Lopinavir
| File:Lopinavir structure.svg | |
| File:Lopinavir ball-and-stick.png | |
| Systematic (IUPAC) name | |
|---|---|
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(2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
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| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a602015 |
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| Legal status | |
| Routes of administration |
Oral |
| Pharmacokinetic data | |
| Bioavailability | Unknown |
| Protein binding | 98-99% |
| Metabolism | Hepatic |
| Biological half-life | 5 to 6 hours |
| Excretion | Mostly fecal |
| Identifiers | |
| CAS Number | 192725-17-0  |
| ATC code | J05AR10 (WHO) (with ritonavir) |
| PubChem | CID: 92727 |
| DrugBank | DB01601 |
| ChemSpider | 83706 |
| UNII | 2494G1JF75 |
| KEGG | D01425 |
| ChEMBL | CHEMBL729 |
| Chemical data | |
| Formula | C37H48N4O5 |
| Molecular mass | 628.810 g/mol |
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Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir, under the trade names Kaletra (high-income countries) and Aluvia (low-income countries). It was first approved by the FDA on 15 September 2000.[1]
Pharmacology
Lopinavir is highly bound to plasma proteins (98–99%).[2]
Reports are contradictory regarding lopinavir penetration into the cerebrospinal fluid (CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC50 in 77% of samples.[3]
Side effects
Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir.
Research
A 2014 study indicates that lopinavir is effective against the human papilloma virus (HPV). The study used the equivalent of one tablet twice a day applied topically to the cervices of women with high-grade and low-grade precancerous conditions. After three months of treatment, 82.6% of the women who had high-grade disease had normal cervical conditions, confirmed by smears and biopsies.[4]
References
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.
