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The grapefruit-drug interaction debate: role of statins. Simvastatin, sold under the brand name Zocor among others, is a lipid-lowering medication. Although there have been no systematic investigations of a grapefruit-simvastatin interaction regarding the duration of consumption, to be on the safe side, patients taking simvastatin are advised now not to eat grapefruit or drink grapefruit juice. Lilja JJ, Kivisto KT, Neuvonen PJ. Currently, more than 85 drugs, most of which are available in Canada, are known or predicted to interact with grapefruit. Manufacturer advises avoid. Is grapefruit unsafe with all statins? 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. Common Questions and Answers about Simvastatin and grapefruit juice interaction. Doctors give trusted answers on uses, effects, side-effects, and cautions: Dr. Weixel on zocor and grapefruit interaction: When fluvoxamine is taken with grapefruit juice, or even taken some time apart, the grapefruit juice may cause the fluvoxamine to build up in your body. View abstract. The effect of grapefruit juice with regard to drug absorption was originally discovered in 1989. Provides a summary of interactions with vitamins, herbs, and food Plasma concentrations of simvastatin and simvastatin acid were determined up to 24 h. Results But I do love grapefruit. Simvastatin and the Grapefruit Connection. Simvastatin and grapefruit juice interaction. 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. Grapefruit juice does not affect all the drugs in the categories above. Answers from Katherine Zeratsky, R.D., L.D. The news is based on a review that has highlighted grapefruit-medication interactions that can cause serious side effects. 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. The first published clinical report on grapefruit drug interactions was in 1991 in The Lancet entitled "Interactions of Citrus Juices with Felodipine and Nifedipine." Duration of effect of grapefruit … Clin Pharmacol Ther 1998;64(5):477-83. Grapefruit has the following interaction information: Abemaciclib. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. 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. I like to drink grapefruit juice but hear that it can interfere with some prescription medications. Some can cause potentially dangerous health problems. Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin. Grapefruit juice is predicted to increase the exposure to abemaciclib. Either of these situations can lead to serious health complications. Clin Pharmacol Ther 1998;64(5):477-83. Repeated consumption has a greater effect than one exposure but certain medications’ effects are sensitive to consistent drug levels (e.g. One of the unique properties of simvastatin is very low bioavailability (<5%) due to high firstpass metabolism. Clin Pharmacol Ther. Clin Pharmacol Ther 1999;66(2):118-27. Yes. This increased amount of fluvoxamine will have a greater effect of both desired and undesired effects. This interaction enhances … History. Simvastatin Interactions with Food and Herbs Grapefruit Juice: Grapefruit juice increases the concentration of simvastatin in the blood stream leading to possible side effects. Simvastatin: Avoid grapefruit juice and the whole fruit: Tacrolimus: Avoid grapefruit juice and the whole fruit : Adapted from New Zealand Formulary - Interactions. 7. Eating a whole grapefruit or drinking a cup of grapefruit juice can cause a clinically significant interaction with a host of medications. Why can’t I eat grapefruit? It is used along with exercise, diet, and weight loss to decrease elevated lipid levels. Avoid grapefruit juice when taking simvastatin Effects of other medicinal products on simvastatin. 1, 2 This interaction was discovered by coincidence in the course of an ethanol–drug interaction study in which grapefruit juice was used to mask the taste of the ethanol vehicle. Clinical pharmacology and therapeutics. Additional grapefruit juice drug interactions, and interactions with other juices, can be researched in the Drug Interaction Checker. Interaction between ergotamine for migraine and grapefruit juice may cause gangrene or stroke. Grapefruit juice moderately decreases the exposure to aliskiren. 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. In stroke, interaction with nimodipine may cause systemic hypotension. 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. Background: Grapefruit juice greatly increases the bioavailability of lovastatin and simvastatin. 5. Grapefruit and certain other citrus fruits, such as Seville oranges, can interfere with several kinds of prescription medications. Lilja JJ, Kivisto KT, Neuvonen PJ. 4. 5. vytorin. The probable mechanism of this interaction was inhibition of CYP3A4‐mediated first‐pass metabolism of simvastatin by grapefruit juice in the small intestine. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. 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. 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. We studied the effect of grapefruit juice on the pharmacokinetics of atorvastatin and pravastatin. I was picking up my prescription as usual. Reamy BV, Stephens MB. It is also used to decrease the risk of heart problems in those at high risk. On day 3, a single 40‐mg dose of simvastatin was administered with grapefruit juice 200 ml or water. But this time the pharmacist’s assistant had me talk to the pharmacist about the prescription drug. Common side effects include constipation, headaches, and nausea. Is that true? This interaction substantially increased the systemic exposure to felodipine and by this amplified its pharmacodynamic effects. 1998;64:477–83. 4 The impact of other bergamottin sources is unclear. [Dr. Bailey was part of the Canadian research team that discovered grapefruit interactions with the blood pressure medicine felodipine (Lancet, Feb. 2, 1991). 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. Simvastatin is a substrate of cytochrome P450 3A4. Side effects of an interaction between statins and grapefruit include potentially fatal liver, kidney, ... (Lipitor®), simvastatin (Zocor®), and lovastatin (Mevacor®). Interactions involving inhibitors of CYP3A4. Clin Pharmacol Ther 1998;64:477-83. Not all statins have the same dangerous interaction with grapefruits. Further information about fruit/medicine interactions is available in Stockley's Drug Interactions. cyclosporine). There is hope if you really enjoy grapefruit. Yes. Am Fam Physician 2007;76(2):190, 92; author reply 92. Don't take these interactions lightly. 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). They informed me not to eat any grapefruit. It is taken by mouth. Simvastatin and the Grapefruit Connection came up today. Aliskiren. Grapefruit juice, which is widely consumed for its positive health benefits, can have severe, sometimes fatal, interactions with drugs. This time it was about Simvastatin. 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. As little as one grapefruit or one 8-ounce glass of grapefruit juice can cause an effect that may last more than 24 hours. For example, if a 20-mg dose is administered, only 1 mg reaches the systemic circulation. Severity of interaction: Moderate Evidence for interaction: Theoretical. Grapefruit juice–simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. “Our research group discovered the interaction between grapefruit and certain medications more than 20 years ago. the maximum recommended dose for simvastatin in conjunction with amlodipine or diltiazem is now 20 mg/day A full updated listing of all the interactions is provided in the table below. There was a marked interindividual variability in the grapefruit juice–simvastatin interaction, e.g. 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. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. In a randomized cross‐over study with two phases, 10 healthy volunteers ingested grapefruit juice 200 ml or water (control) for 3 days. 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. Although all statins may be affected by drug interactions, simvastatin is exceptionally sensitive for several reasons. Manufacturer advises avoid.

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