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Anxiety_Insomnia Flashcards

1
Q
  • PAMs
  • ZOLAMs
  • Other
A

Benzodiazepines

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2
Q

Benzos __________ GABA

A

POTENTIATE (the effects of)

→Improves GABAα so ↑ Cl- at postynaptic membrane → depresses nerve impulses

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3
Q

L-O-T benzos

→Why are they unique?

A 
Lorazepam
Oxazepam
Temazepam
→ NO active metabolites 
→ Metabolized via conjugation 
(*all others are cyp450 metabolized & so liver metabolized)
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4
Q

Benzos are metabolized into ________ ________ & excreted _________.

A

inactive drug

renally

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5
Q

IV Benzos

A
  1. Lorazepam
  2. Diazepam
  3. Midazolam
    L-D-M
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6
Q

Benzos Absorption

A

90% rapid & complete absorption from GI

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7
Q

Benzos for the elderly….

→ Good or bad idea?

A

BAD idea!
→ make things worse like…
amnesia, groggy, respiratory interactions, drug interactions, FALL RISK

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8
Q

Benzos Contraindications (5)
vs.
Precautions (5)

A
  1. Allergy to benzos
  2. ANAG (acute narrow angle glaucoma)
  3. Sleep apnea
  4. Severe respiratory insufficiency
  5. Myasthenia gravis
  6. Cocomitant CNS depressants
  7. Withdrawal
  8. Lorazepam IV (avoid if possible)
  9. Tolerance
  10. NEVER use as an analgesic, antidepressants, or antipsychotics
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9
Q

Benzos Contraindications (5)
vs.
Precautions (5)

A
  1. Allergy to benzos
  2. ANAG (acute narrow angle glaucoma)
  3. Sleep apnea
  4. Severe respiratory insufficiency
  5. Myasthenia gravis
  6. Co-concomitant CNS depressants
  7. Withdrawal
  8. Lorazepam IV (avoid if possible)
  9. Tolerance
  10. NEVER use as an analgesic, antidepressants, or anti-psychotics
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10
Q

Benzo:

Conscious sedation

A

Diazepam

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11
Q

Benzo:

Unconscious sedation

A

Midazolam IV

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12
Q

Benzo:

Inability to STAY asleep

A

Temazepam

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13
Q

Benzo:

Inability to FALL asleep

A

Triazolam

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14
Q

2 big reasons not to use benzos for sleep

A
  1. Habit forming

2. Tolerance-withdrawal causes rebound insomnia

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15
Q

Benzo:

Anticonvulsant

A

Clonazepam (maintenance)

Diazepam or Lorazepam (IV for status epilepticus)

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16
Q

Benzo:

Muscle relaxant

A

Diazepam

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17
Q

Benzo:

Anticipatory for chemo for N/V

A

Lorazepam

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18
Q

Benzo:

Ethanol Withdrawal

A

Lorazepam
Diazepam
Oxazepam, chlordiazepoxide

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19
Q

Benzos:
High doses ________
Low doses ________

A

→ Sedation

→ Anti-anxiety

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20
Q

Zolpidem
Eszopiclone
Zaleplon

A

Nonbenzodiazepine Benzodiazepine Receptor Agonist (NBBRAs)

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21
Q

NBBRA

MOA

A

Binds near the GABA receptor → similar effect to benzos w/ opening postsynaptic Cl- channels

22
Q

What do you do for females taking a NBBRA?

A

Check if it is Zolpidem?

→ MUST adjust the dose b/c females have 45% ↑ AUC & Cmax

23
Q

NBBRA

Metabolism & Excretion

A

Mostly 3A4 at liver

→excreted in urine

24
Q

NBBRA

Warnings (2)

A
  1. Complex sleep behaviors

2. Dependence

25
Q

NBBRA Clinical Utility:

  1. Zolpidem
  2. Eszopiclone
  3. Zaleplon
A

Utility: Insomnia

Zopidem: sublingual & lingual spray
Eszopiclone: only use up to 6 mo
Zaleplon: better than zopidem w/ psychomotor effects (faster elimination)

26
Q 
Amobarbital 
Pentobarbital 
Thiopental 
Secobarbital 
Phenobarbital
A 
Barbiturates 
Amobarbital 
Pentobarbital 
Thiopental → ultra-short action 
Secobarbital → short acting
Phenobarbital → long acting
27
Q

Barbiturates

MOA

A
  1. Bind GABA at MULTIPLE sites in CNS
  2. ↑ DURATION that Cl- channels are open
  3. ↓ glutamate
  4. Non synaptic membrane effects
28
Q

GABA mimetic at high concentrations

A

Barbiturates

29
Q

Barbiturates & their big differences with benzos (4)

A
  1. Different binding sites
  2. Less selective
  3. Non synaptic membrane effects
  4. MORE CNS depression than barbiturates
30
Q

Can cross the placenta and depress the fetus

A

Barbiturates

31
Q

Distribution of barbiturates in body

A

Brain → splanchnic areas → skeletal muscle → adipose tissue

32
Q

Barbiturates

Metabolism

33
Q

Why should you be careful with barbiturates & other drugs?

A

MANY CYP 450 interactions

Barbiturates are INDUCERS

34
Q

Death
Many interactions→ induce CYP 450
Drowsiness, impaired concentration, mental/physical sluggishness
Synergistic CNS effects w/concomitant CNS depressants
Hypnotic doses→ “hangover effect”

A

ADR of Barbiturates

35
Q

Barbiturates

Contraindications

A
  1. Acute Intermittent Porphyria
  2. Marked Hepatic Impairment
  3. Nephritic pts
36
Q

Barbiturate used in surgery as anesthesia

A

Thiopental IV (old school)

37
Q

Barbiturate used as anticonvulsant

A

Phenobarbital (not 1st line)

38
Q

Barbiturate used for HA

A

Butalbital → combo product for migranes

39
Q

Buspirone

MOA

A

Unknown
→Partial Serotonin Agonist (1A & 2A)
→Dopamine D2 affinity

…getting hit by a BUS

40
Q

Buspirone
Metabolism
Elimination

A

→Extensive 1st pass metabolism
→ > 1 active metabolite

Elimination: Urine & Stool

41
Q

Buspirone

Use

A
  1. Chronic Generalized Anxiety

→Onset of full effect: 4-8 weeks

42
Q

Doesn’t interact w/ alcohol or other CNS depressants

43
Q 
Hypertensive reactions when given with MAO-is
Dependence unlikely
Dizziness
Light-headnessness
Insomnia
Tachycardia, palpitations, HA
44
Q

Ramelteon

Tasimelteon

A

Melatonin Receptor Agonist

45
Q

Activates melatonin receptors in the suprachiasmic nucleus

A

Melatonin Receptor Agonist

MOA

46
Q

Melatonin Receptor Agonist

Utility

A
  1. Sleep disorders

* Can be used longer term

47
Q

Dizziness, fatigue, somnolence

Minimal potential for abuse- no evidence of dependence or withdrawal effects

A

Melatonin Receptor Agonist

ADR

48
Q

Antagonize Orexin A and B peptides in hypothalamic neurons

A

Suvorexant

49
Q

Suvorexant

Utility

A
  1. Helps fall asleep 5-10 min sooner

2. Helps stay asleep 15-25 min longer

50
Q

What do Orexin A & B control?

A

↑ orexin A & B control wakefulness

*so suvorexant antagonizes these and does the opposite → promotes sleeping

Clinical Medicine (6 decks)

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