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Protease inhibitors

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Related Terms
  • Antiretroviral therapy, antiretrovirals, ART, fusion inhibitors, HAART, highly active antiretroviral therapy, HIV, HIV protease enzyme, human immunodeficiency syndrome, immune defense system, immune system, immunocompromised, immunodeficiency, infection, inhibitor, non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, OI, opportunistic infections, polyprotein, protease, protease enzyme, reverse transcriptase inhibitors, virion, virus.

Background
  • Protease inhibitors (PIs) disrupt the replication of HIV (human immunodeficiency virus). These drugs interfere with the protease enzyme that HIV uses to produce infectious viral particles. When protease is blocked, the new copies of HIV are not formed properly, and they are unable to infect new cells.
  • The U.S. Food and Drug Administration (FDA) has approved 10 protease inhibitors, including Agenerase®, Aptivus®, Crixivan®, Invirase®, Kaletra®, Lexiva®, Norvir®, Prezista®, Reyataz®, and Viracept®.
  • Since HIV primarily targets the body's CD4 T-cells, which are white blood cells that help coordinate the immune system's response to infections and diseases, HIV patients are vulnerable to opportunistic infections (OIs). Opportunistic infections occur in patients who have weakened immune systems. Although antiretrovirals are not curative, they are able to suppress HIV subsequently boosting the patient's immune system. These drugs have also shown to dramatically slow the progression of OIs.
  • HIV patients typically receive a combination of antiretroviral drugs because, as the virus reproduces, different strains emerge, and some are resistant to certain drugs. This happens less often when patients adhere to their medication regimens. Therefore, highly active antiretroviral therapy (HAART), which is a combination of drugs from at least two different classes, is recommended.
  • Currently, the FDA has approved 28 antiretroviral drugs to treat HIV patients. These drugs fall into four major classes: fusion inhibitors, protein inhibitors, nucleoside reverse transcriptase inhibitors (NRTIs), and non-nucleoside reverse transcriptase inhibitors (NNRTIs).

Author information
  • This information has been edited and peer-reviewed by contributors to the Natural Standard Research Collaboration (www.naturalstandard.com).

Bibliography
  1. AIDS Treatment Data Network. Protease Inhibitors. .
  2. Natural Standard: The Authority on Integrative Medicine. . Copyright © 2010.
  3. The Body: The Complete HIV/AIDS Resource. .
  4. U.S. Food and Drug Administration (FDA). .
  5. Vaughn G, Detels R. Protease inhibitors and cardiovascular disease: analysis of the Los Angeles County adult spectrum of disease cohort. AIDS Care. 2007 Apr;19(4):492-9. .

Integrative therapies
  • Note: Integrative therapies should not replace antiretroviral therapy (ART) in HIV patients. Patients should consult their healthcare providers before taking any herbs or supplements because they may interact with treatment. Patients should not take St. John's wort because it may interact with HIV treatment.
  • Unclear or conflicting scientific evidence:
  • Aloe vera: Clear gel from the pulp of Aloe vera leaves has been used on the skin for thousands of years to treat wounds, skin infections, minor burns and other skin conditions. Although aloe has been suggested as a possible treatment for HIV, further research is needed before a firm conclusion can be made.
  • Avoid if allergic to aloe or other plants of the Liliaceae family (garlic, onions, tulips). Avoid injecting aloe. Do not apply to open skin, surgical wounds or pressure ulcers. Avoid taking by mouth with diarrhea, bowel blockage, intestinal diseases, bloody stools or hepatitis. Avoid with a history of irregular heartbeat (arrhythmia), electrolyte imbalances, diabetes, heart disease or kidney disease. Avoid taking by mouth if pregnant or breastfeeding.
  • Antineoplastons: Antineoplastons are substances found in human blood and urine. A small preliminary study reported increased energy and weight in patients with HIV, as well as a decreased number of opportunistic infections, and increased CD4 cell counts. These patients were treated with antineoplaston AS2-1. However, this evidence cannot be considered conclusive. Currently, there are drug therapy regimens available for HIV with clearly demonstrated effects (highly active anti-retroviral therapy), and patients with HIV are recommended to consult with their physicians about treatment options.
  • Avoid if allergic or hypersensitive to antineoplastons. Use cautiously with high medical or psychiatric risk. Use cautiously with an active infection due to a possible decrease in white blood cells. Use cautiously with high blood pressure, heart conditions, chronic obstructive pulmonary disease, liver disease/damage or kidney disease/damage. Avoid if pregnant or breastfeeding.
  • Beta sitosterol: Beta-sitosterol is found in plant-based foods, such as fruits, vegetables, soybeans, breads, peanuts and peanut products. It is also found in bourbon and oils (such as olive oil, flaxseed and tuna). Due to data that suggest immune modulating effects of beta-sitosterol and beta-sitosterol glucoside, these sterols have been studied in combination in the treatment of HIV. Larger populations of patients with HIV should be evaluated in randomized controlled trials to draw any conclusions.
  • Avoid if allergic or hypersensitive to beta-sitosterol, beta-sitosterol glucoside or pine. Use cautiously with asthma or breathing disorders, diabetes, primary biliary cirrhosis (destruction of the small bile duct in the liver), ileostomy, neurodegenerative disorders (like Parkinson's disease or Alzheimer's disease), diverticular disease (bulging of the colon), short bowel syndrome, celiac disease and sitosterolemia. Use cautiously with a history of gallstones. Avoid if pregnant or breastfeeding.
