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Neuromusculoskeletal & Psychiatry I Exam #1 > Sedative and Hypnotic Drugs > Flashcards

Sedative and Hypnotic Drugs Flashcards

1
Q

Generally, which suffix correlates with Benzodiazepines?

What are 2 exceptions?

A

-pam/lam

Chlordiazepoxide
Chlorazepate

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2
Q

What is the Benzodiazepine antagonist?

A

Flumazenil

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3
Q

What is the suffix for Barbiturates?

A

-tal

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4
Q

Which Benzos are considered short, intermediate and long acting?

A

Short acting: Triazolam

Intermediate acting: Alprazolam

Long acting: Flurazepam

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5
Q

Which Barbiturates are considered ultra-short acting, short acting and long acting?

A

Ultra-short acting: Thiopental

Short acting: Secobarbital

Long acting: Phenobarbital

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6
Q

What is the progression of CNS effects of ingested drugs?

A

Sedation -> Hyponosis -> Anesthesia -> Coma

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7
Q

What is the MOA of Benzodiazepines?

What is there a risk of?

A

Binds to GABAA receptor and enhances GABA’s effects (shifts dose-response curve left).
-increase Cl- influx, hyperpolarization, and decreased number of APs.

Dependence and tolerance.

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8
Q

What are the advantages and disadvantages to treating anxiety with Benzodiazepines?

A

Advantages: high therapeutic index, antidote available if overdose, low risk of drug-drug interactions, minimal CVS effects.

Disadvantages: risk of dependence, CNS depression.

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9
Q

Under which circumstances are Benzodiazepines more likely to cause cumulative effects?

A

When taken as multiple doses, due to long half-life.

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10
Q

Which drug is bound to serum albumin (80%) most of the time in vitro?

A

Alprazolam

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11
Q

Which CYP metabolizes Alprazolam?

What is it used for?

A

CYP3A4

Management of anxiety disorder or short-term relief of anxiety symptoms. Can also be used for panic disorder, w/ or w/o agoraphobia.

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12
Q

In which patients is Alprazolam contraindicated? (3)

A

Paatients w/ a known sensitivity to the drug or other Benzos.

Patients with acute narrow angle glaucoma.

Ketoconozole and Itraconozole (because they impair oxidative metabolism by CYP3A).

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13
Q

Which warnings are associated with Alprazolam?

A

Dependence and withdrawal reactions, including seizures.

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14
Q

Which drug is given IM/IV for preoperative sedation/anxiolysis/amnesia?

What is the black box warning?

A

Midazolam

IV Midazolam has been associated w/ respiratory depression and arrest, especially used in non-critical care settings.

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15
Q

Diazepam’s effects are the result of facilitation of what?

What is the half-life and elimination process?

A

GABA (inhibitory NT)

Initial distribution phase is followed by prolonged terminal elimination phase (half-life up to 48 hrs.). The terminal elimination half-life of the active metabolite N-desmethyldiazepam can be up to 100 hrs.**

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16
Q

What happens to the half-life of Diazepam in patients with mild to moderate cirrhosis?

A

It increases, possibly from 2 to 5-fold.

17
Q

What are the indications for Diazepam?

A

Management of anxiety disorders or short-term relief of symptoms.

May improve symptoms in acute alcohol withdrawal.

18
Q

What are the contraindications of Diazepam?

A

Patients with a known hypersensitivity to the drug.

Pediatric patients < 6 mo.

Patients with myasthenia gravis, severe respiratory insufficiency, hepatic insufficiency and sleep apnea.

Patients with acute narrow-angle glaucoma.

19
Q

What is the warning associated with Diazepam?

A

NOT recommended in the treatment of psychotic patients.

20
Q

Indication for Oxazapam:

A

Treatment of anxiety, anxiety w/ depression and acute alcohol withdrawal.

21
Q

Indication for Triazolam:

What is the black box warning?

A

Short-term relief of insomnia (7-10 days).

BB warning: concomitant use in patients with opioids may cause severe sedation, respiratory depression, coma and death.

22
Q

Indications for Chlordiazepoxide (3)

What is the black box warning?

A

(1) Management of anxiety disorders or short-term relief of symptoms of anxiety, (2) acute alcohol withdrawal symptoms, and (3) pre-op apprehension and anxiety.

Concomitant use with opioids may cause severe sedation, respiratory depression, coma and death.

23
Q

Indications for Flurazepam:

What should be done if symptoms do not improve?

A

Used for the treatment of insomnia characterized by trouble falling asleep, frequent awakenings and early awakenings.

