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PRESENTED BY PHARM. MAMZA
JOSHUA
3rd, OCT., 2014
 Myocardial infarction also known as
Heart attack is a medical condition that
occurs when blood stops flowing
properly to a part of the heart
 Usually this is because one of the
coronary arteries that supplies blood to
the heart develops a blockage due to an
unstable buildup of white blood cells,
cholesterol and fat.
 Chest pain
 Dypsnoea
 Diaphoresis, weakness, light-
headedness, nausea, vomiting, and
palpitations
 Loss of consciousness
 Sudden death
 The most common triggering event is
the disruption of an atherosclerotic
plaque in an epicardial coronary
artery, which leads to a clotting
cascade, sometimes resulting in total
occlusion of the artery
 Atherosclerosis is the gradual
buildup of cholesterol and fibrous
tissue in plaques
 Lovastatin
 Simvastatin
 Pravastatin
 Atorvastatin
 Fluvastatin
 Rosuvastatin
 Mevastatin
 Cerivastatin
 Breastfeeding
 High alcohol intake
 Myopathy
 Increase in liver enzymes
 Active liver disease or persistent
abnormal liver function test
 Pregnancy
 Rhabdomyolysis
 Kidney injury
 Liver damage
 Neuropathy
 Memory defects
 Acceleration of ageing
 Infection and Cancer
 Diabetes
 Increase in liver enzymes
 Taking a statin drug with amiodarone,
clarithromycin, cyclosporine,
erythromycin, fluconazole, gemfibrozil,
itraconazole, ketoconazole, or niacin
increases the risk of myopathy or
rhabdomyolysis
 Lovastatin, rosuvastatin and simvastatin
may increase the risk of bleeding when
administered with warfarin
 Most of the statins (lovastatin, simvastatin, and
atorvastatin, ) are metabolized by the
cytochromal P450 3A4. Drugs that inhibit P450
3A4, such as itraconazole, cyclosporine, and
erythromycin, increases plasma statin level
 Grapefruit juice can inhibit intestinal metabolism
of the statins and can result in an increase in
artovastatin, lovastatin, and simvastatin serum
levels.
 Co-administration of fluvastatin with warfarin
increases warfarin toxicity, because they are
both metabolised by cytochrome P450 2C9
 food increases the bioavailability of lovastatin
 Conversely bioavailability of pravastatin,
atorvastatin, and fluvastatin is decreased by
food
Statin equivalent dosages
% LDL
reduction
(approx.)
Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin Simvastatin
10–20% – 20 mg 10 mg 10 mg – 5 mg
20–30% – 40 mg 20 mg 20 mg – 10 mg
30–40% 10 mg 80 mg 40 mg 40 mg 5 mg 20 mg
40–45% 20 mg – 80 mg 80 mg 5–10 mg 40 mg
46–50% 40 mg – – – 10–20 mg 80 mg*
50–55% 80 mg – – – 20 mg –
56–60% – – – – 40 mg –
* 80-mg dose no longer recommended due to increased risk of rhabdomyolysis
Starting dose
Starting dose 10–20 mg 20 mg 10–20 mg 40 mg 5–10 mg 20 mg
If higher LDL
reduction goal
40 mg if
>45%
40 mg if
>25%
20 mg if
>20%
--
20 mg if LDL
>190 mg/dL
(4.87 mmol/L)
40 mg if
>45%
Optimal
timing
Anytime Evening
With
evening
meals
Evening Anytime Evening
 Primary prevention: prevention of heart
disease in those with high cholesterol
 Secondary prevention: decreasing mortality in
people with pre-existing CVD
 Familial hypercholesterolemia In children:
statins are effective at reducing their
cholesterol level when lifestyle changes are
not enough
 Meanwhile statins in children should be
started at age 8
 Researchers hypothesize that statins
prevent cardiovascular disease via four
proposed mechanisms
 Improve endothelial function
 Modulate inflammatory responses
 Maintain plaque stability
 Prevent thrombus formation
 Oyster mushroom
 Red yeast rice
 Fish oil
 Flax seeds
 The statins that produce the greatest percentage change
in LDL cholesterol levels are atorvastatin and
simvastatin
 Atorvastatin and fluvastatin are least affected by
alterations in renal function
 Fewer pharmacokinetic drug interactions are likely to
occur with pravastatin and fluvastatin, because they are
not metabolized through the cytochrome P450 (3A4)
system
 The most cost-effective statins, based on cost per
percentage change in LDL cholesterol levels, are
fluvastatin and atorvastatin
 CIPRIDE: Simvastatin tablet 10mg,
marketed by VIXA Pharmaceutical
 LIPIVASTIN: Atorvastatin tablet
10mg, marketed by NEROS
Pharmaceutical
THANK YOU!
