Universal reference book for medicines
Name of the preparation: HOLETAR ® (HOLETAR)

Active substance: lovastatin

Type: Lipid-lowering drug

Manufacturer: KRKA (Slovenia)
Composition, form of production and packaging
Tablets 1 tab.
lovastatin 20 mg
Excipients: lactose monohydrate, pregelatinized starch, butyl hydroxy anisole (BHA), Color Patient Blue V (E131), corn starch, microcrystalline cellulose, magnesium stearate.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
Tablets 1 tab.
lovastatin 40 mg
Excipients: lactose monohydrate, pregelatinized starch, butyl hydroxy anisole (BHA), coloring material Quinoline Yellow (E104), coloring material Patient Blue V (E131), corn starch, microcrystalline cellulose, magnesium stearate.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Lovastatin is an inhibitor of endogenous cholesterol synthesis in the liver. In the body, lovastatin, in the form of an inactive lactone, is directly hydrolyzed to the corresponding β-hydroxy acid, a therapeutically active form. This active form acts as a competitive inhibitor of 3-hydroxy-3-methylglutaryl-
Coenzyme A reductase (HMG-CoA reductase) is an enzyme that catalyzes the conversion of HMG-CoA into mevalonate, the initial stage of cholesterol biosynthesis.
Highly effective in reducing total cholesterol in the blood and cholesterol in the composition of LDL (low-density lipoproteins) and VLDL (very low-density lipoproteins). It also reduces the concentration of triglycerides in the blood plasma and moderately increases the concentration of HDL (high-density lipoproteins). Other effects
lovastatin (improved endothelial function, plaque stabilization, anti-inflammatory and antithrombogenic effect), some of which are not directly related to the effect of lipid lowering, contribute to the antiatherosclerotic effect of lovastatin. The expressed therapeutic effect of the drug manifests itself within 2 weeks, and the maximum - in 4-6 weeks from the start of treatment.
PHARMACOKINETICS
In the gastrointestinal tract, lovastatin is absorbed slowly and not completely - about 30% of the dose taken, taking an empty stomach reduces absorption by 30%. C max therapeutic is achieved in 2-4 hours, then the concentration in the blood plasma rapidly decreases, making after 24 hours 10% of the maximum. Binding to blood plasma proteins - 95%. C ss lovastatin and its active metabolites with a single appointment for the night is achieved on the 2-3 day of therapy and 1.5 times higher than after a single dose. The drug penetrates through blood-brain and placental barriers. It is subjected to intensive metabolism at the first passage through the liver. T 1/2 - 3 hours. It is excreted through the intestine - 83%, kidneys - 10%.
INDICATIONS
- Primary hyperlipidemia (types IIa and IIb), including hereditary hypercholesterolemia and mixed hyperlipidemia;
- slowing the progression of coronary atherosclerosis, in the treatment of patients with coronary heart disease as part of a combination therapy.
DOSING MODE
Dosage and duration of admission are determined by the attending physician.
Tablets are taken orally.
The initial dose - 20 mg is taken 1 time / day during dinner. If necessary, in order to achieve the target values ​​of serum cholesterol level, the dose of Hoolatera can increase - up to 80 mg / day in one or more receptions. If necessary, 4 weeks after the start of the dose, the dose can be adjusted: in the case of a decrease in the concentration in the plasma of total cholesterol to 140 mg / 100 ml (3.6 mmol / L) or LDL cholesterol - to 75 mg / 100 ml (1.94 mmol / l ) dose should be reduced. The maximum recommended dose for patients taking cyclosporine simultaneously is 20 mg / day.
Increase doses above 20 mg / day in patients with severe renal failure (creatinine clearance less than 30 ml / min) should be taken with caution.
SIDE EFFECT
Holletar, as a rule, is well tolerated.
On the part of the digestive system: in the mouth, a taste disorder, a decrease in appetite, gastralgia, cholestatic jaundice, a violation of liver function, hepatitis, acute pancreatitis.
From the side of the central nervous system: dizziness, headache, general weakness, insomnia, convulsions, paresthesia, mental disorders.
From the musculoskeletal system: myalgia, myositis, myopathy, rhabdomyolysis (in patients receiving simultaneously cyclosporine, gemfibrozil or nicotinic acid), arthralgia.
From the hemopoiesis: hemolytic anemia, leukopenia, thrombocytopenia.
From the senses: fog before the eyes, lens opacity, cataracts, atrophy of the optic nerve.
Laboratory indicators: increased activity of hepatic transaminases, increased activity of creatine phosphokinase (CKF).
Allergic reactions: urticaria, Quincke's edema, toxic epidermal necrolysis (Lyell's syndrome), skin rash, itching.
Other: decreased potency, acute renal failure (due to rhabdomyolysis), chest pain, palpitations.
Patients should inform the attending physician of any emerging side effects, including those that are not described in the instructions for use.
CONTRAINDICATIONS
- liver disease in the active phase;
