Pravastatin - instructions for use, doses, side effects, contraindications

Active substancePravastatinPravastatin

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Pravastatin

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VALENTA PHARM, PAO Russia

Dosage form: & nbsppills

Composition:

1 tablet contains:

active substance: pravastatin sodium 0.010 g or 0.020 g;

Excipients: potato starch, milky sugar, aerosil, magnesium oxide, kollidon CL-M or Kollidon CL, calcium stearate.

Description:Tablets are white or almost white in color, flat-cylindrical with a bevel.

Pharmacotherapeutic group:lipid-lowering agent - HMG-CoA reductase inhibitor

ATX: & nbsp

C.10.A.A.03 Pravastatin

Pharmacodynamics:

Pravastatin belongs to the class of statins (inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A-reductase (HMG-CoA reductase), a key enzyme of endogenous cholesterol biosynthesis whose reversible inhibition of activity leads to suppression of cholesterol synthesis in the stage of mevalonic acid and a moderate decrease in it intracellular contents. Pravastatin compensatory increases the number of low-density lipoprotein (LDL) receptors on the cell surface, increases the catabolism of LDL cholesterol through the receptors, and increases the excretion of LDL in the bloodstream. Oppresses the synthesis in the liver of very low density lipoproteins (VLDL),which are the precursors of LDL; slightly increases the plasma content of high-density lipoprotein (HDL), having anti-atherogenic properties, reduces the content of total cholesterol and triglycerides. It has a tissue selectivity: its suppressive activity is most pronounced in those tissues where synthesis cholesterol is carried out with maximum speed, in particular, in the liver, iliac gut.

Unlike other inhibitors of HMG-CoA reductase, less affects the synthesis of cholesterol in other tissues.

Pharmacokinetics:

Absorption is fast (30-54% of the administered dose), bioavailability is 15-20% (due to the effect of "first passage" through the liver). Admission for 1 hour before meals or along with food reduces systemic bioavailability and specific activity. The concentration of pravastatin in blood plasma is directly proportional to the administered dose. The maximum concentration in the blood plasma is reached after 1-1.5 hours. The connection with blood plasma proteins is 50%. Penetrates into breast milk.

Metabolized in several ways: isomerization to 6-epipravastatin and 3-hydroxy isomer, enzymatic hydroxylation of the ring and subsequent oxidation to the ketone, oxidation of the ester or carboxyl end of the chain, conjugation.The main products of metabolism - 3-hydroxy isomers - have a specific activity, which is from 1/14 to 1/10 of the original. The half-life is 1.3-2.7 hours.

It is excreted by the kidneys - 20%, through the intestine - 70%. 47% of the total clearance is in the kidneys and 53% in the extrarenal pathway (for example, bile and biotransformation). In connection with the presence of 2 ways of excretion, it is possible to increase the excretory excretion in one of them in case of violation of the other, as well as the development of cumulation of pravastatin and its metabolites in renal and / or hepatic insufficiency.

Indications:

Hypercholesterolemia (primary hyperlipidemia IIa and IIb type, with the exception of family homozygous) (with ineffectiveness of diet therapy in patients with an increased risk of coronary atherosclerosis).

Primary hypercholesterolemia in combination with hypertriglyceridemia.

Contraindications:

Hypersensitivity, acute illness or exacerbation of chronic liver disease, liver failure; persistent change in functional liver samples of unknown etiology; pregnancy, lactation, age under 18 (safety and efficacy not established).

Carefully:

With alcoholism, after organ transplants, with immunosuppressive therapy and renal insufficiency, liver diseases in the anamnesis.

Dosing and Administration:

Before starting therapy with the drug Pravastatin The patient should be prescribed a standard diet for lowering cholesterol. During the treatment with the drug this diet should be observed.

The drug is taken orally, regardless of food intake in the initial dose of 10-20 mg once, before bedtime. With a significant increase in the concentration of cholesterol in the plasma (more than 300 mg / dl), the initial dose is increased to 40 mg once a day at bedtime. The maximum therapeutic effect develops within 4 weeks from the start of treatment. During this period, dose adjustment is possible depending on the dynamics of lipid concentration in the blood plasma.

