Statins - High Cholesterol Lowering Pills

Statins are currently the most commonly used drugs to treat high cholesterol. Statins on the market are: Simvastatin, Atorvastatin, Pravastatin, Rosuvastatin, Lovastatin, Fluvastatin and Pitavastatin.

Statins medications
Statins medications

What is statins?

Our blood cholesterol ratio has two origins: diet and production by the liver. People with high cholesterol may have it because of a high fat diet or because their liver produces more cholesterol than necessary.

Statins are scientifically called inhibitors of the enzyme HMG-CoA reductase. HMG-CoA reductase is one of the liver enzymes responsible for cholesterol production. Depending on the dose and type of statin used, the reduction in LDL (bad cholesterol) cholesterol may be greater than 60%.

Statins are not the only drugs available on the market to treat high cholesterol, but they have the best results in scientific studies.

Statins have been shown to inhibit the accumulation of cholesterol in the arteries, a process called atherosclerosis, which in the long run leads to serious cardiovascular diseases, such as heart attack and stroke.

Best cholesterol lowering remedies

In addition to statins, there are a variety of drugs on the market that are indicated for the treatment of high cholesterol, including Ezetimibe, cholestyramine, nicotinic acid and fibrates. However, none of these have the same performance as statins in scientific studies*.

* Recently entered the market a new class of drugs for lowering cholesterol called PCSK9 inhibitors. In the initial studies, these drugs had similar results to statins in the secondary prevention of infarction. In Brazil, alirocumabe and evolocumab are the two drugs of this family already approved by ANVISA.

Even among statins, the results vary, with some drugs clearly more potent than others.

Rosuvastatin and Atorvastatin are the two most potent statins, with a greater ability to lower LDL cholesterol levels. Simvastatin, Pravastatin and Pitavastatin have intermediate potency, while Fluvastatin and Lovastatin are the least potent statins.

Rosuvastatin and Atorvastatin also have the best results in reducing triglycerides and increasing HDL (good cholesterol) cholesterol. In relation to HDL, high doses of Simvastatin also have good results.

Despite the different results, all statins are effective in lowering LDL cholesterol and increasing HDL cholesterol. Rosuvastatin and Atorvastatin are the most effective statins, but also the most expensive ones. Not every patient needs the most potent drug to control their cholesterol. Even Fluvastatin, which is the least potent of statins, when at high doses, can achieve reductions of up to 40% in LDL cholesterol values, which is sufficient for many patients.

Ideally, you should research the prices of statins well in the market and talk to your doctor about what is the best option for your individual case. Not everyone needs the more expensive statin.

Side effects of statins

In addition to being the most effective cholesterol-lowering drug group, statins are also the ones with the lowest rates of side effects. This, however, does not mean that they do not occur. Among the potentially more serious effects, we can mention:

Liver injury

Studies show that 0.5 to 1% of patients taking a statin may show signs of mild liver injury, and 0.1% may have more serious injuries, such as drug hepatitis.

The diagnosis of hepatic toxicity is made by assaying blood transaminases (TGO and TGP). Elevated levels of TGO and TGP may indicate hepatic injury caused by statins.

Liver lesions usually appear within the first 3 months of treatment and, if discrete, usually regress spontaneously, even if treatment is not discontinued. In the most relevant liver lesions, as in the case of elevation of GRT and TGF by more than 3 times the normal value, only dose reduction is usually sufficient. In the vast majority of cases, there is no need to permanently stop treatment.

Patients with known liver disease, such as cirrhosis, should avoid the use of statins.

Note: Fluvastatin appears to be the one that most often causes changes in liver exams.

Muscle injury

Toxicity of the muscles is another possible side effect of statins. About 2% to 10% of patients using a statin may complain of muscle pain or cramps. 0.5% provide myositis, which is an inflammation of the muscle, characterized by pain and weakness in some muscle groups, as in thigh muscles. 0.1% presents rhabdomyolysis, which is a severe muscle injury.

Pravastatin and Fluvastatin are the drugs that least cause muscle damage. In patients with complaints of muscle pain and/or increased blood CK levels (CK is the enzyme that increases in cases of muscle damage), try reducing the dose of the statin or switching it to one of the two less toxic to muscles.

Note: Patients with hypothyroidism are at increased risk of muscle damage by statins.

It is not indicated to request tests to dose routine OBT, TGP and CK in patients who use statins. However, before starting treatment, it is interesting to know what the patient's baseline values are for future comparison if necessary.

We have a specific article about muscle damage caused by statins: Muscle Triggered by Cholesterol Remedies .

Diabetes mellitus

In recent years there has been growing concern about the increase in diabetes cases caused by the use of statins. What is currently known is that the risk is low and occurs mainly in patients who take high doses of statins. In these, the incidence of diabetes appears to be 0.5 to 1%.

How to take the cholesterol remedy

The production of cholesterol by the liver seems to be more intense during the night, when the individual is under prolonged fasting. Therefore, we generally advise patients to take their statins at night. However, newer statins, such as Atorvastatin and Rosuvastatin, have a longer duration of action than simvastatin, and can be taken at any time of the day.

Statins can be taken outside or during meals, except for Lovastatin which should be taken together with food, as these potentiate its absorption.

Statins should be taken daily. In rare cases, the doctor may suggest the use on alternate days, especially in patients who have side effects. Apparently taking a statin every other day, is only effective if the dose of the tablet is increased.

Although in theory it is an option, there are no studies that prove that the use of statins on alternate days has the same results as daily use.

Drug interaction

Statins may interact with several other medications. The main risk is increased cases of muscle damage.

The drugs that usually interact with statins are:
  • Antiretrovirals used to treat HIV
  • Erythromycin
  • Itraconazole
  • Clarithromycin
  • Ciclosporin
  • Diltiazem
  • Verapamil
  • Genfibrozil

Excessive alcohol consumption also increases the risk of liver and muscle damage by statins.

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