Is Simvastatin metabolized by the liver?
Is Simvastatin metabolized by the liver?
Additionally, the liver is the main site of statin metabolism. Decreased transport of simvastatin into hepatocytes has been related to increased risk of myopathy.
How is simvastatin metabolized?
Simvastatin is metabolized by the cytochrome P450 isoform 3A4. Certain drugs which inhibit this 4 Page 5 ZOCOR® (simvastatin) 9876252 metabolic pathway can raise the plasma levels of simvastatin and may increase the risk of myopathy.
What is the metabolic enzyme involved in the metabolism of simvastatin?
Most of the statins are metabolized through the cytochrome P450 (CYP) metabolic pathway; atorvastatin (Lipitor), simvastatin (Zocor), and lovastatin (Mevacor, Altocor) via the CYP3A4 isoenzyme, and fluvastatin (Lescol) via CYP2C9.
What is the mechanism of action of simvastatin?
Simvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
Does simvastatin affect liver?
Of all statins, simvastatin and atorvastatin are responsible for most reported incidents of liver damage, but this is likely just due to the fact that they are prescribed the most. The Spanish Hepatotoxicity Registry identified 858 cases of drug-induce liver injury.
How are statins metabolized?
Statins are metabolized by CYP450 isoenzymes, with the exception of pravastatin, which is metabolized in the cellular cytosol by sulfation. In addition, they present gastrointestinal and hepatic first-pass metabolism.
Where is simvastatin excreted?
Following an oral dose of 14C-labeled simvastatin in man, 13% of the dose was excreted in urine and 60% in feces. Patients with this genotype have a greater reduction in risk of a major cardiovascular event with high dose simvastatin.
When is simvastatin contraindicated?
Patients with contraindications to simvastatin pharmacotherapy include those with active liver disease, including those who have elevated hepatic enzymes, pregnancy, and women who may become pregnant or who are breastfeeding.
What functional groups are in simvastatin?
Simvastatin is also a nonpolar molecule. Its functional groups include two esters and an alcohol. The pKa’s are 16 and 25 respectively.
Does simvastatin raise liver enzymes?
Standard doses of statins elevate liver enzymes in about 1 percent of patients, usually within the first four months. The likelihood of this elevation increases in older people and in those taking other medications that might interact with statins or also raise liver enzymes.
Can statins affect liver function?
Statins should not be taken if you have severe liver disease or if blood tests suggest that your liver may not be working properly. This is because statins can affect your liver, and this is more likely to cause serious problems if you already have a severely damaged liver.
Is simvastatin bad?
A very small number of people taking simvastatin may have mild memory problems or confusion. If these rare effects occur, talk to your doctor. Rarely, statins may cause or worsen diabetes. Talk to your doctor about the benefits and risks.
Can simvastatin cause liver disease?
Warnings and Precautions Because simvastatin can affect the liver, it is used with caution in people who drink more than a moderate amount of alcohol or have a history of liver disease. Simvastatin is not recommended for people with liver disease or high liver enzymes before treatment begins.
Is simvastatin safe?
Simvastatin seems to be a very safe medicine. It’s unusual to have any side effects. Keep taking simvastatin even if you feel well, as you will still be getting the benefits. Most people with high cholesterol don’t have any symptoms. Do not take simvastatin if you’re pregnant, trying to get pregnant or breastfeeding.
