Lopinavir

Background

Lopinavir is usually given in combination with ritonavir for both treatment of HIV and HIV post-exposure prophylaxis. It is currently being studied in the use of COVID-19 as well.

Administration

  • Type: antiviral
  • Dosage Forms: 100 mg/25 mg, 200 mg/50 mg (tabs); 400 mg/100 mg per 5 mL solution
  • Routes of Administration: PO
  • Common Trade Names: Kaletra (lopinavir/ritonavir)

Adult Dosing

Pediatric Dosing

  • HIV treatment
    • 14 days-12 months old: 16mg/5mg/kg PO BID (solution)
    • 13 months and older, <15 kg:
      • Treatment-naive: 12 mg/3 mg/kg PO BID (solution)
      • Treatment-experienced: 13 mg/3.25 mg/kg PO BID (solution)
    • 13 months and older, 15-45 kg: 11 mg/2.75 mg/kg PO BID (solution)
    • 13 months and older, >45 kg: 400 mg/100 mg PO BID (solution)
  • HIV post-exposure prophylaxis
  • 14 days-12 months old: 16 mg/4 mg/kg PO BID (solution)
  • 13 months and older, <15 kg: 12 mg/2 mg/kg PO BID (solution)
  • 13 months and older, 15-40 kg: 10 mg/2.5 mg/kg PO BID (solution)
  • 13 months and older, >40 kg: 400 mg/100 mg PO BID (solution)

Special Populations

Pregnancy Rating

Safe to use in pregnancy (avoid oral solution due to alcohol content)

Lactation risk

  • Avoid breastfeeding

Renal Dosing

  • Adult: No adjustment
  • Pediatric: No adjustment

Hepatic Dosing

  • Adult: Not defined, caution advised in hepatic impairment
  • Pediatric: Not defined, caution advised in hepatic impairment

Contraindications

Adverse Reactions

Serious

Common

  • Nausea/vomiting
  • Diarrhea
  • Paresthesia
  • Fatigue
  • Rash
  • Abdominal pain
  • Cough
  • Dysgeusia
  • Oropharyngeal pain
  • Dizziness
  • AST, ALT, CK elevation
  • Edema
  • Acne
  • Lipodystrophy

Pharmacology

  • Half-life: 5-6 hr
  • Metabolism: Liver (CYP450)
  • Excretion: Fecal

Mechanism of Action

Binds to active site of HIV protease, preventing maturation of the virus

Comments

A trial of lopinavir/ritonavir is currently being done to study use in COVID-19. So far, studies have not shown significant benefit in time to clinical improvement. Mortality at 28 days is lower but not statistically significant.[1]

See Also

References

  1. Cao B, Wang Y, Wen D, et al. A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19 [published online ahead of print, 2020 Mar 18]. N Engl J Med. 2020;10.1056/NEJMoa2001282. doi:10.1056/NEJMoa2001282
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