Types of HIV Medications

There is no cure for HIV, but treatments to help minimize the impact of the virus on people who have been infected, and preventive medications can lower the risk of HIV transmission. There are over 48 U.S. Food and Drug Administration (FDA)-approved drugs to treat HIV today.

Your healthcare provider will decide which drug you should take depending on your viral load, T cell count, what strain of HIV you have, how severe your infection is, other drugs you are taking, and other illnesses. Typically, HIV is treated with at least two medications at the same time to attack the virus and prevent resistance to the medication. 

Medications that Reduce HIV 

Antiretroviral therapy (ART) is prescribed for people who are infected to reduce the viral load (amount of HIV in the body of someone who is infected).

HIV attacks and destroys the infection-fighting CD4 cells of the immune system. Loss of these cells makes it hard for the body to fight off infections and diseases. ART prevents the virus from multiplying. Having less HIV in the body gives the immune system a chance to produce more CD4 cells that help defend the body from infections and diseases.

The ART drugs used for treating HIV are divided into seven drug classes based on how each drug interferes with the HIV life cycle, including:

• Nucleoside reverse transcriptase inhibitors (NRTIs)
• Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
• Protease inhibitors (PIs)
• Fusion inhibitors
• CCR5 antagonists
• Post-attachment inhibitors
• Integrase strand transfer inhibitors (INSTIs)

Treatment with ART is recommended for everyone who is HIV-positive, as soon as possible. A person's initial HIV regimen generally includes three HIV medicines from at least two different HIV drug classes. 

Nucleoside Reverse Transcriptase Inhibitors (NRTIs) 

NRTIs are the most effective form of ART. When HIV enters a healthy cell, it attempts to make copies of itself by using an enzyme called reverse transcriptase. NRTIs work by blocking that enzyme so HIV can't make new copies of itself.

NRTIs are the first class of antiretroviral drugs to be approved by the FDA. Many NRTIs are used in combination with other drugs that rapidly reduce the HIV retrovirus.

Different NRTI drugs include:

• Ziagen (abacavir)
• Emtriva (emtricitabine)
• Epivir (lamivudine)
• Viread (tenofovir disoproxil fumarate)
• Retrovir (zidovudine)

An HIV-positive individual usually starts on two NRTIs followed by either an NNRTI, a protease inhibitor (with ritonavir boosting), or an integrase inhibitor.

These medications can have serious and life-threatening side effects, including a buildup of lactic acid in the blood (lactic acidosis), liver problems, and pancreatitis. They can be used to treat HIV infection in adults, children, and infants.

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) 

NNRTIs stop the virus from replicating by binding to and later altering reverse transcriptase.

The currently available NNRTI drugs include:

• Pifeltro (doravirine)
• Sustiva (efavirenz)
• Intelence (etravirine)
• Viramune, Viramune XR (nevirapine)
• Edurant (rilpivirine) 

Serious side effects of these medications include immune reconstitution inflammatory syndrome (changes in your immune system), mental problems, and liver problems.

Integrase Inhibitors 

Integrase inhibitors block HIV integrase, another enzyme that HIV needs to make copies of itself. 

Integrase inhibitor drugs include:

• Isentress (raltegravir)
• Tivicay (dolutegravir)
• Vitekta (elvitegravir)
• Triumeq (dolutegravir + abacavir + lamivudine)
• Stribild (elvitegravir + cobicistat + tenofovir + emtricitabine)
• Genvoya (elvitegravir + cobicistat + tenofovir AF + emtricitabine)
• Juluca (dolutegravir + rilpivirine)
• Biktarvy (bictegravir + tenofovir AF + emtricitabine)

Integrase inhibitors have simple dosing schedules, fewer side effects, and are a preferred treatment choice. Their side effects include allergic reactions and liver problems.

Protease Inhibitors (PIs) 

PIs block HIV protease, another enzyme HIV needs to make copies of itself. Typically, PIs have to be taken three times a day due to their rapid metabolization. Drug toxicity is also common with this drug because it is taken so frequently.

