What are the drugs that treat HIV?
Treatment for HIV (human immunodeficiency virus) infections has advanced mightily in the decades since the global pandemic in the 1980s, but there is still no cure. That means people with the infection must stay on antiviral therapy for their entire lives to stave off AIDS (acquired immune deficiency syndrome). AIDS is the condition in which the HIV overwhelms the body’s immune system, leaving the infected person vulnerable to opportunistic bacteria, fungi, and cancers that eventually kill them.
There is no evidence people infected with HIV can currently be cured. In general, those who are treated for years and are repeatedly found to have no virus in their blood by standard viral load assays will experience a prompt rebound in the amount of virus when therapy is discontinued. Consequently, the decision to start therapy must balance the risks versus the benefits of treatment. The risks of therapy include the short- and long-term side effects of the drugs, described in subsequent sections, as well as the possibility that the virus will become resistant to the therapy, which can limit options for future treatment. The risks of both of these problems are quite small with the treatment options currently available.
Still, it’s important to know the potential side effects of all the drugs you take, as well as potential drug interactions. All of the NNRTIs (nonnucleoside analogue reverse transcriptase inhibitors), for example, are associated with important drug-drug interactions so they must be used with caution in patients on other medications. The following is a list of the standard treatment medication classes used in managing HIV:
- nucleoside and nucleotide analogue reverse transcriptase inhibitors (NRTIs)
- nonnucleoside analogue reverse transcriptase inhibitors (NNRTIs)
- protease inhibitors
- fusion inhibitors
- CCR5 antagonists
- integrase strand transfer inhibitors, and
- entry inhibitors
This article will discuss some of the most common and most dangerous side effects in each drug class. This is by no means a comprehensive list. People should read the package information and discuss with their doctor or pharmacist each drug they are prescribed.
What are the side effects of NRTIs?
D4T (stavudine) can damage nerves and cause peripheral neuropathy, a neurological condition with numbness and/or tingling of the feet and hands, and inflammation of the pancreas (pancreatitis) that causes nausea, vomiting, and mid/upper abdominal pain.
DDI (didanosine) also causes pancreatitis and, to a lesser extent, peripheral neuropathy. Peripheral neuropathy can become permanent and painful, and pancreatitis can be life-threatening if therapy is not discontinued. The drug ddC also is associated with peripheral neuropathy, as well as oral ulcers.
ABC (abacavir) can cause a hypersensitivity reaction during the first two to six weeks of therapy in approximately 5% of individuals. The hypersensitivity reaction most often causes fever and other symptoms, such as muscle aches, nausea, diarrhea, rash, or cough. The symptoms generally get worse with each dose of ABC and, if suspected, therapy must be discontinued and never restarted for fear of developing a life-threatening reaction. There is now a simple blood test (HLA-B*5701) that can be performed to determine whether a patient is at risk for developing the hypersensitivity reaction. If the test is positive, the patient should never receive this medication. There is also conflicting data stating that abacavir may or may not be associated with increased risk of cardiovascular events.
TDF (tenofovir) is generally well tolerated although there may be rare kidney damage and may have a greater impact on reducing bone density than other agents. Both of these problems appear to be attenuated with the new formulation of tenofovir called TAF.
FTC (emtricitabine)is also well tolerated except for the occasional development of hyperpigmentation, most often on the palms and soles. This hyperpigmentation occurs more frequently in people of color.
Although all NRTIs can be associated with lactic acidosis (a serious condition in which lactic acid accumulates in the blood), it may occur more often with some drugs, such as D4T. Although this complication of treatment is rare, it can be severe and life-threatening. Early symptoms of lactic acidosis are nausea, fatigue, and sometimes shortness of breath. Lactic acidosis needs to be watched for and, if suspected, requires that therapy be discontinued until symptoms and laboratory test abnormalities resolve.
