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Non-nucleoside reverse transcriptase inhibitors

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Related Terms
  • Achlorhydria, acquired immune deficiency syndrome, acquired immunodeficiency syndrome, AIDS, antiretrovirals, antiretroviral therapy, ART, CD4 cells, delavirdine, efavirenz, fusion inhibitors, immune, immune defense system, immunocompromised, immunodeficiency, HAART, highly active antiretroviral therapy, HIV, human immunodeficiency virus, nevirapine, nucleoside reverse transcriptase inhibitors, nucleotide reverse transcriptase inhibitors, OI, opportunistic infections, protease inhibitors, reverse transcriptase, reverse transcriptase inhibitors, suppressed virus, viral infection, viral suppression, virus, weakened immune system, white blood cells.

Background
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs), also called non-nucleoside analogues, are a type of medication called antiretrovirals. They are used to treat patients with HIV (human immunodeficiency virus). These drugs interfere with the virus' ability to multiply. Although they are not curative, these drugs have been shown to effectively slow the replication of the virus in the body when taken in combination with other antiretrovirals. As a result, the patient's immune system is strengthened and the patient has an increased life expectancy.
  • Currently, the U.S. Food and Drug Administration (FDA) has approved three NNRTIs, including delavirdine (Rescriptor®), efavirenz (Sustiva®), and nevirapine (Viramune®)
  • HIV primarily targets the body's CD4 T-cells, which are white blood cells that help coordinate the immune system's response to infection and disease. Therefore, HIV patients are vulnerable to opportunistic infections. These infections occur in patients who have weakened immune systems. Some opportunistic infections may lead to the development of AIDS (acquired immune deficiency syndrome).
  • Antiretrovirals are able to suppress HIV, which boosts the patient's immune system. These drugs have also been shown to dramatically slow the progression of opportunistic infections.
  • HIV patients typically receive a combination of antiretroviral drugs because a single patient may have several different strains (types) of the virus circulating in the blood. The different strains of the virus may respond differently to specific types of drugs. Therefore, highly active antiretroviral therapy (HAART), which is a combination of drugs from at least two different classes, is recommended. There are four major classes of antiretrovirals: fusion inhibitors, protease inhibitors, nucleoside reverse transcriptase inhibitors (NRTIs), and non-nucleoside reverse transcriptase inhibitors (NNRTIs). Each drug class disrupts different stages of HIV's life cycle.

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

Bibliography
  1. AIDS. . Accessed May 25, 2007.
  2. AIDSmeds.com. . Accessed May 25, 2007.
  3. De Clercq E. Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future. Chem Biodivers. 2004 Jan;1(1):44-64. .
  4. Natural Standard: The Authority on Integrative Medicine. . Copyright © 2007. Accessed May 25, 2007.
  5. Rivero A, Mira JA, Pineda JA. Liver toxicity induced by non-nucleoside reverse transcriptase inhibitors. J Antimicrob Chemother. 2007 Mar;59(3):342-6. Epub 2007 Jan 25. .
  6. U.S. Food and Drug Administration (FDA). . Accessed May 25, 2007.
  7. Vrouenraets SM, Wit FW, van Tongeren J, et al. Expert Opin Pharmacother. 2007 Apr;8(6):851-71. .
  8. Waters L, John L, Nelson M. Non-nucleoside reverse transcriptase inhibitors: a review. Int J Clin Pract. 2007 Jan;61(1):105-18. .

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, and 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 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 a 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 a history of esophageal stricture, ileus, gastrointestinal stricture, or bowel obstruction. Avoid with a 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 a 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 behaviors 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 a 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 that 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 a 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 that is derived from two sources: retinoids and carotenoids. Retinoids are found in animal sources (such as 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 the 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 the 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 Hypericaceaefamily. 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 a 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 a history of mania, hypomania, or seasonal affective disorder (SAD). Avoid if pregnant or breastfeeding.

Function
  • Normally, the HIV enzyme called reverse transcriptase uses the nucleic acids (building blocks) inside the patient's cell to multiply. When patients take non-nucleoside reverse transcriptase inhibitors (NNRTIs), the drug attaches to HIV's enzyme before it can use the patient's nucleic acid to multiply. As a result, the virus' ability to replicate and infect new cells is significantly reduced.
  • NNRTIs have been shown to decrease the amount of viral particles in the patient's blood (viral load), boost the immune system, and increase life expectancy.

