Japet An Thien Treatment of hypercholesterol blood cholesterol (3 blisters x 10 tablets)

Ezetimibe lower blood cholesterol by inhibiting molecules involved in the absorption of cholesterol in the small intestine.

Combining 2 components of Atorvastatin and Ezetimibe in the drug helps reduce cholesterol in plasma due to inhibiting cholesterol in the intestine, and reduces endogenous cholesterol synthesis.

pharmacokinetic

absorption

ezetimibe

After drinking, Ezetimibe is quickly absorbed and combined into the Ezetimibe-Glucuronid form. The maximum concentration in plasma (CMAX) reaches about 1-2 hours after drinking for ezetimibe -glucuronid, and about 4 -12 hours after drinking for ezetimibe. Food does not affect the bioavailability of Ezetimibe.

Atorvastatin

Atorvastatin is quickly absorbed by oral, maximum concentration in plasma is achieved within 1-2 hours. The amount of Atorvastatin is absorbed and the plasma concentration increases in the dose ratio.

distribution

Ezetimibe and Ezetimibe-Glucuronid

Mount with plasma protein at 99.7% and 88 ~ 92%.

Atorvastatin

transformation

ezetimibe

Modified mainly in the small intestine and liver through a combination of glucuronid. Both Ezetimibe and Ezetimibe-Glucuronid are slowly eliminated from plasma due to the intestinal cycle. The half-life of Ezetimibe and Ezetimibe-Glucuronid is about 22 hours.

Atorvastatin

Metabolic mainly into hydroxylation derivatives at Ortho and Para positions and oxidized products at Beta.

Elimination

ezetimibe

After taking 14C-Ezetimibe (20mg), about 93% Ezetimibe is present in plasma. About 78% and 11% are found in feces and urine within 10 days. After 48 hours, there is no drug present in plasma.

Atorvastatin

Atorvastatin and metabolites are excreted mainly through bile after the metabolism in the liver or outside the liver. However, the drug does not seem to go through the gut cycle. The average selling time in the plasma of Atorvastatin in humans is about 14 hours, but the half -life of HMG -CAA eliminating enzyme inhibits is 20-30 hours due to the contribution of active metabolites. After drinking, less than 2% of Atorvastatin's dose is found in urine.

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.

Be cautious when using

Should check the level of creatinin kinase (CK) in patients:

Monitoring patients during medication. If there are symptoms such as fatigue, muscle weakness, should stop using the drug.

The ability to drive and operate machinery

Pregnancy

Contraindications in pregnant women.

Breastfeeding period

Contraindicated in breastfeeding women.

Medicinal interaction

CYP3A4 enzyme inhibitors: Used along with CYP3A4 enzyme inhibitors may increase the concentration of Atorvastatin in plasma, leading to increased risk of muscle and muscle disease.

Amiodaron: When used with amiodaron, do not use more than 20 mg atorvastatin/ day because of the increased risk of muscle pattern. For patients who have to take a dose of over 20 mg/ day to be effective for treatment, the doctor may choose another statin (such as pravastatin).

Coumarin derivatives: Statin medications slightly increase the anticoagulant effect of cooumarin. In patients who are taking anticoagulant drugs, prothrombin should be used before and during Atorvastatin treatment.

Should be cautious when used in combination with niacin or immunosuppressive drugs.

The risk of muscle disease during treatment with these groups will increase when used simultaneously with cyclosporin, the derivatives of fibric acid, erythromycin, antifungal group Azol or niacin.

antacids: Use Atorvastatin simultaneously with antacids containing magnesi and aluminum hydroxyd, plasma concentration of Atorvastatin is reduced by about 35%. However, the effect of reducing cholesterol low molecular weight does not change.

Antyrin: Because Atorvastatin does not affect the pharmacokinetics of antipipin, there is no interaction with other drugs metabolized through the same type of cytochrom.

Colestipol: When using Colestipol with Atorvastatin, Atorvastatin's concentration is reduced by about 25%. However, the effect on lipid increases when using Atorvastatin and Colestipol compared to when using a separate drug.

Digoxin: When using multiple doses of digoxin and 10 mg atorvastatin simultaneously, plasma digoxin concentrations in a stable state are not affected. However, Digoxin concentration increased by about 20% when using digoxin with 80 mg atorvastatin daily. Should follow the appropriate monitoring for patients using digoxin.

erythromycin/ clarithromycin: simultaneously use atorvastatin and erythromycin (500 mg x 4 times/ day) or Clarithromycin (500 mg x 2 times/ day) is Cytochrom P450 3A4 inhibitor: Increased plasma concentration of Atorvastatin.

azithromycin: simultaneously use Atorvastatin (10 mg x 1 time/ day) and azithromycin (500 mg x 1 time/ day) does not change the serum concentration of Atorvastatin.

terfenadin: simultaneously using Atorvastatin and Terfenadin does not create a significant influence on the pharmacokinetics of Terfenadin.

Oral contraceptive: Concomitance with oral contraceptive pills contains norethindron and ethinyl estradiol, increasing the value of the area under the concentration - time (AUC) curve (AUC) of Norethindron and Ethinyl estradiol is about 30% and 20%. This increase should be considered when choosing oral contraceptives for women to use Atorvastatin.

warfarin: A study of drug interaction between Atorvastatin and Warfarin has been conducted: There is no clinical interaction.

cimetidin: A study of drug interaction between Atorvastatin and Cimetidin has been conducted: There is no clinical interaction.

Protease inhibitors: simultaneously use Atorvastatin and protease inhibitors are Cytochrom P450 3A4 inhibitors that increase the plasma concentration of Atorvastatin.