Rozulip

• Structure
• Release form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications to use
• Contraindications
• Side effects
• Application instruction of Rozulip (Way and dosage)
• Overdose
• Interaction
• Terms of sale
• Storage conditions
• Period of validity
• Analogs
• Responses

Structure

Depending on a dosage can contain in Rozulip's tablet 5,34 mg, 10,68 mg, 21,36 mg or 42,72 mg of a rozuvastatin of zinc that respectively 5 mg, 10 mg, 20 mg, 40 mg of active ingredient — a rozuvastatin are equivalent.

Act as excipients ludipress, monohydrate of lactose, povidone, krospovidon and magnesium stearate.

The film cover of Opadry II of white color consists of polyvinyl alcohol, titanium of dioxide, a macrogoal and talc.

Release form

Rozulip is issued in tablets of a round biconvex form, white or almost white color, a covering in the form of a film cover, on one of the parties — the engraving "Е", on other party — "591" (a dosage of 5 mg), "592" (a dosage of 10 mg), "593" (a dosage of 20 mg), "594" (a dosage of 40 mg). These tablets are packed into blisters on 7 pieces, in a cardboard pack there are 2, 4 and 8 blisters.

Pharmacological action

Rozulip possesses hypolipidemic action.

Pharmacodynamics and pharmacokinetics

Rozuvastatin as active ingredient is a selective competitive inhibitor of enzyme of HMG-CoA reductase which catalyzes substance transformation KOA 3-hydroxy-3-methylglutaryl in mevalonat – the famous predecessor of cholesterol.

Due to the increase in number of receptors of LPNP on hepatocytes under the influence of a rozuvastatin, processes of absorption and a catabolism of LPNP amplify, and also there is a suppression of synthetic processes of lipoproteins of very low density in a liver. Besides, rozuvastatin makes clinically significant impact on such biochemical indicators as:

• increases concentration of cholesterol and the maintenance of lipoproteins of high density (abbr. Hs — LPVP);
• reduces concentration of the general cholesterol with triglycerides;
• reduces concentration of B (APOB) apolipoprotein, triglycerides, and also lipoproteins of very low density (abbr. TG-LPONP);
• increases the content of A-I (APOA-I) apolipoprotein;
• reduces the increased content of cholesterol with lipoproteins of low density (abbr. Hs — LPNP), cholesterol and NELPVP (Hs — NELPVP), cholesterol with lipoproteins of very low density (Hs — LPONP), and also their ratio which is expressed: Hs — LPNP / Hs — LPVP, general Hs/Hs — LPVP, Hs – NELPVP / Хс – LPVP, APOB/APOA-I.

Usually it is possible to reach therapeutic effect in a week, and after 2 weeks of therapy the efficiency level making about 90 percent from greatest possible is reached. Achievement of the maximum effect requires 4 weeks of therapy, and then maintenance by regular reception.

The maximum plasma concentration of a rozuvastatin at oral administration is reached approximately in 5 hours. Level of absolute bioavailability — to 20% (increases in proportion to a dose). Rozuvastatin, being exposed to intensive absorption by a liver, then acts in synthesis of cholesterol and Hs-LPNP is removed. About 90% of active agent contact proteins in a blood plasma (we rot. with albumine).

Metabolism of a rozuvastatin: as non-core substrate of isoenzymes (main CYP2C9) of P450 cytochrome; the main metabolites are active N-desmetil rozuvastatin, inactive lactonic metabolites.

Nearly 90% of the accepted dose of not changed rozuvastatin eliminirutsya through intestines, 5% of a dose — kidneys. An elimination half-life — 19 h, regardless of increase in a dose.

Indications to use

• the IIa type on Fredrikson's classification primary hypercholesterolemia, the IIb type of the mixed hypercholesterolemia (as addition to a diet);
• in a combination with the diet and other methods of treatment capable to reduce the level of lipids in blood (for example, aferez LPNP) at a hereditary homozygous hypercholesterolemia;
• type IV on Fredrikson's classification gipertriglitseridemiya as addition to a diet;
• in a combination with the diet and therapy reducing the level of general Hs, Hs-LPNP for delay of the progressing atherosclerosis;
• for prevention of various cardiovascular complications, among which: a myocardial infarction, a stroke, an arterial revaskulyation without clinical manifestations, but with the increased risk of development of coronary heart disease, with such risk factors as arterial hypertension, low HS-LPVP, smoking, presence at the family anamnesis of a prematurity of an ischemic disease.

Contraindications

• hypersensitivity to Rozulip's components;
• active phase of the diseases of a liver including permanent increase in activity of serumal transaminases;
• heavy functional disturbances of kidneys, at clearance of creatinine to 30 ml a minute;
• myopathy and predisposition to miotoksichesky complications;
• therapy by Cyclosporine;
• women during pregnancy and a lactation;
• age group till 18 flyings;
• in connection with the content in lactose drug contraindication is its intolerance, deficit of enzyme – lactase, including glyukozo-galaktozny malabsorption.

This drug is used with care in the presence of risk of development of a myopathy or a rabdomioliz, a renal failure, liver diseases in the anamnesis, at sepsis, arterial hypotension, a hypothyroidism.

Besides, with care carry out therapy by Rozulip to the patients who are excessively taking alcohol, age 65 years are more senior, than Asian race, applying fibrata, having the increased plasma concentration of a rozuvastatin, extensive surgical interventions or injuries.

