Lopinavir

Aka: Lopinavir, Lopinavir/Ritonavir, Lopinavir/r, Kaletra, LPV, LPV/r

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II. Indications

  1. HIV Infection (part of combination therapy)

III. Mechanism

  1. See Protease Inhibitor

IV. Medications

  1. Lopinavir/Ritonavir (Kaletra) Tablets: 100/25 and 200/50 mg
    1. Do not crush, cut or chew
  2. Lopinavir/Ritonavir (Kaletra) Solution: 80/20 mg/ml
    1. Give buffered Didanosine either at least 1 hour before or 2 hours after Lopinavir/Ritonavir
    2. Ritonavir solution contains Alcohol
      1. With Feeding Tube administration, use only silicone or PVC
      2. Avoid polyurethane tubing due to Alcohols in solution

V. Dosing

  1. General
    1. Better tolerated when taken with food
    2. Typically used in its boosted form with Ritonavir (combined in Kaletra)
    3. Use in combination with other Antiretrovirals
  2. Adult
    1. Lopinavir/Ritonavir 800/200 mg orally once daily
    2. Lopinavir/Ritonavir 400/100 mg orally twice daily
      1. Dose twice daily if risk of resistance (>=3 resistance genes), pregnancy
      2. Dose twice daily if on Carbamazepine, Phenobarbital, Phenytoin
      3. Increase dose to 500/125 (tabs) or 533/133 (solution) twice daily if on Efavirenz, Nevirapine, Nelfinavir
  3. Child (off-label, but per guidelines)
    1. Doses are based on Lopinavir component (assumes use of Kaletra, combined Lopinavir with Ritonavir)
    2. Age 14 days to 12 months: Lopinavir 300 mg/m2
      1. Lopinavir 16 mg/kg orally twice daily
    3. Age 1 to 18 years
      1. Standard Dosing: All Lopinavir doses based on 300 mg/m2
        1. Weight: 13 to 15 kg: Lopinavir 13 mg/kg orally twice daily
        2. Weight: 15 to 45 kg: Lopinavir 11 mg/kg (up to 400 mg) orally twice daily
      2. Treatment-Naive Lower Dosing: All Lopinavir doses based on 230 mg/m2
        1. Weight: 13 to 15 kg: Lopinavir 12 mg/kg orally twice daily
        2. Weight: 15 to 45 kg: Lopinavir 10 mg/kg (up to 400 mg) orally twice daily
  4. Pregnancy
    1. Lopinavir/Ritonavir 400/100 mg orally twice daily
    2. Consider increasing to 600/150 mg orally twice daily in second and third trimesters
      1. Treatment experienced with prior Protease Inhibitor
      2. Viral load >50 copies/ml
      3. Higher dose directed by serum Lopinavir levels

VI. Adverse Effects

  1. See Protease Inhibitor for adverse effects attributed to the class
  2. Pancreatitis
    1. May be life threatening
  3. Cardiovascular
    1. Prolonged use increases risk of Myocardial Infarction
    2. PR Prolongation
    3. QT Prolongation

VII. Safety

  1. Avoid in Lactation
  2. Pregnancy
    1. Pregnancy registry exists
    2. Considered an alternative Protease Inhibitor for pregnant women, when other preferred agents are contraindicated

VIII. Drug Interactions

  1. See dosing above for interactions that lower Lopinavir/Ritonavir serum levels (and require twice daily and/or higher dose)
  2. Tenofovir
    1. Lopinavir/Ritonavir increases Tenofovir levels
  3. Oral Contraceptives (OCP)
    1. Decreased OCP effectiveness
  4. Statins
    1. Rosuvastatin dose limited to 10 mg
    2. Atorvastatin limited to lowest effective dose
  5. Voriconazole
    1. Ritonavir decreases Voriconazole levels and efficacy
    2. Avoid concurrent use if possible
  6. Opioids
    1. Methadone dose may need to be increased
    2. Fentanyl serum levels may be increased
  7. Clarithromycin
    1. Decrease Clarithromycin dose if Creatinine Clearance <60 ml/min
  8. Seizure medications
    1. Some antiepileptic agents lower Lopinavir levels (see dosing above)
    2. Monitor levels of Lamotrigine, Phenytoin and Valproic Acid

