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Pharmacology > Sedative-Hypnotic and Anxiolytic drugs > Flashcards

Sedative-Hypnotic and Anxiolytic drugs Flashcards

1
Q

Benzodiazepines

A 
Alprazolam
Chlordiazepoxide
Diazepam
Estazolam
Flurazepam
Triazolam
Clonazepam
Midazolam
Lorazepam
Oxazepam
Temazepam
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2
Q

Benzodiazepines - MoA

A

They bind between the a and g subunit and increase the affinity of GABA for its binding site on the GABAa receptors-Cl ion channel complex –> Increase the frequency of the channel opening, and increase the influx of Cl at postsynaptic cell –> neuronal membrane hyperpolarization –> counteract the depolarizing effect of excitatory neurotransmitters.
They also inhibit neuronal reuptake of adenosine –> increases inhibitory effect of adenosine on neurons that release ACh from pedunculopontine nucleus of the reticular formation which mediates arousal.

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3
Q

Benzodiazepines - Clinical use

A 
Anxiety disorders
Insomnia
Muscle spasm
Seizure disorders
Spasticity
Alcohol withdrawal
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4
Q

Benzodiazepines - Advers effects

A 
CNS depression
Mild respiratory depression
Drug dependence
Sedation
Anxiolytic effect
Motor incoordination
Dizziness
Excessive drowsiness
Impaired cognitive processing
Affect concentration
Judgment and planning 
Interfere with driving and other psychomotor skills
Hypotension
Arrhythmia

Long-term use:
Physical dependence

If the medication is abruptly discontinued after several months of continues use: withdrawal syndrome; rebound anxiety, insomnia, headache, irritability, muscle twitches, seizures (alprazolam)

Mild euphoria
Reduce behavioral inhibitors

All sedative-hypnotic agents indicated for sleep disorders: increased risk of hypersensitivity reactions (anaphylaxis, angioedema), + complex sleep-related behaviors

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5
Q

Benzodiazepines - Interactions

A

Increase Sedative effect after eating a high-fat meal: fatty meal causes the gallbladder to empty –> delivers bile containing diazepam to intestines for reabsorption into the circulation.

Antidote: Flumazenil;

b-carboline derivatives: inverse agonists (decreased response of an effector system below the basal level). Act to decrease chloride conductance by the GABAa receptor-Cl ion channel –> anxiety and seizures.

Chronic use not recommended during pregnancy

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6
Q

Alprazolam - MoA

A

Converted to short-acting a-hydroxyl metabolite before undergoing glucuronide formation.

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7
Q

Alprazolam - Clinical use

A

Anxiety (primarily)

Panic disorder

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8
Q

Alprazolam - Interactions

A

Alcohol and other CNS depressants potentiate effects

Fluoxetine and fucoxamine increase serum levels and effects

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9
Q

Chlordiazepoxide and Diazepam - MoA

A

Converted to long-acting metabolites: desmethyldiazepam (nordiazepam) –> converted to oxazepam –> excreted as a polar glucuronate conjugate

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10
Q

Chlordiazepoxide, Diazepam - Clinical use

A 
Anxiety
Alcohol detoxification (prevent seizures and other withdrawal symptoms)
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11
Q

Diazepam - Clinical use

A

Terminate acute recurrent seizures
Severe muscle spasm
Spasticity ass with degenerative and demyelinating neurologic disorders.

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12
Q

Chlordiazepoxide, Diazepam, Estazolam, and Flurazepam - Interactions

A

Alcohol and other CNS depressants potentiate effects

Cimetidine increases and rifampin decreases serum levels

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13
Q

Flurazepam - Adverse effects

A

Because it is longer acting: drowsiness and drug hangover the next day

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14
Q

Triazolam - Adverse effects

A

Rebound insomnia when it is discontinued

Amnesia, confusion, delirium; esp in old pat

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15
Q

Triazolam - Interactions

A

Alcohol and other CNS depressants potentiate effects

Cimetidine, erythromycin, ketoconazole and oral contraceptives increase serum levels

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16
Q

Midazolam - Clinical use

A

Anesthetic for endoscopy, other diagnostic procedures or minor surgery.
Lethal injection

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17
Q

Midazolam - Adverse effects

A

Respiratory depression

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18
Q

Midazolam - Interactions

A

Alcohol and other CNS depressants potentiate effects

Ca channel blockers, erythromycin and ketoconazole increase serum levels

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19
Q

Which benzodiazepines are not metabolized?

A

Lorazepam
Oxazepam
Temazepam

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20
Q

Lorazepam - Clinical use

A

Anxiety

Control seizures

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21
Q

Lorazepam and Oxazepam - Interactions

A

Alcohol and other CNS depressants potentiate effects

Rifampin decreases serum levels

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22
Q

Oxazepam - Clinical use

A

Anxiety

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23
Q

Temazepam - Clinical use

A

Primarily Insomnia

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24
Q

Temazepam - Interactions

A

Alcohol and other CNS depressants potentiate effects

Cimetidine increases and rifampin decreases serum levels

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25
Q

Barbiturates

A

Amobarbital
Pentobarbital
Phenobarbital
Thiopental

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26
Q

Barbiturates - MoA

A

Bind to GABAa receptor at the alpha or beta subunit. Barbiturates increase the affinity of the receptor for GABA and the duration of the time the chloride channel remains open. Decrease activity of excitatory neurotransmitter (Ach, glutamate).
It also directly increase Cl influx in the absence of GABA –> no ceiling effect.

