Autifan 40 An Thien treats lipid disorders (3 blisters x 10 tablets)

Fluvastatin increases the number of LDL receptors on the cell surface in the liver, thus increasing the absorption and catabolism of LDL and inhibiting the synthesis of VLDL in the liver, thus reducing VLDL and LDL components.

Fluvastatin reduces total cholesterol, ldl-cholesterol, APO B, and triglycerides, and increases HDL-cholesterol in patients with hyperchemical hypertension and mixed lipid disorders.

pharmacokinetic

absorption

Fluvastatin is absorbed quickly and completely (98%) after drinking in a volunteer when hungry. Fluvastatin's absolute bioavailability is 24%. Time reaches the peak concentration of less than 1 hour. Food reduces bioavailability, reduces speed and/or absorption level, but due to low reduction, it does not significantly change the clinical effect of blood lipid regulation.

Distribution

Fluvastatin distributed and the main effect in the liver, is also the main organs of drug metabolism. The distribution of the drug is 330 liters. More than 98% of the drug is associated with plasma proteins, and this cohesion is not affected by fluvastatin levels, or by warfarin, salicylic acid or glybid.

Metabolism

Fluvastatin is metabolized mainly in the liver. The main types of circulation in the blood are fluvastatin and non -active metabolism N - Desisopropyl - Propionic Acid. Hydroxy metabolites have pharmacological activity but do not circulate in the blood. There are many roads metabolic fluvastatin via cytochrom P450 (CYP450), Fluvastatin is not sensitive to CYP450 inhibition.

Fluvastatin only inhibits the metabolism of substances metabolized by CYP2C9. Despite the potentially competitive interaction between fluvastatin and metabolites through CYP2C9 such as Diclofenac, Phenytoin, Tolbutamid and Warfarin, clinical data shows that this interaction does not occur.

Elimination

After using 3H - fluvastatin in healthy volunteers, about 6% of substances are marked radioactive excreted in the urine and 93% in feces, with Fluvastatin measured less than 2% compared to the amount used.

Fluvastatin's in the plasma clearance in strangers 1.8 ± 0.8 liters/minute. Plasma drug concentration in a stable state shows no evidence of the accumulation of drugs after the dose of 80 mg/day. After taking the dose of 40mg, the sale time is 2.3 ± 0.9 hours.

Pharmacokinetics on special subjects

The concentration of plasma drugs does not change with the age or gender of the patient. However, increased treatment has been observed in women and the elderly.

Fluvastatin is excreted mainly through bile and can be metabolized before entering the circulatory system, so it is capable of accumulating drugs in patients with liver failure.

Children and teenagers increases heterozygous family blood cholesterol: No pharmacokinetics data in children.

Instructions on how to handle ADR

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Precautions when using

Adults

It is necessary to consider when taking drugs belonging to the statin group for patients with risk factors leading to muscle damage. The drug in the statin group is at risk of causing harmful reactions to the muscle system such as muscle atrophy, especially for patients with risk factors such as patients over 65 years old, patients with untrained thyroid diseases, patients with kidney disease, closely monitoring harmful reactions during the use of drugs.

impact on liver function

Cases of liver function decline can be fatal when using statins including fluvastatin that have been reported.

Although the causal relationship with the unidentified Fluvastatin treatment, patients should be advised to report any symptoms or signs of liver failure (such as vomiting, nausea, anorexia, jaundice, impaired brain function, vulnerable to bruising or bleeding) and when the symptoms appear should be considered to stop treatment.

Recommended the liver enzyme test before starting statin treatment and in the case of clinical indications for testing later.

If the aspartat aminotransferase (AST) or Alanin Aminotransferase (ALT) increases more than 3 times the upper limit of normal and prolonged level, it is necessary to stop using fluvastatin. The case is very rare for drugs due to drugs that have been observed and removed after stopping treatment with fluvastatin.

Be careful when using fluvastatin in patients with a history of liver or alcoholism.

Acting on muscle - bone

can cause muscle pain, muscle disease and very rare cases of muscle pattern in patients treated with fluvastatin.

In patients with unexplained muscle pain, muscle pain or muscle weakness, and/or creatin kinase (CK) level, muscle disease, muscle inflammation or muscle pattern must be considered.

Therefore patients need advice to promptly report the unexplained muscle pain, muscle pain or muscle weakness, especially if it comes with discomfort or fever.

