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TABLE of CONTENTS LOPINAVIR and RITONAVIR Tablets, for Oral Use

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TABLE of CONTENTS LOPINAVIR and RITONAVIR Tablets, for Oral Use TABLE OF CONTENTS LOPINAVIR and RITONAVIR tablets, for oral use 2 HIGHLIGHTS OF PRESCRIBING INFORMATION 2 FULL PRESCRIBING INFORMATION 3 1 INDICATIONS AND USAGE 3 2 DOSAGE AND ADMINISTRATION 3 3 DOSAGE FORMS AND STRENGTHS 6 4 CONTRAINDICATIONS 6 5 WARNINGS AND PRECAUTIONS 7 6 ADVERSE REACTIONS 10 7 DRUG INTERACTIONS 16 8 USE IN SPECIFIC POPULATIONS 24 10 OVERDOSAGE 27 11 DESCRIPTION 27 12 CLINICAL PHARMACOLOGY 29 13 NONCLINICAL TOXICOLOGY 37 14 CLINICAL STUDIES 38 16 HOW SUPPLIED/STORAGE AND HANDLING 43 17 PATIENT COUNSELING INFORMATION 44 MEDICATION GUIDE 46 HIGHLIGHTS OF PRESCRIBING INFORMATION ---------------------------CONTRAINDICATIONS----------------------------- Hypersensitivity to lopinavir and ritonavir (e.g., toxic epidermal These highlights do not include all the information needed to use necrolysis, Stevens-Johnson syndrome, erythema multiforme, urticaria, LOPINAVIR AND RITONAVIR TABLETS safely and effectively. angioedema) or any of its ingredients, including ritonavir. (4) See full prescribing information for LOPINAVIR AND RITONAVIR Co-administration with drugs highly dependent on CYP3A for TABLETS. clearance and for which elevated plasma levels may result in serious and/or life-threatening events. (4) LOPINAVIR and RITONAVIR tablets, for oral use Co-administration with potent CYP3A inducers where significantly Initial U.S. Approval: 2000 reduced lopinavir plasma concentrations may be associated with the potential for loss of virologic response and possible resistance and --------------------------INDICATIONS AND USAGE------------------------ cross resistance. (4) Lopinavir and ritonavir is an HIV-1 protease inhibitor indicated in combination with other antiretroviral agents for the treatment of HIV-1 ----------------------WARNINGS AND PRECAUTIONS-------------------- infection in adults and pediatric patients (6 months and older weighing at The following have been observed in patients receiving lopinavir and least 15 kg). (1) ritonavir: The concomitant use of lopinavir and ritonavir and certain other drugs -----------------------DOSAGE AND ADMINISTRATION------------------ may result in known or potentially significant drug interactions. Tablets: May be taken with or without food, swallowed whole and not Consult the full prescribing information prior to and during treatment chewed, broken, or crushed. (2.1) for potential drug interactions. (5.1, 7.3) Pancreatitis: Fatalities have occurred; suspend therapy as clinically Adults (2.3): appropriate. (5.3) Total recommended daily dosage is 800/200 mg given once or twice Hepatotoxicity: Fatalities have occurred. Monitor liver function before daily. and during therapy, especially in patients with underlying hepatic Lopinavir and ritonavir can be given as once daily or twice daily disease, including hepatitis B and hepatitis C, or marked transaminase regimen. See Full Prescribing Information for details. elevations. (5.4, 8.6) Lopinavir and ritonavir once daily dosing regimen is not recommended QT interval prolongation and isolated cases of torsade de pointes have in: been reported although causality could not be established. Avoid use in Adult patients with three or more of the following lopinavir patients with congenital long QT syndrome, those with hypokalemia, resistance-associated substitutions: L10F/I/R/V, K20M/N/R, L24I, and with other drugs that prolong the QT interval. (5.1, 5.5, 12.3) L33F, M36I, I47V, G48V, I54L/T/V, V82A/C/F/S/T, and I84V. PR interval prolongation may occur in some patients. Cases of second (12.4) and third degree heart block have been reported. Use with caution in In combination with carbamazepine, phenobarbital, or phenytoin. patients with pre-existing conduction system disease, ischemic heart (7.3) disease, cardiomyopathy, underlying structural heart disease or when In combination with efavirenz, nevirapine, or nelfinavir. (12.3) administering with other drugs that may prolong the PR interval. (5.1, In pregnant women. (2.5, 8.1, 12.3) 5.6, 12.3) Patients may develop new onset or exacerbations of diabetes mellitus, Pediatric Patients (6 months and older weighing at least 15 kg) (2.4): hyperglycemia (5.7), immune reconstitution syndrome. (5.8), Lopinavir and ritonavir once daily dosing regimen is not recommended redistribution/accumulation of body fat. (5.10) in pediatric patients. Total cholesterol and triglycerides elevations. Monitor prior to therapy Twice daily dose is based on body weight or body surface area. and periodically thereafter. (5.9) Hemophilia: Spontaneous bleeding may occur, and additional factor Concomitant Therapy in Adults and Pediatric Patients: VIII may be