Absorption and Distribution Flashcards
What are the 4 stages of pharmacokinetics?
- Absorption
- Distribution
- Metabolism
- Excretion
What is absorption?
Transfer of the drug from site of administration into the general or systemic circulation
If drugs given orally are wanting to reach small intestine, how are they protected?
Bulking agents added
How does particle size affect absorption?
Has to breakdown into small enough particles to be absorbed via GI tract
If disintegrates slowly, the rate at which the drug is absorbed is limited by the rate of release and dissolution of drug from formulation
How much of drug needs to disintegrate in GI tract to form solution before becoming absorbed?
75%
How does formulation of particle affect absorption?
Has to be lipid soluble to be absorbed by gut (phospholipid bilayer)
Highly polar agents are absorbed slowly and incompletely
What do GI tract enzymes/acid aid in?
Breaking down drugs
How does slow motility of GI tract affect absorption?
Reduced absorption as takes long to reach SI
How does hypermotility / slow motility of GI tract affect absorption?
Hypermotility –> Bowels are moving excessively, reduced absorption, drug won’t be in bowels long enough
Slow motility –> Reduced absorption as takes long to reach SI
Do drugs have to be charged or uncharged to cross membrane?
Uncharged (and lipid soluble)
What is the degree of ionisation dependent on?
pH of their environment
What happens to drugs in stomach (ionisation wise)?
Stomach very acidic - acids become more ionised but bases become more unionised
Acids are proton donors, bases are proton acceptors
Basic drugs will cross membrane more easily than acidic ones in stomach
What happens to drugs in small intestine (ionisation wise)?
Acidic drugs cross membrane more easily than basic drugs
What happens to strong acids and bases in water?
Dissociate 100%
Why do you not need a higher dose for drugs delivered via injection?
Delivered straight into systemic circulation - bypasses liver (1st pass metabolism)