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Ezetimibe and grapefruit juice: Does grapefruit affect my medicine?

Does grapefruit affect my medicine?

Eating grapefruit or drinking grapefruit juice can affect some medicines. In most cases, it increases the level of the medicine in your blood. This can increase the risk of side effects or alter the effect the medicine has.

If your usual diet includes grapefruit or grapefruit juice and you’ve been prescribed a medicine that’s affected by grapefruit, speak to your GP or pharmacist. Do not stop taking your medication without advice.

Some medicines affected by grapefruit are listed below, although there may be others that are not mentioned.

Medicines affected by grapefruit

Statins

Statins are medicines that lower your cholesterol. Grapefruit or grapefruit juice affects some statins.

Do not drink grapefruit juice if you’re taking simvastatin. Grapefruit juice increases the level of simvastatin in your blood and makes side effects more likely.

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.

Currently, healthcare professionals advise it is safe to drink grapefruit juice and eat grapefruit if you’re taking other types of statins.

Calcium channel blockers

Calcium channel blockers are medicines that relax the muscles that make up the walls of your arteries. They’re used as part of the treatment of conditions such as high blood pressure (hypertension) and coronary heart disease.

Grapefruit juice interacts with some calcium channel blockers and increases the level of the medicine in your blood. If you’re taking any of the medicines below, seek advice from your pharmacist or doctor if you wish to include grapefruit or grapefruit juice in your diet.

  • amlodipine
  • felodipine
  • isradipine
  • lacidipine
  • lercanidipine
  • nicardipine
  • nifedipine
  • nimodipine
  • verapamil

Grapefruit juice does not affect diltiazem.

Ciclosporin and immunosuppressants

Ciclosporin, sirolimus and tacrolimus are medicines that moderate your immune system (the body’s natural defence system).

If you’re taking any of these medicines, do not drink grapefruit juice without consulting your doctor.

Entocort

Entocort is a medicine that contains budesonide and is used to treat Crohn’s disease, a condition that affects the digestive system.

Do not eat grapefruit or drink grapefruit juice while you’re taking this medicine, as the level of budesonide in your blood will increase.

Cytotoxic medicines

Some medicines used in the treatment of cancers may interact with grapefruit juice. You should check with your doctor before drinking grapefruit juice.

This list is not exhaustive and there are a number of other drugs that may interact with grapefruit. The risk of experiencing the effect of a drug interaction as a result of grapefruit can vary a lot from person to person.

For more information check the patient information leaflet that comes with your medicine, or you can ask your pharmacist or GP or call NHS 111 for advice.

Read the answers to more questions about medicines.

Ezetimibe-Simvastatin | PeaceHealth

Drug Information

Common brand names:

Vytorin

Summary of Interactions with Vitamins, Herbs, & Foods

Types of interactions:
Beneficial
Adverse
Check

Replenish Depleted Nutrients

  • Coenzyme Q10

    In a group of patients beginning treatment with atorvastatin, the average concentration of coenzyme Q10 in blood plasma decreased within 14 days, and had fallen by approximately 50% after 30 days of treatment. Many doctors recommend CoQ10 supplementation to prevent the drug-induced decline in CoQ10 levels.

Reduce Side Effects

  • Coenzyme Q10

    In a preliminary study, supplementation with 100 mg of CoQ10 per day reduced the severity of muscle pain by 40% in people with muscle pain caused by a statin drug. A double-blind trial also found that CoQ10 (200 mg per day) significantly decreased drug-induced muscle symptoms in people taking statin drugs.

    However, in another double-blind trial, CoQ10 in the amount of 60 mg twice a day for one month was not more effective than a placebo for relieving muscle pain. Although the evidence is conflicting regarding whether supplementing with CoQ10 relieves statin-induced muscle symptoms, many doctors recommend CoQ10 supplementation to prevent the drug-induced decline in CoQ10 levels.

  • Creatine Monohydrate

    In a preliminary study, ten patients who had to discontinue statin drugs because of muscle-related side effects were given creatine (as creatine monohydrate) in the amount of 5 grams twice a day for five days, then 5 grams per day. Eight of the ten patients experienced no muscle symptoms upon resuming the statin drug.

  • Vitamin D

    In a preliminary trial, supplementation with vitamin D appeared to prevent muscle-related side effects in patients taking statin drugs. The amount of vitamin D used in this study was very large (up to 50,000 IU twice a week) and potentially toxic. People taking statin drugs should consult with their doctor regarding how much vitamin D can be taken.

  • Vitamin E

    Oxidative damage to LDL (“bad”) cholesterol is widely believed to contribute to heart disease. In a double-blind trial, lovastatin was found to increase oxidative damage to LDL cholesterol and vitamin E was reported to protect against such damage, though not to completely overcome the negative effect of lovastatin. This study suggests that people taking lovastatin might benefit from supplemental vitamin E.

Support Medicine

  • Fish Oil

    In a preliminary trial, taking an HMG-CoA reductase inhibitor (“statin”) for about three years significantly lowered triglyceride levels and raised levels of HDL (“good”) cholesterol in people with high cholesterol who had also been supplementing with either 900 mg or 1,800 mg of EPA for three months. The authors of the study concluded that the combination of the statin and EPA may prevent coronary heart disease better than the drug alone. Since drugs in the statin family have similar mechanisms of action, people taking any statin drug may benefit from fish oil.

  • Psyllium

    In one study, supplementation with 15 grams of psyllium per day for eight weeks enhanced the cholesterol-lowering effect of simvastatin.

  • Sitostanol

    A synthetic molecule related to beta-sitosterol, sitostanol, is available in a special margarine and has been shown to lower cholesterol levels. In one study, supplementing with 1.8 grams of sitostanol per day for six weeks enhanced the cholesterol-lowering effect of various statin drugs.

Reduces Effectiveness

  • Magnesium

    A magnesium- and aluminum-containing antacid was reported to interfere with atorvastatin absorption. People can avoid this interaction by taking atorvastatin two hours before or after any aluminum/magnesium-containing antacids. Some magnesium supplements such as magnesium hydroxide are also antacids.

  • St. John’s Wort

    In patients taking simvastatin, treatment with St. John’s wort increased serum cholesterol levels, apparently because St. John’s wort interfered with the effect of the medication.

Potential Negative Interaction

  • Grapefruit

    Grapefruit contains substances that may inhibit the body’s ability to break down simvastatin; consuming grapefruit or grapefruit juice might therefore increase the potential toxicity of the drug. In a study of healthy volunteers, ingesting 200 ml of grapefruit juice along with simvastatin increased blood levels of the drug, compared with taking simvastatin with water. There is one case report of a woman developing severe muscle damage from simvastatin after she began eating one grapefruit per day. Although there have been no reports of a grapefruit–simvastatin interaction, to be on the safe side, people taking simvastatin should not eat grapefruit or drink grapefruit juice.

