Kaletra – brand name

Aluvia – brand name in some parts of the world

lopinavir/ritonavir – generic name

Kaletra belongs to a class of HIV drugs called protease inhibitors (PIs). Kaletra is actually two PIs combined into one tablet: lopinavir and ritonavir (Norvir).

The PIs block protease, a protein that HIV needs to make more copies of itself. This may slow down HIV disease.

The Food and Drug Administration (FDA) has approved Kaletra for use in combination with other HIV drugs for the treatment of HIV infection in adults and children 14 days old and over.

Kaletra comes in:

• Tablets that contain 200 milligrams (mg) lopinavir and 50 mg Norvir (200/50 mg)
• Tablets that contain 100 mg lopinavir and 25 mg Norvir (100/25 mg)
• Oral solution (liquid)

There are two options for taking Kaletra:

Once a day

• The standard dose is four 200/50 mg tablets of Kaletra once a day
• Once a day dosing is approved for HIV+ people who are starting therapy for the first time
• Once a day dosing is also approved for HIV+ people who have taken other HIV medications in the past, but who do not have significant drug resistance to Kaletra (have )– (see our info sheet on resistance for more info).
• Do not use once a day dosing in combination with Sustiva (efavirenz), Viramune (nevirapine), Lexiva (fosamprenavir), or Viracept (nelfinavir)
• Do not use once a day dosing in people less than 18 years old

Twice a day

• The standard dose is two 200/50 mg tablets of Kaletra twice a day
• Twice a day dosing is approved for HIV+ people who are starting therapy for the first time
• Twice a day dosing is approved for HIV+ people who have taken other HIV medications in the past

You can take Kaletra tablets with food or on an empty stomach, but taking it with food may cut down on side effects. Kaletra oral solution must be taken with food.

Refrigeration of Kaletra tablets is not necessary. The tablets can be stored at room temperature: 68°F to 77°F (20°C to 25°C). Kaletra liquid can be refrigerated or stored at room temperature for up to two months.

Check with your child’s health care provider for children’s dosing. Tell your health care provider if your child’s weight changes.

Kaletra must be used with other HIV medications to treat HIV.

Tell your health care provider if you have liver problems, heart problems, diabetes, or hemophilia.

If you forget to take Kaletra, take the missed dose right away. If it is almost time for your next dose, do not take the missed dose. Instead, follow your regular dosing schedule by taking your next dose at its regular time. Do not take more than one dose of Kaletra at one time.

As with all HIV drugs, it is important to take Kaletra as prescribed by your health care provider. Missing or skipping doses can cause your blood levels of Kaletra to fall too low and the virus can become resistant to it. This may cause Kaletra and other HIV drugs you are taking to stop working.

Kaletra can be used both for HIV+ people being treated for the first time and for those who are switching from other drugs that no longer work. Kaletra has worked well for many people who have failed other PIs in the past.

You and your health care provider can use resistance testing and your treatment history to guide the use of Kaletra and to determine which drugs are likely to work best for you.

If your virus develops resistance to Kaletra then it may stop working or not work as well for you. You also may not get as much benefit from the other PIs.

Sometimes taking more than one medication can cause drug interactions. This may cause the drugs not to work as well or cause an increased risk of side effects.

Kaletra can interact with other medications. Taking Kaletra with certain drugs can change the amount of each drug in your blood. Your health care provider may need to either adjust the doses of your drugs to avoid under- or overdosing or change the drugs you currently take.