Patients receiving concomitantly ciclosporin in combination with other immunosuppressants, treatment starts with a dose of 10 mg with a gradual increase. The maximum dose is 20 mg.

With hepatic or renal failure, the initial dose should not exceed 10 mg.

For elderly patients, a dose of 20 mg / day is usually effective.

Side effects:

From the nervous system: dizziness, headache, dysfunction of cranial nerve (taste dysfunction, involuntary eye movement, facial nerve paresis), peripheral neuropathy, tremor, anxiety, insomnia (rarely), depression, amnesia, paresthesia.

From the sense organs: ophthalmoplegia, cataract progression.

From the gastrointestinal tract: nausea, loss of appetite, gastralgia, diarrhea or constipation, flatulence, hepatitis (including chronic active and cholestatic), fatty liver, cirrhosis or hepatic necrosis, hepatoma, increased activity "liver" enzymes (2-3 times compared with the norm) and an alkaline phosphatase, hyperbilirubinemia, hypercreatininemia (3 times the upper limit of the norm), it is theoretically possible - acute pancreatitis.

On the part of the organs of hematopoiesis: thrombocytopenia, leukopenia, hemolytic anemia, eosinophilia.

From the side of the musculoskeletal system: myalgia, myopathy, myositis, rhabdomyolysis.

From the genitourinary system: rarely a decrease in libido and potency.

Allergic reactions: skin rash, itching, lupus-like syndrome, anaphylactic shock, angioedema, dermatomyositis, vasculitis, purpura, toxic epidermal necrolysis (Lyell's syndrome), multiple-form exudative erythema (Stevens-Johnson syndrome).

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

Laboratory indicators: increased activity of creatine phosphokinase, myoglobinuria.

Other: gynecomastia, palpitation, respiratory failure, renal failure (due to rhabdomyolysis).

Overdose:

Symptoms: changes in the biochemical blood test.

Treatment: symptomatic.

Interaction:

Increases the effect of indirect anticoagulants and the risk of bleeding.

With simultaneous administration with acetylsalicylic acid, antacids, cimetidine, gemfibrozil, nicotinic acid and probucol, the bioavailability of these drugs does not change.

Compatible with diuretics, antihypertensive drugs, digitalis preparations, ACE inhibitors, blockers of "slow" calcium channels, beta-adrenoblockers, nitrates.

Fibrates, ciclosporin, erythromycin, a nicotinic acid increase the risk of myopathy; gemfibrozil increases the concentration of creatine phosphokinase in plasma and the risk of side effects from the musculoskeletal system.

Anion exchange resins (colestramine, colestipol) reduce AUC by 40-50% (pravastatin should be prescribed 1 hour before or 4 hours after taking these drugs).

Special instructions:

Before and during treatment, it is necessary to follow a diet that helps lower the cholesterol in the plasma.

Before the appointment, it is necessary to exclude secondary hypercholesterolemia, in particular, with poorly compensated diabetes mellitus, hypothyroidism, nephrotic syndrome, and dysproteinemia.

During the treatment it is necessary to control the transaminase content in the blood serum. In cases when there is a stable excess of activity of "liver" transaminases in relation to the upper limit of the norm 3 times or more, treatment should be stopped.

If there is a period of treatment with myalgia, muscle weakness and / or a significant increase in creatine phosphokinase, the possibility of developing myopathy should be considered. In such cases, the drug is canceled.

In patients receiving immunosuppressive drugs (ciclosporin), monitoring of the level of creatine phosphokinase and symptoms of rhabdomyolysis is mandatory.

If the current dose is skipped, the drug should be taken as soon as possible. If it's time for the next dose, do not double the dose.

Form release / dosage:

Tablets, 10 mg and 20 mg.

Packaging:

For 10 tablets in a planar cell package.

By 2, 3, 5 or 10 contour packs together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003029 / 01

Date of registration:14.08.2008

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Information update date: & nbsp26.08.2015

Illustrated instructions

Instructions

Pravastatin (Pravastatin)