lopinavir and ritonavir, Kaletra

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

HIV/AIDS Myths and Facts

What is lopinavir and ritonavir, and how does it work (mechanism of action)?

Kaletra is an oral medication that is a combination of lopinavir and ritonavir. It is used for treating infections with the human immunodeficiency virus (HIV). It is in a class of drugs called protease inhibitors which, among others, includes ritonavir (Norvir), nelfinavir (Viracept) and saquinavir (Invirase, Fortovase). Although both lopinavir and ritonavir inhibit the HIV virus, they are combined in Kaletra because ritonavir increases the concentration of lopinavir in the body. In fact, the activity of Kaletra against HIV is due to the lopinavir because the amount of ritonavir in Kaletra is not enough to inhibit the HIV virus. During infection with HIV, the HIV virus multiplies within the body's cells. Viruses are released from the cells and spread throughout the body where they infect other cells. In this manner, HIV infection is perpetuated among new cells that the body produces continually. During the production of the viruses, new proteins for the viruses are made. Some of the proteins are structural proteins, that, is, proteins that form the body of the virus. Other proteins are enzymes which manufacture DNA and other components for the new viruses. Protease is the enzyme that forms the new structural proteins and enzymes. The lopinavir in Kaletra blocks the action of protease and results in the formation of defective viruses that are unable to infect the body's cells. As a result, the number of viruses in the body (the viral load) decreases. Nevertheless, Kaletra does not prevent the transmission of HIV among individuals, and it does not cure HIV infections or AIDS. Kaletra was approved by the FDA in September 2000.

What brand names are available for lopinavir and ritonavir?

Kaletra

Is lopinavir and ritonavir available as a generic drug?

GENERIC AVAILABLE: No

Do I need a prescription for lopinavir and ritonavir?

Yes

What are the side effects of lopinavir and ritonavir?

The most common side effects of Kaletra are:

Kaletra may cause liver failure and failure of the pancreas. Like other protease inhibitors use of Kaletra may be associated with:

Kaltera should be used cautiously in patients with pre-existing heart conditions.

Quick GuideHIV AIDS Facts: Symptoms and Treatments

HIV AIDS Facts: Symptoms and Treatments

What is the dosage for lopinavir and ritonavir?

Kaletra tablets may be administered with or without food. Oral solution and capsules should be administered with food. There are several dosing regimens depending on the formulation used, age of the patient, previous exposure to lopinavir, or use of other drugs. Here are some examples.

  • Therapy-naive adult patients: 400/100 tablets (3 capsules) twice daily or 800/200 (6 capsules) once daily; Oral solution, 5 mL twice daily or 10 mL once daily with food.
  • Therapy-experienced adult patients: 200/50 tablets, two twice daily or 3 capsules twice daily; Oral solution 5 mL twice daily. Once daily administration of Kaletra is not recommended.
  • Children between 6 months and 18 years of age: The recommended dose is 230/57.5/m2 of the oral solution given twice daily and not to exceed the recommended adult dose. Kaletra should not be administered once daily in patients less than 18 years of age.
  • Children between 14 days and 6 months of age: The recommended dose is 16/4/kg or 300/75/m2 of the oral solution given twice daily.
  • In combination with efavirenz (Sustiva), nevirapine (Viramune), fosamprenavir (Lexiva) or nelfinavir (Viracept): Once daily administration is not recommended when combined with efavirenz, nevirapine, fosamprenavir or nelfinavir. For adults, the recommended dose is two 200/50 tablets and one 100/25 tablet twice daily; Oral solution, 6.5 mL twice daily. For children, the recommended dose is 300/75/m2 not to exceed the adult dose.

Which drugs or supplements interact with lopinavir and ritonavir?

Kaletra interacts with many drugs. Some of the important interactions are mentioned below. Patients should consult their healthcare provider before combining any drug with Kaletra.

Kaletra should not be used together with amiodarone (Cordarone), quinidine (Quinaglute, Cardioquin), triazolam (Halcion), midazolam (Versed), pimozide (Orap), ergotamine derivatives (for example, Ergostat), propafenone (Rythmol) and flecainide (Tambocor) because Kaletra increases the levels of these drugs in the body and as a result may lead to serious adverse effects of these drugs.

Kaletra may also prevent the break down of lovastatin (Mevacor), simvastatin (Zocor), rosuvastatin (Crestor) and atorvastatin (Lipitor), causing their levels in the body to rise. This may increase the occurrence of muscle breakdown (rhabdomyolysis), which is a side effect of these drugs. Therefore, lovastatin and simvastatin should not be combined with Kaletra; the dose of rosuvastatin should not exceed 10 mg/day and the lowest dose of atorvastatin should be used. The blood concentration of rifabutin (Mycobutin) and sildenafil (Viagra) can be increased by Kaletra. Therefore, the doses of rifabutin and sildenafil should be reduced.

The oral solution contains alcohol, which causes severe side effects when combined with metronidazole (Flagyl) or disulfiram (Antabuse).

Kaletra can reduce the effectiveness of oral contraceptives.

Rifampin (Rifadin), St. John's wort, efavirenz (Sustiva) and nevirapine (Viramune) decrease the blood levels of Kaletra and this can reduce the effectiveness of Kaletra.

Is lopinavir and ritonavir safe to take if I'm pregnant or breastfeeding?

Use of Kaletra during pregnancy has not been adequately evaluated.

It is not known whether Kaletra is excreted in breast milk. Nevertheless, HIV-infected mothers should not breastfeed because of the potential risk of transmitting HIV to an infant that is not infected.

What else should I know about lopinavir and ritonavir?

What preparations of lopinavir and ritonavir are available?

Tablets (mg lopinavir/mg ritonavir): 100/25 and 200/50. Oral solution: 80/20 per mL. Capsules: 133/33.3.

How should I keep lopinavir and ritonavir stored?

Capsules and solution should be refrigerated at 2 C to 8 C (36 F to 46 F). If stored at room temperature, the capsules and solution should be used within 2 months. Tablets should be stored at 15 C to30 C (59 F to 86 F).

Reference: FDA Prescribing Information

Last Editorial Review: 7/9/2015

FDA Logo

Report Problems to the Food and Drug Administration

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.

Reviewed on 7/9/2015
References
Reference: FDA Prescribing Information

Health Solutions From Our Sponsors