Kaletra should not be taken with the following drugs:

• Acid reflux/heartburn medication: Propulsid (cisapride)
• Antibiotics: Priftin (rifapentine), Rifadin (rifampin)
• Antifungal: Vfend (voriconazole)
• Antimigraine medications (ergot-containing medicines): Ergostat, Cafergot, Ercaf, Wigraine (ergotamine), D.H.E. 45 (dihydroergotamine), Ergotrate (ergonovine), Methergine (methylergonovine)
• Antihistamines: Hismanal (astemizole), Seldane (terfenadine)
• Calcium channel blockers: Vascor (bepridil), Norvasc (amlodipine besylate), Procardia (nifedipine)
• Heart arrhythmia medications: Tambocor (flecainide), Rythmol (propafenone)
• Cholesterol-lowering drugs (statins): Zocor (simvastatin), Mevacor (lovastatin)
• Antipsychotic: Orap (pimozide)
• Sedatives: Versed (midazolam), Halcion (triazolam)
• Pulmonary arterial hypertension treatment: Revatio (sildenafil)
• Prostate medication: Uroxatral (alfuzosin)
• Inhaled medications: Serevent and Advair (salmeterol or salmeterol in combination with fluticasone propionate), Flonase (fluticasone propionate)
• Herbal product: St. John’s wort

If you are taking any of the following medications with Kaletra, speak to your health care provider as your doses may need to be adjusted:

• Cholesterol-lowering drugs (statins): Lipitor (atorvastatin), Crestor (rosuvastatin)
• HIV drugs: Atripla, Sustiva (efavirenz ),Viramune (nevirapine), Lexiva (fosamprenavir), Viracept (nelfinavir)
• Erectile dysfunction drugs: Viagra (sildenafil), Cialis (tadalafil), Levitra (vardenafil)
• Antibiotic: Mycobutin (rifabutin)
• Pulmonary arterial hypertension treatment: Tracleer (bosentan), Adcirca (tadalafil)
• Blood thinner: Coumadin (warfarin)

Dosage of methadone may need to be increased when taken with Kaletra.

The drug colchicine needs dose adjustments when taken with Kaletra. Colchicine should not be used at all with Kaletra if you have kidney or liver problems.

Do not take the anticonvulsants medications: Dilantin (phenytoin), Tegretol (carbamazepine), or pphenobarbitalhenobarbital if you are taking Kaletra once a day. The doses of these drugs need to be adjusted if you are taking Kaletra twice a day.

Kaletra decreases the effectiveness of birth control pills and patches, so alternative birth control methods should be used.

People taking liquid Kaletra should not take Antabuse (disulfiram) or Flagyl (metronidazole).

Because there are so many possible drug interactions with Kaletra, it is very important to go over all your medications with your health care provider. Be sure your health care provider knows about all the medications you are taking (including over-the-counter, prescription, street drugs, and herbs), even if you only use them occasionally.

For more information and additional resources to check interactions between the particular drugs you are taking, see our info sheet on drug interactions or go to:

http://www.hiv-druginteractions.org/
OR
http://hivinsite.ucsf.edu/insite?page=ar-00-02

It is not uncommon to experience Kaletra side effects. However, they are likely to be temporary and go away as your body adjusts to the medication. If you experience any of the side effects listed below, call your health care provider for advice. Do not just stop taking your medication.

• Diarrhea
• Nausea
• Vomiting
• Abdominal pain
• Headaches
• Fatigue (unusual tiredness)
• Weakness

More serious side effects:

• Liver toxicity: this may be indicated by elevated liver enzymes or yellowing of the skin and eyes (jaundice). People with liver diseases such as hepatitis B and C may have worsening liver problems. You should have tests to check your liver function before and while taking Kaletra.
• Pancreatitis (inflammation of the pancreas): symptoms include sudden or sharp pains in the middle of the abdomen, fever, nausea, or vomiting.
• Lipodystrophy, which may include elevated blood sugar (glucose), elevated lipid levels ( cholesterol and triglycerides), and fat gain or loss in certain areas. Kaletra can cause significant increases in lipid levels. The exact causes of lipodystrophy are not known, but may include HIV and/or HIV drugs. It is unclear if Kaletra will cause or impact other symptoms of lipodystrophy. For more information on lipodystrophy, see our info sheet.
• High blood sugar (hyperglycemia), diabetes, or worsening of diabetes may occur.
• Increased bleeding problems in some HIV+ people with hemophilia.
• A life-threatening hypersensitivity reaction (Stevens-Johnson syndrome): symptoms may include a severe rash, blisters, mouth sores, swelling, fever, and weakness. Swelling of the face, lips, and tongue (angioedema) has also been reported. Tell your health care provider if you get a rash or develop facial swelling.
• Some patients taking Kaletra have had changes in their heart rhythm. It is not know whether these changes were caused by Kaletra or by an interaction between Kaletra and some other medication the patients were taking. If you have any underlying problems with your heart, discuss with your health care providerdoctor whether you should take Kaletra.