There has been a great deal of attention given to the more recently identified problem of "lipodystrophy." Individuals suffering from this syndrome can be categorized as having lipohypertrophy (fat accumulation) syndromes, such as the "buffalo hump" on the back of the neck, breast enlargement, or increased abdominal girth. Others primarily suffer from lipoatrophy with fat loss under the skin with complaints of prominent veins on the arms and legs, sunken cheeks, and decreased gluteal (buttock) size. These syndromes appear to be related to multiple factors, including, but not limited to, drug therapy. The NRTIs appear to be most closely linked to lipoatrophy, in particular D4T and to a lesser extent ZDV. In fact, some studies have suggested slow accumulation of fat in those who modify the NRTI component of their regimen. Some NRTIs also have been linked to elevation in lipid (fat) levels in the blood. While switching therapy is always a consideration in those experiencing potential drug-related toxicity, this should only be done under the careful supervision of an experienced HIV provider.
What are the side effects of NNRTIs?
The most common side effect associated with NNRTIs is a rash, typically occurring during the first weeks of therapy. This is most common in individuals treated with NVP (nevirapine). In this case, the overall risk of rash is reduced if therapy is started as a single 200 mg NVP pill once per day during the first two weeks before increasing to the full dose of 200 mg twice per day. If the rash is mild, therapy usually can be continued if antihistamines are given, and if the rash resolves, treatment with the NNRTI can be continued. If the rash is severe, associated with liver inflammation or blisters, changes in the mouth or around the eyes, or with high fevers, therapy with the NNRTI usually needs to be discontinued. Decisions regarding continuing or stopping treatment need to be made with the primary care professional. In some patients, NVP can cause a severe allergic reaction characterized by fever, rash, and severe liver inflammation. Recent data suggests that the groups at the greatest risk for the severe reaction are those with stronger immune systems, such as HIV-uninfected people given this treatment after an exposure to HIV, women with CD4+ T cells >250 cells per mm3, and men with CD4+ T cells >400 cells per mm3. There is also likely to be increased risk in pregnant women and individuals with other underlying liver diseases. Consequently, NVP probably should not be used in any of these groups, or if used, used with caution. In addition, whenever NVP is started, liver tests that are markers for liver inflammation should be monitored at regular intervals during the first several months of treatment.
Side effects associated with EFV (efavirenz) are mostly dizziness, confusion, fatigue, and vivid dreams. These tend to be most prominent during the first weeks of therapy and then often decrease in severity. It is generally recommended that EFV be taken at bedtime so that the patient is asleep during the time dizziness and confusion may be most severe. It is also noteworthy that there may be an increased risk of depression associated with the use of this drug, and it should be used with caution in those with poorly managed depression. Rash and liver inflammation can occur with both EFV and DLV (delavirdine), and these drugs may also be linked to abnormalities of lipids in the blood.
The most common side effect reported with the most recently approved NNRTI, ETR (etravirine), is rash and it was generally mild and rarely required that medications needed to be stopped. Side effects appear to be uncommon with RPV (rilpivirine) with some uncertainty as to whether it is associated with various neurologic symptoms.
All of the NNRTIs are associated with important drug-drug interactions so they must be used with caution in patients on other medications. There are numerous resources available to patients on these medications to make sure that they do not adversely interact with other HIV or non HIV-related drugs.
Latest HIV News
What are the side effects of protease inhibitors?
There are currently nine approved PIs that all have distinct toxicities. The most common side effects associated with these drugs are nausea and diarrhea, which occur more often with some PIs than others. For example, diarrhea is more common with NFV (nelfinavir) than other PIs but can occur with any and all drugs in this class. Many of the drugs in this class also increase blood lipid levels, some more than others with ATV (atazanavir) and DRV (darunavir) appearing to have less effect on lipids than other drugs in the class. Other unique toxicities associated with various PIs are kidney stones, kidney damage, and increases in blood bilirubin levels and potentially jaundice with IDV (indinavir) and ATV. Some of these drugs also have been associated with elevations in blood sugar levels and bleeding in hemophiliacs. Finally, little is known regarding the role these drugs may play in the development of lipodystrophy. There is also some data suggesting that LPV/RTV (lopinavir/ritonavir) and DRV may be associated with an increased risk of cardiovascular events.
Most PIs are associated with important drug-drug interactions so they must be used with caution in patients on other medications. There are numerous resources available to patients on these medications to make sure that they do not adversely interact with other HIV or non HIV-related drugs.
