Last Updated June 10, 2016
HIV protease inhibitor antiretroviral
100/25 mg, 200/50 mg tablets; 80/20 mg/mL oral solution (42% alcohol)
Indication: treatment of HIV infection in combination with other antiretrovirals. Postexposure prophylaxis in combination with other antiretrovirals.
Mechanism of action*: Inhibits cleavage of viral gag-pol polyproteins precursors into functional proteins by binding to the HIV protease enzyme.
Pharmacokinetics*: metabolized in the liver CYP 450 3A4. Inhibits CYP 450 3A enzyme. Half life: 5-6 hours. Bioavailability enhanced by food.
Use in Renal or Hepatic Insufficiency: Use with caution in patients with liver disease or preexisting diabetes.
Lopinavir/ritonavir is highly metabolised in the liver and concentrations may be increased in patients with hepatic impairment. Therapeutic drug monitoring should be done if available.†
Use in Pregnancy and Breastfeeding: Excreted into breast milk.
Use in Children:
See Drug–Drug Interactions.
Contraindicated with porphyria.
Fasting lipid profile and blood glucose measurements should be taken before initiation and repeated at 6 months and then annually.
Contraindicated: lovastatin, simvastatin, cisapride, pimozide, oral midazolam, triazolam, dihydroergotamine, ergotamine, methylergonovine, St John’s wort, alfuzosin, sildenafil for pulmonary arterial hypertension.*
Increased concentrations of concomitant medication: antiarrhythmics, warfarin, rivaroxaban, trazodone, ketoconazole, itraconazole, clarithromycin, rifabutin (dose rifabutin 150 mg every other day†),
bosentan, fluticasone, glucocorticoids, atorvastatin, lovastatin, rosuvastatin, simvastatin, avanafil, sildenafil, tadalafil, vardenafil, dihydropyridine, midazolam, colchicine, bedaquiline, quetiapine, vincristine, vinblastine, dasatinib, nilotinib, simeprevir, cyclosporine, tacrolimus, sirolimus, budesonide, salmeterol, fentanyl.*
Decreased concentrations of concomitant medication: methadone, warfarin, lamotrigine, phenytoin, valproic acid, bupropion, voriconazole, ethinyl estradiol, norethindrone, atovaquone, boceprevir.*
Decreased concentrations of lopinavir/ritonavir with concomitant medication: boceprevir, carbamazepine, phenobarbital, phenytoin, dexamethasone, budesonide, prednisone, rifampin.*
Drug interactions between lopinavir/ritonavir and other antiretrovirals*:
See above for pregnancy and lactation.
Use with caution in patients with liver disease or preexisting diabetes.
Do not use in patients with porphyria.
Gastrointestinal symptoms (nausea, vomiting, diarrhoea, flatulence), pancreatitis, hyperlipidaemia, increased liver enzymes, hyperglycaemia/insulin resistance/diabetes, fat maldistribution, potential increased bleeding in patients with haemophilia, PR and QT prolongation possible, elevated serum transaminases.*
*Information from US prescribing information.
†Recommendation from Southern African HIV Clinician Society Guidelines.