Lopinavir

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Lopinavir
Lopinavir structure.svg
Lopinavir ball-and-stick.png
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
  • US: C (Risk not ruled out)
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 YesY
ATC code J05AR10 (WHO) (with ritonavir)
PubChem CID 92727
DrugBank DB01601 YesY
ChemSpider 83706 YesY
UNII 2494G1JF75 YesY
KEGG D01425 YesY
ChEMBL CHEMBL729 YesY
Chemical data
Formula C37H48N4O5
Molar mass 628.810 g/mol
  (verify)

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[edit]

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[edit]

Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir.

Research[edit]

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[edit]

  1. ^ "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004. 
  2. ^ KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
  3. ^ 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). 
  4. ^ HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.

External links[edit]