Module 3 stuff i dont know Flashcards
absorption
passage of drug from site of administration to plasma
acids and bases absorption
weak acids and bases are easily absorbed
strong acids and bases are poorly absorbed (bc mostly/ fully ionised)
penicillin = acid labile = unstable in low pH of stomach
Absorption from GI tract
Stomach
Duodenum
Jejunum
Ileum
Colon
Rectum
Absorption from the GI tract is dependent on
Concentration gradient
Lipophilicity (R value)
Blood flow to site of absorption
Surface area ! (most absorption occurs in small intestine bc of large surface area)
Formulation
GI tract contents
Gut motility
basic principle of metabolism
the body sees all drugs as foreign and wants to get them out asap without causing harm - hence metabolism
two major types of enzymatic reactions
phase 1
- functionalisation (makes more reactive)
- catabolic reaction
e.g. oxidation, reduction, hydrolysis
- liver
phase 2
- conjugation
- anabolic reaction
e.g. add water soluble moiety to a drug
- liver, lungs, kidney
aspirin in an enzymatic reaction
phase 1
- drug
derivative
- salicylic acid
phase 2 - conjugate
- glucuronide
goal of metabolism
get drug out of body
reduce risk of toxicity
- reduce reactivity
BUT it has to become more reactive before it becomes less reactive
Phase 1
Cytochrome P450
Heme proteins that use Fe3+ at active site
- happening inside cell (endo retic)
- mostly in liver
- wide range of substrates
- reaction requires oxygen, NADPH, and cytochrome p450 reductase
the activity of each enzyme varies
- induction
- inhibition
- genetic variation
- induction of CYPs
…
excretion
3 main ways:
- urine
- poop
- sweat (maybe milk)
- air