  • Antioxidants

    In another study, daily supplementation with a combination of antioxidants (800 IU of vitamin E, 1,000 mg of vitamin C, 25 mg of beta-carotene, and 100 mcg of selenium) blocked the beneficial effect of simvastatin-plus-niacin on HDL cholesterol levels. Although there is evidence that some or all of these nutrients may help prevent heart disease, individuals taking simvastatin who wish to take antioxidants should discuss the use of these supplements with their doctor.

    The interaction is supported by preliminary, weak, fragmentary, and/or contradictory scientific evidence.

  • Pomegranate

    Pomegranate juice has been shown to inhibit the same enzyme that is inhibited by grapefruit juice. The degree of inhibition is about the same for each of these juices. Therefore, it would be reasonable to expect that pomegranate juice might interact with simvastatin in the same way that grapefruit juice does.

    The interaction is supported by preliminary, weak, fragmentary, and/or contradictory scientific evidence.

  • Red Yeast Rice

    A supplement containing red yeast rice (Cholestin) has been shown to effectively lower cholesterol and triglycerides in people with moderately elevated levels of these blood lipids. This extract contains small amounts of naturally occurring HMG-CoA reductase inhibitors such as lovastatin and should not be used if you are currently taking a statin medication.

    The interaction is supported by preliminary, weak, fragmentary, and/or contradictory scientific evidence.

Explanation Required 

  • Vitamin B3 (Niacin)

    Niacin is the form of vitamin B3 used to lower cholesterol. Taking large amounts of niacin along with HMG-CoA reductase inhibitors may cause muscle disorders (myopathy) that can become serious (rhabdomyolysis). Such problems appear to be uncommon. Moreover, concurrent use of niacin has been reported to enhance the cholesterol-lowering effect of HMG-CoA reductase inhibitors. Individuals taking simvastatin should consult a doctor before taking niacin.

  • Vitamin A

    A study of 37 people with high cholesterol treated with diet and HMG-CoA reductase inhibitors found blood vitamin A levels increased over two years of therapy. Until more is known, people taking HMG-CoA reductase inhibitors, including simvastatin, should have blood levels of vitamin A monitored if they intend to supplement vitamin A.

    The interaction is supported by preliminary, weak, fragmentary, and/or contradictory scientific evidence.

  • Vitamin E

    In a study of seven patients with hypercholesterolemia, eight weeks of simvastatin plus vitamin E 300 IU improved markers of blood vessel elasticity more than simvastatin alone.

    The interaction is supported by preliminary, weak, fragmentary, and/or contradictory scientific evidence.

The Drug-Nutrient Interactions table may not include every possible interaction. Taking medicines with meals, on an empty stomach, or with alcohol may influence their effects. For details, refer to the manufacturers’ package information as these are not covered in this table. If you take medications, always discuss the potential risks and benefits of adding a new supplement with your doctor or pharmacist.

Ezetimibe; Simvastatin tablets

Brand Name: Vytorin

What is this medicine?

EZETIMIBE; SIMVASTATIN (ez ET i mibe; SIM va stat in) blocks the body’s ability to absorb and make cholesterol. It is used to lower cholesterol. It is only for patients whose cholesterol level is not controlled by diet.


How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take this medicine in the evening with or without food. Take your doses at regular intervals. Do not take your medicine more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 10 years, precautions do apply.


What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:

  • allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
  • confusion
  • dark yellow or brown urine
  • depression
  • fever
  • loss of memory
  • muscle pain, tenderness, cramps, or weakness
  • redness, blistering, peeling or loosening of the skin, including inside the mouth
  • signs and symptoms of high blood sugar such as being more thirsty or hungry or having to urinate more than normal. You may also feel very tired or have blurry vision.
  • trouble passing urine or change in the amount of urine
  • unusually weak
  • yellowing of the skin or eyes

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

  • constipation
  • gas
  • headache
  • heartburn
  • indigestion
  • stomach pain


What may interact with this medicine?

Do not take this medicine with any of the following:

  • antiviral medicines for HIV or AIDS
  • certain antibiotics like clarithromycin, erythromycin, telithromycin
  • certain medicines for fungal infections like ketoconazole, itraconazole, posaconazole, voriconazole
  • conivaptan
  • cyclosporine
  • danazol
  • gemfibrozil
  • idelalisib
  • mifepristone, RU-486
  • nefazodone
  • supplements like red yeast rice

This medicine may also interact with the following medications:

  • alcohol
  • certain medicines for blood pressure or heart disease like amlodipine, diltiazem, verapamil
  • certain medicines for irregular heart beat like amiodarone and dronedarone
  • certain medicines that treat or prevent blood clots like warfarin
  • colchicine
  • digoxin
  • grapefruit juice
  • lomitapide
  • niacin
  • ranolazine


What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.


Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.


What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:

  • diabetes
  • frequently drink alcoholic beverages
  • kidney or liver disease
  • muscle aches or weakness
  • an unusual or allergic reaction to ezetimibe, simvastatin, other medicines, foods, dyes, or preservatives
  • pregnant or trying to get pregnant
  • breast-feeding


What should I watch for while using this medicine?

Visit your doctor or healthcare provider for regular check-ups. You may need regular tests to make sure your liver is working properly.

Tell your doctor or healthcare provider right away if you get any unexplained muscle pain, tenderness, or weakness, especially if you also have a fever and tiredness. Your doctor or healthcare provider may tell you to stop taking this medicine if you develop muscle problems. If your muscle problems do not go away after stopping this medicine, contact your health care professional.

This medicine may increase blood sugar. Ask your healthcare provider if changes in diet or medicines are needed if you have diabetes.

This drug is only part of a total heart-health program. Your doctor or a dietician can suggest a low-cholesterol and low-fat diet to help. Avoid alcohol and smoking, and keep a proper exercise schedule.

Do not use this drug if you are pregnant or breast-feeding. Serious side effects to an unborn child or to an infant are possible. Talk to your doctor or pharmacist for more information.

If you are going to have surgery tell your healthcare provider that you are taking this drug.

Some drugs may increase the risk of side effects from this medicine. If you are given certain antibiotics or antifungals, your doctor or healthcare provider may stop this medicine for a short time. Check with your doctor or pharmacist for advice.

This medicine may cause a decrease in Co-Enzyme Q-10. You should make sure that you get enough Co-Enzyme Q-10 while you are taking this medicine. Discuss the foods you eat and the vitamins you take with your healthcare provider.


