Pravastatin
Pravastatin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Pravastatin
ATX code: C10AA03
Active ingredient: pravastatin (Pravastatin)
Manufacturer: PJSC "Valenta Pharmaceuticals" (Russia)
Description and photo update: 2019-28-11
Pravastatin is a hypolipidemic agent.
Release form and composition
The drug is produced in the form of tablets: flat-cylindrical, with a chamfer, almost white or white (10 pcs. In a blister strip, in a cardboard box of 2, 3, 5 or 10 packages and instructions for the use of Pravastatin).
1 tablet contains:
- active substance: pravastatin sodium - 10 or 20 mg;
- additional components: milk sugar, potato starch, calcium stearate, magnesium oxide, aerosil, Kollidon CL-M or Kollidon CL.
Pharmacological properties
Pharmacodynamics
Pravastatin belongs to the class of statins - inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A-reductase (HMG-CoA reductase), which is the main enzyme of endogenous cholesterol biosynthesis (Chs), the reversible suppression of the activity of which causes inhibition of Chs production at the mevalonic acid stage and a moderate decrease in its intracellular level.
Pravastatin provides a compensatory increase in the number of low density lipoprotein (LDL) receptors on the cell surface, an increase in LDL-C catabolism produced through receptors, and supports an increase in the excretion of LDL, located in the bloodstream. It prevents the synthesis of very low density lipoproteins (VLDL), which are the precursors of LDL, from the liver. Slightly increases the plasma level of high density lipoproteins (HDL), which exhibit antiatherogenic properties, reduces the level of total cholesterol and triglycerides (TG).
The inhibitory activity is most significant in those tissues where Xc is produced at the highest rate, for example, in the liver and ileum, since tissue selectivity is inherent in pravastatin. Due to this, unlike other inhibitors of HMG-CoA reductase, this lipid-lowering agent has a lesser effect on the production of Xc in other tissues.
Pharmacokinetics
Rapid absorption is characteristic of pravastatin (30–54% of the dose taken). Its bioavailability is 15–20% (as a result of the effect of the first passage through the liver). Oral administration 1 hour before meals or at the same time as meals reduces the specific activity and systemic bioavailability of the drug. The plasma level in the blood is directly proportional to the administered dose. The maximum concentration (C max) in plasma is observed 1–1.5 hours after administration. The substance binds to blood plasma proteins by 50%, it is detected in breast milk.
Pravastatin is metabolized in several ways: isomerization to 6-epipravastatin and 3-hydroxy isomer; enzymatic hydroxylation of the ring and further oxidation to ketone; oxidation of the ether or carboxyl ends of the chain; conjugation. The main metabolic products are 3-hydroxy isomers, which differ in specific activity, which can range from 1/14 to 1/10 of the initial one. The half-life (T 1/2) varies from 1.3 to 2.7 hours, the drug is excreted through the intestine - 70% and by the kidneys - 20%.
Up to 47% of the total clearance is accounted for by renal excretion, and the remaining 53% - by excretion through other extrarenal urinary tract, excretion with bile, and biotransformation. As a result of the presence of two ways of elimination, a compensatory increase in excretion along one of them is possible if the other is disturbed. At the same time, against the background of renal and / or hepatic insufficiency, there is a risk of accumulation of the basic substance and its metabolites.
Indications for use
- hypercholesterolemia - primary hyperlipidemia of types IIa and IIb, except for familial homozygous (against the background of an increased risk of developing coronary atherosclerosis in case of ineffective diet therapy);
- primary hypercholesterolemia in combination with hypertriglyceridemia.
Contraindications
Absolute:
- acute diseases or exacerbations of chronic liver damage;
- persistent change in liver function tests of unknown origin;
- liver failure;
- age up to 18 years;
- pregnancy and lactation;
- hypersensitivity to any of the components of Pravastatin.
Relative (use the drug with caution):
- a history of liver disease;
- period after organ transplantation;
- immunosuppressive therapy and renal failure;
- alcoholism.
Pravastatin, instructions for use: method and dosage
Pravastatin tablets are intended for oral administration. The drug is taken once a day before bedtime, regardless of the diet.
Recommended dosage: The initial dose is 10–20 mg. With a significant increase in the plasma content of Xc in the blood (more than 300 mg / dl), the initial dose is increased to 40 mg.
The development of the maximum therapeutic effect is recorded within 4 weeks from the beginning of the course. During this period, taking into account the dynamics of plasma lipids, it is possible to adjust the dose.
Patients receiving cyclosporine in combination with other immunosuppressants at the same time, the course of treatment should be started with a dose of 10 mg, followed by a gradual increase. The maximum daily dose of Pravastatin is 20 mg.
Before and during therapy, a standard diet should be followed to lower plasma cholesterol levels.
