DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

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Therapeutic
effect
Metabolism
T
Excretion
SECTION I
Drug
T
Absorption
Drug level
in blood
T
T
GENERAL PRINCIPLES
T
T
Adverse
drug effect
T
T
T
Excretion
Figure 5–1. Roles of membrane transporters in pharmacokinetic pathways. Membrane transporters (T) play roles in pharmacokinetic
pathways (drug absorption, distribution, metabolism, and excretion), thereby setting systemic drug levels. Drug levels often drive
therapeutic and adverse drug effects.
transporters are the targets for drugs used in the treatment
of neuropsychiatric disorders (Murphy et al.,
2004; Torres and Amara, 2007). SERT (SLC6A4) is a
target for a major class of antidepressant drugs, the
selective serotonin reuptake inhibitors (SSRIs). Other
neurotransmitter reuptake transporters serve as drug
targets for the tricyclic antidepressants, various
amphetamines (including amphetamine-like drugs
used in the treatment of attention deficit disorder in
children), and anticonvulsants (Elliott and Beveridge,
Drug
Drug
Metabolite 1
Drug
Metabolite 1
Metabolite 2
Phase
1
Metabolite 1
Phase
2
Metabolite 2
Hepatocyte
Bile canaliculus
Blood
Figure 5–2. Hepatic drug transporters. Membrane transporters, shown as red ovals with arrows, work in concert with phase 1 and
phase 2 drug-metabolizing enzymes in the hepatocyte to mediate the uptake and efflux of drugs and their metabolites.