HIV and AIDS are part of those diseases for which there is still no absolute cure for them, unfortunately. However, that does not mean that everything is dull and gray for these people.
Pharmaceutical research and innovation, promoted by international associations such as the International AIDS Society , has made great advances in the management of these patients who can now enjoy a full life.
Below, we will describe some of the commonly prescribed drugs, their benefits, contraindications, and even possible adverse effects.
What is treatment for HIV?
HIV treatment, also known as antiretroviral therapy (ART), is the line of defense for immunocompromised patients. Research on the characteristics of HIV and its life cycle have allowed great advances.
Prior to 1996, there were few drug options that directly treated HIV. Health professionals sought, mainly, to treat the diseases that the person suffered from HIV and not the virus itself.
An example of this was Aciclovir , which sought to attack infectious agents that sought to take advantage of the person’s poor immune status, such as the Hepatitis B virus, the Herpes simplex virus and the cytomegalovirus, for example.
However, it was in the mid-1990s, when the doctrine of triple pharmacological treatment began. It consists of a cocktail of drugs that mix different treatments for both HIV and related diseases.
These drugs are categorized into several groups: reverse transcriptase inhibitors, protease inhibitors, entry inhibitors, integrase inhibitors, adhesion inhibitors and many more.
Characteristics of treatment for HIV
ART has become an effective tool to combat the destruction of the immune system caused by said virus. Since its arrival on the pharmaceutical market, more and more therapies have been developed that stop its attack.
In the year 2000, a series of epidemiological figures from more than 14 countries were published, showing the great epidemic that is HIV. This prompted the desire on the part of professionals to stop the transmission of said virus.
Next, we will mention some of its features.
It is known as antiretroviral treatment
Retroviruses do the opposite. Inside, they contain RNA and, upon entering our cells, force their enzymes to carry out reverse transcription. That is, from RNA to DNA.
What do our cells do with this foreign DNA? The same thing they do with our own DNA. Since the cellular machinery has been hijacked by the virus, the cell begins to produce the necessary viral proteins based on this DNA.
It is indicated to all seropositive people
The word seropositive refers to the presence, or not, of serological markers in the patient’s blood. These are small signs or indicators that allow the health professional to discern whether or not you suffer from a disease.
However, it is not that simple. Not all serological tests detect the infectious microorganism, but the antibodies that are formed against them. There is a ‘window period’ between the entry of the virus into the body and the formation of antibodies.
During this interval, serological tests can give false negatives. Over the decades, the effectiveness and early detection of HIV has improved substantially with the advent of tests such as the fourth generation ELISA .
These, and others, help to detect not only the antibodies that are formed against the virus (usually 3 weeks after virus entry), but also detect the virus itself.
Reduces the viral load of infected people
The term viral load refers to the number of copies of a virus present in a patient’s bodily fluids, be it saliva, urine, or blood. The aforementioned tests allow its detection.
The viral load is quantified as the number of copies of HIV in a milliliter (copies/mL). During patient monitoring, it is important to keep these figures in mind.
These allow the clinician to determine: a) the course of the disease and b) the efficacy of ART. A high percentage indicates that the infection worsens or that the virus has developed resistance against the drugs.
It is not a definitive cure
Unfortunately, TARs do not kill the virus. Thanks to the nature of HIV, it becomes an insidious and tireless enemy, hiding inside cells in complete inertness for long years.
Therefore, the virus is not completely eliminated from the person’s system. However, it does not mean that the disease cannot be kept at bay with the early, suitable and constant application of these medications.
Provides higher quality of life
The advent of ART represented a drastic change in morbidity and mortality rates for patients with HIV. In 1995 , mortality was 29.4 per 100 people. In the second quarter of 1997 , mortality dropped to 8.8.
Combination antiretroviral therapies are those that offer the best benefits in contrast to monotherapies. This demonstrates that intensive ART has significant effects as modifiers of the patient’s quality of life.
In this sense, another study , published by the Brazilian Society of Infectious Diseases, observed a series of positive changes in the lifestyle of HIV-positive adult men after only one year of ART.
How does HIV treatment work?
Since its arrival in the Western media 60 years ago, scientific interest in HIV has led to great advances in understanding the disease and how it works.
This knowledge opened the doors to the development of drugs that deal with the virus by attacking certain points in the viral replication cycle, inhibiting its attack and preventing cell death.
Limit the reproduction of the virus
There are various therapeutic targets aimed at blocking the ‘cell hijacking’ process committed by HIV. More than 50% of ARTs are reverse transcriptase inhibitors (ITIs), in turn, divided into several subgroups (NRTIs, tNRTIs, and NNRTIs).
Let us remember that the viral replication mechanism consists of making the cell make copies of the viral DNA, the result of the action of reverse transcriptase. This process is unique to retroviruses and has therefore become a drug target.
Its mechanism is to create molecules that bind to viral DNA strands and act as signals that tell the cell to stop the process. Thus, incomplete and dysfunctional DNA chains are formed and viral replication is prevented.
