MIDTERM 01 - CNS Depressants and Antiseizure Drugs

Question 1

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

Answer 1

CNS depressants

Question 2

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

Answer 2

GABA A receptor complex

Question 3

Drugs that reduce anxiety and exert a calming effect

Answer 3

Sedatives/Anxiolytics

Question 4

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

Answer 4

Hypnotics

Question 5

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

Answer 5

Gamma-aminobutyric acid (GABA)

Question 6

2 types of receptors activated by GABA (IM)

Answer 6

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

Question 7

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

Answer 7

GABA-A receptor

Question 8

GABA A receptor agonist (Drug example)

Answer 8

Benzodiazepines

Question 9

GABA A receptor inverse agonist (Drug example)

Answer 9

β-carbolines

Question 10

GABA A receptor antagonist (Drug example)

Answer 10

Flumazenil

Question 11

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

Answer 11

Benzodiazepines

Question 12

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

Answer 12

β-carbolines

Question 13

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

Answer 13

Flumazenil

Question 14

___________ is required for the activity (SAR of benzodiazepines)

Answer 14

Aromatic/Heteroaromatic ring A

Question 15

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

Answer 15

Aromatic ring

Question 16

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

Answer 16

7

Question 17

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

Answer 17

Higher

Question 18

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

Answer 18

6, 8, 9

Question 19

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

Answer 19

5

Question 20

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

Answer 20

Ortho (2) or diortho (2,6)

Question 21

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

Answer 21

Para

Question 22

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

Answer 22

With

Question 23

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

Answer 23

Without

Question 24

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

Answer 24

C2

Question 25

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

Answer 25

Carbonyl (C=O)

Question 26

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

Answer 26

1

Question 27

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

Answer 27

Triazole, Imidazole

Question 28

Triazolam, midazolam (DOA of benzodiazepines)

Answer 28

Short acting

Question 29

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

Answer 29

Intermediate acting

Question 30

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

Answer 30

Long acting

Question 31

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

Answer 31

Zolpidem

Question 32

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

Answer 32

Eszopiclone

Question 33

Racemic mixture that contains eszopiclone

Answer 33

Zopiclone

Question 34

Isomer of zopiclone that is the primary active hypnotic

Answer 34

S-isomer

Question 35

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

Answer 35

Zaleplon

Question 36

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

Answer 36

Melatonin

Question 37

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

Answer 37

Serotonin

Question 38

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

Answer 38

Ramelteon

Question 39

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

Answer 39

Barbiturates

Question 40

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

Answer 40

Barbituric acid

Question 41

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

Answer 41

5

Question 42

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

Answer 42

Lipophilicity

Question 43

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

Answer 43

R5

Question 44

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

Answer 44

Unsaturation

Question 45

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

Answer 45

R1

Question 46

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

Answer 46

2

Question 47

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

Answer 47

Thiobarbiturates

Question 48

Thiopental, thiamylal (DOA of barbiturates)

Answer 48

Ultra-short acting

Question 49

Pentobarbital and secobarbital (DOA of barbiturates)

Answer 49

Short acting

Question 50

Amobarbital, butabarbital (DOA of barbiturates)

Answer 50

Intermediate acting

Question 51

Mephobarbital, phenobarbital (DOA of barbiturates)

Answer 51

Long acting

Question 52

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

Answer 52

Glutethimide

Question 53

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

Answer 53

8

Question 54

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

Answer 54

Increases

Question 55

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

Answer 55

Tertiary > secondary > primary

Question 56

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

Answer 56

Increases

Question 57

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

Answer 57

Increases

Question 58

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

Answer 58

Ethchlorvynol

Question 59

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)

Answer 59

Meprobamate

Question 60

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

Answer 60

Carisoprodol

Question 61

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

Answer 61

Chlorphenesin carbamate

Question 62

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

Answer 62

Methocarbamol

Question 63

The dihydric parent compound of methocarbamol used as an expectorant

Answer 63

Guaifenesin

Question 64

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

Answer 64

Chloral hydrate

Question 65

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

Answer 65

Trichloroethanol

Question 66

Refers to a combination of ethanol and chloral hydrate

Answer 66

Mickey Finn

Question 67

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

Answer 67

Paraldehyde

Question 68

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

Answer 68

Seizures

Question 69

Phenobarbital and primidone are examples of __________ (Antiseizure drugs)

Answer 69

Barbiturates

Question 70

A derivative of phenobarbital (Antiseizure drugs - barbiturates)

Answer 70

Primidone

Question 71

Phenytoin and fosphenytoin are examples of __________ (Antiseizure drugs)

Answer 71

Hydantoins

Question 72

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

Answer 72

Phenytoin

Question 73

The prodrug of phenytoin (Antiseizure drugs - hydantoins)

Answer 73

Fosphenytoin

Question 74

Trimethadione and dimethadione are examples of __________ (Antiseizure drugs)

Answer 74

Oxazolidinediones

Question 75

Ethosuximide and methsuximide are examples of __________ (Antiseizure drugs)

Answer 75

Succinimides

Question 76

Diazepam and clonazepam are examples of __________ (Antiseizure drugs)

Answer 76

Benzodiazepines

Question 77

Carbamazepine and oxcarbazepine are examples of __________ (Antiseizure drugs)

Answer 77

Iminostilbene (Dibenzazepine) derivates

Question 78

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

Answer 78

GABA analogues

Question 79

A broad spectrum anticonvulsant (Antiseizure drugs - GABA analogues)

Answer 79

Valproic acid

Question 80

A bis-carbamate (Antiseizure drugs)

Answer 80

Felbamate

Question 81

Drug from the phenyltriazine class (Antiseizure drugs)

Answer 81

Lamotrigine

Question 82

A sulfonamide-type anticonvulsant (Antiseizure drugs)

Answer 82

Zonisamide

Question 83

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

Answer 83

Levetiracetam

Question 84

Levetiracetam is an analog of the nootropic agent, __________

Answer 84

Piracetam

Question 85

Contains nipecotic acid as the active moiety (Antiseizure drugs)

Answer 85

Tiagabine