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Pharmacology Review

Pharmacology Review

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Pharmacology Review
Pharmacology Review

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Published by: SUTHAN on May 29, 2009
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Pharmacology Review
Dr. Robert G. LambProfessorPharmacology & Toxicology
Mechanisms of Drug Action I
The method of expressing agonist and antagonistdose-response relationships that produce straightlines [a] , hyperbolic curves [b] , and S-shaped curves [c]a. Lineweaver-Burkeb.Michaelis-Mentenc.Log Dose-Responsed.Law of Mass Actione. Occupancy Theory of Drug Action
Mechanisms of Drug Action II
Lineweaver-BurkeMichaelis-Menten
Mechanisms of Drug Action III
Competitive InhibitorNon-Competitive Inhibitor
Mechanisms of Action IV
A patient ingests an agent that produces various dose-responsecurves. Curve A is the agonist alone, curve B is the agonist plusa low dose of the ingested agent, curve C is the agonist plus amoderate dose of the ingested agent and curve D is the agonistplus a high dose of the ingested agent. The ingested agent is:A competitive antagonist [Fig. 1] [higher K 
D
& lower potency &affinity]A non-competitive antagonist [Fig. 2] [lowerEmax& lowerefficacy]An irreversible antagonist (non-competitive) in the presence of spare receptors [Fig. 3]
Mechanisms of Drug Action V
Competitive Inhibitor Non-Competitive InhibitorNo spare receptors are present.
 
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Mechanisms of Drug Action VI
An irreversible antagonist (non-competitive) inthe presence of spare receptors.
Mechanisms of Drug Action VII
Select the statements that are not true about the effects of acompetitive (I
C
) and a non-competitive (I
NC
) antagonist on anagonist.I
C
increases the agonist’s K 
D
I
C
decreases the agonist’s E
max
***I
C
lowers the agonist’s affinity/potencyI
NC
decreases the agonist’s E
max
I
NC
lowers the agonist’s efficacyI
NC
increases the agonist’s K 
D
***I
NC
decreases the agonist’s K 
D
***I
C
has the sameE
max
, higher K 
D
[lower affinity & potency]I
NC
has the same K 
D
, lowerE
max
[lower efficacy]
Mechanisms of Drug Action VIII
Select the processes that are not associated with receptor-mediated transmembrane signaling processes.influx of extracellular calciumactivation of tyrosine kinaseincrease in gene transcriptioninflux of extracellular sodiumactivation of phospholipase C (DAG, IP
3
, calcium)activation of adenylyl cyclase (c-CAMP)activation ofguanylylcyclase (c-GMP)activation of protein kinaseefflux of intracellular calcium ***activation of phosphodiesterase ***
Mechanisms of Drug Action IX
In the Occupancy Theory of Drug Action an agonist has high _____ and an antagonist has high ______?
K2 K1 [AFFINITY] K3 [EFFICACY]
D +
DR 
RESPONSEK1,K2,K3K1,K3K1,K3K2,K3K2,K3K1,K2K1,K2,K3K1 ***K1,K2K1,K3
Drug Absorption I
99.9%log [B/BH
+
= 1/1000]0.1% log [A
-
/HA = 1/1000]3 units < pKa99% log [B/BH
+
= 1/100]1%log [A
-
/HA = 1/100]2 units < pKa90.9%log [B/BH
+
= 1/10]9%log [A
-
/HA = 1/10]1 unit < pKa50% log [B/BH
+
= 1/1]50% log [A
-
/HA = 1/1]pH = pKa9%log [B/BH
+
= 10/1]90.9% log [A
-
/HA = 10/1]1 unit > pKa1%log [B/BH
+
= 100/1]99%log [A
-
/HA = 100/1]2 units > pKa0.1%log [B/BH
+
= 1000/1]99.9% log [A
-
/HA = 1000/1]3 units > pKaWeak Bases% ionization of 
codeine
Weak Acids% ionization of 
aspirin
pH
Drug Absorption II
What percent of a weak base (pKa= 7.5) and weak acid (pKa= 3.5)will be respectively ionized in urine of pH 5.5?1% and 1%pH –pKa = log Base/Acid9% and 91% [Acid] 5.5 3.5 = 2 log 100 = 2 A
-
/ HA = 100/150% and 50% [Base] 5.5 -7.5 = -2 log .01 = -2 B / BH+ = 1/10091% and 9%99% and 99% ***
 
3
Drug Absorption III
Select the route of administration that will produce theslowest onset of drug action [1], most rapid onset of action [2]and a first-pass liver effect [3].Oral [3]Intravascular [2]Rectal [1]IntramuscularSubcutaneous
Drug Absorption IV
Select the statements that are not true about the advantages anddisadvantages of parenteral andenteralroutes of drugadministration.Enteraladvantages: safe, economical, high bioavailability ***,rapid onset of action***Enteraldisadvantages: slow onset of action, low bioavailability,first pass liver effect, patient compliance***Parenteral advantages: high bioavailability, fast onset of action,patient compliance, safe***, economical***Parenteral disadvantages: expensive, more dangerous, patientcompliance***, first pass liver effect***
Drug Absorption V
Select the mechanism by which small water soluble agents[1], mostlipophilicdrugs [2] and large molecular weighthormones [3] cross membranes.filtration [1]active transportfacilitated transportpassive diffusion [2] [major mechanism]receptor mediated endocytosis [3]
Drug Absorption VI
Which of the following statements is not true aboutsublingual drug administration?by-pass portal circulationrapid onset of drug actionexcellent method of administering nitroglycerin andepinephrinegood method for administering many drugs ***difficult to hold drugs here for significant periods of time
Drug Distribution I
Select the body water compartments that represent 60% ,40% , 20% , 16% and 4% of an individual's total bodyweight.total body water [60%]extracellular water [20%] Vd = Q/Cpintracellular water [40%]plasma water [4%]interstitial water [16%]
Drug Distribution II
Thiopental has a has a ______ duration of action because thisThiopental has a has a ______ duration of action because thisagent is ______.agent is ______.shortshortrapidly excretedrapidly excretedlonglongslowly excretedslowly excretedlonglongslowly metabolizedslowly metabolizedshortshortrapidly redistributed ***rapidly redistributed ***shortshortrapidly metabolizedrapidly metabolizedlonglongslowly redistributedslowly redistributed

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