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Pharmacology > Anxiety, Sedatives, Insomnia, Hypnotic Agents > Flashcards

Anxiety, Sedatives, Insomnia, Hypnotic Agents Flashcards

1
Q

Diazepam resembles other general CNS depressant drugs in:
A.  Promoting psychological dependence
B.  Leading to development of seizures on sudden withdrawal after long-term treatment with large doses
C.  Demonstrating a pattern of cross-dependence to alcohol
D.  All of the above are correct
E.  Both A and C are correct

A

D.  All of the above are correct

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2
Q

Which of the following statements concerning benzodiazepines is CORRECT?
A.  Benzodiazepines directly open chloride channels
B.  Benzodiazepines show analgesic actions
C.  Clinical improvement of anxiety requires 2-4 weeks of treatment with benzodiazepines
D.  All benzodiazepines have some sedative effects
E.  Benzodiazepines, like other CNS depressants, readily produce general anesthesia

A

D.  All benzodiazepines have some sedative effects

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3
Q

BDZ ___ Cl- channel opening in ONLY the presence of GABA

BARBs __ channel opening the presence of BABA AND at higher doses open channel ___

A

ENHANCE

Prolong
directly

*membranes then hyperpolarizes–> decrease CNS neuronal excitability

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4
Q

Used in treatment of benzodiazepine overdose toxicity

A

Flumazenil - antagonist

*not effective for BARB or ethanol toxicity

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5
Q

Benzodiazepines and barbiturates share which of the following pharmacologic properties?
A.  Augment GABA action at the GABA receptor-chloride channel complex at low doses
B.  Ability to maintain surgical anesthesia (stage III) when administered intravenously
C.  Inhibition of GABA neurotransmission
D.  Efficacy in the treatment of seizure disorders
E.  High therapeutic index
F.   Agonist action at benzodiazepine receptors

A

A.  Augment GABA action at the GABA receptor-chloride channel complex at low doses
D.  Efficacy in the treatment of seizure disorders

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6
Q

Which of the following properties is shared by both inhalational general anesthetics and oral benzodiazepine anti-anxiety agents?
A.  Maintenance of Stage III surgical anesthesia
B.  Potentiation of GABA-A receptor activity
C.  Low margin of safety
D.  Relatively low potency
E.  Inhibition of excitatory synaptic transmission

A

B.  Potentiation of GABA-A receptor activity

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7
Q 
This drug used in the management of insomnia facilitates the inhibitory actions of GABA, but it lacks anticonvulsant or muscle-relaxing properties and has minimal effect on sleep architecture. Its actions are antagonized by flumazenil. 
A.  Busprione 
B.  Flurazepam 
C.  Eszopiclone 
D.  Ramelteon 
E.  Zolpidem 
F.   Triazolam
A

C.  Eszopiclone

E.  Zolpidem

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8
Q 
A 45-year-old man who has been injured in a car accident is brought into the ED. His BAC is 0.275%. Hospital records show a prior hospitalization for alcohol-related seizures. His wife confirms that he has been drinking heavily for 3 weeks. What treatment should be provided to the patient if he goes into withdrawal? 
A.  None 
B.  Lorazepam 
C.  Chlordiazepoxide 
D.  Pentobarbital 
E.  Phenytoin 
F.   Buspirone
A

B.  Lorazepam

C.  Chlordiazepoxide

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9
Q

Uses of Benzos at the receptor they work at

A
  1. Anxiolysis receptor: sedation a2-a5
  2. Aniconvulsants Effects receptors: a1
  3. Muscle relaxation: a2-a5
  4. Hypnosis: a1— at high enough doses
  5. Anesthesia adjuncts NOT capable of induction like BARBs
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10
Q

Adverse effects of benzos

A
  1. physiologic-psychologic dependence
  2. rebound insomnia
  3. impaired judgement
  4. risk of falls and ataxia in elderly
  5. excessive daytime drowsiness
  6. Anterograde amnesia - memory impairment (learn new)
  7. Resp. and CV depression
  8. DDI: additive to CNS depressants (alcohol, TCADS, Anti-Convuls, Anti-Hist, Anti-psychotics, opioids)

*more severe in benzos with short half lives

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11
Q

Rapid absorbing benzos

A
  1. diazepam
  2. alprazolam
  3. triazolam
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12
Q

A patient with liver dysfunction is scheduled for a surgical procedure. Lorazepam or oxazepam can be used for preanesthetic sedation in this patient without special concern regarding excessive CNS depression because these drugs are:
A.  Actively secreted in the renal proximal tubule
B.  Conjugated extrahepatically
C.  Eliminated via the lungs
D.  Reversible by administration of naloxone
E.  Selective anxiolytics like buspirone