PI drugs include:

• Reyataz (atazanavir)
• Prezista (darunavir)
• Lexiva (fosamprenavir)
• Lopinavir (available in the combination drug Kaletra)
• Norvir (ritonavir)
• Aptivus (tipranavir)

Many of these drugs must be taken as a combination drug, or if they are taken on their own, they should be taken with another type of HIV medication to complete the antiretroviral therapy.

Currently, ritonavir is prescribed as a booster in treatment. This means that it is utilized as an additional treatment in addition to other medication.

Indinavir, nelfinavir, and saquinavir are less commonly prescribed because they have more side effects, including nausea, headache, diarrhea, vomiting, weakness, and kidney stones.

Entry Inhibitors 

Entry inhibitors prevent HIV from affecting CD4 cells. While PIs, NRTIs, and NNRTIs impact the CD4 cell after HIV has invaded it, entry inhibitors prevent the virus from attaching to the surface of the CD4 cells. Therefore, HIV cannot enter the CD4 cell. Types of entry inhibitors include attachment inhibitors, coreceptor inhibitors, and fusion inhibitors.

Entry inhibitors can also be used for people who have become resistant to PIs, NRTIs, and NNRTIs.

Fusion Inhibitors 

Fusion inhibitors block HIV from entering the CD4 cells of the immune system. This medication is administered twice daily via subcutaneous injection. It can sometimes cause serious side effects like an allergic reaction or pneumonia.

The only fusion inhibitor available in the United States is enfuvirtide. Enfuvirtide is used for people whose infection is not well-controlled by ongoing treatment with other HIV medicines. It is not known if enfuvirtide is safe and effective for use in children younger than 6 years old. Enfuvirtide is always used in combination with other HIV medicines.

Chemokine Coreceptor Antagonists (CCR5 Antagonists)

This medication blocks CCR5 coreceptors (a protein on the surface of a cell that serves as a second binding site for a virus or other molecule) on the surface of certain immune cells that HIV needs to enter the cells. CCR5 antagonists are also rarely used in the United States. It can cause serious, life-threatening side effects, including liver and heart problems.

The only CCR5 antagonist available in the United States is maraviroc. It is always used in combination with other HIV medications. Maraviroc should only be used for people whose strain of HIV uses the CCR5 coreceptor. Your healthcare provider can determine this through a blood test. Maraviroc should not be used in premature newborns or children weighing less than 4.4 pounds.

Post-Attachment Inhibitors 

Post-attachment inhibitors block CD4 receptors on the surface of certain immune cells that HIV needs to enter the cells. They must be used with other medications for a complete HIV regimen. This medication prevents HIV from entering certain immune cells. 

The only post-attachment inhibitor approved by the FDA is Trogarzo (ibalizumab-uiyk). It is used to treat HIV infection for adults for whom other HIV medicines have not worked and who meet certain requirements, as determined by a healthcare provider.

 Attachment Inhibitors 

Attachment inhibitors bind to the gp120 protein on the outer surface of HIV, preventing HIV from entering CD4 cells. The only FDA-approved attachment inhibitor in the United States is Rukobia (fostemsavir), which was approved in 2020.

Combination Drugs

Combination HIV medicines contain two or more HIV medicines from one or more drug classes. Often, two to four antiretroviral drugs are prescribed to work in combination, sometimes in one drug form. This is called a single-tablet regimen (STR), which is typically used for people who are new to HIV medication.

Combination drugs that are made up of two or three NRTIs include:

• Trizivir (abacavir, lamivudine, and zidovudine)
• Epzicom (abacavir and lamivudine)
• Descovy (emtricitabine and tenofovir alafenamide fumarate)
• Truvada (emtricitabine and tenofovir disoproxil fumarate)
• Cimduo, Temixys (lamivudine and tenofovir disoproxil fumarate)
• Combivir (lamivudine and zidovudine)

Pharmacokinetic Enhancers 

Pharmacokinetic enhancers boost the effectiveness of HIV medications. When pharmacokinetic enhancers and ARV drugs are given together, the pharmacokinetic enhancer interferes with the breakdown of the other drug, which allows the drug to remain in the body longer at a higher concentration.

