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Lecture 2 cards
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- 1Oral med pathwaystomach -> small intestine (most absorption) -> liver -> heart -> lungs -> systemic
- 2Cmax oral vs IVOral starts low, grows and decreases (bell curve)
IV starts at Cmax and decreases over time (no GI track to go through) - 3BioavailabilityFraction of an administered dose of drug that reaches systemic circulation unchanged (IV is always 100%)
IV -> Oral may require increased dose - 4First Pass effectConcentration of a medication is greatly reduces before enteric systemic circulation typically oral
- 5FenestrationHigh fenestration = more drug moving through cell membrane (liver/kidney)
Low Fenestration = less to none drug moving through cell membrane (brain) - 6Permeability and lipophilicity/molecular weightPermeability = directly proportional to lipophilicity and indirectly proportional to molecular weight
High perm = high lipophil/low weight
Low perm = low lipophilicity/heavy weight - 7Ion TrappingAcidic medications favor basic conditions and vice versa
ie: asprin is a weak acid therefore it will move from duodenum to blood plasma
(more ion trapping = more absorption) - 8Volume of distribution (Vd)Amount in body at equilibrium/concentration in plasma
Calculate plasma concentration:
C = A/Vd - 9Phase 1 reactionsOxidation
Reduction
Hydrolysis - 10Phase 2 ReactionsGlucuronidation, sulfation, acetylation, peptide conjugation, glutathione conjugation
- 11Phase 2 enzymesTPMT, NAT, GST, UGT, SULT
- 12Acetaminophen metabolism (phase 1 and 2)phase 2's -> non toxic metabolite
phase 1 w/o gsh = toxic metabolistes = oxidative stress/hepatocyte death - 13Renal excretionWeak acids, organic bases
Carrier-mediated transport - 14Half livesTime for drug to reach half its concentration
typical time to removal = 5 half lives - 15Zero order elimination vs First OrderZero = same amount of drug eliminated over time (mg/min)
First = same proportion of drug eliminated per unit of time (%/min) - 16Clearance (L/hr)Rate of eliminate of drug to the concentration of drug in plasma
Elimination rate (mg/hr)/Concentration (mg/L)
usually around 5 half lives to steady state - 17Rate of eliminationClearance x Plasma concentration
- 18Dosing ratePlasma concentration steady state x clearance
- 19Cockcroft-gault equation(140-age) x weight kg/serum creatinine (mg/dL) x 72 (all x .85 if female)
- 20Enzyme inhibitionDecreases metabolic capacity
Increases availability of Parent Drugs
Decrease availability of Prodrugs - 21Enzyme InductionIncreases Metabolic Capacity
Decreases availability of parent drugs
Increases availability of Prodrugs
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- Midterm Pharm 1 Fichas sobre Lecture 2 cards, creado por Jeffrey Simpson el 01/02/2026.
- Creado por
- Jeffrey Simpson
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