NOTE:This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider. Copyright© 2020 Elsevier

6.11: Antilipemics – Medicine LibreTexts

Antilipemic agents reduce hyperlipidemia that may lead to additional health problems such as stroke, myocardial infarction, angina, and heart failure. Medications should be used in adjunct with a healthy diet and exercise regime approved by the patient’s health care provider.

Atorvastatin

Mechanism of Action

Atorvastatin inhibits HMG-CoA reductase and cholesterol synthesis, which reduces LDL (low density lipoprotein).

Indications for Use

This medication is used for hyperlipidemia and the prevention of cardiovascular disease.

Nursing Considerations Across the Lifespan

Do not use with patients who have hepatic disease.

This medication is contraindicated with patients who are pregnant or breastfeeding. Do not give to patients under 10 years of age.

Use caution with geriatric patients due to increased risk for myopathy.

Adverse/Side Effects

Patients who are pregnant or breastfeeding should not take this medication. A health care provider will assess routine liver function for a patient taking atorvastatin. Nausea, diarrhea, dyspepsia, increase in blood glucose, rhabdomyolysis, myalgia, or muscle spasms may be produced by taking this medication. Rhabdomyolysis is a condition in which damaged skeletal muscle breaks down rapidly, causing muscle pain and weakness. Some of the muscle breakdown products are harmful to the kidneys and can cause kidney failure. There may be tea-colored urine or an irregular heartbeat with rhabdomyolysis.

Patient Teaching & Education

Patients should take the prescribed medication as directed and avoid consuming grapefruit juice during drug therapy. The medication should be used with dietary modifications. If the patient experiences muscle pain, tenderness, or weakness, these should be reported to the healthcare provider.

Now let’s take a closer look at the medication grid on atrovastatin in Table 6.11a.

Table 6:11a Atorvastatin Medication Grid
Class/

Subclass

Prototype-

generic

Administration Considerations Therapeutic Effects Adverse/Side Effects
HMG-CoA Reductase Inhibitors atorvastatin Take at the same time each day, with or without food

Report muscle weakness, feeling tired, abdominal pain, or yellowing of skin or eyes

Reduce LDL Rhabdomyolysis, myalgia, and muscle spasms

Abnormal liver enzymes

May increase blood glucose

Nausea, diarrhea, and dyspepsia

Ezetimibe

Mechanism of Action

Ezetimibe blocks the absorption of cholesterol in the small intestines to reduce LDL.

Indications for Use

This medication is used for treatment of hyperlipidemia and familial hypercholesterolemia.

Nursing Considerations Across the Lifespan

If medication is combined with HMG-CoA reductase inhibitors, do not give to pregnant or breastfeeding patients.

Adverse/Side Effects

Use with caution when ezetimibe is combined with additional medication. Patients may experience arthralgia, rhabdomyolysis, hepatic impairment, dizziness, upper respiratory infections, or diarrhea if they are taking this medication. Minimal side effects were reported with monotherapy.

Patient Teaching & Education

Patients should take the prescribed medication as directed and avoid consuming grapefruit juice during drug therapy. The medication should be used with dietary modifications. If the patient experiences muscle pain, tenderness, or weakness, this should be reported to the healthcare provider.

Now let’s take a closer look at the medication grid for ezetimibe in Table 6.11b.

Table 6:11b Ezetimibe Medication Grid
Class/

Subclass

Prototype-

generic

Administration

Considerations

Therapeutic Effects Adverse/Side Effects
Cholesterol Absorption Inhibitor ezetimibe Take at the same time each day, with or without food

Report muscle weakness, feeling tired, abdominal pain, or yellowing of skin or eyes

Reduce LDL Arthralgia, rhabdomyolysis

Hepatic impairment

Dizziness

Upper respiratory infection

Diarrhea

Ezetimibe/Simvastatin, Oral – Tufts Medical Center Community Care

What are other names for this medicine?

Type of medicine: cholesterol lowering medicine

Generic and brand names: ezetimibe/simvastatin, oral; Vytorin

What is this medicine used for?

This medicine is taken by mouth to lower levels of total cholesterol, LDL (bad) cholesterol, and triglycerides in the blood. It also helps to increase the amount of HDL (good) cholesterol in your blood. It is used when you cannot control your cholesterol levels by diet and exercise alone.

High doses of this medicine should only be used by people who have been taking it for 12 months or longer without ill effect.

This medicine may be used to treat other conditions as determined by your healthcare provider.

What should my healthcare provider know before I take this medicine?

Tell your healthcare provider if you have ever had:

  • An allergic reaction to any medicine
  • Diabetes
  • Liver or kidney problems
  • Low blood pressure
  • Problems with alcohol abuse
  • Thyroid problems
  • Unexplained muscle pain or weakness
  • Seizures

Tell your healthcare provider about all the medicines you are taking. Taking certain medicines or foods with this medicine may increase your risk of serious muscle problems. These medicines include certain antifungals and antibiotics, HIV protease inhibitors, certain hepatitis C virus protease inhibitors, nefazodone, gemfibrozil, cyclosporine, and danazol. Do not start any new medicines, supplements, or natural remedies while you are taking this medicine unless your healthcare provider approves.

Females of childbearing age: Do not take this medicine if you are pregnant. This medicine has been reported to cause birth defects. Stop taking this medicine at the first sign that you may be pregnant and contact your healthcare provider right away. Talk with your healthcare provider about effective forms of birth control. Do not breast-feed while taking this medicine.

How do I take it?

Check the label on the medicine for directions about your specific dose. Take this medicine exactly as your healthcare provider prescribes for the length of time prescribed. Do not stop taking this medicine without your healthcare provider’s approval. This medicine will lower your cholesterol level only when you take it regularly. Continue to follow the diet or exercise program your healthcare provider prescribes.

Check with your healthcare provider before using this medicine in children under age 10 or in children who have not reached puberty.

You may take this medicine with or without food. Taking it with meals may lessen the chance the drug will upset your stomach.

If your healthcare provider has also prescribed a another cholesterol lowering medicine such as Colestid, Questran, or WelChol, take this medicine (ezetimibe/simvastatin) at least 2 hours before or at least 4 hours after taking the other medicine.

What if I miss a dose?

If you miss a dose of this medicine, take the missed dose as soon as you remember that same day. If you do not remember until the next day, skip the missed dose. Do not take double doses. If you are not sure of what to do if you miss a dose or you miss more than one dose, contact your healthcare provider.

What if I overdose?

An acute overdose of this medicine is not likely to cause life-threatening symptoms. If you think that you or anyone else may have taken too much of this medicine, call the poison control center at 800-222-1222.

What should I watch out for?

While you are taking this medicine, report any unusual muscle pain, tenderness, or weakness to your healthcare provider right away, especially if you also have a fever or feel ill.