A

B.  Conjugated extrahepatically

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13
Q 
The primary route of elimination for benzodiazepines is hepatic metabolism.  If metabolism is impaired due to liver disease or advancing age benzodiazepines may accumulate in plasma and
tissues and their potential for adverse reactions will increase.  Glucuronidation metabolic pathways are affected least by aging or liver disease, thus benzodiazepines eliminated entirely by this pathway are preferred in these patients.  Such benzodiazepines include: 
A.  Alprazolam (Xanax®) 
B.  Chlordiazepoxide (Librium®) 
C.  Diazepam (Valium®) 
D.  Flurazepam (Dalmane®) 
E.  Oxazepam (Serax ®) 
F.   Triazolam (Halcion®)
A

E.  Oxazepam (Serax ®)

*and Lorazepam!!

These have short half lives

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14
Q

Side effects associated with the use of benzodiazepines in treatment of anxiety disorders could include all of the following EXCEPT:
A.  Development of physical dependence
B.  Development of psychologic dependence
C.  Ataxia and risk of falls in the elderly
D.  Retrograde amnesia
E.  Excessive daytime drowsiness
F.   Impaired judgment

A

D.  Retrograde amnesia

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15
Q

Benzodiazepines and barbiturates share which of the following pharmacologic properties?
A.  Augment GABA action at the GABA receptor-chloride channel complex at low doses
B.  Ability to maintain surgical anesthesia (stage III) when administered intravenously
C.  Inhibition of GABA neurotransmission
D.  Efficacy in the treatment of seizure disorders
E.  High therapeutic index
F.   Agonist action at benzodiazepine receptors
G.  Addiction potential with prolonged use

A

A.  Augment GABA action at the GABA receptor-chloride channel complex at low doses
D.  Efficacy in the treatment of seizure disorders
G.  Addiction potential with prolonged use

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16
Q 
Administration of flumazenil (Romazicon ®) will reverse the toxicities associated with an overdose of: 
A.  Alcohol 
B.  Barbiturates 
C.  Benzodiazepines 
D.  Morphine
A

C.  Benzodiazepines

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17
Q

Administration of which of the following classes of psychoactive agents is most likely to produce memory disturbances such as anterograde amnesia?
A.  Benzodiazepines
B.  Serotonin selective reuptake inhibitors
C.  Tricyclic antidepressants
D.  CNS stimulants
E.  Monoamine oxidase inhibitors

A

A.  Benzodiazepines

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18
Q

Drug categories utilized in tx of anxiety

A
  1. Anti-depressants: SSRIs and SNRIs (NOT NDRIs)
  2. Benzos- declining use
  3. Buspirone
  4. BARBs– rarely!!
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19
Q 
A 40-year-old woman has sporadic attacks of intense anxiety with marked physical symptoms, including hyperventilation, tachycardia, and sweating. If she is diagnosed as suffering from a panic disorder, the most appropriate drug to use is: 
A.  Alprazolam 
B.  Paroxetine 
C.  Clonazepam 
D.  Propranolol 
E.  Diazepam
A

A.  Alprazolam

C.  Clonazepam

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20
Q

Drug categories used for GAD

A
  1. SSRIs
  2. SNRIs
  3. Benzos**
  4. Wellbutrin
  5. TCADs
21
Q

Drug categories used for panic disorder

A
  1. High potency BDZ (alprazolam-clonazepam)**
  2. SSRIs
  3. TCADs
  4. MAOIs
22
Q

Drug categories used for social anxiety disorder

A 
Generalized
1. SSRIs
2. SNRIs
3. MAOIs
Performance:
4. BB (propranolol)
5. high potency BDZs
23
Q 
Which of the following agents has a rapid onset of action and would be best for acute management of anxiety? 
A.  Buspirone
B.  Venlafaxine 
C.  Lorazepam 
D.  Escitalopram 
E.  Duloxetine
F.   Alprazolam
A

C.  Lorazepam

F.   Alprazolam

24
Q

Benzos that are:

  • High potency:
  • IM absorption:
  • Most rapid oral onset:
  • Short half-lives
  • Intermediate half-lives:
A
  • High potency: alprazolam, clonazepam
  • IM absorption: Lorazepam
  • Most rapid oral onset: Diazepam
  • Short half-lives: oxazepam, alprazolam, lorazepam
  • Intermediate half-lives: diazepma, chloridizaepoxide
25
Q

