Quiz 2 Antihyperlipidemics and Antidiabetics Flashcards
Atorvastatin Brand Name
Lipitor
Atorvastatin Class
HMG-CoA Reductace Inhibitor
Atorvastatin Indication
- Hyperlipidemia
- Primary and secondary prevention of atherosclerotic cardiovascular disease
- Secondary prevention of cardiovascular events in patients with or at high risk for CAD
- Familial hypercholesterolemia (homozygous)
Atorvastatin MoA
HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol also can decrease because of decreased production of VLDL-cholesterol or increased VLDL; removal by LDL receptors.
CLARIFICATION OF WHAT THIS MEANS JUST TO UNDERSTAND THE MECHANISM DEEPER WHATS BELOW WILL EXPLAIN WHAT UP THERE MEANS:
Competitively inhibits the conversion of HMG-CoA to mevalonate
Compensatory increase in low density lipoprotein (LDL) receptors which bind and break down circulating LDL cholesterol and VLDL
Note: LDL and VLDL are both bad cholesterol in liver cells – hepatocytes
Ultimately there is less cholesterol. The LDL is turned into bile, excreted, and recycled.
Note: VLDL is turned into LDL
LDL= Low density lipoprotein
VLDL = Very low density lipoprotein
The reduced intracellular concentrations of cholesterol in hepatocytes secondary to statin use activate the proteases that cleave membrane-bound sterol regulatory element-binding proteins (SREBP), which further migrate to the nucleus and bind to sterol response elements. This binding results in increased transcription of the LDL receptor, which translocates to the liver cell membrane. The LDL and VLDL particles in plasma bind to the LDL receptors and endocytose in hepatocytes, where their cholesterol component gets processed into bile salts, which are then excreted or recycled. This process increases the catabolism of LDL and VLDL cholesterol and results in further reduction of plasma cholesterol concentrations.[3]
Statins reduce the plasma concentrations of total cholesterol, LDL-C, VLDL-C, triglycerides, apo-B, and increase the plasma concentrations of HDL-C.
Atorvastatin Pregnancy Category
Pregnancy - contraindicated first trimester, and contraindicated for breastfeeding.
Atorvastatin Contraindication
Hypersensitivity to atorvastatin, use in breastfeeding, active liver disease, unexplained persistent elevations of serum transaminases
Atorvastatin Black Box Warning
N/A
Atorvastatin Counseling points
Avoid excessive alcohol, grapefruit, and grapefruit juice (>1 L/d) consumption while taking drug. Atorvastatin does not take the place of lifestyle changes (diet, exercise) to lower cholesterol levels. Notify prescriber if unexplained muscle tenderness or weakness occurs.
Pravastatin Brand Name
Pravachol
Pravastatin Class
HMG-CoA Reductace Inhibitor
Pravastatin Indications
Cerebrovascular accident (prevention)
Familial hypercholesterolemia
Hyperlipidemia
Pravastatin MoA
HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol decreases because of decreased production of VLDL-cholesterol or increased VLDL removal by LDL receptors.
CLARIFICATION OF WHAT THIS MEANS JUST TO UNDERSTAND THE MECHANISM DEEPER WHATS BELOW WILL EXPLAIN WHAT UP THERE MEANS:
Competitively inhibits the conversion of HMG-CoA to mevalonate
Compensatory increase in low density lipoprotein (LDL) receptors which bind and break down circulating LDL cholesterol and VLDL
Note: LDL and VLDL are both bad cholesterol in liver cells – hepatocytes
Ultimately there is less cholesterol. The LDL is turned into bile, excreted, and recycled.
