Drug therapy is indicated as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate. 80 mg. simvastatin acid. Can You Lower Your âBadâ Cholesterol Too Much? Xarelto is a blood-thinning drug approved to treat people with potential clotting problems, namely those at risk of, or already had, a heart attack, stroke, atrial fibrillation, or other problems. In patients with coronary heart disease (CHD) or at high risk of CHD, Simvastatin tablets can be started simultaneously with diet. Grapefruit juice and some drugs don't mix. Pravastatin is metabolized by yet a different mechanism. When this happens, the drug concentration can increase dramatically and, with it, the risk of side effects. Levels of simvastatin and lovastatin are 260 percent higher if taken with grapefruit juice, while the level of atorvastatin is 80 percent higher. Updated July 18, 2017. It is also used to decrease the risk of heart problems in those at high risk. Unfortunately, a compound in grapefruit known as bergamottin interferes with the enzymesneeded to metabolize certain statin drugs, including atorvastatin (Lipitor®), simvastatin (Zocor®), and lovastatin (Mevacor®). Of the seven statins approved for use in the United States, the drugs most affected by the consumption of grapefruit are: The abnormal accumulation of atorvastatin, lovastatin, or simvastatin in the blood can lead to potentially serious side effects, including: The risk can vary dramatically from one person to the next. A number of studies have suggested that side effects like these are uncommonï»¿ï»¿ and are mostly associated with a pre-existing kidney, liver, or neurologic condition. Changing lifelong eating habits can be scary at first, but our guide will make it easier. Grapefruit juice and some drugs don't mix. Simvastatin, sold under the brand name Zocor among others, is a lipid-lowering medication. Eating half a grapefruit is probably less risky because it contains a relatively small amount of juice but could still have an effect. Grapefruit increases the blood levels of three common statins substantially, increasing the risk of rhabdomyolysis : Atorvastatin (Lipitor) Lovastatin (Mevacor) Simvastatin (Zocor) Read about the pros and cons of using statins. of simvastatin was administered with grapefruit juice 200 ml or water. They also help your body reabsorb cholesterol thatâs already present in your artery walls. If you have been prescribed a statin drug to treat high cholesterol, your doctor or pharmacist may have advised you to avoid grapefruit or grapefruit juice while on treatment. Grapefruit juice decreases the activity of the cytochrome P450 3A4 (CYP3A4) enzymes that are responsible for breaking down many drugs and toxins. According to the Cleveland Clinic, there are instance when consuming moderate amounts of grapefruit appear to be safe. Limit your consumption of grapefruit or switch to "safe" citrus fruits, such as blood oranges, clementines, lemons, limes, mandarins, navel oranges, and tangerines. Dosing of Simvastatin. FDA Drug Safety Communication: New restrictions, contraindications, and dose limitations for Zocor (simvastatin) to reduce the risk of muscle injury AUC. The list includes tangelos, pomelos, bitter oranges, and Seville oranges. What other drugs interact with grapefruit? There is hope if you really enjoy grapefruit. The interaction is caused by an organic compound in grapefruit known as furanocoumarin.1ï»¿ Furanocoumarins are found in otâ¦ Contraindicated with ezetimibe and simvastatin tablets [see Contraindications and Warnings and Precautions ] Telithromycinâ 200 mg QD for 4 days. Some users have reported that they experienced memory loss while taking the medication. If the juice is taken 12 hours before these statins, the reductions are, respectively, 43% and 66%, and for atorvastatin, 42% and 66%. Simvastatin: Simvastatin, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) ... Avoid excessive consumption (>1 L/day) of grapefruit juice. Our website services, content, and products are for informational purposes only. 10â15 % risk of major event in 10 years), max. Is it time to say good night to your old pillow? 80 mg. Simvastatin acid â¡ Simvastatin . What to Know After Xarelto Lawsuit, The 10 Best Pillows for a Better Nightâs Sleep. Grapefruit and certain other citrus fruits, such as Seville oranges, can interfere with several kinds of prescription medications. There are other types of drugs that may be affected by grapefruit, too. Drinking too much alcohol may raise your chance of liver disease. Statins are prescription drugs used to lower cholesterol. Other drugs are equally affected by grapefruit and grapefruit juice. Researchers say the diuretic drug chlorthalidone, taken for high blood pressure, may produce low levels of potassium. Avoid the use of grapefruit products while taking this medicine. Thereâs the risk of increased side effects when mixing grapefruit with lovastatin, atorvastatin, or simvastatin. This doesnât mean that you have to avoid grapefruit altogether if youâre prescribed this medication. Pregnancy, ... Do not drink grapefruit juice while using this drug. New drugs used alongside statins can lower LDL cholesterol to really low levels, but do the risks outweigh the benefits? If you take any drugs (prescription or OTC, natural products, vitamins ) that must not be taken with ezetimibe and simvastatin, like certain drugs that are used for HIV , infections, or depression . Simvastatin is contraindicated in women who are or may become pregnant. 