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Psych 2 > Benzodiazepines and Sedative/Hypnotic Drugs > Flashcards

Benzodiazepines and Sedative/Hypnotic Drugs Flashcards

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1
Q

BDZs
Z-hypnotics
barbiturates
Miscellaneous

A

Prev 1st line for anxiety and sleep…used for acute/short term anxiety tx

DOC for sleep

Primary prior to BDZs…now used as antiepileptics

OTC meds contain antihistmaines

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2
Q

Sdative hyponitcs

A

Dose-dependent CNS depressant effects

Sedatives- decrease aniety excitement, and produce calming

Hypnotics - dowsiness and for sleep

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3
Q

Dose-dependency of BDZs and barbs

A

At higher doses, barbs depresss breathing

Low dose - anxiety, anticonvulsant, muscle relaxer

Mod - sleep

High - anestheti

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4
Q

BDZ safety

A

Not general CNS depressatns like Barbs (no resp effect)

Severe overdose can occur if dosing with other things

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5
Q

MOA of BDZs

A

GABAA receptor chloride ion channels in the CNS

GABA binds to receptors and opens Cl channel, CL hyperpolarizes cell

BDZs are allosteric modulators because bind to other site than GABA

Additive effects can occur wit halcohol

Cross tolerance can occur (alcholoic may be tolerant)

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6
Q

BDZs and Barbs MOA and idfference

A

Both in GABA cl chennls in CNS

BDZs increase opening frequency

barbs increase opening time

at high doses barbs also bind directly to GABA site

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7
Q

Uses of BDZs

A 
Anxiety
insomnia 
Muscle spasm/spasiticty
Epilepsy 
Sedation
Alohol w/d
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8
Q

BDZs for GAD, Panic, social, secondary anxiety

A

GAD - persistent…alprazolam/lorazepam

Panic - sudden onset…alprazolam/clonazepam

Not good for social

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9
Q

To avoid issues with dependence and w/d

A

Favor short term with BZDs and use antidepressants for long term

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10
Q

BDZs vs. antidepressants

A

Benzos can be taken o nas needed basis

Effective immediately

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11
Q

Z-hypotics and definition of insomina

A

Used for sleep

Over 30 minutes to fall asleep…frequent awakenings…early-morning awakennings, less than 6 horus of sleep

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12
Q

Z-hypnotics things to know

A

Bind to BDZ receptors on GABAa receptor channel complex

Selective hypnotic effect but NO anxiety effect (or others)

SE - daytime sleepiness, dizziness, headache, confusion

Worry about using with sleep apena

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13
Q

BDZs vs. z-hypnotcis

Resotriave sleep
Sleep arch
alcohol intx
Anterograde amenia 
Dose in eldery
Dep
Prescrip duration
A

Yes - both
Z changes little while trazolam decreaes 3,4, rem
Yes - both
Very little with Z
Reduced
Lower risk in Z
3-6 months for Z, less than a month for BDZ

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14
Q

Diazepam

A

Used for muscle injuries and muscle spastiicty in degenerative diseases

Increase presynaptic inhibition in the spinal cord

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15
Q

Clonazepam

A

Reduces spastiity at non-hypnotics doses

More potent and shorter 1/2 life than diazepam

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16
Q

Chronic and acute seizrue tx

A

Chronic - clonazepman but will get tolerance

Acute - diazepam, lorazepma in the ER…midazolam on the way

17
Q

midazolam

A

Used for conscious sedation, muscle relaxation, amneisa, no analgesia

Worry about admin with opiodi bc of hypoxia

Contraindication in patients with narcotics or COPD

18
Q

Conscois sedation

A

Minimkkally depressed consciousnness

Ability to maintain airway
Response to commands

Amenisa

19
Q

Tx of acute alcohol withdrawl

A

12-48 hours after last drin (tonic clonic seizures)

Typical - prefer diazepam bc longer active metabolites

With cirrhosis - lorazepam bc no heptaic metabolism

Lots of cross tolerance s oup the dose

20
Q

High potency BZs for anx

A

Pros - more selective at lower doses and fwerr side effects

Drug dependcy and withdrawl

Alpra
Lora
Clona

21
Q

High potency BDZ for sleep

A

Traizolam

Same withdralw issues as above and some amnesia

22
Q

BDZ and elderly

A

Reduce dose

Decreased hepatic metabolism in elderly and most metabolized by liver

23
Q

Long acting
IM acting
Short acting
Very short

A

Diazepam, clonazepam (1-3 days)
Alprazolam, lorazapeam (10-20 hours)
Traizolam (3-8 hours)
Midazolam (1-6 hours)

24
Q

BDZ absorption and distributuon

A

Lipophilic so quikc absoprtion

Raid uptake to brain and other highly perfused

BDZs are redistributied…faster for more lipid soluble (diazapm most*)…more pronounced in acute admin (seizures)

Cross placenta and secreted into breast milk so contraindicated

25
Q

BDZs lipophilicity

A

Diazepam is most

Rate of onset of action determined by this

Diazepam better at stopping seiures but could also have them reappear because exits brain faster

26
Q

Metab of BDZs

A

Diazepam to active metabolite

Half life of active is greater than parent

Lorazepam and alprazolam are shorter 1/2 and are quickly eliminated

27
Q

Diazepam metab

A

Oxidation to active metabolite
Hydroxylation to another active
Conjugated to glucuornic yileds inactive that is excreted

28
Q

BDZ interactions and other metab

A

Lorazepam bypassees phase 1 and has shorter t1/2…all others use phase 1

Phase 1 reduced in elderly and liver d (so use lorzaepaM)

Unlike Barbs, BDZs do NOT induce the heaptic microsomal enzymes

Cimetidine, contraeptivve, fluoxetine, GF juice

29
Q

Ideal insomnia drug

A

Rapid onset, approrpaite DOA, and no reidual action

Traizolam is most potent BDZ…tolerance developed in days…use it on as needed basis

30
Q

Adverse effects of BDZs and Z-hypnotics

A

Drowsiness and confusion
Motor
Cog impairment
Anterograde amnesia (more if IV, more with BDZs and alcohol)

31
Q

Minimizing abuse and dep

A

W/d will occur on abrupt discontinuation

Gradual drug tapering needed

32
Q

BDZ w/d

A

Severity depends on poetncy, dose, duration and t1/2

With long half life, have slef-tapering effect

Rbound insomnia and anxiety more iwth more potenty or shrt acting

33
Q 
Elderly
Liver dz
COPD 
Obsturctive sleep apnea
Alcohol
Pregnancy
A

Use lower doses, shorter 1/2 and no active mtabolites…hip fracutres

Use no active metabolites

Midazolam is porblem

Use caution

Additive effect and can leadto resp depression

Cross placenta nd enter breast milk

34
Q

Buspirone

A

Acts at 5-HT1a receptors

Partial agonist (reduces activity)

Selective anxiolytic effect with minimkal CNS depression

No dependcence or w/d
No cross tolerance wit hBDZs
No alcohol intx

Very slow onset so good for elderly of sub abuse probs

Sme nervousness and tachy

Used for anxiety

35
Q

Flumazenil

A

Reverses BDZ induced conscious sedation or BDZ overdose

36
Q 
Alpra
Clona
Dia
Lora
Tria 
Mida 
Zolp
Fluma
BUsp
A 
Anx
Anx, seiz
Anx, seiz, muscle spaz, alc w/d
Anx
Insom
Conscious sedation and anxiety
Insom
Reersal of BDZs 
Axiety

Psych 2 (15 decks)

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