Anxiety_Insomnia Flashcards

(50 cards)

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
NBBRA Clinical Utility: 1. Zolpidem 2. Eszopiclone 3. Zaleplon
Utility: Insomnia Zopidem: sublingual & lingual spray Eszopiclone: only use up to 6 mo Zaleplon: better than zopidem w/ psychomotor effects (faster elimination)
26
``` Amobarbital Pentobarbital Thiopental Secobarbital Phenobarbital ```
``` Barbiturates Amobarbital Pentobarbital Thiopental → ultra-short action Secobarbital → short acting Phenobarbital → long acting ```
27
Barbiturates | MOA
1. Bind GABA at MULTIPLE sites in CNS 2. ↑ DURATION that Cl- channels are open 3. ↓ glutamate 4. Non synaptic membrane effects
28
GABA mimetic at high concentrations
Barbiturates
29
Barbiturates & their big differences with benzos (4)
1. Different binding sites 2. Less selective 3. Non synaptic membrane effects 4. MORE CNS depression than barbiturates
30
Can cross the placenta and depress the fetus
Barbiturates
31
Distribution of barbiturates in body
Brain → splanchnic areas → skeletal muscle → adipose tissue
32
Barbiturates | Metabolism
Hepatic
33
Why should you be careful with barbiturates & other drugs?
MANY CYP 450 interactions | Barbiturates are INDUCERS
34
Death Many interactions→ induce CYP 450 Drowsiness, impaired concentration, mental/physical sluggishness Synergistic CNS effects w/concomitant CNS depressants Hypnotic doses→ “hangover effect”
ADR of Barbiturates
35
Barbiturates | Contraindications
1. Acute Intermittent Porphyria 2. Marked Hepatic Impairment 3. Nephritic pts
36
Barbiturate used in surgery as anesthesia
Thiopental IV (old school)
37
Barbiturate used as anticonvulsant
Phenobarbital (not 1st line)
38
Barbiturate used for HA
Butalbital → combo product for migranes
39
Buspirone | MOA
Unknown →Partial Serotonin Agonist (1A & 2A) →Dopamine D2 affinity ...getting hit by a BUS
40
Buspirone Metabolism Elimination
→Extensive 1st pass metabolism → > 1 active metabolite Elimination: Urine & Stool
41
Buspirone | Use
1. Chronic Generalized Anxiety | →Onset of full effect: 4-8 weeks
42
Doesn't interact w/ alcohol or other CNS depressants
Buspirone
43
``` Hypertensive reactions when given with MAO-is Dependence unlikely Dizziness Light-headnessness Insomnia Tachycardia, palpitations, HA ```
Buspirone
44
Ramelteon | Tasimelteon
Melatonin Receptor Agonist
45
Activates melatonin receptors in the suprachiasmic nucleus
Melatonin Receptor Agonist | MOA
46
Melatonin Receptor Agonist | Utility
1. Sleep disorders | * Can be used longer term
47
Dizziness, fatigue, somnolence | Minimal potential for abuse- no evidence of dependence or withdrawal effects
Melatonin Receptor Agonist | ADR
48
Antagonize Orexin A and B peptides in hypothalamic neurons
Suvorexant
49
Suvorexant | Utility
1. Helps fall asleep 5-10 min sooner | 2. Helps stay asleep 15-25 min longer
50
What do Orexin A & B control?
↑ orexin A & B control wakefulness | *so suvorexant antagonizes these and does the opposite → promotes sleeping