You will need regular blood tests to see if the medicine is working. You will also have liver function tests to see how the medicine may be affecting your liver. Keep all your appointments.

This medicine may make you dizzy or drowsy. Do not drive or operate machinery unless you are fully alert.

Adults over the age of 65 may be at greater risk for side effects.

If you need emergency care, surgery, lab tests, or dental work, tell the healthcare provider or dentist you are taking this medicine.

A low-fat diet and regular exercise are important to reduce cholesterol. Follow your healthcare provider’s advice. Because alcohol may increase triglyceride levels, do not drink alcohol while you are taking this medicine unless your healthcare provider approves.

What are the possible side effects?

Along with its needed effects, your medicine may cause some unwanted side effects. Some side effects may be very serious. Some side effects may go away as your body adjusts to the medicine. Tell your healthcare provider if you have any side effects that continue or get worse.

Life-threatening (Report these to your healthcare provider right away. If you cannot reach your healthcare provider right away, get emergency medical care or call 911 for help.): Allergic reaction (hives; itching; rash; trouble breathing; tightness in your chest; swelling of your lips, tongue, and throat).

Serious (report these to your healthcare provider right away): Chest pain; unusual muscle pain, tenderness, or weakness, especially if you also have a fever or feel more tired than usual; yellowing of your skin or eyes, dark or reddish urine, light colored bowel movements; severe nausea or vomiting; severe stomach pain; unexplained loss of appetite; unusual tiredness or weakness; trouble or decreased urinating.

Other: Nausea, vomiting, diarrhea, abdominal pain, gas, constipation, mild rash or itching, headache, dizziness, memory loss, confusion, tingling, stuffy or runny nose, constant cough, tiredness, trouble sleeping, erectile dysfunction.

What products might interact with this medicine?

When you take this medicine with other medicines, it can change the way this or any of the other medicines work. Nonprescription medicines, vitamins, natural remedies, and certain foods may also interact. Using these products together might cause harmful side effects. Talk to your healthcare provider if you are taking:

  • Antacids containing aluminum, magnesium, or calcium such as Maalox, Mylanta, or Tums (Take antacids 2 hours apart from doses of this medicine.)
  • Antibiotics such as chloramphenicol, clarithromycin (Biaxin), daptomycin (Cubicin), erythromycin (Ery-Tabs, E.E.S.), norfloxacin (Noroxin), rifampin (Rifadin), rifapentine (Priftin), rifabutin (Mycobutin), tetracycline, and telithromycin (Ketek)
  • Antidepressant medicines such as desipramine and nefazodone
  • Antifungals such as fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral), posaconazole (Noxafil), and voriconazole (VFEND)
  • Anti-HIV medicines such as atazanavir (Reyataz), darunavir (Prezista), delavirdine (Rescriptor), efavirenz (Sustiva), elvitegravir/cobicistat/emtricitabine/tenofovir (Stribild), indinavir (Crixivan), lopinavir/ritonavir (Kaletra), nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir), saquinavir (Invirase), and tipranavir (Aptivus)
  • Antipsychotic medicines such as aripiprazole (Abilify), haloperidol (Haldol), and risperidone
  • Antiseizure medicines such as carbamazepine (Tegretol, Carbatrol), fosphenytoin (Cerebyx), oxcarbazepine (Trileptal), primidone (Mysoline), phenobarbital, and phenytoin (Dilantin)
  • Antiviral medicines such as boceprevir (Victrelis) and telaprevir (Incivek)
  • Aprepitant (Emend)
  • Bosentan (Tracleer)
  • Colchicine (Colcrys)
  • Conivaptan (Vaprisol)
  • Cyclosporine (Sandimmune, Gengraf, Neoral)
  • Danazol
  • Dexamethasone
  • Eltrombopag (Promacta)
  • Heart medicines such as amiodarone (Cordarone, Pacerone), amlodipine (Norvasc), digoxin (Lanoxin), diltiazem (Cardizem, Dilacor), dronedarone (Multaq), nicardipine (Cardene, Cardene SR), quinidine, ranolazine (Ranexa), and verapamil (Calan, Covera, Isoptin)
  • Levothyroxine (Synthroid)
  • Medicines to treat cancer such as abiraterone (Zytiga), bosutinib (Bosulif), crizotinib (Xalkori), dasatinib (Sprycel), enzalutamide (Xtandi), erlotinib (Tarceva), imatinib (Gleevec), and mitotane (Lysodren)
  • Medicines to treat or reduce the chance of blood clots forming such as ticagrelor (Brilinta) and warfarin (Coumadin)
  • Medicine to treat stomach acid such as cimetidine (Tagamet), dexlansoprazole (Dexilant), esomeprazole (Nexium), and omeprazole (Prilosec)
  • Natural remedies such as green tea, red yeast rice, and St. John’s wort
  • Other cholesterol medicines such as cholestyramine (Questran, Prevalite), colesevelam (WelChol), and colestipol (Colestid) (Take this medicine 2 hours before or 4 hours after you take cholestyramine, colesevelam, or colestipol.)
  • Other cholesterol medicines such as fenofibrate (Antara, TriCor), gemfibrozil (Lopid), lomitapide (Juxtapid), and niacin (Niacor, Niaspan, Slo-Niacin, nicotinic acid) or niacin-containing products
  • Quinine
  • Sildenafil (Revatio, Viagra)

Do not eat grapefruit or drink grapefruit juice while taking this medicine. Grapefruit affects the way this medicine works and may increase the risk of side effects.

If you are not sure if your medicines might interact, ask your pharmacist or healthcare provider. Keep a list of all your medicines with you. List all the prescription medicines, nonprescription medicines, supplements, natural remedies, and vitamins that you take. Be sure that you tell all healthcare providers who treat you about all the products you are taking.

How should I store this medicine?

Store this medicine at room temperature. Keep the container tightly closed. Protect it from heat, high humidity, and bright light.


This advisory includes selected information only and may not include all side effects of this medicine or interactions with other medicines. Ask your healthcare provider or pharmacist for more information or if you have any questions.

Keep all medicines out of the reach of children.

Do not share medicines with other people.

Developed by RelayHealth.

This content is reviewed periodically and is subject to change as new health information becomes available. The information is intended to inform and educate and is not a replacement for medical evaluation, advice, diagnosis or treatment by a healthcare professional.

Copyright ©1986-2015 McKesson Corporation and/or one of its subsidiaries. All rights reserved.

