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KALETRA - A Protease Inhibitor for the Treatment of HIV
KALETRA (lopinavir/ritonavir; formerly known as ABT-378/r) was approved by the FDA on September 15, 2000, for the treatment of human immunodeficiency virus (HIV) infection. KALETRA belongs to a class of agents known as protease inhibitors (PIs). KALETRA must be used only in combination with other antiretroviral medications. It is important to note that KALETRA is not a cure for HIV. There is currently no information to support that KALETRA will prevent transmission of HIV to others through sexual contact or blood contamination.
KALETRA decreases the production of HIV by binding to HIV protease and preventing the formation of mature viral particles. In order to effectively slow overall replication of new HIV viruses, KALETRA must be taken with other HIV medications, which work at different parts of the HIV life cycle
KALETRA contains two protease inhibitors, lopinavir and ritonavir. The small amount of ritonavir that is contained in each dose of KALETRA (100mg) does not possess activity against HIV. Ritonavir has been added to increase the blood levels of lopinavir. The antiviral activity of KALETRA is primarily contributed by lopinavir.
Clinical Studies
The approval of KALETRA is based on the response of viral load measurements and CD4 cell counts from a 24-week controlled clinical trial and additional smaller studies of 72 weeks in duration.
Therapy-NaÏve Adults: A randomized, double-blind, placebo-controlled trial compared KALETRA 400mg/100mg (400mg lopinavir/100mg ritonavir) twice daily + Zerit® (stavudine) + Epivir® (lamivudine) to Viracept® (nelfinavir) 750mg three times daily + Zerit + Epivir in 653 patients. After 24 weeks, 79% of patients in the KALETRA group had undetectable viral load levels (<400 copies/mL) compared to 70% of patients in the Viracept group. Through 24 weeks of therapy, there was no significant difference in the median CD4 cell count between the two treatment groups. This study is ongoing and the follow-up results are not yet available.
Therapy-Experienced Adults: A randomized open-label study compared KALETRA dosed at either 400mg/100mg twice daily or 400mg/200mg twice daily + Viramune® (nevirapine) 200mg twice daily + 2 nucleoside reverse transcriptase inhibitors (NRTIs) in 70 PI experienced, non-nucleoside reverse transcriptase inhibitor (NNRTI) naïve patients. After 72 weeks of treatment, 75% of patients in the KALETRA 400mg/100mg group had undetectable viral load levels (<400 copies/mL). The mean increase in the CD4 cell count in this group of patients was 174 cells/mm3. The efficacy of patients receiving KALETRA 400mg/200mg was not reported. This study is ongoing and the follow-up results are not yet available.
Drug Interactions
KALETRA should not be taken with astemizole (Hismanal®), cisapride (Propulsid®), ergot derivatives (D.H.E. 45®, Caffergot®, and others), flecainide (Tambocor®), lovastatin (Mevacor®), midazolam (Versed®), pimozide (Orap®), propafenone (Rythmol®), simvastatin (Zocor®), terfenadine (Seldane®), or triazolam (Halcion®). KALETRA may increase the blood levels of these medications and cause serious or life-threatening adverse events. Rifampin (Rifadin® or Rimactane®) has been shown to significantly reduce the blood levels of KALETRA and therefore should not be taken with KALETRA. It is recommended to reduce the dose of rifabutin (Mycobutin®) by at least 75% of the recommended dosage when given together with KALETRA. The herbal product St. John's Wort (Hypericum perforatum) may reduce the blood levels of KALETRA and should be avoided while taking KALETRA. Administration of KALETRA with sildenafil (Viagra®) is expected to produce in an increase in the blood levels of Viagra and may result in Viagra-related adverse events. Other medications used for the heart, seizures, or lowering cholesterol levels can interact with KALETRA. For more information regarding drug interactions with KALETRA, please contact your doctor or pharmacist.
Side Effects
The most common side effect associated with KALETRA during clinical trials was diarrhea, which was considered mild-to-moderate in intensity. In one clinical trial, the reported incidence of diarrhea was 23.8%. Other less common side effects reported during clinical trials included stomach pain (4.8%), weakness (7.1%), headache (7.1%), nausea (15.5%), vomiting (4.8%) and insomnia (2.4%).
Usual Adult Dose
KALETRA should be taken with food. Moderate to high fat meals have been shown to enhance the absorption of KALETRA. The recommended adult dose of KALETRA is 400mg/100mg (3 capsules or 5 ml) twice daily. When KALETRA is combined with the non-nucleoside reverse transcriptase inhibitors (NNRTIs) Sustivatm or Viramune, a dosage increase of KALETRA to 533mg/133mg (4 capsules or 6.5 ml) should be considered.
KALETRA is also approved for use in children ages 6 months to 12 years old. Talk with your doctor or pharmacist about specific dosing recommendations for these age groups.
Availability and Storage Information
KALETRA is available as soft gelatin capsules. Each capsule contains 133.3mg of lopinavir and 33.3mg of ritonavir.
KALETRA is also available as an oral solution. Each 5-ml (1 teaspoonful) of KALETRA contains 400mg of lopinavir and 100mg of ritonavir.
KALETRA capsules and oral solution do not need to be refrigerated if used within 2 months and stored at temperatures up to 77° F (up to room temperature). If refrigerated, both dosage forms of KALETRA remain stable until the expiration date on the manufacturer's label.
For additional questions regarding treatment with KALETRA, contact your doctor, health-care provider or a PharmaCare pharmacist. A medication counselor can be reached by calling 1-800-238-1548.
Information in this Web site is intended to supplement, not replace, the medical advice you receive from your healthcare providers. If you have a question regarding any information contained in this Web site and how it pertains to your personal condition, please consult your physician.
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