Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) > MIDTERM 01 - CNS Depressants and Antiseizure Drugs > Flashcards

MIDTERM 01 - CNS Depressants and Antiseizure Drugs Flashcards

1
Q

Are drugs that can be used to slow down or “depress” the functions of the CNS

A

CNS depressants

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

CNS depressants often share at least one MOA: positive modulation of the action of γ-aminobutyric acid (GABA) at __________

A

GABA A receptor complex

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

Drugs that reduce anxiety and exert a calming effect

A

Sedatives/Anxiolytics

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

Drugs that produce drowsiness and encourage the onset and maintenance of a state of sleep; involve a more pronounced depression of the CNS than sedation

A

Hypnotics

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

A major inhibitor neurotransmitter in the brain; deficiency of its activity in the CNS is important in the pathophysiology of anxiety and insomnia

A

Gamma-aminobutyric acid (GABA)

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

2 types of receptors activated by GABA (IM)

A

Ionotropic receptors (GABA A and GABA C), Metabotropic receptor (GABA B)

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

GABA receptor that is the target for many anxiolytics and sedative-hypnotic agents

A

GABA-A receptor

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

GABA A receptor agonist (Drug example)

A

Benzodiazepines

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

GABA A receptor inverse agonist (Drug example)

A

β-carbolines

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

GABA A receptor antagonist (Drug example)

A

Flumazenil

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

A GABA A receptor agonist; increases the frequency of opening of the chloride channel

A

Benzodiazepines

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

A GABA A receptor inverse agonist; increases anxiety, produces panic attacks, and improves memory

A

β-carbolines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

A GABA-A receptor antagonist drug; used clinically to counteract the sedative effect of benzodiazepine overdose

A

Flumazenil

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

___________ is required for the activity (SAR of benzodiazepines)

A

Aromatic/Heteroaromatic ring A

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

An __________ has a higher activity than a heteroaromatic ring (SAR of benzodiazepines)

A

Aromatic ring

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

An electronegative substituent at position ___________ is required for activity (SAR of benzodiazepines)

A

7

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

The more electronegative the atoms are, the __________ the activity (SAR of benzodiazepines)

A

Higher

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

Positions __________, ___________, and __________ should NOT be substituted with an electronegative substituent (SAR of benzodiazepines)

A

6, 8, 9

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

A phenyl ring C at position __________ promotes activity (SAR of benzodiazepines)

A

5

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

If a benzodiazepine is ____________ or __________ substituted with electron withdrawing group, it increases activity (SAR of benzodiazepines)

A

Ortho (2) or diortho (2,6)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

A __________ substitution of a benzodiazepine decreases activity (SAR of benzodiazepines)

A

Para

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

A benzodiazepine __________ a 3-OH group ↓ DOA (short-acting) (SAR of benzodiazepines)

A

With

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

A benzodiazepine __________ a 3-OH group ↑ DOA (long-acting)

A

Without

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

A proton-accepting group at __________ is required (SAR of benzodiazepines)

A

C2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

A 2-__________ group is important for activity (SAR of benzodiazepines)

A

Carbonyl (C=O)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

A nitrogen atom at position __________ is important for activity (SAR of benzodiazepines)

A

1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

A 1,2 fused __________ or __________ ring increases activity and is short acting (SAR of benzodiazepines) (TI)

A

Triazole, Imidazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Triazolam, midazolam (DOA of benzodiazepines)

A

Short acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Alprazolam, estazolam, lorazepam, temazepam, oxazepam (DOA of benzodiazepines)

A

Intermediate acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Chlorazepate, chlordiazepoxide, clonazepam, diazepam, flurazepam, quazepam (DOA of benzodiazepines)

A

Long acting

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

An imidazopyridine; a short acting hypnotic (Examples of nonbenzodiazepine BzRAs)

A

Zolpidem

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

A cyclopyrrolone that is a moderate-acting hypnotic (Examples of nonbenzodiazepine BzRAs)

A

Eszopiclone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

Racemic mixture that contains eszopiclone

A

Zopiclone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

Isomer of zopiclone that is the primary active hypnotic

A

S-isomer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

A pyrazolopyrimidine; a short-acting hypnotic (Examples of nonbenzodiazepine BzRAs)

36
Q

A hormone that plays a role in the circadian rhythm of humans; is a poor hypnotic drug

37
Q

Melatonin is a hormone that is the N-acetylated and O-methylated product of __________ found in the pineal gland

38
Q

Drug derived from melatonin; activate melatonin receptors; more efficacious than melatonin but less efficacious than benzodiazepines as a hypnotic

39
Q

Drugs that are 5,5-disubstituted barbituric acids; increase the duration of the GABA-gated chloride channel openings

A

Barbiturates

40
Q

The __________ is 2,4,6,-trioxohexahydropyrimidine, which lacks CNS depressant activity (SAR of barbiturates)

A

Barbituric acid

41
Q

Replacement of both hydrogens at position __________ with alkyl or aryl groups confers (gives) the activity (SAR of barbiturates)

42
Q

In general, increasing __________ increases hypnotic potency, faster onset of action, and shorter duration of action (SAR of barbiturates)

A

Lipophilicity

43
Q

Increasing number of carbon atoms at the __________ position increases lipophilicity (SAR of barbiturates)