  • Bitter melon: Laboratory studies have shown that a protein in bitter melon called MAP30 may have antiviral activity. However, this has not been studied in humans. Further research is needed before a firm conclusion can be made.
  • Avoid if allergic to bitter melon or members of the Curcurbitaceae (gourd or melon) family. Avoid ingesting bitter melon seeds. Avoid with glucose-6-phosphate dehydrogenase deficiency. Use cautiously with diabetes, glucose intolerance or with hypoglycemic agents due to the risk of hypoglycemia. Avoid if pregnant or breastfeeding.
  • Chiropractic: Chiropractic care focuses on how the relationship between musculoskeletal structure (mainly the spine) and bodily function (mainly nervous system) affects health. There is not enough reliable scientific evidence to conclude the effects of chiropractic techniques on CD4 cell count or quality of life in patients with HIV/AIDS.
  • Use extra caution during cervical adjustments. Use cautiously with acute arthritis, conditions that cause decreased bone mineralization, brittle bone disease, bone softening conditions, bleeding disorders or migraines. Use cautiously with the risk of tumors or cancers. Avoid with symptoms of vertebrobasilar vascular insufficiency, aneurysms, unstable spondylolisthesis or arthritis. Avoid with agents that increase the risk of bleeding. Avoid in areas of para-spinal tissue after surgery. Avoid if pregnant or breastfeeding due to a lack of scientific data.
  • Coenzyme Q10: Coenzyme Q10 (CoQ10) is produced by the body, and it is necessary for basic functioning of cells. CoQ10 levels decrease with age. There is limited evidence that natural levels of CoQ10 in the body may be reduced in people with HIV/AIDS. There is no reliable scientific research showing that CoQ10 supplements have any effect on this disease.
  • There are currently no documented cases of allergy associated with Coenzyme Q10 supplements, although rash and itching have rarely been reported. Stop use two weeks before surgery/dental/diagnostic procedures with bleeding risk and do not use immediately after these procedures. Use cautiously with history of blood clots, diabetes, high blood pressure, heart attack or stroke. Use cautiously with anticoagulants (blood thinners), antiplatelet drugs, blood pressure drugs, blood sugar drugs, cholesterol drugs or thyroid drugs. Avoid if pregnant or breastfeeding.
  • DHEA: DHEA (Dehydroepiandrosterone) is a hormone that is secreted by the adrenal glands. Although some studies suggest that DHEA supplementation may be beneficial in patents with HIV, results from different studies do not agree with each other. There is currently not enough scientific evidence to recommend DHEA for this condition, and other therapies are more proven in this area.
  • Avoid if allergic to DHEA. Avoid with a history of seizures. Use cautiously with adrenal or thyroid disorders. Use cautiously if taking anticoagulants, or drugs, herbs or supplements for diabetes, heart disease, seizures or stroke. Stop use two weeks before surgery/dental/diagnostic procedures with bleeding risk, and do not use immediately after these procedures. Avoid if pregnant or breastfeeding.
  • Flaxseed: Flaxseed and flaxseed oil/linseed oil are rich sources of the essential fatty acid alpha-linolenic acid (omega-6). While flaxseed has been used to treat HIV, no strong evidence supports its use, and no recommendation can be made without further research.
  • Flaxseed has been well tolerated in studies for up to four months. Avoid if allergic to flaxseed, flaxseed oil or other plants of the Linaceae family. Avoid with prostrate cancer, breast cancer, uterine cancer or endometriosis. Avoid ingestion of immature flaxseed pods. Avoid large amounts of flaxseed by mouth and mix plenty of water or liquid. Avoid flaxseed (not flaxseed oil) with history of esophageal stricture, ileus, gastrointestinal stricture or bowel obstruction. Avoid with history of acute or chronic diarrhea, irritable bowel syndrome (IBS), diverticulitis or inflammatory bowel disease (IBD). Avoid topical flaxseed in open wounds or abraded skin surfaces. Use cautiously with history of a bleeding disorder or with drugs that increase the risk of bleeding (such as anticoagulants and non-steroidal anti-inflammatories). Use cautiously with high triglyceride levels, diabetes, mania, seizures or asthma. Avoid if pregnant or breastfeeding.
  • Healing Touch: Healing touch (HT) is a combination of hands-on and off-body techniques to influence the flow of energy through a person's biofield. Data from small preliminary studies are insufficient to support any recommendations for or against use of HT in HIV/AIDS. Studies of better design are needed before any conclusions can be reached.
  • HT should not be regarded as a substitute for established medical treatments. Use cautiously if pregnant or breastfeeding.
  • L-carnitine: L-carnitine may be beneficial in AIDS treatment by increasing proliferation of mononuclear cells and increasing CD4 counts. Additional study is needed to make a firm recommendation
  • Avoid if allergic or hypersensitive to carnitine. Use cautiously with peripheral vascular disease, high blood pressure, alcohol-induced liver cirrhosis and diabetes. Use cautiously in low birth weight infants and individuals on hemodialysis. Use cautiously if taking anticoagulants (blood thinners), beta-blockers or calcium channel blockers. Avoid if pregnant or breastfeeding.
