The active ingredient atorvastatin is used to lower elevated blood lipid levels when a low-fat diet does not bring the desired result. The active ingredient mainly reduces increased cholesterol and triglyceride levels. Atorvastatin is also used to prevent atherosclerosis, heart attacks and strokes.
What is this medicine for Atorvastatin
Atorvastatin, sold under the brand name Lipitor among others, is a statin medication used to prevent cardiovascular disease in those at high risk and to treat abnormal lipid levels. For the prevention of cardiovascular disease, statins are a first-line treatment. It is taken by mouth.
Atorvastatin – application, effect, side effects
Statins like atorvastatin are used to lower total cholesterol levels and specifically lower LDL cholesterol levels.
Statins like atorvastatin are used to lower total cholesterol and specifically LDL cholesterol. This is particularly indicated as a preventive measure in the case of hypercholesterolemia. Atorvastatin is also used to reduce the risk of atherosclerosis, especially in the case of coronary heart disease or multiple risk factors for the same, and to prevent secondary cardiovascular diseases.
The early administration of statins such as atorvastatin for acute coronary syndrome is debated and practiced in some clinics. So far, however, their benefit has only been proven for individual patient groups.
Mechanism of action
Like all statins, atorvastatin affects the metabolism of cholesterol. It inhibits the enzyme HMG-CoA reductase, which catalyzes the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate. As a result, cholesterol biosynthesis is interrupted at an early stage and the cholesterol level in the cells drops.
As a consequence, hepatic cells in particular increasingly develop LDL receptors on the plasma membrane. To compensate for the lack of cholesterol in the cell, more LDL cholesterol is absorbed from the plasma. Depending on the dose, the total cholesterol level is reduced by up to 50%. The triglyceride plasma concentration also falls by up to 25%, the LDL cholesterol concentration by 34-63%. Along with the LDL cholesterol, the level of apolipoprotein B is also lowered. Apolipoprotein B is suspected to be a risk factor for stroke and heart attack. As the plasma level falls, the risk of rupturing atheromatous plaques and their progression is reduced. With atorvastatin administration, the HDL cholesterol level in the plasma also increases by 5-10%.
In addition to the effect on the cholesterol level, other pleiotropic effects are ascribed to atorvastatin. It is said to improve endothelial function, stabilize platelets, inhibit atherosclerosis-associated inflammatory reactions, have an antioxidant and vasculoprotective effect and inhibit the maturation and antigen-presenting function of dendritic cells in plaque.
The lipophilic atorvastatin is a prodrug. After oral administration, up to 90% is absorbed in the gastrointestinal tract. The bioavailability is on average 25%, but drops to around 13% if food is consumed at the same time. The maximum plasma concentration is reached less than two hours after administration, the plasma half-life after approximately 14 hours. Atorvastatin at least 98% is bound to plasma proteins.
Atorvastatin is absorbed by the liver cells via polypeptides that transport organic anions, or OATP for short, and after the first passage is broken down into two active metabolites. The cytochrome P450 isoenzyme CYP3A4 metabolizes the prodrug further in the liver cells to ortho- and parahydroxylated derivatives and various beta-oxidation products. The metabolites are eliminated via the bile. A small proportion is also excreted renally.
Due to the first-pass metabolism, the elimination half-life of atorvastatin increases significantly to around 30 hours compared to other statins.
Atorvastatin is offered as tablets with 10 mg, 20 mg, 40 mg and 80 mg of active ingredient. Regardless of the therapeutic indication, therapy should be started with a dose of 10 mg once daily after an initial change in diet. The dose can then be increased or adjusted every four weeks until the target values are reached. The maximum daily dose is 80 mg once a day.
In heterozygous familial hypercholesterolemia, a combination of 40 mg atorvastatin and a bile acid-binding ion exchange resin can be used instead of a maximum dose of 80 mg daily. Studies have shown that a dose of 10 mg per day is sufficient for primary prevention of cardiovascular diseases. However, this should be checked and adjusted for the individual patient in accordance with the current guidelines.
Atorvastatin is recommended for children from the age of ten at the earliest. However, dose recommendations are not possible due to the limited study situation.
- allergic reaction
- a headache
- pharyngolaryngeal pain
- Constipation, gas, nausea, diarrhea
- Pain in the extremities
- Muscle spasms
- Joint swelling
- Back pain
- changes in liver function tests
- increased creatine phosphokinase in the blood.
- Weight gain
- Disorder of taste
- blurred vision
- Upper and lower abdominal pain
- Urticaria, rash
- Neck pain
- Muscle weakness
- Chest pain
- peripheral edema
- positive test for white blood cells in the urine.
- peripheral neuropathy
- Visual disturbances
- angioneurotic edema
- bullous rash including erythema multiforme
- Stevens-Johnson Syndrome
- toxic epidermal necrolysis
- Tendopathy (sometimes complicated by a tendon rupture).
- anaphylactic reactions
- Hearing loss
- Liver failure
Side effects of unknown frequency:
- autoimmune necrotizing myopathy.
All drugs that are also metabolized by or inhibit the CYP3A4 enzyme can interact with atorvastatin. The same applies to drugs that use or attack the same hepatic transport protein, OATP1B1. Both can increase the plasma level of atorvastatin and the associated risk of myopathy. Gemfibrozil, fibrates, fusidic acid, colchicine and ezetimibe have been observed to specifically increase the risk of rhabdomyolysis. Therefore, when these drugs are administered at the same time, a prior risk-benefit assessment is recommended, as well as simultaneous clinical monitoring of the patient.
What are the most common side effects of atorvastatin?
The most common side effects are headaches, feeling sick (nausea), diarrhoea and cold-like symptoms. Do not take atorvastatin if you’re pregnant, trying to get pregnant or breastfeeding. Keep taking atorvastatin even if you feel well, as you will still be getting the benefits.
What does Atorvastatin do to the body?
Atorvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
What should you not take with atorvastatin?
Do not take any red yeast rice products while you are taking atorvastatin because some red yeast rice products may also contain a statin called lovastatin. Taking atorvastatin and red yeast rice products together can increase your risk of serious muscle and liver problems.
Does atorvastatin cause weight gain?
People who did take statins consumed more calories and fat over time, and gained more weight. The study also showed that statin users had a faster increase in body mass index (BMI) than those who didn’t use statins. There are a couple explanations that may be at play: Behavioral.