Brand name: Kaletra

Common name: lopinavir/ritonavir

Class: HIV protease inhibitor (PI)

Standard dose: Three soft-gelatin capsules (133.3 mg lopinavir and 33.3 mg ritonavir each) twice a day, preferably with food; liquid formula available. Take missed dose as soon as possible, but do not double dose.

Wholesale cost: $8,125/yr., $677/month

Patience assistance number: 1 (800) 637–2400, www.kaletra.com

AIDS Treatment Information Service: 1 (800) HIV–0440 (448–0440)

 

 

Potential side effects:

Rash, loose stools, diarrhea, nausea, headache, muscle weakness, and increased cholesterol, triglycerides (fats in the blood) and AST/ALT (liver function tests, a sign of liver damage). These were not fasting samples, needed for the most accurate results. Seen with all older protease inhibitors (except Agenerase) are high blood levels of cholesterol and triglycerides (fats) and perhaps associated heart disease, 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), worsening or new cases of diabetes (symptoms include increased thirst and hunger, frequent urination, unexplained weight loss, fatigue, and dry itchy skin; see your doctor promptly) and increased bleeding in hemophiliacs.

Potential drug interactions:

Dosage of methadone may need to be increased when taken with Kaletra. Dose increase to 4 capsules twice a day with food recommended when using with Sustiva or Viramune in people who previously took HIV drugs, especially protease inhibitors. May lower levels of Retrovir and Ziagen. Do not use Zocor or Mevacor; suggested alternatives are Lipitor, Lescol, Baycol, and Pravachol (looks best on paper for protease inhibitors). Alternatives should still be used with caution because of potential for liver toxicity. Protease inhibitors increase blood levels of Viagra, and Viagra dose should be started at 25 mg (half the normal dose) and increased as needed and tolerated. It’s recommended that people do not exceed 25 mg in a 48 hour period because of potential for fatal reaction. Phenobarbital, phenytoin (Dilantin and others) or carbamazepine (Tegretol and others) may lower blood levels of Kaletra. Reduces effectiveness of birth control pills; use alternative contraceptive. Oral solution contains alcohol, so do not use with Antabuse or Flagyl. Do not take with flecainide, propatenone, Hismanol, Seldane, rifampin, ergot derivatives (such as Cafetrate, Cafergot, Wigraine and Methergine, in any form—serious interactions seen with dilation during gynecological exams), D.H.E. 45, St. John’s Wort, pimozide, Versed and Halcion. (Also dihydropuridine calcium channel blockers.) Videx should be given an hour before (or two hours after) Kaletra is taken with food. Rifabutin dose must be lowered.

Tips:

Doctors and patients report that this protease inhibitor is very tolerable. Great viral load results out to 72 weeks (significant) in people on their first HIV regimen. Good results also seen in heavily treatment-experienced children and adults, even those with protease inhibitor resistance. However, drug-experienced people also used a non-nuke, which may mean that three classes of HIV drugs are needed for them, and which limits future options. Then again, some people don’t have many options. Expected to successfully control HIV that no longer responds to other meds due to drug resistance, but cross-resistance has already been seen. Can have Norvir’s yucky taste and taste aversion—one guy said his beer tasted like soap. There is hope for once a day dosing.

 

 

Manufacturer

Abbott developed Kaletra to fulfill an unmet need for a different PI which combines power and tolerability for patients across the spectrum of HIV, including those new to, and experienced with, HIV therapy. Kaletra’s enhanced pharmacokinetic profile is the key to its strength and durability. Kaletra can be maintained at much higher levels in the blood than any other protease inhibitor. Elevated levels create a high barrier to viral mutations and may prevent resistance. Data from ongoing Phase II and Phase III trials show that genotypic resistance to Kaletra has not developed yet in treatment naive patients. At 48 weeks, data also show that Kaletra continues to be more effective than nelfinavir at suppressing viral load below undetectable levels in a significant portion of patients and is better tolerated, with only 2% of patients discontinuing due to Kaletra-related adverse events. Doses: 3 capsules BID; 4 capsules BID when combined with efavirenz for highly experienced patients.

—Abbott Laboratories

 

 

Doctor

FDA approved 9/15/00 for combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients ages 6 months and older. Patients can keep the drug at room temperature if used within 2 months of dispensing. Administration with food enhances overall drug levels. Dosing of didanosine and Kaletra should be separated by at least 2.5 hours. Elevated cholesterol, triglyceride and liver enzyme levels have been reported. Clinical trials are ongoing in HIV infected patients with various levels of prior treatment experience. Kaletra-based therapy demonstrated antiviral activity in ARV naïve patients through 144 weeks. The rate of discontinuation of therapy due to side effects is low. No evidence of genotypic resistance to Kaletra was observed in any of the isolates from Kaletra-treated ARV-naïve subjects through week 60.

—Carlos H. Zambrano, M.D.

 

 

Activist

When Kaletra came out, the name sounded to me like a new car. It is actually a combination of two drugs, lopinavir and ritonavir. During development of lopinavir the company saw it was not absorbed well enough so they looked on their top shelf and added their booster drug ritonavir. There was great hope that Kaletra would become a good salvage drug since all other PIs are cross resistant. The data so far has been hopeful but not overwhelming. Watch for drug interactions considering that you are taking two drugs in one, one of them being ritonavir.

—Matt Sharp

 

Nukes | Retrovir / AZT / zidovudine | Videx, Videx EC / ddI / didanosine |
| Hivid / ddC / zalcitabine | Zerit / d4t / stavudine | Epivir / 3TC / lamivudine |
| Ziagen / abacavir sulfate | Combivir (Retrovir, Epivir) |
| Trizivir (Retrovir, Epivir, Ziagen) | Viread / tenofovir disoproxil fumarate |

Non-Nukes | Rescriptor / delavirdine | Viramune / nevirapine |
| Sustiva / efavirenz |

HIV Protease Inhibitors | Crixivan / indinavir | Norvir / ritonavir |
| Viracept / nelfinavir | Fortovase / saquinavir soft-gel |
| Agenerase / amprenavir | Kaletra / lopinavir/ritonavir | tipranavir |

Fusion Inhibitor | T-20 / pentafuside

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