LOPINAVIR + ritonavir (Kaletra)

WHAT IS LOPINAVIR?
Lopinavir is a drug used as part of antiretroviral therapy (ART). Lopinavir used to be called ABT-378. It is manufactured by Abbott Laboratories. Lopinavir is a protease inhibitor. The amount of Lopinavir in the blood stream stays much higher if it is taken with a small amount of ritonavir, another protease inhibitor. See Fact Sheet 442 for more information on ritonavir. Kaletra® is a combination of lopinavir and ritonavir in the same tablet. In the developing world, Kaletra is sold as Aluvia.

Protease inhibitors prevent the protease enzyme from working. HIV protease acts like a chemical scissors. It cuts the raw material for HIV into specific pieces needed to build a new virus. Protease inhibitors "gum up" these scissors.
WHO SHOULD TAKE KALETRA?
Kaletra was approved in 2000 as an antiretroviral drug (ARV) for people with HIV infection. It has been studied in adults and children 6 months old or older.

There are no absolute rules about when to start ART. You and your health care provider should consider your CD4 cell count, your viral load, any symptoms you are having, and your attitude about taking ARVs. Fact Sheet 404 has more information about guidelines for the use of ART.

If you take Kaletra with other ARVs, you can reduce your viral load to extremely low levels, and increase your CD4 cell counts. This should mean staying healthier longer.
WHAT ABOUT DRUG RESISTANCE?
Many new copies of HIV are mutations. They are slightly different from the original virus. Some mutations can keep multiplying even when you are taking an ARV. When this happens, the drug will stop working. This is called "developing resistance" to the drug. See Fact Sheet 126 for more information on resistance.

Sometimes, if your virus develops resistance to one drug, it will also have resistance to other ARVs. This is called "cross-resistance."

Kaletra provides blood levels that are high enough to control HIV that has already developed some resistance to other protease inhibitors.

Resistance can develop quickly. It is very important to take ARVs according to instructions, on schedule, and not to skip or reduce doses.
HOW IS KALETRA TAKEN?
A film-coated tablet of Kaletra was approved in October 2005. The tablet replaces the original gelatin capsule version. Each tablet contains 200 milligrams (mg) of lopinavir and 50 mg of ritonavir. The normal dose is two tablets twice a day or four tablets once a day for patients just starting antiviral treatment. It is also available in liquid form. The normal adult dose is 5 milliliters (ml) twice a day. Kaletra tablets can be taken with or without food. Kaletra liquid should be taken with food.

Different doses are used in some combinations. Be sure you know how much Kaletra your health care provider has prescribed for you, and when and how to take each dose.

Kaletra is approved for use by children. Their dosage is based on their body weight.

Kaletra tablets should be kept at room temperature. They are not sensitive to heat. Kaletra liquid can be refrigerated or stored at room temperature for up to 2 months.

The older capsule version of Kaletra will be phased out by Abbott. Where the capsules are used, they should be stored at or below 25 degrees Celsius (77 degrees Fahrenheit). At higher temperatures, they can become soft and sticky and form clumps. The capsules may stick together and be difficult to separate. They may lose potency.
WHAT ARE THE SIDE EFFECTS?
The most common side effects of Kaletra are diarrhea, fatigue, headache, and nausea. None of these side effects seem to be very serious. Kaletra can increase the amount of fat (cholesterol and triglycerides) in your blood. High levels of blood fats can increase your risk of problems with your heart or pancreas. The new tablet formulation is expected to cause fewer side effects.
HOW DOES KALETRA REACT WITH OTHER DRUGS?
Kaletra can interact with other drugs or supplements that you are taking. These interactions can change the amount of each drug in your bloodstream and cause an under- or overdose. New interactions are being identified all the time.

Drugs to watch out for include other ARVs, drugs to treat tuberculosis (see fact sheet 518), for erectile dysfunction (such as Viagra), for heart rhythm (antiarrhythmics), and for migraine headaches. Interactions are also possible with several antihistamines (allergy medications), sedatives, drugs to lower cholesterol, and anti-fungal drugs. Make sure that your health care provider knows about ALL drugs and supplements you are taking.

If you are taking liquid Kaletra and ddI, you should take ddI one hour before or two hours after Kaletra. These restrictions do not apply to the new Kaletra tablets.

Take Kaletra one hour apart from antacids.

Kaletra lowers blood levels of methadone. Watch for signs of excessive sedation with buprenorphine.

Nelfinavir lowers blood levels of Kaletra.

Some birth control pills may not work if you are taking Kaletra. Talk to your health care provider about how to prevent an unwanted pregnancy.

The herb St. John's Wort (See Fact Sheet 729) lowers the blood levels of some protease inhibitors. Do not take it with Kaletra.

Kaletra lowers blood levels of lamotrigine, a drug used to treat epilepsy and neuropathy.