Inbacid 10 Savi medicine for hyperlipidemia, prevent cardiovascular events (3 blisters x 10 tablets)

Provisions of cardiovascular events

In people with hypercholesterolemia, there is no clear clinical manifestation of coronary artery disease but there are many risk factors such as age, smoking, hypertension, low LDL-C or early family history of coronary artery disease, the drug is indicated to:

This enzyme catalyzes HMG-CAA to Mevalonate during cholesterol synthesis, thus reducing the synthesis of cholesterol in the liver and reducing the concentration of cholesterol in the cell. This increases the LDL-C receptors (Low Density Lipoprotein (Cholesterol) on the liver cell membrane, thereby increasing LDL-C clearance from circulation.

Atorvastatin reduces total cholesterol levels, LDL-C and VLDL-C (Very Low Density Lipoprotein-Cholesterol) in plasma. The drug also tends to reduce the concentration of triglycerides and increase HLD -C (high density lipoprotein (cholesterol) in plasma.In addition, Atorvastatin also has a number of other effects such as: slowing down the process of progress and/or retreating atherosclerotic atherosclerosis and/or carotid artery; Reducing blood pressure in humans hypertension and giving cholesterol first blood cholesterol; Anti -inflammatory activity in hypercholesteroline blood hyperiemia, accompanied or does not accompany coronary artery disease; may increase bone density.

The effect of regulating blood lipids is more corresponding to the dosage than with plasma concentrations.

Pharmacokinetics

absorption

Atorvastatin is quickly absorbed after taken, the maximum plasma drug concentration is achieved within 1-2 hours. The level of absorption and concentration of Atorvastatin increases proportional to the dose of Atorvastatin.

Atorvastatin is 95 - 99% of the tablet of the solution. The absolute bioavailability of Atorvastatin is about 14% and the system of systemic use of the HMG-CAA reducing enzyme inhibitors is about 30%. The low -body usability is due to the purification in the gastrointestinal mucosa and/or first metabolism in the liver. Although food reduces the absorption rate of about 25% when rated by the maximum concentration (CMAX) and about 9% when assessed by the area under the curve (AUC: Area Under Curve), the LDL-C decrease is unchanged when Atorvastatin is taken at the same time as food or not. Plasma Atorvastatin concentration after taking the evening in the evening is lower in the morning when used in the morning (about 30% for CMAX and AUC). However, the effectiveness of LDL-C reduction is the same regardless of the time when taking the drug during the day (see the dose and how to use).

Distribution

The average distribution of Atorvastatin is about 381 liters. Over 98% of Atorvastatin is connected to plasma proteins. The ratio of plasma red blood cells is approximately 0.25, showing the permeability into low red blood cells.

Metabolism

Atorvastatin is converted mainly into hydroxy derivatives at Ortho and Para positions and oxidized products at beta. In vitro, the inhibition of HMG-CoA enzyme inhibitors of metabolic substances through the hydroxylation pathway in the Ortho and Para position is equivalent to the inhibition of Atorvastatin. About 70% of the plasma inhibitors of HMG-COA enzyme are caused by active metabolites. In vitro, studies show the importance of Atorvastatin metabolism by Cytochrom P450 3A4 in the liver, suitable for the level of Atorvastatin in plasma increased in humans after simultaneous use with Erythromycin, a known inhibitor of this isozym. In animals, the metabolism of ortho-hyperroxy will undergo more glucuronide.

Elimination

Atorvastatin and its metabolites are excreted mainly through bile after the metabolism in the liver and/or outside the liver. However, the drug does not go through the gut liver cycle.

The average plasma sale time of Atorvastatin in humans is about 14 hours, but half of the time of HMG - COA eliminating enzyme inhibitors is 10-20 hours due to the contribution of active metabolites. Under 2% of the oral atorvastatin is found in the urine.

