HMG-CoA Reductase Inhibitors Flashcards
What class are the following drugs apart of: atorvastatin, simvastatin, lovastatin, rosuvastatin, and pravastatin?
HMG-CoA Reductase Inhibitor
What are the brand names for the following: atorvastatin lovastatin pravastatin rosuvastatin simvastatin
atorvastatin: lipitor
lovastatin: altoprev
pravastatin: pravoachol
rosuvastatin: crestor, ezallor
simvastatin: zocor
What is the mechanism of action of HMG-CoA Reductase Inhibitor?
HMG-CoA Reductase Inhibitors work by completely inhibiting the conversion of HMG-CoA to mevalonate, which is an early rate-limiting step in cholesterol synthesis. results in a compensatory increase in LDL receptors which binds and remove circulating LDL-cholesterol. ALSO production of LDL cholesterol can decrease because of the decreased production of VLDL-cholesterol along with removal of LDL receptors
Atorvastatin Dosage forms
Tablets; 10mg, 20mg, 40mg, and 80mg
Atorvastatin Indications
Hyperlipidemia (10-20mg qd but can increase to 80 mg qd)
Primary and secondary prevention of atherosclerotic cardiovascular disease (10-20 mg qd, may increase to 80mg qd for patients requiring high intensity therapy (LDL>190/high ASCVD risk)
Secondary Prevention of cardio events in pt w/ or @ high risk of CAD (80mg qd, may reduce to 40mg if high dose is not tolerated)
Familial hypercholesterolemia homozygous: children boys and girls (10-17) 10 mg qd (may take up to 40 mg qd ; adults 10-80 mg qd
atorvastatin contraindications
hypersensitivity to atorvastatin
use in breastfeeding
active liver disease
unexplained persistent elevation of serum transaminases
Atorvastatin ADR
Common: myopathy (muscle weakness), diarrhea, headache, nasopharyngitis
Less common: increased liver enymzes, indigestion, insomnia, musculoskeletal pain, myalgia, nausea, increased A1C
Serious: rhadbomyolysis, and tendon rupture
Efficacy Monitoring parameters for HMG-CoA Reductase Inhibitors
check total cholesterol, LDL cholesterol, and triglycerides levels as well as HDL cholesterol levels
With pravastatin, repeat 4–12 wks after initiation or dose adjustment
With simvastatin: obtain baseline fasting panel 4-12 wks after initiation and 3-12 months following
Atorvastatin Key counseling points
Avoid excessive alcohol, grapefruit, and grapefruit juice consumption
Healthy lifestyle changes including diet and exercise to lower levels
notify your provider if explained muscle tenderness or weakness occurs
Lovastatin dosage forms
tablet: 10mg, 20mg, 40mg
tablet ER: 20mg, 40mg, 60mg
Lovastatin Indications
coronary arteriosclerosis, hypercholesterolemia primary and mixed: initial 20mg qd, maintenance 10-80mg qd with evening meal (MAX 80mg/d); ER 20-60 po qhs
Familial hypercholesterolemia, heterozygous: children 10-17 initial 10 po daily, maintenance 10-40mg po qd (MAX 40mg/d)
Lovastatin contraindications
hypersensitivity to lovastatin
active liver disease
use in breastfeeding
concomitant use with strong CYPA4/5 inhibitors
unexplained persistent elevation of liver enymes
lovastatin ADR
common: none
less common: abdominal pain, constipation, diarrhea, headache, increased liver enzymes, myalgia, nausea, rash, hyperglycemia
serious: rhabdomyolysis, hepatotoxicity, increased risk of diabetes
Lovastatin Key counseling points
Immediate- release tablets should be taking in the evening with meals
ER should be taking at bedtime
Avoid grapefruit, grapefruit juice, and alcohol
Report signs of rhabdomyolysis, jaundice, or renal failure
Many drug interaction, so consult with provider for new rx and otc medications
lifestyle changes
Pravastatin dosage forms
tablet: 10mg, 20mg, 40mg, 80mg
Pravastatin indications
Cerebrovascular accident (prevention), coronary arteriosclerosis (primary or secondary prevention): 40 mg po daily
Familial hypercholesterolemia: Children 8-13 y of age, 20 mg po daily; Children 14-18 y of age, 40 mg po daily; Adults, 40 mg po daily, may titrate to 40-80 mg po daily
Hyperlipidemia: Children (boys and postmenarchal girls) 10-17 y of age, 10 mg po daily, may titrate to 20 mg/d; Adults, 40 mg po daily, may titrate to 40-80 mg po daily
Pravastatin contraindication
hypersensitivity to pravastatin
use in breastfeeding
Pravastatin ADR
common: none
Less common: Headache, heartburn, increased liver enzymes, influenza-like symptoms, musculoskeletal pain, myalgia, nausea, rash, vomiting
Serious: Rhabdomyolysis, tendon rupture
Pravastatin Key counseling point
Take in the evening
avoid with heavy alcohol use
health lifestyle changes
Rosuvastatin dosage form
tablet: 5mg, 10mg, 20mg, 40mg
Oral capsule, sprinkle: 5mg, 10mg, 20mg, 40mg
Rosuvastatin indication
Hyperlipidemia: Adults, 10-20 mg po daily, may titrate to 40 mg po daily; Children 10-17 y of age, 5-20 mg po daily, may titrate to 20 mg po daily
Disorder of cardiovascular system, primary prophylaxis, familial hypercholesterolemia, homozygous, hypertriglyceridemia, mixed dyslipidemia: 10-20 mg po daily, may titrate to 40 mg po daily
Rosuvastatin contraindication
hypersensitivity to rosuvastatin
use in breastfeeding
Rosuvastatin ADR
Common: Arthralgia (muscle pain and aches)
Less common: Abdominal pain, asthenia (lack of energy), constipation, diarrhea, indigestion, headache, increased liver enzymes, influenza-like symptoms, myalgia *muscle pain and aches), nasopharyngitis, nausea, pharyngitis, rhinitis
serious: Rhabdomyolysis, tendon rupture
Rosuvastatin key counseling points
Do not drink alcohol
healthy lifestyle changes such as diet and exercise
Simvastatin dosage forms
Tablet: 5mg, 10mg, 20mg, 40mg, 80mg
Oral suspension: 20mg/5mL and 40mg/5mL
Simvastatin indications
Hyperlipidemia: 20-40 mg po daily in the evening
Primary and secondary preventions of atherosclerotic cardiovascular disease: 20-40 mg po daily in the evening
Secondary prevention of cardiovascular events: 5-40 mg po daily in the evening
Familial hypercholesterolemia (homozygous): Children (boys and postmenarchal girls 10-17 y of age), 10 mg po daily, may titrate to 40 mg po daily in the evening; Adults, 20-40 mg po daily in the evening
Simvastatin contraindication
hypersensitivity to simvastatin
active liver disease
use in breastfeeding
Simvastatin ADR
Common: none
Less common: Abdominal pain, constipation, diarrhea, headache, increased liver enzymes, myalgia, nausea, rash
Serious: Rhabdomyolysis, myopathy, hepatotoxicity, tendon rupture, elevated HgA1c, immune-mediated necrotizing myopathy
Simvastatin Key counseling points
Avoid excessive alcohol
many drug interaction, so consult w/ provider before starting any new medications including otc and rx
Lifestyle changes including diet and exercise
initial max starting dose is 40mg (80 mg limited to pts that previously maintained for over 12 months
