Lopinavir
Revision as of 19:24, 22 March 2020 by Ihearttroponin (talk | contribs)
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
- 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)
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
- Allergy to class/drug
- Neonates <14 days old
- Long QT syndrome
- Hypokalemia
Adverse Reactions
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
- 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
- ↑ 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