General precautions
  • Patients should always take their medications exactly as prescribed by 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 should tell their healthcare providers if they have any other medical conditions, especially liver disease or kidney disease, because alternative doses or medications may be needed.
  • Patients should tell their healthcare providers if they are pregnant, think they may be pregnant, or are trying to become pregnant because some antiretrovirals are unsafe during pregnancy and may cause birth defects in the baby.
  • Antiretrovirals do not reduce the risk of transmitting HIV to others. Even if antiretrovirals are able to suppress the virus to undetectable levels, it can still be transmitted to others.
  • Antiretrovirals do not cure HIV/AIDS. However, they have been shown to significantly reduce the amount of HIV in the blood.

Treatment adherence
  • In order for anti-HIV drugs to work correctly, they must be taken exactly as prescribed. Skipping doses or not taking the medications correctly can cause the amount of an antiretroviral drug to decrease in the bloodstream. If the drug level becomes too low, HIV can begin reproducing more quickly. The faster HIV reproduces, the more mutations occur, including those that may be resistant to drugs.
  • When a patient becomes resistant to a drug, the medication is no longer effective, even if it is taken in the future. If a patient becomes resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI), he/she may also be resistant to other drugs within the same class. As a result, patients may have fewer treatment options.
  • According to several studies, HIV patients must be more than 95% adherent to their treatment plans in order for them to remain effective. This means that missing more than one dose a month could decrease the drug's ability to treat HIV.
  • Healthcare providers evaluate the effectiveness of treatments by measuring the patients' CD4 cell counts. These immune cells are the primary targets of HIV. If the CD4 cell count is maintained, the likelihood of the virus mutating into resistant strains is decreased.

Delavirdine (rescriptor®)
  • The U.S. Food and Drug Administration (FDA) approved delavirdine (Rescriptor®) on April 4, 1997 for the treatment of HIV in adults in combination with other antiretrovirals. It is usually combined with two other nucleoside reverse transcriptase inhibitors.
  • Delavirdine is available in tablet form in 100 milligram and 200 milligram strengths. The tablet is usually swallowed. However, the 100-milligram tablet can be dissolved in water if the patient is unable to swallow pills.
  • Adults typically take 400 milligrams three times daily. Some patients may require different doses. Patients should take medications exactly as prescribed by their healthcare providers. If patients are also taking the antiretroviral didanosine (Videx®) or antacids (such as Pepcid®), patients should wait at least one hour before taking delavirdine. This is because delavirdine needs stomach acids in order to be absorbed properly. If patients have a condition called achlorhydria, in which the body does not produce enough stomach acids, patients should take delavirdine with acidic liquids, such as orange juice or cranberry juice. Avoid with liver disease.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements. Delavirdine has been shown to interact with antibiotics, such as rifapentine (Priftin®), rifabutin (Mycobutin®), and rifampin (Rifadin®); antihistamines, such as astemizole (Hismanal®); acid reflux/heartburn drugs, such as cisapride (Propulsid®), cimetidine (Tagamet®), famotidine (Pepcid®), ranitidine (Zantac®), lansoprazole (Prevacid®), esomeprazole (Nexium®), omeprazole (Prilosec®), and pantoprazole (Protonix®); sedatives, such as midazolam (Versed®) and triazolam (Halcion®); ergot medications for migraines (such as Wigraine® and Cafergot®), and cholesterol lowering drugs, such as simvastatin (Zocor®) and lovastatin (Mevacor®).
  • Although other non-nucleoside reverse transcriptase inhibitors (NNRTIs) have been shown to decrease the effectiveness of birth control pills, it remains unknown whether delavirdine has similar effects.
  • Delavirdine has been shown to increase levels of all protease inhibitors. Therefore, doses of protease inhibitors may need to be decreased in patients who are also taking delavirdine.
  • Serious side effects may include severe skin rash that causes blisters and is accompanied by muscle or joint pain, fever, redness, swelling of the eyes, and sores in the mouth. Other severe symptoms may include kidney damage, anemia (low levels of iron in the blood), and liver or muscle damage. Patients should tell their healthcare providers if any of these side effects develop.
  • Delavirdine has been shown to increase blood levels of erectile dysfunction drugs, such as sildenafil (Viagra®) and vardenafil (Levitra®). Therefore, doses of these drugs may need to be decreased in patients taking delavirdine.
  • Many HIV patients develop a less serious skin rash on the upper body and arms one to three weeks after starting the medication. This rash usually clears up in about two weeks. Other less serious side effects may include headache, fatigue, vomiting, nausea, and diarrhea. These side effects generally lessen over time.

