KALETRA

What it is

Kaletra is a co-formulation of lopinavir and ritonavir. Kaletra tablets are available for oral administration in a strength of 200 mg of lopinavir and 50 mg of ritonavir. Kaletra Oral Solution is available for oral administration as 80 mg lopinavir and 20 mg ritonavir per millilitre.

Approved indications

— Treatment of HIV-1 infection, in combination with other antiretroviral agents in adults and children aged 2 years and older.

Dosing overview

**Tablets (adults):** The recommended dosage of Kaletra film coated tablets is 400/100 mg (two 200/50 mg tablets) twice daily. Kaletra tablets may also be administered as 800/200 mg (four 200/50 mg tablets) once daily, in patients with less than three lopinavir-associated mutations. Kaletra tablets may be taken with or without food. **Oral Solution (adults):** The recommended dosage of Kaletra is 5 mL of oral solution (400/100 mg) twice daily taken with food. Kaletra oral solution may also be administered as 10 mL once daily with food, in patients with less than three lopinavir associated mutations. **Paediatric patients:** The adult dose of Kaletra tablets (400/100 mg BD) may be used in children 35 kg or greater. The recommended dosage for children 2 years and older is 230/57.5 mg/m² (or 12/3 mg/kg for children < 15 kg or 10/2.5 mg/kg for children ≥ 15kg) twice daily taken with food, up to a maximum dose of 400/100 mg (5 mL) twice daily.

Key safety warnings

New onset diabetes mellitus, exacerbation of pre-existing diabetes mellitus, and hyperglycaemia have been reported during post-marketing surveillance in HIV-infected patients receiving protease inhibitor therapy. Some patients required either initiation or dose adjustments of insulin or oral hypoglycaemic agents for treatment of these events. In some cases, diabetic ketoacidosis has occurred. Consideration should be given to the monitoring of blood glucose. Pancreatitis has been observed in patients receiving Kaletra therapy, including those who developed marked triglyceride elevations. In some cases, fatalities have been observed. Patients with advanced HIV disease may be at increased risk of elevated triglycerides and pancreatitis, and patients with a history of pancreatitis may be at increased risk for recurrence during Kaletra therapy. Kaletra is principally metabolised by the liver. Therefore, caution should be exercised when administering this drug to patients with impaired hepatic function. Patients with underlying hepatitis B or C or marked elevations in transaminases prior to treatment may be at increased risk for developing further transaminase elevations. There have been post-marketing reports of hepatic dysfunction, including some fatalities. These have generally occurred in patients with advanced HIV disease taking multiple concomitant medications in the setting of underlying chronic hepatitis or cirrhosis. Post-marketing cases of QT interval prolongation and torsade de pointes have been reported although causality of Kaletra could not be established. Avoid use in patients with congenital long QT syndrome, those with hypokalaemia, and with other drugs that prolong the QT interval. Treatment with Kaletra has resulted in increases in the concentration of total cholesterol and triglycerides. Triglyceride and cholesterol testing should be performed prior to initiating Kaletra therapy and at periodic intervals during therapy.

Contraindications

Kaletra is contraindicated in patients with known hypersensitivity to lopinavir, ritonavir, or any excipients. Kaletra should not be co-administered concurrently with drugs that are highly dependent on cytochrome 450 3A (CYP3A) for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. Kaletra Oral Solution is contraindicated in children below the age of 2 years, pregnant women, patients with hepatic and renal failure and patients treated with disulfiram or metronidazole due to the potential risk of toxicity from the excipient propylene glycol.

PBS listing

Information regarding PBS listing, item numbers, restriction types, and ex-manufacturer pricing is not available in the provided source documents.

Regulatory history

Kaletra oral solution was first listed on the ARTG on 7 August 2001, and Kaletra lopinavir 200 mg and ritonavir 50 mg tablets were first listed on 24 May 2006.