  • Meditation: Various forms of meditation have been practiced for thousands of years throughout the world, with many techniques originating in Eastern religious practices. A common goal is to attain a state of "thoughtless awareness" of sensations and mental activities occurring at the present moment. More studies are needed to establish how meditation may be useful as an adjunctive therapy in HIV/AIDS patients.
  • Use cautiously with underlying mental illnesses. People with psychiatric disorders should consult with their primary mental healthcare professionals before starting a program of meditation, and they should explore how meditation may or may not fit in with their current treatment plans. Avoid with risk of seizures. The practice of meditation should not delay the time to diagnosis or treatment with more proven techniques or therapies, and it should not be used as the sole approach to illnesses.
  • Melatonin: Melatonin is a neurohormone produced in the brain. There is a lack of well-designed scientific evidence to recommend for or against the use of melatonin as a treatment for AIDS. Melatonin should not be used in place of more proven therapies, and patients with HIV/AIDS should be treated under the supervision of their healthcare professionals.
  • Based on available studies and clinical use, melatonin is generally regarded as safe in recommended doses for short-term use. There are rare reports of allergic skin reactions after taking melatonin by mouth. Use cautiously with bleeding disorders, seizure disorders or if taking drugs that increase the risk of bleeding.
  • Mistletoe: Once considered a sacred herb in Celtic tradition, mistletoe has been used for centuries for high blood pressure, epilepsy, exhaustion, anxiety, arthritis, vertigo (dizziness) and degenerative inflammation of the joints. Treatment of HIV patients with mistletoe has been done in Europe since the beginning of the AIDS epidemic. Treatment seems to be tolerable with minimal side effects reported. Mistletoe may assist in inhibiting disease progression. However, not all mistletoe preparations have shown equal effects. Further study is needed before a firm conclusion can be made.
  • Avoid if allergic or hypersensitive to mistletoe or to any of its constituents. Anaphylactic reactions (life threatening, shock) have been described after injections of mistletoe. Avoid with acute, highly febrile, inflammatory disease, thyroid disorders, seizure disorders or heart disease. Use cautiously with diabetes, glaucoma or with cholinergics.
  • Prayer/distant healing: Prayer can be defined as a "reverent petition," the act of asking for something while aiming to connect with God or another object of worship. Limited study of prayer in patients with AIDS reports fewer new AIDS-related illnesses and hospitalizations. However, due to methodological problems, these results cannot be considered conclusive.
  • Prayer is not recommended as the sole treatment approach for potentially serious medical conditions, and it should not delay the time it takes to consult with a healthcare professional or receive established therapies. Sometimes religious beliefs come into conflict with standard medical approaches and require an open dialog between patients and caregivers.
  • Psychotherapy: Psychotherapy is an interactive process between a person and a qualified mental health professional. The patient will explore thoughts, feelings and behavior to help with problem solving. Psychotherapy, especially supportive psychotherapy, may reduce depression in HIV-positive patients. It may also help with treating substance abuse when used in combination with prescription medicine. Supportive-expressive group therapy may also have concomitant improvements in CD4 cell count and viral load. More research is needed in this area, especially to determine the best type of psychotherapy.
  • Psychotherapy cannot always fix mental or emotional conditions. Psychiatric drugs are sometimes needed. In some cases symptoms may get worse if the proper medication is not taken. Not all therapists are qualified to work with all problems. Use cautiously with serious mental illness or some medical conditions because some forms of psychotherapy may stir up strong emotional feelings and expression.
  • Relaxation therapy: Relaxation techniques include behavioral therapeutic approaches that differ widely in philosophy, methodology and practice. Mental health and quality-of-life improvements have been seen in preliminary studies of HIV/AIDS patients. These findings suggest the need for further, well-controlled research.
  • Avoid with psychiatric disorders like schizophrenia/psychosis. Jacobson relaxation (flexing specific muscles, holding that position, then relaxing the muscles) should be used cautiously with illnesses like heart disease, high blood pressure or musculoskeletal injury. Relaxation therapy is not recommended as the sole treatment approach for potentially serious medical conditions, and it should not delay the time to diagnosis or treatment with more proven techniques.
  • Selenium: Selenium is a mineral found in soil, water and some foods. Selenium supplementation has been studied in HIV/AIDS patients, and some reports associate low selenium levels with complications, such as cardiomyopathy. It remains unclear if selenium supplementation is beneficial in patients with HIV, particularly during antiretroviral therapy.
  • Avoid if allergic or sensitive to products containing selenium. Avoid with history of non-melanoma skin cancer. Selenium is generally regarded as safe for pregnant or breastfeeding women. However, animal research reports that large doses of selenium may lead to birth defects.
  • Shiitake: Shiitake mushrooms were originally grown on natural oak logs found in Japan. Today, they are available in the United States. These mushrooms are large, black-brown and have an earthy rich flavor. Based on preliminary studies, lentinan may increase CD4 counts and may qualify in future multi-drug studies in HIV patients. Further well-designed studies are needed to confirm these results. Side effects have been reported and more proven therapies are recommended at this time.
  • Avoid if allergic or hypersensitive to shiitake mushrooms. Avoid if pregnant or breastfeeding.
