This document discusses hypolipidemic agents used to treat high cholesterol and triglycerides. It begins by describing cholesterol and lipoproteins, then covers atherosclerosis and its causes. Various drug classes are explained in depth, including HMG-CoA reductase inhibitors (statins), bile acid sequestrants, fibrates, nicotinic acid, and ezetimibe. Combination drug therapies are also used. Statins are generally the preferred first-line treatment due to their ability to significantly lower LDL cholesterol levels. Special considerations include drug interactions and contraindications of the various hypolipidemic agents.
Hypolipidemic drug, also called lipid-lowering drug, any agent the reduces the level of lipids and lipoproteins (lipid-protein complexes) in the blood.
Hypolipidemic drug, also called lipid-lowering drug, any agent the reduces the level of lipids and lipoproteins (lipid-protein complexes) in the blood.
The bile salts such as cholic acid contain a hydrophobic side and a hydrophilic side, thus allowing bile salts to dissolve at an oil-water interface, with the hydrophobic surface in contact with the non-polar phase and the hydrophilic surface in the aqueous medium. This detergent action emulsifies fats and yields mixed micelles, which allow attack by water-soluble digestive enzymes and facilitate the absorption of lipids through the intestinal mucosa. Mixed Micelles also serve as transport vehicles for those lipids that are less water-soluble than fatty acids, such as cholesterol or the fat-soluble vitamins A, D, E, and K. Thus, efficient absorption of lipids depends on the presence of sufficient bile acids to solubilize the ingested lipids.
Hypolipidaemics pharmacology with a note on Statins /Fibrates/ Sterol absorption Inhibitors/ CETP Inhibitors / Lipoprotein Lipase activators and Bile acid sequestrants
The bile salts such as cholic acid contain a hydrophobic side and a hydrophilic side, thus allowing bile salts to dissolve at an oil-water interface, with the hydrophobic surface in contact with the non-polar phase and the hydrophilic surface in the aqueous medium. This detergent action emulsifies fats and yields mixed micelles, which allow attack by water-soluble digestive enzymes and facilitate the absorption of lipids through the intestinal mucosa. Mixed Micelles also serve as transport vehicles for those lipids that are less water-soluble than fatty acids, such as cholesterol or the fat-soluble vitamins A, D, E, and K. Thus, efficient absorption of lipids depends on the presence of sufficient bile acids to solubilize the ingested lipids.
Hypolipidaemics pharmacology with a note on Statins /Fibrates/ Sterol absorption Inhibitors/ CETP Inhibitors / Lipoprotein Lipase activators and Bile acid sequestrants
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
NVBDCP.pptx Nation vector borne disease control programSapna Thakur
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Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
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Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
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Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
2. 29-2
CHOLESTEROL
Critical substrate for the body:
Fundamental building block of steroid hormones
Essential for building cell membranes, the myelin sheath,
and the brain
Core component of bile salts, which helps in digest dietary
fats
3. 29-3
LIPOPROTEINS
There are several different lipoproteins:
Low-density lipoprotein (LDL)
Very-low-density lipoprotein (VLDL)
High-density lipoprotein (HDL)
4. CONTD’…
1.Chylomicrons (TGs): → fat globule formed in GIT from
dietary TG.
2. VLDL (TGs and cholesterol) → endogenously
synthesized in liver.
Degraded by LPL into free fatty acids (FFA) for storage in adipose tissue
and for oxidation in tissues such as cardiac and skeletal muscle.
Chylomicrons are found in the blood and lymphatic fluid where they
serve to transport fat from its port of entry in the intestine to the liver
and to adipose (fat) tissue.
After a fatty meal, the blood is so full of chylomicrons that it looks
5. CONTD’…
3. IDL (TGs, cholesterol); and LDL
(cholesterol) → derived from VLDL hydrolysis by
lipoprotein lipase. Normally, about 70% of LDL is
removed from plasma by hepatocytes.
4. HDL (protective) →exert several anti
atherogenic effects. They participate in retrieval of
cholesterol from the artery wall and inhibit the
oxidation of atherogenic lipoproteins & removes
9. MANAGEMENT OF
HYPERLIPIDEMIA
1.Diet: Avoid saturated fatty acids (animal fats)
and give unsaturated fatty acids (plant fats).
Regular consumption of fish oil which contains
omega 3 fatty acids and vitamins E and C
(antioxidants).
