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
Q

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

A

Flumazenil

Pharmacokinetics, Toxicities, Interactions

25
Q

Barbiturates

A
Amobarbital
Butabarbital
Mephobarbital
Pentobarbital
Phenobarbital
Secobarbital
26
Q

Amobarbital

A

Barbiturate

27
Q

Butabarbital

A

Barbiturate

28
Q

Barbiturate

A

Barbiturate

29
Q

Mephobarbital

A

Barbiturate

30
Q

Pentobarbital

A

Barbiturate

31
Q

Phenobarbital

A

Barbiturate

32
Q

Secobarbital

A

Barbiturate

33
Q

Secobarbital
Pentobarbital
Phenobarbital

Mechanism of action

A

Bind to specific GABA(A) receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening, enhance membrane hyperpolarization

34
Q

Bind to specific GABA(A) receptor subunits at CNS neuronal synapses increasing duration of GABA-mediated chloride ion channel opening, enhance membrane hyperpolarization

A

Secobarbital
Pentobarbital
Phenobarbital

Mechanism of action

35
Q

Secobarbital
Pentobarbital
Phenobarbital

Effects

A

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
Q

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

A

Secobarbital
Pentobarbital
Phenobarbital

Effects

37
Q

Barbiturates

Clinical applications

A

Anesthesia (thiopental)
Insomnia (secobarbital)
Seizure disorders (phenobarbital)

38
Q

Anesthesia (thiopental)
Insomnia (secobarbital)
Seizure disorders (phenobarbital)

A

Barbiturates

Clinical applications

39
Q

Secobarbital
Pentobarbital
Phenobarbital
(Barbiturates in general)

Pharmacokinetics, Toxicities, Interactions

A

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
Q

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

A

Secobarbital
Pentobarbital
Phenobarbital
(Barbiturates in general)

Pharmacokinetics, Toxicities, Interactions

41
Q

Newer hypnotics

A

Eszopiclone
Zaleplon
Zolpidem

42
Q

Eszopiclone

A

Newer hypnotic

43
Q

Zaleplon

A

Newer hypnotic

44
Q

Zolpidem

A

Newer hypnotic

45
Q

Eszopiclone
Zaleplon
Zolpidem

Mechanism of action

A

Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization

46
Q

Bind selectively to a subgroup of GABA(A) receptors, acting like benzodiazepines to enhance membrane hyperpolarization

A

Eszopiclone
Zaleplon
Zolpidem

Mechanism of action

47
Q

Eszopiclone
Zaleplon
Zolpidem

Effects

A

Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence

48
Q

Rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence

A

Eszopiclone
Zaleplon
Zolpidem

Effects

49
Q

Eszopiclone
Zaleplon
Zolpidem

Clinical applications

A

Sleep disorders, especially those categorized by difficulty in falling asleep

50
Q

Sleep disorders, especially those categorized by difficulty in falling asleep

A

Eszopiclone
Zaleplon
Zolpidem

Clinical applications

51
Q

Eszopiclone
Zaleplon
Zolpidem

Pharmacokinetics, Toxicities, Interactions

A

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
Q

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

A

Eszopiclone
Zaleplon
Zolpidem

Pharmacokinetics, Toxicities, Interactions