Proteau's Study Guide Flashcards
Norepinephrine which adrenergic receptors does it agonize? R or S config? Structural features? short or long acting? selective or non-selective?
a1, a2, B1 R Catechol, primary amine group short-acting non-selective
Epinephrine which adrenergic receptors does it agonize? R or S config? Structural features? short or long acting? selective or non-selective?
a1, a2, B1, B2 R Catechol, secondary amine group short-acting non-selective
what does COMT do?
transfers a methyl group onto the oxygen -> hydrogen leaves, CH3 is replaced
what does MOA do?
replaces NH2 with CO2H
1 or B carbon means?
2 carbons away from N group
2 or a carbon means?
C adjacent to N group
if a drug has a COOH group, what enzyme interacts with it and what is the process it undergoes called?
Adding a COOH group to a drug that acts as norepinephrine makes it what?
L-AAAD causes decarboxylation
prodrug
drugs containing ester groups (COO) require what enzyme for activation?
ester hydrolysis
what does N-isopropyl look like? how does this effect MAO metabolism?
N connected to a C that has two methyl groups attached
slows down MAO metabolism
structure containing N-isopropyl has selectivity for which receptor(s)?
what is the exception?
B1 and B2
only B2 selective if structure cannot undergo COMT
what does N-t-butyl look like? how does this effect MAO metabolism?
N connected to a C that has three methyl groups attached
blocks MAO metabolism
structure containing N-t-butyl has selectivity for which receptor(s)?
B2
if you add a methyl to the 2/a position, what receptor is it selective towards?
will the drug undergo MAO metabolism?
a2
no, blocked by a-methyl group
dobutamine has predominantly what receptor agonist activity?
B1
For B2s, if no COMT what is primary route of metabolism?
sulfonation
for SABA inhalers, which is sulfonated faster, R enantiomer or S enantiomer?
R enantiomer
Which of these is NOT a contributor to the long duration of effect of vilanterol/salmeterol? (2 answers)
a. No metabolism by COMT.
b. Metabolism to a reactive intermediate that can alkylate the receptor, resulting in long term effects.
c. It binds tightly to a second non-polar domain on its target receptor, extending the duration of effect.
d. No metabolism by MAO.
e. The high lipophilicity leads to deeper tissue penetration and slowed clearance.
f. Resistance to sulfonation and/or glucuronidation due to the lack of a suitable structural handle for these Phase II reactions.
g. Greater bronchial tissue penetration which leads to decreased clearance from the lungs.
b,f
What is NOT true about the drug Mirabegron?
a. No R3 modification
b. Has a “bulky” extended N-group with some polar features
c. No metabolism by COMT
d. No metabolism by MAO
e. Undergoes sulfonation as the primary route of metabolism
e
Midodrine is a selective agonist for which receptor?
a1
what makes phenylephrine structurally different from epinephrine? it is a selective agonist for which receptor?
has no OH on the 4th carbon in the ring, only has the OH on the 3rd carbon
a1
what makes ephedrine structurally different from epinephrine? it is a selective agonist for which receptor?
no OH groups on ring, has a methyl attached to the 2/a Carbon with same stereochemistry as 1/B OH
both a and B
what makes pseudoephedrine structurally different from epinephrine?
identical to ephedrine but opposite stereochemistry on the OH group of 1/B Carbon
what makes amphetamine structurally different from epinephrine?
Has zero OH groups with an a methyl