Another class of drugs, called entry inhibitors, prevent HIV from entering the cell. The virus enters through a series of interactions between HIV membrane proteins (gp41 and gp120) and the CD4 T lymphocyte.
This series of interactions allows the HIV membrane to fuse with the cell membrane and discharge its contents into the lymphocyte. Enfuvirtide and maraviroc block this entire process.
Subsequently, these drugs, like many others, are metabolized by a group of enzymes called cytochrome p450 .
Reduces the risk of disease transmission
By preventing the replication process, the number of copies of HIV that are released outside the cell and subsequently infect others is decreased. This is reflected in a reduction in viral load.
In addition to favoring the patient, ART brings with it a side effect that is to reduce the risk of transmission of the disease. We know that the only route of transmission for HIV is through bodily fluids.
If the number of viral copies in them is decreased, the chances that this person will become a highly infectious vector decrease. In such a way, that the chain of transmission is broken.
Keeps viral copy number low
As we have said, the purpose of ART is not the absolute eradication of the virus, but to attenuate its presence to such an extent that it is undetectable in serological tests.
A successful therapy is defined as a viral load that has reached undetectable levels in serological tests (less than 200 copies/mL). However, it is important that the patient continue regular check-ups since the virus can develop resistance mechanisms.
Benefits of HIV treatment
The advent of antiretrovirals has represented a positive turning point for people who must bear this condition. They have made the idea of living fully and satisfactorily, despite being HIV positive, a reality.
Here are some examples of how ART has changed these lives for the better.
Decreases the amount of virus in the body
The most notable benefit of these drugs is to reduce the viral load and thus decrease the number of copies that destroy the immune system. As they increase, the defenses worsen and the proclivity to a superimposed infection.
Strengthens the immune system
CD4 T lymphocytes and macrophages are the main targets of HIV. Furthermore, by attacking and destroying CD4 T lymphocytes, they indirectly destroy CD8 T lymphocytes.
The total lymphocyte count is a marker used to quantify the progression of the disease. The Center for Disease Control and Prevention (CDC), located in the US, established parameters to understand the severity of the disease.
When these levels decrease below 200 cells/mm3, it is considered the most serious stage where the patient is highly exposed to infections by opportunistic agents.
ARTs help prevent this by preventing the death of these immune cells and allowing the individual to keep their defenses high against any other microorganisms.
Prevents drug resistance
An HIV seropositive patient is at increased risk of opportunistic infections that tend to show resistance to a range of antibiotics.
One such example is methicillin-resistant Staphylococcus aureus , a bacterium notorious for being resistant to a large number of antibiotics.
Other examples of bacteria resistant to treatment that can affect the patient are Klebsiella pneumoniae, P. Jirovecii or mycobacterium avium.
Reduces the risk of contagion to other people
One of the main risks for a patient with HIV is not only the destruction of their immune system, but also that they may spread the virus to others since they are unaware of their condition.
Another example of a risk would be an HIV-positive patient who discontinues their therapy and whose trail is lost. Epidemiological surveillance is prevailing because it allows knowing the physical and mental evolution of the person, in addition to their interaction with others.
Main HIV treatment drugs
The medications that we will mention below have been developed by the pharmaceutical industry in order to delay the onset of symptoms or damage caused to the body by the human immunodeficiency virus (HIV).
There is a pharmaceutical company that is dedicated solely to HIV called ViiV Healthcare , focused on creating better medicines and the prevention of this disease, in addition, it has an extension for Latin America and the Caribbean.
It is important to emphasize that thanks to these drugs the quality of life of seropositive patients improves, but they are not cured of the infection caused by HIV (hiv infection).
It is the oldest antiretroviral drug, it inhibits the replication of the HIV virus by joining the DNA chain. Regarding its administration, this can be orally or intravenously.
Its clinical use is wide, it is used during pregnancy for the prevention of transmission of the virus from the mother to the fetus during childbirth, in addition, as a treatment of HIV infection in children, in combination with other antiretroviral agents.
Before starting treatment, potential benefits and risks should be assessed, and pregnant women should be made aware that transmission of the virus may still occur in some cases despite treatment with zidovudine.
Didanosine, also called Videx®, is indicated in patients with HIV infection who do not tolerate zidovudine or no longer respond to it. Regarding its administration, it is available in liquid, powder to dissolve and long-acting capsules.
This medicine is usually taken 1 or 2 times a day, on an empty stomach, and should not be taken with acidic liquids such as orange juice or soda.
Nevirapine, also known by the name of Viramune®, is used to treat infections caused by HIV, clinically indicated to control HIV-1 infection in adolescents and children, associated with other antiretrovirals.
Regarding its administration, it is available in the form of 200mg tablets. It is taken twice a day, with the exception of the first 2 weeks of treatment, which is taken once a day, and can also be taken with or without food in the stomach.
The medications should be taken at the same time every day, when a dose is forgotten and more than 8 hours have passed, the next dose should be taken at its usual time, therefore it is advisable to have a reminder not to miss treatment doses.