  • Thymus extract: Thymus extracts for nutritional supplements are usually derived from young calves. Preliminary evidence found no improvement in HIV progression to AIDS or immunostimulation, although some immunological activity was noted in a non-randomized controlled trial. Additional study is needed in this area.
  • Avoid if allergic or hypersensitive to thymus extracts. Use bovine thymus extract supplements cautiously due to potential for exposure to the virus that causes "mad cow disease." Avoid use with an organ transplant or other forms of allografts or xenografts. Avoid if receiving immunosuppressive therapy or hormone therapy. Avoid with thymic tumors, myasthenia gravis (neuromuscular disorder) or untreated hypothyroidism. Avoid if pregnant or breastfeeding. Thymic extract increases human sperm motility and progression.
  • Traditional Chinese medicine (TCM): Traditional Chinese medicine (TCM) is a broad term that refers to many different treatments and traditions of healing. They share a common heritage of technique or theory rooted in ancient Chinese philosophy (Taoism) that dates back over 5,000 years. TCM herbs are a popular complementary therapy in HIV/AIDS. However, study results conflict. More studies are needed before the potential benefits of TCM herbs in HIV/AIDS can be established.
  • Chinese herbs can be potent and may interact with other herbs, foods or drugs. Consult a qualified healthcare professional before taking. There have been reports of manufactured or processed Chinese herbal products being tainted with toxins or heavy metal or not containing the listed ingredients. Herbal products should be purchased from reliable sources. Avoid ma huang, which is the active ingredient in ephedra. Avoid ginseng if pregnant or breastfeeding.
  • Turmeric: Turmeric is a perennial plant native to India and Indonesia, and it is often used as a spice in cooking. Several laboratory studies suggest that curcumin, a component of turmeric, may have activity against HIV. However, reliable human studies are lacking in this area.
  • Avoid if allergic or hypersensitive to turmeric (curcumin), yellow food colorings or plants belonging to the Curcuma or Zingiberaceae (ginger) families. Use cautiously with history of bleeding disorders, immune system deficiencies, liver disease or gallstones. Use cautiously with blood-thinners (e.g. warfarin). Use cautiously if pregnant or breastfeeding.
  • Vitamin A: Vitamin A is a fat-soluble vitamin, which is derived from two sources - retinoids and carotenoids. Retinoids are found in animal sources (such as the liver, kidney, eggs and dairy products). Carotenoids are found in plants like dark or yellow vegetables and carrots. The role of vitamin A in the prevention, transmission, or treatment of HIV is controversial and not well established. A clear conclusion cannot be formed based on the available scientific research.
  • Avoid if allergic or hypersensitive to vitamin A. Vitamin A toxicity can occur if taken at high dosages. Use cautiously with liver disease or alcoholism. Smokers who consume alcohol and beta-carotene may have an increased risk for lung cancer or heart disease. Vitamin A appears safe in pregnant women if taken at recommended doses. Use cautiously if breastfeeding because the benefits or dangers to nursing infants are not clearly established.
  • Zinc: Zinc formulations have been used since Ancient Egyptian times to enhance wound healing. Patients with HIV/AIDS, especially in those with low zinc levels, may benefit from zinc supplementation. Some low quality studies cite reduction in infections, enhanced weight gain and immune system function, including increased CD4 and CD8 cells. However, other low quality studies conflict with these findings. Further research is needed before a conclusion can be drawn.
  • Zinc is generally considered safe when taken at the recommended dosages. Avoid zinc chloride since studies have not been done on its safety or effectiveness. While zinc appears safe during pregnancy in amounts lower than the established upper intake level, caution should be used since studies cannot rule out the possibility of harm to the fetus.
  • Fair negative scientific evidence:
  • Ozone therapy: Ozone molecules are composed of three oxygen atoms. Ozone exists high in the earth's atmosphere and absorbs radiation from the sun. Reports of using ozone for medicinal purposes date to the late 19th Century. Laboratory studies have shown HIV virus to be sensitive to ozone, but no high-quality human studies exist. A preliminary study measured the safety and effectiveness of ozone-treated blood in the treatment of HIV infection and immune disease. Ozone therapy was not shown to enhance immune activation or diminish HIV virus.
  • Autohemotherapy, a therapy in which blood is withdrawn from the body, infused with ozone, then replaced into the body, has been associated with transmission of viral hepatitis and with a possible case of dangerously lowered blood cell counts. Insufflation of the ear carries a risk of tympanic membrane ("ear drum") damage, and colon insufflation may increase the risk of bowel rupture. Consult a qualified health professional before undergoing any ozone-related treatment
  • St John's wort: St. John's wort is a perennial herb that grows up to 32 inches tall and is commonly found in many parts of the world, including eastern North America and the Pacific coast. Anti-viral effects of St. John's wort have been observed in laboratory studies, but were not found in one human study. Multiple reports of significant adverse effects and interactions with drugs used for HIV/AIDS, including protease inhibitors (PIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), suggest that patients being treated for HIV/AIDS should avoid this herb. Therefore, there is evidence to recommend against using St. John's wort in the treatment of patients with HIV/AIDS.
