Lopinavir
in KALETRA
Pronunciation: loe-PIN-a-veer
What it isHIV protease inhibitor co-formulated with ritonavir; HIV.
Why this oneA robust resistance barrier and long global experience, including in pregnancy.
What limits itGI intolerance and dyslipidemia. The ritonavir component drives extensive CYP3A4 interactions.
FDA-approved for
- HIV infection (2000)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection | Adults | 800/200 mg QD or 400/100 mg BID | ||
| HIV-1 infection | Peds ≥14 days to <18 yr | BID by weight/BSA (e.g., 300/75 mg/m² BID) | 400/100 mg BID | |
| HIV-1 infection | Pregnancy | 400/100 mg BID |
Renal Undefined
Hepatic Use with caution (lopinavir levels may rise); not studied in severe impairment
Once-daily dosing not recommended in pediatric patients, pregnancy, or with efavirenz/nevirapine/nelfinavir or carbamazepine/phenobarbital/phenytoin
Instructions
- Tablets: swallow whole with or without food; do not chew, break, or crush
- Oral solution: must be taken with food; avoid in pregnancy and preterm neonates (ethanol/propylene glycol)
- Increase dose when given with efavirenz, nevirapine, or nelfinavir
Available strengths
- tab 100/25, 200/50 mg
- sol 80/20 mg/mL
Contraindications
- Co-administration with drugs highly dependent on CYP3A for clearance where elevated levels cause serious/life-threatening reactions (e.g., alfuzosin, ranolazine, dronedarone, colchicine, lurasidone, pimozide, ergot alkaloids, cisapride, lovastatin, simvastatin, oral midazolam, triazolam)
- Co-administration with potent CYP3A inducers that markedly reduce lopinavir levels (e.g., rifampin, St. John's Wort, apalutamide)
Cautions
- Serious drug interactions via CYP3A
- Toxicity in preterm neonates (oral solution excipients)
- Pancreatitis (fatalities reported)
- Hepatotoxicity (fatalities reported)
- QT prolongation / torsades
- PR prolongation and AV block
- New-onset/worsening diabetes, hyperglycemia
- Immune reconstitution syndrome
- Lipid elevations
- Fat redistribution
- Increased bleeding in hemophilia
Adverse reactions
- Diarrhea
- Nausea
- Vomiting
- Hypertriglyceridemia
- Hypercholesterolemia
Pregnancy Registry data show no increase in overall birth defects; use 400/100 mg BID; avoid oral solution due to ethanol
Lactation Breastfeeding not recommended (HIV transmission risk; potential adverse reactions)
Cost
NO BOXED WARNINGS
Principal riskGI intolerance and dyslipidemia from the ritonavir component