It is important to mention that there are two types of HIV, HIV-1 was discovered first and is more prevalent worldwide, while HIV-2 resides mostly in West Africa.
It is a drug used in the treatment of HIV-1 in combination with other drugs. It is indicated in adults, adolescents and children over 3 years of age.
In the US, the FDA has authorized its use in children older than 3 months of age. It is available as capsules and its long half-life allows once-daily dosing.
It is recommended to take the dose at bedtime and on an empty stomach, since the presence of food may increase absorption and lead to an increased frequency of adverse reactions.
Women of childbearing potential should have a pregnancy test before starting treatment and always use barrier contraceptives, as hormonal contraceptives may not be effective enough while taking efavirenz.
Consult your doctor if you become pregnant during treatment, since the use of efavirenz is not indicated in pregnant women, because a potential risk of teratogenicity has been observed in the first trimester of pregnancy.
Tenofovir disoproxil fumarate
It is a medicine used against the disease caused by the human immunodeficiency virus (HIV-1 and HIV-2) and against the hepatitis B virus. It has the approval of the FDA (Food and Drug Administration) of the United States Joined.
It is indicated as treatment in HIV-1 infected adults on combination antiretroviral therapy, in adolescents and in children over 2 years of age weighing at least 10 kg.
It is always used in combination with other drugs against HIV, as for its pharmaceutical presentation, it is in the form of tablets and powder for oral administration.
It is a selective inhibitor of HIV protease, which prevents the formation of infectious and mature virus particles. It must be in combination with ritonavir and other antiretrovirals.
It is indicated for the treatment of adolescents 16 years of age and older. The drug is administered orally through capsules.
It blocks the penetration of HIV into CD4+ T cells by inhibiting the process by which the viral envelope fuses with the cell membrane. Its route of administration is the subcutaneous route, it is indicated for people over 6 years of age and the doses vary according to age.
Its drug interactions are low, it has excellent tolerance, and as can be seen, the complex treatment used in HIV infection must be combined with other antiretroviral drugs to complete its therapeutic effect.
Indicated for people over 16 years of age, it is administered orally, using coated tablets, which can be consumed with or without food in the stomach, and these tablets should not be chewed or crushed.
It is important to note that there are supplements that can be dangerous when controlled with HIV medications, an example of which is St. John’s wort .
This herb is often used for depression, but it can affect the effectiveness of various anti-HIV medications, so consult your doctor any time you want to add a medication or supplement to your daily routine.
Side Effects of HIV Treatment
Every drug, without exception, carries with it the risk of adverse effects, known as side effects. In certain patients with a certain genetic or acquired susceptibility, these can occur.
nausea and diarrhea
Gastrointestinal (GI) effects can originate from the consumption of drugs belonging to protease inhibitors (PI), ITIs or even any antiretroviral drug.
The appearance of these GI symptoms may be due, in certain cases, not thanks to ART, but to the antibiotic therapy that is part of the treatment.
Headache may be a symptom of a hypersensitivity reaction, caused by the body’s adverse rejection of the medication. Certain patients are genetically predisposed to allergies to certain medications.
Other symptoms that may be indicative of hypersensitivity to antiretrovirals include fever, rash, muscle and joint pain, vomiting, diarrhea, chills, abdominal pain, and respiratory symptoms.
Anemia is a low red blood cell count in the blood. In the ART setting, it may be due to bone marrow suppression, caused by zidovudine. Other concomitant symptoms may be neutropenia.
Fatigue is not only a side effect of certain antiretrovirals (for example, zidovudine), but also a symptom of HIV. So it is common for the patient to experience a perceived decrease in their energies.
Observable side effect in certain patients after prolonged administration of zidovudine and lopinavir. This metabolic phenomenon can trigger even more serious pathologies such as type 2 diabetes mellitus, known to further disturb the immune system.
It is a pathology characterized by the appearance of fat deposits in certain parts of the body and the disappearance of others in certain parts. Generally associated with ITIs.
A subtype of this, lipohypertrophy (increased abdominal fat) has been observed with the use of PIs or others, such as efavirenz. These changes in the individual’s body constitution can arouse insecurities about their body and, in the long term, anxiety and depression.
Increased cholesterol and triglycerides
Increased cholesterol and triglycerides may be due to a direct effect of certain drugs, such as stavudine, didanosine, zidovudine, efavirenz, lopinavir, indinavir, tipranavir, and other members of the protease inhibitor class.
The elevation can also be caused by side effects of potential liver toxicity caused by ITIs. To lessen these effects, we recommend exercising, reducing your intake of saturated fats, and eating foods rich in omega-3s.
Reduced bone density
Reverse transcriptase inhibitors (ITIs), especially tenofovir disoproxil fumarate, are associated with significant loss of bone density. It has also been linked to other pathologies, such as osteomalacia or renal tubulopathies.
Lactic acidosis, accumulation of lactic acid that generates a decrease in the body’s pH and all the symptoms associated with it, was common in the ancients (ITIANt). Among these, we find zidovudine, stavudine and didanosine.