atorvastatin & simvastatin Flashcards
A: clinical use
to prevent coronary heart disease by lowering circulating LDLs
A: site of action
liver, LDL receptors
A: mech of beneficial action
inhibits HMG-CoA reductase, leading to..
- up-regulation of LDL receptors
- increased removal of Apo B-containing lipoproteins in circulation
- reduction in synth & secretion of lipoproteins from liver
- decreased cholesterol production in liver
A: common/serious side effects
common: diarrhoea, nausea, insomnia, myopathies
serious: risk of developing diabetes mellitus
A: mech of disease & beneficial mech of drug
rate-limiting enzyme in cholesterol synth is HMG-CoA reductase; this catalyses conversion of HMG-CoA to mevalonic acid. as Atorvastatin is a specific, reversible, competitive HMG-CoA reductase inhibitor, there is
1. decreased hepatic cholesterol synth
2. up regulation of LDL receptor synth
3. increased LDL clearance from plasma –> liver cells
4. overall reduced plasma LDL to contribute to atherosclerosis
S: clinical use
to treat high cholesterol by lowering circulating LDLs via HMG-CoA reduction inhibition
S: site of action
liver, LDL receptors
S: mech of beneficial action
inhibition of HMG-CoA reductase, preventing the formation of mevalonate, which leads to a reduction in the liver synth of cholesterol & increased synth of LDL receptors in hepatocytes, thereby increasing its uptake from circulation to restore intracellular cholesterol.
S: common/serious side effects
raised liver enzymes and rarely myalgias
S: mech of disease & beneficial acton of the drug
primarily used in patients w Dyslipidaemia, a number of conditions in which fat metabolism disturbances lead to increased lipids in blood, they lower circulating lipids & increase their uptake.