HIV patients are taking Nelfinavir or protease inhibitors to treat hepatitis boceprevir:

Inbacid 10 dose should not exceed 40 mg/day, should use the lowest dose effectively.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What do

do when using overdose? If overdose, symptomatic treatment and necessary support measures. Need to do functional assessment tests and monitor serum ck concentration when overdose. Because the drug is strongly connected to plasma proteins, it is not expected to increase the clearance of Atorvastatin by hemorrhage.

In an emergency, call the 115 emergency center immediately or go to the nearest local health station.

What to do when you forget 1 dose? However, if the time to relax with the next dose is too short, skip the dose and continue the calendar of the drug. Do not use double dose to compensate for missed dose.

Be cautious when using

before and while using Atorvastatin, should try to control blood cholesterol with appropriate diet, exercise, weight loss in obese patients and treat diseases that can be the cause of lipid hypertension.

Atorvastatin can cause increased creatinin phosphokinase and transaminase.

Avoid using drugs with grapefruit juice because of CYP3A4 inhibitors increasing drug concentration.

Liver function: Like the medications that lower blood lipids in the same group, the moderate increase (> 3 times the upper limit of the normal level) of serum transaminase can be seen when treated with Atorvastatin. When stopping the drug, Transaminase will return to the level before treatment. The liver enzyme test is needed before starting statin treatment and in the case of clinical indications for testing later (as if there is a suggestion, there is a liver damage). Caution should be used in patients with alcohol and/or a history of liver pathology.

Persistent liver disease or increased transaminase is not explained as contraindications for the use of Atorvastatin.

Bone muscle system: Muscle pattern accompanied by secondary acute renal failure and myoglobin urine have been reported (rare) when taking Atorvastatin and other drugs in the same group.

History of kidney disease is a risk factor for muscle eligibility. Pay attention to monitor side effects on these patients.

Consider monitoring Creatin Kinase (CK) in the case:

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, the history of liver disease and/or drinking lots of alcohol, elderly patients (> 70 years old) have risk factors for muscle pattern, the ability to occur with special patients. In these cases, the benefits/risks should be considered and monitor patients clinically when treated with statin. If the results of CK test> 5 times the upper limit of normal levels, do not start treatment with statin.

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

It is necessary to stop using Atorvastatin if the CK concentration increases or if diagnosed or suspected of muscle disease. If muscle pain does not increase or moderate serum ck (3-10 times) the high limit of normal) must monitor patients weekly until symptoms, if worse, stop the drug.

Atorvastatin treatment should temporarily reduce the dose or stop treatment in a group of patients with severe and acute disease that suggest to myocarditis or patients with risk factors for acute renal impairment developed by secondary renal impairment after a dramatic myoglobin (such as severe acute infections, hypotension, surgery, trauma, severe metabolic disorders, hormonal disorders, no seizures).

The risk of muscle disease during the treatment of Atorvastatin will increase when used simultaneously with, gemfibrozil, other fibrat blood cholesterol medications, high doses of niacin (> 1 g/day), colchicin, or antifungal groups Azol.

Be cautious when using statin lipid medications with HIV and hepatitis C (HCV) because it can increase the risk of muscle damage, most serious is muscle pattern, kidney damage leading to kidney failure and can be fatal.

Endocrine: HBA1C increases and hungry blood sugar have been reported with HMG-CoA inhibitors, including Atorvastatin.

Statin affects cholesterol synthesis and theoretically can reduce the production of steroids in
adrenal glands. Clinical studies show that Atorvastatin does not affect the level of cortisol in the body and reserves in the adrenal gland. The effect of Atorvastatin on male fertility has not been studied on the appropriate number of patients. The effects on the pituitary -genitals in women have not been evaluated. Precautions when using statin simultaneously with drugs that reduce endogenous hormone secretion such as ketoconazole, spironolacton and cimetidine.

Diabetes: Some evidence suggests that statin increases blood sugar in some patients, increases the risk of future diabetes.

However, statin should not be stopped for the benefit of reducing cardiovascular risk due to statin, which is greater than the risk of hyperglycemia. Patients are at high risk (5.6-6.9 mmol/l, BMI> 30kg/m2, high blood pressure, increase triglycerides) should be clinically and clinically monitored.