Examples of pharmacokinetic enhancers are:

• Norvir (ritonavir)
• Tybost (cobicistat)

Both agents inhibit CYP3A4, an enzyme that metabolizes protease inhibitors, with cobicistat being a more specific CYP inhibitor than ritonavir. Unlike ritonavir, cobicistat does not have antiretroviral activity.

Multidrug Combinations

Because HIV can mutate, taking a combination of antiretroviral drugs helps the drugs take on a tag team role to suppress HIV at various stages of its life cycle. Combination drugs are two or more different HIV medicines combined in one pill, and mostly stop the virus from mutating and replicating. It is also a more convenient regimen since patients only need to take one pill.

Examples of multidrug combinations that include NRTIs and NNRTIs are:

• Delstrigo (doravirine, lamivudine, and tenofovir disoproxil fumarate)
• Symfi, Symfi Lo (efavirenz, lamivudine, and tenofovir disoproxil fumarate)
• Atripla (efavirenz, emtricitabine, and tenofovir disoproxil fumarate)
• Odefsey (emtricitabine, rilpivirine, and tenofovir alafenamide fumarate)
• Complera (emtricitabine, rilpivirine, and tenofovir disoproxil fumarate)
• Dovato (dolutegravir, lamivudine)
• Juluca (dolutegravir, rilpirivine)

Pre-Exposure Prophylaxis (or PrEP)

PrEP is antiretroviral medication prescribed for people who are not infected with HIV but are at high risk of contracting it. It is known to reduce the risk of contracting HIV by 72% to 97%. PrEP should always be used in conjunction with condoms and frequent testing.

There are currently three approved prescription medications:

• Truvada (emtricitabine + tenofovir disoproxil fumarate) is a daily pill approved for those at risk for HIV through sex or injection drug use.
• Descovy (emtricitabine + tenofovir alafenamide) is a daily pill approved for sexually active men and transgender women at risk for HIV.
• Apretude (cabotegravir extended-release injectable suspension), which is approved for at-risk adults and teens, is an injectable given every two months.

High-risk groups who may benefit from PrEP include:

• Men who have sex with men and are not monogamous, engage in condomless sex, have had an STD within the last six months, or are in a serodiscordant relationship (where one partner is HIV positive)
• Heterosexual men or women who have condomless sex or are in a serodiscordant relationship
• Injecting drug users who share needles with others

Post-Exposure Prophylaxis (PEP)

PEP is used for people who believe that they might have been exposed to HIV within the past 72 hours through high-risk activities like sex or drug use. It can prevent the virus from taking hold in the body, but it only works if it's taken within 72 hours. Therefore, anyone who suspects they have been exposed to HIV should talk to their healthcare provider about PEP as soon as possible.

PEP is a 28-day course where a person will take Truvada once a day, plus 400 mg of the integrase inhibitor Isentress (raltegravir) or 50 mg of Tivicay (dolutegravir) once a day.

A Word From Verywell 

When your viral load is lowered while on medication, that means the medication is doing its job. Don’t ever stop taking your HIV medication. Learning about your antiretroviral treatment and what medications you are taking is imperative to your life with HIV. In addition to taking your medication, stop smoking, moderate your drinking, and stay up-to-date on vaccines.

Every medication has its own set of advantages and disadvantages. HIV medication comes in different shapes and forms. There is no one single regimen that is absolutely perfect for a patient. Your healthcare provider will work with you to ensure that you are getting the best treatment. 

People with HIV are living much healthier and longer lives than ever before. HIV medications are life-changing advances in science that have turned a deadly infection into a manageable chronic condition.