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32 Cards in this Set

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The sites of drug action can be subdivided as non-cellular sites or cellular sites. Which sites are non cellular targets and which sites are cellular targets?
Non-cellular targets:
Water
ions
metal ions

Cellular targets:
membrane lipids
Cellular macromolecules (most drugs target cellular macromolecules)
Regulatory proteins, ion channel proteins, enzymes, carrier proteins and structural proteins are the main classes of ______ ___________.
Drug receptors
This is any cell component to which a drug binds to initiate the chain of biochemical events leading to the drug's observed effects.
A drug receptor
What are 4 properties that are common to most receptors and what do they mean?
1.) specificity: only few drugs can bind to the receptor; must be high and strong.
2.) stereo selectivity: confirmational structure that binds the receptor
3.) sensitivity: how well a receptor activates once bound
4.) variability: receptor number may vary with time
Which broad drug categories fall under "regulatory protein receptors"?
Neurotransmitters
Hormones
Autacoids
Vitamin D
Which broad drug categories fall under "ion channel protein" receptors?
Calcium channel blockers
Antiarrhythmics
Local anesthetics
Which broad drug categories fall under " enzymes" receptors?
Cholinesterase inhibitors
ACE inhibitors
cyclooxygenase inhibitors
Phosphodiesterase inhibitors
carbonic anhydrase inhibitors
Which broad drug categories fall under " carrier protein" receptors?
Tricyclic antidepressants
Cardiac glycosides
Loop diuretics
Proton pump inhibitors
The tendency of a drug to bind to a receptor is defined ________. Which bond type has the highest of these?
Affinity

Covalent bonds
What is an intrinsic activity?
The ability of a drug (once bounds to a receptor) to initiate change and bring about a response.

Each drug can have its own affinity and intrinsic activity.
Compare Full, partial and inverse agonists.
Full: activates to produce a maximal response

Partial: activates it to produce a response below the maximum level.

Inverse: A drug which activates a receptor which already fires on its own but somehow decreases its pre-existing activity.
What is a drug antagonist?
A drug which when bound to the receptor fail completely to produce any activation of that receptor (intrinsic activity is 0).
The occupancy theory states:
-reversible reaction of drug and receptor
-equally accessible
-dissociates easily
effective drug concentration does not change significantly during the reaction
-all or none type
-the intensity of the response is the highest (maximal efficacy) when all the receptors are occupied by the drug.
Types of drug antagonism:
-Chemical antagonism?
Or inactivation
it occurs when a drug combines chemically with the drug to be antagonized so making that drug pharmacologically inactive
Types of drug antagonism:
-Pharmacokinetic antagonism?
a drug prevents the absorption or stimulates the elimination of the drug to be antagonized.
types of antagonists
-Physiological antagonism
An antagonist that binds to a DIFFERENT receptor to produce the OPPOSITE action of the agonist.
Types of antagonists
-Pharmacological antagonism
-Receptor block antagonism
Both drugs compete for the same receptor
-The antagonist prevents the activation of the receptor
Receptor-block competitive antagonists compete for the same receptor, so what happens to the affinity of the agonist?
The competitive antagonist decreases the affinity of the agonist.

However, the same response CAN STILL BE ATTAINED by increasing the agonist concentration, AKA the antagonism is surmountable.
Regarding receptor-block competitive antagonism, what kinds of curve shifts would you expect if you increase antagonist concentration (assuming reversible binding)?
You would expect a shift to the right on a dose v effect plot. The more antagonist you add to the system, the more agonist you need to achieve the same result.
It is important to note that with reversible competitive antagonism you can still reach a maximal effect (efficacy isn't affected), it just requires more drug than usual.
What would happen to the efficacy or maximal response involving an irreversible receptor block antagonism situation?
The maximal effect will be reduced because the number of remaining unoccupied receptors may be too low to allow a maximal effect.
Potency vs. Efficacy
Potency is the dose of a drug required to produce a given effect.The lower the dose required to produce the effect, the higher the potency.

Efficacy: the max effect that can be produced by a drug. It is DIRECTLY related to intrinsic activity of the drug.
This is a ratio between a harmful dose and an effective dose.
Therapeutic index.
Three factors LD, TD, ED
ED IS ALWAYS ON THE BOTTOM when compared to the others.
Therapeutic window is?
The range between the minimum effective dose and the minimum toxic dose of a drug (range of doses which have a high probability of success).
What is a regulatory receptor and what are the 5 classes?
A regulatory receptor is a macromolecule that is able to bind specifically to endogenous substances, which carries and amplifies info between cells.
1.) G protein (metabotropic)
2.) intracellular
3.) ion channels
4.) transmembrane enzyme
5.) janus-kinase
What two processes lead to the diminishing effects of a receptor with its agonist?
1.) Desensitization
response diminishes over seconds or minutes and is rapidly reversible (involves phosphorylation of receptor).

2.) Down regulation: Actual decrease in the number of receptors
Explain why if you suddenly remove a chronically inhibiting antagonist drug, the pharmacological response is increased?
While the receptor was antagonized and inhibited, the body upregulated more receptors to compensate in the meantime. When you remove the block, there is WAY MORE receptors than normal to respond to the agonist (supersensitivity).
Which type of drug interaction describes the following:
-The response elicited by combined drugs is equal to the combined responses of the individual drugs (1+1=2)
Addition
Which type of drug interaction describes the following:
-The response elicited by combined drugs is greater than the combined responses of the individual drugs.(1+1>2)
Synergism
-Both have an affect but together the effect is EVEN greater.
Which type of drug interaction describes the following:
-A drug which has no effect by itself but enhances the effect of another drug.
Potentiation
-0+1>1
Which type of drug interaction describes the following:
-The response elicited by combined drugs is lower than the combined responses of the individual drugs.
(1+1<2)
Antagonism
This is a state of decreased responsiveness to the action of a drug which usually results from a prior exposure to that drug or to a related drug.
Tolerance
-It is a quantitative change in sensitivity to a drug.
tolerance may be drug-disposition tolerance or functional (cellular) tolerance. Compare the two.
DD tolerance is a decrease in the effective concentration of the drug at the site of action.

Functional tolerance occurs due to homeostatic adaption (which can be neurophysiological or biochemical) to counteract the drug or MOST COMMONLY Changes in the number and properties of receptors of the drug.