2. Essential Fatty Acids
ā¢ These are group of fats which are not synthesized in the human body but
required for various enzymatic actions for body metabolic processes, hence
it is necessary that should be included in our dietary fats.
ā¢ Only two fatty acids belong to this group.
ā¢ i) Linoleic Acid (LA),Omega-6 fatty acid),
ā¢ ii) Alfa-Linolenic acid (ALA), omega-3 fatty acid
ā¢ Iii) A third group called conditionally essential which includes
Decosahexaenoic acid, an Omega-3 fatty acid, & gamma-linolenic acid
(Omega-6 fatty acid are considered as essential under certain
developmental or disease conditions.
3. sources
ā¢ Common sources are Sea fish, shellfish, seawood oil,flaxseed oil,
flaxseed, chia seeds, pumpkin seeds, sunflower seeds and walnuts.
ā¢ Fish is the main source of EPA and DHA
ā¢ In human body can convert ALA to EPA then toļ DHA, in presence of
some algae if consumed.
PUFA: Poly unsaturated fatty acids ( contain more than one double
bond), LA and ALA are two essential fatty acids.
MUFA: Mono Unsaturated Fatty Acids,( contain only one double bond
carbon atoms).
4. MUFA
ā¢ Most of the MUFA are liqid at room temperature but semi solid or solid when
cooled.
ā¢ Dietary fat should provide 30% of the total calory required and the distributions
as under
ā¢ - 7% from saturated fat
ā¢ - 10% from MUFA
ā¢ - 15-20% from PUFA
ā¢ Sunflower oil 85% MUFA
ā¢ Olive oil 75% MUFA
ā¢ Canola oil 58% MUFA
ā¢ Common Sources of MUFA: Olive, Avocado, Almond, Sesame, Peanut, Sunflower,
Grapeseed,whole grain wheat,corn.
5. PUFA
ā¢ PUFA: Poly Unsaturated Fatty Acids,
ā¢ Liquid at room temperature, viscosity and melting temperature rises
inversely to double bond.
ā¢ Are of two types: Omega-3 and Omega-6.
ā¢ Omega-3, three types. Linoleic acid,
6. Values
NAMES NORMAL BORDERLINE HIGH VALUE VERY HIGH Very Very high
CHOLESTEROL <200mg/dl 200-239 > 240
LDL <70mg/dl 70-100 100-129 >130-159 >160
HDL <40mg/dl ( risk
of Heart Disease
40-59(BETTER) >60 ( BEST)
TRIGLYCERIDES < 150mg/dl < 150-199 200-499 >500
Total Cholesterol
HDL ratio
< 3.5 ( ideal) < 5.0 > 5.0 ( Bad)
LDL HDL ratio < 2 .0 (ideal) < 5.0 Good > 5.0 very high
Triglyceride HDL
ratio
< 2.0 (ideal) 4.0-5.0 (high) > 6.0 ( too high)
9. Mechanism ofactions & Doses
ā¢ 1. HMG- CoA (Hydroxymethylglutaryl-CoA) reductase inhibitors or Statns--> are selective competitive
inhibitors the enzyme responsible for the convertion of the HNG-CoA to mevalonate in the cholesterol
synthesis pathway, there by reducing hepatic cholesterol synthesis.
ā¢ 2. By upregulating of LDL cholesterol receptors --> increases hepatic uptake of LDL cholesterol from
circulation.
ā¢ Lowers Total cholesterol, LDL, and Triglycerides. Increases HDL cholesterol Lowers. May stabilize the
plaques .
ā¢ Can be taken with or without food.
ā¢ Due to hepatic variations in cholesterol synthesis ( synthesis is highest in the morning hours), an
evening dose for some statins are recommended, but should taken in the same time of the day.
ā¢ Atorvastatin along with Rosuvastatin & Pitavastatin .can be taken either in the morning or evening.
ā¢ Start Atorvastatin 10mg per day, can increase the dose after 4 weeks observing the respons.
ā¢ Maximum dose 40mg per day.
ā¢ Atorvastatin is the most commonly used drug.
10. Adverse Effects
ā¢ Most well-tolerated drug.
ā¢ Common adverse effects are: Myopathy, Rhabdomyolysis, Hepato
toxic.
ā¢ Rhabdomyolysis is the most sereious complications of statin therapy.
ā¢ Myopathy is dose dependent and mostly manifaste as deffuse
myeagia, reversible with the discontinuance of the drug.
ā¢ Hepatic toxicity--> Elevated liver enzymes are seen, which are
transient and resoles with continued therapy. FDA no longer
recommends routine LFT with the use of these drugs without the
symptoms of weakness, coloured urine etc.
11. Drug inreactions.
ā¢ CYP3A4 SUBSTRATE STATINS (Atorvastatin, Lovastatn, Simvastatin) inter acts
with drugs those are potent 3A4 inhibitors like - Azoles, Diltiazem,
Erythromycin etc.