  • Avoid if allergic or hypersensitive to plants in the Hypericaceae family. Rare allergic skin reactions like itchy rash have been reported. Avoid with immunosuppressant drugs (such as cyclosporine, tacrolimus or myophenic acid). Avoid with non-nucleoside reverse transcriptase inhibitors or protease inhibitors. Avoid with organ transplants, suicidal symptoms or before surgery. Use cautiously with history of thyroid disorders. Use cautiously with drugs that are broken down by the liver, with monoamine oxidase inhibitors (MAOI) or selective serotonin reuptake inhibitors (SSRIS), digoxin, or birth control pills. Use cautiously with diabetes or with history of mania, hypomania or seasonal affective disorder. Avoid if pregnant or breastfeeding.

Function
  • Once HIV infects a human cell, the virus copies its own genetic makeup into the cell's DNA. This programs the human cell to produce new copies of HIV. The infected cell makes a long strand of genetic material that must be cut up and put back together in order to form new copies of HIV. The protease enzyme is responsible for "cutting up" these strands. Without the protease enzyme, the virus cannot replicate.
  • Protease inhibitors (PIs) prevent the protease enzyme from doing its job. Like a key fitting into a lock, PIs inhibit the activity of the protease enzyme. When protease is blocked, HIV makes copies of itself that are unable to infect new cells. Studies have shown that protease inhibitors can reduce the amount of virus in the blood and increase CD4 cell counts. These drugs have shown to effectively increase CD4 cell counts, even when counts are extremely low.

Types of protease inhibitors
  • Amprenavir(Agenerase®):
  • Amprenavir (Agenerase®) was approved by the U.S. Food and Drug Administration (FDA) on April 15, 1999. It is available in an oral gel capsule or oral solution.
  • Amprenavir is typically taken along with ritonavir (Norvir®). Patients typically take 1,200 milligrams of amprenavir along with 200 milligrams of ritonavir once a day. Alternatively, patients may take 600 milligrams of amprenavir with 100 milligrams of ritonavir twice a day. Adolescents ages 13-16 typically take 1,200 milligrams of amprenavir twice a day. The recommended dosages for children ages four to 12 or adolescents ages 13-16 who weigh less than 110 pounds, vary depending on the patient's weight. Patients should take medications exactly as prescribed by their healthcare providers. Patients should not switch formulations of amprenavir without first consulting their healthcare providers.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. Patients who take blood-thinning drugs (warfarin) or have low levels of vitamin K, should consult their healthcare providers to determine if the vitamin E in amprenavir interferes with treatment. Vitamin E supplements are not recommended in patients taking amprenavir because recent evidence suggests that regular use of high-doses of vitamin E may increase the risk of death (from "all causes") by a small amount.
  • Patients who are taking sildenafil (Viagra®) should consult their healthcare providers because amprenavir may increase the risk of Viagra®-related side effects, including low blood pressure, changes in vision, or penile erection lasting more than four hours.
  • Use cautiously with diabetes medications because amprenavir may increase blood sugar. Amprenavir may cause a serious skin rash or hemolytic anemia (low levels of red blood cells).
  • Other more common side effects may include nausea, vomiting, diarrhea, numbness of the hands or feet, and a tingling sensation around the mouth. These side effects generally subside or disappear as the mediation is continued.
  • Avoid in patients who are pregnant or trying to become pregnant because amprenavir may cause birth defects if taken during pregnancy.
  • Tipranavir (Aptivus®):
  • Tipranavir (Aptivus®), also called TPV, was approved by the U.S. Food and Drug Administration (FDA) on June 22, 2005. Tipranavir is available in a 250 milligrams oral capsule. The drug must be taken at the same time as ritonavir (Norvir®). Tipranavir should be taken with food.
  • Patients typically take 500 milligrams of tipranavir, along with 200 milligrams (or 2.5 milliliters of solution) of ritonavir twice daily. Some patients may require alternative doses. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. For instance, tipranavir has been shown to interact with migraine medicines (ergot alkaloids), triazolam (Halcion®), astemizole (Hismanal®), pimozide (Orap®), cisapride (Propulsid®), quinidine (Quinaglute®), midazolam (Versed®), terfenadine (Seldane®), amiodarone (Pacerone®), bepridil (Vascor®), propafenone (Rythmol®), or flecainide (Tambocor®).
  • Some patients who are taking tipranavir with 200 milligrams ritonavir may develop severe liver disease that may lead to death. Patients should undergo regular blood tests to monitor liver function during treatment. Patients with liver diseases such as Hepatitis B and Hepatitis C may experience a worsening of their liver disease. Symptoms of severe liver disease may include tiredness, flu-like symptoms, loss of appetite, nausea, jaundice (yellowing of the skin and eyes), dark urine, pale stools, and pain or sensitivity on the right side below the ribs. Patients who experience these symptoms should consult their healthcare providers.
  • An estimated 10% of patients who take tipranavir develop mild to moderate rashes or sensitivity to sunlight. Limiting skin exposure to sunlight and wearing sunscreen may help reduce symptoms associated with sunlight sensitivity. Some patients who develop rashes also experience joint pain or stiffness, throat tightness, or generalized itching.
  • Hemophilic patients may experience an increase in bleeding.
  • Tipranavir may increase blood sugar levels and potentially lead to diabetes in some patients. Patients with diabetes before starting treatment may experience a worsening of symptoms, such as increased thirst and urination, flu-like symptoms, sores that heal slowly, swollen or tender gums and weight loss or weight gain. Some patients will need to change their current diabetes treatments.
