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Atorvastatin, commercially known as Lipitor is a 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA Reductase) inhibitor. It is part of a class of medications known as statins that are cholesterol-lowering medications<ref>Phizer Inc. "Lipitor." Lipitor: Atorvastatin Calcium Tablets. Phizer Inc., 2011. Web. 09 Mar. 2011. <http://www.lipitor.com/aboutLipitor.aspx>.</ref>. HMG-CoA reductase catalyzes the committed step in cholesterol synthesis, so by inhibiting this step, low density lipoprotein (LDL) cholesterol can be effectively lowered. By lowering LDL, the likelihood of stroke and heart attack can be decreased<ref>NIH. "Atorvastatin." PubMed Health. National Institutes of Health, 01 July 2010. Web. 09 Mar. 2011. <http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000009/>.</ref>.
Atorvastatin, commercially known as Lipitor is a 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA Reductase) inhibitor. It is part of a class of medications known as statins that are cholesterol-lowering medications<ref>Phizer Inc. "Lipitor." Lipitor: Atorvastatin Calcium Tablets. Phizer Inc., 2011. Web. 09 Mar. 2011. <http://www.lipitor.com/aboutLipitor.aspx>.</ref>. HMG-CoA reductase catalyzes the committed step in cholesterol synthesis, so by inhibiting this step, low density lipoprotein (LDL) cholesterol can be effectively lowered. By lowering LDL, the likelihood of stroke and heart attack can be decreased<ref>NIH. "Atorvastatin." PubMed Health. National Institutes of Health, 01 July 2010. Web. 09 Mar. 2011. <http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000009/>.</ref>.
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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
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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>.
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Atorvastatin was first synthesized in 1985 by Bruce Roth while working at Parke-Davis Warner-Lambert Company (now Pfizer). With 2008 sales of US$12.4 billion, Lipitor was the top-selling branded pharmaceutical in the world.[1] US patent protection is scheduled to expire in June 2011.[2][3] However, Pfizer made an agreement with Ranbaxy Laboratories to delay the generic launch in the US until November 2011. It is sold in India under the trade name Atarvadel.[1]
 
==Considerations When Taking Atorvastatin==
==Considerations When Taking Atorvastatin==

Revision as of 02:57, 10 March 2011

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Contents

Atorvastatin

Atorvastatin, commercially known as Lipitor is a 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA Reductase) inhibitor. It is part of a class of medications known as statins that are cholesterol-lowering medications[1]. HMG-CoA reductase catalyzes the committed step in cholesterol synthesis, so by inhibiting this step, low density lipoprotein (LDL) cholesterol can be effectively lowered. By lowering LDL, the likelihood of stroke and heart attack can be decreased[2].

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[3].


Considerations When Taking Atorvastatin

Atorvastatin should be taken only in conjuction with a complete cholesterol-lowering program which includes diet, exercise, and weight control[4].

Side Effects

There are numerous side effects that can occur from taking atorvastatin. The most serious side effect although the most rare is myopathy (muscular weakness) with increased levels of creatinine kinase and rhabdomyolysis (rapid breakdown of skeletal muscle). Other more common side effects include headache, weakness, insomnia, peripheral edema, urinary tract infections, and flu-like symptoms[5]. Atorvastatin has also been shown to elevate the levels of alanine transaminase (ALT) and aspartate transaminase (AST)[6].

Atorvastatin has been shown to cause fetal harm in pregnant women, so should never be prescribed in women who are pregnant. Cholesterol levels and triacylglycerols increase naturally during pregnancy and are essential for the development of the fetus, and slowing production of cholesterol could have detrimental effects on the fetus [7].

Adverse Food and Drug Interactions

Atorvastatin can interact with many other drugs including, digoxin (E.g. digitalis),warfarin, erythromycin, fenofibrate (E.g. Tricor), niacin, certain antifungal medications (E.g. Diflucan), certain cancer medications and steroids, and HIV/AIDS medications[8].

Vitamin D actually lowers atorvastatin active metabolite concentrations[9]. 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[10].





HMG-CoA Reductase in complex with Lipitor

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References

  1. ↑ Phizer Inc. "Lipitor." Lipitor: Atorvastatin Calcium Tablets. Phizer Inc., 2011. Web. 09 Mar. 2011. <http://www.lipitor.com/aboutLipitor.aspx>.
  2. ↑ NIH. "Atorvastatin." PubMed Health. National Institutes of Health, 01 July 2010. Web. 09 Mar. 2011. <http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000009/>.
  3. ↑ ^"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.
  4. ↑ "Atorvastatin." Cerner Multum, Inc., 12 Aug. 2009. Web. 09 Mar. 2011. <http://www.drugs.com/atorvastatin.html>.
  5. ↑ "Lipitor (atorvastatin)." Medications and Drugs. HealthWise, 12 Aug. 2009. Web. 09 Mar. 2011. <http://www.emedicinehealth.com/drug-atorvastatin/article_em.htm>.
  6. ↑ Williams, D; Feely, J (2002). "Pharmacokinetic-pharmacodynamic drug interactions with HMG-CoA reductase inhibitors". Clin Pharmacokinet 41 (5): 343–70.
  7. ↑ Lipitor: Prescribing Information. Pfizer. June 2009.
  8. ↑ "Lipitor (atorvastatin)." Medications and Drugs. HealthWise, 12 Aug. 2009. Web. 09 Mar. 2011. <http://www.emedicinehealth.com/drug-atorvastatin/article_em.htm>.
  9. ↑ 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.
  10. ↑ Kane, GC; Lipsky, JJ (September 2000). "Drug-grapefruit juice interactions". Mayo Clin Proc 75 (9): 933–42
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