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TCEP Review > Module 1.4: Medicinal Chemistry > Flashcards

Module 1.4: Medicinal Chemistry Flashcards

Oraganic Medicinal Chemistry

1
Q

SAR adrenergic Agonist: Substitution at R2

A

Increase in alpha 2 activity

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2
Q

SAR adrenergic Agonist: Substitution at R2

A

Increases B-activity
Increase CNS & Oral activity
Decrease degradation by MAO

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3
Q

SAR adrenergic Agonist: Aromatic Substitution

A

3-OH is for Alpha activity
* 4-OH is for Beta activity
* 3&4-OH – both

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4
Q

SAR adrenergic Agonist: Aromatic Substitution
3-OH is for
* 4-OH is for
* 3&4-OH – both

A

3-OH is for Alpha activity
* 4-OH is for Beta activity
* 3&4-OH – both

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5
Q

SAR adrenergic Agonist: aromatic substitution at3 and 4
___, ____ oral activity

A

Polar, decreases oral activity

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6
Q

SAR adrenergic Agonist: aromatic sustitution: Metabolized by ___ leading to Shorter DOA

A

COMT

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7
Q

SAR adrenergic Agonist: aromatic sustitution: Metabolized by COMT leading to _____

A

Shorter DOA

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8
Q

Adrenergic agonist means

A

Sympathomimetic activity

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9
Q

SAR of Adrenergoc Agonist:
Lack of 1 OH –__
▪ Absence of both OH – __

A

resistance to COMT
indirect activity

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10
Q

Adrenergic agonist means

A

Fight or flight response: Sympathomimetic

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11
Q

SAR adrenergic Agonist: Aromatic Substitution
3-OH replacement by ___ 3-OH replacement by _________ will
→increase Beta activity
→ decrease degradation by COMT

A

Methanol

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12
Q

SAR adrenergic Agonist: Aromatic Substitution Moving 4-OH to 5-OH will
___
____

A

→increase B2 activity
→ decrease degradation by COMT

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13
Q

SAR adrenergic Agonist: Aromatic Substitution
Moving____ will
→increase B2 activity
→ decrease degradation by COMT

A

4-OH to 5-OH

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14
Q

SAR of Adrenergoc Agonist:
____ – resistance to COMT
_____- indirect activity

A

Lack of 1 OH
Absence of both OH –

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15
Q

SAR of Adrenergoc ANTAGONIST: Alpha blocker
pharmacopore

A

Quinazoline

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16
Q

SAR of Adrenergoc ANTAGONIST: ____

A

Sympatholitic

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17
Q

SAR of Adrenergoc ANTAGONIST: Alpha blocker
Prototype

A

Prazosin

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18
Q

SAvR of Adrenergoc ANTAGONIST: Alpha blocker
____ is essential for the activity

A

4-amino group

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19
Q

SAR of Adrenergoc ANTAGONIST: Alpha blocker
__ 2nd position of quinazoline

A

Piperazine

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20
Q

SAR of Adrenergoc ANTAGONIST: Alpha blocker
Positions __, __, __, __ can be varied

A

5,6,7,8

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21
Q

SAR of Adrenergoc ANTAGONIST: Alpha blocker
Can be any heterocyclic ring

A

Piperazine

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22
Q

SAR of Adrenergoc ANTAGONIST: Alpha blocker
examples

A

Piperazine and piperadine

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23
Q

SAR of Adrenergoc ANTAGONIST: BETA blocker
Pharmacopore

A

Aryloxopropanol

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24
Q

SAR of Adrenergoc ANTAGONIST: BETA blocker
Prototype

A

Propranolol

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25
Q

SAR of Adrenergoc ANTAGONIST: BETA blocker
____ can be varied with other heteroaromatic ring

A

Aryl ring

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26
Q

SAR of Adrenergoc ANTAGONIST: BETA blocker
__, and __ both beneficial to activity

