CA 2 Flashcards
What does Pharmacologic response depend on?
the
drug binding to its target
What are factors that affect drug
receptor binding
Aging, genetic mutation, malnutrition
What is activation
receptor affected by
bound molecule which leads to
tissue response.
What is governed by affinity
Tendency of drug to bind to
receptors governed by its affinity
What is a full agonist + example
Produces the maximum possible response i.e Heroin
What is a partial agonist + example
Produce a sub-maximal response even at full receptor occupancy.
i.e. Buprenorphine
What is a Inverse agonist + example
Binds to receptors and induce an opposite response
i.e. Antihistamines
What is a competitive antagonist + example
Binds to the same site on the receptor as the agonist, competing for
receptor occupancy.
i.e Naloxone
What is a non competitive antagonist + example
Binds to an alternative site on the receptor causing a change that reduces the receptors ability to respond to the agonist
i.e Ketamine
what is reduced in the presence of the
antagonist.
The agonist
What is the dose ratio?
The ratio by which the [agonist]
must be increased in the presence of the
antagonist in order to restore a given level of response.
What are receptors? Give 2 examples
Sensing elements in a chemical
communication system
Many drugs act as
agonists/antagonists on receptors
Beta blockers
Angiotensin receptor blockers
What are the two types of ion channels
Voltage-Gated Ion Channels.
2. Ligand-Gated ion Channel.
How do ion channels open
Ion channel opens when receptor occupied by an agonist.
What drugs effect ion channels
Local anaesthetics, i.e. cocaine
Vasodilators
Give an example of reversible substrate analogue
Atorvastatin on HMG-CoA
Give an example of irreversible substrate analogue
aspirin on cox 1
What are pro drugs
pharmacologically inactive.
* Needs enzymatic conversion to active drug
Example of type 1 and type 2 prodrugs
Type 1: Heroin
Type 2 Aspirin
What are kinase- linked receptors
Large heterogeneous that have 2 domains
1. Extracellular ➔ ligand binding area
2. Intracellular ➔ mostly has catalytic activity.
i.e. insulin
What are Nuclear receptors
Intracellular
* Regulate gene transcription
* Act on nucleus when ligand is bound. i.e. steroids
