Lipitor tablets 40mg Pfizer treat total cholesterol (3 blisters x 10 tablets)

Atorvastatin is designated to support the diet to reduce total cholesterol, LDL - C and APO B in boys and girls who have menstruation from 10 to 17 years old with hyperlested blood cholesterol after treatment of appropriate diet patients still have the following characteristics:

Atorvastatin reduces cholesterol and lipoprotein levels in serum inhibitors by inhibiting HMG - CoA Reductase and cholesterol synthesis in the liver and increasing the number of LDL receptors of the liver on the cell surface to increase LDL recovery and catabolism.

Atorvastatin reduces LDL production and the number of LDL. Atorvastatin creates a strong and sustainable increase in the operation of the LDL receptor along with the beneficial change in the quality of the circulating LDL elements. Atorvastatin is effective in reducing LDL - C in patients with hypercholesteroline hypertension, a population group often does not respond to lipid lowering products.

Atorvastatin has been shown to reduce the concentration of total C (30% - 46%), LDL - C (41% - 61%), Apolipoprotein B (34% - 50%) and triglycerides (14% - 33%) while creating a difference in HDL - C and Apolipoprotein A1 in a study that responds to a dosage study. These results are suitable in patients with heterozygic blood cholesterol, blood cholesterol -hyperplasia, and mixed blood lipids, including insulin -induced diabetes patients.

Discount C, LDL - C and Apolipoprotein B has been shown to reduce the risk of cardiovascular events and cardiovascular death.

pharmacokinetic

absorption

Atorvastatin is quickly absorbed after drinking, the peak of plasma is reached within 1 to 2 hours. The level of absorption and concentration of Atorvastatin in plasma increases proportional to the dose of Atorvastatin. Atorvastatin tablets for bioavailability equal to 95% to 99% of the solution form. The absolute bioavailability of Atorvastatin is approximately 14% and the whole body for HMG - COA inhibitors is approximately 30%.

Low body use is due to the clearance of the gastrointestinal mucosa or the first metabolism through the liver before the circulation. Although the food reduces the rate and absorption of the drug, approximately 25% and 9%, when assessed according to the peak concentration in CMAX plasma and the area under the curve (AUC), the effectiveness of LDL - C is similar regardless of whether Atorvastatin is used or not used with food.

Lower plasma Atorvastatin levels (approximately 30% for CMAX and AUC) when taking the drug in the evening compared to when used in the morning. However, the effectiveness of LDL - C reduction is the same regardless of what time is taking medicine during the day.

Distribution

The average distribution of Atorvastatin is approximately 381L. The ratio of cohesion to the plasma protein of Atorvastatin> 98%. The ratio between the concentration of drugs in red blood cells in plasma is approximately 0.25, which shows the poor penetration of the drug in erythrocytes.

Metabolism

Atorvastatin is converted mainly into hydroxy derivatives at Ortho and Para positions and products of oxidation in beta. On Vitro, the effect of inhibiting HMG - COA enzymes of hydroxy metabolic substances at Ortho and Para is equivalent to this effect of Atorvastatin. Approximately 70% of the inhibition activity in the circulation for HMG - COA enzymes is due to active metabolites.

Intro studies suggest the importance of Atorvastatin metabolism by CYP3A4 suitable for the high level of plasma Atorvastatin levels in humans after using simultaneously with erythromycin, an inhibitor known for this iszym. In vitro studies also show that Atorvastatin is a weak inhibitor for CYP 3A4.

Simultaneous use of Atorvastatin with terfenadin does not affect clinically the plasma concentration of Terfenadin, a compound converted mainly by CYP3A4, so Atorvastatin will not significantly change the names of the substrates of CYP 3A4. In animals, hydroxy metabolites in the ortho position still undergo glucuronide.

Elimination

Atorvastatin and its metabolites are excreted mainly through bile after being metabolized in the liver or outside the liver, but the drug does not seem to have a cycle of re -circulating the intestinal liver. The average selling time in the plasma of Atorvastatin in humans is approximately 14 hours, but the sale time of the inhibitory activity for HMG - COA reducing enzymes is 20-30 hours due to the contribution of active metabolites. Under 2% of the atorvastatin dose is found in pepper water after drinking.

Special target groups

Elderly: Atorvastatin concentration in plasma in elderly subjects (≥65 years) is healthy is higher (approximately 40% for CMAX and 30% for AUC) compared to young people.

