Pharmacy Care Application for antihyperlipidemic and diuretic drugs Flashcards
(32 cards)
Antihyperlipidemics
Used in a wide variety of disease states:
- Cerebrovascular Disease (CVD)
- Coronary Heart Disease (CHD)
- Atherosclerotic Cardiovascular
- Disease (ASCVD)
- Acute Myocardial Infarction (AMI)
- Angina
- Stroke
- Diabetes
STATIN
Chemical Nomenclature
Statins derive their name from molds or fungi
Available statins:
- A bunch with statin in their name (Rosuvastatin: most common)
STATIN
Pharmacological Nomenclature
3-hydroxyl-3-methylglutaryl/Coenzyme A Reductase inhibitor (HMG CoA Reductase Inhibitors)
- HMG CoA reductase is the rate limiting enzyme in cholesterol synthesis
- By inhibiting this enzyme => compensatory increase in LDL receptors => stimulates LDL catabolism
- Additionally, they possess a pleiotropic effect
– Decreases inflammation at site of coronary plaque, inhibits platelet aggregation, and anticoagulant effects
Cholesterol Reduction
Lowers low-density lipoproteins (LDL )
- Low-density lipoproteins (LDL) are referred to
as bad cholesterol
Lowers triglycerides (TG)
- Triglycerides (TG) are the main constituents of
body fat
Raises High-density lipoproteins (HDL)
- High-density lipoproteins (HDL) are referred
to as good cholesterol
Long term benefits
STATIN
Targeting hypercholesterolemia
- Reduced risk of CHD
- Reduced risk of atherosclerosis, stenosis, strokes and MI: “Pleiotropic effect”
- Reduction of LDL-C
- Improvement of HDL-C
Statins with healthy lifestyle help patients regardless of cholesterol counts!
It is recommended patient stay on statins with co-morbid conditions if have ASCVD risk factors regardless of cholesterol levels
STATIN
Therapeutic uses
Antihyperlipidemic drugs are used in a wide variety of disease states for primary & secondary prevention:
- Hypercholesterolemia
- Hypertriglyceridemia
- Cerebrovascular Disease (CVD)
- Coronary Heart Disease (CHD)
- Atherosclerotic Cardiovascular Disease (ASCVD)
- Acute Myocardial Infarction (AMI)
- Angina
- Stroke
- Diabetes
STATIN
Adverse reactions, dosing and monitoring
Adverse drug reactions:
- Diarrhea
- Arthralgia
- Nasopharyngitis
- Insomnia
- Malaise
- Increased hepatic function tests
Dosing/Monitoring
- Pregnancy category X
- Statin should be administered before bedtime (except: Atorvastatin and Rosuvastatin (more side eff)
- Many interact with grapefruit
- Simvastatin can only be used at certain doses when used concurrently with CCBs
Individual STATIN compounds
SimvaSTATIN (Zocor®)
PravaSTATIN (Pravachol®)
FluvaSTATIN (Lescol®)
AtorvaSTATIN (Lipitor®)
LovaSTATIN (Mevacor®)
RosuvaSTATIN (Crestor®)
PitaSTATIN (Livalo®, Zipitamag®)
Combination STATIN products
Advicor® - lovastatin + niacin ER
Simcor® - simvastatin + niacin ER
Vytorin® - simvastatin + ezetimibe (most common)
CHOLES
Chemical Nomenclature
All contain the prefix “Choles-”
Available on the market:
- Cholestyramine (Questran®)
- Cholestipol (Colestid®)
- Cholesevelam (Welchol®)
There is no combination products and all come in powder packets
CHOLES
Pharmacological Nomenclature
Bile acid sequestering agent
Mechanism of action: Forms a non-absorbable complex with bile acids and releases chloride ions in the process
- Inhibits reuptake of intestinal bile salts and increases fecal loss of LDL-C
Mainly decreases LDL-C, with lesser effect on other cholesterol
CHOLES
Therapeutic uses
FDA approved:
- Dyslipidemia
Off-label: Main use
- Chronic diarrhea due to bile acid malabsorption
- Hyperthyroidism
- Pruritus associated with cholestasis
CHOLES
Adverse reactions, dosing and monitoring
Adverse reactions:
- Abdominal pain
- Constipation
- Flatulence
- Abnormal hepatic function tests
- Myalgias
- Osteoporosis
Interactions/monitoring
- Warfarin – monitor for decreased INR
- Statins/fibrates – monitor for increased incidence of myalgias
- Amiodarone– may decrease availability/effectiveness of amiodarone
Fibrate
