Company: AbbVie Ltd.
Legal category: Prescription. Hospital. Sports permitted.
Active ingredients: Tablets: Lopinavir/ritonavir 100/25mg, 200/50mg. Oral solution: Lopinavir/ritonavir 80/20mg per ml.
Description: Tablets: Pale yellow or yellow film-coated tablets marked KC or KA respectively. Oral solution: Light yellow oral solution.
Presentation: Tablets: 100/25mg-60; 200/50mg-120. Oral solution: 60ml-5. Prices available on request.
Indication: In combination with other antiretrovirals for the treatment of HIV-infected children >2 years, adolescents and adults.
Pharmacology: Lopinavir is an antiretroviral of the protease inhibitor class. It inhibits the HIV protease enzyme, thus preventing cleavage of the gag-pol polyprotein, resulting in immature, non-infectious virus particles. Lopinavir is essentially completely metabolised by CYP3A. Ritonavir inhibits the metabolism of lopinavir, thereby increasing the plasma levels of lopinavir.
Dosage: Adult: Tablets: 400/100mg twice daily, or 800/200mg once daily. Swallow tablets whole. Oral soln: 5ml (400/100mg) twice daily with food. Elderly: As per adults. Children: Tablets: ≥2 years, weighing ≥40kg or with a body surface area (BSA) ≥1.4m2, 400/100mg twice daily. BSA ≥0.5 to <0.9m2, 200/50mg twice daily. BSA ≥0.9 to <1.4m2, 300/75mg twice daily. <2 years, safety and efficacy not established. Concomitant therapy with efavirenz or nevirapine: BSA ≥0.5 to <0.8m2, 200/50mg twice daily. BSA ≥0.8 to <1.2m2, 300/75mg twice daily. BSA ≥1.2 to <1.4m2, 400/100mg twice daily. BSA ≥1.4m2, 500/125mg twice daily. Oral soln: ≥2 years, 2.9ml (230/57.5mg) per m2 of body surface area) twice daily with food; maximum 5ml (400/100mg) twice daily. <2 years, contraindicated.
Contraindications: Tablets, oral soln: Hypersensitivity to the active substances or to any of the excipients. Severe hepatic insufficiency. Lactation (in order to avoid transmission of HIV). Oral soln: Hepatic or renal failure. Children <2 years. Pregnancy.
Special precautions: Risk of a lesser sustainability of virologic suppression and higher risk of diarrhoea with once daily dosing in adults. Limit once daily dosing to patients with <3 protease inhibitor-associated mutations. Pre-existing liver dysfunction including chronic hepatitis; consider interruption or discontinuation if liver disease worsens. Reports of increased bleeding in haemophiliacs. Monitor triglyceride and cholesterol levels; suspend if pancreatitis develops. New onset diabetes, hyperglycaemia or exacerbation of diabetes reported. May occur: Lipodystrophy (measure fasting serum lipids and blood glucose), immune reactivation syndrome (e.g. cytomegalovirus retinitis, generalised and/or focal mycobacterial infections, Pneumocystis jiroveci pneumonia), autoimmune disorders (such as Graves’ disease). May prolong the PR interval; patients with underlying structural heart disease or pre-existing conduction system abnormalities (caution). Osteonecrosis reported. Pregnancy (tab.). Oral soln contains alcohol, propylene glycol.
Drug interactions: Tablets, oral soln: Contra: CYP3A metabolites (e.g. alfuzosin, amiodarone, fusidic acid (for dermatological infections), astemizole, terfenadine, pimozide, dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, lovastatin, simvastatin, sildenafil (for pulmonary arterial hypertension (PAH)), vardenafil, oral midazolam, triazolam), St. John’s wort. Not recommended: Tadalafil (for PAH), fusidic acid (for osteo-articular infections), salmeterol, atorvastatin, rifampicin, colchicine, fluticasone or other glucocorticoids such as budesonide metabolised by CYP3A4, other HIV protease inhibitors, rivaroxaban, boceprevir, telaprevir, fosamprenavir, tipranavir, ketoconazole (>200mg/day), itraconazole (>200mg/day). Caution: Drugs which prolong the QT interval (e.g. chlorpheniramine, quinidine, erythromycin, clarithromycin), rosuvastatin, maraviroc, lamotrigine, valproate, tenofovir, fentanyl, digoxin, bepridil, systemic lidocaine, tyrosine kinase inhibitors, warfarin, carbamazepine, phenobarbital, phenytoin, trazodone, ketoconazole, itraconazole, voriconazole, rifabutin, parenteral midazolam, felodipine, nifedipine, nicardipine, dexamethasone, cyclosporin, sirolimus, tacrolimus, methadone, buproprion, bosentan, sildenafil and tadalafil (for erectile dysfunction), see SPC. Oral soln: Contra: Disulfiram, metronidazole. Do not administer Kaletra once daily in combination with efavirenz, nevirapine, amprenavir, nelfinavir, carbamazepine, phenobarbital or phenytoin. Use alternative/additional contraceptives with oestrogen-based oral contraceptives.
Adverse drug reactions: Upper and lower respiratory tract infections, skin infections, anaemia, leucopenia, neutropenia, lymphadenopathy, hypersensitivity, blood glucose disorders, hypertriglyceridaemia, hypercholesterolemia, decreased weight, decreased appetite, anxiety, headache, neuropathy, dizziness, insomnia, hypertension, GI disorders (including pancreatitis), hepatitis, lipodystrophy, dermatitis, night sweats, pruritis, myalgia, musculoskeletal pain, muscle disorders, erectile dysfunction, menstrual disorders, asthenia.
Full prescribing information and references available from AbbVie Ltd. Telephone: (01) 4287900.