Classes
DEA Class; Rx
Common Brand Names; Kaletra
- HIV, Protease Inhibitors
Description
A protease inhibitor (PI)
Indicated to treat HIV-1 infection when used in combination with other antiretroviral agents
Available as an oral solution and as full-strength and half-strength tablets
Indications
Indicated for the treatment of human immunodeficiency virus (HIV) infection in combination with other antiretroviral agents.
Contraindications
Hypersensitivity to ritonavir, lopinavir
Concomitant CYP3A4 inducers and/or major substrates
Drugs that are contraindicated with lopinavir/ritonavir include alpha1-adrenoreptor agonists (eg, alfuzosin), antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine, dronedarone), rifampin, lomitapide, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, lovastatin, simvastatin, lurasidone, ranolazine, pimozide, sildenafil (when used for PAH), midazolam, and triazolam, apalutamide, colchicine, elbasvir/grazoprevir
Adverse Effects
- Diarrhea (7-9%)
- Hyperlipidemia (3-39%)
- Nausea (5-16%)
- Rash (12%)
- Abdominal pain (1-11%)
- Nausea (5-16%)
- ALT increased (1-11%)
- Headache (2-6%)
- Elevated LFTs (2-10%)
- Weakness (< 9%)
- Hyperuricemia (< 5%)
- Flatulence (1-4%)
- Neutropenia (1-5%)
Warnings
Pancreatitis reported; fatalities have occurred; suspend therapy as clinically appropriate
Risk of immune reconstitution syndrome if used with HAART
Hepatotoxicity reported; fatalities have occurred; monitor liver function before and during therapy, especially in patients with underlying hepatic disease, including hepatitis B and hepatitis C, or marked transaminase elevations
Total cholesterol and triglycerides elevations may occur; monitor prior to therapy and periodically thereafter
QT and PR interval prolonation and torsades de pointes have been reported rarely; do not use saquinavir/ritonavir with congenital or documented acquired QT prolongation (>450 msec), refractory hypokalemia or magnesemia, and in combination with drugs that prolong QT interval
Cases of second and third degree heart block reported; use with caution in patients with pre-existing conduction system disease, ischemic heart disease, cardiomyopathy, underlying structural heart disease or when administering with other drugs that may prolong the PR interval
Risks of fat redistribution, hemolytic anemia, hyperglycemia, hyperbilirubinemia if used in combination with other antiretroviral drugs
Increased bleeding, including spontaneous skin hematomas and hemarthrosis reported in patients with hemophilia type A and B treated with protease inhibitors; A causal relationship between protease inhibitor therapy and these events has not been established
New onset diabetes mellitus, exacerbation of pre-existing diabetes mellitus, and hyperglycemia have been reported during post-marketing surveillance in HIV-1 infected patients receiving protease inhibitor therapy; consider monitoring for hyperglycemia, new onset diabetes mellitus or an exacerbation of diabetes mellitus
Adverse effects reported but casual link unclear includes new-onset or worsening of DM and bleeding problems
Pregnancy and Lactation
Available data from the Antiretroviral Pregnancy Registry show no difference in risk of overall major birth defects compared to background rate for major birth defects of 2.7% in the U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP); no treatment-related malformations observed when lopinavir in combination with ritonavir was administered to pregnant rats or rabbits; however embryonic and fetal developmental toxicities occurred in rats administered maternally toxic doses
The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1; because of potential for HIV transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and adverse reactions in breastfed infant, instruct mothers not to breastfeed if they are receiving therapy
Maximum Dosage
NOTE: The following maximum dosage limits apply for typical lopinavir; ritonavir use; maximum dosage limits may be altered based on certain individual patient circumstances, such as in the case of specific drug interactions.
800 mg/200 mg per day PO.
800 mg/200 mg per day PO.
more than 40 kg: 800 mg/200 mg per day.
36 to 40 kg: 800 mg/200 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day for oral solution (Max: 800 mg/200 mg per day) is recommended in the HIV guidelines.
31 to 35 kg: 600 mg/150 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day oral solution or 800 mg/200 mg per day for oral tablets is recommended in the HIV guidelines.
more than 40 kg: 800 mg/200 mg per day PO.
36 to 40 kg: 800 mg/200 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day for oral solution (Max: 800 mg/200 mg per day) is recommended in the HIV guidelines.
31 to 35 kg: 600 mg/150 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day for oral solution or 800 mg/200 mg per day for oral tablets is recommended in the HIV guidelines.
26 to 30 kg: 600 mg/150 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day oral solution is recommended in the HIV guidelines.
21 to 25 kg: 400 mg/100 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day for oral solution or 600 mg/150 mg per day for oral tablets is recommended in the HIV guidelines.
15 to 20 kg: 400 mg/100 mg per day PO for tablets; 20 mg/5 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day for oral solution is recommended in the HIV guidelines.
less than 15 kg: 24 mg/6 mg per kg/day or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day is recommended in the HIV guidelines. Safety and efficacy of the tablet formulation have not been established.
older than 6 months: 24 mg/6 mg per kg/day PO or 460 mg/115 mg per m2/day PO for oral solution is recommended in the FDA-approved labeling; however, up to 600 mg/150 mg per m2/day is recommended in the HIV guidelines. Safety and efficacy of the tablet formulation have not been established.
6 months or younger: 32 mg/8 mg per kg/day PO or 600 mg/150 mg per m2/day PO for oral solution. Safety and efficacy of the tablet formulation have not been established.
14 days postnatal age or older and 42 weeks postmenstrual age or older: 32 mg/8 mg per kg/day PO or 600 mg/150 mg per m2/day PO for oral solution. Safety and efficacy of other formulations have not been established.
younger than 14 days or postmenstrual age younger than 42 weeks: Not recommended.
How supplied
Lopinavir/ritonavir
tablet
- 100mg/25mg
- 200mg/50mg
oral solution
- (400mg/100mg)/5mL
