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Pharm 3 > E1: Sedative-hypnotics And Anxiolytics > Flashcards

E1: Sedative-hypnotics And Anxiolytics Flashcards

1
Q

What kind of drugs are used for short term treatment of insomnia?

A

Sedative hypnotics

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2
Q

What is the DOC for enuresis?

A

TCAs

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3
Q

What kind of channels are GABA receptors?

A

Cl channels

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4
Q

What does activation of GABAa receptors do?

A

Causes depression of electrical activity, which decreases anxiety and promotes sleep

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5
Q

What is the MOA of barbiturates?

A

-Binds to GABA receptor and stimulates Cl influx, which produces inhibition independent of GABA

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6
Q

What are the effects of barbiturates?

A
  • Marked CNS depressant, hypnosis

- cause euphoria

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7
Q

What kind of drug is phenobarbital?

What is it commonly used for?

A
  • Long acting barbiturates

- often used as anticonvulsants

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8
Q

How are barbiturates metabolized?

A
  • metabolized by the liver

- induces CYP450s with chronic use

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9
Q

What are the side effects of barbiturates?

A
  • CNS depression: drowsiness, mood distortion, impaired judgment
  • Paradoxical excitement
  • vertigo, n/v/d
  • severe physiological and psychological dependence
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10
Q

What are the contraindications of barbiturates?

A
  • porphyria: enhance porphyrins synthesis
  • pulmonary insufficiency: may cause respiratory depression
  • Supra-additive effects
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11
Q

Why are barbiturates dangerous drugs?

A

They do not have a ceiling effect and have a low margin of safety
-Supra-additive effects with alcohol

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12
Q

What are the most commonly used group of anxiolytics and sedative-hypnotics?

A

Benzodiazepines

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13
Q

How are benzodiazepines metabolized?

A

-metabolized by CYP34A in the liver where it is converted to active metabolites

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14
Q

Which benzos have a long duration of action?

A

Diazepam and flurazepam

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15
Q

Which benzos have and intermediate duration of action?

A

Alprazolam and oxazepam/lorazepam

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16
Q

Which benzo has a short duration of action?

A

Midazolam

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17
Q

What is the MOA of Benzos?

A
  • Bind to specific sites of the GABAa receptor, increases affinity of the receptor to GABA prolonging its action
  • effect is dependent on GABA
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18
Q

Are benzos or barbiturates safer? Why?

A

Benzos are safer because they have a ceiling effect

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19
Q

What is the DOC for anxiety?

A

Benzos

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20
Q

What are the anxiety disorders that benzos are not used for?

A
  • OCD
  • Agoraphobia and panic disorders
  • post traumatic stress
  • anxiety and children and adolescents
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21
Q

What benzos are commonly used for insomnia?

A

Flurazepam and temazepam

22
Q

What benzos are commonly used for status epilepticus?

A

Diazepam and lorazepam

23
Q

Which benzo is used in preparation for anesthesia for short surgical procedures?

A

Midazolam

24
Q

Which benzo causes anterograde amnesia?

A

Midazolam

25
Q

Which benzo is often used for muscle relaxation?

A

Diazepam

26
Q

Which Benzos can be given to provide a tapered withdrawal?

A

Chlordiazepoxide, diazepam, and lorazepam

27
Q

What are the side effects of Benzodiazepines?

A
  • CNS depression: dizziness, sedation, confusion
  • Paradoxical excitement
  • Supra-additive effects
  • sleep related behaviors
28
Q

What is paradoxical excitement?

A

-stimulation, hyperactivity, and aggressive behavior that may occur due to dis-inhibition of suppressed behavior, common in the elderly

29
Q

What are the contraindications to Benzodiazepines?

A
  • Should not be given during pregnancy unless absolutely necessary
  • sleep apnea
  • elderly
30
Q

What is important to remember about Benzodiazepines and withdrawal?

A
  • Abrupt discontinuation can cause rebound increases in insomnia and anxiety
  • BZs should be tapered very slowly following chronic use
31
Q

What kind of drug is Flumazenil?

A

Benzodiazepine antagonist

32
Q

What is the MOA of Flumazenil?

A

-Competes with BZs for GABA receptor and reverses the effects of BZs

33
Q

What is the major adverse effect of Flumazenil?

A
  • Triggers withdrawal and seizures in patients who are physically dependent upon BZs
  • do not used in patients with history of seizures
34
Q

What are the “Z” drugs?

A

Zolpidem (ambien), Zaleplon (Sonata), and Eszopiclone (lunesta)

35
Q

What is the MOA of the “Z” drugs?

A

Bind to the BZ1 subtype of the GABA receptor to increase GABA mediated inhibition

36
Q

Which of the “z” drugs has a long half life?

A

Eszopiclone

37
Q

What are the side effects of the “z” drugs?

A
  • High margin of safety
  • Diarrhea and nausea
  • sleep related behavior
  • rebound insomnia
  • Withdrawal symptoms
38
Q

What is the MOA of Suvorexant?

A
  • Antagonist at orexin receptors

- Orexins are involved in regulating the sleep wake cycle and promote wakefulness

39
Q

How is suvorexant metabolized?

A

Metabolized by CYP3A4

40
Q

What are the contraindications for suvorexant?

A

Narcolepsy

41
Q

What is the MOA of Ramelteon?

A
  • melatonin analogue, resets the sleep wake cycle

- promotes sleepiness with no GABA effect

42
Q

How is Ramelteon metabolized?

A

CYP450 in the liver

43
Q

What are the side effects of Ramelteon?

A
  • Additive sedation with alcohol and other sedative hypnotics
  • drowsiness, dizziness, and nausea
44
Q

When is Benadryl indicated for insomnia?

A

Useful for occasional insomnia and are especially useful in someone who has been addicted to Benzos or alcohol

45
Q

What is the MOA of Chloral Hydrate?

A

-Acts similarly to barbiturates on GABAa receptor, converted to trichloroethanol which causes sedation

46
Q

Is chloral hydrate a safe drug?

A

No it has a low margin of safety, high doses induce respiratory and vasomotor depression

47
Q

What are the side effects of Chloral hydrate?

A
  • gastric irritation, nausea, vomiting, and cardiac arrhythmias
  • long term use may cause liver damage and fatal intoxication
48
Q

What is the use of Buspirone?

A

Relieves anxiety without producing sedation

49
Q

What is the MOA of Buspirone?

A

Partial agonist at the postsynaptic serotonin receptor

-Full agonist for presynaptic serotoninc receptors

50
Q

How is Buspirone metabolized?

A

CYP3A4 in the liver

Pharm 3 (20 decks)

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