Drug Action Flashcards
What are the types of agonists?
- Full inverse agonist
- Partial inverse agonist
- Partial agonist
- Full agonist
- Super agonist
What is an endogenous agonist?
Compound naturally produced by the body which binds to and activates a given receptor
What is a full inverse agonist? (efficacy%)
Not only prevents agonist causing a response, but has the maximum opposite effect of the endogenous agonist (-100%)
What is a partial inverse agonist? (efficacy%)
Not only prevents agonist causing a response, but has a portion of the maximum opposite effect of the endogenous agonist (-1-99%)
What is a partial agonist? (efficacy%)
Causes a portion of the full response of the endogenous agonist (1-99%)
What is a full agonist? (efficacy%)
Causes the full response of the endogenous agonist (100%)
What is a super agonist? (efficacy%)
Causes a response greater than the maximum of the endogenous agonist (>100%)
Ways of regulating cell function
- Altered membrane potential
- Altered enzyme activity
- Altered gene expression
What is an allosteric effect on a receptor?
The drug binds to the receptor, changing its shape and therefore its response to sitmulus
Agonist(s) of benzodiazepine receptors
- Diazepam
- Lorazepam
Antagonist(s) of benzodiazepine receptors
Flumazenil
Inverse agonist(s) of benzodiazepine receptors
Beta-carbolines
