Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Drug Action I > Block 1 - Respiratory Med Chem > Flashcards

Block 1 - Respiratory Med Chem Flashcards

(84 cards)

Start Studying
1
Q

What are esters metabolized to?

A

carboxylic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

How are histamine receptors similar to muscarenic?

A

Contains ionic and h-binding sites

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Describe the SAR of 1st gen Antihistamines

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the classes of 1st gen antihistamines?

A
  1. ethanolamine ethers
  2. tricyclic
  3. piperazine
  4. alkylamines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Why does ethanol amine have short half lives?

A

N-dealkylation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What gives doxylamine antimuscarinic effects?

A

CH3 on X and ionic binding of 3 amine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

How does alkyl amines different from other 1st AH?

A

longer duration of action, less sedation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the primary metabolism of alkyl amines?

A

N-dealkylation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are piperazine?

A

Hydroxyzine -> cetirizine
anticholinergic ADRs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What gives tricyclic AH LA?

A

S brings more lipophilicity to rings

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What makes tricyclic different than antipsychotics phenothiazines?

A

Antipsychotics are unbranched and have a substituent on ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What makes 2nd gen AH differ from 1st?

A
  1. Less anticholinergic
  2. Less CNS/ sedation
  3. More hydrophilic
  4. long half-life
  5. Varied structures
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Why does Fexofenadine have less CNS activity?

A

effluxes out of BBB by the p-gp
Folds on itself to bind to H1 receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Why should you drink fruit juice with allegra?

A

Juices inhibit OAT1A2 from absorbing drug into the blood stream

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What drug is pseudo irreversible? why?

A

Zyrtec because will strongly bind to receptor and slowly release from it

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Why does Zyrtec not have CNS activity?

A

Folds on itself like Allegra and removed by p-gp

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is the difference between loratadine and desloratidine?

A

Des is more potent with a longer half-life, a metabolite of loratadine.
Both are removed by p-gp by do not fold

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What are the characteristics of olopatadine?

A
  1. Zwitterion
  2. Topical
  3. Long duration and rapid onset
  4. Inhibits mediators and mast cell stabilizer
  5. Minimal must effect from N and COOH
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the MAO of azelastine?

A
  1. Mast cell stabilizer
  2. LTC4 inhibition
  3. Antihistamine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What is the MOA for cromolyn?

A
  1. Mast cell degranulation inhibitor
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Why is cromolyn polarity absorbed?

A

Contains 2- charges that must both be neutralized to pass through membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the endogenous steroids?

A

Hydrocortisone and cortisone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Out of the 2 endogenous steroids which is active?

A

hydrocortisone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What makes a steroid active?

