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P2 > Sedatives/Hypnotics > Flashcards

Sedatives/Hypnotics Flashcards

1
Q

Benzo Receptor Agonists

Z-Hypnotics

BDZ Ant

SRPA

A

Alprazolam/Clonazepam/Diazepam/Lorazepam?triazolam/midazolam

Zolpidem

Flumazenil

Buspirone

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2
Q

BDZs def

A

Sedative-hypnotics that produce dose-dependent CNS depressing effects

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3
Q

Sedative (anxiolytic)

Hypnotic

A

Dec activity, excitement, calming

Drowsiness, onset/maintenance of sleep

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4
Q

BDZs use

Z-hyp

Barb

Misc

A

Acute/short term anx
Antidep favored long term
DOC for sleep

Antiepileptics for HA

OTC sleep meds contain antihistamines (diphen)

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5
Q

Dose-dependent effects
BDZ

Barbs

A

Low - anx relief, anticonvulsant, muscle relax
Mod= sleep effects
High- anesthetic effects

Same with BDZs, very high doses can dep breathing/lead to coma

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6
Q

Safety

A

BDZs safe- not general CNS dep (unlike Barb), dont affect CNS resp centers
Safe when alone
Severe overdose can occur if used with S/H/alcohol/CNS depressant drugs

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7
Q

Mech of action of BDZ/Barb

GABA Cl ion channels in CNS (inhib)

A 
GABA- binds neuronal rec, open Cl channel (hyperpolarizes, dec act)
Allosteric modulators (bind distinct sites)
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8
Q

Special considerations for BDZ/Barbs

A

Additive effects- complex has binding sites for other CNS dep (alchol)/ think OD

Cross tolerance- multiple CNS dep sites on single complex (alcholics may be tolerant to BDZ)

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9
Q

BDZ/ Barb action @ Cl channel

A

BDZ- inc channel opening freq

Barb- inc channel open time
High doses, can bind GABA & potentiate inhibition

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10
Q

Therapeutic use of BDZs

A 
Anx DO
Insomnia
Muscle spasms/spasticity
Epilepsy/seizures
Sedation for procedures
AW
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11
Q

BDZ and anx

A

Chronic primary/secondary, anx w/ other psych illness/ acute anx

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12
Q

Primary anx

Secondary anx

A

GAD= alprazolam/lorazepam
Panic- Alprazolam/Clonazepam
Social Anx- BDZ not first line

Due to illness/condition/medication

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13
Q

BDZ popularity

A 
Effective immediately (AD longer)
As needed basis
AD have neg SE= weight gain/sex dysfunction
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14
Q

Chronic insomnia

Risk factors

A

immune dysreg, altered stress response, dec 5HT, WG, DM

HBP, Breathing DO, GI DO, Cancer, Chronic Pain

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15
Q

Insomnia

A

> 30 min to fall asleep
Frequent awakenings
Early morning awakenings
<6hrs of sleep

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16
Q

Z hyp (Zolpidem)

A

Bind BDZ receptors on GABAa complex
Selective hypnotic effect
Minimal anxiolytic/anticonvulsant/muscle relaxant

SE- daytime sleepiness, dizziness, HA, confusion
Caution w/ Sleep Apnea

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17
Q

Z hypnotics vs BDZ

Restorative sleep
Sleep Arch
Interaction w Alcohol
AA

A

Zolpidem- Yes, little change, Yes, Little

Triazolam- Yes, dec stages 3/4/REM, Yes, Yes

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18
Q

Z Hyp vs BDZ

Dose in elderly
Phys dependence
Duration of Px

A

Zolpidem- Dec, Low risk, 3-6m

Triazolam- Dec, High risk, 1-4 w

19
Q

BDZ in muscle spasm

A

Inc presynaptic inhib in SC
Diazepam- muscle injuries, spasticity in deg DO

Clonazepam- red spasticity @ non-hypnotic doses, more potent than diazepam, shorter 1/2 than D

20
Q

BDZ epilepsy/seizure

A

Chronic Seizure Tx- Clonazepam (absence)

Acute Seizure Tx- Diazepam (IV), Lorazepam (IV), Midazolam IM

21
Q

Midazolam

A

DOC for sedation in procedures

Conscious sedation, muscle relax, amnesia, NO analgesia

22
Q

Conscious sedation

A

Min depressed consciousness
Maintain airway
Response to stimulation/verbal commands
Accompanied with amnesia

