Potential drug interactions resulting from cassette dosing
Process | Protein Involved | Saturable? | Direct Consequence of Competitive Inhibition |
---|---|---|---|
Gut lumenal hydrolysis | |||
Nonenzymatic | None | No | None |
Enzymatic | Hydrolases | Yes | Increased F |
Gut wall uptake | |||
Passive | None | No | None |
Active | Transporters | Yes | Decreased F |
Gut wall efflux | PGP | Yes | Increased F |
Gut wall metabolism | P450, UGT, etc. | Yes | Increased F |
Hepatic uptake | Transporters | Yes | Decreased CL/Increased F |
Hepatic metabolism | P450, UGT, etc. | Yes | Decreased CL/Increased F |
Biliary efflux | Transporters | Yes | Decreased CL/Increased F |
Plasma protein binding | Albumin, AGP | Yes | Increased CL of low clearance drugs |
Renal glomerular filtration | None | No | None |
Renal metabolism | P450, UGT, etc. | Yes | Decreased CL |
Renal tubular secretion | |||
Passive | None | No | None |
Active | Transporters | Yes | Decreased CL |
Renal tubular reuptake | |||
Passive | None | No | None |
Active | Transporters | Yes | Increased CL |
P450, cytochrome P450; PGP, P-glycoprotein; UGT, UDP-glucuronyl transferase; AGP, α1-acid glycoprotein.