2.Exercise: ↑ HDL levels and insulin sensitivity.
3.Drug therapy: the primary goal of therapy is
to decrease levels of LDL .
10. 29-10
MONITORING THE DISEASE
The goals of treatment are:
Lowering LDL cholesterol
Reducing total serum cholesterol and triglycerides
Increasing HDL cholesterol
15. INHIBITOR OF VLDL SECRETION
AND LIPOLYSIS
Niacin (Nicotinic acid)
Miscellaneous: Gugulipid and fish oil
derivatives
16. 29-16
HMG-COA REDUCTASE
INHIBITORS
Also referred to as statins
MOA—inhibit enzyme that causes cholesterol
synthesis
IND—adjunct to dietary treatment to decrease total
serum and LDL cholesterol:
Reduce LDL level up to 30%
Raise HDL level up to 20%
17. 1-17
HMG-COA REDUCTASE INHIBITORS
An early, very important
step in this process is the
conversion of acetyl-CoA
molecules into HMG-CoA,
which is then converted to
mevalonic acid by HMG-
CoA reductase.
Mevalonic acid is a rate-
limiting pivotal step in
steroid and cholesterol
biosynthesis.
The liver makes two-
thirds of the daily
18. HMG-COA REDUCTASE INHIBITOR
All of the statins reduce LDL up to 30 percent.
When a greater reduction of LDL is required, simvastatin
(Zocor), atorvastatin (Lipitor), and rosuvastatin (Crestor)
reduce more than 45 percent; in fact, rosuvastatin and
atorvastatin have been demonstrated to reduce up to 60
percent.
All of the statins raise the HDL level up to 20
percent.
Again, simvastatin (Zocor), atorvastatin (Lipitor), and
19. HMG-COA REDUCTASE INHIBITORS
Adverse effects:
Headache, dizziness, alteration of taste,
insomnia, abdominal cramping and
photosensitivity
May cause myalgias, leg ache, and
muscle weakness
Contraindicated during pregancy
20. CHOLESTEROL ABSORPTION
INHIBITORS
Ezetimibe:
Inhibits intestinal cholesterol absorption → ↓
concentration of intrahepatic cholesterol→
compensatory ↑ in LDL receptors →↑ uptake of
circulating LDL →↓ serum LDL cholesterol levels
(17%).
Used in hypercholesterolemia together with statins
& diet regulation.
Adverse effects: diarrhea and abdominal pain,
coughing, back pain, and arthralgia
21. BILE ACID SEQUESTRANTS
Cholestyramine, colestipol and
colesevelam.
MOA: anion exchange resins; bind bile
acids in the intestine forming complex
→so, bile acids loss in the stools →↑
conversion of cholesterol into bile acids in
the liver in results, dec’ed concentration
of intrahepatic cholesterol → compensatory
22. NICOTINIC ACID
MOA: It strongly inhibits lipolysis in adipose tissues which is the
primary producer of circulating free fatty acids
The liver normally utilizes these circulating fatty acids as a major
precursor for triacylglycerol synthesis.
Thus Dec’ in liver triacylglycerol synthesis required for VLDL
production dec’ VLDL which dec’ plasma LDL conc.
Thus both plasma triacylglycerol and cholesterol are lowered.
Increases HDL cholesterol levels
Boosting secretion of tissue plasminogen activator and lowering the
level of plasma fibrinogen red’ thrombosis
IND—hyperlipidemia
Adverse effects—cutaneous flushing, nausea, vomiting, and diarrhea
23. THERAPEUTIC USES
&PHARMACOKINETICS:
Treatment of type IIA and IIB hyperlipidemias (along with statins
when response to statins is inadequate or alternative when they are
contraindicated).
Useful for Pruritus in biliary obstruction (↑ bile acids).
Treatment of diarrhea resulting from bile acid mal-absorption or
secondary to Crohn's disease or the postcholecystectomy syndrome.
Pharmacokinetics:
Orally given but neither absorbed nor metabolically altered by
intestine, totally excreted in feces.
24. ADVERSE EFFECTS:
CONSTIPATION IS MAJOR
↓ absorption of fat soluble vitamins (A, D, K, E)
, ↓ Vit K → hypoprothrombinemia.
↓ absorption of many drugs as digitoxin,
warfarin, aspirin, phenobarbitone.
