Sedative and Hypnotic Drugs (Wolff) Flashcards

1
Q

The following drugs make up what class?

1) alprazolam
2) clonazepam
3) diazepam
4) lorazepam
5) midazolam
6) temazepam

A

Benzodiazepines

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2
Q

eszopiclone and zolpidem are from what class of drugs?

A

Non-Benzodiazepine BZ1 agonists

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3
Q

flumazenil is from what class of drugs?

A

Benzodiazepine antagonist

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4
Q

The following drugs make up what class?

1) pentobarbital
2) phenobarbital
3) thiopental

A

Barbiturates

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5
Q

ramelteon is from what class of drugs?

A

Melatonin agonist

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6
Q

suvorexant is from what class of drugs?

A

Dual orexin receptor antagonist

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7
Q

doxepin is from what class of drugs?

A

Antihistamine

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8
Q

Why are Benzodiazepine widely distributed throughout the body (CNS, placenta, breast-milk)?

A

They are highly lipid soluble

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9
Q

What is MOA of benzodiazepines?

What effect does this have?

A

1) Facilitate GABA interactions with GABA(A) receptor which increases frequency of Cl- channel opening
2) Causes local hyperpolarization, meaning cell is less likely to fire

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10
Q

What is the most common side effect of benzodiazepines?

A

Drowsiness

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11
Q

What population are particular susceptible to side effects of Benzodiazepine?

What populations are resistant?

A

1) Elderly

2) Alcoholics and barbiturate drug abusers

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12
Q

While patients adapt quickly to the change in normal sleep patterns from benzodiazepines, what happens with abrupt discontinuation?

A

Rebound insomnia

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13
Q

What black box warning do benzodiazepines have?

A

Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death

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14
Q

Because benzodiazepines create a calming effect on the brain, how can the user appear?

A

Drunk

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15
Q

diazepam (Valium) is a major substrate of which CYP?

A

CYP3A4

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16
Q

What is the MOA of zolpidem (Ambien)

What does it act like?

A

1) Binds selectively to BZ1 receptors, a subgroup of GABA(A) receptors
2) Benzodiazepines

17
Q

What is the clinical application for zolpidem?

A

Insomnia

18
Q

What black box warning does zolpidem have?

A

Complex sleep behaviors including sleep-walking and sleep-driving

19
Q

What is the MOA of flumazenil?

A

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

20
Q

Flumazenil blocks the actions of?

A

1) Benzodiazepines

2) Zolpidem

21
Q

What black box warning does flumazenil have?

A

Can cause seizures

22
Q

Which barbiturate is used to control tonic-clonic seizures?

A

Phenobarbital

23
Q

Which barbiturate was among those used as a sedative-hypnotic but was largely replaced by benzodiazepines in clinic?

A

Pentobarbital

24
Q

Which barbiturate was used as intravenous sedatives/anesthetics but was largely replaced by propofol?

A

thiopental

25
Q

What is the MOA of barbiturate?

A

Binds to the GABA(A) receptor and increases the duration of Cl- channel opening

26
Q

Why do barbiturates cause an increasing rate of metabolism of many drugs?

A

They are classic “inducers” of CYP3A4

27
Q

What drug is a nonbenzodiazepine anxiolytic that causes minimal psychomotor impairment?

A

buspirone

28
Q

What is the MOA of ramelteon?

A

Activates MT1 and MT2 (melatonin) receptors in suprachiasmatic nuclei in the CNS

29
Q

What is the clinical application of ramelteon?

A

Sleep disorders characterized by difficulty falling asleep

30
Q

What is the MOA of suvorexant?

A

Blocks binding of orexins which are neuropeptides that promote wakefulness

31
Q

What is the clinical application of suvorexant?

A

Sleep disorders characterized by difficulty falling asleep

32
Q

What is the MOA of doxepin?

What effect does this have?

A

1) H1 receptor antagonist

2) Sedation

33
Q

What is the clinical application of doxepin?

A

Insomnia

34
Q

What is usually the first line medication therapy for anxiety disorders, panic disorders and agoraphobia?

A

Selective serotonin reuptake inhibitors

35
Q

What are efficacious for acute and long-term treatment of Generalized Anxiety Disorder, but should generally be reserved for patients without a history of a substance use disorder?

A

Benzodiazepines