When comparing the EPI to ISO what statment is true?
A. EPI is more stable than ISO
B. Isopropyl is added to epinephrine to make the ISO
C. Adding the Isopropyl group on EPI makes it less likely to undergo MAO metabolism
D. B & C
What kind of metabolism can this group undergo?
This group can undergo ___ metabolism and convert to a(n)____.
A. COMT, Aldehyde
B. MAO, Aldehyde
C. COMT, Carboxylic
D. MAO, Carboxylic
Which of these groups can undergo COMT metabolism?
Which of these statments is true?
A. Metaproterenol is a salt
B. There is only an isopropyl group present in ISO
C. Both are equally succeptable to COMT
D. There is only an Isopropyl grou present in Metaproterenol
In this reaction the green _____ group is changed into a blue ____ goup.
A. Catechol, Resorcinol
B. Resorcinol, Catechol
The two groups circiled are known as ____ and make the structure ____ stable and make it an ____ drug.
A. Ethers, More, Active
B. Ester, Less, Active
C. Ester, More, Pro
D. Ether, Less, Pro
What kind of metabolism is requred to change Bitolterol to the active Colterol metabolite?
A. Ester Hydrolysis
What do the ester groups and rings add to the molecule? (Select All)
C. B2 Selectivity
D. Resistance to COMT metabolism
What is the name of the group circled in levalbuterol?
B. Salicyl alcohol
Levalbuterol is the active ___ isomer of albuterol and requres ___ times less than the normal dose of albuterol
A. R, 4
B. S, 4
C. R, 2
D. S, 2
What is true about the group circled in levalbuterol
A. Makes it harder for MAO to metabolize the amine
B. Increases B2 selectivity
C. Tert-butyl group
D. All of the above
What is the key difference between albuterol and Pirbuterol?
A. Catechol group was changed to a pyrimidine
B. Catechol group was changed to a Pyradine
C. T-butyl group was added
D. Salicyl alcohol
What is the name of this large functional group in Salmeterol?
Based off the structure of salmeterol what can you infer? (Select All)
A. Salicyl alcohol group ensures COMT resistance
B. N-Phenylbutoxyhexyl group ensures MAO resistance
C. Larger groups make the drug short acting
D. Larger groups make the drug more hydrophilic
E. Larger groups make the drug more lipophilic and longer lasting.
T/F N-Phenylbutoxyhexyl, Beta-OH and salicyl alcohol in salmeterol ensure direct activity, B2 selectivity and potency
In the structure of formoterol fumarate the red structure is an _____ and the blue structure is an _____.
A. P-Formamide-OH-Phenyl, Isopropyl-O-Methoxy Phenyl
B. M- Formamide-OH-Phenyl, Isopropyl-M-Methoxy Phenyl
C. M-Formamide-OH-Phenyl, Isopropyl-P-Methoxy Phenyl
D. O-Formamide-OH-Phenyl, Isopropyl-P-Methoxy Phenyl
When they changed formotorol fumarate to arformoterol the OH and CH3 groups were changed to a ____ configuration and made the molecule ____ potent
A. R, R, Less
B. S, S, Less
C. R, R, More
D. S, S, More
Based on the circled structures in Indacterol what statement is true?
A. Makes the molecule an "Ultra-long Acting" molecule (40-56hr)
B. Increase COMT resistance
C. Increase MAO resistance
D. Slower dissociation from lung tissue
E. All of the above
In the drug molecule Indacterol the red structure is a____ and the blue structure increases ____ resistance and _____
A. 8-hydroxyquinolinone, COMT, Lipophilicity
B. 8-hydroxyquinolinone, MAO, Hydrophilicity
C. 8-hydroxyquinolinone, MAO, Lipophilicity
D. 8-Hydroxyquinolinone, COMT, Hydrophilicity
What kind of reaction is occuring in Olodaterol?
A. Sulfation using SULT
B. Glucuronidation using SULT
C. Glucuronidation using UGT
D. Sulfation using UGT
What is the name of this circled group?
In the general SAR for Adrenergic agents what statments are true? (Select All)
A. R1 bulky groups increase beta 2 selectivity AND MAO resistance
B. R2 Alpha-groups increase MAO resistance
C. R3 Beta-hydroxy group is not required for direct activity
D. R3 Beta-hydroxy group is required for direct activity.
E. Changing catechol group does not affect DoA (duration of action)
A, B, D
T/F In the general SAR for adrenergic agents the R conformation for the chiral carbons increases activity
T/F Selectivity of Beta adrenergic agonists is dose dependent
Given the answer choices below, Molecule X would be most susceptible to ____ metabolism.
T/F Antimuscarinics will block M3 receptors and cause bronchoconstriction
Ipratropium is an antimuscarinic that resembles the drug ____
In comparison to Ipratropium, Tiotropium is more ____ due to the _____ groups circled.
A. Lipophilic, Thiophene
B. Hydrophilic, Thiophene
C. Lipophilic, Furan
D. Hydrophilic, Furan
In comparison to Ipratropium, Tiotropium dissoaciates from the M3 receptors more ____ due to the ____ funcitional group
A. Quickly, Thiophene
B. Slowly, Quarternary Amine
C. Quickly, Quarternary Amine
D. Slowly, Thiophene