Pharmacokinetics 1 Flashcards
Which 4 processes constitute a drug becoming therapeutic?
- Pharmaceutical process
- Pharmacokinetic process
- Pharmacodynamic process
- Therapeutic process
Which 2 mechanisms constitute a drug coming into the body?
- Absorption
- Distribution
Which 2 mechanisms constitute a drug coming out of the body?
- Metabolism
- Elimination
What are the 3 routes of administration?
- Focal
- Enteral
- Parenteral
Where does absorption of an oral drug occur and what is the normal transit time?
- Small intestine
- 3-5 hours
What types of drug can use passive diffusion transport?
- Lipophilic drugs
- Weak acids/bases
What does a long transit time allow for when a drug is transported using passive diffusion?
Gives more time for more of the drug to be absorbed due to the maintenance of equilibrium
What transport molecule does facilitated diffusion use and what are its two types?
- Solute Carrier Transporters (SLC)
- Organic Anion Transporters (OATs)
- Organic Cation Transporters (OCTs)
Where are solute carrier transport proteins most abundant?
- GI epithelia
- Hepatic epithelia
- Renal epithelia
What is secondary active SLC transport? Give an example
- Transport given by pre-existing electrochemical gradients
Fluoxetine - co-transported with Na+ ion
Penicillin - co-transported with H+ ion
Name 3 factors that can affect drug absorption
- GI surface area/length
- Drug lipophilicity/pKa
- SLC expression density
- Blood flow
- GI motility
- Food/pH
What is first pass metabolism?
Metabolism that occurs before the drug has entered the systemic circulation
What are the 2 families of enzymes involved in first pass metabolism in the gut wall and liver
- Cytochrome P450s
- Conjugating Enzymes
How can first pass metabolism be avoided?
Use of different routes - parenteral, rectal, sublingual
What is oral bioavailability?
The fraction of a defined dose of drug given orally that reaches the circulation unchanged