IX. Resources

  1. Lopinavir/Ritonavir (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8290add3-4449-4e58-6c97-8fe1eec972e3

X. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  3. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]

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Related Studies

Ontology: lopinavir (C0674432)

Definition (NCI) A peptidomimetic HIV protease inhibitor that retains activity against HIV protease with the Val 82 mutation. Lopinavir is less affected by binding to serum proteins than the structurally-related drug ritonavir.
Definition (NCI_NCI-GLOSS) A drug used with another drug, called ritonavir, to treat infection with HIV (the virus that causes AIDS). It is also being studied in the treatment of some types of cancer. Lopinavir blocks the ability of HIV to make copies of itself and may help some anticancer drugs work better. It is a type of anti-HIV agent and a type of protease inhibitor.
Definition (MSH) An HIV protease inhibitor used in a fixed-dose combination with RITONAVIR. It is also an inhibitor of CYTOCHROME P-450 CYP3A.
Definition (CSP) very potent inhibitor of HIV-1 protease; often coadministered with RITONAVIR.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D061466
SnomedCT 129475001, 387067003
LNC LP28756-2, MTHU014678
English LOPINAVIR, Lopinavir, N-(4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahydro-alpha-(1-methylethyl)-2-oxo-1(2H)-pydrimidineacetamide, lopinavir, Lopinavir [Chemical/Ingredient], Lopinavir (product), Lopinavir (substance)
French N-(4-(((2,6-diméthylphénoxy)acétyl)amino)-3-hydroxy-5-phényl-1-(phénylméthyl)pentyl)tétrahydro-alpha-(1-méthyléthyl)-2-oxo-1(2H)-pydrimidineacétamide, Lopinavir
Portuguese Lopinavir
Russian ЛОПИНАВИР, LOPINAVIR
Spanish Lopinavir, lopinavir (producto), lopinavir (sustancia), lopinavir
Czech Lopinavir
Polish Lopinavir, Lopinawir
Italian Lopinavir
German N-(4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahydro-alpha-(1-methylethyl)-2-oxo-1(2H)-pydrimidineacetamide, Lopinavir
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: lopinavir / Ritonavir (C0939237)

Definition (NCI) A fixed combination of two protease inhibitors, lopinavir and ritonavir, used to treat human immunodeficiency virus (HIV) infection. The ritonavir in the combination drug increases the concentration and biological half-life of lopinavir but is not present in sufficient concentration to act as a protease inhibitor.
Definition (NCI_NCI-GLOSS) A combination of the drugs ritonavir and lopinavir. It is used to treat infection with HIV (the virus that causes AIDS). It is also being studied in the treatment of some types of cancer. Lopinavir/ritonavir blocks the ability of HIV to make copies of itself and may help other anticancer drugs work better or may block the growth of cancer cells. Ritonavir blocks the breakdown of lopinavir. Lopinavir/ritonavir is a type of anti-HIV agent and a type of protease inhibitor.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
SnomedCT 134573001
LNC LP28548-3, MTHU018893
English RITONAVIR/LOPINAVIR @ @ UNIDENTIFIED, RITONAVIR/LOPINAVIR UNIDENTIFIED, LOPINAVIR/RITONAVIR, lopinavir + ritonavir, lopinavir + ritonavir (medication), Lopinavir + Ritonavir, lopinavir / Ritonavir, lopinavir ritonavir, lopinavir-ritonavir, lopinavir and ritonavir, Lopinavir+Ritonavir, lopinavir/ritonavir, Lopinavir+ritonavir (product), Lopinavir+ritonavir, Lopinavir+ritonavir (substance), Lopinavir/Ritonavir, Lopinavir and Ritonavir
Spanish lopinavir+ritonavir (producto), lopinavir+ritonavir
Derived from the NIH UMLS (Unified Medical Language System)

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