Note: VLDL is turned into LDL
LDL= Low density lipoprotein
VLDL = Very low density lipoprotein
The reduced intracellular concentrations of cholesterol in hepatocytes secondary to statin use activate the proteases that cleave membrane-bound sterol regulatory element-binding proteins (SREBP), which further migrate to the nucleus and bind to sterol response elements. This binding results in increased transcription of the LDL receptor, which translocates to the liver cell membrane. The LDL and VLDL particles in plasma bind to the LDL receptors and endocytose in hepatocytes, where their cholesterol component gets processed into bile salts, which are then excreted or recycled. This process increases the catabolism of LDL and VLDL cholesterol and results in further reduction of plasma cholesterol concentrations.[3]
Statins reduce the plasma concentrations of total cholesterol, LDL-C, VLDL-C, triglycerides, apo-B, and increase the plasma concentrations of HDL-C.
Pravastatin Pregnancy Category
Contraindicated - first trimester
Pravastatin Contraindications
Hypersensitivity to pravastatin, do not use in breastfeeding
Pravastatin Black Box Warning
N/A
Pravastatin Counseling Points
Take in the evening. Avoid concurrent heavy alcohol use. Pravastatin does not take the place of diet and exercise to lower cholesterol levels.
Ezetimibe Brand Name
Zetia
Ezetimibe Class
Antihyperlipidemic, Cholesterol Absorption Inhibitor
Ezetimibe Indications
- Familial hypercholesterolemia-homozygous, with atorvastatin or simvastatin
- Mixed hyperlipidemia
- Primary hypercholesterolemia
Ezetimibe MoA
Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins and of fenofibrate.
Ezetimibe Pregnancy
Pregnancy - limited human data.
Contraindicated breastfeeding
Ezetimibe Contraindication
Hypersensitivity to ezetimibe, gallbladder disease, severe hepatic dysfunction, concurrent use with a statin in a pregnant or nursing mother
Ezetimibe Black Box Warning
N/A
Ezetimibe Counseling Points
Take with or without food and may be taken at the same time as a concurrent statin. In patients receiving a bile acid sequestrant concurrently, ezetimibe should be taken at least 2 h before or 4 h after the bile acid sequestrant is taken.
https://www.verywellhealth.com/what-are-bile-acid-sequestrants-697489
Fenofibrate Brand Name
Antara
Fenofibrate Class
Antihyperlipidemic
Fenofibrate Indication
- Hypercholesterolemia
- Hypertriglyceridemia
Fenofibrate MoA
Fibric acid derivatives activate peroxisome proliferator-activated receptor α (PPARα), which increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity). The resulting fall in triglycerides produces an alteration in the size and composition of LDL from small, dense particles to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly.
Fenofibrate Pregnancy Category
Pregnancy - limited human data
breastfeeding - no human data - potential toxicity
Fenofibrate Contraindication
Hypersensitivity, gallbladder disease, severe renal or hepatic dysfunction, nursing mothers
Fenofibrate Blackbox warning
N/A
Fenofibrate Counseling Points
Fenoglide tablets and Lipofen R capsules should be given with food; others can be taken without food. Take 1 h before or 4-6 h after a bile acid binding resin. Products are not interchangeable. Do not use if you have severe kidney disease or liver disease.
Lovastatin Brand Name
Altoprev
Lovastatin Class
HMG-CoA Reductace Inhibitor
Lovastatin Indications
- Coronary arteriosclerosis, hypercholesterolemia, primary andmixed
- familial hypercholesterolemia, heterozygous
Lovastatin MoA
HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol decreases because of decreased production of VLDL-cholesterol or increased VLDL removal by LDL receptors.
