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NMSP Exam 1 > [PHARM] Sedative-Hypnotic drugs [Izard] > Flashcards

[PHARM] Sedative-Hypnotic drugs [Izard] Flashcards

1
Q

What are the 4 classes of Sedative/Hypnotic Drugs?

A

Benzodiazepines

Benzodiazepine Antagonists

Barbiturates

Misc/Newer Drugs

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2
Q

Give examples of each of the following:

Benzodiazepine

Short Acting –>

Intermediate Acting –>

Long Acting –>

A

Short Acting –> Triazolam

Intermediate Acting –> Alprazolam

Long Acting –> Flurazepam

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3
Q

Give examples of each of the following:

Barbiutrates

Ultra Short Acting –>

Short Acting –>

Long Acting –>

A

Ultra Short Acting –> Thiopental

Short Acting –> Secobarbital

Long Acting –> Phenobarbital

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4
Q

What is the difference between a Sedative and a Hypnotic?

A

A Sedative is a drug that DECREASES CNS ACTIVITY (Calms reciepient)

–(Usually an adverse effect of many other drugs, but these are faster acting)

A Hypnotic is a drug that PRODUCES DROWSINESS and facilitates onset of sleep

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5
Q

With increased continued doses of Benzodiazepines vs Barbiturates what are the effects of each on the CNS?

A

Benzodiazepines –> LEVEL OFF

Barbiturates –> CONTINUE LINEARLY affecting CNS.

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6
Q

List the receptors that each work on:

Benzodiazepines

Barbiturates

Misc (Newer)

A

Benzos –> GABA (A) Receptors

Barbiturates –> GABA (A) Receptors

Misc –> GABA (A) and Melatonin Receptors

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7
Q

How are Benzos metabolized and excreted?

A

CYP3A4 (phase 1) and then Glucoronidation (phase II)

Excreted via Kidneys (Elimination Half life [2-100 hours])

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8
Q

What is the MOA of Benzos?

A

Binds to GABA (A) Receptor, and enhances GABA’s effects (Shifts dose response curve to the left)

Increases Cl influx

Increases Hyperpolarization

Decreases AP

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9
Q

What are the 10 Benzodiazepines?

A

Alprazolam

Chlordiazepoxide

Clonazepam

Clorazepate

Diazepam

Flurazepam

Lorazepam

Midazolam

Oxazepam

Triazolam

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10
Q

Which Benzos are used to treat Anxiety?

Which drugs are NOW better used to treat anxiety?

A

Alprazolam

Diazepam

Clonazepam

Lorazepam

(etc)

SSRI’s

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11
Q

Which of the following would be more likely to cause cumulative effects (drowsiness) with multiple doses, and why?

Diazepam or Alprazolam?

A

Diazepam, because its half life is >100 hours, and with longer half lives you are more likely to have an increase in the active metabolite in the system, and this will cause cumulative effects.

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12
Q

Alprazolam is metabolised by what enzyme?

it is indicated for what uses?

What specific cases can it be used and not used in?

What are some general warnings?

A

CYP3A4

Anxiety, Panic Disorder (w or w/o Agoraphobia)

Okay for use in –> Open Angle Glaucoma

NO for use in –> Acute Narrow Angle Glaucoma

Dependence and Withdrawl reactions, and Seizures

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13
Q

How is the drug Midazolam given?

What is it given for?

What is the black box warning for Midazolam?

A

Given IM or IV

For Preop sedation/anxiolysis/amnesia (in combo with other CNS depressants)

IV midazolam can cause Respiratory Depression/Arrest

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14
Q

When taking the Drug Diazepam, how long is the terminal elimination half-life of the active metabolite N-Desmethyldiazepam?

in what situations can this half-life be increased?

What is Diazepam used for?

A

up to 100 hours

With mild to moderate cirrhosis (+500 hours)

Tx of Anxiety, and Acute Alcohol Withdrawl

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15
Q

What situations are Diazepam contraindicated?

A

Known Hypersensitivity to Diazepam

Pediatric Pts (under 6 months)

Myasthenia Gravis

Severe Respiratory Insuff

Severe Hepatic 3 Insuff

Sleep Apnea

Open Angle Glaucoma –> can be used

Acute Narrow Angle Glaucoma –> can’t be used

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16
Q

When can you not used Diazepam?

A

tx of Psychotic Pts

with ingestion of Alcohol and other CNS Depressant drugs

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17
Q

Uses:

Oxazepam –>

Triazolam –>

Chlordiazepoxide –>

A

Oxazepam –> Anxiety, Anxiety w/ Depression, Acute Alcohol Withdrawl

Triazolam –> Short Term Tx of Insomnia (Cant be used with OPIODS)

Chlordiazepoxide –> Anxiety, Acute Alcholism Withdrawl, Preop Apprehension/Anxiety (Cant be used with OPIODS)

18
Q

Uses:

Flurazepam –>

Lorazepam –>

A

Flurazepam –> Insomnia

Lorazepam –> Seizures (Epilepsy), Pre Op Anxiety

19
Q

What is the drug Flumazenil used for?

