Lopinavir

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Lopinavir
Clinical data
Other namesABT-378
AHFS/Drugs.comInternational Drug Names
MedlinePlusa602015
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityUnknown
Protein binding98-99%
MetabolismLiver
Elimination half-life5 to 6 hours
ExcretionMostly fecal
Identifiers
  • (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
JSmol)
  • O=C(N[C@@H](Cc1ccccc1)[C@@H](O)C[C@@H](NC(=O)[C@@H](N2C(=O)NCCC2)C(C)C)Cc3ccccc3)COc4c(cccc4C)C
  • InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1 checkY
  • Key:KJHKTHWMRKYKJE-SUGCFTRWSA-N checkY
  (verify)

Lopinavir is an anti

fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir).[1]

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

LMIC, especially among children living with HIV. Lopinavir and ritonavir can be taken as a tablet or an oral solution, a preferred option in children. In the early stages of COVID-19 pandemics, lopinavir was repurposed against the SARS-CoV-2 virus in the hope of disturbing its protease activity.[3]

Side effects

Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir. They include nausea, vomiting, and stomach aches.[citation needed]

Pharmacology

Lopinavir is highly bound to plasma proteins (98–99%).[4]

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.[5]

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.[6] Lopinavir has been shown to impair protein synthesis via AMP-activated protein kinase (AMPK) and eEF2 kinase (eEF2K) activation, a mechanism that is similar to the antiviral effect of protein phosphatase 1 inhibitors.[7][8]

Lopinavir was found to inhibit

MERS-CoV replication in the low-micromolar range in cell cultures.[9] In 2020, lopinavir/ritonavir was found not to work in severe COVID-19. In this trial the medication was started typically around 13 days after the start of symptoms.[10]

A long-acting injectable formulation of lopinavir is under clinical trial aiming at monthly dosing (NCT05850728).

References

  1. ^ "FDA Approved Drug Products: Kaletra". Retrieved 30 April 2004.
  2. ISBN 9783527607495
    .
  3. PMC 7689305
    .
  4. ^ Kaletra (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
  5. S2CID 3162858
    .
  6. ^ HIV drug used to reverse effects of virus that causes cervical cancer University of Manchester, 17 February 2014.
  7. PMID 34335531
    .
  8. PMID 25073485
    .
  9. PMID 24841269
    .
  10. PMID 32187464
    .

External links

  • "Lopinavir". Drug Information Portal. U.S. National Library of Medicine.
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