required. (5.11) Dose adjustments of lopinavir and ritonavir may be needed when co- administering with efavirenz, nevirapine, or nelfinavir. (2.3, 2.4, 7.3) -----------------------------ADVERSE REACTIONS--------------------------- Commonly reported adverse reactions to lopinavir and ritonavir included Pregnancy (2.5): diarrhea, nausea, vomiting, hypertriglyceridemia and 400/100 mg twice daily in pregnant patients with no documented hypercholesterolemia. (6.1) lopinavir-associated resistance substitutions. There are insufficient data to recommend a lopinavir and ritonavir dose To report SUSPECTED ADVERSE REACTIONS, contact Cipla Ltd. for pregnant patients with any documented lopinavir and ritonavir- at 1-866-604-3268 or FDA at 1-800-FDA-1088 or associated resistance substitutions. www.fda.gov/medwatch No dose adjustment of lopinavir and ritonavir is required for patients during the postpartum period. ------------------------------DRUG INTERACTIONS-------------------------- Co-administration of lopinavir and ritonavir can alter the plasma ----------------------DOSAGE FORMS AND STRENGTHS---------------- concentrations of other drugs and other drugs may alter the plasma Tablets: 200 mg lopinavir and 50 mg ritonavir (3) concentrations of lopinavir. The potential for drug-drug interactions must Tablets: 100 mg lopinavir and 25 mg ritonavir (3) be considered prior to and during therapy. (4, 5.1, 7, 12.3) ------------------------USE IN SPECIFIC POPULATIONS------------------ Lactation: Breastfeeding not recommended. (8.2) See 17 for PATIENT COUNSELING INFORMATION and Medication Guide. Revised: 12/2018 FULL PRESCRIBING INFORMATION: CONTENTS* 8 USE IN SPECIFIC POPULATIONS 1 INDICATIONS AND USAGE 8.1 Pregnancy 2 DOSAGE AND ADMINISTRATION 8.2 Lactation 1 2.1 General Administration Recommendations 8.3 Females and Males of Reproductive Potential 2.3 Dosage Recommendations in Adults 8.4 Pediatric Use 2.4 Dosage Recommendations in Pediatric Patients 8.5 Geriatric Use 2.5 Dosage Recommendations in Pregnancy 8.6 Hepatic Impairment 3 DOSAGE FORMS AND STRENGTHS 10 OVERDOSAGE 4 CONTRAINDICATIONS 11 DESCRIPTION 5 WARNINGS AND PRECAUTIONS 12 CLINICAL PHARMACOLOGY 5.1 Risk of Serious Adverse Reactions Due to Drug Interactions 12.1 Mechanism of Action 5.3 Pancreatitis 12.2 Pharmacodynamics 5.4 Hepatotoxicity 12.3 Pharmacokinetics 5.5 QT Interval Prolongation 12.4 Microbiology 5.6 PR Interval Prolongation 13 NONCLINICAL TOXICOLOGY 5.7 Diabetes Mellitus/Hyperglycemia 13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility 5.8 Immune Reconstitution Syndrome 14 CLINICAL STUDIES 5.9 Lipid Elevations 14.1 Adult Patients without Prior Antiretroviral Therapy 5.10 Fat Redistribution 14.2 Adult Patients with Prior Antiretroviral Therapy 5.11 Patients with Hemophilia 14.3 Other Studies Supporting Approval in Adult Patients 5.12 Resistance/Cross-resistance 14.4 Pediatric Studies 6 ADVERSE REACTIONS 16 HOW SUPPLIED/STORAGE AND HANDLING 6.1 Clinical Trials Experience 17 PATIENT COUNSELING INFORMATION 6.2 Postmarketing Experience 7 DRUG INTERACTIONS *Sections or subsections omitted from the full prescribing information 7.1 Potential for Lopinavir and Ritonavir to Affect Other Drugs are not listed. 7.2 Potential for Other Drugs to Affect Lopinavir 7.3 Established and Other Potentially Significant Drug Interactions 7.4 Drugs with No Observed or Predicted Interactions with Lopinavir and Ritonavir FULL PRESCRIBING INFORMATION 1 INDICATIONS AND USAGE Lopinavir and ritonavir tablets are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients (6 months and older weighing at least 15 kg). Limitations of Use: Genotypic or phenotypic testing and/or treatment history should guide the use of lopinavir and ritonavir. The number of baseline lopinavir resistance-associated substitutions affects the virologic response to lopinavir and ritonavir [see Microbiology (12.4)]. 2 DOSAGE AND ADMINISTRATION 2.1 General Administration Recommendations Lopinavir and ritonavir tablets may be taken with or without food. The tablets should be swallowed whole and not chewed, broken, or crushed. 2 2.3 Dosage Recommendations in Adults Lopinavir and ritonavir can be given in once daily or twice daily dosing regimen at dosages noted in Tables 1 and 2. Lopinavir and ritonavir once daily dosing regimen is not recommended in: Adult patients with three or more of the following lopinavir resistance-associated substitutions: L10F/I/R/V, K20M/N/R, L24I, L33F, M36I, I47V, G48V, I54L/T/V, V82A/C/F/S/T, and I84V [see Microbiology (12.4)]. In combination with carbamazepine, phenobarbital, or phenytoin [see Drug Interactions (7.3)]. In combination with efavirenz, nevirapine, or nelfinavir [see Drug Interactions (7.3) and Clinical Pharmacology (12.3)]. In pediatric patients younger than 18 years of age [see Dosage and Administration (2.4)]. In
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