THANK YOU!!
THANK YOU!!!

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Statins

  • 1. PRESENTED BY PHARM. MAMZA JOSHUA 3rd, OCT., 2014
  • 2.  Myocardial infarction also known as Heart attack is a medical condition that occurs when blood stops flowing properly to a part of the heart  Usually this is because one of the coronary arteries that supplies blood to the heart develops a blockage due to an unstable buildup of white blood cells, cholesterol and fat.
  • 3.  Chest pain  Dypsnoea  Diaphoresis, weakness, light- headedness, nausea, vomiting, and palpitations  Loss of consciousness  Sudden death
  • 4.  The most common triggering event is the disruption of an atherosclerotic plaque in an epicardial coronary artery, which leads to a clotting cascade, sometimes resulting in total occlusion of the artery  Atherosclerosis is the gradual buildup of cholesterol and fibrous tissue in plaques
  • 5.
  • 6.  Lovastatin  Simvastatin  Pravastatin  Atorvastatin  Fluvastatin  Rosuvastatin  Mevastatin  Cerivastatin
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  • 11.  Breastfeeding  High alcohol intake  Myopathy  Increase in liver enzymes  Active liver disease or persistent abnormal liver function test  Pregnancy
  • 12.  Rhabdomyolysis  Kidney injury  Liver damage  Neuropathy  Memory defects  Acceleration of ageing  Infection and Cancer  Diabetes  Increase in liver enzymes
  • 13.  Taking a statin drug with amiodarone, clarithromycin, cyclosporine, erythromycin, fluconazole, gemfibrozil, itraconazole, ketoconazole, or niacin increases the risk of myopathy or rhabdomyolysis  Lovastatin, rosuvastatin and simvastatin may increase the risk of bleeding when administered with warfarin
  • 14.  Most of the statins (lovastatin, simvastatin, and atorvastatin, ) are metabolized by the cytochromal P450 3A4. Drugs that inhibit P450 3A4, such as itraconazole, cyclosporine, and erythromycin, increases plasma statin level  Grapefruit juice can inhibit intestinal metabolism of the statins and can result in an increase in artovastatin, lovastatin, and simvastatin serum levels.
  • 15.  Co-administration of fluvastatin with warfarin increases warfarin toxicity, because they are both metabolised by cytochrome P450 2C9  food increases the bioavailability of lovastatin  Conversely bioavailability of pravastatin, atorvastatin, and fluvastatin is decreased by food
  • 16.
  • 17. Statin equivalent dosages % LDL reduction (approx.) Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin Simvastatin 10–20% – 20 mg 10 mg 10 mg – 5 mg 20–30% – 40 mg 20 mg 20 mg – 10 mg 30–40% 10 mg 80 mg 40 mg 40 mg 5 mg 20 mg 40–45% 20 mg – 80 mg 80 mg 5–10 mg 40 mg 46–50% 40 mg – – – 10–20 mg 80 mg* 50–55% 80 mg – – – 20 mg – 56–60% – – – – 40 mg – * 80-mg dose no longer recommended due to increased risk of rhabdomyolysis Starting dose Starting dose 10–20 mg 20 mg 10–20 mg 40 mg 5–10 mg 20 mg If higher LDL reduction goal 40 mg if >45% 40 mg if >25% 20 mg if >20% -- 20 mg if LDL >190 mg/dL (4.87 mmol/L) 40 mg if >45% Optimal timing Anytime Evening With evening meals Evening Anytime Evening
  • 18.  Primary prevention: prevention of heart disease in those with high cholesterol  Secondary prevention: decreasing mortality in people with pre-existing CVD  Familial hypercholesterolemia In children: statins are effective at reducing their cholesterol level when lifestyle changes are not enough  Meanwhile statins in children should be started at age 8
  • 19.  Researchers hypothesize that statins prevent cardiovascular disease via four proposed mechanisms  Improve endothelial function  Modulate inflammatory responses  Maintain plaque stability  Prevent thrombus formation
  • 20.  Oyster mushroom  Red yeast rice  Fish oil  Flax seeds
  • 21.  The statins that produce the greatest percentage change in LDL cholesterol levels are atorvastatin and simvastatin  Atorvastatin and fluvastatin are least affected by alterations in renal function  Fewer pharmacokinetic drug interactions are likely to occur with pravastatin and fluvastatin, because they are not metabolized through the cytochrome P450 (3A4) system  The most cost-effective statins, based on cost per percentage change in LDL cholesterol levels, are fluvastatin and atorvastatin
  • 22.  CIPRIDE: Simvastatin tablet 10mg, marketed by VIXA Pharmaceutical  LIPIVASTIN: Atorvastatin tablet 10mg, marketed by NEROS Pharmaceutical