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46 Cards in this Set

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  • Back
Macromolecules that mediate biochemical and physiologic change in an organism (upon binding to a drug)
Chemical compound that may be used on or administered to humans or animals as an aid in the diagnosis, treatment, or prevention of disease or other abnormal condition, for the relief of pain or suffering, or to control or improve any physiological or pathological condition
Any substance that bring about a change in biological function through its chemical actions
Molecules that interact with specific molecular components of an organism
Value which measures the attraction of a drug for a receptor
Affinity constant
Tendency of a drug to complex with a receptor
The drug must have a molecular conformation which permits binding with a particular receptor surface
Drug selectivity
Refers to the amount of drug necessary to elicit a response
Often expressed as the dose of a drug required to achieve 50% of the desired therapeutic effect
Drug that binds to and activates receptors and in turn, produces a biologic response
Drug that binds to receptors to inhibit a biological response.
In the presence of __________, you require an increased concentration of agonist to produce the same effect as the agonist alone.
Compound that binds to a separate site on the receptor from which normally binds agonists
Allosteric Modulators
separate site on the receptor from which normally binds agonists
Allosteric site
Occupation of _______site can either increase or decrease the response to natural agonist, depending on whether it is a positive or negative modulator.
Allosteric site
Tendency of a drug to complex with a receptor
What are the 4 major receptor families?
1. ligand gated ion channels (eg. cholinergic nicotinic receptors)
2. G-protein coupled receptors (e.g.,alpha and beta adrenoreceptors)
3. enzyme linked receptors (e.g., Insulin receptor)
4. intracellular receptors (e.g., steroid receptors)
What are the 5 types of chemical interactions involved in drug-receptor binding and which has the strongest bond strength?
Covalent (strongest)
van der Waals (weakest)
Binds to receptor and activates it, like a key fits into a lock and turns it
Activation of a receptor by this initiates conformational change in the receptor and activates one or more downstream signaling pathways
These can fit the lock but can't open it
This inhibits activation by agonists
This curves shows and all-or-none response to a drug in a given population
Quantal Dose Curve
This curse shows a range of responses
Graded Dose Curve
Presence of ______ shifts the agonist concentration-effect curve to th left of the Kd for binding of agonist to receptor, and the degree of shift is proportional to the proportion of these
spare receptors
_____makes a tissue more sensitive to an agonist without changing its affinity for the receptor
Spare receptors
Ability of the agonist to cause the receptor to assume and active conformation
Measure of drug safety
Therapeutic Index
Therapeutic Index
More realistic estimate of drug safety LD?/ED?
What does TD50/ED50 mean?
Toxic dose in 50%/Effective dose in 50%
What is the protective index?
ED50(undesirable effect)/ED50 (desirable effect)
Time before the therapeutic effect becomes the unwanted adverse effect
Therapeutic Window
Competes with agonist for the same binding site on a given receptor.
Competitive antagonist
This type of antagonist makes the agonist look less potent by shifting the dose-response curve to the ______. (left OR right?)
Binds irreversibly to a different site than the agonist
Noncompetitive antagonist
This type of antagonist reduces the max response that an agonist can produce
Noncompetitive antagonist
Decreased ability of a receptor to respond to stimulation by a drug or ligand
Decreased response of a single class or receptor
Homologous desensitization
Decreased response of multiple classes of receptor
Heterologous desensitization
After chronic exposure of an agonist to a receptor ___________-regulation of the receptor occurs
After chronic exposure of an agonist, this occurs, resulting in a decreased # of receptors present
After chronic exposure of an antagonist to a receptor ___________-regulation of the receptor occurs
After chronic exposure of an antagonist, this occurs, resulting in as increased # of receptors present
List 2 classes of mechanisms which can confer selectivity of drug action
1. Cell type specificity of receptor subtypes
2. Cell type specificity of receptor-effector coupling