What are the side effects of fusion inhibitors?
The only drug in this class is T-20 (enfuvirtide), which is administered as a twice-daily subcutaneous injection. The most common side effects are redness and pain at the site of injection. Rarely, infection can occur at the injection site. There also are reports of generalized allergic reactions.
What are the side effects of CCR5 antagonists?
Although there were some early concerns of liver inflammation for drugs in this class, MVC (maraviroc) appeared to be well tolerated in clinical trials without any specific toxicities attributable to the drug. However, it is a new drug in a new class and the first to actually target the cell. For these reasons, longer follow-up from clinical trials and those followed in the clinic will be very important for assessing the overall safety of the drug. There are important drug-drug interactions with MVC, so it too must be used with caution in patients on other medications.
What are the side effects of integrase strand transfer inhibitors?
RAL (raltegravir) has not been strongly linked to any specific side effect in clinical trials. However, there have been some cases of muscle problems and of increasing depression that needs to be watched for when starting this or any new medications. EVG (elvitegravir) appears to be well tolerated when used as the fixed-dose combination of Stribild or Genvoya, with the anticipated effect on measures of kidney function and bone mineral density with Stribild and COBI component (cobicistat) of the regimen being associated with drug-drug interactions. DTG (dolutegravir) has been associated with mild headache, insomnia, and nausea in some patients and like COBI is associated with mild early decrease in measures of renal function that actually do not reflect true kidney damage.
Subscribe to MedicineNet's General Health Newsletter
Health Solutions From Our Sponsors
DHHS Panel on Antiretroviral Guidelines for Adults and Adolescents. "Guidelines for the Use of Antiretroviral Agents in HIV-1 Infected Adults and Adolescents." Washington D.C.: Department of Health and Human Services, 2018. <https://aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf>
Top What Are the Side Effects of HIV Medications Related Articles
Biktarvy (bictegravir, emtricitabine, and tenofovir alafenamide)Biktarvy (bictegravir, emtricitabine, and tenofovir alafenamide) is a prescription medicine that is used without other anti-HIV-1 medicines to treat Human Immunodeficiency Virus-1 (HIV-1) in adults and children who weigh at least 55 pounds (25 kg). Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), and may occur with discontinuation of Biktarvy. Do not take Biktarvy if pregnant or breastfeeding.
Can HIV be Cured Naturally?HIV stands for human immunodeficiency virus. If someone has HIV it means that they have been diagnosed with the HIV infection. AIDS (acquired immune deficiency syndrome); however, is the most advanced or final stage of the HIV infection. It is important to get tested for HIV in the early stages of infection to minimize the damage to the immune system. Successful treatment aims to reduce HIV load to a level that is harmless to the body.
HIV Early Signs and StagesHuman immunodeficiency virus or HIV, destroys important cells that fight disease and infection, which weakens a person's immune system. Some people with HIV don’t have any signs or symptoms. Early signs and symptoms of HIV infection include mononucleosis-like or flu-like symptoms, which include body aches, fever, and headache. Signs and symptoms begin around seven or eight years after HIV infection, which include weight loss, loss of energy and appetite, and swollen lymph nodes. There are 3 stages of HIV.
HIV/AIDS Facts: What Is HIV?
HIV (human immunodeficiency virus) is the precursor infection to AIDS (acquired immunodeficiency syndrome). HIV is transmitted through blood and genital secretions; most people get it through sexual contact or sharing needles for illegal IV drug use. HIV can be controlled by a strict drug regimen, but left unchecked, it leads to AIDS. In AIDS, the immune system collapses and the body falls prey to secondary, opportunistic infections and cancers that typically kill the person.
HIV/AIDS Infection Transmission and PreventionHIV (human immunodeficiency virus) is spread through contact with genital fluids or blood of an infected person. The spread of HIV can occur when these secretions come in contact with tissues such as those lining the vagina, anal area, mouth, eyes (the mucus membranes), or with a break in the skin, such as from a cut or puncture by a needle.
HIV/AIDS Testing: Diagnosis and MonitoringHIV/AIDS diagnosis and monitoring have come a long way from the days when a diagnosis was a death sentence. Crucial parts of the effective treatment regimens developed in the last 40 years are consistent monitoring of the viral load (the amount of virus in the blood), and the immune cell count, which function as biological markers of the disease’s progression. Doctors also must test for drug resistance.
