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KALETRA

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Basic Informations

Kaletra is an HIV medication. It is in a category of HIV medicines called protease inhibitors (PIs). Kaletra prevents cells infected by HIV from producing new virus. This reduces the amount of virus in your body, and can increase the number of CD4 cells.

Kaletra, sold as Aluvia in some parts of the world, is manufactured by Abbott Laboratories. The U.S. Food and Drug Administration (FDA) approved it for the treatment of HIV infection, in both adults and children, in 2000.

Kaletra is actually two drugs combined into a single capsule: lopinavir and low dose ritonavir (Norvir), another protease inhibitor manufactured by Abbott Laboratories. This is because ritonavir increases the amount of lopinavir in the blood, thus making it more effective against HIV.

Drugs Interactions

Kaletra is broken down (metabolized) by the liver, like many medications used to treat HIV and AIDS. This means that Kaletra can interact with other medications. Kaletra can lower or raise the levels of other medications in the body. Similarly, other medications can lower or raise the levels of lopinavir and/or ritonavir found in Kaletra in the body. While many interactions are not a problem, some can cause your medications to be less effective or increase the risk of side effects.

Kaletra tablets and Kaletra capsules should be treated the same with respect to drug interactions. Both formulations of Kaletra can interact with other drugs.

Tell your doctors and pharmacists about all medicines you take. This includes those you buy over-the-counter and herbal or natural remedies, such as St. John’s Wort. Bring all your medicines when you see a doctor, or make a list of their names, how much you take, and how often you take them. Your doctor can then tell you if you need to change the dosages of any of your medications.

The following medications should not be taken while you are being treated with Kaletra:

  • Acid reflux/heartburn medications: Propulsid (cisapride)

  • Antibiotics: Rifadin (rifampin)

  • Antimigraine medications: Ergostat, Cafergot, Ercaf, Wigraine (ergotamine) or D.H.E. 45 (dihydroergotamine)

  • Pulmonary hypertension medications: sildenafil (Revatio)

  • Cholesterol-lowering drugs (statins): Zocor (simvastatin) and Mevacor (lovastatin)

  • Antipsychotics: Orap (pimozide)

  • Sedatives: Versed (midazolam) and Halcion (triazolam)

  • Enlarged prostate: Uroxatral (alfuzosin)

HIV protease inhibitors can interact with Kaletra. In fact, the interactions between Kaletra and other protease inhibitors can be very tricky, given that three protease inhibitors are being used, which can result in confusing three-way drug interactions. For example, Kaletra can significantly lower blood levels of Prezista (darunavir), whereas it can increase blood levels of Reyataz (atazanavir), Crixivan (indinavir), Viracept (nelfinavir) and Invirase (saquinavir). These protease inhibitors can also affect lopinavir levels in the blood. Until dosing studies are completed, Kaletra should not be combined with Prezista, Lexiva (fosamprenavir) or Aptivus (tipranavir). If Kaletra is used with Crixivan, the Crixivan dose should be lowered to 600 mg twice daily. If Kaletra is combined with Invirase, the Invirase dose should be 1000 mg twice-daily. Dosing recommendations for Kaletra combined with either Reyataz or Viracept have not been established.

HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs) can also interact with Kaletra. Viramune (nevirapine) and Sustiva (efavirenz) can decrease the amount of lopinavir in Kaletra in the bloodstream. If Kaletra is combined with Viramune or Sustiva, the Kaletra dose should be increased to two 200/50 mg tablets plus one 100/25 mg tablet twice a day. Intelence (etravirine) may slightly decrease lopinavir blood levels, though it is not clear if the dose of Intelence of Kaletra requires adjustment if both are used together.

Viread (tenofovir), a nucleotide reverse transcriptase inhibitor, can decrease Kaletra levels in the bloodstream. Kaletra increases Viread levels in the bloodstream. If Kaletra and Viread are used together, it is important to watch out for potential side effects of Viread (e.g., kidney problems).

Kaletra can increase blood levels of the painkiller Sublimaze (fentanyl). Careful monitoring for Sublimaze side effects is necessary if the two are combined.

Another painkiller, methadone, commonly used to treat drug addiction, can interact with Kaletra. Methadone levels in the bloodstream can decrease when combined with Kaletra. Because of this, it might be necessary to increase the dose of methadone.

