Pharmacokinetics: Absorption, Distribution, Protein Binding, Metabolism (including first-pass and Phase I and II)
- Absorption
- Affected by weight, solubility, and other factors: Influences how a drug enters the bloodstream.
- GI factors like food can change absorption: Presence of food can alter drug absorption rates.
- Distribution
- Membrane permeability (e.g., blood-brain barrier): Determines which drugs can enter the CNS.
- Plasma protein binding
- If not bound, higher levels in blood and tissues: Only unbound drugs are active.
- Storage
- Lipophilic drugs accumulate in fats, calcium in teeth: Affects drug storage and release.
- Metabolism
- Phase I (non-synthetic): drugs are oxidized or reduced to more polar forms
- Phase II (synthetic): polar groups like glutathione are conjugated to the drug
- Cytochrome P450 metabolism
- Mixed function, catalyzes the metabolism of many drugs, delays metabolism or extends life of competing drugs: Plays a crucial role in drug interactions.
Excretion: Renal, Biliary, Other (e.g., for volatile drugs)
- Renal
- Organic anion transport: HCTZ, furosemide, PCN G, salicylates: Mechanism for drug excretion through kidneys.
- Biliary excretion
- Drugs excreted into bile and eliminated in feces: Alternative route of excretion.
- Other
- Volatile drugs excreted through lungs: e.g., anesthetic gase