44
Q

__________ increase the lipid solubility of the barbituric acid derivatives (SAR of barbiturates)

A

Unsaturation

45
Q

Addition of alkyl group at __________ increases lipophilicity; leads to quicker onset and shorter duration of action (SAR of barbiturates)

46
Q

Replacement of oxygen by sulfur at position __________ in thiobarbiturates increases lipophilicity (SAR of barbiturates)

47
Q

Barbiturates that are ultra-short acting; they are used as anesthetic, not as sedative-hypnotics (SAR of barbiturates)

A

Thiobarbiturates

48
Q

Thiopental, thiamylal (DOA of barbiturates)

A

Ultra-short acting

49
Q

Pentobarbital and secobarbital (DOA of barbiturates)

A

Short acting

50
Q

Amobarbital, butabarbital (DOA of barbiturates)

A

Intermediate acting

51
Q

Mephobarbital, phenobarbital (DOA of barbiturates)

A

Long acting

52
Q

Structurally similar to the barbiturates, especially phenobarbital (Amidines and imides - miscellaneous sedative-hypnotics)

A

Glutethimide

53
Q

CNS depressant potency increases up to __________ carbon atoms, with activity decreasing thereafter (SAR of alcohols and their carbamate derivatives)

54
Q

Branching of the alkyl chain __________ depressant activity (SAR of alcohols and their carbamate derivatives)

55
Q

Order of potency (SAR of alcohols and their carbamate derivatives)

A

Tertiary > secondary > primary

56
Q

Replacement of a hydrogen atom in the alkyl group by a halogen __________ potency (SAR of alcohols and their carbamate derivatives)

57
Q

Carbamylation of alcohols generally __________ depressant potency (SAR of alcohols and their carbamate derivatives)

58
Q

A mild sedative-hypnotic with a quick onset and short duration of action (Alcohols and their carbamate derivatives - miscellaneous sedative-hypnotics)

A

Ethchlorvynol

59
Q

Officially indicated as an anxiety agent; also a sedative-hypnotic agent and a centrally acting skeletal muscle relaxant (Alcohols and their carbamate derivatives - miscellaneous sedative-hypnotics)

A

Meprobamate

60
Q

A mono-N-isopropyl-substituted relative of meprobamate; indicated in acute skeletomuscular conditions (Alcohols and their carbamate derivatives - miscellaneous sedative-hypnotics)

A

Carisoprodol

61
Q

The p-chloro substituted and 1-carbamate derivative of mephenesin (Alcohols and their carbamate derivatives - miscellaneous sedative-hypnotics)

A

Chlorphenesin carbamate

62
Q

More sustained in effect that mephenesin; the dihydric parent compound, guaifenesin, is used as an expectorant (Alcohols and their carbamate derivatives - miscellaneous sedative-hypnotics)

A

Methocarbamol

63
Q

The dihydric parent compound of methocarbamol used as an expectorant

A

Guaifenesin

64
Q

Used as a sedative in nonoperating room procedures for the pediatric patient (Aldehydes and their derivatives - miscellaneous sedative-hypnotics)

A

Chloral hydrate

65
Q

Chloral hydrate is thought to act principally through a metabolite, __________

A

Trichloroethanol

66
Q

Refers to a combination of ethanol and chloral hydrate

A

Mickey Finn

67
Q

A cyclic trimer of acetaldehyde (Aldehydes and their derivatives - miscellaneous sedative-hypnotics)

A

Paraldehyde

68
Q

Are symptoms of disturbed electrical activity in the brain that cause involuntary movement, sensation, or thought

69
Q

Phenobarbital and primidone are examples of __________ (Antiseizure drugs)

A

Barbiturates

70
Q

A derivative of phenobarbital (Antiseizure drugs - barbiturates)

71
Q

Phenytoin and fosphenytoin are examples of __________ (Antiseizure drugs)

A

Hydantoins

72
Q

Also known as 5,5-diphenylhydrantoin (Antiseizure drugs - hydantoins)

73
Q

The prodrug of phenytoin (Antiseizure drugs - hydantoins)

A

Fosphenytoin

74
Q

Trimethadione and dimethadione are examples of __________ (Antiseizure drugs)

A

Oxazolidinediones

75
Q

Ethosuximide and methsuximide are examples of __________ (Antiseizure drugs)

A

Succinimides

76
Q

Diazepam and clonazepam are examples of __________ (Antiseizure drugs)

A

Benzodiazepines

77
Q

Carbamazepine and oxcarbazepine are examples of __________ (Antiseizure drugs)

A

Iminostilbene (Dibenzazepine) derivates

78
Q

Gabapentin, pregabalin, and vigabatrin are examples of __________ (Antiseizure drugs)

A

GABA analogues

79
Q

A broad spectrum anticonvulsant (Antiseizure drugs - GABA analogues)

A

Valproid acid

80
Q

A bis-carbamate (Antiseizure drugs)

81
Q

Drug from the phenyltriazine class (Antiseizure drugs)

A

Lamotrigine

82
Q

A sulfonamide-type anticonvulsant (Antiseizure drugs)

A

Zonisamide

83
Q

A pyrrolidone derivate; an analog of the nootropic agent, piracetam (Antiseizure drugs)

A

Levetiracetam

84
Q

Levetiracetam is an analog of the nootropic agent, __________

85
Q

Contains nipecotic acid as the active moiety (Antiseizure drugs)

PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) (7 decks)

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