Anticonvulsants, such as Tegretol ( carbamazepine), Luminal (phenobarbital), and Dilantin (phenytoin), may interact with Kaletra and should be used with caution. Combining these drugs with once-daily Kaletra is not recommended.

Antabuse (disulfiram) is a medication taken by people with an alcohol-dependency problem. This medication can make people very sick if they consume even small amounts of alcohol. Because liquid Kaletra contains small amounts of alcohol, it should not be combined with Antabuse. Kaletra capsules can be combined Antabuse.

Flagyl (metronidazole) is used to treat some types of parasitic infections. People should not drink alcohol—or take medications that contain alcohol—while taking this drug. The combination of alcohol and Flagyl can cause someone to become very ill. In turn, HIV-positive people taking liquid Kaletra should not take Flagyl. Kaletra capsules can be taken with Flagyl.

Kaletra can interact with some medications used to treat TB, MAC, and other bacterial infections. Rifadin (rifampin) can decrease Kaletra levels and Kaletra can increase Rifadin levels (these drugs should not be used together). Kaletra can increase Mycobutin (rifabutin) (the Mycobutin dose will need be reduced to 150mg every other day or three-times-weekly). Kaletra also raises Biaxin (clarithromycin) levels in the bloodstream and a lower dose of Biaxin should be used in people with kidney problems.

Kaletra can interact with some medications used to treat thrush (candidiasis) and other fungal infections. Kaletra can increase Nizoral (ketoconazole) and Sporanox (itraconazole) levels in the bloodstream and lower Vfend (voriconazole) blood levels, so other antifungal drugs should be used instead wherever possible.

Kaletra decreases the amount of oral contraceptives (taken by women to help avoid pregnancy) in the bloodstream. This means that there may be a higher risk of becoming pregnant if Kaletra and oral contraceptives are taken at the same time. To reduce the risk of pregnancy, barrier protection (e.g., condoms) should be used.

Kaletra can increase the blood levels of two anti-cancer chemotherapies, Oncovin (vincristine) and Velbe (vinblastine), and increase the side effects of those drugs. People taking Kaletra combined with either of these two drugs who develop severe chemotherapy side-effects should switch to an alternative HIV regimen.

Kaletra can alter blood levels of two common antidepressants. It decreases Wellbutrin (bupropion) levels and increases Desyrel (trazadone) levels. Combining these drugs with Kaletra should be done with caution.

Kaletra can lower the blood levels of a drug called Mepron (atovaquone), which is used to treat parasites. An alternate antiparastic drug should be used.

Cholesterol-lowering drugs, also known as "statins," can interact with Kaletra. There are two statins that should not be used with Kaletra: Zocor (simvastatin) and Mevacor (lovastatin). Levels of these two drugs can become significantly increased in the bloodstream if they are combined with Kaletra, which increases the risk of side effects. The two statins that are considered to be the safest in combination with Kaletra are Pravachol (pravastatin) and Lescol (fluvastatin). It is also possible to take Kaletra with Lipitor (atorvastatin) and Crestor (rosuvastatin), although Kaletra can increase the levels of these drugs in the bloodstream. If Lipitor or Crestor is prescribed, it's best to begin treatment with the lowest possible dose of the drug and then increase the dose if necessary.

Kaletra can increase blood levels of cochicine, which is used to treat gout. Lower doses of colchicine are recommended, and the two drugs should not be used together in people with liver or kidney impairment.

Some patients with asthma, bronchitis, or emphysema (chronic obstructive pulmonary disorder) take a drug called theophylline. Kaletra can decrease the amount of theophylline in the bloodstream. If these two drugs are taken at the same time, a doctor can order a blood test to check the level of theophylline in the bloodstream. If the theophylline level is too low, the dose can be increased.

Some patients with asthma, bronchitis, or emphysema also take a drug called fluticasone (found in Flovent and Advair), an inhaled medication known as a corticosteroid. Some patients taking fluticasone while taking ritonavir have experienced Cushing's syndrome, a hormonal disorder that can cause a variety of symptoms (e.g., extreme puffiness, easily damaged skin, fatigue, weakness). It is possible that ritonavir increases fluticasone levels in the body, leading to an increased risk of Cushing's syndrome. Care should be taken if Kaletra and fluticasone are used together, until more studies are completed.