2017;25(1):71-83. doi:+10.1016/j.jfda.2016.11.008, Mcdonnell AM, Dang CH. It is taken by mouth. Furanocoumarins are organic chemical compounds present in many different plants, including grapefruit. Simvastatin â¦ What are the risks of mixing grapefruit and certain statins? The use of simvastatin with gemfibrozil is contraindicated (see section 4.3). These include:ï»¿ï»¿. Grapefruit juice (more than 1 quart per day) Avoid atorvastatin, lovastatin, and simvastatin 11 , 22 , 26 CYP3A4/organic anion transporting polypeptide inhibitors Thus, in the normal state, smaller amounts of the drugs get into the body than are ingested. According to the FDA, grapefruit might also affect your body if youâre taking allergy medication, such as fexofenadine (Allegra). Acute liver disease or unexplained persistent elevations of serum transaminases. In others, it can interfere with protein transporters in the blood, reducing the concentration and effect of the drug. The interaction is caused by an organic compound in grapefruit known as furanocoumarin.ï»¿ï»¿ Furanocoumarins are found in other fruits and vegetables (such as celery, parsnips, and pomegranates), but are especially high in grapefruit and grapefruit juice. For this reason, you might avoid the fruit altogether. Avoid eating foods that are high in fat or cholesterol. Increased plasma concentrations resulting to increased risk of myopathy and rhabdomyolysis with grapefruit juice. Most doctors will tell you that an occasional serving of juice or fruit will do you no harm. The changes recommended against using 80-mg doses of simvastatin, added 4 drugs to the list of contraindicated agents, and included several new simvastatin dose limitations when prescribed with drugs that inhibit its elimination. Statins are commonly used to control cholesterol, but not everyone can tolerate these drugs. Simvastatin is contraindicated in patients with active hepatic disease including cholestasis, hepatic encephalopathy, hepatitis, jaundice or unexplained persistent elevations in â¦ Can You Have Grapefruit Juice If You Take Plavix? Grapefruit and certain other citrus fruits, such as Seville oranges, can interfere with several kinds of prescription medications. However, have you heard that you shouldnât mix grapefruit and certain medications? Itâs rich in antioxidants, vitamins, and fiber. Dosing of Simvastatin. In addition to lowering "bad" LDL cholesterol and raising "good" HDL cholesterol, statin drugs can also decrease the level of triglyceridescirculating in your blood. Grapefruit is one of the healthiest citrus fruits you can eat. Chemistry and health effects of furanocoumarins in grapefruit, Basic review of the cytochrome p450 system. View abstract. Most incidents of negative reactions involved consuming large amounts of grapefruit. These drugs work by blocking a chemical called the HMG-CoA reductase, which is needed for the formation of cholesterol in the body. C max. It is also effective in reducing the risk of a second heart attack. For example, you might need to stop taking lovastatin, atorvastatin, or simvastatin, but you might be able to take fluvastatin, pitavastatin, pravastatin, or rosuvastatin to lower your cholesterol. Updated contraindications and ... We have previously communicated on the increased risk of myopathy associated with use of high-dose simvastatin ... Avoid grapefruit juice when taking simvastatin: Myopathy risk increases when statins are taken with medications known to inhibit their metabolism .11, 17, 18, 21 â 32 Serum levels of simvastatin and lovastatin are increased four- to â¦ Plasma con-centrations of simvastatin and simvastatin acid were determined up to 24 h. Results Grapefruit juice increased the area under the plasma concentrationâtime curves from 0 to 24 h [AUC(0â24)] of simvastatin 3.6-fold (range 1.8â6.0-fold; P < 0.01) and The effect of grapefruit juice on some drugs may last longer than 24 hours and avoiding drinking any grapefruit juice is wise advice. The problem with furanocoumarins is that they deactivate a kidney enzyme known as cytochrome P4503A4 (CYP3A4),ï»¿ï»¿ which the body uses to break down certain drugs so that they can be excreted from the body. Some can cause potentially dangerous health problems. Keep in mind that both fresh and frozen juices have the same effect. Statins are known to be highly effective in preventing