Chemical Nomenclature
All contain “–fibr-”
Available on the market:
- Gemfibrozil (Lopid®)
- Fenofibrate (TriCor®)
- Fenofibric Acid (Trilipix®)
Fibrate
Pharmacological Nomenclature
Fibric acid derivatives
MOF: Exact mechanism is unknown: In theory, inhibits lipolysis and decreases hepatic fatty reuptake as well as inhibit secretion of VLDL
Very good triglyceride lowering agents: Also decrease LDL and increase HDL
Fibrate
Therapeutic Use
FDA approved:
- Hypertriglyceridemia
- Hypercholesterolemia
Off-label:
- Primary biliary cholangitis
Fibrate -
Adverse reactions, dosing and monitoring
Adverse reactions:
- Increased serum transaminases
- Abdominal pain
- Abnormal hepatic function tests
- Myalgias
Interactions/monitoring:
- All can increase incidence of myalgias when combined with statins
- Gemfibrozil has several drug-drug interaction that
are contraindications
– All statins, ezetimibe, any CYP2C8 substrates (many
antiretrovirals): Also use with caution in patient on warfarin
OCUMABS
PCSK-9 inhibitors
- Mechanism of action: Human monoclonal antibodies that aid in clearance of LDL (lower LDL primarily)
Counseling points: Rotate injection sites, injections are given in the thigh, belly, or upper arm
Two agents available:
- Alirocumab (Praluent®) – 75mg/mL, 150 mg/mLpen injectors
- Evolocumab (Repatha®) – 140 mg/mL syringe
Relatively newer medications and place in
therapy in not completely known currently
Miscellaneous antihyperlipidemics
Niacin (nicotinic acid, Vitamin B3)
MOF: Not fully understood, potentially related to
inhibition of release of free fatty acids from adipose tissue
Adverse reactions: flushing, pruritus, GI distress, vomiting, diarrhea, hepatotoxicity
Clinical pearls: Different products of niacin are not
interchangeable
Increases HDL while lowering LDL and TG
Miscellaneous antihyperlipidemics
Omega-3 polyunsaturated Fatty acids
MOF: Reduction in hepatic production of TG-rich very low-density lipoproteins + reduction in hepatic synthesis of TG
Adverse reactions: Diarrhea, nausea, fishy burps
Available products:
- Lovaza® – high grade fish oil
- Vascepa® – Icosapent Ethyl
Clinical Pearls: Primarily used in hypertriglyceridemia secondary to its effect lowering of TG after other 1st line options
Ezetimibe (Zetia®)
MOA: cholesterol absorption inhibitor at the brush border of the small intestine
Adverse reactions: Diarrhea, arthralgia, fatigue, increased serum transaminases
Clinical pearls:
- Generally used as adjunctive therapy with statins
or in addition to dietary changes
- Works primarily lowering LDL but also slightly
lowers TG and raises HDL
Bempedoic Acid (Nexletol®)
Mechanism of action: adenosine triphosphate- citrate lyase (ACL) inhibitor which lower LDL by inhibiting synthesis in the liver
- Enzyme upstream of HMG CoA reductase
Adverse reactions: abdominal pain, arthralgias,
gout, increased serum transaminases
Clinical pearls:
- Generally used as adjunctive therapy with statins or in addition to dietary changes
- Works primarily lowering LDL
- Also available in a combo product with ezetimibe
(Nexlizet®)
- Marketed as the alternative for patients with statin
induced myalgias
Inclisarin (Leqvio®)
Mechanism of action: Utilizes the RNA interference mechanism and directs catalytic breakdown of mRNA for PCSK-9
- Increase LDL receptor recycling and uptake
Adverse reactions: antibody development, injection site reactions, arthralgias, bronchitis
Clinical pearls:
- Generally used as adjunctive therapy with statins
or in addition to dietary changes
- Works primarily lowering LDL
- Works through patient’s medical insurance instead
of Rx insurance
New to the market in 12/2021
PIB
Not currently on the market for use
Potentially promising category of drugs
- Mechanism: inhibits cholesterol ester transfer protein resulting in increases in HDL and decreasing LDL
Currently in the pipeline:
- Torcetrabpib
- Anacetrapib
- Evacetrapib