Some patients with asthma, bronchitis, or emphysema also take a drug called salmeterol (found in Serevent and Advair), a long-acting beta2-adrenergic receptor agonist that is inhaled. Using salmeterol and Kaletra together is not recommended, as salmeterol levels can become increased and cause heart rhythm abnormalities.

Kaletra can affect the blood levels of a variety of medications used to treat different manifestations of heart disease, including high blood pressure and heart rhythm disturbances. Kaletra increases the blood levels of many calcium channel blockers (used for high blood pressure), including Plendil (felodipine), Procardia (nifedipine) and Cardene (nicardipine). These should be used with caution when combining them with Kaletra.

Kaletra can also increase the blood levels of Coumadin (warfarin), which is used to inhibit blood clots. Caution is also warranted when combining these two drugs. Kaletra can also significantly increase the blood levels of drug used to treat heart rhythm disturbances, including: Cordarone (amiodarone), Vascor (bepridil), systemic lidocaine and Quinaglute/Quinidex (quinidine). Caution is also warranted when using these drugs with Kaletra.

There is a class of drugs, known as PDE-5 inhibitors that are used to treat both erectile dysfunction and pulmonary arterial hypertension. Their brand names differ, depending on their use. Kaletra can significantly increase blood levels of these drugs.
When used to treat erectile dysfunction, it is best to use a lower dose of Viagra (sildenafil), Levitra (vardenafil) and Cialis (tadalafil) in order to reduce the risk of side effects. When used to treat pulmonary arterial hypertension, the dose of tadalafil (Adcirca) must be reduced if combined with Kaletra. Revatio (sildenafil) and Kaletra should not be used together.

Tracleer (bosenstan) is another type of drug used to treat pulmonary arterial hypertension, called an endothelin receptor antagonist. Kaletra can increase Tracleer blood levels, so the dose of Tracleer should be reduced.

Kaletra can increase the blood levels of several drugs used to suppress the immune system, generally after transplants. Therapeutic drug monitoring of these drugs—which include Gengraf (cyclosporine), Prograf (tacrolimus), Sirolimus (rapamycin)—is recommended.

Herbal products can also interact with Kaletra. St. John's wort should not be used with Kaletra, since it can greatly reduce the amount of the Kaletra in the bloodstream. HIV-positive people should also be cautious about using garlic supplements or milk thistle with Kaletra—test tube studies suggest that both herbal products can interact with the same liver enzyme system (cytochrome P450 3A4) responsible for metabolizing Kaletra. This may alter the amount of Kaletra in the bloodstream. These and other herbal products should be used with caution, until further studies are conducted.

Other drug interactions are possible. Be sure to tell your doctor about all the medications you are taking (or plan to take), including those you buy over-the-counter at your pharmacy or health-food store, while taking Kaletra.

Side Effects

The most common side effects seen in people taking Kaletra are abnormal stools (bowel movements), feeling weak/tired, headache, diarrhea, nausea, and vomiting. Children may sometimes get a skin rash.
Blood tests in people taking Kaletra may show possible liver problems. People with liver diseases such as hepatitis B or C who take Kaletra may have worsening liver disease. Liver problems including death have occurred in patients taking Kaletra, but it is unclear if Kaletra caused these liver problems because some patients had other illnesses or were taking other medicines.

Some people taking Kaletra can develop serious problems with their pancreas (pancreatitis), which may cause death. This is especially true in people who have had pancreatitis in the past. Tell your doctor if you have nausea, vomiting, or abdominal pain, since these may be signs of pancreatitis.

Some people may have large increases in their lipid levels (triglycerides and cholesterol). The long-term chance of getting complications such as heart attacks or stroke due to increases in blood lipids caused by protease inhibitors is not known at this time. Click here for our lesson called "Risks To Your Heart (Hyperlipidemia)".

Diabetes and high blood sugar may occur in people who take Kaletra or other protease inhibitors.

HIV drug regimens containing protease inhibitors, including Kaletra, can cause abnormal body-shape changes (lipodystrophy; including increased fat around the abdomen, breasts, and back of the neck, as well as decreased fat in the face, arms, and legs).