  • Throughout treatment, a qualified healthcare provider should regularly monitor the patient's triglycerides and cholesterol (amount of fat in the blood) because some patients may experience dramatic increases in these levels. It is currently unknown whether tipranavir increases the likelihood of heart attack or stroke.
  • Changes in body fat may also occur in some patients. Tipranavir may cause fat to accumulate on the upper back and neck ("buffalo hump"), as well as in the breast, chest, and stomach area. Other patients may experience a loss of fat in the arms, legs, and/or face. The exact cause and long-term effects of these conditions remain unknown.
  • Common side effects include diarrhea, nausea, vomiting, stomach pain, tiredness, and headache. Women who are taking birth control pills have an increased risk of developing a skin rash.
  • Indinavir (Crixivan®):
  • Indinavir (Crixivan®) was approved by the U.S. Food and Drug Administration (FDA) on March 13, 1996 for the treatment of HIV in adults in combination with other antiretrovirals. Indinavir is an oral capsule, which is available in 100 milligram, 200 milligram, 333 milligrams, and 400 milligram strengths.
  • Indinavir should be taken on an empty stomach, either one hour before or two hours after eating a meal. This allows for better absorption of the drug in the intestine. Adults typically take 800 milligrams of indinavir every eight hours. Some patients, including those with liver disease, may require different doses. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. For instance, patients should not take indinavir if they are taking amiodarone (Cordarone®), ergot medications (Wigraine®, Cafergot®, Migranal®, Ergotrate®, or Methergine®), triazolam (Halcion®), astemizole (Hismanal®), lovastatin (Mevacor®), pimozide (Orap®), cisapride (Propulsid®), or simvastatin (Zocor® or Vytorin®).
  • Some patients may develop kidney stones, which can potentially lead to more severe kidney problems such as kidney failure, inflammation of the kidneys, or kidney infection. Drinking at least six, eight-ounce glasses of liquid each day may help reduce the likelihood of developing kidney stones.
  • Some patients experience hemolytic anemia (low levels of red blood cells in the body), which in some cases may be severe and even result in death. Patients may also experience severe liver problems, which may lead to liver failure or even death.
  • Indinavir may increase blood sugar levels and potentially lead to diabetes in some patients. Patients who have diabetes before starting treatment may experience a worsening of symptoms, and they may need to change their current diabetic medications.
  • Patients with hemophilia have an increased risk of bleeding.
  • Severe muscle pain and weakness have been reported in patients taking indinavir, along with cholesterol-lowering medicines called "statins," such as atorvastatin (Lipitor® or Torvast®) or fluvastatin (Lescol®).
  • Because some patients may experience dramatic increases in the levels of triglycerides and cholesterol (fat) in the blood, regular blood tests should be performed during treatment. It remains unknown whether indinavir increases the likelihood of heart attack or stroke.
  • Increases in bilirubin (yellow-red pigment of human bile in the liver) have occurred in about 14% of patients. In rare cases, this may lead to jaundice (yellowing of the skin and eyes).
  • Less serious side effects include change in sense of taste, diarrhea, nausea, vomiting, dizziness, drowsiness, fatigue, headache, stomach pain, and trouble sleeping. These symptoms generally subside or disappear as the medication is continued.
  • Saquinavir mesylate (Invirase®):
  • Saquinavir mesylate (Invirase®) was approved by the U.S. Food and Drug Administration (FDA) on November 7, 1997 for the treatment of HIV in combination with other antiretrovirals.
  • Saquinavir mesylate is available as a tablet and capsule, and it should be taken with food. It must be taken along with ritonavir (Norvir®), according to the FDA. Patients typically receive 1,000 milligrams of squinavir mesylate in combination with 100 milligrams of ritonavir twice daily. Some patients may require alternative doses. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any other medications (prescription or over-the-counter), herbs, or supplements because they may interact with treatment.
  • Common side effects include diarrhea, abdominal pain or discomfort, nausea, loss of appetite, ulcers in the mouth, dizziness, numbness of the hands or feet, headache, musculoskeletal pain, muscle pain, nausea, abnormal sensation (like burning or prickling on the skin), peripheral neuropathy (nerve disorder), itchy skin, and rash.
  • Rare side effects include confusion, loss of muscle coordination, muscle weakness, acute myeloblastic leukemia, hemolytic anemia (low levels of red blood cells), Stevens-Johnson syndrome, seizures, severe skin reaction associated with increased liver function tests, isolated elevation of transaminases, thrombophlebitis (inflammation of a vein that occurs when blood clots), headache, thrombocytopenia, worsening of chronic liver disease, jaundice (yellowing of the skin and eyes), fluid in the abdomen, drug fever, blisters, polyarthritis (inflammation of many joints), pancreatitis (inflammation of the pancreas), kidney stones, internal bleeding of the brain, peripheral vasoconstriction, high blood pressure, and intestinal obstruction.
  • Protease inhibitors may increase the risk of bleeding in hemophilic patients.
  • Because some patients may experience dramatic increases in the levels of triglycerides and cholesterol in the blood, regular blood tests should be performed during treatment. It remains unknown whether saquinavir mesylate increases the likelihood of heart attack or stroke.
