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44 Cards in this Set

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  • Back
What is the duration of symptoms required for diagnosing generalized anxiety disorder?
1 month
What are 3 relatively common complications of anxiety disorders?
-Alcohol abuse
-Sedative abuse
-Anti-anxiety med abuse
What is the term Insomnia used to describe?
Disorders of initiating and maintaining sleep.
How many stages of sleep are there, and what is the normal order in which they occur?
1, 2, 3, 4, 3, 2, REM
What stages predominate
-Earlier in the night
-Later in the night
Earlier = 3/4
Later = more REM
What is the amplitude/duration of waves during the Awake state?
-Low amplitude
-Rapid waves
What is the lightest stage of sleep? What amplitude of waves is seen on EEG in this stage?
Stage 1 - REM sleep
-Low amplitude
What happens to the EEG waves' amplitude/speed as sleep progresses through deeper stages?
Amplitude increases
Speed increases
What are Stages 3/4 referred to collectively?
Delta wave sleep
How do drugs treat insomnia?
By normalizing abnormal sleep patterns
What NT is more important in slow wave sleep and NREM?
Serotonin
What NT's are more important in REM sleep?
NE/ACh
So what is Insomnia?
A disorder of initiating and maintaining sleep
What is hypersomnia? What is a common term for it?
Excessive sleep/sleepiness
-Narcolepsy
What type of receptor is the GABA-A receptor?
Ligand gated ion (Cl) channel
What type of receptor is the GABA-B receptor?
A GPCR receptor
What drug targets the GABA-B receptor?
Baclofen
What type of NT is GABA?
An inhibitory neurotransmitter
How is the action of GABA terminated?
1. By active uptake mechanisms
2. By GABA transaminase
What drugs act on the Ligand gated Cl channels that are GABA-A receptors?
Benzodiazepines
Barbiturates
What is the bottom line of the mechanism of Benzodiazepines?
They enhance the effects of GABA at the GABA-A receptor
How do Benzodiazepines enhance the effects of GABA at the GABA-A receptor?
-Increase freq of Cl channel opening
-Increase the amt of binding of GABA to the GABA-A receptor
How do the Benzodiazepines increase the degree of GABA binding to its GABA-A receptor?
Through allosteric interactions between the 2 binding sites on the receptors
How does increased opening of the Cl channel affect the nerve terminals at which GABA receptors are located?
They become hyperpolarized and unable to transmit AP's and excitation.
What drug can reverse the effects of Benzodiazepines?
Flumazenil
What is Flumazenil
A pure antagonist of the benzodiazepine binding site on GABA-A receptors
How do the Barbiturates mechanism of action compare to that of benzodiazepines?
They do not increase the frequency of Cl channel opening, only increase the duration.
How do inverse agonists of Benzodiazepine receptors affect the actions of BDZ's? What effect do they produce
They block the actions of BDZ's and hence produce anxiogenic effects.
Do we know what the endogenous agonist of the bzd receptor is?
No - it could be anxiolytic or anxiogenic.
Why have the benzodiazepines supplanted the barbiturates in being used for treating anxiety and insomnia disorders?
1. Less likely to cause resp depression and death
2. Less addictive
What are the 2 most important pharmacokinetic properties of benzodiazepines?
-Lipophilicity
-Metabolism
What benzodiazepine is very rapidly absorbed from the GI tract? Why?
Diazepam - it is very lipophilic
What else does lipophilicity determine?
Rate of entry into the CNS
What determines the duration of action of a benzodiazepine after a single dose?
The rate of redistribution from the CNS
So what is the duration of action of Diazepam after a SINGLE dose?
Short
Why does Diazepam often have long duration of effects?
Because it is metabolized to an active metabolite with a very long half life, so that it builds up in the bloodstream.
What 2 benzodiazepines do NOT have active metabolites?
-Lorazepam
-Oxazepam
So what is the onset and duration of action of lorazepam after a single dose?
-Slow onset
-Longer duration than a single dose of Diazepam will have
What are 7 important effects of Benzodiazepines to remember?
ASHMAMA
What is ASHMAMA?
Anxiolytic
Sedative
Hypnotic
Muscle relaxation
Anterograde amnesia
Minimal CV/Resp depression
Anticonvulsant
What type of administration most often results in Anterograde amnesia with BDZ's?
IV infusion - during anesthesia
How do the BDZ's produce their Hypnotic effects?
-Decrease sleep latency
-Decrease the # of awakenings
What benzodiazepine is used for its muscle relaxation effects?
Diazepam
pg 7
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