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92 Cards in this Set

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Gastric ulcer
MI
Disease related anxiety
Treat the disease
Short term Rx of sedative-hypnotic
death of family member
surgery
Situational anxiety
Short term Rx
generalized anxiety disorder
panic disorder
Chronic anxiety
psychotherapy and Rx
sleep apnea
do not use hypnotics- dec arousal response to hypoxia; exacerbate obstructive sleep apnea by reducing muscle tone
circadian rhythm disturbances
hypnotics can help
disease-related insomnia (depression, anxiety, psychosis, chronic heart failure, pain)
treat medical condition first
Rx/substance related insomnia (alcohol, SSRIs, anti-Parkinson's, methylxanthines, diuretics)
first alter dosing regimen or medication choices
Transient insomnia
Rx for 2-3 days, not more than 2-3 wks --> than taper
chronic insomnia
first change exercise, diet, behavior
some new hypnotics are safe(r)
long term use is problematic/not recommended
Name six classes of sedative hypnotics
1. barbituates
2. benzodiazepine receptor ligands
3. older sedative-hypnotics
4. serotonergic agents
5. OTC sleep aids
6. GHB/sodium oxybate
Where do barbituates work?
bind barbituate site on GABA-A receptor --> allosteric enhancement of GABA --> inc duration of GABA induced Cl channel opening
Where do barbituates work at higher doses?
directly activate GABA-A receptors
inhibit AMPA receptor
What is the barbituate dose dependent continuum of CNS depression?
sedation -> sleep -> coma -> anesthesia -> death
Barbituates...
Do/do not induce phsyiologic sleep?
High/low therapeutic index?
Do/do not have drug interactions?
Do/do not cause abuse and addiction?
Do not
low
significant drug interactions
yes to abuse and addiction
Mechanism of barbituate tolerance?
1. pharmacokinetic- induces CYP450
2. pharmacodynamic- neurons less sensitive and have cross tolerance to other CNS depressants
What happens with barbituate withdrawal?
1-2 nights rebound insomnia --> life threatening CNS excitation --> seizures --> coma --> death
When do you use long acting barbituates?
daytime, antiseizure
When do you use intermediate acting barbituates?
hypnotic, preoperative sedative, emergency management of seizures
When do you use short acting barbituates?
induction or maintenance of anesthesia
mephobarbital
long acting barbituate
10-70 hrs
phenobarbital
long acting barbituate
80-120 hrs
also used for hypnosedative withdrawal
amobarbital
intermediate acting barbituate
10-40 hrs
secobarbital
intermediate acting barbituate
15-40 hrs
pentobarbital
intermediate acting barbituate
15-50 hrs
thiopental
short acting barbituate
8-10 hrs
methohexital
short acting barbituate
3-5 hrs
Are barbituates used as anxiolytics?
no
still used as hypnotics and antiseizure agents in limited settings
How are barbituates metabolized?
metabolism/conjugation in liver --> renal excretion

short acting- highly lipophyllic--> terminated by redistribution from CNS into muscle and fat
When are older sedative-hypnotics used?
rarely, but still in some institutionalized patients
Which older sedative-hypnotic is similar to benzodiazepines (with greater abuse) instead of barbituates
meprobamate
How do they work?
bind benzodiazepine site on GABA-A receptor --> allosteric enhancement of GABA --> inc FREQUENCY of cl channel openings
chloral hydrate
older sedative-hypnotic
ethchlorvynol
older sedative-hypnotic
paraldehyde
older sedative-hypnotic
methyprylon
older sedative-hypnotic
ethinamate
older sedative-hypnotic
glutethimide
older sedative-hypnotic
meprobamate
(mep-ro-ba'-mate)
older sedative-hypnotic
Name two serotonergic agents
buspirone (byoo-SPY-rone)- partial 5-HT1A agonist
and
SSRIs
Name three uses of serotonergic agents?
1. anxiety
2. depression
3. many other psych ds
3 advantages of serotonergic agents over benzodiazepines
safer
less psychomotor impairement
less abuse potential
4 disadvantages of buspirone
weak anxiolytic
dizziness
headache
nausea
4 disadvantages of SSRIs
slow onset
non-responders to anxiolytic effects
sexual dysfunction
sleep disturbances
Name 3 OTC sleep aids
antihistamines
melatonin
valerian
What's wrong with antihistamines as sleep aids
rapid tolerance
inadequate dosages
pradoxical stimulation
residual daytime sedation
Where is melatonin made?
pineal gland, controlled by light
What does melatonin do?
lightens skin pigment
suppresses ovarian function
sold to reduce jet lag/promote sleep
What exactly is valerian
dietary supplement from valerian plant- used forever to treat sleep disorders but no convincing clinical data
doxylamine
antihistamine
diphenhydramine
antihistamine
pyrilamine
antihistamine
Mechanism of action of GHB/sodium oxybate
metabolite of GABA --> CNS depressants
Why is GHB a schedule I controlled substance?
addictive, abused for euphoric/hallucinogenic properties, now more popular than rohypnol as a date rape drug
When is sodium oxybate a schedule III controlled substance?
when it is used as prescribed for tx of cataplexy in patients with narcolepsy
Adverse effects of GHB/sodium oxybate when abused?
amnesia
vomiting
respiratory and cardiovascular depression
LOC
seizures
death
Adverse effects of GHB/sodium oxybate when used as prescribed?
confusion
headacthe
nausea
vomiting
dizziness
urinary incontinence
When are spasmolytics used?
tx sk mm spasms from MS, ALS, spinal cord transection, CP, stroke or local muscle trauma
Which two benzodiazepines are spasmolytic?
What is their adverse effect?
diazepam
clonazepam

