Term
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Definition
Class: lipid-lowering
Mechanism: blocks synthesis of tryglyceride and processing into VLDL; blocks HDL catabolism
Indications: reduces major coronary events, possible reduction in total mortality, reduces TGs (25-30%) and LDL (10-25%), raises HDL (15-40%)
Contraindications: liver disease, severe gout, peptic ulcer
Drug interactions: NSAIDs 30 minutes before can reduce facial flushing
Adverse effects: ulcers; facial flushing, dyspepsia, pruritis, hyperglycemia, hyperuricemia, N, V, D, myopathy, HA, hepatotoxicity, orthostatic hypotension, impaired insulin sensivity
Absorption: 1.5-6.0g, near complete, 30-60minutes, 2-3xdaily
Half-life: ~60min, |
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Term
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Definition
Class: lipid-lowering, statin
Mechanism: competitively inhibits HMG-CoA; reduce LDL (increase uptake), reduce LDL susceptibility to oxidation, reduces cholesterol synthesis
Indications: Reduce incidence of recurrent MIs and total mortality by reducing LDL levels
Contraindications: hepatotoxicity, pregnancy, nursing
Drug interactions: P4503A4 metabolized drugs will increase this drug level, OATP2 inhibitors (gemfibrozil) will increase this drug level
Adverse effects: RHABDOMYOLYSIS, HEPATOTOXICITY, neuropathy, mild GI symptoms, HA, rash, muscle cramps, insomnia
Administration: take with meal in evening
Absorption: 30-80%, high first pass, F = 5-30%
Distribution: >95% ppb
Metabolism: P450 3A4 and 2C9, take up by OATP2
Elimination: 70% liver |
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Term
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Definition
Class: lipid-lowering, statin
Mechanism: competitively inhibits HMG-CoA; reduce LDL (increase uptake), reduce LDL susceptibility to oxidation, reduces cholesterol synthesis
Indications: Reduce incidence of recurrent MIs and total mortality by reducing LDL levels
Contraindications: hepatotoxicity, pregnancy, nursing
Drug interactions: P4503A4 metabolized drugs will increase this drug level, OATP2 inhibitors (gemfibrozil) will increase this drug level
Adverse effects: RHABDOMYOLYSIS, HEPATOTOXICITY, neuropathy, mild GI symptoms, HA, rash, muscle cramps, insomnia
Administration: take w/ or w/o food at any time of day
Absorption: 30-80%, high first pass, F = 5-30%
Distribution: >95% ppb
Metabolism: P450 3A4 and 2C9, take up by OATP2
Elimination: 70% liver |
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Term
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Definition
Class: lipid-lowering, statin
Mechanism: competitively inhibits HMG-CoA; reduce LDL (increase uptake), reduce LDL susceptibility to oxidation, reduces cholesterol synthesis
Indications: Reduce incidence of recurrent MIs and total mortality by reducing LDL levels
Contraindications: hepatotoxicity, pregnancy, nursing
Drug interactions: P4503A4 metabolized drugs will increase this drug level, OATP2 inhibitors (gemfibrozil) will increase this drug level
Adverse effects: RHABDOMYOLYSIS, HEPATOTOXICITY, neuropathy, mild GI symptoms, HA, rash, muscle cramps, insomnia
Administration: w/ or w/o food, any time of day
Absorption: 30-80%, high first pass, F = 5-30%
Distribution: >95% ppb
Metabolism: P450 3A4 and 2C9, take up by OATP2
Elimination: 70% liver |
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Term
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Definition
Class: lipid-lowering, bile acid resin
Mechanism: cationic polymer, binds anionic bile acids in intestinal lumen, cannot be absorbed and is excreted into stool; REDUCE LDL 10-20%, RAISE HDL 3-5%
Indication: reduce major coronary events, reduce coronary heart disease mortality
Contraindication: hypertriglyceridemia (high TG w/o high LDL)
Adverse effects: increase TG, GI distress (constipation, bloating), decrease absorption of other drugs
Administration: take w/ large amount of fluid, take other drugs 1hr before or 4hr after |
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Term
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Definition
Class: lipid-lowering, bile acid resin
Mechanism: cationic polymer, binds anionic bile acids in intestinal lumen, cannot be absorbed and is excreted into stool; REDUCE LDL 10-20%, RAISE HDL 3-5%
Indication: reduce major coronary events, reduce coronary heart disease mortality
Contraindication: hypertriglyceridemia (high TG w/o high LDL)
Adverse effects: increase TG, GI distress (constipation, bloating), decrease absorption of other drugs
Administration: take w/ large amount of fluid, take other drugs 1hr before or 4hr after |
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Term
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Definition
Class: lipid-lowering, fibrate
Mechanism: inc. FA oxidation in muscle and liver and lipogenesis in liver; lower TGs (20-50%), raise HDL (0-10%), lower LDL (5-20%)
Indications: reduce major coronary events, reduce coronary heart disease mortality
Adverse effects: myalgia, rhabdomyolysis, increased gallstones, increased transaminases, GI distress
Absorption: >90%
Peak conc: 1-4hrs
Distribution: >95% ppb
T1/2: 1.1 hr |
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Term
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Definition
Class: lipid-lowering, fibrate
Mechanism: inc. FA oxidation in muscle and liver and lipogenesis in liver; lower TGs (20-50%), raise HDL (0-10%), lower LDL (5-20%)
Indications: reduce major coronary events, reduce coronary heart disease mortality
Adverse effects: myalgia, rhabdomyolysis, increased gallstones, increased transaminases, GI distress
Absorption: >90%
Peak conc: 1-4hrs
Distribution: >95% ppb
T1/2: 20hr |
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Term
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Definition
Class: lipid-lowering
Mechanism: inhibits cholesterol absorption in intestines (block NPC1L1 in jejunum), reduce by 55%; REDUCES LDL BY 18%
Indications: reduce major coronary events, reduce coronary heart disease mortality
Adverse effects: fatigue, GI (D, abdominal pain), rhabdomyolysis RARE |
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Term
| safe combinations of lipid-lowering drugs |
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Definition
statin + bile resin
statin + cholesterol absorption inhibitor
niacin + bile acid resin |
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