Kaletra
lopinavir / ritonavir, or LPV / r
PI: Protease inhibitor
image of drug

MANUFACTURER:
AbbVie
kaletra.com
(800) 222–6885

AWP:
$977.22 / month for tablets; $488.60 for 160 mL oral solution

Standard Dose:

Four tablets (200 mg lopinavir / 50 mg ritonavir) once a day for people with less than three lopinavir resistance-related mutations; or two 200 / 50 mg tablets twice daily. Do not use once daily if taken with Sustiva or Viramune, or anticonvulsants. Three tablets twice a day may be considered for treatment-experienced people, pregnant women during the second and third trimesters, or those taking it in combination with Sustiva or Viramune. 100 mg lopinavir / 25 mg ritonavir tablets are also available.

Take missed doses as soon as possible, unless it is closer to the time of your next dose. Do not double up on your next dose.

Potential side effects and toxicity

Diarrhea is the most common and can be severe, but generally less severe with tablets than liquid. It is also associated with high incidence of elevated cholesterol and triglycerides, as well as insulin resistance. Rash, nausea, vomiting, stomach pain, headache, muscle weakness, lipodystrophy, and elevated liver enzymes (a sign of liver damage—may be more common in people with hepatitis B or C).

Check for potential drug class side effects.

Potential drug interactions

See package insert for the most complete list of interactions. Tell your provider or pharmacist about all medications, herbs, and supplements you are taking, prescribed or not. Do not take with alfuzosin, Revatio (sildenafil), Tambocor (flecainide), Rythmol (propafenone), Cordarone (amiodarone), midazolam (oral Versed), rifampin, pimozide, Priftin (rifapentine), triazolam, garlic, supplements, or the herb St. John’s wort. Do not use lovastatin and simvastatin or co-formulations containing these drugs (Advicor and Vytorin). Alternatives are Crestor, Lescol, Lipitor, and Pravachol, but should be used with caution and started at the lowest dose possible; monitor closely for increased side effects. Oral solution contains alcohol, so do not use with Antabuse or Flagyl. Use calcium channel blockers with caution. Dosage of methadone may need to be increased. Current U.S. HIV treatment guidelines state the Kaletra dose should total 500 mg lopinavir and 125 mg ritonavir twice daily when used with Sustiva or Viramune. Not recommended to be taken with Lexiva. Kaletra may lower levels of AZT and Ziagen. Videx and Kaletra can be taken together without food. If Kaletra is taken with food, Videx should be taken an hour before or two hours after Kaletra. If taking Kaletra with Viread (tenofovir) or other combinations containing tenofovir (Atripla, Complera, Stribild, and Truvada), monitor for side effects from tenofovir. Rifabutin dose should be reduced to 150 mg every other day (or 150 mg three times per week) when used with Kaletra. Effectiveness of birth control pills may be decreased; consider the use of other contraception. Mepron levels may be reduced with Kaletra. Avoid Sporanox or Nizoral doses greater than 200 mg per day with Kaletra. Monitor for side effects when taken with Noxafil. Decreases voriconazole levels. People with kidney impairment may require lower clarithromycin doses with Kaletra. Monitor blood levels of immunosuppressants because levels may increase. Kaletra may alter warfarin levels; additional monitoring may be required. Steroids, especially Decadron, may decrease Kaletra levels. Kaletra increases levels of steroids, particularly fluticasone (found in Advair, Flonase, and Flovent). Monitor for signs of Cushing’s syndrome (increased abdominal fat, fatty hump between the shoulders, rounded face, and more) as well as for signs of liver inflammation (elevated liver enzymes, yellowing of the eyes or skin, etc.) if you have a history of hepatitis B infection. Kaletra increases levels of trazodone. Use caution with anti-convulsants carbamazepine, phenobarbital, and phenytoin, as they may lower levels of Kaletra. Bupropion levels are lowered; titrate dose based on clinical response. Doses of certain ED drugs should not exceed 10 mg Cialis or 2.5 mg Levitra per 72 hours, or 25 mg Viagra per 48 hours. Use with caution with bosentan, salmeterol, and immunosuppressants, and use lower dose of colchicine. Kaletra can decrease the effects of Malarone. Taking with Olysio is not recommended. Incivek or Victrelis along with a Norvir-boosted PI can potentially reduce the effectiveness of both drugs—combined use is not recommended.

More information

According to U.S. treatment guidelines, the need for 200 mg a day of Norvir (contained in Kaletra) and the higher rate of gastrointestinal side effects compared to other PIs using 100 mg Norvir, make Kaletra an alternative (instead of “preferred”) drug for treatment-naïve people. It is on the preferred list for pregnancy and pediatrics along with boosted Reyataz, but data from 2012 adds to concerns about a link to premature births with Kaletra and other Norvir-boosted PIs (Sibiude, J et al. Premature delivery in HIV-infected women starting protease inhibitor therapy during pregnancy: Role of the ritonavir boost? Clinical Infectious Diseases, 2012 May 1; 54:1348). Four tablets once daily can increase side effects, especially diarrhea. Taking with food and anti-diarrheal medicine helps lessen diarrhea. Kaletra should not be taken once a day by children under 18. Solution cannot be given to premature babies until 14 days after their due date because it contains propylene glycol. See package insert for more complete information on potential side effects and interactions.

Doctor’s comments

Lopinavir is a PI that requires boosting and is available only in the form of Kaletra. The co-formulation is both its advantage and disadvantage: Taking combined lopinavir and ritonavir prevents you from taking one without the other, but it also means you’re stuck taking four pills and 200 mg of ritonavir a day, twice what you’d take with better-tolerated Prezista (darunavir) or Reyataz (atazanavir). Kaletra causes more gastrointestinal and lipid effects than those two drugs, which is why its use has been gradually falling off. In addition, its co-formulation advantage won’t be unique much longer, since we’re expecting darunavir/cobicistat and atazanavir/cobicistat combination pills soon.
—JOEL GALLANT, MD, MPH

Activist’s comments

This was the first boosted and co-formulated PI combination. Kaletra was another game changer as it formalized boosting in a simplified regimen (although the original formulation has changed) for PIs at a time when many were trying to get away from PI-based regimens. Although Kaletra causes lipid abnormalities and a number of GI side effects, it reigned over the PI market for quite a while. Today Kaletra is used less frequently, although many have been on Kaletra for more than a decade and continue to use it successfully. It is still listed as a preferred PI for use in pregnancy.
—DAWN AVERITT