NAGELHOUT CHAPTER 5 QUESTIONS
AND ANSWERS 100% CORRECT
MOA of GA - ANSWER-Is unknown, but thought to be caused by activation of
receptors, not manipulation of the lipid bilayer.
Thought to be caused by potentiation of the inhibitory NT gamma amnio butyric acid.
3 common properties of receptors? - ANSWER-Specificity - the response that comes
from activation of a receptor is always the same because the cell determines the
function
Sensitivity - how low of a dose can cause a response?
Selectivity - familiar chemicals bind to the receptor
7 classifications of receptors - ANSWER-GCPR
Ligand-gated ion channels
Catalytic receptors
Nuclear receptors
Enzymes
Transporters
Other
Receptor family suggested as primary site of IV anesthetic agents? - ANSWER-GABAa
(ionotropic receptor family a)
except ketamine
It is thought this is how inhalation agents achieve their responses also
When an agonist binds a receptor, which type of bonding is most prominent? what
about with volatile anesthetics? - ANSWER-The alignment of a drug with its receptors is
aided by various bonding forces, of which van der Waals and ionic bonding are
prominent.
Volatile anesthetics bond to receptors by nonspecific hydrophobic bonding.
What is an acceptor? Example? - ANSWER-an endogenous site taht drugs bind to and
reduce the amount of unbound drug - albumin (especially acid drugs)
alpha 1 acid glycoprotein and beta-globulin favor basic drugs
, Second messenger pathways of GCPR, their response, and common drugs -
ANSWER-cyclic adenosine monophosphate (cAMP) - releases protein kinases, beta
receptor stimulation of energy release, ionotropic and chronotropic cardiac effects,
production of adrenal and sex steroids, many other endocrine and neural process -
catecholamines, caffeine, milrinion
phosphoinositides and calcium - activate calmodulin - lithium
cyclic gunaosine monophosphate (cGMP) - activate protein kinases - NTG, SNP
Drug response equation? What is it derived from - ANSWER-D+R <->DRC <-> TR;
derived from law of mass actio
The occupancy theory - ANSWER-the magnitude of a drug's effect is proportional to the
number of receptors occupied
2 types of response curves - ANSWER-Graded and quantal
Graded response curve - ANSWER-plotted in a linear fashion; characterizes the change
in measured reponse as an administered dose is increased (pg 52)
increasing the dose increases the response (more NE means more vasoconstriction)
until you hit 100% saturation.
when plotted on a logarithmic scale, it takes an S shape. at the lowest dose, the
response is small or even nonexistent. at the highest doses, the response is maximal
and approaches a a plateau. between 20% and 80% it is a straight line because it is
more proportional.
Quantal dose response curves - ANSWER-provides information on the frequency which
a given dose produces a desired therapeutic response. Measured in an all-or-nothing
fashion.
Equation for determining safety margin - ANSWER-LD1 - ED 99/ED99 x 100;
So is determined by LD1 and ED99
Therapeutic index - ANSWER-LD50/ED50
What is the ED50? - ANSWER-The dose at which 50% of the population responses as
desired
Competitive vs noncompetitive antagonists - ANSWER-Competitive - bind to the site but
may be displaced by an agonist
AND ANSWERS 100% CORRECT
MOA of GA - ANSWER-Is unknown, but thought to be caused by activation of
receptors, not manipulation of the lipid bilayer.
Thought to be caused by potentiation of the inhibitory NT gamma amnio butyric acid.
3 common properties of receptors? - ANSWER-Specificity - the response that comes
from activation of a receptor is always the same because the cell determines the
function
Sensitivity - how low of a dose can cause a response?
Selectivity - familiar chemicals bind to the receptor
7 classifications of receptors - ANSWER-GCPR
Ligand-gated ion channels
Catalytic receptors
Nuclear receptors
Enzymes
Transporters
Other
Receptor family suggested as primary site of IV anesthetic agents? - ANSWER-GABAa
(ionotropic receptor family a)
except ketamine
It is thought this is how inhalation agents achieve their responses also
When an agonist binds a receptor, which type of bonding is most prominent? what
about with volatile anesthetics? - ANSWER-The alignment of a drug with its receptors is
aided by various bonding forces, of which van der Waals and ionic bonding are
prominent.
Volatile anesthetics bond to receptors by nonspecific hydrophobic bonding.
What is an acceptor? Example? - ANSWER-an endogenous site taht drugs bind to and
reduce the amount of unbound drug - albumin (especially acid drugs)
alpha 1 acid glycoprotein and beta-globulin favor basic drugs
, Second messenger pathways of GCPR, their response, and common drugs -
ANSWER-cyclic adenosine monophosphate (cAMP) - releases protein kinases, beta
receptor stimulation of energy release, ionotropic and chronotropic cardiac effects,
production of adrenal and sex steroids, many other endocrine and neural process -
catecholamines, caffeine, milrinion
phosphoinositides and calcium - activate calmodulin - lithium
cyclic gunaosine monophosphate (cGMP) - activate protein kinases - NTG, SNP
Drug response equation? What is it derived from - ANSWER-D+R <->DRC <-> TR;
derived from law of mass actio
The occupancy theory - ANSWER-the magnitude of a drug's effect is proportional to the
number of receptors occupied
2 types of response curves - ANSWER-Graded and quantal
Graded response curve - ANSWER-plotted in a linear fashion; characterizes the change
in measured reponse as an administered dose is increased (pg 52)
increasing the dose increases the response (more NE means more vasoconstriction)
until you hit 100% saturation.
when plotted on a logarithmic scale, it takes an S shape. at the lowest dose, the
response is small or even nonexistent. at the highest doses, the response is maximal
and approaches a a plateau. between 20% and 80% it is a straight line because it is
more proportional.
Quantal dose response curves - ANSWER-provides information on the frequency which
a given dose produces a desired therapeutic response. Measured in an all-or-nothing
fashion.
Equation for determining safety margin - ANSWER-LD1 - ED 99/ED99 x 100;
So is determined by LD1 and ED99
Therapeutic index - ANSWER-LD50/ED50
What is the ED50? - ANSWER-The dose at which 50% of the population responses as
desired
Competitive vs noncompetitive antagonists - ANSWER-Competitive - bind to the site but
may be displaced by an agonist
