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Brand Name: Kaletra
Common Name: lopinavir/ritonavir (LPV/r)
Class: HIV protease inhibitor
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. Soft-gelatin capsules (133.3 mg lopinavir and 33.3 mg ritonavir each) were phased out in early 2006. 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: $764.41 / month
Manufacturer contact: Abbott Laboratories,
www.kaletra.com, 1 (800) 222–6885
AIDSInfo:1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
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| 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 AST/ALT (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 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.
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| Potential drug interactions: |
Interacts with many—tell your provider all the drugs you are taking. Do not take with Tambocor, Rythmol, Cordarone, Versed, Halcion, Uroxatral, Rifadin, Orap, ergot derivatives (such as Cafergot, Wigraine and Methergine, D.H.E. 45), garlic supplements, or the herb St. John’s wort. Do not use Zocor or Mevacor; lipid-lowering alternatives are Lipitor, Lescol, and Pravachol, 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. 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 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. Transplant medicines require close monitoring with Kaletra. Kaletra may alter coumadin levels. Steroids, especially Decadron, may decrease levels of Kaletra.
Protease inhibitors increase blood levels of Viagra, Cialis and Levitra. Use with caution. Initially the Viagra dose should be 12.5 mg (1/2 of 25 mg tablet) and increased as needed and tolerated. It’s recommended that people on PIs do not exceed 25 mg of Viagra in a 48-hour period because of potential for serious reaction such as low blood pressure, visual changes, and prolonged erection leading to permanent tissue damage. Use Cialis at reduced doses of 10 mg every 72 hours and Levitra at reduced doses of no more than 2.5 mg every 72 hours, with increased monitoring for adverse events.
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| Tips: |
Kaletra twice daily was the first protease inhibitor recommended by U.S. treatment guidelines for first-time therapy. The new tablet formulation of Kaletra with the same dosage but less pills and hopefully fewer side effects. The newer formulation doesn’t require refrigeration (especially important for resource-poor countries) and has fewer food restrictions. Three capsules equal two tablets, except for patients also taking Sustiva or Viramune. 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. 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.
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| Doctor |
| Lopinavir/ritonavir (LPV/RTV) remains as a protease inhibitor of choice due to potency, a high barrier to resistance, durability, fair tolerability (generally better with the new formulations), no need for refrigeration (unlike other boosted PIs), flexible dosing (once or twice-a-day for naïve patients) and cost (Abbott can bundle their two PIs versus over-pricing ritonavir for use as a boosting drug for use with PIs made by competitors). The October 2006 DHHS ART Guidelines now lists three boosted PI regimens (lopinavir, atazanavir, or fosamprenavir) as first tier recommended starting drugs. Problems with Kaletra include considerable gastronintestinal toxicity (small subset of patients seem unable to tolerate ritonavir), lipid elevations, fat distribution issues, and concern about risk for increased atherosclerosis. My own practice is to often use a Kaletra-based regimen initially until the viral load is suppressed (I place a high value on avoiding early resistance and patients cannot avoid taking their ritonavir with the lopinavir) and then individualize to a simpler maintenance regimen, avoiding the long-term problems from use of Kaletra.—Keith Henry, MD |
| Activist |
| Still considered to be the “Big Gun” in its class, Kaletra has made a name for itself as a PI with one of the more forgiving resistance profiles, and the ability to hit hard and long. The old gel caps were done away with last year in favor of the new Meltrex formulation, which is more stable in heat than the big orange capsules were. This new formulation requires no refrigeration and the dose is two fewer pills a day. Despite its new outfit and its great reputation at controlling viral replication in most people, it still carries a lot of the same GI (gastrointestinal) side effects that it used to have and has shown no real improvement in triglycerides.—Cathy Olufs |
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