Classifications: antiretroviral agent; protease inhibitor; Therapeutic: antiretroviral agent; protease inhibitor
Prototype: Saquinavir mesylate
Pregnancy Category: C
200 mg lopinavir/50 mg ritonavir tablets; 400 mg lopinavir/100 mg ritonavir/5 mL suspension
Lopinavir, an HIV protease inhibitor that inhibits the activity of HIV protease and prevents the cleavage of viral polyproteins
essential for the maturation of HIV. Ritonavir inhibits the CYP3A metabolism of lopinavir, thereby, increasing the blood
level of lopinavir.
Decreases plasma HIV RNA level; reduces viral load as a result of the combined therapy of the two drugs in HIV infected
Treatment of HIV infection in combination with other antiretroviral agents.
Hypersensitivity to lopinavir or ritonavir; concurrent administration with drugs that utilize CYP3A or CYP2D6 for metabolism
(e.g., ergotamine, pimozide); pregnancy (category C), lactation. Safety and efficacy in children <6 mo are not established.
Hepatic impairment, patients with hepatitis B or C, older adults; diabetes mellitus.
Route & Dosage
|HIV InfectionTreatment Na?ve
Adult: PO 800/200 mg q.d.
HIV InfectionTreatment Experienced
Adult: PO 400/100 mg (3 capsules or 5 mL suspension) b.i.d., increase dose to 533/133 mg (4 capsules or 6.5 mL) b.i.d., with concurrent
efavirenz or nevirapine
Child: PO 6 mo12 y, 715 kg, 12/3 mg/kg; 1540 kg, 10/2.5 mg/kg; >40 kg, 400/100 mg b.i.d., increase dose 715 kg, 13/3.25 mg/kg; 1540 kg, 1?.75 mg/kg; >40 kg, 533/133 mg b.i.d., with concurrent efavirenz or nevirapine
Note: Take with food. Oral
- Give with a meal or light snack.
- Note: If didanosine is concurrently ordered, give didanosine 1 h before or 2 h after lopinavir/ritonavir.
- Store refrigerated at 2°8° C (36°46° F). If stored at room temperature ≤25°
C (77° F), discard after 2 mo.
Adverse Effects (≥1%)Body as a Whole:
Asthenia, pain. GI:
Abdominal pain, abnormal stools, diarrhea, nausea,
InteractionsDrug: Flecainide, propafenone, pimozide
may lead to life-threatening arrhythmias; rifampin
may decrease antiretroviral response; dihydroergotamine, ergonovine, ergotamine, methylergonovine
may lead to acute ergot toxicity
; hmg-coa reductase inhibitors
may increase risk of myopathy and rhabdomyolysis; benzodiazepines
may have prolonged sedation or respiratory depression; efavirenz, nevirapine, anticonvulsants
may decrease lopinavir levels; delavirdine, ritonavir
may increase lopinavir levels; may increase levels of amprenavir, indinavir, saquinavir, ketoconazole, itraconazole, midazolam, triazolam, rifabutin, sildenafil, atorvastatin, cerivastatin, immunosuppressants
; may decrease levels of atovaquone, methadone, ethinyl estradiol.
Also see INTERACTIONS
monograph. Herbal: St. John's wort, garlic
may decrease antiretroviral
Increased absorption when taken with food. Peak:
4 h. Distribution:
9899% protein bound. Metabolism:
Extensively metabolized by CYP3A. Elimination:
Primarily in feces. Half-Life:
56 h lopinavir.
Assessment & Drug Effects
- Monitor for S&S of: Pancreatitis, especially with marked triglyceride elevations; new onset diabetes or loss of glycemic
control; hypothyroidism or Cushing's syndrome.
- Lab test: Periodically monitor fasting blood glucose, AST & ALT, total cholesterol & triglycerides, serum amylase, inorganic
phosphorus, CBC with differential, and thyroid functions.
Patient & Family
- Report all prescription and nonprescription drugs being taken. Do not use herbal products, especially St. John's wort, without
first consulting the physician.
- Become familiar with the potential adverse effects of this drug; report those that are bothersome to physician.
- Concurrent use of sildenafil (Viagra) increases risk for adverse effects such as hypotension, changes in vision, and sustained
erection; promptly report any of these to the physician.
- Use additional or alternative contraceptive measures if estrogen-based hormonal contraceptives are being used.