Atorvastatin: What it is, What to Use, Side Effects and Contraindications of I.Randi

Generality

Atorvastatin is an active ingredient used to reduce excessively high levels of lipids in the blood (cholesterol and triglycerides).

Atorvastatin - Chemical Structure

Belonging to the statin group, atorvastatin can be used either alone, as a single agent, or in combination with other active ingredients .

To carry out its activity, atorvastatin must be taken orally ; in fact, the medicines that contain it are formulated in the form of tablets to be taken by mouth .

Dispensing of atorvastatin-based medicines can take place in the pharmacy only upon presentation of a specific repeatable medical prescription .

Examples of Medicinal Specialties Containing Atorvastatin

  • Arkas®
  • Atoris®
  • Atorvastatin Aurobindo®
  • Atorvastatin DOC®
  • Atozet® (in association with ezetimibe)
  • Euvascor® (in association with perindopril)
  • Stapressial® (in combination with amlodipine and perindopril)
  • Torvast®
  • Trinomia® (in association with acetylsalicylic acid and ramipril)

Therapeutic indications

When is the use of Attorastastatin indicated?

The use of atorvastatin is indicated to reduce excessively high levels of blood lipids (cholesterol and triglycerides).

The use of this active ingredient, however, should be done only when lifestyle changes (diet, physical activity, etc.) have not been successful in lowering excessively high concentrations of lipids in the blood.

Atorvastatin can also be administered even if blood cholesterol levels are not elevated in order to prevent the onset of cardiovascular events in patients considered to be at risk.

Did you know that ...

Atorvastatin-based medicines are commercially available in association with other active ingredients - such as acetylsalicylic acid, amlodipine, ramipril, perindopril - used for the management / prevention of cardiovascular risk in patients with high cholesterol levels.

Furthermore, in some medicines, atorvastatin is contained in combination with ezetimibe, another active ingredient that can reduce blood cholesterol levels and, in particular, LDL levels.

Warnings

Warnings and Precautions for the use of Atorvastatin

Before taking atorvastatin medicines, you should tell your doctor if:

  • You are suffering or have suffered in the past from liver disease;
  • You suffer from severe respiratory failure;
  • It has a history of stroke;
  • You suffer from hypothyroidism;
  • You are suffering from muscle problems or diseases;
  • You suffer from constant muscle weakness;
  • Fusidic acid (an antibiotic) is being taken or has recently been taken;
  • You are over 70 years of age;
  • Significant amounts of ethyl alcohol are consumed.

In any case, as a precautionary measure, before taking atorvastatin-based medicines, it is advisable to inform your doctor of your health conditions, informing you of the possible presence of disorders or diseases of any kind, even if not indicated in the above list .

Interactions

Interactions of atorvastatin with other drugs

Because of the drug interactions that could occur and because of the risk of occurrence / exacerbation of even serious side effects (such as rhabdomyolysis), atorvastatin should not be taken in conjunction with certain types of drugs.

In detail, before starting treatment with atorvastatin, you must tell your doctor if you are taking, or if you have recently been taken:

  • Other drugs used to decrease cholesterol levels in the blood (such as, for example, fibrates);
  • Fusidic acid and other types of antibiotic drugs (eg, erythromycin);
  • Some types of antifungal drugs (eg, ketoconazole);
  • Immunosuppressive drugs (for example, cyclosporine);
  • Antiviral drugs used against HIV and hepatitis C;
  • Calcium channel blockers;
  • Anticonvulsant drugs;
  • Anti-gout drugs;
  • Anticoagulant drugs such as warfarin;
  • Oral contraceptives;
  • Digoxin;
  • Antacids;
  • cimetidine;
  • phenazone;
  • Hypericum (or St. John's wort), its derivatives and products that contain it.

However, before starting atorvastatin therapy (alone or in combination with other active ingredients), it is necessary to tell the doctor if you are taking, or have recently taken, drugs or products of any kind. including medicines without a medical prescription (SOP), over-the-counter drugs (OTC), herbal and herbal products and homeopathic products.

Interactions with Foods and Beverages

During treatment with atorvastatin it is good to avoid taking excessive amounts of alcohol and grapefruit juice, as these drinks can alter the activity of the active substance in question.

Side effects

Side effects caused by the intake of atorvastatin

Like any other active ingredient, atorvastatin can also cause side effects, although not all patients experience or experience them in the same way. In fact, each person reacts subjectively to the administration of the drug manifesting side effects that are different in type and intensity, or not manifesting them at all.

However, below are some of the major side effects that can be experienced during atorvastatin treatment.

Musculoskeletal and connective tissue disorders

Atorvastatin therapy may give rise to:

  • Myalgia;
  • Muscle spasms;
  • Muscle fatigue;
  • arthralgia;
  • Joint swelling;
  • Backache;
  • myopathy;
  • myositis;
  • Rhabdomyolysis;
  • Tendinopathy, sometimes complicated by rupture.

