STATIN-CHOLESTROL LOWERING DRUG...
DO U THINK STATIN COMPLETELY PREVENTS THE RISK OF CARDIOVASCULAR DISEASES???
- Statins or HMG-CoA reductase inhibitors are class of drugs used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase,which plays a central role in the production of cholesterol in the liver.
- Increased cholesterol levels are associated with increased risk of cardiovascular diseases.
- Statins are therefore being used in prevention of diseases related to cardiovascular system.
- But these drugs cannot give a complete cure to these diseases.
- They can be taken only as a secondary prevention method.
SECONDARY PREVENTION:
- Statins are effective in reducing the mortality rate of people with cardiovascular diseases.
- On an average they lower the LDL level of cholesterol by 1.8mmol/l(70mg/dl) ie it produces a 60% decrease in the number of cardiac events like heart attack and stroke.
CONDITIONS FOR WHICH STATINS ARE USED???
- Statins are used for preventing and treating atherosclerosis that causes chest pain,heart attacks,stroke and in patients who have or are at the risk for atherosclerosis.
- The risk factors for atherosclerosis includes:
- abnormally elevated cholestrol levels
- hereditary or having a family history of heart attacks(particularly at a young age)
- diabetes.
AVAILABLE FORMS OF STATINS:
STATIN
|
BRAND NAME
|
METABOLISM
|
ATORVASTATIN
|
LIPITOR,BAYCOL,TORVAST
LIPOBAY
|
CYP3A4
|
CERIVASTATIN
|
LESCOL
|
VARIOUS
CYP3A4 ISOFORMS
|
FLUVASTATIN
|
XL
|
CYP2C9
|
LOVASTATIN
|
MEVACOR,ALTOCOR,ALTOPREV
|
CYP3A4
|
MEVASTATIN
|
COMPACTIN
|
CYP3A4
|
PITAVASTATIN
|
LIVALO,PIVATA
|
-
|
PRAVASTATIN
|
PRAVACHOL,LIPOSTAT
|
NON CYP
|
ROSUVASTATIN
|
CRESTOR
|
CYP2C9 AND
CYPC19
|
SIMVASTATIN
|
ZOCOR,LIPEX
|
CYP3A4
|
DIFFERENCES AMONG STATINS???
- They differ from each other in several ways, the main difference is in their ability to reduce cholesterol i.e their potency.
- Presently, Atorvastatin(Lipitor) and Rosuvastatin(Crestor) are the most potent whereas the Fluvastatin(Lescol) is the least potent.
ADVERSE EFFECTS:
- The statins also differ in how strong they interact with other drugs.
- Specifically, Pravastatin(Pravachol) and Rosuvastatin(Crestor) levels are less likely to be elevated by the other drugs.
- This is because the enzymes in liver that eliminate the above two drugs are not blocked effectively by these enzymes, hence the levels of these drugs increases which leads to toxicity such as myopathy(inflammation of the muscles).
- Statins also differ in the frequency with which they cause a severe type of myopathy called Rhabdomyolysis, in which the muscles are severely been damaged.
- Recently, the drug Atorvastatin(Lipitor) which was withdrawn from market as it showed some signs of causing Rhabdomyolysis was recalled by the Ranbaxy Laboratories Ltd.
RANBAXY RECALLS GENERIC LIPITOR IN U.S.
[ Courtesy: The Hindu, 25th November,2012,Saturday]
SIDE EFFECTS:
- headache
- nausea
- vomiting
- constipation
- diarrhea
- rash
- weakness
- muscle pain
DRUG INTERACTIONS:
The first type of interactions include the enzymes responsible for the elimination of statins by the liver. Liver enzymes (specifically cytochrome P-450 liver enzymes) are responsible for the elimination of these enzymes with the exception of Pravastatin and Rosuvastatin.
Drugs that eliminate or block the elimination of the drugs are:
- protease inhibitors
- erthromycin
- itraconazole
- clarithromycin
- cyclosporin
- verampil
- grapefruit juice
RECENT FACTS ABOUT STATIN:
- Out of the 100 persons taking he drug statin only below 5 of them are benefitted from the prevention of heart attack.
- Statindrugs do not increase the levels of HDL cholesterol. But can reduce the levels of both HDL and LDL at the same time, thereby increasing the chances of cardiovascular diseases.
- For the prevention of first heart attack, Statin drug may not be helpful. And another fact is that it is not at all useful for treatment in women.
- There are many side effects of the drug.
CONCLUSION:
Statin drug can produce results of lowering the cholesterol level but if it is used properly. We should try our maximium to reduce the levels of LDL so that it is under control then the rest can be regulated with the help of the drug. By this way we can reduce the dose and side effects produced. For lowering the LDL levels changes must be brought in one's lifestyle. Exercise regularly. Together with all these we can reduce the risks of diseases associated with the cardiovascular system...
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