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SMUSPG-Behavioral > Sedation > Flashcards

Sedation Flashcards

1
Q

Sedative anxiolytic

A 
exert calmng and reduce anxiety
hypnotic- produce drowy
Insomnia
GAD
Reduce anxiety at low dose
sedation at high
GABA is major inhibitory neurotransmitter of CNS
3- A- Etoh, z, drugs, BZD, Barbs
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2
Q

Tolerance and Dependence

A

Tolerance- physiological state, reduced drug effect with repeated use of the drug (higher doses needed to produce same effect)

Cross-tolerance- individuals tolerant to one drug will be tolerant to other drugs in the same class-barbiturates, benzodiazepines, and ethanol

Dependence- s/sx of withdrawal when drug levels fall

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3
Q

Binding Site Ligands

A

Agonists: facilitate GABA actions

Antagonists: blocks the effects of agonist reverse some drugs, but not barbiturates or alcohol

Inverse Agonist: cause anxiety and seizures, can block the binding and effects of benzodiazepines.

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4
Q

GABAA Receptor α Subunits

A

α1 sedation, anticonvulsant actions, amnesia- Z DRUGS

α2-α3 anxiolytic, muscle relaxant, alcohol potentiating

α5 cognition and other functions

BZD- NON SELECTIVE inc SE, a12,3,5

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5
Q

GABA/Glutamate effect w/ ETOH

A

Gaba-inhibotory slows down
Glutamate- excitatory

Drink ETOH occasion- GABA inc, Glut dec.
Chronic ETOH regu- balance
ETOH WD- GABA leve fall, Glutamate cravings

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6
Q

Barbiturates - Indications

A

RARE used
MOA – Binds to barbiturate site within GABAA receptor

Phenobarbital – long-acting (days) used to treat epilepsy

Sedation
Hypnotic - Lose effectiveness after 2 weeks
Anesthesia: thiopental, methohexital (rarely used)

Anticonvulsant-Emergency control of certain acute convulsive episodes

Liver cleared
Long 1/2 life
Narrow TI
Lots of DI
LETHAL OD
WITHDRAWL sx LETHAL
HIGH dependenc abuse
CNS respistory distress
ADE-
Dose related:
Drowsiness
Ataxia
Slurred speech
Lethargy
Cognitive difficulties
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7
Q

Benzodiazepines (PAM)

A

Elimination half-life – determined by the rate of liver metabolism and/or renal excretion
Duration of action is the time the drug is present at the GABA receptors in the brain

Binds to GABAA ( 1,2,3,5) – enhances GABA

All benzos reduce anxiety and produce sedation (in contrast to barbiturates)
PDD
GAD
insomnia
Seizure
Etoh WD
Msk spasm
Preop

NOT FOR LONG TERM
HIGH LIPOPHICLITY

Caution Elderly and Liver dz
SAFE LOT- lorazepam, oxazepam, temazepam

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8
Q

Benzodiazepines (PAM) ADE

A 
ADE- sedation fatigue
CNS respirtariy depression if combined
ETOH
BArbs
Opiods
TCA
CPD
OSA
Etoh-acute intox
Toleranc
Pregancy X
Phyical dependence-inc higher lipophilicity

WD***- occure after 4 weeks
DONT GIVE >4WKS USE INTERMITENT DOSING TO AOVID DEPENCED AND TOLERANCE
tapering:
Switching to a longer acting benzodiazepine ,
Reduce dose by 50% the first 4 weeks, maintain on that dose for 1–2 months,
then reduce dose by 25% every 2 weeks

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9
Q

BZD SCALE

A

BENEFITS- Rapid SX relife
Risk- SE, not for PTSD
ABuse

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10
Q

Flumazenil (Romazicon®)

A

Benzodiazepine Antagonist:

Reversal of conscious sedation
Suspected BDZ overdose

Seizure risk

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11
Q

‘Z’ drugs
Zolpidem (Ambien®)
Zaleplon (Sonata®)
Eszoplicone (Lunesta®)