Ezetimibe and Simvastatin: Dosage, Mechanism/Onset of Action, Half-Life

Drug Interactions

Acipimox: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Monitor therapy

Amiodarone: May increase the serum concentration of Simvastatin. Management: Consider using a non-interacting statin (pravastatin) in patients on amiodarone. If combined, limit the adult simvastatin dose to 20 mg daily and monitor for evidence of simvastatin toxicities (eg, myalgia, liver function test elevations, rhabdomyolysis). Consider therapy modification

AmLODIPine: May increase the serum concentration of Simvastatin. Management: Avoid the concurrent use of amlodipine with simvastatin when possible. If used together, avoid doses of simvastatin greater than 20 mg/day (for adults). Consider therapy modification

Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Asunaprevir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Monitor therapy

Azithromycin (Systemic): May enhance the myopathic (rhabdomyolysis) effect of Simvastatin. Monitor therapy

Bezafibrate: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Avoid combination

Bile Acid Sequestrants: May decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Consider therapy modification

Bosentan: May decrease the serum concentration of Simvastatin. Monitor therapy

Cilostazol: May increase the serum concentration of Simvastatin. Monitor therapy

Ciprofibrate: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Management: Avoid the use of HMG-CoA reductase inhibitors and ciprofibrate if possible. If concomitant therapy is considered, benefits should be carefully weighed against the risks, and patients should be monitored closely for signs/symptoms of muscle toxicity. Consider therapy modification

Clarithromycin: May increase the serum concentration of Simvastatin. Avoid combination

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Colchicine: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Colchicine may increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Consider therapy modification

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

CycloSPORINE (Systemic): May increase the serum concentration of Simvastatin. Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Simvastatin. Avoid combination

Cyproterone: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Avoid use of statins metabolized by CYP3A4 (eg, simvastatin) and consider avoiding fluvastatin as well in patients receiving high dose cyproterone (300 mg/day). Consider use of pravastatin, rosuvastatin, or pitavastatin if statin therapy is needed. Consider therapy modification

Dabigatran Etexilate: Simvastatin may enhance the anticoagulant effect of Dabigatran Etexilate. Monitor therapy

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Daclatasvir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Monitor therapy

Danazol: May increase the serum concentration of Simvastatin. Avoid combination

DAPTOmycin: Simvastatin may enhance the adverse/toxic effect of DAPTOmycin. Avoid combination

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

DilTIAZem: Simvastatin may increase the serum concentration of DilTIAZem. DilTIAZem may increase the serum concentration of Simvastatin. Management: Avoid concurrent use of diltiazem with simvastatin when possible. If used together, limit adult doses to simvastatin 10 mg/day and diltiazem 240 mg/day; avoid Simcor (simvastatin/niacin) because fixed simvastatin doses exceed the maximum. Consider therapy modification

Dronedarone: May increase the serum concentration of Simvastatin. Management: Limit simvastatin to a max of 10 mg/day (in adults). Increase monitoring for signs of simvastatin toxicity (e.g., myositis, rhabdomyolysis). Consider therapy modification

Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Efavirenz: May decrease the serum concentration of Simvastatin. Monitor therapy

Elbasvir: May increase the serum concentration of Simvastatin. Monitor therapy

Eltrombopag: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates. Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Erythromycin (Systemic): May increase the serum concentration of Simvastatin. Avoid combination

Eslicarbazepine: May decrease the serum concentration of Simvastatin. Monitor therapy

Etravirine: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). This applies to atorvastatin, lovastatin and simvastatin. Monitor therapy

Fenofibrate and Derivatives: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Monitor therapy

Fluconazole: May increase the serum concentration of Simvastatin. Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosphenytoin: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Consider therapy modification

Fostamatinib: May increase the serum concentration of Simvastatin. Monitor therapy

Fusidic Acid (Systemic): May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk for muscle toxicities, including rhabdomyolysis may be significantly increased. Management: Avoid concurrent use whenever possible. Use is listed as contraindicated in product characteristic summaries in several countries, although UK labeling suggests that use could be considered under exceptional circumstances and with close supervision. Avoid combination

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Gemfibrozil: May enhance the myopathic (rhabdomyolysis) effect of Simvastatin. Gemfibrozil may increase the serum concentration of Simvastatin. Concentrations of the active simvastatin acid metabolite may also be increased by gemfibrozil. Avoid combination

Gemfibrozil: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Gemfibrozil may increase the serum concentration of Ezetimibe. Avoid combination

Glecaprevir and Pibrentasvir: May increase the serum concentration of Simvastatin. Avoid combination

Grapefruit Juice: May increase the serum concentration of Simvastatin. Avoid combination

Grazoprevir: May increase the serum concentration of Simvastatin. Monitor therapy

Green Tea: May increase the serum concentration of Simvastatin. Specifically, Simvastatin lactone concentrations may be increased. Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Imatinib: May decrease the metabolism of Simvastatin. Monitor therapy

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Lanthanum: HMG-CoA Reductase Inhibitors (Statins) may decrease the serum concentration of Lanthanum. Management: Administer HMG-CoA reductase inhibitors at least two hours before or after lanthanum. Consider therapy modification

Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Lercanidipine: May increase the serum concentration of Simvastatin. Management: Administer lercanidipine in the morning and simvastatin in the evening in patients receiving these drugs in combination. Consider therapy modification

Letermovir: May increase the serum concentration of Simvastatin. Avoid combination

Levamlodipine: May increase the serum concentration of Simvastatin. Management: Avoid the concurrent use of amlodipine with simvastatin when possible. If used together, avoid doses of simvastatin greater than 20 mg/day (for adults). Consider therapy modification

Lomitapide: May increase the serum concentration of Simvastatin. Management: Reduce the recommended simvastatin dose by 50%. Generally, limit the maximum adult simvastatin dose to 20 mg/day. A 40 mg/day dose can be considered in patients who previously received 80 mg/day for at least a year without evidence of muscle toxicity. Consider therapy modification

Lorlatinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. Consider therapy modification

MiFEPRIStone: May increase the serum concentration of Simvastatin. Management: Avoid simvastatin during and 2 weeks following mifepristone for treatment of hyperglycemia in Cushing’s syndrome. The interaction magnitude could be lower with single doses used to terminate pregnancy, but neither effect has been studied clinically. Avoid combination

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Niacin: May enhance the myopathic (rhabdomyolysis) effect of Simvastatin. Niacin may increase the serum concentration of Simvastatin. Management: Use of simvastatin with niacin should be avoided in Chinese patients; some non-US labeling state this combination is not recommended in any Asian patients. Consider therapy modification

Niacinamide: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

PAZOPanib: Simvastatin may enhance the adverse/toxic effect of PAZOPanib. Specifically, the risk for ALT/AST elevations may be increased. Monitor therapy

Phenytoin: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Consider therapy modification

Protease Inhibitors: May increase the serum concentration of Simvastatin. Avoid combination

