Kaletra should be prescribed by physicians who are experienced in the treatment of HIV infection.
Kaletra tablets must be swallowed whole and not chewed, broken or crushed.
Posology
Adults and adolescents
The standard recommended dosage of Kaletra tablets is 400/100 mg (two 200/50 mg) tablets twice daily taken with or without food. In adult patients, in cases where once-daily dosing is considered necessary for the management of the patient, Kaletra tablets may be administered as 800/200 mg (four 200/50 mg tablets) once daily with or without food. The use of a once-daily dosing should be limited to those adult patients having only very few protease inhibitor (PI) associated mutations (i.e. less than 3 PI mutations in line with clinical trial results, see section 5.1 for the full description of the population) and should take into account the risk of a lesser sustainability of the virologic suppression (see section 5.1) and higher risk of diarrhoea (see section 4.8) compared to the recommended standard twice-daily dosing. An oral solution is available to patients who have difficulty swallowing. Refer to the Summary of Product Characteristics for Kaletra oral solution for dosing instructions.
Paediatric population (2 years of age and above)
The adult dose of Kaletra tablets (400/100 mg twice daily) may be used in children 40 kg or greater or with a Body Surface Area (BSA)* greater than 1.4 m2. For children weighing less than 40 kg or with a BSA between 0.5 and 1.4 m2 and able to swallow tablets, please refer to the Kaletra 100 mg/25 mg tablets Summary of Product Characteristics. For children unable to swallow tablets, please refer to the Kaletra oral solution Summary of Product Characteristics. Based on the limited data currently available, Kaletra should not be administered once daily in paediatric patients (see section 5.1).
* Body surface area can be calculated with the following equation:
BSA (m2) = √ (Height (cm) X Weight (kg) / 3600)
Children less than 2 years of age
The safety and efficacy of Kaletra in children aged less than 2 years have not yet been established. Currently available data are described in section 5.2 but no recommendation on a posology can be made.
Concomitant Therapy: Efavirenz or nevirapine
The following table contains dosing guidelines for Kaletra tablets based on BSA when used in combination with efavirenz or nevirapine in children.
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Paediatric dosing guidelines with concomitant efavirenz or nevirapine
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Body Surface Area (m2)
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Recommended lopinavir/ritonavir dosing (mg) twice daily.
The adequate dosing may be achieved with the two available strengths of Kaletra tablets: 100/25 mg and 200/50 mg.*
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≥ 0.5 to < 0.8
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200/50 mg
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≥ 0.8 to < 1.2
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300/75 mg
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≥ 1.2 to < 1.4
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400/100 mg
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≥ 1.4
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500/125 mg
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* Kaletra tablets must not be chewed, broken or crushed.
Hepatic impairment
In HIV-infected patients with mild to moderate hepatic impairment, an increase of approximately 30% in lopinavir exposure has been observed but is not expected to be of clinical relevance (see section 5.2). No data are available in patients with severe hepatic impairment. Kaletra must not be given to these patients (see section 4.3).
Renal impairment
Since the renal clearance of lopinavir and ritonavir is negligible, increased plasma concentrations are not expected in patients with renal impairment. Because lopinavir and ritonavir are highly protein bound, it is unlikely that they will be significantly removed by haemodialysis or peritoneal dialysis.
Pregnancy and postpartum
• No dose adjustment is required for lopinavir/ritonavir during pregnancy and postpartum.
• Once-daily administration of lopinavir/ritonavir is not recommended for pregnant women due to the lack of pharmacokinetic and clinical data.
Method of administration
Kaletra tablets are administered orally and must be swallowed whole and not chewed, broken or crushed. Kaletra tablets can be taken with or without food.
Hypersensitivity to the active substances or to any of the excipients.
Severe hepatic insufficiency.
Kaletra contains lopinavir and ritonavir, both of which are inhibitors of the P450 isoform CYP3A. Kaletra should not be co-administered with medicinal products that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life threatening events. These medicinal products include:
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Medicinal product class
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Medicinal products within class
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Rationale
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Concomitant medicinal product levels increased
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Alpha1-adrenoreceptor antagonist
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Alfuzosin
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Increased plasma concentrations of alfuzosin which may lead to severe hypotension. The concomitant administration with alfuzosin is contraindicated (see section 4.5).
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Antiarrhythmics
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Amiodarone, dronedarone
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Increased plasma concentrations of amiodarone and dronedarone. Thereby, increasing the risk of arrhythmias or other serious adverse reactions.
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Antibiotic
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Fusidic Acid
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Increased plasma concentrations of fusidic acid. The concomitant administration with fusidic acid is contraindicated in dermatological infections. (see section 4.5).
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Anti-gout
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Colchicine
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Increased plasma concentrations of colchicine. Potential for serious and/or life-threatening reactions in patients with renal and/or hepatic impairment (see sections 4.4 and 4.5).
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Antihistamines
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Astemizole, terfenadine
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Increased plasma concentrations of astemizole and terfenadine. Thereby, increasing the risk of serious arrhythmias from these agents.
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Antipsychotics/ Neuroleptics
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Pimozide
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Increased plasma concentrations of pimozide. Thereby, increasing the risk of serious haematologic abnormalities, or other serious adverse effects from this agent.
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Quetiapine
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Increased plasma concentrations of quetiapine which may lead to coma. The concomitant administration with quetiapine is contraindicated (see section 4.5).
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Ergot alkaloids
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Dihydroergotamine, ergonovine, ergotamine, methylergonovine
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Increased plasma concentrations of ergot derivatives leading to acute ergot toxicity, including vasospasm and ischaemia.
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GI motility agent
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Cisapride
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Increased plasma concentrations of cisapride. Thereby, increasing the risk of serious arrhythmias from this agent.
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HMG Co-A Red |
