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Drugs For Lipid Disorders 2023

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20 views17 pages

Drugs For Lipid Disorders 2023

Uploaded by

aguilarjanica
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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PHARMACOLOGY OF THE

CARDIOVASCULAR SYSTEM
DRUGS FOR LIPID DISORDERS Kirsten Culver,
PhD
Science Lead
BScN Program
LIPIDS
Three main types of lipid
1. Triglycerides
 Account for 90% of total lipids in the body
 Important source of energy (fuel in times of energy need)
2. Phospholipids
 Essential for the formation of plasma membranes
3. Steroids (e.g., cholesterol)
 Essential component of plasma membranes
 Building block for bile acids, vitamin D, cortisol, estrogen & testosterone
 Liver can synthesize cholesterol; no need for source from diet
LIPIDS
Lipoproteins
 Lipids are not soluble in plasma and require “special packaging” to be
distributed to body tissues
 Complex of triglycerides, cholesterol and phospholipids with a protein
carrier (apoprotein)
 3 major types of lipoproteins - characterized by composition, size and
density
 High-density lipoprotein (HDL)
 Low-density lipoprotein (LDL)
 Very low-density lipoprotein (VLDL)
LIPIDS
LDL
 Transports cholesterol from the liver to tissues; used to create
plasma membranes and other steroids; cholesterol can be
stored for later use
VLDL
 Primary carrier of triglycerides, converted/reduced into LDL
HDL
 Transports cholesterol from tissues back to the liver “reverse
cholesterol transport”
 Cholesterol eliminated from body via biliary excretion in feces
DYSLIPIDEMIA
 Increases the risk of
atherosclerosis and coronary
artery disease
 Occurs predominately in men
compared to non-menopausal
women
 After menopause (> 50 years
of age), risk becomes higher
in women

2021 Canadian Cardiovascular Society Guidelines for the Management of Dyslipidemia for the Prevention of
Cardiovascular Disease in the Adult Canadian Journal of Cardiology 37: 11129 – 1150
NON-PHARMACOLOGICAL
MANAGEMENT
Lifestyle factors play a significant role in the management and prevention lipid
disorders. These changes are also effective at reducing the risk of cardiovascular
disease, cancer, HTN and T2DM
 Smoking cessation
 Abstaining from alcohol or reducing alcohol intake to 2 drinks/day or less
 Maintain weight and waist circumference
 Regular exercise and stress reduction
 Reduce dietary saturated fat, trans-fats and cholesterol (Mediterranean diet)
 Cholesterol intake should not exceed 300mg/day
 Increase consumption of plant sterols/stanols & soluble fiber
 Sterols and stanols complete with cholesterol for absorption
 Nuts, olive oil, corn, rye, oats, rice and wheat
PHARMACOLOGICAL MANAGEMENT

Selective
cholesterol
absorption
inhibitors
2021 Canadian Cardiovascular Society Guidelines for the Management of
Dyslipidemia for the Prevention of Cardiovascular Disease in the Adult
Canadian Journal of Cardiology 37: 1129 – 1150
STATINS
Statins
 HMG-CoA Reductase Inhibitors (e.g., atorvastatin)
 First-line therapy in the treatment of lipid disorders
 Inhibits activity of HMG-CoA reductase, blocking cholesterol synthesis
 Increases the # of LDL receptors in the liver and stimulates removal of LDL
from the blood
 High efficacy
 Significant reduction in LDL, lower VLDL, increased HDL levels
 Slows progression of CAD & reduces CVD associated mortality
 Effects are reversible, may take up to a month to achieve
STATINS

Whalen, K. (2019). Lippincott’s Illustrated Reviews: Pharmacology. 7th ed. Figure


22.5
STATINS
Statins
 May be combined with other cholesterol lowering medications &
antihypertensive medications
 Contraindicated in people who are pregnant or may become pregnant;
contraceptive coverage recommended
 Therapy must be discontinued during pregnancy; treatment can be resumed
after breastfeeding is completed
 Some statins are more hydrophilic (pravastatin); should be considered in
people who may become pregnant
 Adverse effects: headache, heart burn, GI upset (take with evening meal)
STATINS
Statins
 Drug-Drug & Drug-Food interactions
 Clients should avoid alcohol & grapefruit juice
 Small but significant risk of rhabdomyolysis, especially in elderly clients
 Waste products cause acute renal failure, associated with significant
muscle pain
 Risk increased with higher doses or co-administration of drugs
(macrolides, antifungal agents) that inhibit CYP 450 enzymes or drugs that
increase the bioavailability of statin drugs (PPIs and H2RAs)
 Statins potentiate the effects of warfarin
 Longer duration of use associated with increased risk of new onset T2DM
SELECTIVE CHOLESTEROL
ABSORPTION INHIBITORS
Ezetimibe
 Inhibits intestinal cholesterol absorption; first line “add-on therapy”
 Blocks absorption by as much as 50%
 Can be used as monotherapy in clients with complete statin intolerance for
LDL lowering
 GI distress most common adverse effect
 Co-administered with statin therapy for clients that fail to reach their LDL
targets with statin therapy alone
 Reduces LDL levels ~20% in addition to statin
 Combination tablets available together as they act synergistically to inhibit
cholesterol absorption (ezetimibe) and cholesterol synthesis (statin)
PCSK9 INHIBITORS
PCSK9 inhibitors
 Evolocumab (Repatha) & alirocumab (Praluent)
 PCSK9 binds to LDL receptors on hepatocytes causing them to degrade
 Inhibitors are antibodies that bind to PCSK9, and inactivate it so that LDL
receptors are not degraded
 Lower LDL levels by 50 - 70% in addition to statin
 Inject subcutaneously every 2 weeks, or once a month
 Significant reduction in clinical outcomes (~50%) associated with
atherosclerotic cardiovascular disease
 Approved for use in clients whose LDL levels are above target despite
maximally-tolerated statin dosing; with or without Ezetimibe co-therapy
PCSK9 INHIBITORS
BILE ACID RESINS
Bile Acid Sequestrants
 Non-absorbed; bind to bile acids and impede enterohepatic circulation,
increasing the excretion of cholesterol (via the feces)
 Reduction in cholesterol levels induces the formation of additional LDL
receptors in the liver, increasing the rate at which LDL is removed from the
blood and promoting the conversion of cholesterol to bile acids
 Bile acid sequestrants ultimately reduce blood cholesterol levels and reduce risk
of major cardiovascular events
 ~20% drop in LDL cholesterol levels
 Additive effect when co-prescribed with statins; considered an alternative to
ezetimibe as an “add-on” to statin therapy
BILE ACID RESINS
Bile Acid Sequestrants (e.g., colesevelam)
 No systemic side effects, but often cause GI upset
 May induce abdominal pain, bloating, diarrhea, steatorrhea, constipation
 Can interfere with the absorption of other drugs
 Thiazide diuretics, warfarin, thyroid hormones, corticosteroids
 Take other medications 1 hour before, or 4 hours after
 May induce vitamin deficiency
 Vitamin A, D and E
 Vitamin K deficiency leads to increased bleeding times

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