A

Branching & extension

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27
Q

SAR of Cholinergic agonists: ___

A

parasympathomimetic

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28
Q

SAR of Cholinergic agonists: Direct Acting
Pharmacopore

A

Acetylcholine

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29
Q

SAR of Cholinergic agonists: Direct Acting
Prototype

A

Acetylcholine

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30
Q

SAR of Cholinergic agonists: Direct Acting
Acetylcholine components Functional group

A
  • Acetoxy/Ester Portion
  • Ethylene Bridge
  • Quaternary Nitrogen
    All are essential for the activity – overall size of the molecule should not be altered
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31
Q

SAR of Cholinergic agonists: Direct Acting
Acetylcholine components Functional group
All are essential for the activity – overall size of the molecule ___ be altered

A

should not

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32
Q

SAR of Cholinergic agonists: Direct Acting
_____
* The methyl group cannot be extended
but may be replaced with NH2 (Carbamate)
* Not easily hydrolyzed
* Longer DOA

A

Acetoxy/Ester Portion

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33
Q

SAR of Cholinergic agonists: Direct Acting
Acetoxy/Ester Portion
* ____ cannot be extended
but may be replaced with NH2

A

The methyl group

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34
Q

SAR of Cholinergic agonists: Direct Acting
_____ cannot be altered

A

Ammonium group

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35
Q

SAR of Cholinergic agonists: Direct Acting
Acetoxy/Ester Portion
Not easily ____
Longer ___

A

hydrolyzed
DOA

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36
Q

SAR of Cholinergic agonists: Direct Acting
___: Addition of methyl increase muscarinic selectivity; longer duration of action

A

choline/ ethylene bridge

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37
Q

SAR of Cholinergic agonists: INDIRECT Acting
- Prototype: Physostigmine
* Equivalent to the ester of acetylcholine (recognize by AChE but not easily hydrolyzed by the enzyme

A

Carbamate

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38
Q

SAR of Cholinergic agonists: Direct Acting
choline/ ethylene bridge : Addition of ___ increase muscarinic selectivity; longer duration of action

A

methyl

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39
Q

SAR of Cholinergic agonists: INDIRECT Acting
Prototype of Carbamate

A

Physostigmine

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40
Q

SAR of Cholinergic agonists: INDIRECT Acting
Carbamate:
Equivalent to the ____ (recognize by AChE but not easily hydrolyzed by the enzyme)

A

ester of acetylcholine

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41
Q

SAR of Cholinergic agonists: INDIRECT Acting
Carbamate: has a ___ group

A

amino group

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42
Q

SAR of Cholinergic agonists: INDIRECT Acting
Carbamate: has an amine group to prevent ____

A

hydrolysis

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43
Q

SAR of Cholinergic ANTAGONIST:
_____
Prototype drug: Atropine
Contains Tropane ring system

A

Amino Alcohols Esters SAR

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44
Q

SAR of Cholinergic ANTAGONIST:
Amino Alcohols Esters SAR
Prototype drug: ___
Contains Tropane ring system

A

Atropine

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45
Q

SAR of Cholinergic ANTAGONIST:
Amino Alcohols Esters SAR
Prototype drug: Atropine
Contains _____system

A

Tropane ring

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46
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
MOA: Increase ______________ of opening of GABA-gated Chloride Channel

A
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47
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
__
C=O – is essential for the activity
* Fused triazole or Imidazole ring at positions 1 and 2 – increases activity
* Fused ring – Imidazole = Midazolam

A

Benzodiazepine

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48
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
____
MOA: Increase frequency of opening of GABA-gated Chloride Channel

A

Benzodiazepine

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49
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
MOA: Increase frequency of opening of ____

A

GABA-gated Chloride Channel

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50
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
MOA: Increase ______________ of opening of GABA-gated Chloride Channel

A

Frequency

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51
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
___ – is essential for the activity
* Fused triazole or Imidazole ring at positions 1 and 2 – increases activity
* Fused ring – Imidazole = Midazolam