  • Lopinavir/ritonavir (Kaletra®):
  • Lopinavir/ritonavir (Kaletra®) is a combination pill made from two protease inhibitors. The drug was approved by the U.S. Food and Drug Administration (FDA) on September 15, 2000. This combination pill was developed because lopinavir breaks down too quickly in the body if it is taken alone. Ritonavir prolongs the amount of time it takes to break down the pill, allowing for complete absorption of the drug.
  • Lopinavir/ritonavir is available as a tablet or oral solution. The tablets contain 200 milligrams of lopinavir and 50 milligrams of ritonavir. Every 5 milliliters of lopinavir/ritonavir oral solution contains 400 milligrams of lopinavir and 100 milligrams of ritonavir. Adults who have taken antiretroviral drugs before typically take two tablets or 5 milliliters of oral solution twice daily. Patients who have never received antiretroviral therapy before typically take four tablets once daily. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. If lopinavir/ritonavir is taken once daily, certain antiretrovirals, including amprenavir (Agenerase®), efavirenz (Sustiva®), nelfinavir (Viracept®), nevirapine (Viramune®), and phenytoin (Dilantin®), should be avoided. Lopinavir/ritonavir should not be taken with dihydroergotamine (D.H.E. 45®), ergonovine (Ergotrate®), ergotamine (Cafergot®, Ercaf®), triazolam (Halcion®), astemizole (Hismanal®), pimozide (Orap®), cisapride (Propulsid®), terfenadine (Seldane®), midazolam (Versed®), rifampin (Rimactane®, Rifadin®, Rifater®, or Rifamate®), fluticasone (Flonase®), lovastatin (Mevacor®), simvastatin (Zocor®), phenobarbital (Luminal® Sodium), carbamazepine (Tegretol®), or products containing the herb St. John's wort (Hypericum perforatum).
  • Use cautiously with sildenafil (Viagra®), tadalafil (Cialis®), or vardenafil (Levitra®) because lopinavir/ritonavir may increase the risk of developing side effects associated with these drugs.
  • Pancreatitis (inflammation of the pancreas) and liver problems, which can be fatal, have been reported in patients taking lopinavir/ritonavir.
  • The most commonly reported side effects of moderate severity include abdominal pain, abnormal bowel movements, diarrhea, fatigue, headache, and nausea. Children are more susceptible to side effects and have an increased risk of developing a skin rash.
  • Because some patients may experience dramatic increases in the levels of triglycerides and cholesterol in the blood, regular blood tests should be performed during treatment. It remains unknown whether lopinavir and ritonavir increase the likelihood of heart attack or stroke.
  • Fosamprenavir calcium (Lexiva®):
  • The U.S. Food and Drug Administration approved fosamprenavir calcium (Lexiva®) on October 20, 2003. Fosamprenavir calcium is available as a 700 milligrams oral tablet. This drug should not be taken with amprenavir (Agenerase®).
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. For instance, patients taking fosamprenavir calcium should not take triazolam (Halcion®), ergot medications (Cafergot®, Migranal® or D.H.E. 45®), cisapride (Propulsid®), midazolam (Versed®), pimozide (Orap®), simvastatin (Zocor®), lovastatin (Mevacor®), rifampin (Rifadin®), delavirdine mesylate (Rescriptor®), or any products containing the herb St. John's wort (Hypericum perforatum). Fosamprenavir calcium should not be taken with hormonal contraceptives (birth control pills) because it may reduce their safety and effectiveness.
  • Life-threatening drug interactions may occur if patients take medications, such as amiodarone (Cordarone®), intravenous lidocaine, amitriptyline HCl (Elavil®), imipramine pamoate (Tofranil®), tricyclic antidepressants, or quinidine (Quinaglute®), with fosamprenavir calcium.
  • Use cautiously with sildenafil (Viagra®), tadalafil (Cialis®), or vardenafil (Levitra®) because fosamprenavir calcium may increase the risk of developing side effects associated with these drugs.
  • Fosamprenavir calcium may increase blood sugar levels and can potentially lead to diabetes in some patients. Patients who are diagnosed with diabetes before starting antiretroviral therapy may experience a worsening of symptoms, and they may require changes in their current diabetic medications.
  • The most common side effects include diarrhea, headache, nausea, rash, and vomiting.
  • Ritonavir (Norvir®):
  • The U.S. Food and Drug Administration (FDA) approved ritonavir (Norvir®) on March 1, 1996 for the treatment of HIV in adults and children older than two years old.
  • Ritonavir is available as 800 milligrams/milliliter oral solution or 100 milligrams oral capsule. Both forms should be taken with food. Adults typically take 600 milligrams of ritonavir twice daily. The recommended doses for children vary, depending on the patient's weight. Pediatric doses should not exceed 600 milligrams twice a day. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment.
  • Pancreatitis (severe inflammation of the pancreas) is a serious side effect that may cause stomach pain, nausea, or vomiting. Other serious side effects may include changes in body fat distribution, increased bleeding in hemophilia patients, increased blood sugar levels (which may lead to the onset or worsening of diabetes symptoms), and increased triglyceride and cholesterol levels in the blood.
  • Other less serious side effects may include fatigue, burning or prickling sensation in the hands and/or feet, stomach pain, diarrhea, constipation, indigestion, gas, nausea, vomiting, loss of appetite, change in sense of taste, headache, dizziness, drowsiness, insomnia, fever, skin rash, sore throat, and increased sweating.
