Lopinavir
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| Systematic (IUPAC) name | |
|---|---|
|
(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 | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a602015 |
| Pregnancy category |
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| Routes of administration | Oral |
| Legal status | |
| Legal status | |
| 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 |
| Molar 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
- ↑ "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004.
- ↑ KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
- ↑ Capparelli E, Holland D, Okamoto C, et al. (2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV". AIDS (London, England) 19 (9).
- ↑ HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.