Pravastatin (Pravastatinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Statins

Included in the formulation
  • Pravastatin
    pills inwards 
    VALENTA PHARM, PAO     Russia
    • АТХ:

    C.10.A.A.03   Pravastatin

    Pharmacodynamics:

    The drug inhibits 3-hydroxymethylglutaryl coenzyme A-reductase (HMG-CoA) in hepatocytes, which prevents its conversion to mevalonic acid. This leads to inhibition of cholesterol synthesis and, as a consequence, to a compensatory increase in the catabolism of LDL cholesterol, an increase in the number of receptors for LDL on the hepatocyte membrane, stimulation of the receptor-dependent endocytosis of LDL from blood plasma. Reducing the concentration of LDL cholesterol, VLDL and triglycerides (to a lesser extent) in blood plasma. In addition to lipid-lowering effects, statins have a positive effect on endothelial dysfunction (preclinical signs of early atherosclerosis), on the vascular wall, atheroma state, improve the rheological properties of blood, and possess antioxidant, antiproliferative properties.

    Pharmacokinetics:

    30-54% of the administered dose is absorbed, bioavailability is 15-20%. The connection with plasma proteins is 50%. The drug is metabolized in the liver (CYP3A3, 3A4). Metabolites of the drug are not active. The half-life is 1.3-2.7 hours. Excreted by the kidneys (20%), the gastrointestinal tract (70%).

    Indications:
    • Combined hypercholesterolemia and triglyceridemia
    • Hyperlipoproteinemia IIa and IIb types
    • Hyperlipidemia without CHD (reduced risk of myocardial infarction), atherosclerosis and CHD, including myocardial infarction (to slow the progression of atherosclerosis and reduce the likelihood of recurrent myocardial infarction)
    • Family hypercholesterolemia (in patients with a transplanted heart to reduce the likelihood of developing coronary angiopathy)
    ICD-10

    IV.E70-E90.E78.2   Mixed hyperlipidemia

    IV.E70-E90.E78.5   Hyperlipidemia, unspecified

    IX.I20-I25.I25   Chronic ischemic heart disease

    Contraindications:
    • Diseases of the liver
    • Increased activity of hepatic transaminases
    • Pregnancy and lactation
    • Hypersensitivity
    • Children, adolescence and adolescence (up to 18 years).
    Carefully:
    • Diseases of the liver
    • Kidney Diseases
    • After organ transplantation
    • With immunosuppressive therapy
    • Chronic alcoholism
    Pregnancy and lactation:

    Category FDA - X. The drug is contraindicated in pregnancy and breastfeeding.

    Dosing and Administration:

    Dosing regimen is individual. Recommended 10-40 mg orally once a day.Elderly patients, as well as patients with diseases of the liver and kidneys recommended a low dose of 10 mg.

    If there is no result within 4 weeks the dose is gradually increased to 40 mg. In most cases, the effective daily dose is 20 mg. For people receiving immunosuppressive drugs (ciclosporin), monitoring of the level is mandatory creatine phosphokinase and the symptoms of rhabdomyolysis.

    Side effects:

    From the side nervous system: vertigo, insomnia, amnesia, headache, involuntary eye movements, peripheral polyneuropathy, anxiety, depression, paresthesia, ophthalmoplegia, cataract progression.

    From the side skin integument: alopecia, photosensitivity, skin depigmentation, dry skin and mucous membranes.

    From the side musculoskeletal system: increased activity of creatine phosphokinase, myopathy, rhabdomyolysis, myalgia, myositis.

    From the side gastrointestinal tract: nausea, diarrhea, flatulence, increased activity of hepatic transaminases and alkaline phosphatase, hypercreatininemia, hepatitis, cirrhosis or necrosis of the liver, hepatoma, vomiting, abdominal pain, constipation, hyperbilirubinemia, fatty liver infiltration, acute pancreatitis.

    From the side blood: Thrombocytopenia, hemolytic anemia, leukopenia, eosinophilia.

    Other: decreased libido and potency, palpitation, myoglobinuria, gynecomastia, respiratory failure, renal failure (due to rhabdomyolysis).

    Overdose:

    Change in biochemical blood test. Treatment symptomatic: stimulation of vomiting, gastric lavage, reception of activated charcoal; it is necessary to monitor the liver function and the activity of creatine phosphokinase. There is no specific antidote.

    Interaction:

    Gemfibrozil, clofibrate, immunosuppressants (including ciclosporin), macrolides, a nicotinic acid, fenofibrate - increase the risk of rhabdomyolysis with acute renal failure (combined use is not recommended), risk of necrosis of skeletal muscles.

    Increases the effect of indirect anticoagulants.

    When used simultaneously with colestipol, colestyramine, the concentration of pravastatin in the blood plasma decreases, while the overall lipid-lowering effect is enhanced.

    Special instructions:

    During the treatment, it is necessary to monitor the lipid spectrum of the blood.

    The impact on the ability to drive vehicles and control mechanisms has not been studied.

    Instructions
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