A

C=O Carboxyl

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52
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
C=O – is essential for the activity
_____ or Imidazole ring at positions 1 and 2 – increases activity
* Fused ring – Imidazole = Midazolam

A
  • Fused triazole
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53
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
C=O – is essential for the activity
* Fused triazole or ____ at positions 1 and 2 – increases activity
* Fused ring – Imidazole = Midazolam

A

Imidazole ring

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54
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
C=O – is essential for the activity
* Fused triazole or Imidazole ring at positions ____ – increases activity
* Fused ring – Imidazole = Midazolam

A

1 and 2

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55
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
C=O – is essential for the activity
* Fused triazole or Imidazole ring at positions 1 and 2– _____
* Fused ring – Imidazole = Midazolam

A

increases activity

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56
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
C=O – is essential for the activity
* Fused triazole or Imidazole ring at positions 1 and 2– increases activity
*______ – Imidazole = Midazolam

A

Fused ring

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57
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine

A
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58
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
______ substitution with EWG increases the
activity= increases CNS Activity

A

X - Carbon7

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59
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine
X: substitution with EWG increases the
activity= _______

A

increases CNS Activity

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60
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine= _____ group – increases the activity
* Prime numbering in the aromatic ring
indicates the possible attachment of
substituents
* 2’ or 2’ and 6’ – substitution with EWG will
increase the drug activity
* 4’ substitution – will decrease the activity

A

5-phenyl

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61
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine= 5-phenyl group – ___
* Prime numbering in the aromatic ring
indicates the possible attachment of
substituents
* 2’ or 2’ and 6’ – substitution with EWG will
increase the drug activity
* 4’ substitution – will decrease the activity

A

increases the activity

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62
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine= 5-phenyl group – increases the activity
* ______ numbering in the aromatic ring
indicates the possible attachment of
substituents
* 2’ or 2’ and 6’ – substitution with EWG will
increase the drug activity
* 4’ substitution – will decrease the activity

A

Prime

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63
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine= 5-phenyl group – increases the activity
* Prime numbering in the aromatic ring indicates the possible attachment of substituents
*______ – substitution with EWG will
increase the drug activity
* 4’ substitution – will decrease the activity

A

2’ or 2’ and 6’

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64
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
BenSAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine= 5-phenyl group – increases the activity
* Prime numbering in the aromatic ring
indicates the possible attachment of
substituents
* 2’ or 2’ and 6’ – substitution with EWG will
increase the drug activity
*______ – will decrease the activityzodiazepine= 5-phenyl group – increases the activity

A

4’ substitution

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65
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Benzodiazepine= 5-phenyl group – increases the activity
* Prime numbering in the aromatic ring
indicates the possible attachment of
substituents
* 2’ or 2’ and 6’ – substitution with EWG will
increase the drug activity
* 4’ substitution – will ____ the activity

A

decrease

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66
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates MOA: Increase duration of
____

A

opening of GABA-gated Chloride Channel

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67
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates MOA: Increase _____________ of
opening of GABA-gated Chloride Channel

A

duration

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68
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates
_______
* Increase lipophilicity
* Quick Onset and Short DOA

A

R1 Alkyl substitution

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69
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates
R1 Alkyl substitution
*___
* Quick Onset and Short DOA

A

Increase lipophilicity

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70
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates
R1 Alkyl substitution
* Increase lipophilicity
* Quick Onset and ___

A

Short DOA

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71
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates
______
* Increase lipophilicity
* Ultra-short acting effect

A

Replacing oxygen w/ sulfur

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72
Q

SAR of Anxiolytics, Sedative, and Hypnotic agents
Barbiturates
R5 Alkyl or Aryl (Aromatic ring)
substitution
* Increase ____

A

lipophilicity

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73
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
_______
* Increases the potency

A

R2 EWG substitution

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74
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
R2 EWG substitution
* _____

A

Increases the potency

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75
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
3 degree Amine
* ____ must have a
N-containing side chain on the ring N and must be separated by at least 3C!
* Essential for the activity