Central nervous toxicity: Cerebral hemorrhage has been observed in an individual dog that is treated for 3 months at a dose of 120 mg/kg/day. The dose of 120 mg/kg/day causes an increase in AUC about 16 times compared to the dose of 80 mg/day in humans. Cerebral hemorrhage and optic neurological degeneration have been observed in other bitches in a state of dying after 11 weeks of treatment with increasing dose to 280 mg/kg/day. In a 2 -year study, observing convulsions in two male dogs. No nerve damage in the mouse is not seen when treated within 2 years with a dose of up to 400 mg/kg/day.

Preventive stroke provision by sharply reducing cholesterol levels (SparCl: Stroke Prevention by Aggressive Reduction In Cholesterol Levels): In the analysis of experimental stroke in patients without coronary artery disease recently or with air anemia, Atorvastatin 80 mg has a higher hemorrhage rate than a placebo. The risk of an increase in people with a history of hemorrhagic stroke or defect infarction. For patients with a history of hemorrhagic stroke or defect infarction, the benefits and risks of the use of Atorvastatin 80 mg have not been assessed firmly and should consider the risk of causing hemorrhagic stroke at the beginning of treatment.

Interstitial lung disease: has been reported in some statins, especially when used for prolonged use. Symptoms include: shortness of breath, dry cough and health impairment (fatigue, weight loss and fever). If the patient is suspected of developing interstitial lung disease, the drug should be stopped immediately.

Colonel: The product contains lactose. Patients have rare genetic problems such as galactose intolerance, lactase deficiency or glucose-galactose metabolic disorders should not use this drug.

The effect of the drug on driving and operating machinery

studies to determine the influence of Atorvastatin on driving and operating machinery has not been done.

When driving or operating the machine, it should be noted that dizziness may occur during treatment.

Using drugs for women during pregnancy and lactation

The case of pregnancy

Atorvastatin reduces cholesterol synthesis and maybe many other substances have biological activity from cholesterol, so the drug can be harmful to the fetus.

contraindicated use of Atorvastatin for women during pregnancy. Atorvastatin is used for women who give birth only when these patients are not pregnant and are provided with information about the risk to the fetus.

Cases of breastfeeding

It is not clear whether this drug is excreted through breast milk or not. Due to the ability to cause adverse feedback to breastfeeding, contraindicated use of Atorvastatin in nursing mothers.

Drug interaction

The effect of other drugs on Atorvastatin:

Atorvastatin is metabolized by cytochrom P450 3A4 and is a substrate of transport proteins.

CYP3A4 inhibitors

Strong CYP3A4 inhibitors cause significant increase in Atorvastatin levels. The coordination of strong CYP3A4 inhibitors (such as Ciclosporin, Telithromycin, Clarithromycin, Delavirdin, Stiripentol, Ketoconazol, Voricazol, Itraconazol, Posaconazol and HIV Ritonavir, Lopinavir, Lopinavir, actazanavir, indomavir, indomavir, indomavir, indomavir, indomavir, indoma Darunavir, ...). In case of compulsory use, it is advisable to consider the starting dose, the maximum dose appropriately and closely monitor patients.

medium inhibitors CYP3A4 (erythromycin, diltiazem, verapamil and fluconazole) may increase the plasma concentration of Atorvastatin. The risk of increased muscle disease has been observed when used in combination with erythromycin and statin. Researching and assessing the interaction of Amiodaron or Verapamil on Atorvastatin has not been done. Amiodaron and Verapamil are known to inhibit CYP3A4 and the same use with Atorvastatin can cause increased Atorvastatin levels. Therefore, it is necessary to consider lowering atorvastatin doses and should monitor patients closely when used in combination with CYP3A4 inhibitors. Should follow the appropriate clinical monitoring after starting or after adjusting the dose of inhibitors.

