core drugs of CKD Flashcards
what are the main classes of drugs used to treat CKD?
Statins
Examples:
Simvastatin, artorvastatin
Aspirin
Trimethoprim (but this is an antibiotic, might just have been for tutorial)
Gentamicin
Calcium channel blockers
Examples:
Amlodipine
Felodipine
Angiotensin converting enzyme inhibitors Examples: Ramipri Lisinopril Perindopril
Angiotensin receptor blockers Examples: Losartan Irbesartan Candesartan
what is the primary mechanism of action of statins?
Statins are a selective, 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 of statins?
Hydroxymethylglutaryl-CoA (HMG-CoA) reductase
what are the side effects of statins?
Muscle toxicity can occur with all statins, however the likelihood increases with higher doses and in certain patients at increased risk of muscle toxicity.
Constipation or diarrhoea. Other gastrointestinal symptoms.
what is some extra information about statins?
Effective at reducing the risk of adverse cardiac events in people.
All patients should be regularly followed up to monitor for hyperkalaemia and acute renal failure.
Coadministration with potent 3A4 inhibitors may result in increased statin serum concentrations.
In 2020, artorvastatin was the 1st and simvastatin the 11th most commonly prescribed drugs in the West London area
what is the primary mechanism of action 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 of aspirin?
Cyclo-oxygenase
what are the 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.
what is some extra information about aspirin?
Low dose aspirin is the most cost effective medicine for the prevention of secondary events of thrombosis.
Blockade of COX1 in gastric mucosal cells reduces mucus/bicarbonate production which can expose the stomach lining to acid.
In 2020, aspirin was the 8th most commonly prescribed drugs in the West London area
what is the primary mechanism of action of Trimethoprim?
Direct competitor of the enzyme dihydrofolate reductase. Inhibits the reduction of dihydrofolic cid to tetrahydrofolic acid (active form) – a necessary component for synthesising purines required for DNA and protein production.
what is the drug target of Trimethoprim?
Dihydrofolate reductase
what are the side effects of Trimethoprim?
Diarrhoea
Skin reactions
what is some extra information about Trimethoprim?
Often administered with sulfamethoxazole – known as co-trimoxazole. In combination, they block two steps in bacterial biosynthesis of essential nucleic acids and proteins.
Need to monitor blood counts with long term use or in those at risk of folate deficiency. Also monitor serum electrolytes in patients at risk of developing hyperkalaemia.
what is the primary mechanism of action of Gentamicin?
Binds to the bacterial 30s ribosomal subunit disturbing the translation of mRNA leading to the formation of dysfunctional proteins.
what is the drug target of Gentamicin?
30s ribosomal subunit
