Lopinavir

in KALETRA

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

FDA dosing	Population	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

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

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)

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)

NO BOXED WARNINGS

Principal riskGI intolerance and dyslipidemia from the ritonavir component

Direct muscarinic antagonism0 / 4