What is the black box warning for this drug?

A

Management of Benzo overdose, by complete or partial reversal of the sedative effects of benzos

May cause Seizures

20
Q

List the 6 Barbiturates?

A

Amobarbital

Butabarbital

Pentobarbital

Phenobarbital

Secobarbital

Thiopental

21
Q

Barbiturates are used for?

A

Anxiety

Epilepsy/Seizures

Induce Sleep (Extreme Insomnia)

Anesthetics

Tension Headaches

Counteracts stimulant effects of Cocaine/Meth

22
Q

Which drug classes are widely distributed throughout the body (Into the CNS, Placenta, Breast Milk)?

A

Barbiturates

Benzodiazepines

23
Q

How are Barbiturates metabolized and excreted?

A

Metabolized –> via Liver

Excreted –> via Kidney

Can induce CYP450 enzymes

24
Q

Which Barbiturate is excreted unchanged (20-30%)?

A

Phenobarbital

25
Q

USES:

Ultra Short Acting –> Thoipental –>

Short Acting –> Secobarbital –>

Long Acting –> Phenobarbital –>

A

Ultra Short Acting –> Thoipental –> Anesthesia

Short Acting –> Secobarbital –> Insomnia

Long Acting –> Phenobarbital –> Seizures

26
Q

Thiopental is administered via what route?

and is indicated for what uses?

A

IV

Sole Anesthetic Agent (15 min procedures)

induction of Anesthesia

Hypnosis during balanced anesthesia

controling convulsive state following inhalation anesthesia

Neurosurgical pts with increased intracranial pressure

27
Q

What are some of the unique adverese rxns of Thiopental?

A

Respiratory Dep

Myocardial Dep

Cardiac Arrhythmias

Prolonged Somnolence

Sneezing

Coughing Bronchospasm

Laryngospasm/Shivering

28
Q

Secobarbital is used for what?

Contraindicated in whom?

A

Short term tx of Insomnia (loses its affect after 2 weeks)

NO in:

Hypersensitivty to barbiturates

History of manifest or latent porphyria

impairment of liver fxn

Respiratory dz

29
Q

What do you need to think about if a pt is taking Secobarbital/Phenobarbital/Flurazepam/Zaleplon and they have failure of insomnia to remit after 7-10 days of tx?

A

Primary Psychiatric or Medical Illness

30
Q

Phenobarbital is contraindicated in what patients?

In which pts should you administer Phenobarbital with caution?

A

Known Barbiturate Sensitivity

History of Manifest or Latent Porphyria

Mentally Depressed, Suicidial tendencies, Drug Abuse pts

31
Q

Which drug has been shown to induce liver microsomal enzymes, thus increasing and/or altering the metabolism of barbiturates and other drugs?

A

Phenobarbital

32
Q

In treatment of Insomnia list the uses?

Benzos –>

Zolpidem/Zaleplon/Eszopiclone –>

A

Benzos –> Daytime sedation

Zolpidem/Zaleplon/Eszopiclone –> Sustained Sleep Maintenance

33
Q

Ramelteon is an agonist at what receptors?

It is metabolized by which enzyme?

Which drugs can you not take with this drug?

What warnings are given for this drug?

A

Melatonin (MT1, MT2) Receptors

CYP1A2

Fluvoxamine, SSRI, CYP1A2 Inhibitor

Be careful with Psychiatric Disrder pts

34
Q

What are the only approved tx of

Eszopiclone (Lunesta)

Zolpidem (Ambien)

Zaleplon (Sonata)

A

Tx of Sleep Disorders

35
Q

These Newer Sleep aides (Eszopiclone, Zolpidem, Zaleplon) are metabolized in the liver by what enzymes and exctreted by what?

A

CYP3A4 (p450 metabolism)

Excreted via the Kidney

Short Half-lifes

36
Q

Do the newer hypnotics (sleep aides) have any Anxiolytic, Anesthetic, Anti-convulsant, muscle relaxing, respiratory or cardiovascular effects?

A

NO!

37
Q

Buspirone is used for?

Does it cause Sedation, Hypnotic, Euphoric, anticonvulsant, muscle relaxant effects?

It is extensively metabolized by?

A

Generalized Anxiety Disorder

NO! (its a newer sedative-hypnotic drug)

CYP3A4

38
Q

List the 7 Misc/ Sedative Hypnotic Drugs

A

Buspirone

Chloral Hydrate

Eszopiclone

Meporbamate

Ramelteon

Zaleplon

Zolpidem

39
Q

Zolpidem can cause what in depressed pts?

A

Worsening of depression, suicidal thinking (like SSRI’s)

40
Q

Uses:

Meprobamate –>

Chloral Hydrate –>

A

Meprobamate –> Anxiety Disorders (slows activity of the brain to relax)

Chloral Hydrate –> Short-term use as a Sedative (Sleep Medicine)

NMSP Exam 1 (22 decks)

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