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Pharmacokinetics and Pharmacodynamics, pharmacokinetics, drug interaction,…
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Enzyme kinetics
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lineweaver-Burk plot
the more right x-intercept, the greater Km→lower affinity
competitive inhibitor cross each other, noncompetitive inhibitor do not
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Dosage calculations
in renal and liver disease, ↓maintenance load
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receptor binding
competitive antagonist
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shift curve right(↓potency), no change in efficiency
noncompetitive inhibitor
shift curve down(efficacy), cannot be overcome
partial agonist
act at same as full agonist, but with lower maximal effect(↓efficasy)
elimination of drug
pH
weak acid: trapped in basic envitonment, treat overdose with sodium bicarbonate to alkalinize urine (eg. phenobarbital, methotrexate, aspirin
weak base: trapped in acidic environment, treat overdose with ammonium chloride (eg. TCAs, amphetamines)
ionized species are trapped in urine and cleared quickly, neutral form is reabsorbed
TCA toxicity is treated with sodium bicarbonate, too
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zero-order elimination
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eg. phenytoin, ethanol, aspirin
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drug metabolism
phase1
reduction, oxidation, hydrolysis with cytochrome P-450 yield slightly polar, water-soluble metabolite
phase2
conjugation (methylation, glucuronidation, acethylation, surfation) yield very polar, inactive metabolites