sedation
Baclofen
spasmolytic
baclofen mechanism of action
GABA-B agonist
- inc K perm, dec Ca influx --> dec transmitter release
tizanidine
spasmolytic
tizanidine mechanism of action
central alpha-2 adrenergic agonist
inc pre and post-synaptic inhibition of motor neurons
dantrolene
spasmolytic
dantrolene mechanism of action
direct action of sk mm --> dec Ca release from sarcoplasmic reticulum --> inhibits excitation/contraction coupling
other uses for dantrolene
malignant hyperthermia
Name four reasons why benzodiazepines positive modulators have replaced barbituates and older agents as sedative hypnotics?
1. higher Therapeutic index
2. lower toxicity w/ overdose
3. fewer sleep pattern alterations
4. dec. tolerance and abuse
Do benzodiazepine positive modulators work in the absence of GABA?
no
Are benzodiazepine positive modulators general CNS depressants?
no
continuum is sedation --> sleep
Why should patients on benzodiazepine modulators not take alcohol>
even though respiratory and CV function depression is rare with overdose, depressant actions are additive with other CNS depressants
alprazolam
(xanax)
benzodiazepine for anxiety (short acting)
chlordiazepoxide
benzodiazepine for anxiety, alcohol withdrawal, preanesthetic
(short acting)
clonazepam
benzodiazepine for seizures, mania, movement disorders
(intermediate)
clorazepate
benzodiazepine for anxiety and seizures
(very short)
PRODRUG
diazepam
(valium)
benzodiazepine for anxiety, status epilepticus, muscle relaxant, preanesthetic
(long)
estazolam
benzodiazepine for insomnia
(short)
flurazepam
benzodiazepine for insomnia
(very long)
lorazepam
benzodiazepine for anxiety, status epilepticus, preanesthetic
midazolam
benzodiazepine for preanesthetic and intraoperative medication
oxazepam
benzodiazepine for anxiety
(short)
quazepam
benzodiazepine for insomnia
(long)
temazapam
benzodiazepine for insomnia
(short)
triazolam
benzodiazepine for insomnia
(short)
Common benzodiazepine drug interaction?
Cyp450 3A4 inhibitors
What is the metabolism of benzodiazepines
first go to high perfusion areas (bain) than to lower areas (mm, fat)
--> metabolized in liver to other active metabolites
adverse effects of benzodiazepines
1. alters sleep patterns
2. impaired mental/motor function, ataxia, daytime sedation, anterograde amnesia, additive with other CNS depressants
3. Abrupt withrdawal can cause anxiety, nausea, seizures
4. Abuse- flunitrazepam as date rape drug
advantages of non-benzodiazepine modulators?
no anxiolytic, mm relaxant, antiseizure properties, no rebound insomnia or other withdrawal sx
(Blind to BZ)
zolpidem
(ambien)
non-benzodiazepine modulator
for use as hypnotic, maintain nl sleep patterns
zaleplon
(sonata)
non-benzodiazepine modulator
for use as hypnotic, maintain nl sleep patterns
adverse effects of non-benzodiazepine modulators?
abuse potential like benzodiazepines
morning sedation w/ late night use of zolpidem
flumazenil
competitive benzodiazepine site antagonist for decreasede recovery time from benzodiazepine modulators
flumazenil fast or slow acting? fast or slow metabolism?
rapid onset, short half life
Adverse effects of flumazenil
agitation, confusion, dizziness, nausea
inc risk of seizures/other withdrawal sx in patients with benzodiazepine tolerance or barbituate, tricyclic antidepressant overdose