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Flashcards in Sedative-Hypnotic Drugs Deck (53):
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Benzodiazepines

Alprazolam
Chlordiazepoxide
Clonazepam
Diazepam
Lorazepam
Triazolam

1

Alprazolam

Benzodiazepine

2

Chlordiazepoxide

Benzodiazepine

3

Clonazepam

Benzodiazepine

4

Diazepam

Benzodiazepine

5

Lorazepam

Benzodiazepine

6

Lorazepam

Benzodiazepine

7

Diazepam
Lorazepam

Mechanism of action

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

8

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

Diazepam
Lorazepam

Mechanism of action

9

Diazepam
Lorazepam

Effects

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

10

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

Diazepam
Lorazepam

Effects

11

Diazepam
Lorazepam

Clinical applications

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

12

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

Diazepam
Lorazepam

Clinical applications

13

Diazepam
Lorazepam
(Benzodiazepines in general)

Pharmacokinetics, Toxicities, Interactions

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

14

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

Diazepam
Lorazepam
(Benzodiazepines in general)

Pharmacokinetics, Toxicities, Interactions

15

Benzodiazepine antagonist

Flumazenil

16

Flumazenil

Benzodiazepine antagonist

17

Flumazenil

Mechanism of action

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

18

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

Flumazenil

Mechanism of action

19

Flumazenil

Effects

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

20

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

Flumazenil

Effects

21

Flumazenil

Clinical applications

Management of benzodiazepine overdose

22

Management of benzodiazepine overdose

Flumazenil

Clinical applications

23

Flumazenil

Pharmacokinetics, Toxicities, Interactions

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