Hepatobiliary disorders

Atorvastatin intake could lead to hepatitis, cholestasis and liver failure.

Nervous system disorders

During treatment with atorvastatin may occur:

  • Headache;
  • dizziness;
  • paresthesia;
  • Hypoaesthesia;
  • dysgeusia;
  • Amnesia;
  • Peripheral neuropathy.

Gastrointestinal disorders

Atorvastatin intake could lead to the appearance of:

  • Nausea or vomiting;
  • Dyspepsia;
  • Belching;
  • Diarrhea or constipation;
  • Flatulence;
  • Abdominal pain;
  • Pancreatitis.

Skin and subcutaneous tissue disorders

Atorvastatin therapy may promote the appearance of:

  • Urticaria;
  • Itch;
  • Skin eruptions;
  • Alopecia;
  • Erythema multiforme, Stevens-Johnson syndrome or toxic epidermal necrolysis.

Alteration of laboratory test results

Atorvastatin intake may:

  • Alter the results of liver function tests;
  • Increase blood levels of creatine phosphokase;
  • Bring to positive leukocyte urine test.

Other side effects

Other side effects that could occur during treatment with atorvastatin consist of:

  • Allergic reactions, even serious, in sensitive individuals;
  • Thrombocytopenia;
  • Sleep disorders, such as insomnia and nightmares;
  • Epistaxis;
  • Laryngopharyngeal pain;
  • Visual disturbances (eg, blurred vision);
  • Hearing loss;
  • Tinnitus;
  • Hyperglycemia or hypoglycemia;
  • Anorexia;
  • Weight gain;
  • Gynecomastia;
  • General malaise;
  • Asthenia and fatigue;
  • Temperature;
  • Chest pain;
  • Peripheral edema.

Overdose

In the event of an overdose - ascertained or presumed - from atorvastatin, it is necessary to contact the doctor immediately or go to the nearest emergency department, taking care to bring along the packaging of the medicinal product used.

Unfortunately, there is no specific antidote; therefore, if excessive doses of atorvastatin are taken, the treatment will be symptomatic and supportive.

Action mechanism

How does Attorvastatin work?

Atorvastatin is able to reduce blood cholesterol levels by inhibiting the enzyme 3-hydroxy-3-metiglutaryl coenzyme A reductase (HMG-CoA reductase). This enzyme is responsible for the conversion of 3-hydroxy-3-methylglutaryl coenzyme A into mevalonate, a fundamental precursor in the biosynthesis of sterols, including cholesterol.

In particular, atorvastatin performs its action in the liver; therefore, it inhibits the production of endogenous cholesterol in the liver . Furthermore, this active ingredient is able to favor the increase in the number of LDL receptors on the cell surface, consequently leading to an increase in LDL uptake and catabolism.

Method of use and Posology

How to take atorvastatin

Atorvastatin is available as tablets for oral use which should be swallowed whole with a little water. The tablets can be taken at any time of the day, with or without food . However, it is advisable to take atorvastatin at the same time each day.

The dose of active ingredient to be taken will be established by the doctor on an individual basis for each patient.

However, the usual starting dose used in therapy is 10 mg of active ingredient per day. After that, the doctor can gradually increase the amount of drug administered until the ideal maintenance dose is reached for each patient. In any case, the maximum dose of 80 mg of atorvastatin per day should never be exceeded.

Did you know that ...

Before starting the treatment, the doctor will prescribe the patient a proper low cholesterol diet . This diet should also be followed by the patient during atorvastatin therapy.

Pregnancy and breastfeeding

Can Atorvastatin be taken during pregnancy and during breastfeeding?

Animal studies have shown that atorvastatin can cause reproductive toxicity and is excreted in breast milk. However, the safety in use of atorvastatin during pregnancy and breastfeeding in humans has not yet been established.

For these reasons, in pregnancy and during breastfeeding, the use of atorvastatin is contraindicated .

Contraindications

When attorvastatin should not be used

Atorvastatin should not be administered in the following cases:

  • Known hypersensitivity to atorvastatin itself and / or to one or more of the other active ingredients and / or excipients contained within the medicinal product that should be used;
  • In patients who have suffered or who suffer from liver disease;
  • In women of child-bearing age who do not use methods of contraception;
  • In women who are planning a pregnancy;
  • In pregnancy and during breastfeeding.

Please note

For more in-depth information on indications, warnings and precautions, interactions, side effects, use during pregnancy and during lactation and contraindications of the different atorvastatin-based medicines, it is advisable to consult your doctor and read the leaflet carefully illustrative of the medicinal specialty that one needs to use.

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