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