QuiNINE: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Monitor therapy

Raltegravir: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Monitor therapy

Ranolazine: May increase the serum concentration of Simvastatin. Management: Avoid the concurrent use of ranolazine with simvastatin when possible. If used together, avoid doses of simvastatin greater than 20 mg/day. Consider therapy modification

Red Yeast Rice: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Avoid combination

Repaglinide: HMG-CoA Reductase Inhibitors (Statins) may increase the serum concentration of Repaglinide. Monitor therapy

Rifamycin Derivatives: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Consider use of noninteracting antilipemic agents (note: pitavastatin concentrations may increase with rifamycin treatment). Monitor for altered HMG-CoA reductase inhibitor effects. Rifabutin and fluvastatin, or possibly pravastatin, may pose lower risk. Consider therapy modification

Rupatadine: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk for increased CPK and/or other muscle toxicities may be increased. Monitor therapy

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Simeprevir: May increase the serum concentration of Simvastatin. Monitor therapy

St John’s Wort: May increase the metabolism of HMG-CoA Reductase Inhibitors (Statins). Management: Consider avoiding the concomitant administration of St Johns Wort with interacting HMG-CoA reductase inhibitors in order to avoid the potential for decreased antilipemic effects. Monitor for decreased effects during concomitant therapy. Consider therapy modification

Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Telithromycin: May increase the serum concentration of Simvastatin. Avoid combination

Teriflunomide: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates. Monitor therapy

Ticagrelor: May increase the serum concentration of Simvastatin. Management: Avoid using doses of simvastatin greater than 40 mg/day with ticagrelor. This specific recommendation is found in the U.S. prescribing information but not in the Canadian product monograph. Consider therapy modification

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Tolvaptan: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates. Consider therapy modification

Trabectedin: HMG-CoA Reductase Inhibitors (Statins) may enhance the myopathic (rhabdomyolysis) effect of Trabectedin. Monitor therapy

Verapamil: May increase the serum concentration of Simvastatin. Management: Avoid concurrent use of verapamil with simvastatin when possible. If used together, limit adult maximum simvastatin dose to 10 mg/day, and avoid Simcor (simvastatin/niacin) because fixed simvastatin doses in the product exceed this maximum. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): HMG-CoA Reductase Inhibitors (Statins) may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy

Voxilaprevir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Use the lowest statin dose possible if combined with voxilaprevir and monitor patients for increased statin effects/toxicities. Avoid concomitant use of voxilaprevir with rosuvastatin or pitavastatin, and limit pravastatin doses to 40 mg daily. Consider therapy modification

Source: Wolters Kluwer Health. Last updated February 4, 2020.

Which Supplements Should Be Avoided When Taking Statins?

Answer:

Atorvastatin (Lipitor), rosuvastatin (Crestor), and other cholesterol-lowering statin drugs can be affected by taking supplements and can affect your ability to absorb certain vitamins and minerals. Certain herbal supplements, such as St. John’s wort, may decrease blood levels of some statin drugs, and when taken with atorvastatin, may actually result in increased cholesterol levels. Certain forms of magnesium may also decrease blood levels of statin drugs — particularly Crestor. Red yeast rice, which contains a naturally occurring statin, should not be combined with prescription statin drugs without medical supervision.

Berberine should be avoided or used with caution when taking certain statin drugs, such as atorvastatin (Lipitor), lovastatin (Mevacor) and rosuvastatin (Crestor).

While high doses of niacin may help to lower cholesterol, studies show that if you already take a statin drug, adding high-dose niacin does not appear to provide additional benefit and may carry serious risks. Nevertheless, some physicians believe taking niacin in addition to statin medication may be helpful for certain people; however do not try this combination without consulting your physician.

Some fruit juices can also be a problem, particularly grapefruit juice, which impairs the body’s normal breakdown of certain statins, allowing them to build up to potentially excessive levels in the blood. Since the effects of grapefruit juice may last as long as 3 days, it should be avoided if you are taking atorvastatin (Lipitor), lovastatin (Mevacor, Altoprev) or simvastatin (Zocor). However, some other statins do not seem to be affected by grapefruit juice, including pravastatin (Pravachol), fluvastatin (Lescol) and rosuvastatin (Crestor). 

Although green tea can help lower cholesterol, it can also decrease absorption of some, but not all, statin drugs. To play it safe, it may be best to take statins at least a couple of hours before consuming a green tea supplement or beverage.

On the other hand, CoQ10 and fish oil may offer particular benefits to people on statin drugs.

Grapefruit’s mortal danger named the danger of grapefruit

The use of grapefruit in combination with taking medications can cause serious harm to the body up to death, according to … RIA Novosti, 29.03.2020

2020-03-29T18: 05

2020-03-29T18: 05

2020-03-29T21: 36

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MOSCOW, March 29 – RIA Novosti. Eating grapefruit in combination with medications can cause serious harm or death, according to online newspaper SasaPost. Many people include this fruit in their diet due to its low calorie content and high fiber, which makes you feel full. grapefruit juice contains active substances furanocoumarins, which disrupt the work of cytochrome P45.This enzyme controls the concentration of drugs and toxins in the blood. Due to a malfunction in the P45 function, the active substances of medicines can accumulate in the body in quantities that are hazardous to health. Or, conversely, the effectiveness of drugs may be reduced due to too low a concentration. “One glass of grapefruit juice or a whole fruit can suppress the function of enzymes in your body for up to 24 hours, and therefore it is simply pointless to maintain the interval between taking the medicine and eating the fruit. “, – writes SasaPost.Grapefruit affects the effectiveness of about 50 drugs for the treatment of a wide variety of diseases, in most of which it is important to observe the exact dosage. At the same time, in many cases, due to the need to adhere to a healthy diet, patients add these citrus fruits to the menu. The authors of the article have listed medications that are undesirable to combine with the use of grapefruits. These include statins, a number of antiarrhythmic and pain relievers, blood pressure medications, some antihistamines, antineoplastic and estrogen medications, including birth control pills, and Viagra.Otherwise, side effects such as abnormal heart rhythms, sudden cardiac arrest, blood clots, kidney damage, bone marrow damage, destruction of muscle fibers may occur. The authors of the material advise you to carefully consider your diet and check product labels – they may contain grapefruit. Read the full version of the material on the website of Inosmi & gt; & gt;

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MOSCOW, March 29 – RIA Novosti. The use of grapefruit in combination with medications can cause serious harm to the body, including death, according to the online newspaper SasaPost.

Many people include this fruit in their diet because of its low calorie content and high fiber content, which makes you feel full.

November 6, 2019, 17:27

Doctors told who should not eat persimmons.At the same time, grapefruit juice contains active substances furanocoumarins, which disrupt the work of cytochrome P45. This enzyme controls the concentration of drugs and toxins in the blood. Due to a malfunction in the P45 function, the active substances of medicines can accumulate in the body in quantities that are hazardous to health.Or, conversely, the effectiveness of drugs may be reduced due to too low a concentration.

