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Lipids

 Lipids are a diverse group of substances ( fats, oils, hormones, and


certain components of membranes)whose common property is
inability to mix ( dissolve) with water but soluble in organic
solvents like alcohol, ether

 Hydrophobic

 They are made mainly of carbon, hydrogen and oxygen atoms and
some contains additional elements like nitrogen or phosphorus.

Main Functions
1. Store Energy
2. Structural components of Cell Membrane

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Types of Lipids

lipids can be classified into a 4 major


groups:
1. fatty acids,
2. fatty acid derivatives,
3. Cholesterol and its derivatives, and
4. lipoproteins. 

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Fatty Acids

• Fatty acids rarely occur as free


molecules in nature but are usually
found as components of many
complex lipid molecules such as
 Fats (energy-storage compounds)
and
 Phospholipids (the primary lipid
components of cellular membranes)

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Saturated fatt
y acids Unsaturated
 fatty acids
saturated indicates that unsaturated  indicates
the maximum possible that fewer than the
number of hydrogen maximum possible
atoms are bonded to number of hydrogen
each carbon in the  atoms are bonded to
molecule.  each carbon in the
molecule. 
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Source of fatty acids
• The main source of fatty acids in
the diet is triglycerides,
generically called fats

• Triglycerides consist of three 


fatty acid molecules.

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• After ingested triglycerides(Fat) pass through the stomach and into the 
small intestine,

• detergents called bile salts are secreted by the liver via the gall bladder and disperse
the fat as micelles.

• Pancreatic enzymes called lipases then hydrolyze the dispersed fats to give


monoglycerides and free fatty acids.

• These products are absorbed into the cells lining the small intestine, where they are
resynthesized into triglycerides.

• The triglycerides, together with other types of lipids, are then secreted by these cells
in lipoproteins(Lipid + Proteins), large molecular complexes that are transported in
the lymph and blood to recipient organs.

• There they are transported into adipose cells, where once again they are
resynthesized into triglycerides and stored as droplets.

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There are four major classes of circulating lipoproteins, each with
its own characteristic protein and lipid composition. They are

1. Chylomicrons,
2. very low-density lipoproteins (VLDL),
3. low-density lipoproteins (LDL),
4. Intermediate-density lipoproteins (IDL)
and high-density lipoproteins (HDL)

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There are 4 main types of lipoprotein

1. Chylomicrons: (Rich in TGS)forms in GIT


(intestinal Lining) from dietary TG and
secreted into the lymphatic circulation.
These lipoproteins move into the blood
stream where they got hydrolyzed by
endothelial lipoprotein lipase which
hydrolyzes the triglyceride into glycerol and non-
esterified fatty acids.

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 The lymphatic system is a network of tissues, vessels and organs that work
together to move a colorless, watery fluid called lymph back into our
circulatory system .

 Some 20 liters of plasma flow through our body’s arteries and smaller
arteriole blood vessels and capillaries every day.

 After delivering nutrients to the body’s cells and tissues and receiving their
waste products, about 17 liters are returned to the circulation by way of
veins.

 The remaining 3 liters seep through the capillaries and into our body’s
tissues.

 The lymphatic system collects this excess fluid, now called lymph, from
tissues in your body and moves it along until it's ultimately returned to our
bloodstream.

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2. VLDL (Rich in Colesterol & TGs)

After which the chylomicron


remnants are absorbed in the liver
and packaged with
cholesterol,cholesteryl esters and
ApoB100 to form VLDL.

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3. IDL( TGs and Cholesterol)
After the release of VLDL into the blood stream it will
be converted into IDL by the action of lipoprotein
lipase and hepatic lipase.

4. LDL (Cholesterol)
After the hydrolysis by hepatic lipase, IDL will be
converted to LDL

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• Cholesterol is lost from cells in 
peripheral tissues by transfer to
another type of circulating
lipoprotein (HDL) in the blood and
is then returned to the liver, where it
is metabolized to bile acids and salts.

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LDL (BAD LIPIDS ):
Low density lipoproteins (LDL) are considered “bad”
cholesterol.
While they carry needed cholesterol to all parts of the body,

too much LDL in the system can lead to coronary artery


disease, due to the buildup of LDL deposits in the artery walls

 Together with other substances, it can form plaque, a thick,


hard deposit that can narrow the arteries and make them less
flexible.

