Lipitor (Statin Drug for Cholesterol) has a Potential in Kidney Disease

Lipitor Indications

Lipitor is a medications falling into the group of Atorvastatins. It is a hypolipidemic agent and inhibitor of HMG-CoA reductase.

• Primary hypercholesterolemia (heterozygous familial and non-familial hypercholesterolemia), combined (mixed) hyperlipemia, dysbetalipoproteinemia, familial endogenous hypertriglyceridemia, resistant to dietetic methods of treatment.
• Homozygotic hereditary hypercholesterolemia (in the capacity of addition to cholesterol-lowering treatment).
• Heart-vascular system disorders on the setting of dyslipidemia, secondary prophylaxis with the purpose of decrease of accumulation risk of death, myocardial infarction, and re-hospitalization due to cardiac angina.

Posology and Administration

Lipitor tablets are taken perorally at all times of the day, regardless of food intake. Initial dose of Lipitor is 10mg once a day. The dose may be changes with interval of not less than four weeks. Maximal daily dose is 80mg in a scoop.

• In case of initial hypercholesterolemia and combined hyperlipemia, Lipitor is prescribed by 10mg once a day. Therapeutic effect occurs within two weeks, and maximal effect is achieved within four weeks.
• In case of homozygous familial hypercholesterolemia, Lipitor is prescribed by 80mg once a day (decrease of low-density lipoproteins by 18-46%). Before starting therapy, a patient should be prescribed a standard cholesterol lowering diet which is to be observed during therapy with Lipitor.

Pharmacological Effect

Lipitor is a hypolipidemic agent falling into the group of statins. It is a selective competitive inhibitor of HMG-CoA reductase, enzyme turning 3-hydroxy-3methyl glutaryl coenzyme A into mevalonic acid which is a predecessor of sterols, including cholesterol.

Triglycerides and cholesterol in liver are included into the composition of very low-density lipoproteins. They get into blood plasma and are transported in peripheral tissues. Low-density lipoproteins are formed of very low-density lipoproteins during their interaction with receptors of low-density lipoproteins. Lipitor intake decreases the levels of cholesterol and lipoproteins in blood plasma due to inhibition of HMG-CoA reductase, synthesis of cholesterol in liver and increase of quantity of hepatic receptors of low-density lipoproteins on cells surface which leads to enhancement of seizure and katabolism of low-density lipoproteins.

Lipitor decreases production of low-density lipoproteins and causes pronounced and steady increase of low-density lipoprotein receptors activity. Lipitor decreases level of low-density lipoprotein in patients suffering from homozygous familial hypercholesterolemia which is not treated with lipid-lowering medications.

Lipitor decreases the level of total cholesterol by 30-45%, low-density lipoprotein – by 41-60%, Apo-B – by 35-50% and triglycerides – by 15-33%; causes level increase of cholesterol-high-density lipoprotein and Apo-A.

Lipitor administration is dose-dependent decreases the level of low-density lipoproteins in patients with homozygous familial hypercholesterolemia resistant to therapy, and other lipid-lowering medications.

Lipitor therapy decreases the risk of ischemic complications development (including lethal outcome of myocardial infarction) by 16%, risk of re-hospitalization due to cardiac angina accompanied by symptoms of myocardial ischemia – by 26%. Lipitor active substance doesn’t take cancerogenic or mutagenic effect.

Lipitor Contraindications

The medication is not to be taken in the following cases:

• Hypersensitivity to Lipitor components
• Active hepatic disorders (including chronic hepatitis, chronic alcoholic hepatitis)
• Increase of hepatic transaminases activity (more than by three times) of unclear genesis
• Liver decompensation
• Pregnancy
• Lactation period

Lipitor should be administered with caution in case of severe electrolyte disturbance, endocrine and metabolic disorders, alcoholism, hepatic diseases in the past medial history, arterial hypotension, severe acute infections, uncontrolled cramps, major surgeries, traumas, pediatric use (efficiency and safety of administration are not confirmed).

Side-Effects of Lipitor

Nervous system: oftener than 2% – insomnia, vertigo; rarer than 2% – headache, asthenia, sickliness, drowsiness, unusual dreams, amnesia, paresthesia, peripheric neuropathy, emotional instability, ataxia, facial nerve palsy, hyperkinesis, depression, hyperesthesia, loss of consciousness.

Sensory organs: rarer than 2% – amblyopia, singing in the ears, xerosis, accommodation disorder, blood effusion in eyes, deafness, glaucoma, parosmia, taste-blindeness, dysgeusia.

Alimentary system: oftener than 2% – nausea; rarer than 2% – epigastric burning, constipation, diarrhea, gases, gastralgia, stomachache, anorexia, decrease or increase of appetite, dryness in mouth, belch, odynophagia, vomit, stomatitis, esophagitis, glossitis, canker of oral mucosa, gastroenteritis, hepatitis, gallstone colic, cheilitis, peptic ulcer, pancreatitis, cholestatic jaundice, hepatic failure, rectal bleeding, melena, ulaemorrhagia, tenesmus.

Respiratory apparatus: oftener than 2% – bronchitis, rhinitis; rarer than 2% – pneumonia, labored breathing, bronchial allergy, nasal bleeding.

Cardio-vascular system: rarer than 2% – chest pain, rarer than 2% – tachycardia, vasodilation, blind headache, postural hypotension, arterial blood pressure increase, phlebitis, arrhythmia, cardiac angina.

Hemopoietic system: rarer than 2% – anemia, lymphoadenopathy, thrombocytopenia.

Supporting-motor apparatus: oftener than 2% – arthritis; rarer than 2% – myotonia, bursitis, peritendinitis, myitis, myopathia, arthralgia, myodynia, rhabdomyolysis, loxia, great tonicity of contracture.

Urinary system: oftener than 2% – urogenital infections, peripheral edemas; rarer than 2% – dysuria (including pollakiuria, nocturnal enuresis, urinary incontinence or retention of urine, urgency of urination), nephritis, haematuria, vaginal bleeding, metrorrhagia, epididymitis, decreased libido, impotency, impairment of ejaculation.

Skin covering: oftener than 2% – alopecia, xerodermia, excessive sweating, weeping dermatitis, seborrhea, ecchymoma, petechia.

Allergic reactions to Lipitor ingredients: rarer than 2% – rash, itching, contact dermatitis; rare – urticarial fever, angioedema, swelling of the face, photosensitivity, anaphylaxis, erythema multiforme (including Stevens Johnson’s syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Safety Note

Lipitor therapy may cause increase of CPK index which is to be taken into account in case of differential diagnostics of retrosternal pain. It is important to control hepatic indicators regularly before therapy course, in 6 and 12 weeks after the initial intake of the remedy or after Lipitor dosage increase, as well as during the whole period of application (until complete normalization of patient’s condition). Increased level of hepatic transaminases is generally observed within the first three months of medications usage.

Drug Interaction

In case of co-administration of Lipitor with CsA cyclosporine A, fibrates, erythromycin, clarithromycin, immune-suppressive agents, antifungal remedies (belonging to azoles) and nicotinamide, Lipitor concentration n blood plasma increases.

• Antacids decrease concentration by 35% (influence of cholesterol doesn’t change).
• Combination of Lipitor with protease inhibitors known as CYP3 A4 inhibitors is accompanied by increase of medication’s concentration in blood plasma.
• Digoxin combined with Lipitor (80mg a day) causes enhancement of digoxin concentration by 20%, the same is caused by co-administration with norethindrone and ethinylestradiol.