Ritonavir and Lopinavir

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Inhibits
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names


Austria: Kaletra; Belgium: Kaletra; Bulgaria: Kaletra; Czech Republic: Kaletra; Denmark: Kaletra; Estonia: Kaletra; Finland: Kaletra; France: Kaletra; Germany: Kaletra; Greece: Kaletra; Hungary: Kaletra; Ireland: Kaletra; Italy: Kaletra; Latvia: Kaletra; Lithuania: Kaletra; Luxembourg: Kaletra; Malta: Kaletra; Netherlands: Kaletra; Poland: Kaletra; Portugal: Kaletra; Romania: Kaletra; Slovakia: Kaletra; Slovenia: Kaletra; Spain: Kaletra; Sweden: Kaletra; UK: Kaletra.

North America

Canada: Kaletra; USA: Kaletra.

Latin America

Argentina: Kaletra; Brazil: Kaletra; Mexico: Kaletra.


Japan: Kaletra.

Drug combinations


Ritonavir: C~37~H~48~N~6~O~5~S~2~. Mw: 720.94. (1) 2,4,7,12-Tetraazatridecan-13-oic acid, 10-hydroxy-2-methyl-5-(1-methylethyl)-1-[2-(1-methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-5-thiazolylmethyl ester [5S-(5R*,8R*,10R*,11R*)]-; (2) 5-Thiazolylmethyl [(αS)-α-[(1S,3S)-1-hydroxy-3-[(2S)-2-[3-[(2-isopropyl-4-thiazolyl)methyl]-3-methylureido]-3-methylbutyramido]-4-phenylbutyl]phenethyl]carbamate. CAS-155213-67-5 (1995).

Lopinavir: C~37~H~48~N~4~O~5~. Mw: 628.80. (1) [1S-[1R*(R*),3R*,4R*]]-N-[4-[[(2,6-Dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-α-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetamide; (2)(αS)-Tetrahydro-N-[(αS)-α-[(2S,3S)-2-hydroxy-4-phenyl-3-[2-(2,6-xylyloxy)acetamido]butyl]phenethyl]-α-isopropyl-2-oxo-1(2H)-pyrimidineacetamide. CAS-192725-17-0 (1998).

Drug Combination

Ritonavir and Lopinavir.

Pharmacologic Category

Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE03 and J05AE06).

Mechanism of action

Lopinavir component is the active inhibitor of HIV protease. Ritonavir component inhibits CYP3A metabolism of lopinavir, allowing increased lopinavir plasma levels.

Therapeutic use

Treatment of HIV infection in combination with other antiretroviral agents.

Pregnancy and lactiation implications

Lopinavir/ritonavir crosses placenta, however, teratogenic effects not observed in humans. Pregnancy and protease inhibitors both associated with increased risk of hyperglycemia. HIV-infected mothers are discouraged from breast-feeding to decrease potential transmission of HIV.

Unlabeled use


Hypersensitivity to lopinavir, ritonavir, or any component of the formulation. Administration with medications highly dependent upon CYP3A4 for clearance for which increased levels are associated with serious and/or life-threatening events, including cisapride, dihydroergotamine, ergonovine, ergotamine, methylergonovine, midazolam, pimozide, and triazolam. Co-administration with lovastatin or simvastatin, or strong CYP3A4 inducers, such as rifampin and St. John’s wort.

Warnings and precautions

May cause fat redistribution. Patients may develop immune reconstitution syndrome resulting in occurrence of inflammatory response to indolent or residual opportunistic infection. Increases in total cholesterol and triglycerides reported. Changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, DKA, and new-onset diabetes mellitus reported in patients receiving protease inhibitors. Use with caution in hemophilia A or B. May cause hepatitis and/or exacerbate pre-existing hepatic dysfunction (use with caution in underlying hepatic disease, such as hepatitis B or C, cirrhosis, or unspecified hepatic impairment). Use with caution in increased triglycerides (pancreatitis observed). Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates. Contraindicated with certain CYP3A4 substrates and inducers. Contraindicated with ergot derivatives, midazolam, pimozide, and triazolam. Avoid concurrent use with St. John’s wort. Dyslipidemia common (use caution with clozapine, olanzapine, and quetiapine). Diarrhea common (use caution with lithium, valproic acid, and SSRIs). Increased LFTs common (use caution with olanzapine and valproic acid). May cause hyperglycemia (use caution with clozapine and olanzapine). May cause thrombocytopenia (use caution with valproic acid). Carbamazepine, phenytoin, and phenobarbital may decrease levels of lopinavir. Ritonavir may increase levels of zolpidem. Solution contains ethanol (use caution with disulfiram).



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