Failure of insomnia to remit after 7-10 days may indicate a primary pyschiatric medical illness that should be evaluated.

24
Q

What are the indications for Lorazepam? (2)

A

Treatment of epilepsy.

Used before surgery and medical procedures to relieve pre-op anxiety.

25
Q

What are the indications for Flumazenil? (2)

What is the black box warning?

A
  • Complete or partial reversal of sedative effects of Benzos in cases where general anesthesia has been induced/maintained w/ Benzos.
  • Management of Benzo overdose.

May cause seizures.

26
Q

How is Thiopental given?

What are the indications? (5)

A

Only IV.

Sole anesthetic for brief (< 15 min) procedures.
To supplement regional anesthesia.
To provide hypnosis during balanced anesthesia.
To control convulsive states.
In neurosurgical patients with elevated intracranial pressures.

27
Q

What are the adverse reactions of Thiopental?

A

Respiratory depression, myocardial depression, arrhythmias, prolonged somnolence, sneezing, coughing, etc.

28
Q

What are the indications for Secobarbital? (2)

What is the warning?

A

Hyponotic, for short-term insomnia, because it loses its effectiveness after 2 wks.
Preanesthetic.

If insomnia does not remit after 7-10 days of treatment may suggest a primary psychiatric disorder.

29
Q

What is the indication of Phenobarbital?

Who is it contraindicated in?

What is the warning?

It has been shown to…

A

Use as a sedative or hypnotic.

Patients with a barbiturate sensitivity and in patients with a history of porphyria.

If insomnia does not remit after 7-10 days of treatment may suggest a primary psychiatric disorder.

Induces liver microsomal enzymes, thus increasing metabolism of other meds.

30
Q

In general, what is the risk of giving Benzos for insomnia?

What is the benefit of using Zolpidem, Zaleplon and Eszopiclone?

A

May cause daytime sedation and patients may develop anterograde amnesia and tolerance.

They are highly effective, rapid onset and with minimal hangover effects.
Zolpidem is given for sustained sleep maintenance.
Eszopiclone has a longer half-life.

31
Q

What is the MOA of Ramelteon?

What is the indication?

A

Agonist at MT1 and MT2 melatonin receptors.

Treatment of insomnia characterized by difficulty with sleep onset.

32
Q

What is the MOA of newer sleep aids (Zolpidem, Zaleplon and Eszopiclone)?

What is a benefit of using them?

A

Binds to GABAA receptors w/ a1-subunit.
-increased Cl- influx, increased hyperpolarization, and decreased APs (CNS depression).

There are minimal depressive effects on organ systems.

33
Q

Buspirone is used for:

How long does it take to work?

What is the benefit of using it?

Metabolized by…

A

Treatment of generalized anxiety disorder.

May take more than a week.

Does not cause sedation, euphoria, hypnosis, etc.

CYP3A4

34
Q

What is the MOA for Zaleplon?

What is the indication?

What is the warning associated with it?

A

It is a non-benzo with a unique structure that interacts with GABA-BZ complex.

Short-term treatment for short-term treatment of insomnia.

If insomnia does not remit after 7-10 days of treatment may suggest a primary psychiatric disorder.

35
Q

What is the indication for Zolpidem?

Who is it contraindicated in?

What drugs may interact with it?

What are the warnings? (2)

A

Short-term treatment of insomnia characterized by trouble initiating sleep. It has been shown to decrease sleep latency for up to 35 days.

Patients with known hypersensitivity to zolpidem tartate or other active ingredients.

CNS depressants.

If insomnia does not remit after 7-10 days of treatment may suggest a primary psychiatric disorder.
Worsening depression or suicidal thinking may occur.

36
Q

What is the indication for Eszopiclone?

What is the warning?

What are the adverse reactions?

A

Treatment of insomnia and improve sleep maintenance.

It is a CNS depressant.

Unpleasant taste, HA, somnolence, respiratory infection, dizziness, dry mouth, etc.

37
Q

How does Meprobamate work?

What is the indication?

A

It slows brain activity to allow for relaxation.

Anxiety treatment or short-term relief of anxiety symptoms.

38
Q

What is the indication for chloral hydrate?

A

Short-term use as a sedative or sleep medicine.

May be used to treat alcohol withdrawal symptoms, or to treat withdrawal from other meds.

39
Q

Which drugs are strictly used for insomnia? (9)

A 
Triazolam
Flurazepam
Secobarbital
Phenobarbital
Zolpidem
Zaleplon
Eszopiclone
Ramelteon
Chloral hydrate

Neuromusculoskeletal & Psychiatry I Exam #1 (20 decks)

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