Drug Absorption Flashcards
What are the 3 physic-chemical factors that affect the transferral of drugs across cell membranes?
- Ionisation
- Lipid solubility
- Structure
What environmental factor does the degree of dissociation of a drug depend on?
pH
What are ionised drugs unable to do?
Cross the membrane
What can unionised drugs do?
Cross the membrane
What is an example of a lipophobic drug that will not readily pass across the membrane?
Gentamicin
How will a drugs structure affect its ability to cross the membrane?
If its shape resembles naturally occurring substances it can diffuse easier
What are the 3 factors unrelated to the drug that affect the absorption of a drug from the GI tract?
- Motility
- Food
- Illness
How does motility affect absorption?
The speed at which the drug reaches the absorption site
How can motility be influenced?
- Illness
- Food and drink
- Other drugs
How can illness impair absorption?
- Malabsorption
Name two conditions that alter the ability of drug absorption (you have one of them)
- Coeliacs disease
- Migraines reduce stomach emptying rate therefore reduce analgesic absorption
What is the first pass metabolism?
The metabolism of the drug prior to it being absorbed
How can rapid first pass metabolism be avoided?
Different delivery methods
What three places does first pass metabolism occur?
- Gut lumen
- Gut wall
- Liver
What breaks down drugs in the gut lumen
- Acid
- Enzymes
What breaks drugs down in the gut wall
- Enzymes
What metabolises drugs in the liver?
- Hepatic extraction ratio
What are the benefits of intravenous administration?
- 100% bioavailability
- Avoids first pass metabolism
What are the benefits of topical administration?
- Can be used for local and systemic effects
- Can be easily controlled
- Easy to keep up dosage
- Avoids first pass metabolism
What are the benefits of inhalation?
- Drug delivered to site directly
- Very fast
- Very small doses
- Mostly local absorption
What is bioavailability?
The amount of drug which reaches circulation and is ready for action
What 4 factors affect bioavailability?
- Formulation
- Drug’s ability to pass physiological barriers
- GI effects
- First pass metabolism
What 3 factors affect a drugs ability to pass physiological barriers?
- Particle size
- Lipid solubility
- pH and ionisation