Benzodiazepines are preferred over barbiturates when use of a sedative-hypnotic agent is needed in sedation procedures. Reasons for this preference include
A.  Barbiturates have a much lower therapeutic index than
benzodiazepines.
B.  Barbiturates (Schedule II) have a higher abuse potential than benzodiazepines (Schedule IV).
C.  Barbiturates are classic inducers of cytochrome P450 enzymes with a greater potential for drug-drug interactions.
D.  Barbiturate overdose is more likely to result in death by respiratory depression than is benzodiazepine overdose.
E.  All of the above

A

E.  All of the above

26
Q

Which statement concerning barbiturates is accurate?
A.  Abstinence syndromes are less severe during withdrawal from phenobarbital than from pentobarbital
B.  Acidification of the urine accelerates the elimination of phenobarbital
C.  Barbiturates may decrease the half-lives of drugs metabolized by CYP450
D.  Compared with barbiturates, benzodiazepines exhibit a more shallow dose-response relationship
E.  Respiratory depression caused by barbiturate overdose can be reversed by flumazenil

A

A.  Abstinence syndromes are less severe during withdrawal from phenobarbital than from pentobarbital
C.  Barbiturates may decrease the half-lives of drugs metabolized by CYP450

27
Q

A 24-year-old stockbroker has developed a “nervous disposition”. He is easily startled, worried about inconsequential matters, and sometimes complains of stomach cramps. At night he grinds his teeth in his sleep. There is no history of drug abuse. Diagnosed as suffering from generalized anxiety disorder, he is prescribed buspirone. The patient should be informed to anticipate:
A.  A need to continually increase drug dosage because of tolerance
B.  A significant effect of the drug on memory
C.  Additive CNS depression with alcoholic beverages
D.  That the drug is likely to take a week or longer to begin working
E.  That if stops taking the drug abruptly, he will experience withdrawal signs

A

D.  That the drug is likely to take a week or longer to begin working

  • *No sedation, additive CNS depression, anti-convulsants or myorelaxant action
  • Not PRN
28
Q

What type of med is Buspirone

A

5HT partial agonist–> moderate D2 receptor block

*monitor for EPS SE

29
Q

Where do the Z drugs work

A

A1 (Cortex)

anticonvulsants

30
Q

Both benzodiazepines (e.g., temazepam [Restoril®]) and non-benzodiazepines (e.g., zolpidem [Ambien®]) are used in the treatment of insomnia. All of the pharmacologic properties listed below are shared by both classes of drugs, except that only zolpidem:
A.  Produces additive CNS depression if taken with ethanol
B.  Can produce tolerance and dependence (controlled substance)
C.  Has a high therapeutic index relative to barbiturates
D.  Can cause anterograde amnesia
E.  Binds selectively to GABA receptors containing the α1 subunit

A

E.  Binds selectively to GABA receptors containing the α1 subunit

31
Q

Drug tx for insomina

A
  1. Nonbenzos (Z-drugs, ramelteon)

2. shorter acting BDZ (temazepam)

32
Q

Properties of ideal hypnotic agents

A
  1. Rapidly induce sleep
  2. sufficient duration to maintain sleep (t1/2)
  3. No tolerance
  4. No rebound insomnia w/ d/c
  5. high therapeutic index
  6. normalize disturbed sleep w/o distrubing normal sleep

***Z-drugs (zolpidem) closest to ideal

33
Q

Z drug used for insomnia

A
  1. Zolpidem (Ambien)
  2. Eszopiclone (Lunesta)
  3. Zaleplon (Sonata)
34
Q

Effective for:

  • Decreasing time to sleep onset – rapid oral onset
  • NOT for reducing nocturnal awakenings - short t
  • BUT suitable to aid sleep onset for middle-of-the-night awakenings with elimination by morning
A

Zaleplon (Sonata)

35
Q

Effective for:

  • Sleep maintenance – longest half-life of “Z”-drugs
  • Safe for long-term use (6 months) – little evidence for tolerance-dependence-abuse – BUT Schedule IV
A

Eszopiclone (Lunesta)

36
Q

Effective for:

  • Reducing sleep latency (immediate release formulation®)
  •   Reduce nocturnal awakenings (sustained release formulation - CR®)
  •  Insomnia associated w/ middle-of-the-night awakening (low dose sublingual formulation - Intermezzo®)
A

Zolpidem – most widely prescribed agent for insomnia

37
Q

Adverse drug reactions of Z drugs

A
  • safety similar to benzos
    1. drowsy
    2. amnesia
    3. GI compaints
    4. HA
    5. rarely bizarre behavioral disturbance*
    6. POSSIBLE tolerance-dependence WD (schedule IV)
38
Q