HIV Medications List and Drug ChartsThe ultimate goal of HIV treatment is getting the viral load down below detectable levels. As long as those viral load and antibody levels are below a proscribed range, people with HIV can stave off AIDS and other serious symptoms. Antiviral treatment options usually include combinations of two NRTIs, often referred to as "nucs," and a third drug, typically being a boosted protease inhibitor, a NNRTI, often called "non-nucs," and integrase strand transfer inhibitors.
HIV vs. AIDSHuman immunodeficiency virus causes HIV infection. Acquired immunodeficiency syndrome (AIDS) is a condition that results after HIV has extensively damaged a person's immune system. Risk factors for HIV and AIDS include use of contaminated needles or syringes, unprotected sex, STDs, receiving a blood transfusion prior to 1985 in the United States, having many sex partners, and transmission from a mother to her child.
How Do You Feel When You Have HIV?About four weeks after contracting HIV (human immunodeficiency virus), you may experience flu-like symptoms including fever, rash, sore throat, nausea, swollen glands and achy joints. You may remain symptomless for some time, however. That doesn't mean you don't need treatment; HIV can quickly progress into AIDS, in which the immune system collapses and you die of a secondary cancer or infection.
How Long Does It Take to Notice Signs of HIV?HIV (human immunodeficiency virus) is a virus that attacks and damages the cells of the immune system in the body. If left untreated, HIV can lead to the AIDS (acquired immunodeficiency syndrome) disease. AIDS is the final stage of HIV infection which occurs when the body’s immune system is severely damaged because of the virus and unusual infections result. Untreated, HIV infection has a mortality of 90%.
Human Immunodeficiency Virus (HIV)
HIV (human immunodeficiency virus) infection left untreated causes AIDS (acquired immunodeficiency syndrome). Still incurable, AIDS describes immune system collapse that opens the way for opportunistic infections and cancers to kill the patient.
- Early symptoms and signs of HIV infection include flu-like symptoms and fungal infections, but some people may not show any symptoms for years.
- Highly active antiretroviral therapy (ART) is the standard treatment for HIV infection. These combination drug regimens have made HIV much less deadly, but a cure or vaccine for the pandemic remains out of reach.
- HIV is usually transmitted through sexual contact or sharing IV drug needles, but can also infect someone through contact with infected blood.
- Sexual abstinence, safe sex practices, quitting IV drugs (or at least using clean needles), and proper safety equipment by clinicians and first responders can drastically reduce transmission rates for HIV/AIDS.
What Are the Four Stages of HIV?The World Health Organization (WHO) classifies human immunodeficiency virus (HIV) into four stages. Stage 1 (HIV infection): The CD4+ cell count is at least 500 cells per microliter. Stage 2 (HIV infection): The CD4+ cell count is 350 to 499. Stage 3 (advanced HIV disease or AHD): The CD4+ cell count is 200 to 349. Stage 4 (Acquired immunodeficiency syndrome [AIDS]): The CD4+ cell count is less than 200.
What Is the Difference Between HIV-1 and HIV-2?There are two main types of the human immunodeficiency virus (HIV), HIV-1 and HIV-2. HIV-1 is the most common type of HIV and accounts for 95% of all infections, whereas HIV-2 is relatively uncommon and less infectious. HIV-2 is mainly concentrated in West Africa, is less deadly and progresses more slowly.
What Is Usually the First Sign of HIV?Human immunodeficiency virus (HIV) attacks the cells of the immune system, leading to AIDS and death if left untreated. The first signs of the human immunodeficiency virus infection are flu-like symptoms, which mainly start around two to four weeks after getting HIV. This stage is known as acute HIV infection.
When should you start HIV medication?Nearly everyone who is infected with HIV (human immunodeficiency virus) should start antiviral medication therapy as soon as they are diagnosed. Older guidelines recommended delaying treatment to help reduce the potential for drug side effects and viral resistance to treatment. Current thinking theorizes that early treatment may preserve more of the body's immune function.