Drug Absoprtion Flashcards
What is bioavilability?
Fraction of unchanged drugs that reaches the systemic circulation
What gives 100% bioavaiability?
IV injection
What must generics have a bioaviability of?
must have a bioavailability of 80-125% compared to the reference product (EU regulation)
What is generic substiution?
occurs when a different formulation of the same drug is substituted. All generic versions of a drug are considered by the licensing authority to be equivalent to each other and to the originator drug
What is therapuetic substitution?
is the replacement of the originally prescribed drug with an alternative molecule with assumed equivalent therapeutic effect. The alternative drug may be within the same class of from another class with assumed therapeutic equivalence
What are the advantages of the oral route of administration of drugs?
- cheap
- safe
- convienent
What are the disadvantages of the oral route of drug administration?
- patient compliance
- variation in the bioaviability of the drug
What are the main contributors to particle size and formulation of oral drugs?
Excipients, binding agents, lubricants and coatings
What are the 5 main oral routes?
- Buccal/sublingual mucosa
- Gastric mucosa
- Small intestine
- Large Intestine/colon
- Rectal mucosa
describe the buccal/sublingual mucosa route
- Direct absorption into blood stream
- Avoids first pass metabolism
- Not ideal surface for absorption
How are drugs adapted to by-pass the gastric mucosa?
Enteric coating
What is the main site for drug absoprtion?
- Small intestine
- Main site of drug absorption
- Large surface area, more neutral pH
How do drugs enter the systemic circualtion via the rectal mucosa?
Direct entry
What are the 4 ways small molecules cross the cell membrane?
- Diffusing directly through the lipid
- Lipid solubility highly important
- Diffusing through aqueous pores
- More likely important for diffusion of gases
- Transmembrane carrier protein
- E.g. solute carriers
- Pinocytosis
- Mostly macromolecules, not drugs
What are the 2 main methods that drugs cross cell membranes?
- Diffusing directly through the lipid
- Lipid solubility highly important
- Transmembrane carrier protein
- E.g. solute carriers
Describe the drug ionisation of weak bases
- Ionised in acidic pH
- Absorbed in small intestine
- Ionisation in plasma?
Describe the drug ionisation of weak acids
- Unionised in acidic pH
- BUT also absorbed in the small intestine
- Large surface area
Draw the henderson-hasselbach for a weak base
compartment 1 = blood
compartment 2 = SI