heart disease but there have been concerns over side effects. âThis is an issue only for lovastatin and simvastatin and is only problematic at the highest dosages,â says Dr. Nissen, Cardiovascular Medicine Department Chair at Cleveland Clinicâs Heart and Vascular Institute. As far as natural alternatives to chemical ingredients go, capric acid and caprylic triglyceride is one of the cleanest ingredients that you can findâ¦. History. J Food Drug Anal. January 20, 2016. Statins and Memory Loss: Is There a Link? (generic name: atorvastatin) has been an extremely effective medication in lowering cholesterol and reducing the risk of heart attack and stroke. The problem with furanocoumarins is that they deactivate a kidney enzyme known as cytochrome P4503A4 (CYP3A4), ï»¿ ï»¿ which the body uses to break down certain drugs so that they can be excreted from the To be safe, check with your doctor if you take one of the three statins mentioned above. Among other warnings, this page covers the safety of taking simvastatin if you are pregnant or nursing, or drink alcohol or grapefruit juice often. They include: Everyone with high cholesterol doesnât need to take statins. At present, no one really knows where the "safe" line is. Geometric Mean Ratio (Ratio* with/without coadministered drug) No Effect = 1. Speak with your doctor or pharmacist if you regularly consume grapefruit to ensure that it doesn't interfere with your medications. Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. C max. 200 mg QD for 4 days. Basic review of the cytochrome p450 system. Learn the facts. Drugs and food that interact with statins. The fruit doesnât affect all statins. AUC. Atorvastatin interacts with grapefruit juice if you drink large quantities (more than 1.2 litres daily), but an occasional glass is thought to be safe. Q: I've heard that people shouldn't drink grapefruit juice if they're taking a statin. Examples of common medications that interact with grapefruit juice include certain statin cholesterol drugs such as atorvastatin (Lipitor), lovastatin, simvastatin (Zocor), felodipine (Plendil) and other calcium channel blockers, clarithromycin (Biaxin), and loratadine (Claritin). However, some other statins do not seem to be affected by grapefruit juice, including pravastatin (Pravachol), fluvastatin (Lescol) and rosuvastatin (Crestor). How much grapefruit is ok while on certain statins? A number of other medications also shouldnât be taken with grapefruit. WebMD provides common contraindications for Simvastatin Oral. Do not exceed 20 mg simvastatin daily Grapefruit juice ; Avoid grapefruit juice â¢ Other Lipid-lowering Medications: Use with other fibrate products or lipid-modifying doses (â¥1 g/day) of niacin increases the risk of adverse skeletal muscle effects. Do your statins and grapefruit safely mix? Find out what health conditions may be a health risk when taken with Simvastatin Oral Simvastatin, a prodrug, is converted to its active metabolite simvastatin acid ... Contraindications . Switch to oranges or other safe fruits and save grapefruit for special occasions. Contraindications . Written by the Healthline Editorial Team, How grapefruit interacts with certain statins. By using Verywell Health, you accept our, Learn About Taking Lipitor or Zocor With Grapefruit Juice. The FDA recommends that people taking statins should avoid consuming more than a quart (946 ml) of grapefruit juice per day. Women and people ages 65 and older are at a higher risk of developing side effects from these statins. If you use a skin patch or receive your medication through an injection, you may have a lower risk of adverse effects. You only need to avoid grapefruit if your doctor prescribes lovastatin, atorvastatin, or simvastatin. Grapefruit has many health benefits but can be dangerous if combined with certain medications. TABLE 3:Effect of Coadministered Drugs or Grapefruit Juice on Simvastatin Systemic Exposure. Concomitant intake of large quantities (over 1 litre daily) of grapefruit juice and simvastatin resulted in a 7-fold increase in exposure to simvastatin acid. How this translates to the "safe" consumption of grapefruit remains unclear. Effects of Grapefruit Juice Consumption on Pharmacokinetics of Low Dose Simvastatin: Cross-over Study with a Review of the Literature. Hydantoins: (Moderate) Hydantoin anticonvulsants induce hepatic microsomal enzymes and may increase the metabolism of other drugs, such as simvastatin, leading to reduced efficacy of simvastatin. Both Red and White Meat Raise Cholesterol Levels, Study Finds. Don't take these interactions lightly. Intake of 240 ml of grapefruit juice in the morning and simvastatin in the evening also resulted in a 1.9-fold increase. This compound deactivates the CYP3A4 enzyme that the body uses to metabolize, or process, these particular statins. This is because the two drugs are broken down by an entirely different enzyme known as CYP2C9.