 This condition is known as atherosclerosis. If a clot forms and


blocks a narrowed artery, heart attack or stroke can result

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HDL (GOOD LIPIDS):

High-density lipoproteins – collect


cholesterol particles as they travel through
blood vessels and deposits them in the liver
where they are transferred to bile acids and
disposed off.
A higher HDL score is desirable and will
improve overall cholesterol score.

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Hyperlipidemia classification
• Hyperlipidemia general can be classified to:

Primary:
It is also called familial due to a genetic defect,

1. It may be Monogenic: a single gene defect


or
2. Polygenic: multiple gene defects.

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Secondary:
• it is acquired because it is caused by another
disorder like

• diabetes, nephritic syndrome, chronic alcoholism,


hypothyroidism and with use of drugs like
corticosteroids, beta blockers and oral
contraceptives.

• Secondary hyperlipidemia together with significant


hypertriglyceridemia can cause pancreatitis.

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Symptoms of Hyperlipidemia

• can develop xanthomas which are


deposits of cholesterol may form
under the skin, especially under the
eyes.

• may develop numerous pimple-like


lesions at different sites in their body
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Complications of Hyperlipidemia
• Atherosclerosis: Hyperlipidemia is the
most important risk factor for
atherosclerosis, which is the major cause
of cardiovascular disease.

• Atherosclerosisis a pathologic process


characterized by the accumulation of
lipids, cholesterol and calcium and the
development of fibrous plaques with in
the walls of large and medium arteries
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Fatty deposits build up in blood vessel walls and.
resulting in narrowing of the the arteries that
supply blood to the myocardium, and results in
limiting blood flow and insufficient amounts of
oxygen to meet the needs of the heart
• The resulting condition, called atherosclerosis
often leads to eventual blockage of the coronary
arteries and a “heart attack”.

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• Eventually, the reduced blood flow may
cause chest pain (angina), shortness of
breath, or other coronary artery disease
signs and symptoms. A complete blockage
can cause a heart attack.
• Because coronary artery disease often
develops over decades, one might not
notice a problem until you have a
significant blockage or a heart attack

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Myocardial Infarction (MI):
• MI is a condition which occurs when blood
and oxygen supplies are partially or
completely blocked from flowing in one or
more cardiac arteries, resulting in damage
or death of heart cells. The occlusion
may be due to ruptured atherosclerotic
plaque.
• The studies show that about one-fourth of
survivors of myocardial infarction were
hyperlipidemic
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Ischemic stroke:
• Strokes occur due to blockage of an artery
by a blood clot or a piece of atherosclerotic
plaque that breaks loose in a small vessel
within the brain.

• Many clinical trials revealed that lowering


of low-density lipoprotein(LDL) and total
cholesterol by 15% significantly reduced
the risk of the first stroke24
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Classification of drugs
1. HMG-CoA reductase inhibitors:
Atorvastatin, Simvastatin,Rosuvastatin, Pravastatin,
Fluvastatin
2. Bile acid Sequestrants (resin): Cholestyramine,
Colestipol
3. Activate Lipoprotein Lipase (Fibric acid derivatives):

Clofibrate, Gemfibrozil,

Fenofibrate
4. Inhibit lipolysis & triglyceride synthesis: Nicotinic acid
5. Others: Ezetimibe,
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Mixed dyslipidemia
• Mixed dyslipidemia is defined as
elevations in LDL cholesterol and
triglyceride (TG) levels that are often
accompanied by low levels of HDL
cholesterol.

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MOA
 Significantly decrease plasma
triglycerides
 Moderate decrease in LDL cholesterol
 Increase in HDL cholesterol
concentrations
 Decrease in VLDL production
 Increase hepatic excretion of
cholesterol
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Triglycerides
• Stimulation of lipoprotein lipolysis.
• Increase hepatic fatty acid (FA) uptake and

• reduction of hepatic triglyceride production.