“One glass of grapefruit juice or a whole fruit can suppress the function of enzymes in your body for up to 24 hours, and therefore it is simply pointless to maintain the interval between taking the medicine and eating the fruit,” writes SasaPost.

Grapefruit affects the effectiveness of about 50 drugs for the treatment of a wide variety of diseases, in most of which it is important to observe the exact dosage. Moreover, in many cases, due to the need to adhere to a healthy diet, patients add these citrus fruits to the menu.

5 March 2020, 03:07

The nutritionist told how to eat apples correctly

The authors of the article have listed medications that are undesirable to combine with the use of grapefruit. These include statins, a number of antiarrhythmic and pain relievers, blood pressure medications, some antihistamines, antineoplastic and estrogen medications, including birth control pills, and Viagra.

Otherwise, side effects such as abnormal heart rhythms, sudden cardiac arrest, blood clots, kidney damage, bone marrow damage, and muscle fiber destruction may occur.

The authors of the material advise you to be careful about your diet and check product labels – they may contain grapefruit.

Read the full version of the material on the Inosmi website >>

February 21, 2020, 02:00

Taste or benefit? The doctor spoke about the unique properties of buckwheat

The active ingredient is Pitavastatin in Beloozerskoe

Special instructions

Pitavastatin tablets contain lactose, so they should not be prescribed for lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Indications for use

Primary hypercholesterolemia, including heterozygous familial hypercholesterolemia (Fredrickson type IIa hyperlipidemia), or mixed hypercholesterolemia (Fredrickson type IIb hyperlipidemia), hypertriglyceridemia (Fredrickson type IV hyperlipidemia and other treatments) as an adjunct (eg exercise, weight loss) are insufficient.

Pharmacological action

hypolipidemic inhibiting HMG-CoA reductase Pharmacodynamics Pitavastatin is a competitive inhibitor of HMG-CoA reductase, an enzyme that catalyzes the initial stage of cholesterol synthesis (CS) – the formation of mevalonic acid from HMG-CoA Since the conversion of HMG-CoA to mevalonic acid is the initial stage of cholesterol synthesis, the use of pitavastatin does not cause the accumulation of potentially toxic sterols in the body.HMG-CoA is readily metabolized to acetyl-CoA, which is involved in many synthesis processes in the body. Clinical studies have shown the effectiveness of pitavastatin in reducing the concentration of total cholesterol (TC) in blood plasma, LDL cholesterol, VLDL cholesterol, triglycerides (TG) and apolipoprotein B (Apo-B), as well as increasing the concentration of HDL cholesterol and apolipoprotein A1 (Apo-A1 Dose response in patients with primary hypercholesterolemia (adjusted mean percent change from baseline) Data are presented as dose (or placebo).number of patients (N). LDL cholesterol. OXC1. HDL cholesterol. TG. Aro-B. Aro-A1 Placebo: 51. -4. -1.3. 2.5.-2.1. 0.3. 3.2.1 mg: 52. -33.3. -22.8. 9.4. -14.8. -24.1. 8.5.2 mg: 49. -38.2. -26.1. 9. -17.4. -30.4. 5.6.4 mg: 50.-46.5. -32.5. 8.3. -21.2. -36.1. 4.7.1 Unadjusted In controlled clinical trials involving 1687 patients with primary hypercholesterolemia and combined (mixed) dyslipidemia, including 1239 patients who received therapeutic doses (mean baseline LDL cholesterol concentration of about 4.8 mmol / l), pitavastatin significantly reduced cholesterol levels LDL, TC, non-HDL cholesterol, TG and Apo-B and increased the concentration of HDL cholesterol and Apo-A1.Decreased ratios of total cholesterol / cholesterol HDL and Apo-B / Apo-A1. The concentration of LDL cholesterol decreased by 38–39% with the use of pitavastatin at a dose of 2 mg and by 44–45% at a dose of 4 mg. Most patients who received a dose of 2 mg reached the target LDL-C as recommended by the European Atherosclerosis Society (EAS) (

Overdose

There is no specific treatment for overdose. It is necessary to carry out symptomatic therapy, to monitor the activity of CPK and liver function.Hemodialysis is ineffective.

Contraindications

Hypersensitivity to pitavastatin and other HMG-CoA reductase inhibitors (statins). severe hepatic impairment (more than 9 points on the Child-Pugh scale) or class C according to the Child-Pugh classification, liver diseases in the active phase, including a persistent increase in the activity of hepatic transaminases in the blood serum (more than 3 times compared with VGN).myopathy, concomitant use of cyclosporine. pregnancy, breastfeeding period, lack of adequate contraceptive methods in women of childbearing age. age up to 18 years (efficacy and safety have not been established).

Application during pregnancy and lactation

The use of pitavastatin during pregnancy is contraindicated. Women of childbearing age should use reliable contraceptive methods when treated with pitavastatin.Since cholesterol and other cholesterol biosynthetic products are required for fetal development, the potential risk of inhibition of HMG-CoA reductase outweighs the benefits of pitavastatin treatment during pregnancy. Animal studies have shown that pitavastatin has reproductive toxicity, but no teratogenic potential. If the patient is planning a pregnancy, treatment should be discontinued at least 1 month before conception. If pregnancy occurs while using pitavastatin, treatment should be stopped immediately.The use of pitavastatin during breastfeeding is contraindicated. Pitavastatin is excreted in the milk of lactating rats. There are no data on the excretion of pitavastatin in breast milk of lactating women. If it is necessary to use pitavastatin during lactation, breastfeeding should be discontinued. -reductases.In a prospective follow-up of about 100 pregnancies in women treated with other HMG-CoA reductase inhibitors, the incidence of congenital anomalies, spontaneous miscarriages, and fetal death / stillbirth did not exceed the frequency expected in the general population. However, this study could exclude only a 3-4-fold increased risk of congenital anomalies compared to the baseline frequency. In 89% of these cases, drug treatment was started before pregnancy and stopped during the first trimester, when pregnancy was established.Reproductive toxicity studies in rats have shown that pitavastatin crosses the placenta and is found in fetal tissues at a concentration of & le. 36% of the concentration in the mother’s plasma after a single dose of 1 mg / kg / day during pregnancy.