Efavirenz (sustiva®)
  • The U.S. Food and Drug Administration (FDA) approved efavirenz (Sustiva®), also called EFV, September 17, 1998 for the treatment of HIV with other antiretrovirals (usually two nucleoside reverse transcriptase inhibitors) in patients ages three and older. Efavirenz has also been used in combination with other antiretrovirals to prevent the transmission of HIV in patients who were accidentally exposed to the virus at work.
  • Efavirenz is taken by mouth as a capsule or tablet. A liquid formulation is currently under development. This drug can be taken with or without food. However, it should not be taken with a high-fat meal because this reduces the amount of drug that is able to be absorbed into the blood.
  • According to the U.S. Department of Health and Human Services (DHHS) treatment guidelines, efavirenz is the recommended non-nucleoside reverse transcriptase inhibitor (NNRTI) for HIV patients who are just starting treatment.
  • Adults and children who weigh more than 88 pounds typically take 600 milligrams once daily. Pediatric doses for children who way less than 88 pounds is dependent on weight. Some patients 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. Efavirenz has been shown to interact with other drugs, including cisapride (Propulsid®), midazolam (Versed®), triazolam (Halcion), and ergot medicines (like Cafergot®). Also, efavirenz may reduce the effectiveness of birth control pills. A second method of birth control is recommended. Avoid if pregnant or thinking of becoming pregnant because efavirenz may cause birth defects.
  • Serious side effects may include confusion, hallucinations (seeing or hearing things that are not there), and memory loss. There have been a few reports of depression, paranoia, and suicidal thoughts, which is more common among patients with a history of mental illnesses. Some patients may develop a severe rash that causes blisters. Patients should tell their healthcare providers if they experience any of these side effects.
  • Other less serious side effects may include diarrhea, nausea, difficulty sleeping, abnormal dreams, dizziness, headache, and difficulty concentrating. These side effects generally lessen over time. Because efavirenz may cause dizziness, some healthcare providers recommend taking it before bed.
  • Efavirenz may cause patients to test positive for marijuana during a test for illicit drug use. Patients should tell the person collecting a urine sample that they are taking efavirenz. That way, the laboratory technician can consider a more sensitive drug test to prevent a false-positive result.

Nevirapine (viramune®)
  • The U.S. Food and Drug Administration (FDA) approved nevirapine (Viramune®) on June 21, 1996 for the treatment of HIV with other antiretrovirals (usually two nucleoside reverse transcriptase inhibitors) in adults and children.
  • Nevirapine is available as an oral tablet and a powder that is mixed with liquid (oral suspension).
  • Adults typically take 200 milligrams once daily for the first 14 days, followed by 200 milligrams twice daily. Pediatric doses are dependent on age and weight. No patient should receive doses greater than 400 milligrams a day. Patients with kidney problems who are on dialysis generally take a 200-milligram tablet after each treatment. Patients should always take medications exactly as prescribed.
  • Recent research shows that nevirapine can pass into the brain, which may help suppress HIV that is infecting brain cells. When HIV infects brain cells, conditions, such as AIDS-related dementia, may develop. Studies suggest that nevirapine may help treat and prevent the risk of developing such conditions.
  • Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements. Nevirapine has been shown to interact with other drugs including antibiotics such as rifampin (Rifadin®) and rifapentine (Priftin®) and antifungals such as ketoconazole (Nizoral®). Also, nevirapine may reduce the effectiveness of birth control pills. A second method of birth control is recommended. Nevirapine has been shown to decrease the amount of ethinyl estradiol in the blood, which can increase the risk of pregnancy.
  • Nevirapine has been shown to reduce the amount of several protease inhibitors in the blood, including atazanavir (Reyataz®), saquinavir (Invirase®), indinavir (Crizivan®), lopinavir/ritonavir (Kaletra®), fosamprenavir (Lexiva®), and amprenavir (Agenerase®). Therefore, doses of these protease inhibitors may need to be increased if taken with nevirapine.
  • Nevirapine has been shown to increase the amount of some protease inhibitors, including nelfinavir (Viracept®) and ritonavir (Norvir®), in the blood. Therefore, doses of these protease inhibitors may need to be decreased if taken with nevirapine.
  • If patients develop severe skin rashes, sore throat, chills, fever, or other flu-like symptoms, they should consult their healthcare providers immediately because they may be signs of liver damage.
  • Other less serious side effects may include diarrhea, stomach pain, nausea, and headache. These symptoms generally lessen over time.

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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