Hmg-Coa Reductase Inhibitors

Front 1

1) TC dec = 15-35%
2) LDL dec = 20-40%
3) HDL inc = 2-15%
4) TG dec = 7-25%

Back 1

LFT monitoring
1) Atorv = inital and elevation, 6 weeks, 12 weeks, semiannually
2) fluv = inital and evlevation, 6, 12, semiannually
3) lov = inital and elevation, 6, 12, semiannually
4) prav = inital and elevation, 12
5) simv = inital and elevation, semiannually

Comparative doses
1) atorv 10 mg
2) fluv 20 mg (recomm by man but < effective than others)
3) lov 20 mg
4) prav 20 mg
5) 10 mg

Front 2

1) Pravachol: pravastatin
2) Primary prevention; secondary prevention; dec total choles, LDL, apo-B, and TG and inc HDL
3) Preg: X
4) CI: hyperS; active liver dz; persistent unexplained inc LFTs; preg/lactation
5) Warn: may elavate LFTs (baseline and Q4-6 weeks during 1st 12-15 months and periodically therafter); myalgia and rhabdo; caution in pts consume large amts of EtOH
6) AI: HA; N/V; diarrhea; increased transams;
7) SAR: myalgia, neuropathy; weakness

Back 2

8) DI: CYP2C9; antacids = mag-alum-hydroxide (dec conc but no alterd efficacy); cholestyramine (separate admin by 4 hours--dec prav abs); clofibrate, gemfibrozol, niacin and fenofibrate may inc risk of rhabdo; colestipol (dec prav abs)
9) MOA: HMG-CoA reductase inhib
10) PK/PD: poor abs (17% BA); metab in liver (at least 2 metabs); t1/2 = ~2-3 hours; time to peak = 1-1.5 hours; up to 20% excreted in urine (8%) unchg
10) Dosage: 10-40 mg QD; renal = 10 mg QD
11) Dosge forms (as sodium): 10, 20, 40 mg
12) Monitor: CPK, LFTs, choles
13) Patient info: promptly report unexplained muscle pain, tenderness, or weakness, esp if accom by malaise or fever

Front 3

1) Lipitor: Atorvastatin
2)Indication: reduction of elevated total and LDL cholesterol levels and to incrase HDL-C in patients with hypercholesterolemia; to reduce risk of MI in patients with heart dz;
3) Pregnancy category X
4) CI: hyperS; active liver dz; preg/lactation
5)Warn: rhabdo; LFTs prior to and at 12 weeks following initation and change, periodically thereafter
6)AR: HA, Chest pain, peripheral edema, arthralgia, myalgia, sinusitis, infection
7) SAR: elevated LFTs, pneumonia, gastroenteritis, xerostomia, postural hypotension, hyperglycemia, nephritis, tinitis

Back 3

8)DI: CYP3A3/4 substrate; Increased toxicity: gemfibrozil (rhabdo), clofibrate, niacin, erythromycin (rhabdo), cyclosporine, oral anticoags; Protease inhibitors (increase lip levels): amprenavir, nelfinavir, ritonavir; levothyroxine (inc levo tox); antacids (dec lip levels c mag-alum-hyroxide antacids)
9) MOA: HMG-CoA reductase inhib--dec production of mevalonic acid) results in compensatory LDL receptor expression on hepatocyte membranes and stimulation of LDL catbolism
10) PK/PD: rapid abs; 98% bound; t1/2 = 14 hours; tim to peak = 1-2 hours (max reduc = 2 weeks); 2% unchang in urine
11) Dosage: 10 mg QD, titrate up to 80 mg QD; no adj in renal, dec dose with severe liver dz
12) Dosage forms: 10, 20, 40 mg
13) monitor: lipid levels = 2 weeks; LFTs, CPK
14) Pt info: may take with food and regardless of time of day

Front 4

1) Lescol: fluvastatin
2) intervention in pts at risk for atherosclerosis vascular dz; dec TC, LDL, TG, and apo-B; inc HDL
3) Preg: X
4) CI: preg/lactation, myopathy, inc CPK
5) Warn: r/o 2nd causes of hyperlipid; LFTs monitor periodically; rhabdo; tem d/c experinceing renal failure due to rhabdo; not for <18 years
6) AR: URI; HA; dyspepsia; diarrhea; abdominal pain; back pain/myalgia; cold/flu symptoms

