Class 5 - Sleep Flashcards

1
Q

Common pharmaceuticals

A
  • Melatonin
  • Zopiclone
  • Zolpidem
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2
Q

Pharmacology is used to…

A

Control behavioural alterations
- Sleeplessness
- Anxiety
- Agitation
- Depression

Maintain function in dementia
- helps maintain memory, thinking, speaking skills

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3
Q

Benzodiazepines MOA

A

Depress CNS activity
- Affect hypothalamic, thalamic, and limbic system of the brain
- Potentiate the inhibitory effects of endogenous GABA, but there is a cieling effect

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4
Q

Benzodiazepines: Withdrawal

A

Insomnia, anxiety, agitation, tremor, tachycardia, anroexia

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5
Q

Benzodiazepines: Other

A

Does not increase metabolism of other drugs (fewer drug interactions)

PO route is preferred - less side effects

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6
Q

When drugs bind to GABA receptor, inhibitory effects of GABA are enhanced, the effects are:

A

Anxiety is reduced –> Wakefulness is reduced, sedation to anaesthesia –> Memory and awareness is affected, amnesia, hypnotic effect –> Neuro-excitability is reduced, anti-convulsant effect

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7
Q

How does the GABA receptor-chloride channel complex work

A

When bonzos and barbituates bind to the receptor, this opens the chloride channel inhibiting the neuron from firing

Makes the channel very negative inside and inhibits firing

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8
Q

Good sedative-hypnotics

A

Benzodiazepines potentiate GABA
- Diazepam (Valium - long actong)
- Lorazepam (Ativan - intermediate acting)
- Midazolam (versed - short acting)

Other benzo-like effects: Zopiclone

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9
Q

Benzodiazepines: OD Mild

A

Drowsiness, impaired coordiation, confusion, lethargy

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10
Q

Benzodiazepines: OD Serious

A

Ataxia (clumsy muscle mvmt), hypotonia, hypotension, respiratory depression, coma

Think LESS of everything… too LESS

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11
Q

Benzodiazepines: OD Serious

A

Ataxia (clumsy muscle mvmt), hypotonia, hypotension, respiratory depression, coma

Think LESS of everything… too LESS

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12
Q

Benzodiazepines: OD Rare

A

Cardiac arrest when combined with alcohol/other CNS depressants

Flumazenil is antidote

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13
Q

Benzodiazepines and enzyme inducers

A

Reduce effect of benzos by speeding its breakdown

Ex. Carbamazepine, phenobarbital, phenytoin, St John’s Wort

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14
Q

Benzodiazepines and enzyme inhibitors

A

Increase effect of benzos by delaying breakdown

Ex. Grapefruit (diazepam), diltiazem, verapamil, macrolide antibiotics

fluconazole, omeprazole, OC

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15
Q

Benzodiazepines interactions

A

Do not induce hepatic drug-metabolizing enxymes but additive with other CNS depressants (alcohol, opioids)

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16
Q

Other sedative-hypnotics

A

Zopiclone (Immovane) - PO, short term use for insomnia
Buspirone (Buspar) - 2nd line for general anxiety

17
Q

Melatonin

A
  • Secreted by pineal gland to maintian sleep-wake cycle
  • Naturally stimulated by darkness (11pm - 3am)
  • Synthetically produced to mimic melatonin
18
Q

Bad sedative-hypnotics

A

Barbituates
- Phenobarbital (PO), pentobarbital (IV, IM), thiopental (IV)

Easy to OD, interacts with MANY drugs

19
Q

Barbituates: General outline

A

Sedative -> hypnotic -> GA -> Deep coma -> Death

20
Q

Barbituates: MOA

A

Enhancing and/or mimicking the effect of GABA that does NOT have a ceiling effect (WHICH IS BAD)

Very narrow therapeutic index