Nelfinavir (Viracept) FACT SHEET Summary Published Nelfinavir is a type of anti-HIV drug called a protease inhibitor. 2014 The most common side effect of nelfinavir is diarrhea. It is usually taken at a dose of 1,250 mg twice daily with food.
CONTACT US What is nelfinavir? by telephone Nelfinavir, sold under the brand name Viracept, is a type of anti-HIV drug (antiretroviral) called a protease inhibitor (PI). Nelfinavir is used in combination 1-800-263-1638 with other anti-HIV drugs to treat (but not cure) HIV. 416-203-7122
by fax How does nelfinavir work? 416-203-8284 To explain how nelfinavir works, we need to first tell you some information about HIV. When HIV infects a cell, it takes control of that cell. HIV then forces by e-mail the cell to make many more copies of the virus. To make these copies, the cell [email protected] uses proteins called enzymes. When the activity of these enzymes is reduced the production of HIV slows. by mail Nelfinavir belongs to a group or class of drugs called protease inhibitors. 555 Richmond Street West Nelfinavir interferes with an enzyme called protease, which is used by HIV- Suite 505, Box 1104 infected cells to make new viruses. Since nelfinavir inhibits, or reduces Toronto ON M5V 3B1 the activity of this enzyme, this drug causes HIV-infected cells to produce fewer viruses.
How do people with HIV use nelfinavir? Treatment guidelines developed by the United States Department of Health and Human Services suggest that nelfinavir is not a preferred choice for the treatment of HIV infection. Clinical trials have shown that other protease inhibitors used such as the combination of lopinavir/ritonavir (in Kaletra) are superior to nelfinavir. All in all, nelfinavir is no longer commonly used in Canada and other high-income countries.
Nelfinavir is used in combination with several other anti-HIV drugs, usually nukes (nucleoside analogues), and sometimes including drugs from other classes such as non-nukes (non-nucleoside reverse transcriptase inhibitors). Combinations such as this are called antiretroviral therapy, or ART. For more information on ART, see CATIE’s Your Guide to HIV Treatment.
For many people with HIV, the use of ART has increased their CD4+ cell counts and decreased the amount of HIV in their blood (viral load). These beneficial effects help to reduce the risk of developing a life-threatening infection. CATIE FACT SHEET: Nelfinavir (Viracept)
Neither nelfinavir nor any other anti-HIV medication 3. Bleeding is a cure for HIV. It is therefore important that you do the following: Women may experience heavier menstrual periods when using protease inhibitors. Hemophiliacs who • see your doctor regularly so that he/she use protease inhibitors may experience increased monitors your health bleeding. If you are a hemophiliac who uses nelfinavir and has this problem, let your doctor • continue to practice safer sex and take other know about it. precautions so as not to pass HIV on to other people 4. Blood sugar problems Side effects In some people with HIV who use protease inhibitors, levels of sugar (glucose) in the blood 1. General become higher than normal. Prolonged bouts of higher-than-normal blood sugar levels may lead Common side effects that have been reported by to diabetes, although for the average person, the some nelfinavir users include abdominal pain, gas, risk of developing this complication is low. Regular nausea, rash, and unexpected tiredness. Always monitoring of your blood to assess sugar levels and tell your doctor, nurse, and pharmacist about side other measurements will help your doctor be aware effects that occur when you take nelfinavir or of changes that might suggest problems with your other medications. blood sugar.
