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pharm III exam 1 > Sedative > Flashcards

Sedative Flashcards

1
Q

Which anxiety disorders are treated with benzodiazepines

A
  • acute anxiety
  • generalized anxiety disorder
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2
Q

what class of medications are used to treat generalized anxiety disorder

A
  • benzodiazepines
  • buspirone
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3
Q

DOC for tx of enuresis (bed wetting)

A

tricyclic antidepressants

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4
Q

What type of medications are most useful for short term insomnia, which occurs with situational stress

A
  • sedative-hypnotics
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5
Q

MOA of GABA

A
  • CNS depressant
  • major inhibitory neurotransmitter
  • relieves anxiety and promotes sedation
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6
Q

describe GABA receptors

A
  • Cl- channels
    • ​activation allows Cl- to enter cell hyperpolarizing membrane
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7
Q

The majority of sedative-hypnotics and anxiolytics (barbiturates, benzodiazepines, and the “z-drugs”) act by binding to a modulatory site on

A

GABAA receptor complex, to either intensify or prolong the actions of GABA.

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8
Q

MOA of Barbiturates

A
  • Bind to GABAA receptor, and increase the duration of GABA action.
  • At high concentrations, they may increase Cl- influx and produce inhibition independent of GABA.
  • Marked CNS depressant effect -> produce hypnosis
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9
Q

why are Barbiturates a drug of abuse

A

they cause euphoria

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10
Q

What drug class is Thiopental in? Use?

A
  • short acting Barbiturate
  • induction of anesthesia
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11
Q

What drug class is Phenobarbital in? Use?

A
  • Long acting Barbiturates
  • anticonvulsant
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12
Q

List the barbituates

A
  • Pentobarbital
  • Phenobarbital
  • Secobarbital
  • Thiopental
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13
Q

Barbituates are metabolized in what organ

A

liver

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14
Q

with chronic use, Barbituates induce what liver enzymes

A
  • CYP450s
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15
Q

Side effects of Barbituates

A
  • CNS depression
  • paradoxical excitement
  • severe physiological and psychological dependence
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16
Q

contraindications to use Barbituates

A
  • Porphyria: enhance porphyrin synthesis
  • Pulmonary insufficiency: may cause respiratory depression
  • Supra-additive effects when combined with alcohol
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17
Q

Why do barbituates have No ceiling effect

A
  • because the action of barbiturates is not dependent on GABA, as the dose increases, the effect continues to increase; it does not plateau
    • Especially dangerous when combined with alcohol.
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18
Q

Do the elderly metabolize benzodiazepines more slowly or more quickly

A

more slowly

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19
Q

Duration of action of benzodiazepines is very clinically relevant. BZs that are converted to active metabolites have what duration of action

A

longer duration of action

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20
Q

List the benzodiazepines with long duration of action

A
  • Diazepam : 75 hrs
  • Chlordiazepoxide
  • Flurazepam
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21
Q

List the benzodiazepines with intermediate duration of action

A
  • Alprazolam (6 hr)
  • Oxazepam
  • Lorazepam
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22
Q

List the benzodiazepines with short duration of action

A
  • Midazolam
23
Q

List the Benzodiazepines

A
  • Diazepam
  • Chlordiazepoxide
  • Flurazepam
  • Midazolam
  • Temazepam
  • Alprazolam
  • Lorazepam
  • Oxazepam
24
Q

MOA of benzodiazepines

A
  • bind to specific BZ receptor on the GABAA receptor complex.
    • Intensify the actions of GABA by enhancing its binding to the GABAA receptor.
    • effect is dependent on GABA
25
Q

explain why benzodiazepines have a ceiling effect

A
  • Act only when GABA is present.
    • As the concentration increases, GABA release is inhibited. This produces a ceiling to the effect, and respiratory depression is far less likely than with barbiturates. This is why benzodiazepines are relatively safe drugs.
26
Q

List the anxiety disorders for which benzodiazepines are not used

A
  • obsessive compulsive disorder
  • Agoraphobia and panic disorders
  • Post traumatic stress
  • anxiety in children and adolescents
27
Q

DOC anxiety

A

benzodiazepines

28
Q

Which benzodiazepines are commonly used as hypnotics.

