Swamped with your writing assignments? Take the weight off your shoulder!
Submit your assignment instructions
This assignment is about: The role of drug transporter pharmacogenetics in affecting drug (Rosuvastatin) disposition and bioavailability.
Explore the effect of this polymorphism on the transporter expression and/or functionality and Explain
the extent to which the transporter pharmacogenetics affects any aspect of the pharmacokinetics (ADME)
Rosuvastatin: Effects of polymorphisms in the ABCG2 gene on Rosuvastatin
Drug class: HMG-CoA Reductase Inhibitor
Dosage forms: Oral Tablet (5 mg, 10 mg, 20 mg, 40 mg), Oral Capsule (5 mg, 10 mg, 20
mg, 40 mg).
Indication: hyperlipidemia, Disorder of cardiovascular system, primary
prophylaxis, familial hypercholesterolemia, homozygous, hypertriglyceridemia,
MOA: competitively inhibit conversion of HMG-CoA to mevalonate, an early
rate-limiting step in cholesterol synthesis. A compensatory increase in LDL
receptors, which bind and remove circulating LDL-cholesterol, results. Production
of LDL-cholesterol can also decrease because of decreased production of
VLDL-cholesterol or increased VLDL removal by LDL receptors.
Pharmacokinetics of Rosuvastatin:
Absorption: F = 20%, food slows absorption
Distribution: Vd = 134 L; 88% protein bound
Metabolism: minimal hepatic
Excretion: Fecal 90% with half-life of 13-20 hours
What is ABCG2 polymorphism?
Drug transporter aka BCRP, an efflux pump
Usually expressed in tissues: kidney, brain, liver, placenta and the
Plays the role as a tissue barrier that limits the absorption in the
GI, BBB & placenta.
Xenobiotic substrates are excreted primarily in the bile & urine
Questions that you should do for this assignment:
1/The Role of ABCG2 Pharmacogenomics affecting
2/Explain the role of drug transporter pharmacogenetics in affecting
drug disposition ( rosuvastatin ) and bioavailability.
3/Effects of the rs2231142 on the Pharmacokinetics
4/Explore the effect of this polymorphism on the transporter
expression and/or functionality
Please DO NOT forget to write the work references.