simvastatin
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Simvastatin is a lipid-lowering drug that belongs to the statin class. It works by inhibiting HMG-CoA reductase and is derived synthetically from lovastatin, which is produced by the fungus Aspergillus terreus. Simvastatin lowers LDL and triglyceride levels while raising HDL. It is used to treat high cholesterol and reduce heart disease risk. The document describes simvastatin's mechanism of action, pharmacokinetics, production method from lovastatin, side effects, and clinical uses.
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UNIT-5 Protein Engineering: Brief introduction to protein engineering,Use of ...
UNIT-5 6th Sem B.PHARMA PHARMACEUTICAL BIOTECHNOLOGY)
Protein Engineering: Brief introduction to protein engineering, Use of microbes in industry, Production of enzymes-general considerations, Amylase, Catalase, peroxidase, Lipase Basic principles of genetic engineering
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In this context, there is a need to use “biodetergent or biocleaners”, which offer a better option to the synthetic detergents with respect to their biodegradability, low toxicity, non-corrosiveness environmental-friendliness, enhanced cleaning properties and their increased efficiency and stability in different formulations.
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FERMENTATION OF STATINS/SAGAR SHARMA/DEPARTMENT OF PHARMACEUTICAL SCIENCES KUK
Fermentation using fungi is used to produce statins. Lovastatin was the first statin produced through fermentation of Aspergillus terreus. Both solid substrate fermentation and submerged liquid fermentation techniques are used to produce statins like lovastatin. Lovastatin is then converted chemically to produce other statins like simvastatin. Statins lower cholesterol and have other pleiotropic effects, making them useful for treating disorders beyond just high cholesterol.
Industrial production of important amino acids
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Please share your feedback and queries. Constructive criticism is appreciated.
Thank you
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simvastatin
- 1. SIMVASTATIN BY PROTTAY DUTTA MPH/10055/20 M.PHARM IN PHARMACEUTICAL CHEMISTRY PHARMACEUTICAL PROCESS CHEMISTRY(MPC 204T)
- 2. INTRODUCTION • Simvastatin is a Hypolipedemic drug belonging to the class of Statins. • It is a Lipid-lowering Agent, and is derived synthetically from Lovastatin (formerly known as Mevinclin) which was isolated from Aspergillus Terreus. • Simvastatin is chemically modified derivative of lovastatin. • It reduces very low density lipoprotein (VLDL), triglycerides (TG) and increases high density lipoprotein cholesterol (HDL-C).
- 3. • It is used along with exercise, diet, and weight loss to decrease elevated lipid levels. • It is also used to decrease the risk of heart problems in those at high risk. • It is taken by mouth. • They are improvement in Endothelial Function, Decreasing Vascular Inflammation, Inhibiting Smooth muscle Proliferation And Immunomodulation. • In the present study, Anti-inflammatory effect of simvastatin was evaluated and it was compared with diclofenac sodium by using Digital Plethysmometer.
- 4. • Simvastatin (Zocor) is used to treat hypercholesterolemia. • Half life -2 hrs. • HMG-CoA reductase inhibitor. • Metabolized by : CYP3A4 and carboxyl esterases. • Bioavailability of simvastatin is 5 %.
- 5. SIDE EFFECTS • A very small number of people taking simvastatin may have mild memory problems or confusion. • may cause or worsen diabetes. • may rarely cause liver problems. • symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
- 7. PRODUCTION OF SIMVASTATIN Monacolin J is manufactured through alkaline hydrolysis of lovastatin, a fungal polyketide produced by Aspergillus terreus. Multistep chemical processes for the conversion of lovastatin to simvastatin are laborious, cost expensive and environmentally unfriendly. A biocatalysis process for monacolin J conversion to simvastatin has been developed. However, direct bioproduction of monacolin J has not yet been achieved. Here, we identified a lovastatin hydrolase from Penicillium chrysogenum, which displays a 232-fold higher catalytic efficiency for the in vitro hydrolysis of lovastatin compared to a previously patented hydrolase, but no activity for simvastatin. Furthermore, we showed that an industrial A. terreus strain heterologously expressing this lovastatin hydrolase can produce monacolin J through single-step fermentation with high efficiency, approximately 95% of the biosynthesized lovastatin was hydrolyzed to monacolin J. Our results demonstrate a simple and green technical route for the production of monacolin J, which makes complete bioproduction of the cholesterol-lowering drug simvastatin feasible and promising.
- 8. PHARMACOKINETICS PARAMETER • Cmax = Maximum drug concentration • Tmax = The time of the maximum concentration. • AUC= Area under the curve. • Ke = Elimination rate . • t1/2 = The drug half life. t1/2 = ln2/ke
- 9. REFERENCE • https://www.sciencedirect.com/science/article/abs/pii/S1096717617301180 • rxList the internet drug index . Zocor. http://www.rxlist.com/zocor-drug.htm. Accessed on 13/10/2013. • https://www.drugs.com/simvastatin.html#side-effects • https://pubmed.ncbi.nlm.nih.gov/12067471/