How is ritonavir metabolized?
Rachel Newton
Updated on February 18, 2026
How is ritonavir metabolized?
Ritonavir is primarily metabolized by the CYP3A subfamily (5, 6) through N-demethylation, hydroxylation of the isopropyl side chain, and oxidation and cleavage of the terminal isopropyl-thiazole group (7).
What are the physicochemical properties of Lopinavir?
Lopinavir has the following structural formula: Ritonavir is chemically designated as 10-Hydroxy-2-methyl-5-(1-methylethyl)-1- [2-(1- methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-2,4,7,12-tetraazatridecan-13-oic acid, 5-thiazolylmethyl ester, [5S-(5R*,8R*,10R*,11R*)].
Is ritonavir an enzyme inducer or inhibitor?
Data synthesis: Ritonavir is a well-known inhibitor of the metabolism of numerous medications that are substrates of the CYP3A and CYP2D6 pathways. It also exhibits a biphasic, time-dependent effect on P-glycoprotein of inhibition followed by induction.
What is Lopinavir used for?
The combination of lopinavir and ritonavir is used with other medications to treat human immunodeficiency virus (HIV) infection. Lopinavir and ritonavir are in a class of medications called protease inhibitors. They work by decreasing the amount of HIV in the blood.
What are the side effects of ritonavir?
Diarrhea, nausea, vomiting, heartburn, stomach pain, dizziness, tiredness, weakness, changes in taste, or tingling/numbness of mouth area may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
How are protease inhibitors metabolized?
All the currently available protease inhibitors are metabolised by the cytochrome P450 (CYP) enzyme system. All are inhibitors of CYP3A4, ranging from weak inhibition for saquinavir to very potent inhibition for ritonavir.
What is Lopinavir made of?
Lopinavir is a novel and strong protease inhibitor developed from ritonavir with high specificity for HIV-1 protease [139-141].
What company makes Lopinavir?
As one of the first pharmaceutical companies to respond to the emerging novel coronavirus (COVID-19) crisis, in late January, AbbVie donated a supply of Kaletra/Aluvia (lopinavir/ritonavir) to the Chinese health authorities for use as an experimental treatment option.
What is the brand name for ritonavir?
Ritonavir (brand name: Norvir) is a prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of HIV infection in adults and children older than 1 month. Ritonavir is always used in combination with other HIV medicines.
What is CYP3A4 enzyme?
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14. 13.97) is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body.
Is Lopinavir used for Covid?
In conclusion, we found that lopinavir–ritonavir treatment did not significantly accelerate clinical improvement, reduce mortality, or diminish throat viral RNA detectability in patients with serious Covid-19.
Does ritonavir cause stomach pain?
Lopinavir and ritonavir can cause changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist)….Adverse Reactions In Adults.
| System Organ Class (SOC) and Adverse Reaction | n | % |
|---|---|---|
| diarrhea* | 510 | 19.5 |
| nausea | 269 | 10.3 |
| vomiting* | 177 | 6.8 |
| abdominal pain (upper and lower)* | 160 | 6.1 |