• Friday July 10,2020

abacavir

Abacavir is a drug that inhibits the proliferation and release of viruses. Specifically, abacavir is used as an antiviral in HIV-infected patients. It is an element in a combination therapy.

What is Abacavir?

Abacavir is a drug that inhibits the proliferation and release of viruses. Specifically, abacavir is used as an antiviral in HIV-infected patients.

GlaxoSmithKline plc. (GSK) as a British pharmaceutical company is the manufacturer of the drug Abacavir. As part of a combination antiretroviral therapy, HIV-1 patients are being treated.

Abacavir belongs to the group of nucleoside reverse transcriptase inhibitors (NRTIs). It is a nucleoside analogue. This is similar to the natural nucleoside. They start in their action on the enzyme reverse transcriptase. This enzyme is part of retroviruses and transcribes the viral RNA genome into DNA.

Abacavir competes with the natural nucleosides. However, it does not have a 3rd hydroxyl group. Thus, no chain extension can take place. Therapy with abacavir should be started only after a genetic test, as a certain gene marker (HLA-BSternchen5701) can cause life-threatening reactions.

Pharmacological action

Abacavir is a nucleoside analog. It lacks the 3rd hydroxyl group. This prevents chain extension during transcription. Transcription is the biological process in which genetic information is transferred from the DNA strands to the RNA.

The base sequences of RNA and DNA must be complementary. Transcription is then catalyzed in the nucleus. Abacavir works against it. It inhibits viral regeneration. Pharmacodynamically, abacavir is first converted into a triphosphate. These are chemically synthesized equivalents of phosphoric acid. Furthermore, the base portion is biochemically rebuilt or degraded by the body's own enzyme systems. The result is a biochemically active metabolite.

This metabolite (carborvir triphosphate) inhibits chain extension and thus blocks transcription. In addition to the manipulation of transcriptase, there is also an end to DNA chain formation. The missing hydroxyl group prevents linking to 2 pages. Treatment with abacavir or a combination of NRTI reduces viral load.

At the same time an increase in the CD4 cell count is caused. According to scientific studies, the use of abacavir slows down the progression of immunodeficiency, reduces AIDS-typical infections and thus significantly prolongs life. According to other study results, however, the benefit loses over time. This is due to the mutability of the H virus.

Medical application & use

Abacavir is a synthetic molecule that builds up inhibitory activities against immune deficiency AIDS in the body. The degradation of abacavir in the body is not by the cytochrome P450 system, but by alcohol dehydrogenase and further by glucuronyl - transferase.

Interactions with other drugs are avoided as far as possible. In vitro, abacavir shows good activity against HIV-1 and its effects can be enhanced by amprenavir, nevirapine and zidovudine. Also combined drugs, such as lamivudine and stavudine, significantly enhance the effect. Only slowly develops the viral resistant to abacavir. It needs a lot of mutations.

In adults who were treated with a combination of abacavir with lamivudine and zidovudine, 70 percent had a viral load at 48 weeks that was undetectable. Also, the CD-4 cell count increased significantly. In children with HIV-1, a comparative study was conducted. These children had unblinded NRTI and the proportion of detectable viral load (less than 400 copies / ml) was significantly higher in combination with abacavir than comparable drugs.

Risks & Side Effects

In known hypersensitivity to abacavir (checked by genetic test) or in severe liver dysfunction the drug should not be taken. Limited use of abacavir is recommended during pregnancy or lactation.

Furthermore, hepatitis, metabolic acidosis or hepatomegaly are against the use of the drug. If the patient is known to have high risk factors for liver disease or if the patient carries a very high viral load, the use of abacavir, especially in combination with lamivudine and zidovudine, is of concern.

Also, moderate liver dysfunction or end-stage renal disease is one of the relative contraindications of abacavir. About 5 percent of patients show hypersensitivity reactions. Symptoms include rash, nausea, vomiting, abdominal pain, cough, elevated liver function, mouth ulcers, headache, and a general malaise.

Interesting Articles

erythroderma

erythroderma

Erythroderma is a reddening of the skin that occurs throughout the body. It is a collective name for various skin diseases. What is erythroderma? As a rule, the complaints of erythroderma occur on the entire body of the affected person. It comes to the whole body to a reddening of the skin. © ksenia_bravo - stock.

Angina pectoris

Angina pectoris

Angina pectoris or chest tightness is a heart disease that belongs to the group of coronary heart disease (CHD). The symptoms are often similar to those of myocardial infarction. Angina should be examined immediately by the doctor if suspected. The call of the emergency doctor or urgent medical help is therefore more than advisable

vetiver

vetiver

Above all, Vetiver is a well-known perfume ingredient and is also called moth root because of its insect repellent effect. The essential oil is pure or mixed with carrier oils available and can depending on the application still much more than just perfume. Occurrence & cultivation of vetiver Vetiver is a sweet grass species that thrives in the tropical climate of Asia and has long been known as a cultivated plant

ribose

ribose

Ribose is a sugar that is very common in nature. Ribose is a component of ribonucleic acid and nucleotides. The human body is able to synthesize ribose itself. What is ribose? Ribose is a monosaccharide consisting of five carbon atoms (pentose) and a group of aldehydes. The structural formula of the ribose is H2COH-HCOH-HCOH-HCOH-COH

Juvenilphase

Juvenilphase

The juvenile phase refers to the phase of a living being after birth and before sexual maturity. Afterwards they are considered adult (adolescence), before they are in the embryonic stage. In humans, the juvenile phase goes from childhood to early adolescence (pubescent). What is the juvenile phase? The juvenile phase refers to the phase of a living being after birth and before sexual maturity

Lyme disease

Lyme disease

The Lyme disease or Lyme disease is an infectious disease, which is mainly transmitted by ticks or wooden blocks and triggered in humans. The causative bacteria are the so-called Borrelia. What is Lyme disease? A tick bite or tick bite can transmit various diseases into the host organism. The best known here is the Lyme disease