Lipitor

$ 111.94$ 335.82

Category: Heart & Cholesterol
Commercial name: Lipitor
Active ingredient: Atorvastatin
Production form: Pills
Available dosage: 10 mg, 20 mg, 40 mg

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Description

Lipitor (Atorvastatin). Dosage, Side Effects, Interactions

Lipitor (Atorvastatin) is used to treat high blood fat levels (LDL levels) when a low-fat diet has not worked as desired. The active ingredient primarily reduces elevated cholesterol and triglyceride levels. Atorvastatin is also used to prevent arteriosclerosis, heart attacks and strokes.

Application

Statins such as atorvastatin are used to lower total cholesterol and specifically LDL cholesterol. This is indicated as a preventive measure , particularly 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.

Early administration of statins such as atorvastatin in acute coronary syndrome is debated and practiced in some clinics. So far, however, its benefit has only been proven for individual patient groups.

 

How Lipitor (Atorvastatin) works

Like all statins, atorvastatin interferes with 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 form LDL receptors on the plasma membrane. To compensate for the lack of cholesterol in the cell, more LDL cholesterol is taken up from the plasma. Depending on the dose, the total cholesterol level drops 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 reduced. Apolipoprotein B is suspected to be a risk factor for stroke and heart attack . With the falling plasma level, the risk of rupturing atheromatous plaques and their progression is reduced. In addition, atorvastatin administration increases plasma HDL cholesterol levels by 5-10%.

In addition to the effect on cholesterol levels, other pleiotropic effects are attributed 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.

Pharmacokinetics

The lipophilic atorvastatin is a prodrug. After oral administration, up to 90% is absorbed in the gastrointestinal tract. The bioavailability is 25% on average, but drops to about 13% when consumed at the same time. The maximum plasma concentration is reached almost two hours after administration, the plasma half-life after about 14 hours. At least 98% of atorvastatin is bound to plasma proteins.

Atorvastatin is taken up by the liver cells via organic anion-transporting polypeptides, OATP for short, and after the first passage is broken down into two active metabolites. The  cytochrome P450 isoenzyme  CYP3A4  further metabolizes the prodrug in the liver cells to ortho- and para-hydroxylated derivatives and various beta-oxidation products. The metabolites are eliminated via the bile. A small proportion is also excreted renally.

Due to first-pass metabolism, the elimination half-life of atorvastatin is approximately 30 hours, which is significantly longer than that of other statins.

 

Dosage of Lipitor (Atorvastatin)

Atorvastatin is available as tablets containing 10 mg, 20 mg, 40 mg, and 80 mg of the active ingredient. Irrespective of the indication for therapy, therapy should be started after an initial change in diet with a dose of 10 mg once a day. 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 hypercholesterolaemia, a combination of 40 mg atorvastatin and a bile acid sequestrant ion exchange resin can be used instead of a maximum daily dose of 80 mg. According to studies, a dose of 10 mg per day is sufficient for the purpose of primary prevention of cardiovascular diseases. However, this should be checked and adjusted according to the current guidelines for the individual patient.

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.

 

Side effects of Lipitor (Atorvastatin)

Often:

  • nasopharyngitis
  • allergic reaction
  • hyperglycemia
  • headache
  • pharyngolaryngeal pain
  • nosebleeds
  • Constipation, bloating, nausea, diarrhea
  • dyspepsia
  • myalgia
  • arthralgia
  • pain in the extremities
  • muscle spasms
  • joint swelling
  • back pain
  • altered liver function tests
  • increased blood creatine phosphokinase

Occasionally:

  • hypoglycemia
  • weight gain
  • anorexia
  • nightmares
  • insomnia
  • drowsiness
  • paresthesias
  • hypoesthesia
  • Taste disturbance
  • amnesia
  • blurred vision
  • tinnitus
  • Vomit
  • upper and lower abdominal pain
  • burping
  • pancreatitis
  • hepatitis
  • Urticaria , skin rash
  • pruritus
  • alopecia
  • neck pain
  • muscle weakness
  • malaise
  • asthenia
  • chest pain
  • peripheral edema
  • exhaustion
  • Fever
  • positive test for white blood cells in the urine

Rarely:

  • thrombocytopenia
  • peripheral neuropathy
  • visual disturbances
  • cholestasis
  • angioneurotic edema
  • bullous rash including erythema multiforme
  • Stevens-Johnson Syndrome
  • toxic epidermal necrolysis
  • myopathy
  • myositis
  • rhabdomyolysis
  • tendinopathy (sometimes complicated by a tendon rupture)

Very rare:

  • anaphylactic reactions
  • hearing loss
  • liver failure
  • gynecomastia

Interactions

All drugs that are also metabolised by, inhibit or induce 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 pharmaceuticals are administered at the same time, a prior risk-benefit assessment is recommended, as well as simultaneous clinical monitoring of the patients.

The following substances have also shown interactions with atorvastatin in studies:

  • Digoxin : slightly increased steady-state plasma concentration of digoxin
  • Colestipol : decrease in atorvastatin plasma levels
  • Contraceptives : increase in plasma levels of norethisterone and ethinyl estradiol
  • Coumarin derivatives : transient decrease in prothrombin time. In the case of simultaneous administration, close monitoring of the thromboplastin time is recommended in the first phase of therapy
  • Grapefruit juice: increase in side effects

Contraindication

The use of atorvastatin is contraindicated in the following cases:

  • Hypersensitivity to atorvastatin or other components of the respective preparation
  • Active liver disease or unexplained, persistent elevations in serum transaminases to three times the upper limit of normal
  • pregnancy and breast feeding period
  • Women of childbearing potential who are not using an appropriate method of contraception
  • children
  • Impaired liver function

Pregnancy

Women of childbearing potential should only use atorvastatin in combination with appropriate contraceptive measures. Atorvastatin is contraindicated during pregnancy. Reproductive toxicity has been demonstrated in animal studies.

 

Lactation

There are insufficient data on the use of atorvastatin during breast-feeding. Since atorvastatin and active metabolites could be detected in breast milk in animal experiments on rats, atorvastatin is contraindicated during lactation.

 

Driving ability

There are no known effects.

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Additional information

Dosage

10 mg, 20 mg, 40 mg

Quantity

30, 60, 90, 120, 180

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