clinical Oncology
Kannan Sridharan, Gowri Sivaramakrishnan
INTRODUCTION: Cyclosporine is an immunosuppressant with narrow therapeutic window, metabolized mainly by cytochrome P450 3A4 (CYP3A4) and minimally by cytochrome P450 3A5 (CYP3A5). Citrus juices such as grapefruit juice (GFJ), orange, lemon, pomelo and lime were known to interact with cyclosporine in several randomized controlled trials. The present review is a systematic compilation and quantitative synthesis on the changes of cyclosporine pharmacokinetics with concomitant citrus juice administration...
December 2016: European Journal of Drug Metabolism and Pharmacokinetics
Tonya Ng, Nadine Badry, Mário L de Lemos
OBJECTIVE: The objective of this study is to develop a systematic approach to standardize the use of auxiliary labels for oral oncology drugs. DESIGN: The project was multi-phased: environmental scan of auxiliary labels used at six BC Cancer Agency centre pharmacies, develop guidelines to support auxiliary labels standardization, develop inclusion criteria for common warnings and standardize warnings based on guiding principles and evidence (Canadian Compendium of Pharmaceutical Specialties, BC Cancer Agency Cancer Drug Manual, British National Formulary, literature)...
May 20, 2016: Journal of Oncology Pharmacy Practice
Neville F Ford
The major metabolic pathway of clopidogrel is conversion to carboxylic acid by an esterase (CES1), forming clopidogrelic acid (SR26334) that is inactive. There is agreement on the structure of the active metabolite; however, there are differing views about the mechanism of its formation. Sanofi studied the conversion of clopidogrel to the active metabolite using human liver microsomes. It was concluded that 2-oxo-clopidogrel was formed via CYP3A oxidation. From a subsequent in vitro study by Sankyo of the metabolism of clopidogrel using recombinant DNA CYPs, it was concluded that CYP2C19 was the major oxidative pathway...
December 2016: Journal of Clinical Pharmacology
Guohua An, Jatinder Kaur Mukker, Hartmut Derendorf, Reginald F Frye
Beverage-drug interactions have remained an active area of research and have been the subject of extensive investigations in the past 2 decades. The known mechanisms of clinically relevant beverage-drug interactions include modulation of the activity of cytochrome P450 (CYP) 3A and organic anion-transporting polypeptide (OATP). For CYP3A-mediated beverage-drug interaction, the in vivo CYP3A inhibitory effect is limited to grapefruit juice (GFJ), which increases the bioavailability of several orally administered drugs that undergo extensive first-pass metabolism via enteric CYP3A...
December 2015: Journal of Clinical Pharmacology
Zhi-Yu Wang, Meng Chen, Ling-Ling Zhu, Lu-Shan Yu, Su Zeng, Mei-Xiang Xiang, Quan Zhou
BACKGROUND: Coprescribing of clopidogrel and other drugs is common. Available reviews have addressed the drug-drug interactions (DDIs) when clopidogrel is as an object drug, or focused on combination use of clopidogrel and a special class of drugs. Clinicians may still be ignorant of those DDIs when clopidogrel is a precipitant drug, the factors determining the degree of DDIs, and corresponding risk management. METHODS: A literature search was performed using PubMed, MEDLINE, Web of Science, and the Cochrane Library to analyze the pharmacokinetic DDIs of clopidogrel and new P2Y12 receptor inhibitors...
2015: Therapeutics and Clinical Risk Management
S Mouly, M Morgand, A Lopes, C Lloret-Linares, J-F Bergmann
Orally administered medications may interact with various fruits, vegetables, herbal medicines, functional foods or dietary supplements. Drug-food interactions, which are mostly unknown from prescribers, including internists, may be responsible for changes in drug plasma concentrations, which may decrease efficacy or led to sometimes life-threatening toxicity. Aging, concomitant medications, transplant recipients, patients with cancer, malnutrition, HIV infection and those receiving enteral or parenteral feeding are at increased risk of drug-food interactions...
August 2015: La Revue de Médecine Interne
M A Nguyen, P Staubach, I Tamai, P Langguth
Naringin is considered the major causative ingredient of the inhibition of intestinal drug uptake by grapefruit juice. Moreover, it is contained in highly dosed nutraceuticals available on the market. A controlled, open, randomized, crossover study was performed in 10 healthy volunteers to investigate the effect of high-dose naringin on the bioavailability of talinolol, a substrate of intestinal organic anion-transporting polypeptide (OATP)-mediated uptake. Following 6-day supplementation with 3 capsules of 350 mg naringin daily, 100mg talinolol were administered orally with 3 capsules of the same dietary supplement (1050 mg naringin) on the seventh day...
February 20, 2015: European Journal of Pharmaceutical Sciences
Chittaranjan Andrade
Organic anion transporting polypeptides (OATPs) are a group of membrane transport proteins that facilitate the influx of endogenous and exogenous substances across biological membranes. OATPs are found in enterocytes and hepatocytes and in brain, kidney, and other tissues. In enterocytes, OATPs facilitate the gastrointestinal absorption of certain orally administered drugs. Fruit juices such as grapefruit juice, orange juice, and apple juice contain substances that are OATP inhibitors. These fruit juices diminish the gastrointestinal absorption of certain antiallergen, antibiotic, antihypertensive, and β-blocker drugs...
November 2014: Journal of Clinical Psychiatry
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