A

R-group

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76
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
3 degree Amine
* R-group must have a
___ side chain on the ring N and must be separated by at least 3C!
* Essential for the activity

A

N-containing

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77
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
3 degree Amine
* R-group must have a
N-containing side chain on the ring N and must be separated by at least ___
* Essential for the activity

78
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
3 degree Amine
* R-group must have a
N-containing side chain on the ring N and must be separated by at least 3C!
* ______

A

Essential for the activity

79
Q

SAR of antipsychotic and antidepressant drug
______
SAR is somehow related to antipsychotic

A

Antidepressants:

80
Q

SAR of antipsychotic and antidepressant drug
Antipsychotic :
Tertiary amine is essential for the activity of___, and ___

A

antihistamine and anticholinergic

81
Q

SAR of antipsychotic and antidepressant drug
_____
The ring side and side chain Nitrogen is separated by 3C

A

Antidepressants

82
Q

SAR of antipsychotic and antidepressant drug
___
The Central Ring System makes the two aromatic rings “skewed” which is required for the activity

A

Antidepressants

83
Q

Isolated from Papaver
somniferum

A

SAR of Opiod Analgesic

84
Q

What is the pharmacopore of SAR of Opiod Analgesic

A

aromatic ring
Phenol
tertiary amine

85
Q

Opiod Analgesic SAR: It is the aromatic ring

86
Q

Opiod Analgesic SAR: ___ + 3-OH is the phenol

87
Q

Opiod Analgesic SAR: contains the tertiary amine

88
Q

Opiod Anlagesic: Addition of ___ to 3C will result to Codeine

89
Q

Opiod Anlagesic: Addition of methyl to 3C will result to _____

90
Q

Opiod Anlagesic: Addition of methyl to 3C will result to codeine
Addition of either ___or ___ will decrease the activity

91
Q

Opioid Analgesic SAR:
▪______ removal of a particular part of the molecule and observe its effect to the activity

A

Drug dissection:

92
Q

Opioid Analgesic SAR:
Drug dissection: removal of a 6-OH or Alkene at position 7 or 8= _____

A

Retained activity

93
Q

Opioid Analgesic SAR: Drug dissection: removal of ring D= ____

A

Decreased activity

94
Q

Opioid Analgesic SAR:
Drug dissection: removal of ring E
* retained activity
* Will result to ___ such as
Levorphanol which are more potent
and longer acting than Morphine

A

morphinans

95
Q

Opioid Analgesic SAR:
Drug dissection: removal of ring E
* _____
* Will result to morphinans such as
Levorphanol which are more potent
and longer acting than Morphine

A

Retained activity

96
Q

Opioid Analgesic SAR:
Drug dissection: ______
* Retained activity
* Will result to morphinans such as Levorphanol which are more potent and longer acting than Morphine

A

removal of ring E

97
Q

Opiod Analgesic: Drug dissection: removal of ring ___
* Retained activity
* Will result to Benzomorphans such as Pentazocine

A

C and D
also E

98
Q

Opiod Analgesic: Drug dissection: removal of ring C and D
* _____
* Will result to Benzomorphans such as
Pentazocine

A

Retained activity

99
Q

Opiod Analgesic: Drug dissection: removal of ring C and D
* Retained activity
* Will result to ___ such as
Pentazocine

A

Benzomorphans

100
Q

Opiod Analgesic: Drug dissection: removal of ring __, __, and __
* Retained activity
* Will result to 4 phenylpiperidines such as Fentanyl (more flexible molecules)

A

B, C and E

101
Q

Opiod Analgesic: Drug dissection: removal of ring C and D
* Retained activity
* Will result to Benzomorphans such as
___

A

Pentazocine

103
Q

Opiod Analgesic: Drug dissection: removal of ring B, C and E
* ___
* Will result to 4 phenylpiperidines such as Fentanyl (more flexible molecules)

A

Retained activity

104
Q

Opiod Analgesic: Drug dissection: removal of ring B, C and E
* Retained activity
* Will result to 4 ___ such as Fentanyl (more flexible molecules)