2. Diarrhea 5. Lipodystrophy syndrome Nelfinavir is generally well tolerated. Its most The HIV lipodystrophy syndrome is the name given common side effect is diarrhea. This may clear up to a range of symptoms that can develop over after a few weeks of using the drug or it may last time when people use ART. Some features of the longer. Talk with your doctor and nurse about how lipodystrophy syndrome include: to deal with this problem. Nelfinavir-related diarrhea may be controlled with the use of some common • loss of fat just under the skin (subcutaneous supplements, including the following: fat) in the face, arms, and legs
• calcium (at least 500 mg twice daily) • bulging veins in the arms and/or legs due to the loss of fat under the skin • psyllium (Metamucil) or oat bran • increased waist and belly size • L-glutamine • fat pads at the back of the neck (“buffalo If these do not work your doctor can prescribe hump”) or at the base of the neck drugs such as: (“horse collar”) • loperamide (Imodium) • small lumps of fat in the abdomen • diphenoxylate (Lomotil) • increased breast size (in women) Research has found that nelfinavir does not cause Together with these physical changes, lab tests of your body to become more sensitive to milk or your blood may detect the following: dairy products. For more tips on managing diarrhea and other drug side effects, see CATIE’s A Practical • increased levels of fatty substances Guide to HIV Drug Side Effects. called triglycerides
• increased levels of LDL-cholesterol (low-density lipoprotein), or “bad” cholesterol
2 CATIE FACT SHEET: Nelfinavir (Viracept)
• increased levels of sugar (glucose) can develop resistance and your future treatment options may be reduced. • increased levels of the hormone insulin It may also be necessary to avoid drugs that do • decreased sensitivity to insulin not affect nelfinavir drug levels, but cause similar (insulin resistance) side effects. • decreased levels of HDL-cholesterol (high- If you must take a drug that has the potential to density lipoprotein), or “good” cholesterol interact with your existing medications, your doctor The precise causes of the HIV lipodystrophy can do the following: syndrome are not clear and are difficult to • adjust your dose of either your anti-HIV drugs understand because in some people with HIV there or other medications may be one or more aspects of the syndrome taking place. For instance, some people may experience fat • prescribe different anti-HIV drugs for you wasting, others fat gain, and others may experience both fat gain and wasting. What is becoming increasingly clear is that unfavourable changes Drug interactions for nelfinavir in the lab readings of glucose, cholesterol, and The following drugs interact or have the triglycerides over a period of several years increase potential to interact with nelfinavir. These lists are the risk of diabetes and cardiovascular disease. So not exhaustive. far, however, the many benefits of ART are much greater than the increased risk of cardiovascular The manufacturer recommends that the following disease or other side effects. drugs should not be taken by people using nelfinavir because this could lead to serious (or life- Maintaining a normal weight, eating a healthy threatening) interactions: diet, exercising regularly, and quitting smoking are all important in helping you to reduce your risk of • antibiotics / anti-tuberculosis drugs – rifampin diabetes, heart disease, and other complications. (Rifadin, Rifater) Regular visits to your doctor for checkups and blood • anti-psychotic drugs – pimozide (Orap) tests are a vital part of staying healthy. If necessary, your doctor can prescribe lipid-lowering therapy. • gastrointestinal motility agents – cisapride (Prepulsid) Researchers are studying the lipodystrophy syndrome to try to discover ways of helping people • heart drugs – amiodarone (Cordarone), with HIV avoid or reduce this problem. To find out quinidine (Biquin, Cardioquin) more about options for managing aspects of the • herbs – milk thistle, St. John’s wort lipodystrophy syndrome, see CATIE’s A Practical Guide to HIV Drug Side Effects. • high blood pressure drugs (calcium channel blockers) – amlodipine, nifedipine, verapamil
Drug interactions • lipid-lowering drugs – lovastatin (Mevacor), simvastatin (Zocor), fluvastatin (Lescol). Always consult your doctor and pharmacist about The manufacturer suggests considering the taking any other prescription or non-prescription use of other lipid-lowering drugs such as medication, including herbs, supplements, and pravastatin (Pravachol). street drugs. • migraine drugs (ergot derivatives) – Some drugs can interact with nelfinavir, increasing dihydroergotamine (Migranal), ergotamine or decreasing its levels in your body. Increased (Ergomar), ergonovine drug levels can cause you to experience side effects or make pre-existing side effects worse. On the • sedatives – midazolam (Versed), other hand, if drug levels become too low, HIV triazolam (Halcion)
3 CATIE FACT SHEET: Nelfinavir (Viracept)
