Atorvastatin

Atorvastatin is an active ingredient used to treat lipid metabolism disorders and prevent cardiovascular disease. It inhibits the formation of cholesterol and lowers LDL. Atorvastatin belongs to the group of statins. It is usually available as atorvastatin calcium trihydrate and is a white, crystalline powder that is only slightly soluble in water.

Atorvastatin inhibits the liver enzyme HMG-CoA reductase. This is responsible for cholesterol production. The active ingredient slows down the conversion of HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) into mevalonate, the salt of mevalonic acid. This slowdown leads to an increase in the number of LDL receptors on the cell surface in the liver. As a result, more LDL is absorbed into the liver cells and therefore less of it is in the blood. Atorvastatin also lowers VLDL-C (very low-density lipoprotein cholesterol), triglycerides and IDL (intermediate density lipoprotein and apolipoprotein B). Atorvastatin also increases HDL-C (high-density lipoprotein cholesterol).

Atorvastatin is metabolized in the liver, mainly by the enzyme CYP3A4. It is dose-dependent, i.e. the more active ingredient is administered, the higher the concentration in the blood. Due to the massive first-pass effect of atorvastatin, the bioavailability, i.e. the percentage of the active substance available in the blood, is only 14%. The first-pass effect occurs with most active ingredients that are absorbed in the stomach or small intestine. The active substance is absorbed through the mucous membrane of the stomach or small intestine and transported through the portal vein (vena portae) to the liver. In the liver, before the active ingredient enters the systemic circulation, it is metabolized for the first time, so that the active ingredient is then available to the body to a lesser extent. The first-pass effect has a major influence on the bioavailability of the respective active ingredients in the body. The half-life, i.e. the time the body needs to excrete half of the active ingredient, is around 14 hours. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active ingredient in the blood plasma (liquid cell-free part of the blood), is reached after 1-2 hours.

Always take atorvastatin exactly as described in the package leaflet or as advised by your doctor.

Adults:

The usual recommended dose for the prevention of cardiovascular disease is initially 10-20 mg once a day. If the risk is higher, 40 mg once a day may be started.

The maintenance dose is between 10-80 mg daily.

The maximum daily dose of 80 mg should NOT be exceeded.

Children & adolescents:

Use in children and adolescents is intended only for familial hypercholesterolemia and only by physicians experienced in pediatric prescribing.

The usual recommended dose is initially 10 mg daily and can be increased up to 80 mg per day depending on the response.

The maximum daily dose is also 80 mg .

Children under 10 years of age should NOT be treated with atorvastatin!

The following side effects may occur:

Frequent:

• Sinusitis
• Pain in the throat
• nosebleeds
• allergic reactions
• increased blood sugar levels
• increased creatine kinase levels in the blood
• headaches
• nausea
• constipation
• flatulence
• indigestion
• diarrhea
• Joint, muscle and back pain
• Altered liver values

Occasionally:

• Loss of appetite
• Weight gain
• Decreased blood sugar levels
• nightmares
• insomnia
• dizziness
• numbness in extremities
• Decreased sensation of touch and pain
• altered sense of taste
• memory loss
• blurred vision
• ringing in the ears
• vomiting
• belching
• Upper and lower abdominal pain
• pancreatitis
• inflammation of the liver
• (Skin) rash
• itching
• hives
• hair loss
• neck pain
• Muscle fatigue
• fatigue
• malaise
• Feeling of weakness
• Chest pain
• swelling of the ankle
• elevated temperature
• Positive test for white blood cells in the urine

Rarely:

• severe allergic reactions
• severe peeling and swelling of the skin with blistering, fever and pink to red spots
• Abnormal muscle atrophy (rhabdomyolysis)
• muscle weakness
• muscle sensitivity
• muscle pain
• muscle tear
• visual disturbance
• Unexpected bleeding and bruising
• jaundice
• Tendon injury

Very rare:

• wheezing breathing
• Chest pain or tightness in the chest
• Lupus-like syndrome
• Swelling
• Hearing loss
• Gynecomastia

Frequency unknown:

• persistent muscle weakness
• Myasthenia gravis

Interactions may occur if the following medicines are taken at the same time:

• Medications that affect the immune system, e.g. Ciclosporin
• Antibiotics or medicines for the treatment of fungal infections, e.g. erythromycin, clarithromycin, telithromycin, ketoconazole, itraconazole, voriconazole, fluconazole, posaconazole, rifampicin, fusidic acid
• Medication to regulate blood lipid levels, e.g. gemfibrozil, fibrates, colestipol
• Calcium blockers, e.g. amlodipine, diltiazem
• Medication for cardiac arrhythmia
• Letermovir
• Medication for the treatment of HIV infections
• Medication for the treatment of hepatitis C
• Ezetimibe
• warfarin
• oral contraceptives
• stiripentol
• cimetidine
• phenazone
• colchicine
• antacids
• St. John's wort
• Grapefruit juice
• Alcohol

Atorvastatin must NOT be taken in the following cases

• if you are allergic to atorvastatin
• if you have liver disease
• with altered liver values
• women of childbearing age without adequate contraception
• during pregnancy
• during breastfeeding
• when taking a combination of glecaprevir and pibrentasvir

Atorvastatin can be taken from the age of 10 .

Pregnancy

Atorvastatin should NOT be used during pregnancy, as the safety of the active substance has not been proven. There are a few reports of increased risks of malformations or congenital heart defects.

Atorvastatin should only be used in women of childbearing age if a suitable contraceptive method is used.

Lactation

Atorvastatin should NOT be used during breastfeeding, as there are no data on safety during breastfeeding. Due to the possibility of serious side effects, atorvastatin should not be used during breastfeeding.

The first synthesis of atorvastatin was carried out in 1985 by Dr. Bruce Roth. It was approved in the USA in 1996. In the EU for the first time in 1997. Atorvastatin was the most frequently prescribed cholesterol-lowering drug in Germany in 2021. Atorvastatin is also one of the most frequently prescribed medications on the global market.