Side effects

Therapy rozuvastatiny can cause the undesirable phenomena, however, easy and passing side effects where classification of frequency of emergence was reduced to such groups as mainly were registered: often (≥1/100 — <1/10); infrequently (≥1/1000 — <1/100); seldom (≥1/10000 — <1/1000); very seldom (less than 1 case on 10000).

As well as in cases with other inhibitors of HMG-CoA reductase, the frequency of emergence of side reactions is connected with dose size. Side reactions can arise from the following systems and bodies:

• Immune system: seldom there are reactions of hypersensitivity and a Quincke's disease.
• Nervous system: "often" headaches, dizziness were registered; cases of polyneuropathy, memory loss are very rare.
• Alimentary system: "often" there were locks, nausea, abdomialny pains; infrequently — an insignificant, asymptomatic, tranzitorny superactivity of hepatic transaminases; pancreatitis cases are rare; frequency of developing of diarrhea is not specified; very seldom — jaundice and hepatitis.
• Skin and hypodermic structures: infrequently the skin itch, rash and the small tortoiseshell meets; frequency of emergence of a syndrome of Stephens-Johnson is not specified.
• Musculoskeletal system: the mialgiya was "often" observed; seldom — a myopathy (including a miositis), rabdomioliz against or without acute functional insufficiency of kidneys; very seldom registered an arthralgia.
• Urinary system: the dose of 10-20 mg almost and a dose of 40 mg at 3% of patients caused a proteinuria in 1% of patients; "it is very rare" the hamaturia was registered.
• Respiratory organs: cough, short wind.
• Fluctuations of laboratory indicators: increase content of glucose, bilirubin, enzymatic activity of GGTP, ShchF.
• Among others: "often" — an adynamy, and also are possible functional disturbance of a thyroid gland.

Application instruction of Rozulip (Way and dosage)

Tablets are registered to accept orally inside. It is not recommended to chew or crush – it is necessary to swallow entirely and to wash down with water! There is no clinical dependence on time of day and meals.

The application instruction of Rozulip assumes observance of a diet with the low content of cholesterol during all course of treatment. And, the dose of drug is selected individually taking into account indications, therapeutic reaction to treatment, the current recommendations of rather target objective of lipids.

The standard scheme and features of treatment by Rozulip for various groups of patients:

• Initial dose of 5-10 mg for 1 time a day which if necessary later 4 weeks can be increased.
• After 4 weeks of reception of the dose exceeding initial in the subsequent it is raised to 40 mg to patients with heavy degree or family (in the anamnesis) a hypercholesterolemia, having high risk of development of cardiovascular complications (under careful supervision of the specialist).
• To patients 65 years are more senior appoint an initial dose to 5 mg, further it is not required to change a dose in connection with age.
• In the presence of moderate disturbances of functions of kidneys (clearance of creatinine to 60 ml/min.), predispositions to a myopathy and for people of Asian race — the initial dose makes 5 mg, however, the dose in 40 mg is contraindicated.
• Increase of a dose after 2–4 weeks of therapy has to be followed by control of indicators of a lipidic exchange and if necessary — correction of a dosage is carried out.

Overdose

At reception over doses of a rozuvastatin it is necessary to carry out a symptomatic treatment because the specific antidote does not exist for today, and success of a hemodialysis is improbable. Besides carrying out the actions directed to maintenance of the vital functions is necessary, control of level of serumal KFK and functions of a liver is recommended.

Interaction

• With AUC Cyclosporine of a rozuvastatin raises on average seven times, than at healthy volunteers, besides plasma concentration of a rozuvastatin increases by eleven times, and Cyclosporine — does not change.
• With antagonists of vitamin K (for example, Warfarin) at the beginning of therapy by Rozulip or at increase of a dose of drug PV and MHO can increase. Rozulip's cancellation or a dose decline can lead to decrease in MHO therefore control of MHO is necessary.
• The combination of a rozuvastatin with Gemfibrozil and hypolipidemic means can lead to increase twice in the maximum plasma concentration and AUC of a rozuvastatin.
• With Ezetimib perhaps farmakodinamichesky interaction and development of side effects.
• With inhibitors of proteases — perhaps significant increase in exposure of a rozuvastatin.
• With antacids decrease in plasma concentration of a rozuvastatin approximately by 50% is observed.
• With Erythromycin — honor decrease in AUC of a rozuvastatin for 20% and Cmax — for 30% probably that is explained by strengthening of motility of intestines under the influence of Erythromycin.
• With oral contraceptives and in in time gormonozamestitelny therapy increases AUC ethinylestradiol (by 26%) and Norgestrelum (for 34%).
• Combined use of the drugs containing rozuvastatin with Itrakonazol (CYP3A4 isoenzyme inhibitor) leads to increase in AUC of a rozuvastatin approximately for 28% that is clinically insignificant reaction.

Terms of sale

The recipe from the attending physician is required.

Storage conditions

Temperature no more than 30 °tselsiya.

For the purpose of safety – to limit access to juvenile children and domestic animals.

Period of validity

Not to use after 3 flyings.

Rozulip's analogs

Among analogs there is Rozulipa the most available:

• Klivas;
• Rozart;
• Rozuvastatin Sandoz;
• Rozukard;

About Rozulip

About Rozulip are not numerous, however those who accepted this hypolipidemic drug, speak about its efficiency at the small list of side effects, convenience of reception as there is no dependence on time of day and meals is also noted.