Lopinavir

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Lopinavir
Lopinavir structure.svg
Lopinavir ball-and-stick.png
Clinical data
SynonymsABT-378
AHFS/Drugs.comInternational Drug Names
MedlinePlusa602015
License data
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityUnknown
Protein binding98-99%
MetabolismHepatic
Elimination half-life5 to 6 hours
ExcretionMostly fecal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC37H48N4O5
Molar mass628.810 g/mol g·mol−1
3D model (JSmol)
  (verify)

Lopinavir is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir).[1]

It was patented in 1995 and approved for medical use in 2000.[2]

Side effects[edit]

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

Pharmacology[edit]

Lopinavir is highly bound to plasma proteins (98–99%).[3]

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.[4]

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.[5]

References[edit]

  1. ^ "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004.
  2. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 510. ISBN 9783527607495.
  3. ^ KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
  4. ^ Capparelli E, Holland D, Okamoto C, et al. (2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV". AIDS. 19 (9).
  5. ^ HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.

External links[edit]