A
  1. ketone on 3 and 20
  2. alkene on 4
  3. OH on 11, 17, 21
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
At what positions do steroids bind?
beta
26
What is the difference between glucocorticoids and mineralocorticoids?
G: glucose homeostasis, anti-inflammatory M: sodium and water retention
27
Why are ketone and OH groups important for steroids?
to form H bond at GC receptor sites
28
What is the exception on the OH 21 on steroids?
Can be Cl or thioester
29
What make steroids a prodrug?
Ketone on 11 or 21
30
What makes a steroid more acidic?
F on 9a or 12a
31
What are the mechanism of inactivating a GC steroid?
1. Loss of 21 OH 2. Ring A reduction 3. C-17 oxidation 4. C11 keto enol isomerization
32
Why is the purpose of esterfying GC?
1. increase or decrease lipophilicity 2. Increase log P (lipo) -> longer duration of action and more local activity 3. prodrug
33
What portion of the steroid can be esterized?
C21 (easiest) C17 (slower more hindered) C11 (highly hindered so no activity)
34
Why would diesters in steroid be beneficial?
Lipo enhancement and increased duration of action (slow metabolism)
35
What are benefits of hydrophilic esters?
1. IM/IV use 2. Rapid onset 3. easy excretion by kidneys 4. wider distribution and and more ADRs
36
What are the important qualities of Inhaled GC?
1. fast systemic clearance following GI absorption 2. short half-life 3. no active metabolites 4. high affinity for gr
37
What are the endogenous agonists of adrenergics?
NE/E
38
What does the insertion on 16b methyl on a steroid mean?
decrease MC activity
39
What does the insertion on 9a chloro on a steroid mean?
increased GC and MC activity
40
What does the insertion on 9a chloro on a steroid mean?
increased GC and MC activity
41
What does the insertion of 16,17 acetal on a steroid mean?
decreased MC activity
42
Insertion of 6a F?
Increase GC
43
Insertion of 9aF?
Increases MC and GC
44
Double bond on 1?
slows ring A reduction (longer duration of action)
45
Where are b2 receptors located?
skeletal muscle, lungs, live, uterus for relaxation, intestine
46
how does isoproterenol differ from NE and E?
only b selectivity
47
What metabolized E and NE?
COMT and MAO
48
What is metabolized by COMT?
Catechol to methyl on O
49
What is metabolized by MAO?
1 amine to aldehyde
50
How do you slow do COMT on adrenergic?
Don't have OH group on neighboring carbons
51
What is SAR of adrenergic?
1. 2 carbon spacer between amine and phenyl ring 2. Ethyl group on R2 reduces MAO metabolism and increase b selectivity 3. Positively charged amine with pKa of 8.5-10 4. R1 increasing size -> b selectivity blocking MAO 5. 1 H bond former in phenyl
52
What provides b2 selectivity?
tert, but, phenyl ring substitutions, ethyl group on R2
53
What is the difference between albuterol and leva?
AL: racemic Leva: R isomer
54
Why is salemeterol longer acting?
1. resistant to MAO and COMT 2. larger drug that anchors to protein 3. very lipophilic with b2 selectivity
55
How does formoterol differ from salmeterol?
1. faster onset and great water solubility 2. 12 hr duration 3. B2 and resistant to MAO and COMT
56
What is the MOA of Zileuton?
1. Inhibits 5-LOX that produces leukotrienes 2. N-OH chelates iron in enzyme 3. Good absorption and high PPB 4. Increases plasma levels of propranolol, theophylline, and warfarin
57
What is the SAR of leukotriene receptor antagonists?
1. acidic or negative ionizable functional group (COOH etc) 2. H-bond acceptor function 3. 3 hydrophobic regions
58
Why does singular have high PPB?
lipophilic and acidic that binds to albumin
59
Why can food decrease the effects of Zafirlukast?
Food makes the stomach more basic. Drug becomes ionized in the environment and unable to be absorbed into the blood do to its charge
60
What is the difference between levorotatory and dextrotatory isomers?
L: are for pain (analgesic) D: are for cough (antitussive)
61
What is the opiod receptor?
µ OH on 3 is the active form
62
What is the structure of codeine?
Prodrug of mrophine contain a methyl on 3 to improve F
63
How does codeine metabolize to morphine?
O dealkylation by CYP2D6 becoming a phenyl for activity that binds to µ
64
What are the ADRs of opioids (levo isomer)?
Constipation, drowsiness, lightheadedness
65
What make dextromethorphan differ from tradition opioids?
low binding to µ and more for antitussives without ADRs of levos. Parent and metabolite are actives Antagonizes NMDA and ø-1 receptors instead Contains a methoxy
66
Describe the MOAs of Guaifenesin?
1. Muscle relaxant and anticonvulsant, NMDA antagonist 2. Increases volume and reduce viscosity of mucous
67
Describe MOA of Dornase Alfa?
Used for CF that causes over secretion of fluid containing DNA, drug contains DNAse I to breakdown DNA
68
What is the MOA of NAC?
1. antioxidant and expectorant that loosens mucus 2. reduces inflammation in tubes and lung
69
What is important about benzonatate?
Local anesthetic Potential OD if chewed or dissolved
70
Endogenous NT of Antimuscarinics?
ACh
71
Common ADRS of antimuscarinics?
1. Blurred vision 2. Dry mouth 3, Tachycardia 4. Urinary difficulty 5. HA
72
How does ACh bind of receptor?
2 H-bond with O-H Asp-tert amine (ionic)
73
What are the pharmacophores of atropine?
Alcohol, amides, alcohol esters, alcohol ethers
74
What is the SAR of antimuscarinics?
1. Carbon next to ring is more active 2. Methyl on N is optimal 3. Quat N is good for ionic bond but not necessary, can replace with carbon but creates lower affintiy 4. Carbocylic or heterocyclic ring(s)
75
What is the difference between ipratropium and tiotropium?
I: not selective for muscarinic receptors (Short DOA: 6 hr) T: M1 and M3 selectivity (DOA: 24 hr - lipophilic) Poor absorption from quat amine
76
Describe the t1/2 of aclidinium?
Due to rapid hydrolysis of ester bond in plasma to acid and alcohol derivatives M2 and M3 selectivity t1/2: 2.4 min
77
Natural PDEi?
1. Caffeine 2. Theophylline 3. Theobromine
78
How does Theophylline bind to PDEi?
2 hydrophobic bond 2 h-bond
79
Why is theophylline problematic?
1. Narrow TI 2. Poor aqueous solubility 3. Potent
80
What is the salt form of theophylline?
aminophylline
81
What is gives roflumilast its PDE4i activity?
ring with 2 ethers Long t1/2 and active metabolite
82
What are the benefits of Varenicline (Chantix)?
1. reduces cravings 2. partial agonist of nicotine receptor 3. lower efficacy of binding
83
What are the natural inhibitors of dopamine?
CNS stimulats
84
How does bupropion differ from meth?
1. No metabolites with sympathomimetic and anorexigenic properties 2. tert but inhibits N-dealkylation that is associated with meth 3. extensively metabolized

Drug Action I (32 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions