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123 Cards in this Set

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A mixed opiod which at first was thought to be non-addictive, but now is a controlled substance
Talwin (Pentazocine)
Talwin is a _ receptor agonist,
and a _ receptor antagonist
k, mu
0.3 mg of this drug is equivalent to 10 mg or morphine; it must be administered parenterally
Buprenorphine, (Buprenex)
30-60 mg of this drug are equivalent to 10 mg of morphine
Talwin NX
number of mg to achieve desired effect
potency
degree of effect achieved by a drug
efficacy
respiratory depression in mixed opiods differs from true opiods in that
it is not directly proportional to the dose which is administered (reaches a plateau)
dose of morphine where you begin to see respiratory depression
20-30 mg
Pentazocine and Naloxone
Talwin NX
receptor which affects resp. depression
mu
receptor which affects degree of analgesia
k
initally, __ were used as sedatives in the treatment of anxiety
barbiturates
decrease activity, moderate excitement and calms
sedatives
produces drowsiness and facilitates onset and maintenance of sleep
hypnotics
ideally would induce sleep rapidly, increase sleep time and give the patient a sense of well-being with low ADRs
hypnotics
all benzodiazepines have __ effects
sleep-inducing
not all benzodiazepines are ideal __
hypnotics
Flurazpam, Temasepam, Triazolam are
hypnotics
Ambien and Sonatal are
hypnotics
may induce REM rebound on w/d
benzodiazepines
Provides insight into neural activity associated with different phases of sleep
EEG
Appears similar in some ways to wakefulness
REM
Alpha waves – 8-12 Hz
Drowsiness
Frequency of a-waves
8-12 Hz
Theta waves – 3-7 Hz
Stage 1 sleep
Frequency of Theta waves
3-7 Hz
Sleep spindles and K complexes – 12-14 Hz
Stage 2 sleep
Frequency of Sleep spindles and K complexes
12-14 Hz
Delta waves – 0.5-2 Hz
Deep sleep
Frequency of Delta waves
0.5-2 Hz
Low voltage fast
REM sleep and wakefulness
Release is increased in REM sleep
ACh
parasympathetic tone refers to the way
ACh enhances sleep
May help entrain circadian rhythm
ACh
Drowsiness associated with this action on this receptor
H1 antagonists
chemical important for wakefulness
Histamine
promotes sleep through regulation of activity in midbrain cholinergic pathways
Adenosine
inhibits adenosine receptor activity, promoting wakefulness
Caffeine
Decreases sleep through inhibition of reticular activating system
Seratonin
prevent sleep, yet produce REM-like symptoms
5-HT2 agonists
Locus coeruleus activation is associated with
wakefulness
Sleep deprivation associated with increased risk of
psychiatric illness
Insomnia affects 25-30% of population and most prevalent in the
elderly
The effects of insomnia are serious in % of the population
17
Individuals with less than 6 hours of sleep per night have a % higher mortality rate
70
sleep > 50 % of time
Newborns
occupies roughly 50 % of sleep time
REM sleep
Sleep levels are especially low in the
elderly
Involuntary muscle contractions
Myoclonus
Flurazepam
Dalmane
Temazepam
Restoril
Triazolam
Halcion
Quazepam
Dorval
Estazolam
ProSom
Zolpidem
Ambien
Zaleplon
Sonatal
Shorten slow wave (deep) sleep, REM cycle
hypnotics
Increase total sleep time (stage 2)
hypnotics
Increase number of REM cycles (total REM increases)
hypnotics
May induce REM rebound on withdrawal
hypnotics
Gives sense of deep, refreshing sleep
with a decrease in sleep latency
hypnotics
increase chloride (Cl-) conductance through interaction with GABAA receptors
Benzodiazepines
GABAa receptors are of this type
ligand gated Cl- channels
Benzodiazepines __ cells, thereby reducing neuronal activity
hyperpolarize
__ is complete for most benzodiazepines (except flurazepam and zaleplon)
Systemic absorption
Estazolam should be administered
1-2 hours before bedtime
Highly lipophilic, resulting in high CNS penetration
benzodiazepines
Extensive (>90%) binding to plasma proteins
benzodiazepines
benzodiazepines cross placenta during pregnancywhich means they