The following drugs can increase levels of nelfinavir taking anti-HIV drugs to reduce the risk of passing in your body: on HIV to your baby. The use of nelfinavir by pregnant women has not resulted in a significant • anti-HIV drugs – delavirdine (Rescriptor), increase in birth defects. During pregnancy, levels indinavir (Crixivan), ritonavir (Norvir) of nelfinavir may become lower than normal. Talk to The following drugs can decrease levels of nelfinavir your doctor about how to manage this. in the blood:
• antibiotics / anti-tuberculosis drugs – rifabutin Resistance and cross-resistance (Mycobutin) Over time, as new copies of HIV are made in the • anti-seizure drugs – carbamazepine (Tegretol) body, the virus changes its structure. These changes are called mutations and can cause HIV to resist the Nelfinavir can increase levels of the following drugs: effects of anti-HIV drugs, which means those drugs • anti-HIV drugs – indinavir (Crixivan), will no longer work for you. Combining nelfinavir saquinavir (Invirase) with at least two other anti-HIV drugs delays the development of drug resistance. • antibiotics – rifabutin (Mycobutin), azithromycin (Zithromax) To reduce the risk of developing drug resistance, all anti-HIV drugs should be taken every day • erectile dysfunction drugs – sildenafil (Viagra), exactly as prescribed and directed. If doses are tadalafil (Cialis), vardenafil (Levitra). Taking delayed, missed, or not taken as prescribed, levels nelfinavir with any of these drugs can lead to of nelfinavir in the blood may fall too low. If this dangerous side effects and even death. Talk happens, resistant virus can develop. If you find you to your doctor if you have erectile dysfunction are having problems taking your medications as about how you might use these drugs safely. directed, speak to your doctor and nurse about this. They can find ways to help you. • lipid-lowering drugs – atorvastatin (Lipitor), simvastatin (Zocor), fluvastatin (Lescol). When HIV becomes resistant to one drug in a class, The manufacturer suggests considerating it sometimes becomes resistant to other drugs in other lipid-lowering agents such as that class. This is called cross-resistance. Feel free pravastatin (Pravachol). to talk with your doctor about your current and future treatment options. To help you decide what • transplant drugs – cyclosporine (Neoral), these future therapies might be, at some point sirolimus (Rapamune), tacrolimus (Prograf) your doctor can have a small sample of your blood Nelfinavir can decrease levels of the analysed using resistance testing. Should HIV in following drugs: your body become resistant to nelfinavir, your doctor, with the help of resistance testing, can help • anti-HIV drugs – delavirdine (Rescriptor) put together a new treatment regimen for you. • anti-seizure drugs – phenytoin (Dilantin)
• hormones – estrogen found in female Therapeutic drug monitoring (TDM) contraceptive medications In some parts of Canada your doctor may have • narcotics – methadone access to therapeutic drug monitoring (TDM). This is a process whereby a sample of your blood is taken and the amount of nelfinavir in it is assessed. Pregnancy If your nelfinavir levels are too low or too high, If you are a woman who is pregnant or wants to your doctor may adjust your dose of nelfinavir. become pregnant, let your doctor and nurse know TDM can be a useful tool to ensure that nelfinavir about this. If you are pregnant and not currently or other protease inhibitor levels in your blood are taking ART, you should talk with your doctor about
4 CATIE FACT SHEET: Nelfinavir (Viracept)
appropriate, particularly if the following conditions in healthy volunteers. British Journal of Clinical Pharmacology. are present: 2003;55(2):115-125. Bergshoeff AS, Wolfs TF, Geelen SP and Burger DM. Ritonavir- • You are pregnant enhanced pharmacokinetics of nelfinavir/M8 during rifampin use. Annals of Pharmacotherapy. 2003;37(4):521-525. • You are co-infected with hepatitis B or C Bratt G and Stahle L. Sildenafil does not alter nelfinavir pharmacokinetics. Therapeutic Drug Monitoring. 2003;(2):240- • You are taking a complex treatment regimen 242. Feel free to speak to your doctor about whether Burger DM, Hugen PW, Aarnoutse RE, et al. Treatment failure of nelfinavir-containing triple therapy can largely be explained TDM is an option for you and if you will have to pay by low nelfinavir plasma concentrations. Therapeutic Drug for it. Monitoring. 2003;25(1):73-80. Conner SD, Covington DL, Doi PA, et al. Risk of birth defects associated with nelfinavir exposure during pregnancy. 10th Dosage and formulations Conference on Retroviruses and Opportunistic Infections, February 10-14 2003, Boston. Poster 782. Nelfinavir is available as 250 mg and 625 mg Justman JE, Benning L, Danoff A, et al. Protease inhibitor use tablets. The usual standard adult dose of nelfinavir and the incidence of diabetes mellitus in a large cohort of is 1,250 mg (taken as two 625 mg tablets, twice HIV-infected women. Journal of Acquired Immune Deficiency daily or 750 mg (taken as three 250 mg tablet, Syndromes. 