What is Kaletra?
Kaletra is a medicine containing two active substances: lopinavir and ritonavir. It is available as orange capsules (133.3 mg of lopinavir and 33.3 mg of ritonavir), an oral solution (80 mg of lopinavir and 20 mg of ritonavir per milliliter) and tablets (light yellow: 100 mg of lopinavir and 25 mg of ritonavir; yellow: 200 mg of lopinavir and 50 mg of ritonavir).
What is Kaletra used for?
Kaletra is an antiviral medicine used in combination with other antiviral medicines to treat adult patients and children over the age of 2 years with human immunodeficiency virus type 1 (HIV-1) infection, a virus that causes the syndrome of acquired immunodeficiency (AIDS).
The medicine can only be obtained with a prescription.
How is Kaletra used?
Kaletra should be prescribed by doctors who are experienced in managing HIV infection.
In adults and adolescents (at least 12 years of age), the recommended dose of Kaletra is three capsules or two 200/50-mg tablets twice a day. This dosage is also suitable for children (aged between 2 and 12 years), provided they weigh more than 40 kg and have an extension of the body surface (calculated based on the height and weight of the child) greater than 1.4 m2. The dose for smaller children depends on the extent of their body surface and the other medicines they are taking.
If necessary, adults (at least 18 years of age) never treated (not previously subjected to anti-HIV therapy) can take the full dose of 4 tablets as a single daily dose. However, in the long term this could compromise the effectiveness in keeping HIV levels low compared to the dose taken twice a day and increasing the risk of diarrhea.
The oral solution is indicated for patients who cannot take tablets or capsules. The capsules and the oral solution must be taken with food, while the tablets can also be taken on an empty stomach. Kaletra tablets should be swallowed whole, should not be chewed, broken or crushed. For more information, see the package leaflet.
How does Kaletra work?
Kaletra contains two active substances: lopinavir and ritonavir. Both substances are protease inhibitors, which means they block an enzyme called protease which is involved in the reproduction of HIV. If the enzyme is blocked, the virus is unable to reproduce normally, which slows the spread of the infection. In Kaletra, lopinavir expresses activity, while ritonavir is used as an "enhancer" to reduce the rate of breakdown of lopinavir by the liver. In this way, the concentration of lopinavir in the blood increases, and it is possible to use a lower dose of lopinavir obtaining the same antiviral effect. Kaletra does not cure HIV infection or AIDS, but it may delay the damage to the immune system and the development of infections and diseases associated with AIDS.
How has Kaletra been studied?
Two main studies of Kaletra on adults and one on children were conducted. The first study involved 653 untreated adults, and a comparison was made between the Kaletra and nelfinavir capsules (another antiviral medicine). The second study saw the participation of 118 adults who had previously taken another protease inhibitor; in this case the Kaletra capsules were compared with a protease inhibitor chosen on a case-by-case basis by the study doctor. The third study involved 100 children who were given one of two doses of Kaletra oral solution. In all three studies, Kaletra and the medicine used for the comparison were associated with other antiviral medicines. The main measure of effectiveness was the number of patients with undetectable levels of HIV-1 in the blood (viral loads) after treatment.
Further studies were carried out to compare the concentrations of the active ingredients produced in organsimo by the tablets and capsules and to compare the doses taken once a day and twice a day over two years in untreated adult patients.
What benefit has Kaletra shown during the studies?
In all three main studies, Kaletra reduced viral loads. In the untreated adult study a total of 259 (79%) of 326 patients treated with Kaletra had viral loads below 400 copies / ml after 24 weeks, compared with 233 (71%) of 327 patients treated with nelfinavir. In the study on adults previously treated with a protease inhibitor, viral loads below 400 copies / ml were observed in 16 (73%) of 59 patients treated with Kaletra after 16 weeks, compared with 32 (54%) on 59 patients treated with the comparator medicines. Similar results were observed with both doses of Kaletra in the study on children, in which about 70% recorded viral loads below 400 copies / ml after 12 weeks, although the number of children under 2 years of age was too low to support the use of Kaletra in this age group.
Additional studies showed that tablets had somewhat higher concentrations of active ingredients in the blood than capsules. Kaletra tablets with the dose taken once a day and twice a day also produced similar effects in adults never treated over the past two years, although the study suggests that once-a-day dosing is not as effective as the dose taken twice a day to keep HIV levels low over the long term.
What is the risk associated with Kaletra?
The most common side effects seen in adults (seen in more than 1 patient in 10) are increased concentrations of cholesterol, triglycerides (a type of fat) and gamma-glutamyltransferase (a liver enzyme) in the blood and diarrhea. In children the side effects are similar. For the full list of all side effects reported with Kaletra, see the Package Leaflet.
Kaletra is contraindicated in patients who may be hypersensitive (allergic) to lopinavir, ritonavir or any of the other ingredients. Kaletra should not be used in patients with severe liver disease or in patients taking St. John's wort (a herbal preparation used to treat depression) or medicines that are broken down in the same way as Kaletra and which are harmful in high blood concentrations . For the full list of these medicines, see the package leaflet.
As with other anti-HIV drugs, patients receiving Kaletra may be at risk of lipodystrophy (changes in body fat distribution), osteonecrosis (death of bone tissue) or immune reactivation syndrome (infection symptoms caused by system reactivation). immune). Patients with liver problems (including hepatitis B or C) may be at greater risk of liver damage if treated with Kaletra.
Why has Kaletra been approved?
The Committee for Medicinal Products for Human Use (CHMP) decided that Kaletra's benefits are greater than its risks for the treatment of HIV-1 infection in adults and children over the age of 2 years in combination with other antiretroviral medicines. The Committee recommended that Kaletra be given marketing authorization.
Kaletra was initially authorized in "exceptional circumstances" because at the time the authorization was granted, for scientific reasons, only limited information was available. As the company provided the additional information requested, the condition referring to "exceptional circumstances" was removed on 12 November 2002.
What measures are being taken to ensure the safe use of Kaletra?
Since Kaletra was previously only available in capsules and in the oral solution, the manufacturer of Kaletra will provide a letter to those involved in the care of patients taking the medicine, to explain the differences between Kaletra capsules and tablets and in order to provide clarifications on the number of tablets patients should take when they are introduced.
More information on Kaletra
On March 20, 2001, the European Commission granted a marketing authorization valid throughout the European Union for Kaletra to Abbott Laboratories Limited. The marketing authorization was renewed on 20 March 2006.
For the full EPPAR version of Kaletra, click here.
Last update of this summary: 09-2009.
