How does the liver metabolize rosuvastatin?

How does the liver metabolize rosuvastatin?

The liver metabolizes rosuvastatin mainly through CYP2C9. The enzyme adds a hydroxyl group to the drug, producing the inactive metabolite N-desmethyl rosuvastatin. This step accounts for only a small fraction of the dose, so most of the drug leaves the body unchanged.

What role does the liver transporter OATP1B1 play?

OATP1B1 moves rosuvastatin from blood into liver cells. Variants that reduce transporter activity can raise blood levels of the drug, increasing the chance of muscle-related side effects.

Why do some patients need lower doses of rosuvastatin?

People who carry reduced-function SLCO1B1 alleles, take cyclosporine, or use gemfibrozil experience slower hepatic uptake. Slower uptake keeps more drug in circulation, so guidelines recommend starting at 5 mg instead of 10 mg.

When does the liver finish clearing rosuvastatin?

About 90 percent of an oral dose is recovered in feces, mostly as unchanged drug that the liver excreted into bile. The remainder appears in urine. The half-life is roughly 19 hours, so steady-state levels are reached in about four days.

Can other drugs change how the liver processes rosuvastatin?

Rifampin induces CYP2C9 and can speed metabolism slightly, while gemfibrozil inhibits both the enzyme and OATP1B1. These interactions raise exposure and are listed in the prescribing information.

Who makes the original rosuvastatin tablets?

AstraZeneca markets the branded product as Crestor. Several generic manufacturers now supply the same active ingredient once the original patents expired.