are secreted in milk
OHylation at position 3 yields
active compounds
N-desalkylation yields
active compounds
Hydroxylation of a-methyl groups on fused rings results in
active compounds
Dependent on hydroxylation
Glucuronidation
Conjugation with glucuronic acid
Glucuronidation
Glucuronidation results in
inactive metabolites
Flurazepam is metabolized to
N-desalkyl derivative
Desalkylflurazepam accumulates with
repetitive dosing
Half-life longer in elderly (especially men)
Flurazepam
Flurazepam is subject to hydroxylation here
3-position
Metabolite of flurazepam, has a half-life of ~80 hours
N-Desalkylflurazepam
Sustained effect even after discontinuation; hangover effect after initial doses
N-Desalkylflurazepam
No daytime anxiety; daytime somnolence
N-Desalkylflurazepam
Already hydroxylated in the 3-position;
Glucuronidation results in inactivation
Temazepam
Half-life of 13-14 hours
Temazepam
Quazepam is metabolized to
2-oxo-quazepam
Subject to N-desalkylation, resulting in N-desalkyl-flurazepam
Quazepam AND Flurazepam
Net effects similar to N-desalkyl-flurazepam
Quazepam
Metabolized by a-hydroxylation and by 3-hydroxylation then rapid glucuronidation of both hydroxyl groups results in inactivation
Triazolam
Short half-life (1 – 1.5 hours)
Triazolam
Implications of short half-life
Potential for rebound insomnia and daytime anxiety
Estazolam is oxidized to
1-oxoestazolam
Half-life (10 – 24 hours)
Estazolam
Not benzodiazepines, yet enhance GABAa receptor activity
Zolpidem and Zaleplon
Metabolized by oxidation of methyl groups to carboxylic acids
Zolpidem
Zaleplon is metabolized by oxidation to
5-oxo-zaleplon
Minor oxidation pathway through CYP3A4, resulting in desethylation
Zaleplon
Oxidation of most benzodiazepines is inhibited by
cimetidine
do not induce or inhibit mixed function oxidases
Benzodiazepines
Although NOT a benzodiazepine, oxidation of Zaleplon also is inhibited by cimetidine since
cimetidine inhibits aldehyde oxidase
a dopamine agonist which induces n/v
apomorphine
Benzodiazepines have __ abuse potential
low
Headache, irritability, dizziness, abnormal sleep are
w/d sx from benzodiazepines
Rebound insomnia is associated with this benzodiazepine
Triazolam
Benzodiazepines, in combination with __ can be fatal
alcohol
a benzodiazepine antagonist that can be used to block adverse effects of benzodiazepines
Flumazenil
Stomach pump, charcoal, hemodialysis are all ways to treat
benzodiazepine toxicity
drug of choice for the treatment of insomnia
Benzodiazepines
This benzodiazepine can be used for up to one month with little tolerance
Flurazepam
This benzodiazepine can be used for up to three months with little tolerance
Temazepam
Benzodiazepines should be used for no longer than
3 – 6 months
use recommended for benzodiazepines - (frequency of dose)
Intermittent (every three days)
(e.g., flurazepam) produce sustained sleep, but increased risk of daytime somnolence
Benzodiazepines with long half lives
may be best for patients with difficulty falling asleep
Benzodiazepines with short half lives
May be less effective patients having difficulty maintaining sleep
Benzodiazepines with short half lives
Development of tolerance can produce __ in compounds with with short half lives
rebound insomnia
Levels decline rapidly so withdrawal symptoms are more apparent
Benzodiazepines with short half lives
Shortens sleep latency and prolongs sleep time with low abuse potential
Zolpidem
Less likely to produce w/d symptoms than benzodiazepines;
Rebound insomnia after first night of w/d, but soon resolves
Zolpidem
This hypnotic is often prescribed for patients with insomnia
Alprazolam (Xanax®)
Adaptive response to repeated administration of drugs
Tolerance
Repeated doses have diminishing effects and mMore drug required to produce the same effect
Tolerance
Presence of drug required for normal function
Dependance
Usually manifested by emergence of withdrawal symptoms following discontinuation of drug
Dependance