2003;32:298-302. three times a day). Formulations can change, Manfredi R, Calza L, and Chiodo F. Prospective comparison and dosages may need to be customized. All of first-line nelfinavir therapy versus nelfinavir introduction in rescue antiretroviral regimens. AIDS Patient Care and medications should always be taken as prescribed STDs2003;17(3):105-114. and directed. Roge BT, Katzenstein TL, Nielsen HL and Gerstoft J. Drug resistance mutations and outcome of second-line treatment in patients with first-line protease inhibitor failure on nelfinavir- Availability containing HAART. HIV Medicine. 2003;4(1):38-47. Smith DE, Kaufmann GR, Kahn JO, et al. Greater Reversal Nelfinavir is licensed in Canada for the treatment of of CD4(+) Cell Abnormalities and Viral Load Reduction HIV infection in adults, in combination with other after Initiation of Antiretroviral Therapy with Zidovudine, anti-HIV drugs. Your doctor can tell you more about Lamivudine, and Nelfinavir before Complete HIV Type 1 Seroconversion. AIDS Research and Human Retroviruses. 2003; the availability and coverage of nelfinavir in your 19(3):189-199. region. CATIE’s online module Federal, Provincial Hare CB, Vu MP, Grunfeld C, et al. Simvastatin-nelfinavir and Territorial Drug Access Programs also contains interaction implicated in rhabdomyolysis and death. Cinical information about Canadian drug coverage. Infectious Diseases .2002;35(10):e111-e112. Jain AK, Venkataramanan R, Fridell JA, et al. Nelfinavir, a protease inhibitor, increases sirolimus levels in a liver References transplantation patient: a case report. Liver Transplantation. 2002;8(9):838-840. Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected Kosel BW, Aweeka FT, Benowitz NL, et al. The effects of adults and adolescents. Department of Health and Human cannabinoids on the pharmacokinetics of indinavir and Services. Available at http://aidsinfo.nih.gov/ContentFiles/ nelfinavir. AIDS. 2002;16(4):543-550. AdultandAdolescentGL.pdf [Accessed February 28, 2014.] Piscitelli SC, Formentini E, Burstein AH, et al. Effect of milk Regazzi M, Maserati R, Villani P, et al. Clinical thistle on the pharmacokinetics of indinavir in healthy pharmacokinetics of nelfinavir and its metabolite M8 in volunteers. Pharmacotherapy. 2002;22(5):551-556. human immunodeficiency virus (HIV)-positive and HIV- Rossi DR, Rathbun RC, and Slater LN. Symptomatic orthostasis hepatitis C virus-coinfected subjects. Antimicrobial Agents and with extended-release nifedipine and protease inhibitors. Chemotherapy. 2005;49(2):643-649. Pharmacotherapy. 2002;22(10):1312-1316. van Heeswijk RP, Khaliq Y, Gallicano KD, et al. The Walmsley S, Bernstein B, King M, et al. Lopinavir-ritonavir pharmacokinetics of nelfinavir and M8 during pregnancy versus nelfinavir for the initial treatment of HIV infection. New and post partum. Clinical Pharmacology and Therapeutics. England Journal of Medicine. 2002;346(26):2039-2046. 2004;76(6):588-597. de Maat MMR, Hoetelmans RMW, Math tRA, et al. Drug Aarnoutse RE, Droste JA, van Oosterhout JJ, et al. interaction between St John’s wort and nevirapine. AIDS. Pharmacokinetics, food intake requirements and tolerability of 2001;15(3):420-421. once-daily combinations of nelfinavir and low-dose ritonavir
5 CATIE FACT SHEET: Nelfinavir (Viracept)
Schippers EF, Hugen PW, den Hartigh J, et al. No drug- interaction between nelfinavir or indinavir and mefloquine in HIV-1-infected patients. AIDS. 2000;14(17):2794-2795. Author(s): Hosein SR, Ziegler B
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Decisions about particular medical treatments should always be made in consultation with a qualified medical practitioner knowledgeable about HIV- CONTACT US and hepatitis C-related illness and the treatments in question. by telephone CATIE provides information resources to help people living with HIV and/or 1-800-263-1638 hepatitis C who wish to manage their own health care in partnership with 416-203-7122 their care providers. Information accessed through or published or provided by CATIE, however, is not to be considered medical advice. We do not recommend by fax or advocate particular treatments and we urge users to consult as broad a 416-203-8284 range of sources as possible. We strongly urge users to consult with a qualified medical practitioner prior to undertaking any decision, use or action of a medical nature. by e-mail [email protected] CATIE endeavours to provide the most up-to-date and accurate information at the time of publication. However, information changes and users are by mail encouraged to consult as broad a range of sources as possible. Users relying 555 Richmond Street West on this information do so entirely at their own risk. Neither CATIE, nor any of Suite 505, Box 1104 its partners, funders, employees, directors, officers or volunteers may be held Toronto ON M5V 3B1 liable for damages of any kind that may result from the use or misuse of any such information. The views expressed herein or in any article or publication accessed or published or provided by CATIE do not necessarily reflect the policies or opinions of CATIE nor the views of its partners and funders.
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