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PMCOL 344 - Metabolism Exam Latest Update
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PMCOL 344 - Metabolism ExamLatest Update
Simvastatin - Answer Statin; reversibly inhhibits cholesterol biosynthesis by
competitively inhibiting HMG-CoA reductase (rate-limiting step, causing upregulation of
LDL receptors in liver, reduced production of VLDL and LDL, and increased HDL.
Metabolized by CYP enzymes. Side effects: myositis, rhabdomyolysis, type 2 diabetes.
Gemfibrozil - Answer Fibrate; activates PPAR-alpha receptor which alters the
expression of enzymes involved in lipid metabolism. Increases LPL expression,
decrease VLDL and LDL production, increase expression of ApoA1 on HDL (and
increase HDL in general), and increase LDL receptor expression. Side effects: myositis
and rhabdomyolysis
Colesevelam - Answer Resin. Anion exhange resins are positively charged so they bind
to negatively charged bile acids and prevent reabsorption. Leads to increase in bile
synthesis from bodily cholesterol. Increased hepatic expression of LDL receptors. Used
in combo with statins to prevent increase in hepatic cholesterol synthesis. Side effects:
increases TG production so can't use in patients with high TGs, bloating.
Nicotonic acid - Answer Might act through HM74A (orphan receptor). Inhibts lipolysis of
TGs by hormone-sensitive lipase but increased LPL activity, decreased liver TG
synthesis, decreased VLDL and LDL production. Less hepatic clearance of Apo-A1 so
more HDL (and increased expression of ABCA1). Only one that reducs lipoprotein A.
Side effects: facial flushing, itching.
Ezetimibe - Answer Inhibits cholesterol absorption by blocking the NPC1L1 receptor in
duodenum epithelial cells. Doesn't affect the absorption of anything else. Potent.
Sibutramine - Answer SSRI; inhibits reuptake of 5-HT, NA, and DA in arcuate nucleus.
Enhances satiety and increases energy expenditure through thermogenesis (from symp
system). But increases BP and HR.
Lorcaserin - Answer 5-HT(2c) receptor agonist that suppresses appetite by acting on
POMC-producing neurons (have 5-HT2c receptor). Stimulates release of alpha-MSH
which activcates anorexogenic pathways. Low affinity for other 5-HT subtypes so less
off-target effects.
Phenteramine - Answer Sympathomimetic drug (prevents NA reuptake) which enhances
satiety in the CNS and increases thermogenesis in PNS. Can also cause hypertension
and tachycardia bc symp stimulation and potential for addiction.
Topiramate - Answer GABA enhancer (blocks Na channels and activates K channels,
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