Pharm - CKD Flashcards
What are statins?
selective, competitive inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase
What are some examples of statins?
Simvastatin
Artorvastatin
What is the primary mechanism of action for statins?
- competitive inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, which is the enzyme responsible for converting HMG-CoA to mevalonate in the cholesterol synthesis pathway
- By reducing hepatic cholesterol synthesis, an upregulation of LDL-receptors and increased hepatic uptake of LDL-cholesterol from the circulation occurs
What is the drug target for statins?
Hydroxymethylglutaryl-CoA (HMG-CoA) reductase
What are the main side effects of statins?
- Muscle toxicity (however the likelihood increases with higher doses)
- Constipation
- Diarrhoea
- Other gastrointestinal symptoms
What are the uses of statins?
reducing the risk of adverse cardiac events in people
What should patients using statins be followed up for?
monitor for hyperkalaemia + acute renal failure
What can increase statin serum concentrations?
Coadministration with potent 3A4 inhibitors
What is the primary mechanism of aspirin?
- Irreversible inactivation of COX enzyme
- Prevents oxidation of arachidonic acid to produce prostaglandins
- Reduction of thromboxane A2 in platelets reduces aggregation.
- Reduction of PGE2 (i) at sensory pain neurones reduces pain and sensation and (ii) in the brain decreases fever
What is the drug target for aspirin?
cyclo-oxygenase
What are the main side effects of aspirin?
Dyspepsia
Haemorrhage
In the elderly, avoid doses greater than 160mg daily (increased risk of bleeding) and coadminister PPI if past history of peptic ulcer.
Why can aspirin cause GI side effects?
Blockade of COX1 in gastric mucosal cells reduces mucus/bicarbonate production which can expose the stomach lining to acid.
What is the primary mechanism of action of trimethoprim?
Direct competitor of the enzyme dihydrofolate reductase
Inhibits the reduction of dihydrofolic acid to tetrahydrofolic acid (active form) – a necessary component for synthesising purines required for DNA and protein production.
What is the drug target for trimethoprim?
dihydrofolate reductase
What are the main side effects of trimethoprim?
diarrhoea
skin reactions