CPT S3 Steroids & Cholesterol Flashcards
Describe the metabolism of the combined oral contraceptive pill
Metabolised by CYP450 enzymes in the liver
Therefore affected by enzyme inducing and inhibiting drugs
Give some examples of adverse effects of the COCP
Venous thromboembolism MI Hypertension Decreased glucose tolerance Increased risk of stroke in women who get focal migraines Headaches Mood swings Cholestatic jaundice Increased gallstone incidence Precipitate porphyria Endometrial hyperplasia and cancer Breast tenderness
Give the mode of action of the progesterone only pill
Adverse effect on cervical mucous
Adverse effect on endometrium
Give some adverse effects of the POP
Acne Depression, PMS, lack of concentration Weight gain Nausea Irritability
Describe the action of the combined oral contraceptive pill
Suppression of ovulation
Inhibition of FSH and LH
Adverse effect on cervical mucous
Adverse effect on endometrium
Define an atheroma
Infiltration of LDLs into the tunica intima of an artery.
Give some effects of oxidated LDL
Macrophage motility inhibition
T cell activation
Endothelial cell toxicity
Enhanced platelet aggregation
Give some classes of lipid-lowering drugs
Statins Fibrates Nicotinic acids Plant sterols Cholesterol lipase inhibitors Resins Omega-3 fatty acids
Name a statin
Simvastatin
Give the mechanism of action of statins
Inhibits cholesterol synthesis in hepatocytes
Increased clearance of IDL and LDL
Decreased formation of VLDL and LDL
Give some indications for statin therapy
CVS risk prevention
Familial hypercholesterolaemia
Give some adverse drug reactions for statins
Increased transaminase
Myopathy
General: arthralgia, GI upset, headache
What is the mechanism of action of fibric acid derivatives?
PPARα agonist
Increases activity of lipoprotein lipase
Greatly reduces triglyceride production
Variable reduction in LDLs
Give some side effects of fibric acids
GI upset
Cholelithiasis
Myositis
Abnormal LFTs
Give some contraindications for fibric acid derivatives
Gallbladder disease
Renal dysfunction
Hepatic dysfunction
Statin use
What are the actions of nicotinic acids?
Decreases VLDL
Increases HDL (especially HDL-C
Inhibits lipoprotein A synthesis
Give some side effects of nicotinic acid
Flushing Itching Headache GI upset Hepatotoxicity Peptic ulcer activation Hyperglycaemia and decreased insulin sensitivity
Give some contraindications of nicotinic acid
Active liver disease
Unexplained LFT elevation
Peptic ulcer disease
Give the mechanism of action of ezetimibe
Selective inhibition of intestinal cholesterol absorption
Therefore:
-Decreased intestinal delivery of cholesterol to the liver
-Increased expression of hepatic LDL receptors
-Decreased cholesterol content of atherogenic particles
Give and explain some side effects of ezetimibe
Headache
Abdominal pain
Diarrhoea
These are mostly GI ADRs because ezetimibe circulates enterohepatically so systemic exposure is limited
What needs to be considered when prescribing fibric acid derivatives and statins?
Increased incidence of rhabdomyolysis and myopathy with concomitant use
Benefits vs risk analysis
Mostly gemfibrozil responsible for this effect
Statins plus fibric acid derivatives highly effective in lowering TGCs, LDLs and VLDL levels whilst increasing HDL
Give some examples of dietary supplements that have a positive effect on lipid profile
Fish oils Fibre Plant sterols Vitamin C and E Alcohol (on HDL)
Give some dietary factors which have a negative effect on lipid profile
High fat/cholesterol diet
Alcohol (on TGs)