A

phenylpiperidines

105
Q

Opiod Analgesic: Drug dissection: removal of ring B, C and E
* Retained activity
* Will result to 4 phenylpiperidines such as __ (more flexible molecules)

106
Q

It is more potent than benzodiazepines

A

Barbiturates

107
Q

it is 100x more potent than morphine

108
Q

Pharmacopore of what
Lipophilic ring that may be
substituted
* A linker (ester or amide)
* Amine group that is usually
tertiary amine

A

SAR of Local anesthetic:

109
Q

SAR of Local anesthetic:
What Functional group is the linker

A

A linker is an ester and amide

110
Q

SAR of Local anesthetic: __ group that is usually tertiary amine

A

amine group

111
Q

Contain a system of conjugated double bonds in macrocyclic lactone rings. They differ from erythromycin in that they are larger and contain the conjugated –ene system of double bonds

112
Q

this MOA: Binds with ergosterol and acts as false membrane component causing membrane disruption belongs to

A

Antifungal agents: Polyenes

113
Q

Polyenes Contain a system of ___ in macrocyclic lactone rings. They differ from erythromycin in that they are larger and contain the conjugated –ene system of double bonds

A

conjugated double bonds

114
Q

Polyenes Contain a system of conjugated double bonds in ___. They differ from erythromycin in that they are larger and contain the conjugated –ene system of double bonds

A

macrocyclic lactone rings

115
Q

Polyenes Contain a system of conjugated double bonds in macrocyclic lactone rings. They differ from _____ in that they are larger and contain the conjugated –ene system of double bonds

A

erythromycin

116
Q

Polyenes Contain a system of conjugated double bonds in macrocyclic lactone rings. They differ from erythromycin in that they are larger and contain the ___ of double bonds

A

conjugated –ene system

117
Q

Polyenes:
26-membered ring-polyenes: ___

118
Q

Polyenes:
38-membered ring-polyenes: ____, ____

A

nystatin, and amphotericin B

119
Q

Polyenes: MOA: Binds with ___ and acts as false membrane component causing membrane disruption

A

ergosterol

120
Q

Source of Amphotericin B

A

Streptomyces nodosus

121
Q

Antifungal agents that is Indicated for the treatment of severe life-threatening infections; systemic mycoses

A

Amphotericin

122
Q

amphotericin B is indicated for the txt of severe life-threatening infections; systemic mycoses

A

Amphotericin B

123
Q

It is a antifungal agents that is Not absorbed systemically when
given orally and is too toxic to be
given parenterally. Hence, is
administered topically

124
Q

Source of nystatin is ___

A

Streptomyces noursei

125
Q

Antifungal agents:
Azole: Synthetic antifungal agents that can achieve ____ for the infecting fungus over host

A

selectivity

126
Q

Polyenes is similar to ____ (Macrolides)

A

Erythromycin

127
Q

Antifungal agents thatmust not br given IM

A

Amphotericin B

128
Q

In griseofulvin, when there is increase in fats = ____ in absorption

129
Q

Antifungal agents
MOA ofAllylamine and related compounds

A

MOA: Inhibits ergosterol synthesis via inhibiting squalene epoxidase.

130
Q

aNTIFUNGAL AGENT that is not absorbed systematically weh given orally and is toxic ____

A

not absorbedsystematically - orally
toxic - parenterally

131
Q

Antifungal agents:
Azole:
___ functionality confers high lipophilicity except Fluconazole

132
Q

Antifungal agents:
___ Isolated from Penicillum griseofulvum

A

griseofulvin

133
Q

Griseofulvin oral bioavailability is ____

134
Q

Antifungal agents:
Used for ringworm infections

A

Griseofulvin

135
Q

Antifungal agents:
______ MOA : Inhibits ergosterol synthesis via inhibiting squalene epoxidase

