Absorption+distribution

Absorption+distribution - Absorption -> Distribution Ion...

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Absorption -> Distribution
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Ion Trapping Plasma pH=7.4 Stomach pH=2 [A - ] p + [H + ] p [HA] p [HA] s [H + ] s + [A - ] s Thiopental Barbital Secobarbital
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Ion Trapping Plasma pH=7.4 Stomach pH=2 [A - ] p + [H + ] p [HA] p [HA] s [H + ] s + [A - ] s
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Absorption Passive Diffusion lipid membrane ion trapping Facilitated Diffusion Active Transport MAY NOT BE COMPLETE
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Bioavailability Fraction (percentage) of drug that reaches the systemic blood as parent (not metabolite) “F” by convention Oral bioavailability amount “absorbed” in portal circulation amount that avoids liver first pass
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Feces Bile LIVER P L A S M A Stomach ~ 1hr pH ~ 2 Esophagus quick! Small Intestine 3-5 hr pH - neutral active transport LargeIntestine 12-18 hr pH - neutral active transport Rectum Absorption
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Bioavailability High bioavailability usually not much patient variability Low bioavailability can be a lot of patient variability Think in terms of amount not available e.g. liver metabolizes 10% (F=0.9) vs. liver metabolizes 80% (F=0.2)
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Absorption+distribution - Absorption -> Distribution Ion...

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