 |
mechanism of action statins |
statins are useful to decrease the
LDL carrier’s cholesterol synthesis. cholesterol is required for making a fat-soluble vitamin, lipid, bile acid, and triglyceride.
Increase an LDL carrier’s
cholesterol they developed atherosclerosis and some cardiovascular problem.
So, statins are inhibiting the LDL carrier’s cholesterol and prevent some
cardiovascular disease.
Statins are also known as “HMG CO
REDUCTASE INHIBITORS”. These hypolipidemic drugs are introduced in 1980. common
mechanism of action statins, it inhibits the conversion of HMG CoA to
mevalonate (mevalonate is used to synthesis of cholesterol, the precursor of
cholesterol) through HMG COA reductase.
Statin is inhibiting the HMG CoA
reductase and reduce the synthesis of cholesterol.
The potency of medication are
different and also these all medication is dose-dependent.
➤ Mechanism of action statins
In describe as per images, the statin is the most effective drug use to treat hyperlipidemia. It inhibits the HMG Co
reductase.
This reductase enzyme is useful in the formation of malonic acid.
This acid is a precursor of cholesterol. So, indirectly they inhibit the
cholesterol by inhibiting the HMG CoA reductase.
Why inhibits the cholesterol? No
doubt cholesterol is useful in the body to produce a lipid, fat-soluble vitamin and
so and so.
But, an excessive amount of cholesterol, the danger to our health. It
formed atherosclerosis and block some coronary artery. So, statins block
the synthesis of cholesterol and control cholesterol imbalance.
Most of the statins are take a bed
time, and produce its effect on midnight.
➢ Use of statins
Statins are firstly used in primary hyperlipidaemias with the increased LDL carrier’s cholesterol level.
➜ Not affect the TGs level.
➜ Diabetes mellitus
➜ Nephrotic syndrome
➜ Secondary used in hypercholesterolemia.
➜ Statins are dose-dependent; it adjusts the LDL carrier’s cholesterol balance in every 3 to 4 weeks.
➢ An adverse effect of statins
➜ Some GI disturbance (abdominal pain, anorexia, nausea, vomiting and diarrhea)
➜ Headache is a mild side effect
➜ Skin rashes and some sleep disturbance are uncommon.
➜ Sometimes produce liver damage (Rare cases)
➜ Alopecia, dry skin, skin rashes and photosensitive reactions.
➜ Muscle acne, gout, arthralgia and myopathy
➜ Some severe reaction includes Myopathy.
➜ CNS adverse effects include amnesia, facial paralysis, dizziness, cognitive impairment and depression.
➜ Another side effect is angioneurotic, edema, flulike syndrome, weight gain and infection.
➢ List of statins medication:
➩ Lovastatin (Mevacor, Altoprev)
➩ Simvastatin (Zocor)
➩ Pravastatin (Pravachol)
➩ Atorvastatin (Lipitor)
➩ Rosuvastatin (Crestor)
➩ Pitavastatin (Livalo)
➠ Lovastatin
Dose: 10 to 40 mg per day
[Azatatin, Rovacor, Lovameg 10, 20
mg tabs]
Lovastatin is first clinically
used in the statins. It derived from mevalonic acid derivatives. It is given orally
in the precursor of lactone formed. The absorption of lovastatin is incomplete.
Metabolized by the first-pass metabolism. Metabolized are excreted through bile.
The mechanism of action is the same as per
above to inhibit cholesterol synthesis. Liver history and patients who
consume a large amount of alcohol, given lovastatin cautiously.
Lovastatin produces a dose-dependent effect.
Lovastatin 20 mg/day reduce 25%
LDL – cholesterol
Lovastatin 40 mg/day reduce 32%
LDL – cholesterol
Lovastatin 80 mg/day reduce 40%
LDL – cholesterol
➠ Simvastatin
Dose: 5 to 20 mg per day
[Simcard, Zosta, Simvotin 5, 10,
20 mg tabs]
Simvastatin are synthetically
derived a fermentation product of Aspergillus terreus. useful to treat hyperlipidemia.
It is twice effective than lovastatin. In the case of an HDL cholesterol low, it raises
the HDL cholesterol.
Simvastatin is dose-dependent,
various doses of simvastatin is producing a different effect. The mechanism of
action statins are similar as per above.
➠ Pravastatin
[Pravator 10, 20 mg tabs]
It derived from the mevinic acid
derivatives. Pravastatin are given in the active form, at the low dose of
pravastatin it is equipotent the lovastatin, but in the higher dose of
lovastatin, cholesterol-lowering effect produces in less.
Mechanism of action of pravastatin
are similar to as per above.
➠ Atorvastatin
Dose: 10 to 40 mg per day
[Atorva, Aztor, Atorlip 5, 10, 20
mg tabs]
Atorvastatin is the most popular
medication. it is more potent and also a appears highest an LDL cholesterol-lowering
effect produces. Also, a mechanism of action of atorvastatin are same as per
above.
Also, a reduce the triglyceride in
patients. The plasma half-life is much longer than another statin 18 to 24 hours. Also, atorvastatin is produced in additional antioxidant properties.
➠ Rosuvastatin
Dose: 20 mg per day (in starting 5
mg OD)
[Rosyan, Rosuvar 5, 10, 20 mg
tabs]
It is another newer medication.
its twice effect produce than atorvastatin. (10 mg rosuvastatin = 20 mg
atorvastatin). Also, a plasma half-life is the same as per above 18 to 24 hours.
In severe hypercholesterolemia,
produce a greater LDL-cholesterol reduction level. It also raises HDL carrier’s
cholesterol by 15 to 20 %.
