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Sedative-Hypnotic Drugs Flashcards

0
Q

Alprazolam

A

Benzodiazepine

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1
Q

Benzodiazepines

A 
Alprazolam
Chlordiazepoxide
Clonazepam
Diazepam
Lorazepam
Triazolam
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2
Q

Chlordiazepoxide

A

Benzodiazepine

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3
Q

Clonazepam

A

Benzodiazepine

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4
Q

Diazepam

A

Benzodiazepine

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5
Q

Lorazepam

A

Benzodiazepine

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6
Q

Lorazepam

A

Benzodiazepine

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7
Q

Diazepam
Lorazepam

Mechanism of action

A

Bind to specific GABA(A) receptor subunits at central nervous system (CNS) neuronal synapses facilitating frequency of GABA-mediated chloride ion channel opening- enhance membrane hyperpolarization

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8
Q

Bind to specific GABA(A) receptor subunits at central nervous system (CNS) neuronal synapses facilitating frequency of GABA-mediated chloride ion channel opening- enhance membrane hyperpolarization

A

Diazepam
Lorazepam

Mechanism of action

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9
Q

Diazepam
Lorazepam

Effects

A

Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression

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10
Q

Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression

A

Diazepam
Lorazepam

Effects

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11
Q

Diazepam
Lorazepam

Clinical applications

A

Acute anxiety states, Panic attacks, Generalized anxiety disorder, Insomnia and other sleep disorders, Relaxation of skeletal muscle, Anesthesia (adjunctive) Seizure disorders

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12
Q

Acute anxiety states, Panic attacks, Generalized anxiety disorder, Insomnia and other sleep disorders, Relaxation of skeletal muscle, Anesthesia (adjunctive) Seizure disorders

A

Diazepam
Lorazepam

Clinical applications

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13
Q

Diazepam
Lorazepam
(Benzodiazepines in general)

Pharmacokinetics, Toxicities, Interactions

A

Half-lives from 2-40 h, Oral activity, Hepatic metabolism-some active metabolites, TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs

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14
Q

Half-lives from 2-40 h, Oral activity, Hepatic metabolism-some active metabolites, TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs

A

Diazepam
Lorazepam
(Benzodiazepines in general)

Pharmacokinetics, Toxicities, Interactions

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15
Q

Benzodiazepine antagonist

A

Flumazenil

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16
Q

Flumazenil

A

Benzodiazepine antagonist

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17
Q

Flumazenil

Mechanism of action

A

Antagonist at benzodiazepine binding sites on the GABA(A) receptor

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18
Q

Antagonist at benzodiazepine binding sites on the GABA(A) receptor

A

Flumazenil

Mechanism of action

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19
Q

Flumazenil

Effects

A

Blocks actions of benzodiazepines and zolpidem but not other sedative-hypnotic drugs

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20
Q

Blocks actions of benzodiazepines and zolpidem but not other sedative-hypnotic drugs

A

Flumazenil

Effects

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21
Q

Flumazenil

Clinical applications

A

Management of benzodiazepine overdose

22
Q

Management of benzodiazepine overdose

A

Flumazenil

Clinical applications

23
Q

Flumazenil

Pharmacokinetics, Toxicities, Interactions

A

IV, short half-life, TOXICITY: Agitation, Confusion, Possible withdrawal symptoms in benzodiazepine dependence

24
IV, short half-life, TOXICITY: Agitation, Confusion, Possible withdrawal symptoms in benzodiazepine dependence
Flumazenil Pharmacokinetics, Toxicities, Interactions
25
Barbiturates
``` Amobarbital Butabarbital Mephobarbital Pentobarbital Phenobarbital Secobarbital ```
26
Amobarbital
Barbiturate
27
Butabarbital
Barbiturate
28
Barbiturate
Barbiturate
29
Mephobarbital
Barbiturate
30
Pentobarbital
Barbiturate
31
Phenobarbital
Barbiturate
32
Secobarbital
Barbiturate
33
Secobarbital Pentobarbital Phenobarbital Mechanism of action
Bind to specific GABA(A) receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening, enhance membrane hyperpolarization
34
Bind to specific GABA(A) receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening, enhance membrane hyperpolarization
Secobarbital Pentobarbital Phenobarbital Mechanism of action
35
Secobarbital Pentobarbital Phenobarbital Effects
Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression. Steeper dose-response relationship then Benzodiazepines
36
Dose-dependent depressant effect on the CNS including sedation and relief of anxiety, Amnesia, Hypnosis, Anesthesia, Coma and Respiratory depression. Steeper dose-response relationship then Benzodiazepines
Secobarbital Pentobarbital Phenobarbital Effects
37
Barbiturates Clinical applications
Anesthesia (thiopental) Insomnia (secobarbital) Seizure disorders (phenobarbital)
38
Anesthesia (thiopental) Insomnia (secobarbital) Seizure disorders (phenobarbital)
Barbiturates Clinical applications
39
Secobarbital Pentobarbital Phenobarbital (Barbiturates in general) Pharmacokinetics, Toxicities, Interactions
Half-lives from 4-60 h, Oral activity, Hepatic metabolism-phenobarbital 20% renal elimination. TOXICITY: extensions of CNS depressant effects, dependence liability > benzodiazepines. INTERACTIONS: Additive CNS depression with ethanol and many other drugs, induction of hepatic drug-metabolizing enzymes
40
Half-lives from 4-60 h, Oral activity, Hepatic metabolism-phenobarbital 20% renal elimination. TOXICITY: extensions of CNS depressant effects, dependence liability > benzodiazepines. INTERACTIONS: Additive CNS depression with ethanol and many other drugs, induction of hepatic drug-metabolizing enzymes
Secobarbital Pentobarbital Phenobarbital (Barbiturates in general) Pharmacokinetics, Toxicities, Interactions
41
Newer hypnotics
Eszopiclone Zaleplon Zolpidem
42
Eszopiclone
Newer hypnotic
43
Zaleplon
Newer hypnotic
44
Zolpidem
Newer hypnotic
45
Eszopiclone Zaleplon Zolpidem Mechanism of action
Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization
46
Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization
Eszopiclone Zaleplon Zolpidem Mechanism of action
47
Eszopiclone Zaleplon Zolpidem Effects
Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence
48
Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence
Eszopiclone Zaleplon Zolpidem Effects
49
Eszopiclone Zaleplon Zolpidem Clinical applications
Sleep disorders, especially those categorized by difficulty in falling asleep
50
Sleep disorders, especially those categorized by difficulty in falling asleep
Eszopiclone Zaleplon Zolpidem Clinical applications
51
Eszopiclone Zaleplon Zolpidem Pharmacokinetics, Toxicities, Interactions
Oral activity, short half-lives, CYP substrates. TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs
52
Oral activity, short half-lives, CYP substrates. TOXICITY: extensions of CNS depressant effects, dependence liability, INTERACTIONS: Additive CNS depression with ethanol and many other drugs
Eszopiclone Zaleplon Zolpidem Pharmacokinetics, Toxicities, Interactions

Pharma (29 decks)

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