Sandbox 55: Difference between revisions
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Bruce Roth, a Phizer employee, first synthesized atorvastatin in 1985. In 2008 Lipitor was the top-selling pharmaceutical in the world with $12.4 billion in sales. However, Lipitor's US patent protection is scheduled to expire in June 2011<ref>^"Pfizer wins patent extension on cholesterol drug". Associated Press. 6 January 2009. http://www.nj.com/business/index.ssf/2009/01/pfizer_wins_patent_extension_o.html.</ref>. | Bruce Roth, a Phizer employee, first synthesized atorvastatin in 1985. In 2008 Lipitor was the top-selling pharmaceutical in the world with $12.4 billion in sales. However, Lipitor's US patent protection is scheduled to expire in June 2011<ref>^"Pfizer wins patent extension on cholesterol drug". Associated Press. 6 January 2009. http://www.nj.com/business/index.ssf/2009/01/pfizer_wins_patent_extension_o.html.</ref>. | ||
== | =Chemical Properties= | ||
Formula: C<sub>33</sub>H<sub>35</sub>FN<sub>2</sub>O<sub>5</sub> | |||
Molecular Mass: 558.64 g/mol | |||
Half life: 14 hours | Half life: 14 hours | ||
Half-life of HMG-CoA inhibitor activity: 20-30 hours | |||
Excretion: Bile | Excretion: Bile | ||
=Structure= | |||
==Considerations When Taking Atorvastatin== | ==Considerations When Taking Atorvastatin== | ||
Atorvastatin should be taken only in conjuction with a complete cholesterol-lowering program which includes diet, exercise, and weight control<ref>"Atorvastatin." Cerner Multum, Inc., 12 Aug. 2009. Web. 09 Mar. 2011. <http://www.drugs.com/atorvastatin.html>.</ref>. | Atorvastatin should be taken only in conjuction with a complete cholesterol-lowering program which includes diet, exercise, and weight control<ref>"Atorvastatin." Cerner Multum, Inc., 12 Aug. 2009. Web. 09 Mar. 2011. <http://www.drugs.com/atorvastatin.html>.</ref>. | ||
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Vitamin D actually lowers atorvastatin active metabolite concentrations<ref>Schwartz, JB (February 2009). "Effects of vitamin D supplementation in atorvastatin-treated patients: a new drug interaction with an unexpected consequence". Clin Pharmacol Ther 85 (2): 198–203.</ref>. Interestingly, grapefruit juice in co-administration with atorvastatin increases atorvastatin's Cmax (rate of absorption) and AUC (extent of absorption) which can lead to adverse effects. Grapefruit juice is a known inhibitor of Cytochrome P450 3A4 (CYP3A4), which is involved in the deactivation of avtorvastatin for excretion from the body<ref>Kane, GC; Lipsky, JJ (September 2000). "Drug-grapefruit juice interactions". Mayo Clin Proc 75 (9): 933–42</ref>. | Vitamin D actually lowers atorvastatin active metabolite concentrations<ref>Schwartz, JB (February 2009). "Effects of vitamin D supplementation in atorvastatin-treated patients: a new drug interaction with an unexpected consequence". Clin Pharmacol Ther 85 (2): 198–203.</ref>. Interestingly, grapefruit juice in co-administration with atorvastatin increases atorvastatin's Cmax (rate of absorption) and AUC (extent of absorption) which can lead to adverse effects. Grapefruit juice is a known inhibitor of Cytochrome P450 3A4 (CYP3A4), which is involved in the deactivation of avtorvastatin for excretion from the body<ref>Kane, GC; Lipsky, JJ (September 2000). "Drug-grapefruit juice interactions". Mayo Clin Proc 75 (9): 933–42</ref>. | ||
=Targets= | |||
Atorvastatin's main target is HMG-CoA Reductase, however, it also can target Dipeptidyl peptidase 4 and Aryl hydrocarbon receptor<ref>LDL-C, Decreasing. "DrugBank: Atorvastatin (DB01076)." DrugBank: Welcome. Web. 09 Mar. 2011. <http://www.drugbank.ca/drugs/DB01076>.</ref>. | |||
==HMG-CoA Reductase== | |||
<applet load='1hwk' size='400' frame='true' align='right' caption='HMG-CoA Reductase in complex with Lipitor' /> | |||
===Mechanism of Action=== | |||
==Dipeptidyl peptidase 4 and Aryl hydrocarbon receptor== | |||
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==References== | ==References== | ||
<references/> | <references/> | ||
