Physiology - Active and Bulk Transport Through the Plasma Membrane

___ in a drug transporters may result in changes in drug pharmacokinetics leading to reduced drug efficacy and increased risk for drug-induced toxicity; may cause sensitivity to certain drugs.

In the liver, ABC transporters facilitate drug clearance of unmodified drugs or their metabolites by ___ them into the ___.

Oral meds are absorbed in the ___

___ takes meds from GI tract to the liver to be metabolized into a hydrophilic molecule (from a lipophilic molecule); it is then pumped into the ___ or ___.

Protein enzymes in ___ metabolize drugs to be circulated - concentration does down (way to eliminate from system)

Functional unit of kidney

Blood is filtered from the kidneys into the ___

Drugs in the blood will typically end up in the ___ (if small enough to be filtered through the glomerulus)

____ will be lower for drugs with a substrate that will be pushed back by efflux pumps, so absorption will be lower.

In the intestine, ABC transporters are expressed right on the edge of ___

Expression of transporters with major roles in drug efficacy or toxicity in ___, ___, ___, and ____.

It is often the case that a drug will be a substrate for more than one ___

Transmembrane proteins; single proteins, heterodimers, and homodimers

Transport rate =

Depends on number of protein molecules expressed on cell surface