Kaletra (Meltrex). Si tratta di compresse (LPV/rtv 200/50 mg): non richiedono refrigerazione, non richiedono la somministrazione di cibo, non richiedono aggiustamenti di dosaggio con la co-somministrazione di NNRTI o IP nei pz. naive. Schema posologico: 2+2 compresse (BID) al giorno, oppure 4 compresse una sola volta al giorno in pazienti naive.
Questa nuova formulazione permette l’utilizzo di Kaletra in modo molto piu’ semplice: ridotto il numero delle pillole (ora si tratta di compresse), non e’ richiesto il cibo. Minori anche le interazioni farmacologiche.
The following additions and revisions were made to the package insert.
1. The CLINICAL PHARMACOLOGY section contains the following additions:
Pharmacokinetics
Plasma concentrations of lopinavir and ritonavir after administration of two 200/50 mg KALETRA tablets are similar to three 133.3/33.3 mg KALETRA capsules under fed conditions with less pharmacokinetic variability.
Effects of Food on Oral Absorption
KALETRA tablets
No clinically significant changes in Cmax and AUC were observed following administration of Kaletra tablets under fed conditions compared to fasted conditions. Relative to fasting, administration of KALETRA tablets with a moderate fat meal (500 – 682 Kcal, 23 to 25% calories from fat) increased lopinavir AUC and Cmax by 26.9% and 17.6%, respectively. Relative to fasting, administration of KALETRA tablets with a high fat meal (872 Kcal, 56% from fat) increased lopinavir AUC by 18.9%, but not Cmax. Therefore, Kaletra tablets may be taken with or without food.
Drug-drug Interactions
Tables 2 and 3 were updated to clarify which formulations of Kaletra (capsule, oral solution or tablets) were used in the drug-drug interaction studies. Results of the drug-drug interaction study between efavirenz and Kaletra tablets were included.
2. The following text was added and/or revised in the PRECAUTION: Information for patients section:
KALETRA tablets can be taken at the same time as didanosine without food. Patients taking didanosine should take didanosine one hour before or two hours after KALETRA oral solution.
KALETRA tablets may be taken with or without food. KALETA oral solution should be taken with food to enhance absorption.
3. In the PRECAUTION section, Table 10: Established and Other Potentially Significant Drug Interactions, was revised to include the following:
· KALETRA tablets can be taken at the same time as didanosine without food.
· The saquinavir dose is 1000 mg BID when co-administered with Kaletra 400/100 mg BID.
4. The DOSAGE AND ADMINISTRATION section was revised to include the following information regarding the new tablet formulation:
KALETRA tablets may be taken with or without food.
KALETRA oral solution must be taken with food.
KALETRA tablets should be swallowed whole and not chewed, broken, or crushed.
Concomitant therapy: Efavirenz, nevirapine, fosamprenavir or nelfinavir:
KALETRA 400/100 mg tablets can be used twice-daily in combination with these drugs with no dose adjustment in antiretroviral-naive patients.
· A dose increase of KALETRA tablets to 600/150 mg (3 tablets) twice-daily may be considered when used in combination with efavirenz, nevirapine, fosamprenavir without ritonavir, or nelfinavir in treatment-experienced patients where decreased susceptibility to lopinavir is clinically suspected (by treatment history or laboratory evidence).
KALETRA tablets and oral solution should not be administered as a once-daily regimen in combination with efavirenz, nevirapine, amprenavir or nelfinavir.