A

Allylamine and related compounds

136
Q

wha is the MOA of griseofulvin

A

Mitotic spindle poison

137
Q

Antifungal agents
MOA: Mitotic spindle poison

A

Griseovulfin

138
Q

Antifungal agents
Example of Allylamine and related compounds

A

Examples: Naftiline, Terbinafine,
Tolnaftate (not an allylamine)

139
Q

Antifungal agents:
____
▪ MOA: Inhibits lanosterol 14-a-demethylase
* High Conc: Fungicidal
* Low Conc: Fungistatic

140
Q

Antifungal agents:
Azole
▪ MOA: _____
* High Conc: Fungicidal
* Low Conc: Fungistatic

A

Inhibits lanosterol 14-alpha demethylase

141
Q

Antifungal agents:
Azole
▪ MOA: Inhibits lanosterol 14-a-demethylase
* High Conc: _____
* Low Conc: ____

A

Fungicidal
Fungistatic

142
Q

Antifungal agents:
______
▪ MOA: Inhibits lanosterol 14-a-demethylase

143
Q

Antifungal agents:
____Synthetic antifungal agents that can achieve selectivity for the infecting fungus over host

144
Q

Antifungal agents:
_____: Must contain weakly basic imidazole or triazole ring bonded by a nitrogen-carbon linkage to the rest of the structure

145
Q

Antifungal agents:
Azole: Must contain _______ or triazole ring bonded by a nitrogen-carbon linkage to the rest of the structure

A

weakly basic imidazole

146
Q

Antifungal agents:
Azole: The most potent antifungal azoles possess ____ with at least one of which is halogen substitute

A

two or three aromatic rings

147
Q

Antifungal agents:
Azole: Halogen atom that yields most potency is ____

148
Q

Antifungal agents:
Azole:
Non-polar functionality confers ___ except Fluconazole

A

high lipophilicity

149
Q

Antifungal agents:
Azole: Presumably, the large non polar portion of these molecules mimics the non-polar steroidal part of ___

A

lanosterol 14-a-demethylase

150
Q

Antifungal agents:
Azole:
▪ Substitution at other positions of the ring yields ____

A

inactive compounds.

151
Q

Antifungal agents:
Azole: Non-polar functionality confers high lipophilicity except ___

A

Fluconazole

152
Q

Antifungal agents:
Azole: Presumably, the large non polar portion of these molecules mimics the ___part of lanosterol 14-a-demethylase

A

non-polar steroidal

153
Q

Azole SAR:
Imidazole Examples

A

COMET-K
Clotrimazole
Oxiconazole
Miconazole
Econazole
Tioconazole
-
Ketoconazole

154
Q

Azole SAR:
TRIAZOLE, Examples

A

FITVIP
Fluconazole
Itraconazole
Terconazole
Voriconazole
Isavuconazole
Posaconazole

155
Q

Nucleoside
Flucytosine
MOA: Taken up by ___ and is
converted to 5-fluorouracil which
inhibits thymidylate synthase.

156
Q

Nucleoside
____
MOA: Taken up by fungi and is
converted to 5-fluorouracil which
inhibits thymidylate synthase.

A

Flucytosine

157
Q

It is an antifungal agent that is Taken with_____ to decrease its resistance.

A

It is an antifungal agent that is Taken with_____ to
decrease its resistance.

158
Q

Nucleoside
Flucytosine
MOA: Taken up by fungi and is
converted to ____ which
inhibits thymidylate synthase.

A

5-fluorouracil

159
Q

Nucleoside
____
MOA: Taken up by fungi and is
converted to 5-fluorouracil which
inhibits ____

A

thymidylate synthase.

160
Q

It is an antifungal agent that is Taken with_____ to
decrease its resistance.

