Anti-HIV medication, before the cure!
HIV medication Important Points
- There are more than 30 antiretroviral drugs in six classes of drugs; these are listed below.
- Each class of drugs attacks HIV in a different way.
There are six main types ('classes') of antiretroviral drugs.
Each class of drugs attacks HIV in a different way. Generally, drugs of two (or sometimes three) classes are combined to ensure a powerful attack on HIV.
Most people start HIV treatment with two drugs in the nucleoside / nucleotide reverse transcriptase inhibitor class combined with an integrase inhibitor, a non-nucleoside reverse transcriptase inhibitor or a protease inhibitor - hence 'triple therapy'.
Nucleotide reverse transcriptase inhibitors (NRTIs)
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Nucleotide reverse transcriptase inhibitors (NRTIs) and nucleotide reverse transcriptase inhibitors (NRTIs), usually called NRTIs, work towards the action of an HIV protein called reverse transcriptase.
After the HIV virus releases its genetic material into a host cell, reverse transcriptase converts viral RNA into DNA, a process known as 'reverse transcription'. NRTIs interrupt the construction of a new proviral DNA fragment, interrupting the process of reverse transcription and interrupting HIV replication.
The Backbone of Treatment
This class of medication is sometimes called the “backbone” of a combination of first-line HIV treatment. It includes the following medications:
- A can be marketed under the name Ziagen, but generic versions are also available. Abacavir is included in the tablet combination abacavir / lamivudine e Triumeq.
- Emtricitabine is also known as Emtriva. It is included in the combination of tablets emtricitabine / tenofovir disoproxil, Descovy, Atripla, Biktarvy, Eviplera, Genvoya, odefsey, Stribild e Symtuza.
- Lamivudine can be marketed under the name Epivir, but generic versions are also available. Lamivudine is included in the combination of tablets abacavir / lamivudine, lamivudine / zidovudine, Triumeq, Delstrigo e Dovato.
- Tenofovir disoproxil can be marketed under the name viread, but generic versions are also available. Tenofovir disoproxil is included in the tablet combination emtricitabine / tenofovir disoproxil, efavirenz / emtricitabine / tenofovir disoproxil, Delstrigo, Eviplera e Stribild.
- Tenofovir alafenamide, a more recent formulation of tenofovir, is available in combination tablets Biktarvy, Descovy, Genvoya, odefsey e Symtuza.
- Zidovudine can be marketed under the name Retrovir, but generic versions are also available. Zidovudine is included in the tablet combination lamivudine / zidovudine.
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) Reverse transcriptase inhibitors
non-nucleosides (NNRTIs) also target reverse transcriptase, but in a different way than NRTIs.
NNRTIs interfere with the enzyme reverse transcriptase by binding directly to it, blocking the process of reverse transcription.
- Doravirine is also known as Pifeltro. Doravirine is included in the combination tablet Delstrigo.
- Efavirenz can be marketed under the name Sustiva, but generic versions are also available. Efavirenz is included in the combination tablet efavirenz / emtricitabine / tenofovir disoproxil.
- Etravirine is also known as Intelence.
- Nevirapine can be marketed under the name Viramune, but generic versions are also available.
- Rilpivirine is also known as Edurant. Rilpivirine is also available in combination tablets odefsey, Eviplera e Juluca.
integrase target a protein in HIV called integrase, which is essential for viral replication.
Integrase is responsible for inserting viral genomic DNA into the host chromosome. The integrase enzyme binds to the host cell's DNA, prepares an area in the viral DNA for integration, and then transfers that processed chain to the host cell's genome.
Integrase inhibitors stop the infection from evolving by inserting itself into human cell DNA.
- Bictegravir is only available in the combined tablet Biktarvy.
- Dolutegravir is also known as Tivicay. It is included in the tablets combination Juluca e Triumeq, e Dovato.
- Elvitegravir is only available in combination tablets Genvoya e Stribild.
- O is also known as raltegravir Isentress.
Entry inhibitors prevent HIV from entering human cells. There are two types:
CCR5 inhibitors and Fusion inhibitors.
To enter the host cell, HIV must bind to two separate receptors on the cell surface: the CD4 receptor and a co-receptor (CCR5 or CXCR4). Once HIV becomes attached to both, its envelope can fuse with the host cell's membrane and release viral components into the cell. CCR5 inhibitors prevent HIV from using the CCR5 co-receptor when binding to it, blocking viral entry.
CCR5 inhibitors do not work at all and are very rarely used in first-line treatment. You would do a test to see if this type of treatment would be effective before you start. A CCR5 inhibitor is licensed in Europe:
- Maraviroc is also known as Celsentri.
A fusion inhibitor (enfuvirtide) is used only for people who have no other treatment options. It works by disrupting the fusion of the HIV envelope protein with the CD4 cell.
Protease inhibitors (IPs)
Protease inhibitors (PIs) block the activity of the protease enzyme, which HIV uses to break large polyproteins into smaller pieces needed to assemble new viral particles. Although HIV can still replicate in the presence of protease inhibitors, the resulting virions are immature and unable to infect new cells.
- O can be marketed under the name atazanavir Reyataz, but generic versions are also available. Atazanavir is included in the combination tablet Evotaz.
- Darunavir can be marketed under the name Prezista, but generic versions are also available. Darunavir is included in the tablet combination Answer e Symtuza.
- Lopinavir is available only in the combination tablet Kaletra.
The drugs of booster are used to 'increase' the effects of protease inhibitors. The addition of a small dose of a booster to an antiretroviral causes the liver to dismantle the primary drug more slowly, meaning that it stays in the body for longer periods or at higher levels. Without the reinforcing agent, the prescribed dose of the primary drug would be ineffective.
- Ritonavir is also known as Norvir. Ritonavir is included in the combination tablet Kaletra.
- Cobicistat is also known as Tybost. Cobicistat is included in the combined tablets Evotaz, Genvoya, Rezolsta, Stribild e Symtuza.
Regimes of compressed only.
There are some fixed-dose pills that combine two or three antiretroviral drugs from more than one class into a single pill that is taken once a day. Find out more about this on our page Single tablet regimens.
Inhibitors of HIV treatment (Human immunodeficiency virus) Types of antiretroviral drugs
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