Lopinavir: Difference between revisions

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==Background==
Ritonavir is usually given in combination with lopinavir for both treatment of HIV and HIV post-exposure prophylaxis. It is currently being studied in the use of COVID-19 as well.
==Administration==
==Administration==
*Type:  
*Type: [[antiviral]]
*Dosage Forms:
*Dosage Forms: 100 mg/25 mg, 200 mg/50 mg (tabs); 400 mg/100 mg per 5 mL solution
*Routes of Administration:
*Routes of Administration: PO
*Common Trade Names:  
*Common Trade Names: Kaletra (lopinavir/ritonavir)


==Adult Dosing==
==Adult Dosing==
*[[HIV]] treatment
**400 mg/100 mg PO BID
**Dose will need to be increased when used in combination with other [[HIV]] medications
*[[HIV post-exposure prophylaxis]]
**400 mg/100 mg PO BID
==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)




==Pediatric Dosing==




==Special Populations==
==Special Populations==
===[[Drug pregnancy categories|Pregnancy Rating]]===
===[[Drug pregnancy categories|Pregnancy Rating]]===
*
Safe to use in pregnancy (avoid oral solution due to alcohol content)


===Lactation risk===
===Lactation risk===
*
*Avoid breastfeeding


===Renal Dosing===
===Renal Dosing===
*Adult:
*Adult: No adjustment
*Pediatric:
*Pediatric: No adjustment


===Hepatic Dosing===
===Hepatic Dosing===
*Adult:
*Adult: Not defined, caution advised in hepatic impairment
*Pediatric:
*Pediatric: Not defined, caution advised in hepatic impairment


==Contraindications==
==Contraindications==
*Allergy to class/drug
*Allergy to class/drug
*Neonates <14 days old
*[[Long QT syndrome]]
*Hypokalemia


==Adverse Reactions==
==Adverse Reactions==
===Serious===
===Serious===
 
*QT prolongation/[[Torsade de pointes]]
*PR prolongation/AV block
*Hyperglycemia/[[diabetes mellitus]]
*Hypercholesterolemia/hypertriglyceridemia
*Pancreatitis
*Renal failure
*Hepatotoxicity
*Angioedema
*[[Toxic epidermal necrolysis]]
*[[Stevens-Johnson syndrome]]
*[[Immune reconstitution syndrome]]
*Autoimmune disorders
*[[Hypertension]]
*[[Syncope]]
*[[Orthostatic hypotension]]
*Myopathy
*[[Thrombocytopenia]]


===Common===
===Common===
 
*Nausea/vomiting
*Diarrhea
*Paresthesia
*Fatigue
*Rash
*Abdominal pain
*Cough
*[[Dysgeusia]]
*Oropharyngeal pain
*Dizziness
*AST, ALT, CK elevation
*Edema
*Acne
*Lipodystrophy


==Pharmacology==
==Pharmacology==
*Half-life:  
*Half-life: 5-6 hr
*Metabolism:  
*Metabolism: Liver (CYP450)
*Excretion:  
*Excretion: Fecal


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


==Comments==
==Comments==

Revision as of 19:24, 22 March 2020

Background

Ritonavir is usually given in combination with lopinavir 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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