25. FIBRIC ACID DERIVATIVES
(FIBRATES)
Fenofibrate and gemfibrozil
MOA: Agonists at PPAR (peroxisome
proliferator-activated receptor) → expression of
genes responsible for increased activity of
plasma lipoprotein lipase enzyme → hydrolysis
of VLDL and chylomicrons→ ↓ serum TGs
Increase clearance of LDL by liver & ↑ HDL.
IND—Hypertriglyceridemia (the most effective in reduction
TGs, combined hyperlipidemia (type III) if statins are
contraindicated.
Adverse effects—nausea, vomiting, diarrhea, and
26. GUGULIPID
Consists of Z and E gugulsterone
Inhibit cholesterol biosynthesis and also
enhance rate of cholesterol excretion
Dose 25 mg 3 times a day
Reduced total CH, LDL-C with an elevation of
HDL-C
It is well tolerated, no side effect, except
loose stool
27. FISH OIL DERIVATIVE
Omega-3-fatty acids
Eicosa-pentanoic and docosa-
hexanoic acid
Prophylaxis use in high risk patient
of CAD
Usually formulated with vit.E
30. PREFERRED THERAPY
All hypolipidemic drugs are indicated as adjunctive
therapy to reduce elevated cholesterol levels.
HMG-CoA reductase inhibitors are the most
prescribed.
Cholestyramine can also be used in the treatment
of partial biliary obstruction.
31. CONTRAINDICATIONS
Systemic hypolipidemic drugs should not be used in
patients with liver dysfunction.
Bile acid sequestrants should not be used in patients with
biliary obstruction.
Statins should not be used in pregnant women.
Learning Outcomes
29.1 Explain the importance of triglycerides and cholesterol and their role in atherosclerosis.
Learning Outcomes
29.1 Explain the importance of triglycerides and cholesterol and their role in atherosclerosis.
Learning Outcomes
29.1 Explain the importance of triglycerides and cholesterol and their role in atherosclerosis.
Learning Outcomes
29.1 Explain the importance of triglycerides and cholesterol and their role in atherosclerosis.
Learning Outcomes
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
29.4 Explain why the HMG-CoA inhibitors are more effective than other hypolipidemic drugs.
Learning Outcomes
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
29.4 Explain why the HMG-CoA inhibitors are more effective than other hypolipidemic drugs.
Learning Outcomes
29.2 Discuss the treatment of hyperlipidemia.
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
29.6 Explain the essential terminology associated with atherosclerosis and hypolipidemic drugs.
Learning Outcomes
29.2 Discuss the treatment of hyperlipidemia.
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
Learning Outcomes
29.2 Discuss the treatment of hyperlipidemia.
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
Learning Outcomes
29.2 Discuss the treatment of hyperlipidemia.
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
Learning Outcomes
29.2 Discuss the treatment of hyperlipidemia.
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
Learning Outcomes
29.2 Discuss the treatment of hyperlipidemia.
29.3 Explain the mechanism of action of five different hypolipidemic drugs.
Learning Outcomes
29.6 Explain the essential terminology associated with atherosclerosis and hypolipidemic drugs.
The bile acid sequestrants stay in the lumen of the intestine and trap other subtances during transit through the intestine. Cholestyramine binds with fat-soluble vitamins (A, D, and K), folic acid, and many drugs, thus reducing their GI absorption. Supplementation at time intervals when the bile acids are no longer in the absorption area may be necessary to avoid vitamin deficiencies.
Taking some medication in the presence of grapefruit juice can significantly decrease drug metabolism at the intestinal wall and increase its bioavailability. Increasing a drug’s bioavailability will increase risk of developing adverse effects. Grapefruit juice interacts only with drugs that are administered orally.
Atorvastatin, lovastatin, and simvastatin are definitely affected by grapefruit. Although the studies concerning grapefruit interactions with pravastatin, fluvastatin, or rosuvastatin were not as significant, it probably would be prudent not to consume grapefruit a few hours before or after taking these medications. Orange juice does not have any effect on absorption of these drugs.
Drugs that are potent inhibitors of CYP3A4 and also cause an increase in statin blood levels include cyclosporine, itraconazole, ketoconazole, erythromycin, clarithromycin, and HIV protease inhibitors. For patients who require antifungal therapy, the statins should be stopped until the fungal treatment is discontinued.