Can statin cause lactic acidosis?
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Can statin cause lactic acidosis?
It is possible that the lactic acidosis was the result of the combination of both thiamine deficiency and statin treatment, such that removal of one element was sufficient to resolve the metabolic stress and result in the resolution of acidosis.
How do statins inhibit HMG-CoA reductase?
Statins competitively inhibit the HMG-CoA reductase enzyme. Statins bind to the active site of the enzyme and change its structure. As the structure of the enzyme is changed, it cannot bind with the receptor, thus its activity is reduced.
How are statins metabolized?
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.
Is atorvastatin an acid or base?
Atorvastatin is a dihydroxy monocarboxylic acid that is a member of the drug class known as statins, used primarily for lowering blood cholesterol and for preventing cardiovascular diseases.
Why do statins cause rhabdomyolysis?
The primary mechanism of statin therapy-induced rhabdomyolysis is believed to be a decrease in ubiquinone (coenzyme Q) produced by the HMG-CoA pathway. Additionally, different types of lipophilic and hydrophilic statins play a role in causing rhabdomyolysis.
Which statins cause the most rhabdomyolysis?
Simvastatin was the most common statin medication reported in association with rhabdomyolysis (55 cases), most commonly taken at a dose of 40 mg/day. Atorvastatin was the second most common drug (20 cases), used in doses of 10 mg/day.
Which amino acid is involved in the binding of HMG-CoA reductase?
Xu L, Simoni RD: The inhibition of degradation of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase by sterol regulatory element binding protein cleavage-activating protein requires four phenylalanine residues in span 6 of HMG-CoA reductase transmembrane domain.
Which of the following drug decreases cholesterol synthesis by inhibiting the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase?
Inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase commonly known as statins are widely used for treating hypercholesterolemia. However, there is much evidence to suggest that statins may have other properties in addition to their cholesterol-lowering effect.
How is lovastatin metabolized?
Lovastatin is metabolized by the microsomal hepatic enzyme system (Cytochrome P-450 isoform 3A4). The major active metabolites present in human plasma are the β-hydroxy acid of lovastatin, its 6′-hydroxy, 6′-hydroxymethyl, and 6′-exomethylene derivatives.
What enzyme metabolizes statins?
Simvastatin and atorvastatin, two widely prescribed cholesterol lowering medicines, are both metabolised by the isoenzyme cytochrome P450 3A4 (CYP3A4).
Is simvastatin an acid?
simvastatin hydroxy acid belongs to the class of organic compounds known as medium-chain hydroxy acids and derivatives. These are hydroxy acids with a 6 to 12 carbon atoms long side chain. Simvastatin is a hypolipidemic drug used to control elevated cholesterol, or hypercholesterolemia.
Which drug belongs to the class 3-hydroxy-3-methylglutaryl-coenzyme A HMG-CoA reductase inhibitors quizlet?
Atorvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.
Which statin causes least rhabdomyolysis?
Fluvastatin, pravastatin and rosuvastatin may be considered as alternatives as they are not as extensively metabolized by CYP3A4 and therefore less likely to result in rhabdomyolysis but still require careful monitoring [9].
Which statin has the lowest incidence of rhabdomyolysis?
Despite this, in consideration of myalgia as well as other adverse events, including rhabdomyolysis, CPK changes, and liver function test changes, the authors concluded that statins ordered from highest to lowest risk were atorvastatin > pravastatin = simvastatin = lovastatin > fluvastatin.
Which are products of 3-hydroxy-3-Methylglutaryl HMG )- CoA reductase?
Summary. The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase catalyzes the conversion of HMG-CoA to mevalonate, a four-electron oxidoreduction that is the rate-limiting step in the synthesis of cholesterol and other isoprenoids.
Which drug belongs to the class 3-hydroxy-3-methylglutaryl coenzyme A HMG-CoA reductase inhibitors?
3-Hydroxy-3-methylglutaryl–coenzyme A (HMG-CoA) reductase inhibitors (statins) are among the most prescribed medications in the United States. Statins act on the rate-limiting step in cholesterol biosynthesis (the conversion of HMG-CoA to mevalonate) and are effective in treating dyslipidemia.
What are 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors?
What enzyme does lovastatin inhibit?
Lovastatin is an inhibitor of hydroxymethyl glutaryl (HMG)-CoA reductase, the rate-limiting enzyme in cholesterol synthesis.
Is lovastatin a CYP3A4 inhibitor?
The effect of lovastatin on P-gp as well as CYP3A4 activity was also evaluated. Key findings: Lovastatin inhibited CYP3A4 enzyme activity with a 50% inhibition concentration of 6.06 µM.