ā¢ In such cases a reduced dose of the drug or alternatives may be used.
ā¢ DOSE RESTRICTION recommended with the coadministration with Gemfibrozil
or other fibrates.
ā¢ Use of more than one statin not recommended.
ā¢ Contraindicated during pregnancy, and breast feeding.
ā¢ Contraindicated in hepatic disease and incase of persistent elevations in
aminotransferase level.
12. Monitoring
ā¢ Base line LFT & LFT before commencement of the treatment .
ā¢ May be repeated after 3 months to asses efficacy and adherance to
the treatment protocol. a moderate regimen reduces by 30-50% of
the base line value. Repeatation of tests at 3-12 months interval.
ā¢ In case of renal failure dose to be adjusted accorging to GFR.
ā¢ No definite tratment for toxicity or adverse drug reaction, stopage of
drugs, fluid, electrolyte balace are the corner stone of the therapy.
13. Treatment of Hypertriglyceridemia
ā¢ Most of the time it is associated with hypercholesterolmia.
ā¢ Before stating any pharmacological treatment patient should be evaluatated for
the existance of Diabetes, Heart Disease, Obesity, Metabolic Syndrome.
ā¢ Life-style modification, dietary regulation, physical exercise weight reduction are
essential.
Treated mostly with --> Statins, Fibrates, Niacin & Fish oil;
the target is to achieve LDL-C level.
Most of the time Statins alone reduces the Triglyceride levels.
The combination therapy of Fibrates along with Statins increases the chances of
complications like Rhabdomyolysis and Hepatic dysfunction.
Niacin is a better option as regards rhabdomyolysis is concerned.
Fish oil in a dose of 2-4gms/day increases Omega-3 levels.
14. Diet
ā¢ Reduce dietary intake of sugar, because sugar gets converted to triglycerides in
the body, avoid fine sugar, ice cream, sweetened drinks etc.
ā¢ Add more fibers (whole grain, fresh leafy vegetables,fruits) in your diet.
ā¢ Reduce intake of fats in diet, which includes reduction of trans fats (found in
foods such as margarine) and saturated fats (found in foods such as butter,
poultry fat and red meat) should be avoided or reduced.
ā¢ Include, in stead polyunsaturated fats (found in foods like corn, sunflower, and
soybean oils) and monounsaturated fats(found in foods such as olive oil).
ā¢ Consume Omega-3 fatty acids present in foods like sea fish found in most fish,
such as salmon sardines, heron etc.
ā¢ The vegetarian source of Omega-3 fatty acids are flaxseed (linseed) oil, rapeseed
oil, soya oil and soya-based foods, such as tofu, walnuts. Eggs are enriched with
omega-3 fatty acids.
15. Fats
ā¢ Fats are basically are of 3types. Saturated, Poly-unsaturated & Mono-unsaturated.
ā¢ Essential fatty acids (EFA) are a group of fats essential for body metabolism but not synthesized in our body so these are to be taken from external source.
ā¢ There are two types EFA known to be essential for humans: alpha-linolenic acid (an omega-3 fatty acid) and linoleic acid (an omega-6 fatty acid).
ā¢ PUFA: Poly unsaturated fatty acids. It can be short chain or long chain depending upon the number of carbon atoms present.
ā¢ MUFA: Mono unsaturated fatty acids.
ā¢ Polyunsaturated fatty acids with 16-carbon and 18-carbon chains are sometimes classified as short chain polyunsaturated fatty acids (SC-PUFA), as opposed to long-chain polyunsaturated fatty acids (LC-PUFA), which have more than 18 carbon atoms.[6]
ā¢ Both the essential fatty acids are SC-PUFA with an 18-carbon chain:
ā¢ Ļ-3 fatty acid:
ā¢ Ī±-linolenic acid or ALA (18:3n-3)
ā¢ Ļ-6 fatty acid:
ā¢ linoleic acid or LA (18:2n-6)
ā¢ These two fatty acids cannot be synthesized by humans because humans lack the desaturase enzymes required for their production.
ā¢ They form the starting point for the creation of more desaturated fatty acids, most of which also have a longer carbon chain:
ā¢ Ļ-3 fatty acids:
ā¢ eicosapentaenoic acid or EPA (20:5n-3)
ā¢ docosahexaenoic acid or DHA (22:6n-3)
ā¢ Ļ-6 fatty acids:
ā¢ gamma-linolenic acid or GLA (18:3n-6)
ā¢ dihomo-gamma-linolenic acid or DGLA (20:3n-6)
ā¢ arachidonic acid or AA (20:4n-6)
ā¢ Except for GLA, which has a short 18-carbon chain, these fatty acids have more than 18 carbon atoms and are typically classified as LC-PUFA.[6]
ā¢ Ļ-9 fatty acids are not essential in humans because they can be synthesized from carbohydrates or other fatty acids.