• enhance the production of fatty acid transport


protein and acyl-CoA synthetase, which contribute
to the increase uptake of fatty acid by the liver
and

• as a result in a lower availability of fatty acids for


triglyceride production
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Dose of Fenofibrate

• Fenofibrate capsules are administered orally once daily with or without


food.
• Dose adjustments are made at 4 to 8-week
intervals based on the individual patient response.

• Hypertriglyceridemia (type IV or V)
– 40 to 160 mg daily
• Hypercholesterolemia
– 120 to 160 mg daily
• Mixed dyslipidemia
– 120 to 160 mg daily

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Precautions
• Patients with hepatic impairment should
avoid the use of fenofibrate. No dose
adjustment is necessary for patients with
renal impairment if creatinine clearance is
above 80 mL/min

• Fenofibrate is contraindicated if creatinine


clearance is under 30mL/min or if the
patient has severe renal dysfunction. 

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CI

• Fenofibrate is contraindicated for


patients with a history of
hypersensitivity to fenofibrate, liver
disease, severe renal dysfunction,
preexisting gallbladder disease, or
breastfeeding.

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Fenofibrate Market size

• Yearly: Around 4.5 crore


• Major 3 brand
• TGR (Intas) : 2.3 crore
• Fenocard (Quest): 1.3 crore
• LIPICARD(USV): 0.8 crore
• Fenolip (CIPLA):
• Triglide (Grace):
KNOW
• Know Prescriber

• Know Counters selling Fenofibrate


PROMOTION

• Promote Doctors

• Promote to Stockiest

• Promote – Pharmacy
Community Pharmacy
Hospital Pharmacist

POB
• Sampling

• Promotional Out Put


Review

• Feed Back
• Stockiest feed back
• Stockist staff
• Does thy know about Trichek
• Similar brand
• Trichek strength
FAST
• Face(Facial Weakness) – has their face fallen on one
side? Can they smile? Has their mouth or eye drooped?
• Arms Weakness – can they raise both their arms and
keep them there?
• Speech Problems– is their speech slurred? If they
notice any of these symptoms it is:
• Time – time to call 999 if you see ANY of these signs

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STROKE
• Stroke refers to any damage to the brain or spinal cord
caused by an abnormality of the blood supply.

• The terms STROKE is typically used when


symptoms begin abruptly

• WHO:- Clinical syndrome consisting of rapidly


developing clinical signs of focal disturbances of
cerebral function, lasting more than 24 h or leading to
death with no apparent cause other than that of vascular
origin

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Types of brain Damage in Stroke

• There are two major categories of brain damage in


stroke patients.
1. ISCHEMIA: Which is lack of blood flow depriving
brain tissue from energy and oxygen

2. HEMORRHAGE: Which is the release of blood into


the brain and into the extravascular spaces within the
cranium.

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• Ischemia
Further subdivided into 3 different mechanisms
-Thrombosis
-Embolism
-decreased systemic perfusion

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• Thrombosis

• Refers to an obstruction of blood flow due to a


localised occlusive process within one or more blood
vessels.

• The lumen of vessel is narrowed or occluded

• The main cause is atherosclerosis

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• EMBOLISM

Material formed else where within vascular system lodges


in an artery and blocks the flow

Blockage can be transient or may persist for hours or days.

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Cardiac sources of embolism:
• Include from heart valves and clots or tumors within
the atrial or ventricular cavities
• Artery-to-artery emboli.
Are composed of clots, platelet clumps, or fragments of
plagues that break off from the proximal vessels

Pradocical embolism: clots originating in systemic veins


travel to the brain
Ocassionally air, fat, particulate matter from injected
drugs, bacteria, foreign bodies, and tumor cells enter
the vascular system and embolize to brain arteries.
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• Decreased Systemic Perfusion

Diminished flow to brain tissue is caused by low systemic


pressure.

The most common causes are


1. Cardiac pump failure:most often due to myocardial
infarction or arrthmia
2. Systemic hypotension: due to blood loss or
hypovolemia

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Sub arachnoid haemorrhage

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• Infarction: Permanent injury

• The brain requires 75 to 100 mg of glucose each minute.

• Brain measures only 2% of adult body weight but uses


approx. 20% of the cardiac output

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