23
Q

Midazolam Contraindicated in COPD

A

Death w/ RA when pt uses narcotics or COPD

24
Q

BDZ AW

A

Alcoholism- inc risk of tonic-clonic seizure (12-48 hrs later)

Typ Tx- LA BDZ w active metabolites (ie Diazepam)

Tx with adv cirrhosis- BDZ w/out hepatic met (lorazepam)

Due to cross tolerance, max doses needed

25
Q

BDZ Potency

A 
Comp to Diazepam
L= 5x
A= 10x
C= 20x
T= 40x
26
Q

High Potency BDZ & Anx

High Potency BDZ & sleep

A

A/L/C= more selective at lower dose, less SE, inc risk of drug dependency, drug withdrawal issues

T= drug withdrawal issues, amnestic effect

27
Q

Reduce BDZ dose in elderly

A

Dec by 1/2 to 1/3
Hep met dec in elderly
BDZ= lot of Hep met
Blood levels elevated if reduced metabolism not accounted for

28
Q

Considerations with BDZ

A 
Age
Liver dz
Competing drugs
Hx of SUD
Duration of action of BDZ
29
Q

Pharmacokinetics of BDZ

A

LA- D/C
Intermediate- A/L
SA- T
Very short acting- M

30
Q

Absorption/Distrib of BDZ

A 
Absorbed quick (Lipophilic)
Rapid uptake to brain/HPO
Redist to LPT
Fastest w/ highest lipid solubility (D)
Redis dec CNS effects for acute admin
Contraindicated in preg (cross placenta/BM)
31
Q

BDZ vary in lipophilicity

A

Rate of OoA determining
D= more lipo than L, stops seizures faster
But shorter 1/2, so seizures reappear

32
Q

BDZ metabolism

A 
Hep met to water soluble compounds for elim
Usually active (greater 1/2 than parent)
Mult doses of BDZ w long 1/2 can have lots of SE
Shorter 1/2 life= not active, quickly eliminated (L/A)
33
Q

Diazepam LA

A

Phase 1A- oxidation yields AM
Phase 1B- hydrox yields AM
Phase 2- conjug to IM, excreted in urine

34
Q

BDZ Met Cont

A

BDZ that bypass phase 1= shorter 1/2 (L)
Phase 1 less in elderly/liver dz (use those that bypass phase 1 ie L)
Do not induce hep microsomal enzymes

35
Q

BDZ/Hypnotic Pathway of Met

A

Phase 1= A/C/D/Zolpidem

Phase 2= L

36
Q

Drug inhibition of phase 1

A

Fluoxetine
Oral contraceptives
Cimetidine
Grapefruit Juice

37
Q

Insomnia drugs

A

RO- Triaz/ Zolp
SA- least with Z/T (short 1/2)

Before ZHyp, T used
But very potent, tolerant w/in days (use as needed)

38
Q

Adverse effects of BDZ and Hyp

A 
Drowsiness/confusion
Motor incoordination (high dose)
Cog impairment
Anterograde amnesia (more potent BDZ &amp; alcohol, as anesthetic, IV)
Angioedema
Sleep talking/driving/eating

Dissipate in wks
Use caution

39
Q

Avoid/Minimize probs with Abuse/Dep

A 
Identify suscept pt
explain dependence with long term use
Taper gradual (withdrawal can occur)
40
Q

BDZ withdrawal

A

Symp similar to before using BDZ (insomnia/anx)
Depends on drug potency, dose, duration of use, 1/2
More potent, shorter 1/2= more severe, prevalent
Long 1/2= self tapering effect

withdraw graudally

41
Q

Contraindications

A

Elderly= low dose, shorter 1/2, no AM, inc risk of hip fx

LD- dec hep met, no AM

COPD- m exaggerates asthma/bronchitis/COPD

OSA- aggravate sleep breathing DO, use caution with snoring

Alcohol/ others= BDZ effect is additive, lead to OD (resp dep)

Preg/Nursing= BDZ cross BM/placenta

42
Q

Buspirone

A

5HT1A receptors
Partial Agonist, red 5HT act
Selective anxiolytic effect, min CNS dep

No phys dependence/wdr/cross tolerance w BDZ/interaction w alcohol

43
Q

Buspar

A

Very slow OoA (2-4 wks)
Good for elderly, SUD
Some nervousness, tachycardia

P2 (6 decks)

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