There have been very rare reports of muscle necrosis through the immunity (IMNM) during or after treatment with some statin drugs. The clinical feature of IMNM is the prolonged weakened speculation and the high levels of creatin kinase, which still exists when stopping statin treatment.

measure the concentration of creatin kinase (ck)

Do not measure the concentration of CK after exertion or the presence of a certain cause increases the CK because this may falsify the results. If CK concentration before treatment> 5 times the upper limit of normal level (ULN) should not start treatment with rosuvastatin.

Consider monitoring Creatin Kinase (CK) in the case of

Before treatment, CK tests should be conducted in the following cases: impaired renal function, hypothyroidism, self -history or family history of genetic muscle disease, a history of muscle disease due to the use of statin or fibrat before, a history of liver disease and/or drinking lots of alcohol, elderly patients (> 70 years old) with risk factors for muscle pattern, special possibility of drug interactions and some special patients. In these cases, the benefits/risks should be considered and monitor patients clinically when treated with statin.

If the CK concentration increases> 5 times the upper limit of the normal level, it is necessary to measure within 5-7 days to confirm the results. If the test results CK> 5 times the upper limit of the normal level, do not start treatment with statin.

During statin treatment, patients need to notify when there are muscle manifestations such as muscle pain, stiffness, muscle weakness, cramps ... When there are these manifestations, patients need to test CK to take appropriate interventions.

If CK> 5 x ULN concentration, Fluvastatin should be discontinued. If there are serious and daily -causing symptoms, even if the concentration of CK

Treatment of these symptoms and CK concentrations should be returned to normal, then can use Fluvastatin or other statin at the lowest dose and under strict supervision.

The risk of increased muscle disease in patients using immunosuppressants (including ciclosporin), fibrat, nicotinic acid or erythromycin simultaneously with HMG - Coa Reductase inhibitors.

Cases of muscle disease are reported after simultaneous use of fluvastatin with ciclosporin or colchicin. Fluvastatin should be used carefully in patients in combination with the above drugs.

Fluvastatin is not used simultaneously Fusidic acid uses systemic sugar or within 7 days after stopping treatment with fusidic acid.

In patients with mandatory fusidic acid system, Statin treatment should be discontinued during treatment with fusidic acid. There have been reports on muscle disease (including a number of deaths) in patients using fusidic acid and statin.

Patients need advice to promptly report to health workers if they experience any symptoms of muscle weakness, muscle pain.

Statin therapy is used after 7 days after the last dose of fusidic acid. In special cases, when it is necessary to use long body fusidic acid, for example, to treat severe bacterial infections, if it is necessary to use fluvastatin, it is necessary to consider each case and under tight medical supervision.

Patients with interstitial lung disease

If using fluvastatin, especially long -term use, can suffer from interstitial lung disease with symptoms of dyspnea, dry cough, general health decline (fatigue, weight loss, fever).

If the patient is detected, the development of interstitial lung disease should be discontinued.

Patients with diabetes

Some evidence suggests that statin increases blood glucose and increases the risk of diabetes. However, this risk is not significant compared to reducing the cardiovascular risk of statin, so it is not the reason to stop treating statin.

For patients with high risk such as glycemic glycemic 5.6 to 6.9 mmol/l, BMI ≥ 30 kg/m2, increased triglycerides, hypertension needs to monitor both biochemistry and clinical.

Children

Children and adolescents with hypertension family blood cholesterol

In patients aged

The long -term effect of fluvastatin in childhood to reduce incidence and death in adulthood has not been studied.

Fluvastatin is only studied in children 9 years old and older with hyperlested hyperplastic hypertension.

In the case of children before puberty, experience is very limited in this group, the risks and benefits should be carefully assessed before starting treatment.

Children with hyperlest hypertension of homozygous type

There is no data on the use of fluvastatin in patients with hyperlested hypertension.

The ability to drive and operate machinery

Some unwanted effects such as headache, insomnia may occur, if affected by patients should not drive a train, operate machinery or work on high.

Pregnancy

There is no enough data on the use of fluvastatin during pregnancy. HMG - CoA Reductase inhibitors reduce cholesterol synthesis and may reduce biological substances derived from cholesterol, which can be dangerous to the fetus when used for pregnant women. Therefore, Fluvastatin is contraindicated for pregnant women.

Breastfeeding period

Based on clinical data, Fluvastatin is excreted into breast milk. There is not enough information about the effects of fluvastatin in babies. Fluvastatin is contraindicated in nursing women.

Drug interaction

Fibrat, Niacin

Simultaneous use Fluvastatin with Bezafibrat, Gemfibrozil, Ciprofibrat or high doses of niacin (> 1 g/day) Clinically active effects related to the bioavailability of fluvastatin or other lipid medications.

