Bioavailability of simvastatin
WebOct 10, 2011 · One of the unique properties of simvastatin is very low bioavailability (<5%) due to high firstpass metabolism. For example, if a 20-mg dose is administered, only 1 mg reaches the systemic circulation. Increasing the bioavailability to 50% with a CYP3A4 inhibitor will increase the systemic exposure by 10-fold, to 10 mg. WebOct 10, 2011 · One of the unique properties of simvastatin is very low bioavailability (<5%) due to high firstpass metabolism. For example, if a 20-mg dose is administered, …
Bioavailability of simvastatin
Did you know?
WebDec 8, 2009 · The influence of the dietary flavonol quercetin on the pharmacokinetics of the HMG-CoA reductase inhibitor simvastatin was investigated in pigs. Simvastatin (0.25 mg/kg body weight) was orally administered to six pigs either without or with quercetin (10 mg/kg). In addition, simvastatin was administered to three pigs that had received a diet ... WebSon et al has showed that extensive metabolizers yielded a decrease in simvastatin bioavailability of 81% and a decrease in simvastatin clearance by 4.6-fold compared with poor metabolizers, when CYP3A4/5 polymorphisms were concerned. 14 Where the pharmacogenetic status (CYP3A4/5 polymorphism) is concerned, elevated C max and/or …
WebOct 23, 2012 · After absorption in humans, simvastatin undergoes extensive first-pass metabolism in the liver, the primary site of action, with subsequent excretion of drug in bile. The systemic bio-availability of the drug is therefore low: the absolute bioavailability of β-hydroxyacid-simvastatin is less than 5%. WebOct 6, 2024 · Co-administration of simvastatin with fluoxetine resulted in a significant increase in the bioavailability of simvastatin in the plasma (41.8%) and brain (68.7%) compared to administration of simvastatin alone (P < .05). Conversely, no significant changes in PK parameters of fluoxetine were observed during simvastatin co …
WebApr 15, 2004 · The objectives of this study were to develop and characterize the optimal formulation of SMEDDS containing simvastatin and to assess its bioavailability compared with a simvastatin tablet (Zocor ®, simvastatin 20 mg) in beagle dogs. Mean particle size of microemulsion was conducted by dynamic light scattering (DLS). WebJul 1, 2024 · The cholesterol-lowering agent, simvastatin (SIM), is poorly water-soluble and undergoes extensive first pass metabolism, resulting in a low oral bioavailability of approximately 5%. Hence, the current pre-clinical studies investigated the application of SLH technology to SIM with a supersaturation approach, aiming to enhance bioavailability ...
Metabolized by CYP3A4; does not inhibit CYP3A4. Substrate of organic anion transport protein (OATP) 1B1. When used in fixed combination … See more
WebNov 30, 2010 · Simvastatin is an antihyperlipidemic drug with poor oral bioavailability (<5%) due to the first pass metabolism. Present work has attempted to improve oral bioavailability of simvastatin by ... high end car door speakersWebFeb 25, 2002 · Verapamil significantly increased mean peak serum concentration and bioavailability of simvastatin, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. 63 This interaction probably … how fast is 5 horsepowerWebJan 4, 2024 · This application note is based on content from Pohlen et al. [1]. Simvastatin (CAS number 79902-63-9) is a cholesterol-lowering agent with a low bioavailability of … high end car coversWebJun 23, 2024 · More accurately, bioavailability is a measure of the rate and fraction of the initial dose of a drug that successfully reaches either; the site of action or the bodily fluid … high end canned tunaWebThe bioavailability of the statins differs greatly, from 5% for lovastatin and simvastatin to 60% or greater for cerivastatin and pitavastatin. Clinical studies have demonstrated rosuvastatin to be the most effective for reducing low-density lipoprotein cholesterol, followed by atorvastatin, simvastatin and pravastatin. ... how fast is 5.5 on treadmillWebApr 2, 2024 · Simvastatin (SIM), a lipophilic statin, is a commonly prescribed cholesterol-lowering drug accepted by the Food and Drug Administration (FDA) to treat high cholesterol levels related to high low-density lipoproteins (LDL) cholesterol levels and heart disease [1,2].The cholesterol-lowering effect of SIM is due to the inhibition of the 3-hydroxy-3 … high end car partsWebMar 15, 2002 · Bioavailability varies widely among the statins: simvastatin is less than 5 percent bioavailable, while fluvastatin is approximately 24 percent bioavailable. The … high end car paint shops