  • Darunavir (Prezista®):
  • The U.S. Food and Drug Administration (FDA) approved darunavir (Prezista®) on June 23, 2006 for the treatment of HIV in adults.
  • Darunavir is available as a 300 milligrams oral tablet. Adults typically take 600 milligrams of darunavir in combination with 100 milligrams of ritonavir (Norvir®) twice daily. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. Darunavir may interact with estrogen-based contraceptives (birth control pills), antiarrhythmics (used to treat irregular heart beat), anticoagulants (blood thinners), anticonvulsants (anti-seizure drugs), anti-depressants, anti-infectives (drugs that treat bacterial infections), antifungals (drugs that treat fungal infections), antimycobacterials (drugs that treat bacterial infections), corticosteroids (drugs that treat inflammation or asthma), HMG-CoA reductase inhibitors (drugs that lower cholesterol), immunosuppressants, narcotic analgesics, PDE-5 inhibitors (drugs that treat erectile dysfunction), and selective serotonin reuptake inhibitors (drugs that treat depression, anxiety, or panic disorder). Avoid with antihistamines (used to treat allergy symptoms), migraine medications, gastrointestinal motility agents, psychiatric drugs, or drugs that treat sleeping disorders because they may cause serious side effects.
  • In some patients, darunavir has caused severe or life-threatening rashes. Patients should contact their healthcare providers if a rash develops.
  • Other serious side effects may include changes in body fat distribution, increased bleeding in hemophilia patients, increased blood sugar levels (that may lead to the onset or worsening of diabetes symptoms), and increased triglyceride and cholesterol levels in the blood.
  • Patients with advanced HIV infection who have had opportunistic infections may develop symptoms of inflammation from previous infections soon after antiretroviral therapy is started. These symptoms are thought to be a sign that the body's immune system is improving because the body is now able to fight against infections.
  • The most common side effects include diarrhea, nausea, headache, sore throat, and common cold.
  • Atazanavir sulfate (Reyataz®):
  • The U.S. Food and Drug Administration (FDA) approved atazanavir sulfate (Reyataz®) on June 20, 2003 for the treatment of HIV in adults.
  • Atazanavir sulfate is available as an oral capsule in 100 milligram, 150 milligram, 200 milligram, and 300 milligram strengths. Adults who have received antiretrovirals before typically take 300 milligrams in combination with 100 milligrams of ritonavir (Norvir®) once daily. Adults who have never received antiretrovirals before typically take 400 milligrams of atazanavir sulfate once daily. Patients should always take medications exactly as prescribed. Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment.
  • Serious side effects may include jaundice (yellowing of the skin or eyes), irregular heartbeat, increased blood sugar levels (that may lead to the onset or worsening of diabetes symptoms), diarrhea, increased risk of bleeding in hemophilic patients, changes in body fat distribution, blood in the urine, and nausea. Patients who have liver diseases, such as hepatitis B or C, may experience a worsening of symptoms when taking atazanavir sulfate.
  • Other, less severe, side effects may include headache, stomach pain, skin rash, vomiting, depression, cough, difficulty sleeping, fatigue, back pain, joint pain as well as numbness, tingling, or burning of the hands or feet.
  • Some patients taking atazanavir sulfate in combination with other antiretrovirals called nucleoside analogues may develop lactic acidosis syndrome. This life-threatening condition is a severe buildup of acid in the blood. Lactic acidosis syndrome is a medical emergency that must be treated in the hospital. Symptoms of lactic acidosis syndrome include nausea, vomiting, or unexpected stomach discomfort, fatigue, and difficulty breathing.
  • Nelfinavir mesylate (Viracept®):
  • The U.S. Food and Drug Administration (FDA) approved nelfinavir mesylate (Viracept®) on March 14, 1997 for the treatment of HIV and for the prevention of HIV infection in individuals who have been exposed to the virus.
  • Nelfinavir mesylate is available as a 500 milligram oral suspension (powder) and 250 milligram, or 625 milligram oral tablets. Adults typically take 1,250 milligrams twice daily or 750 milligrams three times a day. The recommended dose for children ages two years and older varies depending on their weight. Patients should always take medications exactly as prescribed.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment. For instance, nelfinavir mesylate should not be taken with amiodarone (Cordarone®), triazolam (Halcion®), midazolam (Versed®), pimozide (Orap®), rifampin (Rifadin®), simvastatin (Zocor®), lovastatin (Mevacor®), ergot medicines (D.H.E. 45®), or products containing the herb St John's wort.
  • Serious side effects may include changes in body fat distribution, increased bleeding in hemophilia patients, increased blood sugar levels (that may lead to the onset or worsening of diabetes symptoms), and increased triglyceride and cholesterol levels in the blood.
  • Other less serious side effects may include gas, diarrhea (mild to moderate), nausea, and skin rash. These symptoms generally subside or disappear as treatment continues.

Copyright © 2011 Natural Standard (www.naturalstandard.com)


The information in this monograph is intended for informational purposes only, and is meant to help users better understand health concerns. Information is based on review of scientific research data, historical practice patterns, and clinical experience. This information should not be interpreted as specific medical advice. Users should consult with a qualified healthcare provider for specific questions regarding therapies, diagnosis and/or health conditions, prior to making therapeutic decisions.

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