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Common Name:
lopinavir/ritonavir (LPV/r)
Brand Name:
Kaletra |
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Class: HIV protease inhibitor (PI)
Standard dose: Two 200/50 mg tablets twice a day or four 200/50 mg tablets once daily for first time therapy (no once-daily dose if taken with Sustiva or Viramune). Three tablets twice a day may be considered for treatment experienced or those taking it with Sustiva or Viramune. Half-strength film-coated tablet now available: 100 mg lopinaivr and 25 mg ritonavir. Take with or without food, preferably with food to lessen side effects; liquid formula available. Take missed dose as soon as possible, but do not double up on your next dose.
AWP: $794.99 / month
Manufacturer contact: Abbott Laboratories,
www.kaletra.com, 1 (800) 222–6885
AIDSInfo:
1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
Potential side effects and toxicity: Diarrhea is the most common. Rash, nausea, vomiting, stomach pain, headache, muscle weakness, increased cholesterol and triglycerides (fats in the blood), and liver function tests, a sign of liver damage—this may be more common in people with hepatitis B or C. As seen with other protease inhibitors, there can be increased levels of cholesterol and triglycerides (except possibly unboosted Reyataz) which may be associated with an increased risk of heart disease. Other possible side effects seen with protease inhibitors are lipodystrophy (body fat changes, including thinning of the face, arms and legs, with or without fat accumulation in the stomach, breasts and sometimes the upper back), onset of new cases or worsening of diabetes (see your doctor promptly) and increased bleeding in hemophiliacs. Immune Reconstitution Inflammatory Syndrome (IRIS) may occur as the immune system regains strength; report symptoms of illness, such as shingles and TB, to health care provider.
Potential drug interactions: e taking. Do not take with Tambocor, Rythmol, Cordarone, Versed, Halcion, Uroxatral, rifampin, pimozide, ergot derivatives (such as Cafergot, Wigraine, Methergine, and D.H.E. 45), garlic supplements, or the herb St. John’s wort. Do not use Zocor, Vytorin or Mevacor; lipid-lowering alternatives are Lipitor, Lescol, and pravastatin, but they should be used with caution due to potential for liver toxicity. Oral solution contains alcohol, so do not use with Antabuse or Flagyl (metronidazole). Avoid certain calcium channel blockers.
Dosage of methadone may need to be increased when taken with Kaletra. Increase Kaletra dose to three tablets twice-a-day with food recommended when using with Sustiva or Viramune in people who previously took HIV drugs, especially protease inhibitors. Not recommended to be taken with Lexiva. Kaletra may lower levels of zidovudine (Retrovir) and Ziagen. Videx should be given an hour before or two hours after Kaletra, if Kaletra is taken with food. Mycobutin (rifabutin) dosage should be reduced to 150 mg every other day (or 150 mg three times per week) when used with Kaletra. Phenobarbital, phenytoin or carbamazepine may lower blood levels of Kaletra. Reduces effectiveness of birth control pills; use alternative contraceptive. Mepron levels may be reduced with Kaletra. Avoid Sporanox doses greater than 200 mg per day with Kaletra. People with kidney impairment may require lower Biaxin doses with Kaletra. Immunosuppresants require close monitoring with Kaletra. Kaletra may alter Coumadin levels. Steroids, especially Decadron, may decrease levels of Kaletra. Increases levels of fluticasone (active component of Advair, Flonase, Flovent) and trazodone. Cialis, Levitra, and Viagra levels are increased; doses should not exceed 10 mg Cialis per 72 hours, 2.5 mg Levitra per 24 hours, or 25 mg Viagra per 48 hours.
Tips: Kaletra twice daily was the first protease inhibitor recommended by U.S. treatment guidelines for first-time therapy. The newer formulation doesn’t require refrigeration (especially important for resource-poor countries) and has fewer food restrictions. Great viral load results out to 7 years in people on their first HIV regimen. Good results also seen in heavily treatment-experienced adults, when compared to Reyataz, even those with protease inhibitor resistance. Use Kaletra with caution in people with mild to moderate liver impairment. The taste may be unappealing due to Norvir. Four tablets once daily can increase side effects, especially diarrhea. Solution (40% alcohol with peppermint taste) should be stored in the refrigerator, but is stable for up to 60 days at room temperature (77 F°). However, avoid extreme heat and bright light. New healthcare letter on pediatric dosing following a death from overdose: carefully follow instructions. Lower blood concentrations during the third trimester of pregnancy have been observed. This may require dose adjustment. Avoid the oral solution during pregnancy. Please see package insert for more complete potential side effects and interactions.
Kaletra is the only PI that contains a boosting dose of Norvir within the same tablet as the active PI (lopinavir). That’s probably its strongest advantage over other PIs, because it means fewer prescriptions, fewer co-pays, and no concerns about refrigeration or running out of one before the other. The new tablet formulation has also reduced the pill burden to 4 per day and has made it easier on the stomach. Kaletra is also the most extensively studied of the boosted PIs, and has been the “gold standard” in that class for a long time. It’s effective at high viral loads and low CD4 counts, and can be taken with or without food, once or twice a day, though twice daily dosing may be a little more effective. Now that Viracept has been taken off the list, Kaletra is the only PI recommended for pregnant women. However, Kaletra has lost its “king of the world” status in the last few years. Other PIs appear to be as effective (Reyataz, Lexiva, and Invirase) or maybe even better (Prezista), and some, such as Reyataz and Prezista, may have fewer side effects (diarrhea and lipid elevation). Sustiva also outperformed Kaletra in a recent trial, though it wasn’t a complete win: Kaletra increased CD4 counts more than Sustiva, and although Kaletra was more likely to fail, there was a lot less resistance with Kaletra failure than with Sustiva failure.—Joel Gallant, M.D.
Kaletra has created a strong marketing advantage for Abbott Labs. Everyone else requires the patient to order Norvir separately, often at highly inflated prices. Kaletra has proven to be extremely durable (lasts a long time without failure or resistance), can be dosed once daily and has even performed quite well in studies as a single drug regimen. While not as successful as the best 3-drug regimens, it works well and for a long time in many patients as monotherapy. This has given researchers and patients alike legitimate hope that treatment can someday be simplified. Additional studies of simplified regimens are underway.—Martin Delaney
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