mechanism of action statins #all statins in details

mechanism of action statins #all statins in details

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 %.

Conclusion: in this article, I will discuss the mechanism of action statins, side effects of statins, use of statins, and its drugs in detail if you like it comment out.