Hepatic failure: Atorvastatin's plasma concentrations are significantly increased (approximately 16 times for CMAX and 11 times for AUC) in patients with chronic liver disease due to drinking alcohol (Childs - PUGH type B).

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

affect the liver

Liver function tests should be done before starting treatment and periodically. Patients with any signs or symptoms suggest liver damage should be performed with liver function tests. Patients develop increased transaminase levels should be monitored until (the abnormal) abnormalities. If the increase of transaminase is 3 times greater than the upper limit of the normal level (ULN) continues, should reduce the dose or stop Atorvastatin.

Atorvastatin should be used carefully for patients who drink plenty of alcohol or have a history of liver disease.

Prevention of stroke by reducing depression of cholesterol levels (Sparcl).

In a post -production analysis of stroke in patients without coronary heart disease (CHD) recently suffering from a transient ischemic (ray), higher hemorrhagic stroke rate in patients who start using Atorvastatin 80mg than placebo. The increased risk is especially recorded in patients with previous hemorrhagic stroke or redimentary infarction at the beginning of research.

For patients with previous hemorrhagic stroke or reduction infarction, the balance between the risk and benefits of Atorvastatin 80mg is uncertain, and the potential risk of hemorrhage stroke should be carefully considered before starting treatment.

Muscle effects

Atorvastatin, like other HMG - Coa Reductase inhibitors, in some rare cases, can affect skeletal muscles and cause muscle pain, muscle inflammation and muscle disease that can progress into pattern, a condition that is likely to be life -threatening by creatine kinase levels (CK) significantly increased (> 10 times ULN), Myoglobinemiaemia and Myoglobin to kidney failure.

Very rare report on muscle necrosis through immunompered (IMNM) during or after treatment with some statins. IMNM has a clinical characteristic that is near persistent muscle weakness and increased serum creatine kinase, still exists despite stopping treatment with statin.

Before treatment

Atorvastatin should be prescribed carefully in patients with elements of the previous muscle destruction. CK levels should be measured before starting statin treatment in the following cases:

In such situations, the risk of treatment should be considered related to possible benefits, and should be clinically monitored.

If CK concentration increases significantly (> 5 times ULN) at first, should not start treatment.

CREATINE KINASE measurement

Do not measure Creatine Kinase (CK) after exertion exercise or when there is any reasonable replacement cause increases CK because this makes explaining the value difficult. If the CK concentration increases significantly at the beginning (> 5 times ULN), it is advisable to measure the concentration within 5 to 7 days then to confirm the results.

during treatment

Interstitial lung disease

The exceptions of interstitial lung disease have been reported to some statins, especially when long -term treatment. The characteristics of expression may include shortness of breath, cough without sputum and general health impairment (fatigue, weight loss and fever). If a patient suspects that the patient has developed interstitial lung disease, he should stop treating with statin.

The ability to drive and operate machinery

unknown.

Pregnancy

contraindicated atorvastatin during pregnancy. Women are likely to be pregnant using the full method of prevention. Only use Atorvastatin for women of reproductive age if these patients are definitely not pregnant and later informed about the risks that may occur for embryos.

Breastfeeding period

contraindicated atorvastatin during breastfeeding.

Drug interaction

The effect of drug products used with Atorvastatin

Atorvastatin is metabolized by Cytochrome P450 3A4 (CYP3A4) and is the substrate of the liver transport, polypeptide transporting organic anion 1B1 (OATP1B1) and 1B3 (OATP1B3). The metabolites of Atorvastatin are the substrate of OATP1B1. Atorvastatin is also identified as a substrate of multi -drug protein 1 (MDR1) and breast cancer protein (BCRP), which can limit the absorption of the intestine and the clearance of Atorvastatin.

Concentrated use of CYP3A4 inhibitors or transportation proteins can lead to increased Atorvastatin levels in plasma and increase the risk of muscle disease. The risk can also increase when using Atorvastatin simultaneously with other drug products that can cause muscle disease.

CYP3A4 inhibitors

Moderate CYP3A4 inhibitors (such as erythromycin, diltiazem, verapamil and fluconazole) may increase the level of Atorvastatin in plasma. Increased risk of muscle disease has been observed when using erythromycin combined with statin. Interactive studies evaluate the effects of Amiodarone or Verapamil on Atorvastatin has not been done.