A
  • Flurazepam (Dalmane®)
    • may cause a drug “hangover” effect
  • Temazepam (Restoril®)
29
Q

Which benzodiazepines are commonly used for status epilepticus

A
  • Diazepam
  • Lorazepam
30
Q

which benzodiazepine is frequently used in preparation for anesthesia and for short surgical procedures

A
  • Midazolam
31
Q

route of administration of Midazolam

A

IV

32
Q

In addition to sedation and a calming effect, midazolam causes

A
  • anterograde amnesia
    • the patient will be unable to recall events that occurred after the drug was administered.
33
Q

Which benzodiazepine can be used for acute muscle spasm and pain as a result of injury

A

Diazepam

34
Q

Long-term use of alcohol or barbiturates can produce physical dependence and result in

A
  • withdrawal that is very severe and can be life threatening
    • Abrupt discontinuation of BZs can cause rebound increases in insomnia and anxiety
    • BZ shoulde be tapered very slowly following chronic use
35
Q

which benzodiazepines are used to provide a more tapered withdrawal?

A
  • Long acting benzodiazepines
    • Chlordiazepoxide
    • Diazepam
    • Lorazepam
36
Q

side effects of benzodiazepines

A
  • CNS depression
  • paradoxical excitement: dis-inhibition of suppressed behavior
  • supra-additive: CNS depression more profound when BZs are combined with alcohol
  • sleep-related behaviors: sleep driving, eating, walking
37
Q

contraindications to benzodiazepines

A
  • pregnancy: category D
  • sleep apnea: may decrease tone of upper airway
  • elderly
38
Q

overdose of benzodiazepines causes

A
  • BZs are relatively safe
  • overdose results in long deep sleep (24-48 hrs)
  • fatalities occur in people with respiratory difficulties, children, and when combined with alcohol
39
Q

MOA of Flumazenil

A
  • Benzodiazepine antagonist
    • competes with BZs for GABA receptor
    • reverses the effects of BZs
      • ex: reverses effect of Midazolam (versed)
40
Q

adverse effect and CI of Flumazenil

A
  • triggers withdrawal and seizures in patients who are physically dependent upon BZ
  • do not used in patients with h.o. seizures
41
Q

List the “Z” drugs used for insomnia

A
  • Zolpidem (Ambien®)
  • Zaleplon (Sonata®)
  • Eszopiclone (Lunesta®
42
Q

MOA of Zolpidem (Ambien®) Zaleplon (Sonata®) Eszopiclone (Lunesta®

A
  • bind to the BZ1 subtype of the GABA receptor to increase GABA-mediated inhibition
  • very strong and rapid sedative effects
  • no anxiolytic, anticonvulsant or muscle relaxant properties
43
Q

route of administration and duration of action of Zolpidem (Ambien®) Zaleplon (Sonata®)

A
  • oral
  • short duration of action
    • morning drowsiness is unlikely
44
Q

route of administration and duration of action of Eszopiclone

A
  • oral
  • long half life
  • used in long term treatment
45
Q

side effects of Zolpidem (Ambien®) Zaleplon (Sonata®) Eszopiclone (Lunesta®

A
  • GI: diarrhea and nausea
  • CNS: drowsiness and dizziness
  • sleep related behaviors
  • confusion and memory loss in elderly
  • rebound insomnia after rapid discontinuation
46
Q

abrupt cessation after long term use of Eszopiclone (Lunesta®) can cause

A
  • withdrawal
    • CNS sitmulation
    • anxiety
    • seizures
47
Q

MOA of Ramelteon

A
  • melatonin analogue
  • resets sleep-wake cycle
  • promotes sleepiness with out GABA effect
48
Q

what happens when Ramelteon is taken with alcohol or other sedative hypnotics

A

additive sedation

49
Q

side effects of Ramelteon

A
  • drowsiness
  • dizziness
  • nausea
50
Q

MOA of Chloral Hydrate

A
  • converted to tricholorethanol which causes sedation
    • acts similarly to barbiturates on GABAA receptor
51
Q

adverse effects of Chloral Hydrate

A
  • low margin of safety
    • high doses induce respiratory and vasomotor depression
  • long term use -> liver damage and fatal intoxication
52
Q

use of Chloral Hydrate

A
  • cheap
  • in children for sedation during dental procedures
  • use as a sedative-hypnotic not recommended
53
Q

MOA of Buspirone

A
  • partial agonist at the postsynaptic 5-HT1A (serotonin) receptor -> inhibition of cell signaling
  • full agonist at the presynaptic 5-HT1A (serotonin) receptor -> decreased release of 5-HT
54
Q

Use of Buspirone

A
  • relieves anxiety without producing sedation
    • no muscle relaxant or anticonvulsant properties
    • does not potentiate CNS depression with alcohol or BZs
      • very low addiction potential: excellent choice for anxiety in recovering alcoholics/addicts

pharm III exam 1 (11 decks)

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