A

Amphotericin B

161
Q

__
Generalities: Have one common
structural features – a quinoline ring or a quinoline with an additional benzene added (an acridine ring)

A

Antimalarial agents

162
Q

Antimalarial agents
Generalities: Have one common
structural features – a _____ring or a ____ with an additional benzene added (an acridine ring)

163
Q

Antimalarial agents
Generalities: Have one common
structural features – a quinoline ring or a quinoline with an additional ____ added (an acridine ring)

165
Q

Used against the Plasmodium
species

A

Antimalarial agents

166
Q

Antimalarial agents: is used as____ species

A

Plasmodium species

167
Q

Antimalarial agents
Cinchona Alkaloid
______
Quinine’s spectrum of activity is considered to narrow for prophylactic use relative to the synthetic agents.

A

Quinine and Quinidine

168
Q

Quinine and Quinidine
of activity is considered to narrow for prophylactic use relative to the synthetic agents.

A

Quinine’s spectrum

169
Q

Antimalarial agents
Quinine and Quinidine
Quinine’s spectrum of activity is considered to narrow for ____ relative to the synthetic agents.

A

prophylactic use

170
Q

Antimalarial agents
Cinchona Alkaloid: Is still indicated for malaria caused by ___ to other agents like chloroquine

A

P.falciparum resistant

171
Q

Antimalarial agents
Side effects of Cinchona Alkaloid

A

Cinchonism (nausea, vomiting,
tinnitus, and vertigo)

172
Q

Antimalarial agents
Cinchona Alkaloid: Is still indicated for malaria caused by P.falciparum resistant to other agents lwhat is the ike____

A

chloroquine

173
Q

What is the manifestation of Cinchonism

A

nausea, vomiting, tinnitus, and vertigo

174
Q

antimalarial agents
Are the closest of the anti-malarial that are based on the quinine structure.

A

4-aminoquinolines

175
Q

Antimalarial agents
This group is substituted at the same position 4 as quinine and have an asymmetric carbon equivalent to quinine’s C-9 position

A

4-aminoquinolines

176
Q

Just as with quinine, both isomers are active and the 4-aminoquinoline racemic mixtures are used

A

4-aminoquinolines

177
Q

considered the prototype of
anti-malaria

A

Chloroquine & Chloroquine PO4

178
Q

Antimalarial agents
Chloroquine & Chloroquine PO4 considered the prototype of anti-malarial
HCl- ____
PO4- ____

A

HCl – parenteral
PO4 – oral

179
Q

DOC for erythrocytic malaria; also
used in SLE and RA

A

4-aminoquinolines

180
Q

4-aminoquinolines is a DOC for
___, ___, and ____.

A

DOC for erythrocytic malaria; also
used in SLE and RA

181
Q

____ – the only drug effective against the exoerythrocytic stages of malaria

A

Primaquine: antimalarial agents

182
Q

Primaquine: the only drug effective against the ____ stages of malaria

A

exoerythrocytic

183
Q

What should be watch out for (WOF) 8-aminoquinolines

A

WOF: hemolytic anemia – G6PD px

184
Q

G6PD stands for

A

Glucose 6 phosphate deficiency

185
Q

what should be watch out for (WOF) 4-aminoquinolines

A

▪ WOF: QT Prolongation- affects the heart

186
Q

Antimalarial agents: Polycyclic Drugs
___ – newest of the
anti-malarial drug from the
natural source of Artemisia
annua

A

Artemisinin

187
Q

Antimalarial agents: Polycyclic Drugs
Artemisinin – newest of the
anti-malarial drug from the
natural source of ____

A

Artemisia annua

188
Q

Used in DMARD (Demodifying anti-rheumatic drug) and also anti-malarial drug

A

Hydroxychloroquine

189
Q

BEQ: What drug has Gemtocidal activity (Vs Vivax, Ovale, Malariae)

A

Quinine Choloquine

190
Q

BEQ: drugs that have an activity to Gametocidal (vs. all plasmodium spp.)

A

Primaquine, Artremisinin

191
Q

BEQ: drugs that have an activity to tissues schizonticide

A

Primaquine

192
Q

BEQ: drugs that have an activity as radical cure

A

Primaquine

193
Q

BEQ: drugs that have an activity as prevention of relapse

A

Primaquine

TCEP Review (6 decks)

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