Ritonavir and lopinavir Oral Solution

Kaletra oral solution is available for oral administration as 80 mg lopinavir and 20 mg ritonavir per milliliter with the following inactive ingredients acesulfame potassium, alcohol, artificial cotton candy flavor, citric acid, glycerin, high fructose com symp, Magnasweet-110 flavor, men- 

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METRONIDAZOLE PROTEASE INHIBITORS t adverse effects, e.g. disulfiram-like reaction, flushing, with ritonavir (with or without lopinavir) Ritonavir and lopinavir oral solutions contain alcohol Warn patient and give alternative preparation if possible... 

Soft gelatin Oleic acid capsule 133.3 mg Polyoxyl 35 lopinavir and castor oil 33.3 mg ritonavir (Cremophor EL) Oral solution Propylene glycol... 

Lopinavir and ritonavir are co-formulated as both Kaletra soft gelatin capsules and Kaletra oral solution. Kaletra fixed-dose combination oral solution contains 80 mg/mL of lopinavir and 20 mg/mL of ritonavir solubilized in propylene glycol, 42% ethanol, water, glycerin, cremophor RH 40 and peppermint oil. Kaletra oral solution is packaged in a 160-mL multi-dose container and should be stored refrigerated at 2-8°C or at room temperature for no more than two months. Kaletra oral solution has been available in the UK since 2001 and is also available in the USA. 

Children (6 months to 12 years of age) The recommended dosage of lopinavir/ritonavir oral solution is 12/3 mg/kg for those weighing 7 to less than 15 kg and 10/2.5 mg/kg for those 15 to 40 kg (approximately equivalent to 230/57.5 mg/m ) twice daily with food, up to a maximum dose of 400/100 mg in children greater than 40 kg (5 mL or 3 capsules, or 2 tablets) twice daily. It is preferred that the prescriber calculate the appropriate milligram dose for each individual child 12 years of age and younger and determine the corresponding volume of solution or number of capsules or tablets. 

Administration - Lopinavir/ritonavir tablets may be taken with or without food capsules and oral solution must be taken with food. Tablets should be swallowed whole and not chewed, broken, or crushed. 

Similar labeling language also in the labeling of INVIRASE (Roche Laboratories) (saquinavir mesylate) capsules, December 2003 KALETRA (Abbott) (lopinavir/ritonavir) capsules, (lopinavir/ritonavir) oral solution, February 2004 and LEXIVA (GlaxoSmithKline) (fosamprenavir calcium) tablets. May 2004. 

Fosamprenavir PI2 1400 mg bid or 700 mg bid with ritonavir 100 bid or 1400 mg daily with ritonavir 100-200 mg daily. Adjust dose in hepatic insufficiency Separate dosing from antacids by 2 h. Avoid concurrent high-fat meals Diarrhea, nausea, vomiting, hypertriglyceridemia, rash, headache, perioral paresthesias, t liver enzymes See footnote 4 for contraindicated medications. Do not administer with lopinavir/ritonavir or in severe hepatic insufficiency. Also avoid cimetidine, disulfiram, metronidazole, vitamin E, ritonavir oral solution, and alcohol when using the oral solution... 

Lopinavir/ritonavir PI/PI2 400 mg/100 mg bid or 800 mg/200 mg daily. May need dose adjustment in hepatic insufficiency Take with food. Separate dosing from ddl by 1 h. Store capsules and solution in refrigerator Diarrhea, abdominal pain, nausea, hypertriglyceridemia, headache, t liver enzymes, See footnote 4 for contraindicated medications. Also avoid fosamprenavir. Avoid disulfiram and metronidazole with oral solution... 

Ethanol 2.1 ml, b.i.d. Kaletra Oral Solution (Lopinavir and Ritonavir)... 

Ritonavir, an HIV protease inhibitor with peptidelike structure, has an intrinsic water solubility of l.Opg/ml. Norvir is a thermodynamically stable solution formulation containing 100 mg of ritonavir dissolved in a mixture of oleic acid, Cremophor EL, ethanol, and the antioxidant butylated hydroxytoluene (BHT), and filled into soft gelatin capsules. However, Norvir is being replaced by Kaletra oral solution and soft gelatin capsule, which is a combination of 133.3 mg of lopinavir and 33.3 mg ritonavir dissolved in a mixture of oleic acid, polyoxyl 35 castor oil (Cremophor EL), and propylene glycol. The water-insoluble HIV protease inhibitor, saquinavir, is solubilized by a mixture of Vitamin E and medium-chain mono- and diglycerides in 200 mg Fortovase soft gelatin capsules. 

Ritonavir is solubilized in a cosolvent mixture of propylene glycol, ethanol, water, the surfactant Cremophor EL, and peppermint oil to 80 mg/ml in the Norvir oral solution. A similar cosolvent mixture of propylene glycol, 42% ethanol, water, glycerin, the surfactant Cremophor RH 40, and peppermint oil is used to cosolubilize ritonavir to 20 mg/ml and lopinavir, a non-ionizable water-insoluble HIV protease inhibitor, to 80 mg/ml in the Kaletra oral solution. The dose of Kaletra Oral Solution is up to 5 ml twice daily, which is 2.1 ml of ethanol per dose representing the estimated maximum amount of ethanol administered orally per dose. 

Propylene glycol, 42% ethanol, glycerin, Gremophor RH 40, peppermint oil, water. 11.9% Ethanol, dl-Q -tocopherol, corn oil-mono-di-triglycerides, Gremophor RH 40, propylene glycol. Kaletra oral solution (Lopinavir and ritonavir) Neoral oral solution (Cyclosporin A)... 

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