CYP3A4 induction

Use Atorvastatin combination with CYP3A4 touch substances (Nhur Efavirenz, Rifampin, St. John's Wort) can reduce Atorvastatin levels in plasma. Due to the double interactive mechanism of Rifampin (P450 3A touch and inhibition of transport protein absorption in OATP1B1 liver), the sharing of Atorvastatin and Rifampin is recommended, because of the time of taking atorvastatin after drinking Rifampin causes atorvastatin concentration. However, it is not known the effect of rifampin on the concentration of Atorvastatin in liver cells, so if they have to be used together, the patient should be carefully monitored about the effectiveness of the drug.

Transport protein inhibitors

Transport protein inhibitors (such as ciclosporin) may increase Atorvastatin levels. It is unknown the effect of the inhibitor of transportation protein absorption in the liver on the concentration of Atorvastatin in liver cells.

If shared, do the dose and follow the patient carefully.

gemfibrozil/ Fibric acid leading

The solitary use of fibrats is related to side effects, including pattern. Increased risk when used with Atorvastatin. If this combination must be used, the lowest dose of Atorvastatin should be used and need to monitor the patient appropriately.

ezetimib

Ezetimib also causes side effects, including muscle pattern. Therefore, the risk of side effects will increase when used in combination with ezetimib with atorvastatin.

Should follow the appropriate patient.

Colestipol

When used with Colestipol, Atorvastatin's concentration and its metabolites are reduced. However, when using this combination, the effect of lowering blood lipids increases compared to when using each single drug.

cholestyramin

Atorvastatin concentration in plasma decreases (about 25%) when using cholestyramin along with Atorvastatin. However, the effectiveness of treatment on blood lipids when using 2 drugs is higher when only 1 of 2 drugs.

Fusidic acid

The risk of muscle disease, including muscle pattern, may increase when sharing fusidic acid with statin. The mechanism of this interaction has not been clarified. There have been reports on cases of muscle pattern (some deaths) when using this combination. Atorvastatin should be stopped during treatment with fusidic acid.

colchicin

Although the drug interaction between Atorvastatin and Colchicin has not been studied, there have been reports of some muscle lesions when used in this combination. Therefore, it is necessary to be cautious when indicated for the patient to use this combination.

antacid

Simultaneous use of Atorvastatin with oral antacid contains magnesi and aluminum hydroxyd, which will reduce the concentration of Atorvastatin in plasma by about 35%, however, the effect of the drug on the effectiveness of LDL-C does not change.

Pomelo juice

Using pressed grapefruit juice (there are many ingredients inhibited CYP 3A4) with Atorvastatin may increase the concentration of drugs in the blood.

niacin

The risk of side effects may increase when using atorvastatin with niacin, should consider reducing the dose of Atorvastatin in this case.

The influence of Atorvastatin on other drugs

digoxin

Simultaneous use of Atorvastatin and Digoxin increases plasma digoxin concentrations in a stable state of nearly 20%. Proper monitoring of patients who are using digoxin.

Oral contraceptives: Concomitance with oral contraceptive tablets containing norethindron and ethinyl estradiol increases the AUC of Norethindron and of Ethinyl Estradiol nearly 20%. When choosing contraceptives for women who are taking Atorvastatin should consider this.

warfarin

In the patient in patients with long -term warfarin therapy, the combination of Atorvastatin 80 mg daily with wafarin reduces PT (prothrombin time) about 1.7 seconds during the first 4 days and returns to normal after 15 days of treatment with Atorvastatin.

Once the face is very rare for drug interaction with anticoagulant drugs, PT should also be checked before taking Atorvastatin in patients who are taking anticoagulants and should be monitored regularly during the early stages of the treatment process to ensure no major changes in PT. When PT has stabilized, patients taking anticoagulants are recommended to monitor PT periodically. If the dose changes or stops atorvastatin, this process is needed.

Atorvastatin is known to be unrelated to bleeding or changing PT in non -anticoagulants.

Other drugs

In clinical studies, when concurrent Atorvastatin with antihypertensive drugs and estrogen replacement therapy, there is no clinical adverse drug interaction.