What BCS class is nifedipine?
Nifedipine is a BCS Class II drug used for treatment of hypertension and preterm labor. Large inter-patient variability in nifedipine absorption results in variable exposure among different patients.
What do you mean by BCS classification?
Biopharmaceutical Classification System
The Biopharmaceutical Classification System (BCS) is an experimental model that measures permeability and solubility under prescribed conditions.
What are BCS Class 1 drugs?
By definition, BCS Class I drugs are highly absorbed, and have neither solubility nor permeability limited absorption. Therefore, they generally represent a low risk group of compounds in terms of the potential for excipients to affect absorption, compared to other BCS classes.
How is nifedipine metabolized?
Nifedipine is metabolized via the cytochrome P450 3A4 system. Drugs that are known to either inhibit or induce this enzyme system may alter the first pass or clearance of nifedipine.
Is nifedipine an immunosuppressant?
After 4 months of therapy interleukin-2 inhibitor activity was normal in 7 of 9 patients regardless of the severity of symptoms, which indicated that nifedipine exerted an immunosuppressive effect.
Where is nifedipine metabolized?
Nifedipine is extensively metabolized to highly water soluble, inactive metabolites accounting for 60% to 80% of the dose excreted in the urine. Only traces (less than 0.1% of the dose) of the unchanged form can be detected in the urine.
Is nifedipine a CYP inhibitor?
Results: Administration of nifedipine resulted in inhibition CYP3A4 activity with an IC50 value of 7.8 μM, and nifedipine significantly inhibited P-gp activity in a concentration-dependent manner.
Is nifedipine an ACE inhibitor?
This study showed that nifedipine retard was as effective as ACE inhibitors in reducing the incidence of cardiac events in extremely high-risk hypertensive patients with complications of diabetes and coronary artery disease.
How are drugs classified according to BCS?
The drugs are classified in BCS on the basis of solubility, permeability, and dissolution. Solubility class boundaries are based on the highest dose strength of an immediate release product.
What are CYP3A4 inhibitors?
Potent inhibitors of CYP3A4 include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal and grapefruit. Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.
What is the BCS classification for acetaminophen?
Abacavir (BCS Class – III) Abiraterone acetate (BCS Class – IV) Acetaminophen (BCS Class – III) Acetazolamide (BCS Class – IV)
What is the model input value for captopril absorption fraction?
The model input value for the absorbed drug fraction was 0.715. These model input values are consistent with the reported literature as captopril belongs to Biopharmaceutical Classification System (BCS) class I and has a high permeability and solubility34. Distribution The minimal PBPK model was used for predicting captopril distribution.
What are the uses of captopril?
Captopril is used to treat high blood pressure (hypertension), congestive heart failure, kidney problems caused by diabetes, and to improve survival after a heart attack. Captopril may also be used for purposes not listed in this medication guide.
Is captopril a vasoconstrictor?
IDENTIFICATION AND USE: Captopril is angiotensin-converting enzyme (ACE) inhibitor and antihypertensive agent. HUMAN STUDIES: Captopril prevents the conversion of angiotensin I to angiotensin II (a potent vasoconstrictor) by competing with the physiologic substrate (angiotensin I) for the active site of ACE.