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Information |
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Drug Groups
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approved |
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Description
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Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is marketed by Abbott as Kaletra, a co-formulation with a sub-therapeutic dose of ritonavir, as a component of combination therapy to treat HIV/AIDS. |
| Indication |
Indicated in combination with other antiretroviral agents for the treatment of HIV-infection. |
| Pharmacology |
Lopinavir is an antiretroviral of the protease inhibitor class. Inhibiting HIV-1 protease (responsible for protein cleavage), results in selectively inhibiting the cleavage of HIV gag and gag-pol polyproteins, thereby preventing viral maturation. |
| Toxicity |
Although human experience of acute overdosage with lopinavir is limited, accidental ingestion of the product by a young child could result in significant alcohol-related toxicity and could approach the potential lethal dose of alcohol. |
| Affected Organisms |
| • |
Human Immunodeficiency Virus |
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| Biotransformation |
Hepatic. Lopinavir is extensively metabolized by the hepatic cytochrome P450 system, almost exclusively by the CYP3A isozyme. |
| Absorption |
Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4. |
| Protein Binding |
Lopinavir is highly bound to plasma proteins (98-99%). |
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