TORVACARD 0.01 N90 TABLE P / PLEN / SHELL

Before starting therapy with TORVACARD®, it is necessary to try to control hypercholesterolemia by adequate diet therapy, increased physical activity, weight loss in obese patients and treatment of other conditions.The use of HMG-CoA reductase inhibitors to reduce the concentration of lipids in the blood plasma can lead to changes in the biochemical parameters of liver function, which should be monitored before starting therapy, 6 and 12 weeks after starting TORVACARD® and after each dose increase, as well as periodically eg every 6 months. An increase in the activity of “hepatic” transaminases in the blood serum can be observed during therapy with TORVACARD®, usually in the first three months.Patients who have an increase in the activity of “hepatic” transaminases should be under the supervision of a physician until the indicators return to normal.

A retrospective analysis of stroke subtypes in patients without coronary artery disease who have had recent stroke or TIA revealed a high incidence of hemorrhagic stroke in patients receiving atorvastatin 80 mg compared with placebo. An increased risk was noted at the beginning of the study in patients with previous hemorrhagic stroke or lacunar cerebral infarction.The risk-benefit ratio of atorvastatin 80 mg in patients who have had hemorrhagic stroke or lacunar cerebral infarction has not been determined, and the potential risk of hemorrhagic stroke should be carefully assessed before starting treatment with TORVACARD®.

Effect on skeletal muscle

Treatment with TORVACARD® in rare cases can cause myalgia, myositis and myopathy, which can progress to rhabdomyolysis, a potentially life-threatening condition characterized by a significant increase in CPK activity (> 10 times compared with the upper limit of normal), myoglobinemia and myoglobinuria, which can lead to renal failure.The drug TORVACARD® can cause an increase in the activity of serum CPK, which should be taken into account in the differential diagnosis of chest pain. Patients should be warned to see a doctor immediately if they develop unexplained muscle pain or weakness, especially if they are accompanied by malaise or fever. Therapy with TORVACARD® should be temporarily discontinued or completely canceled if signs of possible myopathy appear or if there is a risk factor for the development of renal failure associated with rhabdomyolysis (for example, severe acute infection, arterial hypertension, serious surgery, trauma, severe metabolic, endocrine and water-electrolyte disturbances and uncontrolled seizures).

Before starting treatment

TORVACARD® should be prescribed with caution to patients with factors predisposing to the development of rhabdomyolysis. CPK activity should be measured before starting treatment with statins in the following situations:

– with renal failure;

– with hypothyroidism;

– if you have a personal or family history of hereditary muscle diseases;

– if there is evidence of previous toxic effects on skeletal muscles caused by taking statins or fibrates;

– with a history of liver disease and / or alcohol abuse;

– in patients over 70 years of age, such a measurement is necessary in the presence of other predisposing factors of rhabdomyolysis;

– in situations where an increase in the concentration of atorvastatin in blood plasma may occur, for example, during drug interactions and in special populations, including genetic subpopulations.

In such situations, an assessment of the ratio of the risk of developing adverse reactions to the possible benefits of treatment should be carried out, in addition, it is recommended to carefully monitor the patient’s condition.

If the baseline values ​​of CPK activity are significantly increased (> 5 times compared to the upper limit of the norm), treatment should not be started.

Measurement of creatine phosphokinase

Determination of CPK activity should not be carried out after physical exertion or in the presence of any possible alternative reason for an increase in its indicators, as this complicates the interpretation of the test results.If the initial indicators of CPK activity are significantly increased (> 5 times, compared to the upper limit of the norm), a second analysis should be performed after 5-7 days to confirm the results.

During treatment

Patients should be warned that they should see a doctor immediately if they experience pain, cramps or muscle weakness, especially if they are accompanied by malaise or fever.

If similar symptoms occur in patients during treatment with TORVACARD®, their CPK activity should be assessed.With a significant increase in indicators (> 5 times, compared with the upper limit of the norm), treatment with TORVACARD® should be discontinued.

If muscle symptoms are serious and cause daily discomfort, even if the activity values ​​of CPK ns exceed the upper limit of the norm by less than 5 times, you should consider discontinuing treatment with TORVACARD®.

With the resolution of symptoms and the return of CPK values ​​to normal values, a decision can be made to prescribe a repeated course of atorvastatin or the introduction of an alternative statin at the lowest dose under close supervision.

Treatment with atorvastatin should be discontinued with a clinically significant increase in CPK activity (> 10 times compared to the upper limit of normal), or when rhabdomyolysis is diagnosed, or if it is suspected.

Concomitant treatment with other drugs

The risk of rhabdomyolysis increases with the concomitant use of atorvastatin and certain drugs that can increase the concentration of atorvastatin in blood plasma, such as potent inhibitors of the CYP3A4 isoenzyme or transport proteins (e.g. clarithromycin, delavirdine, styripentol, ketoconazole, voriconazole, itraconazole, posaconazole, and HIV protease inhibitors including ritonavir, lopinavir, atazanavir, indinavir, darunavir, etc.etc.). The risk of myopathy may also increase with the simultaneous use of gemfibrozil and other derivatives of fibric acid, erythromycin, nicotinic acid in lipid-lowering doses (more than 1 g per day) and ezetimibe. If possible, alternative (non-interacting) drugs should be used instead of these drugs.

In cases where the simultaneous use of these drugs and atorvastatin is necessary, the potential benefits and risks of concomitant therapy should be carefully evaluated.When patients receive medications that increase the concentration of atorvastatin in the blood plasma, it is recommended to prescribe TORVACARD® in the minimum maximum dose. In addition, in the case of the use of powerful inhibitors of the isoenzyme CYP3A4, it is recommended to use the minimum initial dose of TORVACARD® and establish clinical observation of the condition of these patients.

The simultaneous use of TORVACARD® and fusidic acid is not recommended, therefore, a decision may be made to temporarily discontinue treatment with TORVACARD® for the period of fusidic acid therapy.

Use in children

The safety of the drug in children has not been established.

Interstitial lung disease

With the use of some HMG-CoA reductase inhibitors, especially with prolonged therapy, rare cases of interstitial lung disease have been reported. Its manifestations can include shortness of breath, unproductive cough, and worsening of general condition (increased fatigue, weight loss, and fever).If interstitial lung disease is suspected, therapy with TORVACARD® should be discontinued.

Diabetes mellitus

Drugs of the statin class can cause an increase in the concentration of glucose in the blood. In some patients with a high risk of developing diabetes mellitus, such changes can lead to its manifestation, which is an indication for the appointment of hypoglycemic therapy. However, the reduction in the risk of cardiovascular diseases while taking HMG-CoA reductase inhibitors (statins) exceeds the risk of developing diabetes mellitus, so this factor should not serve as a basis for discontinuation of statin treatment.Patients at risk (fasting blood glucose concentration 5.6-6.9 mmol / l, body mass index (BMI)> 30 kg / m2, hypertriglyceridemia, history of arterial hypertension) should be monitored by a doctor and regularly monitored biochemical parameters …

Patients with rare hereditary diseases

TORVACARD® contains lactose.