Back 4

7) DI: CYP; cimetidine, colestipol, ranitidine, omeprazole (inc fluv conc); clofibrate, fenofibrate, gemfibrozil (rhabdo)--separate by 2 hours; diclofenac (inc dic levels); dig (inc dig levels); glyburide, phenytoin (inc both), rifampin (dec fluv levels); warfarin (inc warf effect); St. John's Wort
8) protect from light
9) MOA: HMG-CoA
10) PK/PD: >98% bound; extensive 1st pass metab; Absolute BA = 24%; tmax = </= 1 hour; t1/2 = 1.2 hours; urine 5%; feces 90%
11) Dosage: <25% dec = 20 mg QD; >/= 25% dec = 40 mg or 80 mg XL QPM (may use 40 mg BID); range 20-80 mg QD; max response 4-6 weeks; no adj mild/mod renal; no adj elderly; s regard to meals
12) Dosage forms: 20, 40 mg; 80 mg XL
13) Monitor: baseline LFTs and Choles; repeat at 12 weeks after initiation and increase and periodically thereafter; LDL >/= 4 weeks; CPK when muscle pain; interacts with thyroid fxn tests

Front 5

1) Simvastatin: Zocor
2) Indication: Secondary preven c coronary heart dz and hypercholesterolemia to dec risk of total mortality; dec risk of nonfatal MI; dec risk of myocard revascularization proced; dec risk of strok or TIA; dec elevated serum total and LDL, apo-B, and TG and inc HDL
3) Preg: X
4) hyperS to other HMG-CoA red inhib; active liver dz; unexplained inc of serum transams; preg/lactation
5) AR: HA; myalgia; weakness; increase CPK; URI; abnormal taste; blurred vision; lenticular opacities
6)DI: CYP3A3/4 substrate; CYP3A3/4 inhib (amprenavir, clarithro, cyclo; danazol, diltiazem, fluvoxamine, erythormycin, fluconazole, indinavir, itraconazole, ketoconazole, miconazole, nefazodone, nelfinavir, ritonavir, saquinavir, troleandomycin, verapamil);

Back 5

Warfarin and Dig (may increase their effect); clofibrate, fenofibrate, gemfibrozil, cyclosporine and niacin (rhabdo); rifampin, nicotinic acid, isradipine (dec sim efficacy); antacids
7) MOA: HMG-CoA reductase inhib
8) PK/PD: 85% abs (<5% reaches circ due to 1st pass effect); time to peak = 1.3-2.4 hours; 95% bound; 12% excreted in urine/60% in feces; t1/2 = unkn c severe renal dz;
9) Dosage: 20 mg QPM (start at 10 with mod reduc and 40 >45% reduc); Maint = 5-80 mg QPM; Adj at >/= 4 weeks; homozygous fam hyperchol = 40 mg QPM or 80 mg (20, 20 and 40 PM); elderly = </= 20 mg; cyclosporine = 5 mg (max = 10); fibrates/niacin = max 10; renal = SCR <10 mL/min = 5 mg QPM.
10) Dosage forms: 5, 10, 20, 40, 80 mg
11) Monitor: CPK, Cholest, LFTs
12) Patient info: report unexplained muscle pain, tenderness, or weakeness esp if accom by malaise or fever; follow diet; take with meals

Front 6

1) Mevacor: lovastatin
2) dec total, LDL in hypercholes
3) Preg: X
4) CI: preg; active liver dz; hyperS
5) Warn: may inc LFTs (perform baseline and Q4-6 weeks during 1st 12-15 months and periodically thereafter); myalgia and rhabdo; caution c consume large amts EtOH/ h/o liver dz
6) AR: Inc CPK > 2x nomral; acid regurg; insomnia; leg pain; paresthesia; xerostomia

Back 6

7) CYP3A3/4; inhibitors (amprenavir, clarithro, cyclosporine, danazol, diltiazem, fluvoxamine, erytho, fluconazole, indinavir, itraconazole, ketoconazole, miconazole, nefazodone, nelfinavir, ritonavir, saquinavir, troleandomycin, verapmail)--inc lov levels; antacids (mg-al-hydroxide) may dec lov levels; cholestyramine (separate by 4 hours); clofibrate, fenofibrate, gemfivrozil, niacin (inc risk rhabdo); isradipine (dec lov levels); warfarin (inc warf effect); Grapefruit juice; admin with meals
8) Dosage forms: 10, 20, 40 mg
9) MOA: HMG-CoA reductase inhib
10) PK/PD: onset of effect = 3 days; 30% abs; 95% bound; t1/2 1.1-1.7; peak conc = 2-4 hours; 80-85% in feces and 10% in urine
11) Dosage: initial = 20 mg QPM c meal; adj at 4 week intervals; max dose = 80 mg QPM with meal;
12) Monitor: TG, Choles; LFTs; interact with thyroid fxn tsts
13) Pt info: report any muscle pain, tenderness, or wakness esp if accompanied by malaise or fever; don't interupt, inc or dec dose with out advice of MD; take with meals