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PHAR3816 Lecture Notes - Lecture 9: Organic Anion-Transporting Polypeptide, Slco1B1, Hmg-Coa Reductase

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School
University of Sydney
Department
Pharmacy
Course
PHAR3816
Professor
Ingrid Gelissen

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Document Summary

Class of drugs aimed at lowering plasma cholesterol, in particular ldl (low density lipoprotein) cholesterol. They work by inhibiting a rate-limiting enzyme in the cholesterol synthetic pathway called hmgcoa reductase. They are targeted to reduce cholesterol synthesis in the liver as the majority of cholesterol in our body is synthesized there: however, most side effects of statins are due to off-target effects. Statins are safe to use but side effects are experienced in a subset of the population (proportion depends on the type of statin). These include: diarrhea, nausea, dyspepsia, musculoskeletal pain most common, muscular spasms, myopathy- muscle weakness, rhabdomyolysis. Statistics available up to 2004 show steady increase in statin prescriptions: higher doses and more potent statins are being prescribed. Statin dose is determined by starting on lowest dose, testing efficacy (plasma and cholesterol, ldl) after approximately 4 weeks, and titrate up. Doubling the dose is estimated to give an additional 4-6% reduction in ldl.

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