If you are experiencing persistent, unusual, or serious side effects, call your health care provider right away.

Research on Kaletra pharmacokinetics (how the drug is processed by the body) has produced conflicting results. Some shows that the drug behaves similarly in the bodies of women and men, some suggests that women eliminate Kaletra faster than men, and some indicates that concentrations of Kaletra reach higher levels (as much as 20 percent higher) in women. The drug manufacturer does not recommend any dose adjustments based on weight or sex.

Studies to date show that Kaletra is one of the most effective HIV drugs. Study 863 compared Zerit (stavudine or d4T) plus Epivir (lamivudine or 3TC) plus Kaletra to Zerit plus Epivir plus Viracept (nelfinavir) in people who had not been treated before with PIs. This study included 20 percent women, or about 130 women out of 653 total participants. In this trial Kaletra worked better that Viracept, especially in people with high viral loads.

Study 888 compared Kaletra to other PIs when used with Viramune (nevirapine) plus nucleoside reverse transcriptase inhibitors (NRTIs). It included 288 participants who had experience taking other PIs, 14 percent (or about 40) of whom were women. In this study, people taking Kaletra were more likely to have undetectable HIV viral loads.

Study AI424-043 looked at 290 participants who had already used HIV drugs, 19 percent (or about 52) of whom were women. In this trial, Kaletra plus two NRTIs worked better than Reyataz (atazanavir) plus two NRTIs.

STAR and STELLA were two German studies that looked at people who had never taken HIV drugs before and were starting a Kaletra-based regimen. The studies reported no differences between men and women regarding treatment outcome (similar viral load decreases and CD4 cell increases) and similar rates of adverse events.

The CASTLE study compared Reyataz plus Norvir to Kaletra. The study found that Reyataz/Norivir and Kaletra worked equally well. It also found that CD4 cell increases and rates of adverse events were similar between genders.

In terms of side effects, some research suggests that women are more likely to experience gastrointestinal side effects while taking Kaletra, but that men are more likely to develop high blood fat levels. Some studies suggest that the metabolic side effects (lipodystrophy) associated with PIs may be somewhat different in women and men. However, it is still unclear if women are more likely to gain or lose body fat in certain areas than men.

Studies have shown that pregnant women who use HIV drugs can greatly reduce the risk of passing HIV on to their babies. There have been no formal studies of Kaletra during pregnancy.

An Antiretroviral Pregnancy Registry has been established to collect information on pregnant women who take HIV drugs, including Kaletra. If you are pregnant and taking Kaletra or other HIV drugs, your health care provider can register you by calling 1-800-258-4263 or going to www.apregistry.com.

It is not known whether Kaletra passes into breast milk. HIV+ women should not breast-feed because their babies could be infected with HIV through the breast milk.

Check with your health care provider about the best treatment options for you and your baby if you are thinking of getting pregnant.

Click this link for more information about pregnancy.

People who are starting HIV treatment for the first time may develop Immune Reconstitution Syndrome or IRS (also called Immune Reconstitution Inflammatory Syndrome or IRIS). IRS can happen as a result of the immune system getting stronger and responding to an HIV-related infection such as Mycobacterium avium infection (MAC), cytomegalovirus (CMV), Pneumocystis jirovecii pneumonia (PCP), or tuberculosis (TB). People may have been treated for these infections in the past or not even know they have them. If you notice any unusual symptoms soon after starting HIV drugs for the first time, let your health care provider know right away so you can be evaluated and, if necessary, treated.