Lovastatin Pregnancy Category
Contraindicated - first trimester
Lovastatin Contraindication
Hypersensitivy to lovastatin, active liver disease, use in breastfeeding, concomitant use with strong CYP3A4/5 inhibitors, and unexplained persistent elevation of liver enzymes
Lovastatin Blackbox
N/A
Lovastatin Counseling Point
Immediate-release tablets should be taken with the evening meal. Extended-release tablets should be taken at bedtime. Swallow extended-release tablets whole; do not chew, crush, or cut. Avoid alcohol, grapefruit, and grapefruit juice. Report signs/symptoms of rhabdomyolysis, jaundice (yellowing of skin or eyes), or renal failure. There are multiple significant drug-drug interactions with lovastatin. Consult a health-care professional prior to starting any new prescription or OTC medications. Lovastatin does not take the place of lifestyle changes (diet, exercise) to lower cholesterol levels
Rosuvastatin Brand Name
Crestor
Rosuvastatin Class
HMG-CoA Reductace Inhibitor
Rosuvastatin Indication
- Hyperlipidemia
- Disorder of cardiovascular system, primary prophylaxis, familial hypercholesterolemia, homozygous, hypertriglyceridemia, mixed dyslipidemia
Rosuvastatin MoA
HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol can also decrease because of decreased production of VLDL-cholesterol or increased VLDL removal by LDL receptors.
Rosuvastatin Pregnancy Category
Contraindicated - first trimester
Rosuvastatin Contraindication
Hypersensitivity of rosuvastatin, active liver disease, use in breastfeeding
Rosuvastatin Blackbox Warning
N/A
Rosuvastatin Counseling Points
Do not drink alcohol. Rosuvastatin does not take the place of diet and exercise to lower cholesterol levels.
Simvastatin Brand Name
Zocor
Simvastatin Class
HMG-CoA Reductace Inhibitor
Simvastatin Indication
- Hyperlipidemia
- Primary and secondary preventions of atherosclerotic cardiovascular disease
- Secondary prevention of cardiovascular events
- Familial hypercholesterolemia (homozygous)
Simvastatin MoA
HMG-CoA reductase inhibitors competitively inhibit conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis. A compensatory increase in LDL receptors, which bind and remove circulating LDL-cholesterol, results. Production of LDL-cholesterol also can decrease because of decreased production of VLDL-cholesterol or increased VLDL removal by LDL receptors.
Simvastatin Pregnancy Category
Contraindicated - first trimester
Simvastatin Contraindication
hypersensitivity of simvastatin, active liver disease, use in breastfeeding
Simvastatin Blackbox Label
N/A
Simvastatin Counseling Points
Avoid excessive alcohol. There are multiple significant drug-drug interactions with simvastatin. Consult a health-care professional prior to starting any new medications, including OTC and herbal drugs. Simvastatin does not take the place of lifestyle changes (diet, exercise) to lower cholesterol levels.
Dulaglutide Brand Name
Trulicity
Dulaglutide Class
Antidiabetic Agent, Glucagon-like peptide-1 receptor agonist
Dulaglutide Indication
Diabetes mellitus, type 2
Dulaglutide MoA
Dulaglutide is an agonist of human glucagon-like peptide-1 (GLP-1) receptor and augments glucose-dependent insulin secretion and slows gastric emptying.
Dulaglutide Pregnancy Category
N/A
Dulaglutide Contraindication
Family history of medullary thyroid carcinoma, MEN2
Dulaglutide Black Box
Risk of thyroid cancers
Dulaglutide Counseling Points
Inject subcutaneously into the upper arm, thigh, or abdomen; use a different injection site each week. Administer once weekly on the same day each week, without regard to meals or time of day. Administration day can be changed as long as at least 3 d have passed. If using concomitantly with insulin, administer as separate injections (do not mix); may inject in the same body region as insulin, but do not administer both agents directly adjacent to one another. Keep refrigerated, but is stable at room temperature for 14 d. Be aware of symptoms of thyroid cancer (lump in neck, trouble breathing or swallowing) and kidney problems (decreased urination, blood in urine) and report to HCP.
Empagliflozin Brand Name
Jardiance
Empagliflozin Class
Sodium-glucose co-transporter 2 (SGLT2) inhibitors
Empagliflozin Indication
Diabetes Mellitus 2
Reduce risk of cardiovascular death in adult patients with Diabetes Mellitus 2 and established cardiovascular disease