Barbiturates increase chloride conductance independent of the presence of GABA –> greater SNS depression and toxicity

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27
Q

Barbiturates - Clinical use

A

Insomnia
Seizure disorders
Induction of general anesthesia

28
Q

Barbiturates - Adverse effects

A

Higher dose; Respiratory depression, coma, death

CNS depression, drug dependence

29
Q

Barbiturates - Interactions

A

Induce CytP450: accelerate their own metabolism + other drugs metabolized by these enzymes.

Potentiated effects of other CNS depressants

Induce a-aminolevulinate synthase –> exacerbate porphyria

30
Q

Amobarbital and Pentobarbital - Clinical use

A

Insomnia

31
Q

Phenobarbital - Clinical use

A

Seizures disorders

Jaundice

32
Q

Thiopental - Clinical use

A

Induction to anesthesia

33
Q

Estazolam, Flurazepam and Triazolam - Clinical use

A

Insomnia

34
Q

Antihistamines

A

Diphenhydramine
Hydroxyzine
Doxepine

35
Q

Antihistamines - MoA

A

Cross blood-brain barrier and produce varying degrees of sedation.
Sedative action due to their ability to bind to H1 receptors and reduce ACh released by neurons in the reticular nuclei. Drug that block ACh release induce drowsiness and sleep via their effects on the cholinergic projections of the reticular nuclei.
In contrast: caffeine and methylxanthines can increase arousal by blocking presynaptic adenosine receptors –> increase cholinergic activity in the reticular nuclei.

36
Q

Antihistamines - Adverse effects

A

Anticholinergic effects: blurred vision, dry mouth, urinary retention, dizziness, drowsiness

Some tolerance can occur during the long-term use

37
Q

Antihistamines - Interactions

A

Alcohol, barbiturates, CNS depressants potentiate CNS effects

38
Q

Diphenhydramine and Doxepine - Clinical use

A

Insomina

39
Q

Hydroxyzine - Clinical use

A

Anxiety, sometimes used as a sedative before surgery

40
Q

Zolpidem, Zaleplon and Eszopiclone - MoA

A

Facilitate the activity of g-aminobutyric acid (GABA), GABAa receptor- Cl ion channels. They bind on the a subunit and increase the frequency which the channel open and cause hyperpolarization.

41
Q

Zolpidem, Zaleplon and Eszopiclone - Clinical use

A

Insomnia

Zaleplon: midsleep awakenings

42
Q

Zolpidem and Zaleplon - Adverse effects

A

Dizziness
Drowsiness
Headache

43
Q

Eszopiclone - Adverse effects

A

Drowsiness
Dizziness
Difficulty with coordination

44
Q

Zolpidem, Zaleplon and Eszopiclone - Interactions

A

Effects potentiated by alcohol and other CNS depressants

45
Q

Flumazenil - MoA

A

Competitive benzodiazepine receptor antagonist. Block effects of agonists such as diazepam, but also inverse agonists

46
Q

Flumazenil - Clinical use

A

Counteract the adverse effects of benzodiazepines, such as respiratory depression due to IV adm or in the case of accidental or intentional overdose.

47
Q

Flumazenil - Adverse effects

A 
Seizures
Arrhythmia
Blurred vision
Emotional lability
Dizziness
48
Q

Melatonin - MoA

A

Interacts with specific receptors in the CNS and elsewhere, and is believed to be the principal mediator of the biologic clock that determines circadian, seasonal and reproductive rhythms in animal species.
In humans: released before the onset of sleep and produces drowsiness

49
Q

Melatonin - Clinical use

A 
Jet-lag
Insomnia  in shift-change workers
Insomnia in elderly pt who do not secrete adequate melatonin.
Delayed sleep-phase syndrome
Non-24-hour sleep-wake disorder
50
Q

Melatonin - Adverse effects

A

If taken at bedtime for a few nights –> accelerate the resetting of the biologic clock

51
Q

Ramelteon - MoA

A

Act selectively at melatonin receptors

52
Q

Ramelteon - Clinical use

A

Sleep-onset insomnia

53
Q

Ramelteon - Interactions

A

Fluvoxamine (strong CYP1A2 inh): increase plasma conc.

54
Q

Tasimelteon - MoA

A

Melatonin agonist

55
Q

Tasimelteon - Clinical use

A

Insomnia: non-24 hour sleep-wake disorder

56
Q

Chloral Hydrate - MoA

A

Prodrug that is converted to its active metabolite, trichloroethanol.

57
Q

Chloral Hydrate - Clinical use

A

Preanesthetic sedation in pediatric patients

58
Q

Chloral Hydrate - Interactions

A

Effect are potentiated by alcohol

59
Q

Buspirone - MoA

A

Partial agonist at serotonin 5-HT1A receptors and activated feedback inhibition of serotonin release –> upregulation of postsynaptic serotonin receptors.

60
Q

Buspirone - Clinical use

A

Chronic anxiety

61
Q

Buspirone - Adverse effects

A

Headache
Dizziness
Nervousness

62
Q

Propranolol - MoA

A

b-adrenoceptor antagonists

63
Q

Propranolol - Clinical use

A

Prevent physiologic manifestations of stage fright or acute situational or performance anxiety –> prevent tachycardia and pther signs and symptoms of acute anxiety caused by symptomatic stimulation.

64
Q

Propranolol - Adverse effects

A 
Bradycardia
Bronchoconstriction
Depression
Fatigue
Hypersensitivity
Hypotension
Impaired glycogenolysis
Vivid dreams.
65
Q

Propranolol - Interactions

A

Cardiac depression increased by CCBs

Pharmacology (55 decks)

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