A 
Non-benzodiazepines: MOA
Selective GABAA 1 receptor agonist 
INSOMNIA ONLY
no myorelaxant, 
no anxiolytic, 
no anticonvulsant activity

Common:
dizziness, HA
Dose-related: Sleep-related behaviors,

FDA suggesting reduced doses due to this

NOT SAFE FOR LT- 2X LIKELY ADE

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12
Q

Suvorexant (Belsomra®)

A

MOA: orexin receptor antagonist
Orexins are chemicals that are involved in regulating the sleep-wake cycle, keeping people awake.

within 30 minutes of going to bed, with at least 7 hours remaining before
ADE- driving, deep sleepingness

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13
Q

Buspirone (Buspar®)

A

Useful in OCD, anxiety disorders, Depression
MOA:
Partial 5HT1A postsynaptic agonist

Slow onset - May take up to 2-4 weeks to see improvement
Must be taken daily

***Side effects (infrequent)

Drug Interactions: MAOIs – closely monitor BP

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14
Q

Sedating Antidepressants

A

Trazodone- effective when used with an antidepressant in patients with depressive disorders

Mirtazapine

TCAs-Amitriptyline and Doxepin (Sinequan®)
May be preferred in patients with concomitant pain or migraine disorders
risk for suicide due to risk of toxicity in overdose

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15
Q

Other: Sedative-Hypnotics/Anxiolytics

Antihistamines

A
  • Histamine modulates neuronal firing during wakefulness
    Diphenhydramine, Hydroxzine, Doxylamine
    Contraindications: BPH, narrow-angle glaucoma, CV disease
    Dose Adjustment: elderly
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16
Q

Medical condtions Related to Anxiety

A

Respiratory (SABA, LABA, theophylline)

Stimulants (caffeine, pseudoephedrine, cocaine, methylphenidate, amphetamine)

CNS sedative withdrawal

***High-dose SSRI

Hyperthyroidism, pheochromocytoma, hypoglycemia
Angina, arrhythmias, MI
Asthma/COPD

17
Q

Medical condtions Related to Insomnia

A

Antidepressants (bupropion, SSRI, MAOIs)

Stimulants (appetite suppressants, decongestants, nicotine, caffeine)

Beta agonists

Corticosteroids, alcohol, diuretics,

Sleep disorders (sleep apnea, restless leg syndrome, nocturnal myoclonus)
Thyroid disorders
Persistant nocturnal cough

18
Q

Insomnia Classification

A

Transient-2-3 days duration

Short-term-Lasts up to 3 weeks

Chronic/Long-term-Lasts longer than 3 weeks

19
Q

Gabapentin

A

increase slow-wave sleep (deep sleep), reduce sleep latency and reduce arousals

reduce drinking, promote abstinence and improve sleep in patients with alcohol use disorders

20
Q

Generalized Anxiety Disorder (GAD)

Onset of clinical effect

A

Benzodiazepines: 1 – 2 weeks; 60 – 80% response rate

Antidepressants – start with lower than normal doses; takes 8-12 weeks for full effect, SSRI, mirtazapine, nefazodone, SNRI; ***not bupropion, inc AnXiety

Duration: 4 – 6 months after sx free

21
Q 
Panic Disorder (PD)
Onset of clinical effect
A

Antidepressants (SSRI, TCA, MAOIs)

BDZ – not as needed use, dosed continously
Duration
Adequate trial: 8 – 12 weeks

When DCing, taper off over 4 to 6 months

22
Q

Other Anxiety Disorders

A

Situational Anxiety-propranolol

(PTSD)-SSRIs (fluoxetine, sertraline, paroxetine), mirtazapine

Prazosin – sympatholytic (blocker)-nightmares

Anxiolytics –buspirone, cyproheptidine; BDZ (limited efficacy, may be harmful)

Mood stablizers

Atypical antipsychotics SGA-limited data

(OCD)-SSRIs (fluoxetine, fluvoxamine, sertraline)

(PMDD)-Fluoxetine (Prozac®), Sertraline; citalopram

SMUSPG-Behavioral (11 decks)

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