Simultaneous use of HMG - Coa Reductase inhibitors with the above drugs has been reported to increase the risk of muscle disease and/or muscle pattern, so careful consideration of benefits/risks and use carefully.

colchicin

Cases of muscle disease, including pattern, have been reported when using Fluvastatin simultaneously with Colchicin. Should be cautious when prescribing fluvastatin with colchicin.

Fusidic acid

Risk of muscle pattern may increase due to simultaneous use of bodyIdic acid with statin. The mechanism of this interaction is unclear. There have been reports on Tieu Co Van (including some deaths) in patients who use this combination. If necessary to treat with all over the body, Fluvastatin treatment should be discontinued during fusidic acid treatment.

ciclosporin

Studies in kidney transplant patients show that Fluvastatin's bioavailability (up to 40 mg/day) does not increase significantly in patients with stable doses of ciclosporin.

Results from another study, of which 80 mg Fluvastatin is used for kidney transplant patients with stable ciclosporin doses, showing the area under the curve of Fluvastatin (AUC) and maximum concentration (CMAX) increased by 2 times compared to healthy people.

Although the increase in the level of fluvastatin is not clinically significant, this combination should be used carefully. Start and maintain Fluvastatin dose as low as possible when combined with ciclosporin.

Fluvastatin (40 mg and 80 mg) does not affect the bioavailability of ciclosporin when used simultaneously.

warfarin and other Coumarin derivatives

In healthy volunteers, the use of fluvastatin and warfarin (single dose) does not adversely affect the concentration of warfarin and prothrombin time compared to the use of single -rise warfarin.

rifampicin (rifampin)

Use fluvastatin on healthy volunteers before treatment with rifampicin (Rifampin), resulting in a decrease in the bioavailability of fluvastatin about 50%. Although there is currently no clinical evidence of the effectiveness of flew -ftidin lipid concentration, in patients with long -term treatment of rifampicin (for example, tuberculosis treatment), the appropriate adjustable dose of fluvastatin should be adjusted to ensure blood lipid effect.

Oral diabetes

For patients using oral sulfonylea (Glibenclamid (Glybid), Tolbutamid) to treat insulin -dependent diabetes (type 2), used in combination with fluvastatin does not change the clinical effect significantly in blood sugar control.

A study in patients with Type 2 diabetes (n = 32), treated with glibenclamids simultaneously with fluvastatin (40mg 2 times/day in 14 days) increasing the average CMAX, AUC, and T1/2 of glibenclamid, respectively, about 50%, 69%and 121%.

Glibenclamid (5 - 20 mg per day) increases the average CMAX and AUC of fluvastatin, respectively 44% and 51%. In this study, there was no change in glucose, insulin and c-peptide levels. However, patients treated simultaneously Glibenclamid (Glybid) and Fluvastatin should continue to be closely monitored when the Fluvastatin dose increased to 80 mg per day.

resin

Fluvastatin should be used for at least 4 hours after using resin (eg cholestyramin) to avoid the interaction due to the cohesion of the drug with resin.

fuconazol

Use fluvastatin on healthy volunteers before treatment with fluconazole (CYP2C9 inhibitor) leads to increased contact concentration and peak concentration of fluvastatin respectively about 84% and 44%. Although there is no clinical evidence of the safety of the use of fluvastatin in patients before treatment with fluconazole for 4 days, should be cautious when using Fluvastatin simultaneously with fluconazole.

Antihistamine H2 and proton pump inhibitors

Use Fluvastatin combination with cimetidine, ranitidin or omeprazole that increases the bioavailability of fluvastatin, but has no clinical significance.

phenytoin

Phenytoin pharmacokinetic changes when used simultaneously with Fluvastatin is not clinically significant. Monitor phenytoin concentration in plasma when used simultaneously with fluvastatin.

Cardiovascular medicine

Mobile pharmacokinetic interaction occurs when using Fluvastatin simultaneously with propranolol, digoxin, losartan, clopidogrel or amlodipine. Based on pharmacological data, do not need to monitor and adjust the dose when using Fluvastatin combined with cardiovascular drugs.

iTraconazole and erythromycin

Simultaneously using Fluvastatin with strong inhibitors P450 CYP3A4 Itraconazole and erythromycin has a very small impact on the bioavailability of fluvastatin. These enzymes participate very little in the metabolism of fluvastatin, so it is thought that other CYP3A4 inhibitors (such as ketoconazole, ciclosporin) are not likely to affect the bioavailability of fluvastatin.

taboo

Due to the absence of studies on the correlation of the drug, not mixing this drug with other drugs.