Active Ingredients

Stavudin – Wirkung, Anwendung & Risiken

Stavudine

Stavudine is a nucleoside reverse transcriptase inhibitor. It is used to treat HIV infections .

What is stavudine?

The active ingredient stavudine is used to treat HIV diseases such as AIDS . It is administered as part of an antiretroviral combination therapy. Stavudine is part of the nucleoside reverse transcriptase inhibitors (NRTIs).

Stavudine was synthesized as early as 1966 by the American chemist Jerome Phillip Horwitz (1919-2012). However, it was not until the mid-1990s that the drug was used in Europe. It is manufactured by the US pharmaceutical company Bristol-Myers Squibb (BMS).

Nowadays, however, stavudine is hardly used in western industrialized countries. The reason for this is the poor tolerability of the drug. Occasionally, however, its administration can be useful in the case of special mutation combinations as part of a salvage therapy. Stavudine is offered under the trade name Zerit®.

Pharmacological action

Stavudine is classified as a nucleoside reverse transcriptase inhibitor. This means that the drug has an inhibitory effect on the enzyme reverse transcriptase. The enzyme is extremely important for the HI viruses to overwrite the viral RNA into human DNA , which allows the pathogens to multiply.

Stavudine is also one of the so-called prodrugs. The drug represents an active ingredient precursor that itself has no effect against viruses . It is only inside the body that the substance is converted into the actually effective drug.

This has the property of inhibiting reverse transcriptase, which means that the HI viruses in the body can no longer multiply. This effect in turn leads to a reduction in the amount of virus in the organism. At the same time, the number of special white blood cells , which include the CD-4 positive T lymphocytes , may increase. This effect strengthens the body’s defense system .

One of the disadvantages of stavudine is that the HI viruses often quickly become insensitive to the active substance. The reason for this is the pronounced ability of the HI virus to adapt and change. For this reason, stavudine is always used as part of a combination therapy and is administered with several other drugs.

Once stavudine has reached and been taken up by the infected body cell, the substance is converted there into an active metabolite, which then blocks the reverse transcriptase enzyme.

The oral bioavailability of stavudine is quite high at around 90 percent. A simultaneous intake of food hardly has a negative effect on the active ingredient. The plasma half-life of stavudine is approximately 1.5 hours.

Medical Application & Use

Stavudine is used to treat HIV infections such as AIDS. The active ingredient strengthens the human immune system and fights the immune deficiency disease or at least delays its onset. There is no cure for AIDS with stavudine. However, the drug has a positive effect on the life expectancy and quality of life of the patient.

However, stavudine is only used when all other treatment options have failed. The reason for this is the strong side effects of the drug. For this reason, the anti-AIDS drug should only be administered for a short time.

Stavudine is taken in the form of hard capsules that have a dose of 30 to 40 milligrams. The recommended dosage is two times 30 milligrams for patients weighing less than 60 kilograms and two times 40 milligrams for patients weighing more than 60 kilograms. The capsules should be taken on an empty stomach 60 minutes before meals.

Risks & side effects

Taking stavudine often has unwanted side effects. The most common symptoms are pain or numbness in the hands and feet, tingling , chest pain , headache , chills , fever , general malaise , diarrhea , nausea , vomiting , the breakdown of fatty tissue in the limbs, back pain and an increased susceptibility to infection.

Other common side effects are sleep problems , pancreatitis , constipation , benign skin tumors, performance limitations, redistribution of body fat, mild liver dysfunction, pain in muscles and joints , hives , rashes on the skin , itching , acidification of the body, anxiety and depression . Sometimes those affected can also suffer from anemia , enlarged mammary glands , blood disorders in theBone marrow , jaundice , or an inflamed liver .

A problem with AIDS patients is that it is often difficult to distinguish the side effects of the drug from their disease-related symptoms. In addition, the side effects can also arise from the combination therapy, so that an exact trigger cannot be assigned.

The extent of the undesirable side effects is also influenced by the dose and the duration of therapy. It is sometimes possible to reduce serious side effects by lowering the dose. Occasionally, switching to another reverse transcriptase inhibitor is helpful.

In the early stages of stavudine treatment, AIDS patients often experience deterioration in their health. The reason for this is the reaction of the stronger immune system to the pathogens that are in the body. In such cases, doctors speak of an immune reactivation syndrome. However, if the patient responds positively to the drug, then after a few weeks the symptoms of the disease improve significantly.

If there is hypersensitivity to stavudine, the drug must not be administered. The same applies to inflammation of the pancreas and severe kidney dysfunction .

Stavudine may only be used during pregnancy if the doctor has carefully weighed the benefits and risks of the treatment beforehand. Animal testing revealed harmful effects on the child.

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.