Fluvastatin

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Fluvastatin

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Lescol forte is taken orally, regardless of the meal. Patients who need to reduce the level of LDL cholesterol to ≥25% - the initial dose of 80 mg (1 tab.) 1 time per day in the evening. Patients who need to lower LDL cholesterol to

For children: the recommended initial dose of 20 mg.

Before starting treatment, the patient is transferred to a standard hypocholesterol diet, which is followed during the entire course of therapy.

Adverse reactions

From the hemopoietic system: very rarely - thrombocytopenia.

From the nervous system: insomnia; often - headache; very rarely - paresthesia, dysesthesia, hypesthesia, possibly associated with the underlying disease.

Since the cardiovascular system: very rarely - vasculitis.

From the digestive system: often - dyspepsia, abdominal pain, nausea; very rarely - hepatitis.

Dermatological reactions: rarely, hypersensitivity reactions (rash, urticaria); very rarely - other skin reactions (eczema, dermatitis, bullous rash), swelling of the face, angioedema

From the musculoskeletal system: rarely - myalgia, muscle weakness, myopathy; very rarely - myositis, rhabdomyolysis, lupus-like reactions.

From the laboratory indicators: increased levels of transaminases to values ​​of more than 3 times higher than VGN (1-2%), a pronounced increase in levels of CPK more than 5-fold excess of VGN (0.3-1%).

Contraindications

• active liver disease or a persistent increase in the concentration of serum transaminases of unknown etiology;
• pregnancy;
• lactation period (breastfeeding);
• hypersensitivity to the components of Lescol forte.

Drug interactions

Effect of various drugs on fluvastatin

With the simultaneous appointment of fluvastatin with bezafibrat, gemfibrozil, ciprofibrate or nicotinic acid, no clinically significant changes in the bioavailability of these drugs were noted. However, since the simultaneous use of other HMG-CoA reductase inhibitors with the above drugs showed an increased risk of myopathy, such combinations should be used with caution.

The simultaneous administration of fluvastatin and such powerful inhibitors of CYP3A4 as itraconazole and erythromycin has a very small effect on the bioavailability of fluvastatin. Since CYP3A4 does not play any significant role in the metabolism of fluvastatin, it can be expected that other inhibitors of this isoenzyme (ketoconazole, cyclosporine) will not affect the bioavailability of fluvastatin.

Since fluvastatin does not interact with substances that are substrates for CYP3A4 isoenzyme, its interaction with grapefruit juice is not expected.

Appointment of fluvastatin to healthy volunteers who had previously received fluconazole (CYP2C9 inhibitor) resulted in an increase in plasma AUC and Cmax of fluvastatin by 84% and 44%, respectively. Although there has been no clinical evidence of a change in the safety profile of fluvastatin in patients who have received prior 4-day fluconazole treatment, caution should be exercised when fluvastatin is used together with fluconazole.

Despite possible competition between fluvastatin and CYP2C9 isoenzyme substrates, such as diclofenac, phenytoin, tolbutamide, and warfarin, according to clinical studies, drug interaction is unlikely.

In clinical studies in patients with a transplanted kidney who received stable maintenance doses of cyclosporine, there was no clinically significant increase in the bioavailability of fluvastatin administered in a daily dose of up to 40 mg. In another study, when Lescola Forte was prescribed in a dose of 80 mg, patients with a transplanted kidney who received stable maintenance doses of cyclosporine showed a 2-fold increase in the AUC and Cmax of fluvastatin by a factor of 2 compared with healthy volunteers. Although the increase in fluvastatin AUC and Cmax were not clinically significant, caution should be exercised when using this combination.

Fluvastatin should be taken no less than 4 hours after taking Kolestiramin to avoid significant drug interactions due to the binding of the drug to the resin.

There were no significant differences in the lipid-lowering effect of fluvastatin when administered with evening meals or 4 hours after it was observed.

When fluvastatin was prescribed to healthy volunteers who received prior treatment with rifampicin, a decrease in the bioavailability of fluvastatin by about 50% was noted. Although there is currently no convincing clinical evidence of a change in the lipid-lowering activity of fluvastatin when it is prescribed to patients receiving long-term treatment with rifampicin (for example, with tuberculosis), nevertheless, to achieve the required reduction in lipid levels, a corresponding dose adjustment of fluvastatin may be required.

The simultaneous appointment of fluvastatin with cimetidine, ranitidine or omeprazole increases the bioavailability of fluvastatin, which has no clinical significance. Although studies on the interaction of fluvastatin with other drugs of these pharmacological groups have not been conducted, however, any significant effect of these drugs on the bioavailability of fluvastatin is unlikely.

The effect of phenytoin on the pharmacokinetic parameters of fluvastatin is very small, so changing the dose of fluvastatin is not required.

There was no clinically significant pharmacokinetic interaction with simultaneous use of fluvastatin with propranolol, digoxin, losartan or amlodipine, therefore using such combinations does not require monitoring of plasma concentrations of the drugs and dose adjustment.

Influence of fluvastatin on other drugs

With simultaneous use of fluvastatin in a dose of 80 mg (Lescol Forte) with cyclosporine, the bioavailability of the latter was not observed.

Changes in the pharmacokinetic parameters of phenytoin with simultaneous use of fluvastatin are relatively small and clinically insignificant; therefore, using such combinations, it is sufficient to carry out conventional monitoring of plasma phenytoin concentrations.

In healthy volunteers, when taking a single dose of fluvastatin and warfarin, there was no adverse effect on the concentration of warfarin in the plasma and on the prothrombin time. However, there are very rare reports of bleeding and / or an increase in prothrombin time reported in patients treated with fluvastatin, while warfarin or other coumarin derivatives are given. Therefore, in patients undergoing treatment with warfarin or other coumarin derivatives, it is recommended to monitor the prothrombin time in case of initiation or withdrawal of fluvastatin therapy, as well as in case of a change in its dose.

In patients with type 2 diabetes mellitus (insulin-dependent) who are treated with sulfonylurea derivatives (glibenclamide, tolbutamide), the addition of fluvastatin to therapy does not lead to clinically significant changes in the glycemic profile.

In 32 patients with non-insulin-dependent diabetes mellitus treated with glibenclamide, against the background of simultaneous use of fluvastatin at a dose of 40 mg 2 times / day for 14 days, there was an increase in the average values ​​of Cmax, AUC and T1 / 2glibenclamide by about 50%, 69% and 121% respectively. At the same time, glibenclamide in a dose of 5 mg to 20 mg caused an increase in the mean Cmax and AUC values ​​for fluvastatin by 44% and 51%, respectively. No changes in glucose, insulin and C-peptides were observed in this study. However, for patients taking both fluvastatin and glibenclamide, appropriate monitoring is recommended when fluvastatin dose is increased to 80 mg / day.

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