Methods: Two randomized, two-phase crossover studies were performed--study I with atorvastatin in 12 healthy volunteers and study II with pravastatin in 11 healthy volunteers. Is that true? You can also check your Patient Medication Guide that accompanies your prescription, and your pharmacist may include a label on your bottle warning you of an interaction. For example, if a 20-mg dose is administered, only 1 mg reaches the systemic circulation. Manufacturer advises avoid. In a randomized cross‐over study with two phases, 10 healthy volunteers ingested grapefruit juice 200 ml or water (control) for 3 days. When simvastatin is taken 24 hours after ingestion of “high‐dose” grapefruit juice, the effect of grapefruit juice on the AUC of simvastatin is only about 10% of the effect observed during concomitant intake of grapefruit juice and simvastatin. 5. Grapefruit juice moderately decreases the exposure to aliskiren. Simvastatin and the Grapefruit Connection came up today. Clin Pharmacol Ther 1998;64(5):477-83. Clin Pharmacol Ther 1998;64(5):477-83. The first published clinical report on grapefruit drug interactions was in 1991 in The Lancet entitled "Interactions of Citrus Juices with Felodipine and Nifedipine." Interactions involving inhibitors of CYP3A4. Currently, more than 85 drugs, most of which are available in Canada, are known or predicted to interact with grapefruit. [Dr. Bailey was part of the Canadian research team that discovered grapefruit interactions with the blood pressure medicine felodipine (Lancet, Feb. 2, 1991). I was picking up my prescription as usual. Simvastatin Interactions with Food and Herbs Grapefruit Juice: Grapefruit juice increases the concentration of simvastatin in the blood stream leading to possible side effects. It is taken by mouth. Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin. It is already known that grapefruits contain a group of chemicals, furanocoumarins, which can affect drug metabolism – the amount of time it takes for a drug to be broken down by the body. Duration of effect of grapefruit … They informed me not to eat any grapefruit. “Our research group discovered the interaction between grapefruit and certain medications more than 20 years ago. Evidence shows that only one instance of grapefruit or grapefruit product consumption can be enough to cause these drugs to build up in your system, and timing doesn't matter much either. The probable mechanism of this interaction was inhibition of CYP3A4‐mediated first‐pass metabolism of simvastatin by grapefruit juice in the small intestine. This interaction substantially increased the systemic exposure to felodipine and by this amplified its pharmacodynamic effects. Although all statins may be affected by drug interactions, simvastatin is exceptionally sensitive for several reasons. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. Grapefruit juice–simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. If grapefruit, Pomelos and Seville oranges are a part of your daily diet, notify your physician before starting therapy with Lipitor, since a lower dose might avert a potential problem 2. 7. Grapefruit and certain other citrus fruits, such as Seville oranges, can interfere with several kinds of prescription medications. Clin Pharmacol Ther. The grapefruit-drug interaction debate: role of statins. Further information about fruit/medicine interactions is available in Stockley's Drug Interactions. On day 3, a single 40‐mg dose of simvastatin was administered with grapefruit juice 200 ml or water. the increase in the C max of simvastatin ranged from 2.3‐fold to 9.3‐fold and that in the AUC(0–24) from 1.8‐fold to 6.0‐fold. Severity of interaction: Moderate Evidence for interaction: Theoretical. It is also used to decrease the risk of heart problems in those at high risk. Am Fam Physician 2007;76(2):190, 92; author reply 92. Don't take these interactions lightly. Reamy BV, Stephens MB. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. It is used along with exercise, diet, and weight loss to decrease elevated lipid levels. Why can’t I eat grapefruit? Grapefruit juice-simvastatin interaction : Effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors Author LILJA, J. J; KIVISTÖ, K. T; NEUVONEN, P. J Department of Clinical Pharmacology, University of Helsinki, and Helsinki University Central Hospital, Finland Source. Clin Pharmacol Ther 1999;66(2):118-27. Simvastatin and grapefruit should not be combined because the presence of grapefruit in a person's system makes it hard to break down the active chemical in simvastatin. I like to drink grapefruit juice but hear that it can interfere with some prescription medications. Either of these situations can lead to serious health complications. This can lead to a situation in which there is too much simvastatin in a person's body or where the drug remains in the body for too long. Is grapefruit unsafe with all statins? vytorin. Frequently, when grapefruit becomes a part of the diet, the side effects of a drug-food interaction are noted in those established on Lipitor drug therapy 2. Lilja JJ, Kivisto KT, Neuvonen PJ. 4 The impact of other bergamottin sources is unclear. Clinical pharmacology and therapeutics. Grapefruit juice greatly increased serum concentrations of simvastatin and simvastatin acid and, to a lesser extent, those of active and total HMG‐CoA reductase inhibitors. According to the world’s expert on grapefruit interactions, David Bailey, MD, these statins are safe alternatives to atorvastatin, lovastatin or simvastatin (CMAJ, March 5, 2013). There is hope if you really enjoy grapefruit. Simvastatin and grapefruit juice interaction. Avoid grapefruit juice when taking simvastatin Effects of other medicinal products on simvastatin. This time it was about Simvastatin. Simvastatin: Avoid grapefruit juice and the whole fruit: Tacrolimus: Avoid grapefruit juice and the whole fruit : Adapted from New Zealand Formulary - Interactions. Repeated consumption has a greater effect than one exposure but certain medications’ effects are sensitive to consistent drug levels (e.g. Common side effects include constipation, headaches, and nausea. Provides a summary of interactions with vitamins, herbs, and food Aliskiren. Answers from Katherine Zeratsky, R.D., L.D. Interaction between ergotamine for migraine and grapefruit juice may cause gangrene or stroke.