Atorvastatin 10 mg + Ezetimibe 10 mg
BRAND NAME:-CORAVAS-E Tablet (Atorvastatin 10mg+ Ezetimible 10mg)
COMPOSITION:-Atorvastatine 10mg+ Ezetimble 10mg
- Absorption: – After oral administration, Atorvastatin is rapidly absorbed, with peak serum concentrations reaching within 1 to 2 hours. Extent of absorption increases in proportion to Atorvastatin dose.
- Bioavailability: – The absolute bioavailability of Atorvastatin is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%.
- Distribution: – Mean volume of distribution is approximately 381 liters. Atorvastatin is ≥ 98% bound to plasma proteins.
- Metabolism: – Atorvastatin is extensively metabolized to ortho-and para hydroxylated derivatives and various beta-oxidation products. Approximately 70% of circulatory inhibitory activity for HMG-CoA reductase is attributed to active metabolites.
- Elimination: – Atorvastatin and its metabolites are eliminated primarily in bile following hepatic and/or extra hepatic metabolism; however the drug does not appear to undergo enterohepatic recirculation.
- Half-Life: – 14Hrs
- Absorption: – Ezetimibe is rapidly absorbed and conjugated after oral administration. Tmax of Ezetimibe and Ezetimibe-glucuronide are 4-12 hrs and 1-2 hrs respectively. Concomitant food administration (high fat or non-fat meals) has no effect on the extent of absorption of Ezetimibe.
- Protein Binding: – Ezetimibe-glucuronide are highly bound (>90%) to human plasma proteins. In humans,
- Metabolism: – Ezetimibe gets rapidly metabolized to Ezetimibe-glucuronide. Ezetimibe and Ezetimibe glucuronide are the major drug-derived compounds detected in plasma, constituting approximately 10-20% and 80-90% of the total drug in plasma, respectively.
- Elimination: – Both Ezetimibe and Ezetimibe-glucuronide are slowly eliminated from plasma with a half-life of approximately 22 hours for both Ezetimibe and Ezetimibe-glucuronide.
From the pharmacokinetic profile, it is clear that both the drugs are rapidly absorbed after oral administration. The Tmax for Atorvastatin and Ezetamibe glucuronide (pharmacologically active metabolite of Ezetamibe) are also same (i.e. 1-2 hours) which further supports their use in fixed dose combination as a single dose. Further Atorvastatin and Ezetimibe can be administered as a single dose at any time of the day with or without food
- It is used for the treatment of dyslipidemia and the prevention of cardiovascular disease.
- Ezetimibe is a prescription drug that is used to treat high cholesterol and a rare genetic condition called sitosterolemia