The active medical ingredient Tipranavir is a drug that is used to treat people with HIV type 1. It is used as part of a combination antiretroviral therapy. The drug Tipranavir is available on the pharmacological market under the trade name Aptivus and is distributed by the producer Boehringer. The active ingredient tipranavir is considered to belong to the category of HIV protease inhibitors.
What is tipranavir?
The drug tipranavir represents an antiviral agent that belongs to the pharmacological category of HIV protease inhibitors. However, from a structural point of view, it differs from other substances that also belong to this group. The active ingredient tipranavir is primarily used for the drug therapy of HIV infections. The effect of the drug is due to the fact that it impairs the so-called viral protease. This protease is essential for the replication of viruses. The active ingredient is usually administered orally in the form of capsules. The drug is administered twice a day together with meals. In the majority of cases, the drug Tipranavir is taken together with the booster Ritonavir. This substance is a so-called CYP inhibitor, which slows down the degradation of tipranavir. This mechanism improves the effectiveness of the drug tipranavir. However, various side effects are possible while taking the drug. Among the most common are nausea, headache, and fatigue. It should also be noted that the substance may be toxic to the liver, causing in some cases, for example, hepatitis or other serious diseases of the liver. For this reason, strict medical control is required. The drug tipranavir was approved in Europe and the USA in 2005. The substance tipranavir usually appears in white or faint yellowish color. The structure of the active ingredient tipranavir is non-peptidic. Basically, the drug tipranavir is an antiviral that is usually combined with other types of antivirals.
Pharmacologic Action
The specific mode of action of the drug tipranavir is responsible for its suitability for the therapy of individuals with HIV-1. In principle, the substance tipranavir is an HIV protease inhibitor that inhibits a special viral enzyme. This enzyme is essential for the virus to replicate and produce new viruses. By impairing the viral protease with the active ingredient tipranavir, the viruses are no longer able to continue replicating undisturbed. As a result, the viral load for the affected patient is reduced and the virus is prevented from spreading in the human organism. However, it is problematic that the viruses may quickly develop resistance to the drug tipranavir. Unlike other HIV protease inhibitors, the drug does not have a peptide structure. Thus, it forms the first type of non-peptide HIV protease inhibitor. These structural differences are probably responsible for the fact that cross-resistance occurs less frequently during treatment with the drug tipranavir than with other, peptide protease inhibitors. In this way, the drug tipranavir is also effective against HIV strains that are already resistant to other preparations. Research studies indicate that the drug tipranavir is characterized by significantly increased efficacy with such HIV strains. After oral administration, more than 90 percent of the active ingredient binds to the proteins in the plasma of the blood. Subsequently, the drug is predominantly metabolized in the liver. The cytochrome P450 system is primarily responsible for metabolization and degradation. Finally, excretion of the active substance occurs in the stool. The half-life of the drug tipranavir is on average approximately five to six hours.
Medical application and use
The drug tipranavir is usually used to treat patients infected with type 1 HIV. Tipranavir is used primarily when affected individuals have already developed resistance to other HIV protease inhibitors. However, since serious side effects are possible from taking the drug tipranavir, it is only approved for special conditions.In addition, a combination of the drug tipranavir with ritonavir is recommended.
Risks and side effects
Although the drug tipranavir has better efficacy than other HIV protease inhibitors, there is an increased likelihood of adverse side effects. The most common side effects are nausea, diarrhea, pain in the abdomen, and headache. Rashes on the skin are also possible. When tipranavir is combined with ritonavir, it may have a toxic effect on the liver. Patients with liver function disorders are therefore not suitable for therapy with the active ingredient tipranavir. Other potential side effects include hypersensitivity reactions to the active substance, thrombocytopenia, neutropenia, metabolic disorders, sleep disturbances and dizziness. Various interactions with other substances must also be taken into account. For example, to avoid interactions, concomitant use of rifampicin, simvastatin, and lovastatin should be avoided. Oral contraceptives and some benzodiazepines are also not suitable for combination with the drug tipranavir. Any side effects that occur should be reported to the physician.