__ benzo has a short half-life so has less daytime sedation but more rebound insomnia

A

Triazolam

39
Q

A patient in a rehabilitation facility was having difficulty sleeping and was prescribed the benzodiazepine flurazepam to be given each night. One week later the physical therapist noted the patient’s performance and level of attentiveness were particularly poor during the morning sessions. It appeared that the drug was causing a “hangover effect” in the morning, interfering with the patient’s cognitive skills. Which of the following insomnia drugs would be LEAST likely to have this “hangover effect”?
A.  Alprazolam (Xanax®); t1/2= 6hrs
B.  Eszoplicone (Lunesta®); t/2=6 hrs
C.  Temazepam (Restoril®); t1/2= 12 hrs
D.  Triazolam (Halcion®); t1/2= 2.5hrs
E.  The hangover effect is equal for all agents

A

D.  Triazolam (Halcion®); t1/2= 2.5hrs

40
Q

An 82-year-old woman, otherwise healthy for her age, has difficulty sleeping. Triazolam is prescribed for her at one-half of the usual adult dose. Which statement about the use of triazolam is this elderly patient is accurate?
A.  Ambulatory dysfunction is unlikely to occur in elderly patients taking half of the usual dose
B.  Hypertension is a common adverse effect of benzodiazepines in elderly patients
C.  Over-the counter cold meds may antagonize the hypnotic effects of the drug
D.  The patient may experience amnesia, especially if she also consumes alcoholic beverages
E.  Triazolam can cause rebound insomnia if abruptly discontinued

A

C.  Over-the counter cold meds may antagonize the hypnotic effects of the drug–> pseudoephedrine
D.  The patient may experience amnesia, especially if she also consumes alcoholic beverages
E.  Triazolam can cause rebound insomnia if abruptly discontinued

41
Q

The most likely explanation for the increased sensitivity of elderly patients after a single dose of benzodiazepine is:
A.  Decreases in plasma protein binding
B.  Decreased metabolism of lipid-soluble drugs
C.  Decreases in renal function
D.  Age-dependent changes in brain function
E.  Increased cerebral blood flow

A

D.  Age-dependent changes in brain function

42
Q 
Use of which of the following agents is NOT associated with cognitive impairment, including memory disturbances, when used at recommended doses? 
A.  Diphenhydramine 
B.  Zolpidem 
C.  Triazolam 
D.  Alprazolam 
E.  Ramelteon
A

E.  Ramelteon

43
Q

SE of Trazodone

A
  1. Oversedation
  2. Orthostasis (A1 block)
  3. Priapism
44
Q

SE of Diphenhydramine-Doxyllamine

A

generally minimal but anti-muscarinic actions (no see no pee…)

45
Q 
All of the following agents for the management of insomnia are controlled substances EXCEPT: 
A.  Zaleplon 
B.  Eszopiclone 
C.  Temazepam
D.  Zolpidem 
E.  Triazolam 
F.   Diphenhydramine
A

F.   Diphenhydramine

46
Q 
Which of the following agents utilized in the treatment of insomnia are most likely to cause anticholinergic side effects? 
A.  Diphenhydramine 
B.  Trazodone 
C.  Triazolam 
D.  Zolpidem 
E.  Ramelteon 
F.   Doxylamine
A

A.  Diphenhydramine

F.   Doxylamine

47
Q

Which of the following statements regarding anxiolytic and hypnotic agents is CORRECT?
A.  Phenobarbital shows analgesic properties
B.  Diazepam and phenobarbital induce CYP450
C.  Phenobarbital is useful in the treatment of acute intermittent porphyria
D.  Phenobarbital induces respiratory depression, which is enhanced by the consumption of ethanol
E.  Buspirone has actions similar to those of benzodiazepines

A

D.  Phenobarbital induces respiratory depression, which is enhanced by the consumption of ethanol

48
Q 
Which of the following anxiolytic agents is least sedating, will NOT potentiate the effects of ethanol, and has no appreciable dependence liability? 
A.  Chlordiazepoxide 
B.  Midazolam 
C.  Alprazolam 
D.  Buspirone 
E.  Pentobarbital
A

D.  Buspirone

49
Q

BARB SE

A
  1. Rapid development of tolerance
  2. High abuse potential (Schedule II) – benzos are Schedule IV
  3. Lethality in overdose - low therapeutic index (respiratory depression → coma → death)
  4. Excessive sedation
  5. Drug-drug interactions - via CYP450 induction (classic inducers)
  6. Withdrawal Syndrome: Abstinence syndromes are less severe during withdrawal from phenobarbital than pentobarbital

Pharmacology (31 decks)

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