[Posted 3/1/2012]ISSUE:FDA notified healthcare professionals of updates to the prescribing information concerning interactions between protease inhibitors and certain statin drugs. Protease inhibitors and statins taken together may raise the blood levels of statins and increase the risk for muscle injury (myopathy). The most serious form of myopathy, called rhabdomyolysis, can damage the kidneys and lead to kidney failure, which can be fatal.
BACKGROUND:Statins are a class of prescription drugs used together with diet and exercise to reduce blood levels of low-density lipoprotein (LDL) cholesterol (''bad cholesterol''). HIV protease inhibitors are a class of prescription anti-viral drugs used to treat HIV. HCV protease inhibitors are a class of prescription anti-viral drugs used to treat hepatitis C infection.
RECOMMENDATION:Healthcare professionals should follow the recommendations in the prescribing information (drug labels) when prescribing HIV or HCV protease inhibitors with statins. See the FDA Drug Safety Communication for additional information, including a data summary. For more information visit the FDA website at: Web Siteand Web Site.
Saquinavir is used in combination with ritonavir (Norvir) and other medications to treat human immunodeficiency virus (HIV) infection in patients with or without acquired immunodeficiency syndrome (AIDS). Saquinavir is in a class of antiviral medications called protease inhibitors. It works by slowing the spread of HIV in the body. Saquinavir does not cure HIV and may not prevent you from developing HIV-related illnesses. Saquinavir does not prevent the spread of HIV to other people.
Saquinavir comes as a capsule and a tablet to take by mouth. It is usually taken with ritonavir (Norvir) two times a day within 2 hours after a full meal. It may be easier to remember to take saquinavir if you take it with meals. Take saquinavir at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take saquinavir exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Continue to take saquinavir even if you feel well. Do not stop taking saquinavir without talking to your doctor. If you miss doses, take less than the prescribed dose or stop taking saquinavir, your condition may become more difficult to treat.
Your doctor or pharmacist will give you the manufacturer's patient information sheet (Medication Guide) when you begin treatment with saquinavir and each time you refill your prescription. Read the information carefully and ask your doctor or pharmacist if you have any questions. You can also visit the Food and Drug Administration (FDA) website ( Web Site) or the manufacturer's website to obtain the Medication Guide.
Saquinavir is sometimes used with ritonavir (Norvir) and other medications to help prevent infection in healthcare workers or other people who were exposed to HIV. Talk to your doctor about the risks of taking this medication for your condition.
This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.
Before taking saquinavir,
- tell your doctor and pharmacist if you are allergic to saquinavir, any other medications, or any of the ingredients in saquinavir capsules or tablets. Ask your pharmacist for a list of the ingredients.
- tell your doctor if you are taking any of the following medications: alfuzosin (Uroxatral); cisapride (Propulsid); ergot medications such as dihydroergotamine (Migranal), ergoloid mesylates (Germinal, Hydergine), ergonovine (Ergotrate), ergotamine (Cafergot, Wigraine), methylergonovine (Methergine), and methysergide (Sansert); certain medications for irregular heartbeat such as amiodarone (Cordarone, Pacerone), bepridil (not available in the United States), dofetilde (Tikosyn); flecainide (Tambocor), lidocaine; propafenone (Rhythmol), or quinidine (Quinidex); lovastatin (Advicor, Altocor, Mevacor); midazolam (Versed); pimozide (Orap); rifampin (Rifadin, Rimactane, in Rifamate); sildenafil (Revatio); simvastatin (Zocor); terfenadine (Seldane) (no longer available in the United States); trazodone (Oleptro); or triazolam (Halcion).Your doctor will probably tell you not to take saquinavir if you are taking one or more of these medications.
- tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking or plan to take. Be sure to mention any of the following: anticoagulants ('blood thinners') such as warfarin (Coumadin); antifungals such as fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral), and voriconazole (Vfend); benzodiazepines such as alprazolam (Xanax), clorazepate (ClorazeCaps, Tranxene, others), diazepam (Valium), and flurazepam (Dalmane); beta blockers such as atenolol (Tenormin), labetalol (Normodyne), metoprolol (Lopressor, Toprol XL), nadolol (Corgard), and propranolol (Inderal); bosentan (Tracleer); calcium channel blockers such as amlodipine (Norvasc, in Caduet), diltiazem (Cardizem, Dilacor, Tiazac, others), felodipine (Plendil), isradipine (DynaCirc), nicardipine (Cardene), nifedipine (Adalat, Procardia), nimodipine (Nimotop), nisoldipine (Sular), and verapamil (Calan, Covera, Isoptin, Verelan); certain cholesterol-lowering medications (statins) such as atorvastatin (Lipitor) and rosuvastatin (Crestor); clarithromycin (Biaxin, in Prevpac); colchicine (Colcrys); dapsone (Avlosulfon); dexamethasone (Decadron, Dexone); digoxin (Lanoxicaps, Lanoxin); disopyramide (Norpace); fentanyl (Actiq, Duragesic, Fentora, Onsolis); fluticasone (in Advair, Flovent, Veramyst); certain immunosuppressants such as cyclosporine (Neoral, Sandimmune), tacrolimus (Protopic), or sirolimus (Rapamune); insulin or oral medications for diabetes; medications to treat HIV or AIDS including atazanavir (Reyataz), delavirdine (Rescriptor), efavirenz (Sustiva), enfuvirtide (Fuzeon), indinavir (Crixivan), lopinavir (in Kaletra), nelfinavir (Viracept), nevirapine (Viramune), or tipranavir (Aptivus); certain medications for irregular heartbeat such as procrainamide and sotalol (Betapace, Sorine); medications to treat seizures such as carbamazepine (Carbatrol, Epitol, Tegretol), phenytoin (Dilantin, Phenytek), and phenobarbital (Luminal, Solfoton); methadone (Dolophine, Methadose); omeprazole (Prilosec, in Zegerid); certain phosphodiesterase (PDE5) inhibitors such as sildenafil (Viagra); tadalafil (Adcirca, Cialis) and vardenafil (Levitra); rifabutin (Mycobutin); and certain tricyclic antidepressants including amitriptyline (in Limbitrol) and imipramine (Tofranil). Other medications may interact with saquinavir, so be sure to tell your doctor and pharmacist about all the medications you are taking, even those that do not appear on this list. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- tell your doctor what herbal products you are taking or plan to take, especially St. John's wort and garlic capsules.
- tell your doctor if you have or have ever had liver disease, a prolonged QT interval (rare heart problem that may cause irregular heartbeat, fainting, or sudden death), or low levels of potassium or magnesium in your blood. Also tell your doctor if you have complete atrioventricular (AV) block (slowed electrical activity in the heart) and you do not have a pacemaker. Your doctor will probably tell you not to take saquinavir.
- tell your doctor if you drink or have ever drunk large amounts of alcohol, if you have ever taken any form of saquinavir in the past, and if you or anyone in your family has or has ever had diabetes. Also tell your doctor if you have or have ever had an irregular heartbeat, high cholesterol or triglycerides (fats in the blood); hemophilia (a bleeding disorder); or heart or kidney disease.
- tell your doctor if you are pregnant or plan to become pregnant. If you become pregnant while taking saquinavir, call your doctor. You should not breastfeed if you are infected with HIV or are taking saquinavir.
- you should know that saquinavir may decrease the effectiveness of hormonal contraceptives (birth control pills, patches, rings, or injections). Talk to your doctor about using another form of birth control.
- if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking saquinavir.
- you should be aware that your body fat may increase or move to different areas of your body, such as your upper back, neck (''buffalo hump''), breasts, and around your stomach. You may notice a loss of body fat from your face, legs, and arms.
- you should know that you may experience hyperglycemia (increases in your blood sugar) while you are taking this medication, even if you do not already have diabetes. Tell your doctor immediately if you have any of the following symptoms while you are taking saquinavir: extreme thirst, frequent urination, extreme hunger, blurred vision, or weakness. It is very important to call your doctor as soon as you have any of these symptoms, because high blood sugar that is not treated can cause a serious condition called ketoacidosis. Ketoacidosis may become life-threatening if it is not treated at an early stage. Symptoms of ketoacidosis include: dry mouth, nausea and vomiting, shortness of breath, breath that smells fruity, and decreased consciousness.
- you should know that while you are taking medications to treat HIV infection, your immune system may get stronger and begin to fight other infections that were already in your body. This may cause you to develop symptoms of those infections. If you have new or worsening symptoms after starting treatment with saquinavir, be sure to tell your doctor.
Talk to your doctor about eating grapefruit and drinking grapefruit juice while taking this medication.
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
Saquinavir may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- stomach pain
- back pain
- dry lips or skin
Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately:
- blistering or peeling skin
- flu-like symptoms
- yellowing of the skin or eyes
- extreme tiredness
- lack of energy
- loss of appetite
- pain in the upper right part of the stomach
- slow, irregular, or pounding heartbeat
Saquinavir may cause other side effects. Call your doctor if you have any unusual problems while you are taking this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at Web Site] or by phone [1-800-332-1088].
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.
Symptoms of overdose may include the following:
Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests before and during your treatment to check your body's response to saquinavir. Your doctor may also order an electrocardiogram (ECG; test that measures the electrical activity in the heart) before and during your treatment.
Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
AHFS® Consumer Medication Information. © Copyright, The American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland. All Rights Reserved. Duplication for commercial use must be authorized by ASHP.
Selected Revisions: March 15, 2012.