- persistent elevations in hepatic transaminase activity (unclear etiology);
- severe hepatic impairment;
- the general severe condition of the patient;
- Pregnancy;
- lactation period;
- age under 18 years (efficiency and safety not established);
- increased individual sensitivity to the drug or any of its ingredients.
With caution - liver disease (in history), chronic alcoholism, organ transplantation, concomitant immunosuppressive therapy, chronic renal failure, urgent surgical manipulations (including dental), with simultaneous admission with gemfibrozilom and other fibrates, niacin (because of risk of myopathy).
PREGNANCY AND LACTATION
The drug is contraindicated in pregnancy and lactation. Women of childbearing age are advised to take lovastatin only if the probability of pregnancy can be reliably excluded.
APPLICATION FOR FUNCTIONS OF THE LIVER
Increase doses above 20 mg / day in patients with severe renal failure (creatinine clearance less than 30 ml / min) should be taken with caution.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated:
- liver disease in the active phase;
- persistent elevations in hepatic transaminase activity (unclear etiology);
- marked hepatic insufficiency.
With caution - liver disease (in history).
The therapy with lovastatin may cause an increase in the activity of liver enzymes. This increase, as a rule, is small and clinically insignificant. However, it is recommended to monitor enzyme levels before the start of therapy and during the course of treatment at regular intervals (for 1 year, then at least once every 6 months).
Any special abnormalities that require interruption of treatment are rare. If the increase in activity of ACT and / or ALT exceeds the triple value of the upper limit of the norm, therapy with Hooletar should be discontinued.
APPLICATION FOR CHILDREN
Contraindicated: age under 18 years (efficacy and safety not established).
SPECIAL INSTRUCTIONS
Treatment with lovastatin should be accompanied by an appropriate diet (low in cholesterol)
The therapy with lovastatin may cause an increase in the activity of liver enzymes. This increase, as a rule, is small and clinically insignificant. However, it is recommended to monitor enzyme levels before the start of therapy and during the course of treatment at regular intervals (for 1 year, then at least once every 6 months).
Any special abnormalities that require interruption of treatment are rare. If the increase in activity of ACT and / or ALT exceeds the value of the upper limit of the norm by 3 times, the therapy should be discontinued.
Treatment with Hooletar should be discontinued if the activity of creatine phosphokinase significantly exceeds the norm (10-fold excess of the upper limit). Hletator's therapy can lead to the development of myopathy, and as a result, to rhabdomyolysis and kidney failure. An increased risk of myopathy exists also in patients with severe renal failure, if myopathy is established or suspected, and in patients with severe acute infectious diseases when referring to myopathy or at the risk of developing renal failure as a result of rhabdomyolysis (severe acute infection, arterial hypotension, interference, trauma, severe metabolic, endocrine or electrolyte disorders, and epilepsy that is not amenable to drug control).
Patients should inform their physician in time if there is an unexplained pain in the muscles, especially if it is accompanied by a malaise or fever.
Impact on the ability to drive vehicles and manage mechanisms
There was no impact on the ability to drive a car or work with technical devices.
OVERDOSE
Several cases of accidental administration of large doses of the drug have been described, but no specific symptoms have been observed in patients. When overdose is recommended to monitor liver function.
DRUG INTERACTION
Simultaneous reception of Hooletar and nicotinic acid, cyclosporine, macrolide antibiotics, azole antifungal agents, HIV protease inhibitors, nefazodone may lead to an increase in the concentration of lovastatin in the blood plasma, which may result in myopathy with rhabdomyolysis and renal insufficiency. The same mechanism is involved in the use of grapefruit juice during the course of treatment with lovastatin.
Simultaneous reception of Hooletar with derivatives of fibroic acid (gemfibrozil) can also lead to the development of myopathy, although the mechanism in this case is not clear.
Co-administration of Hoolera and warfarin can increase the influence of the latter on the parameters of blood coagulability, which may increase the risk of bleeding. In the case of joint administration of these two drugs, it is recommended that the prothrombin time be determined with an appropriate frequency until the stable digits of this index are reached.
Kolestyramin and colestipol reduce bioavailability (the use of lovastatin is possible 4 hours after taking these drugs, with an additive effect noted).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. Keep out of reach of children at a temperature of no higher than 25 ° C. Shelf life - 5 years.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!