Side effects
- immune system: itching, skin rash, lupus-like syndrome, vasculitis, purpura, dermatomyositis, angioedema, anaphylactic shock, erythema multiforme (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome);
- nervous system: headache, dizziness; involuntary eye movements, impaired taste and paresis of the facial nerve due to dysfunction of the cranial nerves; anxiety, tremor, insomnia (rarely), paresthesia, peripheral polyneuropathy, amnesia, depression;
- hematopoietic organs: eosinophilia, thrombocytopenia, hemolytic anemia, leukopenia;
- sense organs: cataract progression, ophthalmoplegia;
- skin and subcutaneous tissues: dry skin and mucous membranes, skin depigmentation, alopecia, photosensitivity;
- digestive system: decreased appetite, nausea, gastralgia, flatulence, diarrhea or constipation, hyperbilirubinemia, increased activity of hepatic transaminases (2-3 times compared with the norm) and alkaline phosphatase (ALP), hypercreatininemia 3 times higher than the upper limit of the norm (UHN); isolated cases - hepatitis (including chronic cholestatic and active), fatty liver, hepatoma, cirrhosis or liver necrosis, acute pancreatitis;
- laboratory indicators: an increase in the activity of creatine phosphokinase (CPK), myoglobinuria;
- genitourinary system: rarely - decreased libido and potency;
- musculoskeletal system: myositis, myalgia, myopathy, rhabdomyolysis;
- other reactions: palpitations, gynecomastia, respiratory failure, renal failure (due to rhabdomyolysis).
Overdose
Symptoms of a pravastatin overdose can be changes in the biochemical blood test. In this case, palliative therapy is recommended.
special instructions
Before starting therapy, it is required to exclude secondary hypercholesterolemia, especially against the background of compensated diabetes mellitus, dysproteinemia, hypothyroidism, and nephrotic syndrome.
During treatment, the level of transaminases in the blood serum should be monitored. If there is a stable increase in the activity of hepatic enzymes 3 times higher than VGN, Pravastatin should be discontinued.
If myalgia, muscle weakness and / or a pronounced increase in CPK develop during treatment, the possibility of myopathy should be considered. When the diagnosis is confirmed, it is required to cancel therapy.
Persons undergoing therapy with immunosuppressive drugs (cyclosporine) need mandatory monitoring of the plasma concentration of CPK and the symptoms of rhabdomyolysis.
If you accidentally miss the current dose of Pravastatin, you must take it as soon as possible. If it is time to take the next dose, you should not double the dose in order to compensate for the missed dose.
Application during pregnancy and lactation
During pregnancy, taking Pravastatin tablets is contraindicated.
If drug therapy is necessary during lactation, the issue of transferring the child to artificial feeding should be resolved.
Pediatric use
Due to the fact that in children and adolescents the safety and efficacy of drug treatment have not been established, its use in patients under 18 years of age is contraindicated.
With impaired renal function
In patients with renal insufficiency, the initial dose of Pravastatin should not exceed 10 mg.
For violations of liver function
In the presence of liver disease in the acute phase or exacerbation of chronic liver damage, a persistent increase in the activity of hepatic transaminases of unknown origin, liver failure, Pravastatin therapy is contraindicated.
Patients with a history of liver disease should use the drug with caution.
Use in the elderly
Elderly patients are advised to start treatment with a lipid-lowering agent in a daily dose of 10 mg, gradually increasing it to the most effective dose of 20 mg.
Drug interactions
- indirect anticoagulants: the effect of these funds increases and the threat of bleeding is aggravated;
- antihypertensive drugs, diuretics, digitalis drugs, slow calcium channel blockers, angiotensin-converting enzyme inhibitors (ACE inhibitors), β-blockers, nitrates: combined use of these drugs with pravastatin is allowed;
- acetylsalicylic acid, probucol, antacids, gemfibrozil, cimetidine, nicotinic acid: there is no change in the bioavailability of these agents;
- anion exchange resins (colestipol, colestyramine): the area under the concentration-time curve (AUC) of these agents decreases; it is recommended to take pravastatin 1 hour before or 4 hours after using these drugs;
- gemfibrozil: an increase in the plasma concentration of CPK is recorded and the threat of undesirable reactions from the locomotor system is aggravated;
- erythromycin, cyclosporine, fibrates, nicotinic acid: the threat of myopathy is increasing.
Analogs
The analogues of Pravastatin are Lipostat, Pravapres, Simvastatin, Vasilip, Rosufast, Atoris, Liprimar, Rosuvastatin, Atorvastatin, etc.
Terms and conditions of storage
Store out of the reach of children, protected from light and moisture, at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pravastatin
At the specialized forums, at the moment, there are no reviews about Pravastatin left by patients and specialists, by which it would be possible to objectively assess the effectiveness and disadvantages of this lipid-lowering agent.
Price for Pravastatin in pharmacies
There is no exact data on the price of Pravastatin, since the drug is currently not available in the pharmacy network.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
