Lopinavir/ritonavir

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Lopinavir/ritonavir
Combination of
LopinavirProtease inhibitor
RitonavirProtease inhibitor (pharmacokinetic booster)
Clinical data
Trade namesKaletra, Aluvia
AHFS/Drugs.comMonograph
MedlinePlusa602015
License data
Pregnancy
category
  • AU: B3
By mouth
ATC code
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
KEGG
NIAID ChemDB
CompTox Dashboard (EPA)
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Lopinavir/ritonavir (LPV/r), sold under the brand name Kaletra among others, is a

antiretrovirals.[2] It may be used for prevention after a needlestick injury or other potential exposure.[2] It is taken by mouth as a tablet, capsule, or solution.[2]

Common side effects include

HIV protease inhibitors.[2] Ritonavir functions by slowing down the breakdown of lopinavir.[2]

Lopinavir/ritonavir as a single medication was approved for use in the United States in 2000.[2] It is on the World Health Organization's List of Essential Medicines.[3]

Medical uses

Lopinavir/ritonavir was once a preferred combination for HIV first-line therapy in the United States.[4] But due its higher pill burden compared to than other protease inhibitor-based regimens and increased gastrointestinal intolerance, it is no longer recommended to treatment-naive patients.[5]

Adverse effects

The most common adverse effects observed with lopinavir/ritonavir are

asthenia, headache, vomiting and, particularly in children, rash.[6]

Raised liver enzymes and hyperlipidemia (both hypertriglyceridemia and hypercholesterolemia) are also commonly observed during lopinavir/ritonavir treatment.[citation needed]

Lopinavir/ritonavir is anticipated to have varying degrees of interaction with other medications that are also

P-gp substrates.[7]

People with a structural

ischaemic heart disease, or cardiomyopathies should use lopinavir/ritonavir with caution.[8]

On 8 March 2011 the U.S. Food and Drug Administration notified healthcare professionals of serious health problems that have been reported in premature babies receiving lopinavir/ritonavir oral solution, probably because of its propylene glycol content. They recommend the use should be avoided in premature babies.[9]

History

structure-based drug design approach using the Argonne APS, Abbott was able to develop new products that inhibit the protease, and therefore stop virus replication.[10][11]

Lopinavir was developed by

fixed-dose combination medication with ritonavir.[citation needed
]

Lopinavir/ritonavir was approved by the US Food and Drug Administration (FDA) on 15 September 2000,[12][13] and in Europe on 19 March 2001.[14] Its patent was scheduled to expire in the US on 26 June 2016.[citation needed][needs update]

In March 2020, during the

Israeli government announced that it would force AbbVie to license its patents for lopinavir/ritonavir. In response, AbbVie announced that it would cease enforcing its patents on the drug entirely.[15][16][17]

Society and culture

Cost

As a result of high prices and the spread of HIV infection, the government of

Act Up-Paris and a public call to boycott all of Abbott's medicines by the French NGO AIDES.[20]

Available forms

Heat-stable pellets that can be taken by mouth have been developed for children.[21]

Research

See also:
Coronavirus disease 2019 § Research, and COVID-19 drug repurposing research

While data for

COVID-19.[23][22] In this trial the medication was started typically around 13 days after the start of symptoms.[22]

References

  1. ^ "Kaletra Product information". Health Canada. 19 March 2019. Retrieved 18 March 2020.
  2. ^ a b c d e f g h i j k "Lopinavir and Ritonavir". The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 28 November 2016.
  3. hdl:10665/325771
    . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  4. ^ "Adult and Adolescent Guidelines". AIDSinfo. 4 May 2006. Archived from the original on 6 May 2006. Retrieved 6 May 2006.
  5. ^ "What to Start: Initial Combination Regimens for the Antiretroviral-Naive Patient". AIDSinfo. 18 December 2019. p. Table 10. Antiretroviral Components or Regimens Not Recommended as Initial Therapy. Archived from the original on 31 August 2020. Retrieved 26 August 2020.
  6. ^ a b "Kaletra- lopinavir and ritonavir tablet, film coated Kaletra- lopinavir and ritonavir solution". DailyMed. 26 December 2019. Retrieved 18 March 2020.
  7. PMID 19839641
    .
  8. ^ "FDA Issues Safety Labeling Changes for Kaletra". Medscape. 10 April 2009. Archived from the original on 10 September 2017. Retrieved 18 March 2020.
  9. ^ "Kaletra (lopinavir/ritonavir): Label Change - Serious Health Problems in Premature Babies". Drugs.com. Archived from the original on 11 March 2011.
  10. ^ Foster C. "Research at Argonne helps Abbott Labs develop anti-HIV drug". Archived from the original on 22 October 2006. Retrieved 4 September 2006.
  11. ^
    PMID 9835517
    .
  12. ^ "Drug Approval Package: Kaletra (Lopinavir/Ritonavir) NDA #21-226 & 21-251". U.S. Food and Drug Administration (FDA). 20 November 2001. Retrieved 18 March 2020.
  13. ^ "Generic Kaletra Availability". Drugs.com. Retrieved 18 February 2020.
  14. ^ "Kaletra EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 18 February 2020.
  15. ^ Bonadio E, Baldini A (1 April 2020). "Drug companies should drop their patents and collaborate to fight coronavirus". The Conversation.
  16. ^ "Inoculating the world may mean reviving old curbs on patents". Pittsburgh Post-Gazette. Bloomberg. 14 April 2020. Retrieved 16 April 2020.
  17. ^ Scheer S (19 March 2020). "Israel approves generic HIV drug to treat COVID-19 despite doubts". Reuters. Retrieved 16 April 2020.
  18. ^ "Decree of Department of Disease Control, Ministry of Public Health, regarding exploitation of patent on drugs & medical supplies by the government on combination drug between lopinavir & ritonavir" (PDF). Archived from the original (PDF) on 17 July 2011.
  19. ^ 'Abbott pulls HIV drug in Thai patents protest', Financial Times (14 March 2007)
  20. ^ "People Living with HIV: Let's change the rules imposed by the pharmaceutical industry!" (PDF). AIDES. 1 July 2007. Archived from the original (PDF) on 20 October 2007.
  21. PMID 30549217
    .
  22. ^
    PMID 32284951
    .
  23. PMID 32187464
    . This randomized trial found that lopinavir–ritonavir treatment added to standard supportive care was not associated with clinical improvement or mortality in seriously ill patients with Covid-19 different from that associated with standard care alone.

External links
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