Both Amiodarone and Verapamil are known to inhibit the activity of CYP3A4 and simultaneous use with Atorvastatin can increase the exposure level with Atorvastatin. Therefore, maximum maximum atorvastatin dose should be considered and recommended appropriate patient clinical monitoring when used simultaneously with moderate CYP3A4 inhibitors. Appropriate clinical monitoring is recommended after starting or after adjusting the dose of the inhibitor.

CYP3A4 induction

Simultaneous use of Atorvastatin with Cytochrom P450 3A4 (eg Efavirenz, Rifampin, St. John's Wort) can lead to reduced Atorvastatin levels in plasma. Due to the double interaction mechanism of rifampin, (Cytochrom P450 3A4 touch and inhibit the absorption of OatP1B1 liver cells), it is advisable to simultaneously use Atorvastatin with Rifampin, because of slow Atorvastatin after using Rifampin can significantly reduce at Atorvastatin concentration in plasma. However, the effect of rifampin on Atorvastatin concentration in liver cells has not been well known and if it is impossible to avoid simultaneous use, the patient should be carefully monitored in effectiveness.

Transport inhibitors

Transport protein inhibitors (for example, cyclosporin, letermovir) may increase the body contact of Atorvastatin. The influence of inhibition of liver absorption agents on Atorvastatin concentration in liver cells is not well known. If it is impossible to avoid simultaneous use, should reduce the dose and monitor the clinical effect.

It is not recommended to use Atorvastatin in patients using Letermovir simultaneously with ciclosporin.

gemfibrozil/derivative of fibric acid

The use of fibrat alone is sometimes related to muscle -related events, including muscle pattern. The risk of these events may increase when using simultaneously derivatives of fibric acid and atorvastatin. If it is not possible to avoid simultaneous use, the lowest dose of Atorvastatin should be used to achieve treatment goals and patients must be monitored appropriately.

ezetimibe

The use of Ezetimibe alone is related to muscle -related events, including muscle pattern. Therefore, the risk of these events may increase when used simultaneously ezetimibe and atorvastatin simultaneously. Should follow the appropriate clinical monitoring in these patients.

Colestipol

Atorvastatin concentration in plasma and its active metabolites lower (the ratio between Atorvastatin concentration: 0.74) when Colestipol is used simultaneously with Atorvastatin. However, the effect on lipid is larger when Atorvastatin and Colestipol are used simultaneously compared to when using the medicine alone.

Fusidic acid

The risk of muscle disease, including muscle pattern, may increase when using the body fusidic acid at the same time. The mechanism of this interaction (whether it is pharmacokic or pharmacokinetic, or both) is not known. There have been reports on Tieu Co Van (including some deaths) in patients using this combination of drugs.

If you need to treat with all over the body, Atorvastatin should be discontinued during fusidic acid treatment.

colchicine

Although interactive studies with Atorvastatin and Colchicine have not been conducted, cases of muscle disease have been reported when using Atorvastatin simultaneously with Colchicine, and should be cautious when prescribing Atorvastatin with Colchicine.

Effect of Atorvastatin on shared drug products:

digoxin

When using simultaneous doses of digoxin and 10mg of Atorvastatin, Digoxin concentration in a stable state increases slightly. Patients using digoxin should be followed appropriately.

Oral contraceptives

Simultaneous use of Atorvastatin with oral contraceptives increases the concentration of norethindrone and ethinyl oestradiol in plasma.

warfarin

In a clinical study in patients being treated with chronic warfarin, the simultaneous use of Atorvastatin 80mg daily with warfarin causes a slight decrease of about 1.7 seconds prothrombin time in the first 4 days of medication and return to normal within 15 days after Atorvastatin treatment.

Although there are only a few very rare cases of clinical anticoagulant interaction, which should be determined, prothrombin should be determined before starting Atorvastatin in patients using Coumarin anticoagulants and sufficient regularly during early treatment to ensure that there is no significant change in prothrombin time.

When the stable prothrombin time has been recorded, prothrombin can be monitored at the time when it is often recommended for patients who are taking Coumarin anticoagulant drugs. If changing or stopping using Atorvastatin, the same process should be repeated. Atorvastatin treatment is not related to bleeding or changing prothrombin time in patients without anticoagulants.

Table 1: The effect of shared drug products on pharmacokinetics of Atorvastatin