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63 Cards in this Set
- Front
- Back
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How does GABA work?
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GABA is an inhibitory neurotransmitter. When GABA binds to its site, the proteins change shape,the channel opens and chloride rushes in.
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what happens to the membrane potential when chloride rushes?
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it is lowered (from -90 to -150) and therefore more stimulation is needed in order for it to fire.
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by binding to a site on the GABA complex, benzos/barbs/ETOH/neurosteroids facilitate teh binding of GABA itself. What is this called?
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allosteric modulation
potentiation |
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barbituates have two M of A
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1. facilitate the actions of GABA
2. activate the GABAa receptor directly |
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general clinical uses of barbituates
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-induction of anesthesia
-epilepsy |
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barbiturates are classified according to
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-rate of onset
-duration of action |
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barbituate rate of distribution depends on
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lipid solubility
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barbituate metabolism is altered by
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induction of hepatic enzymes
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one interesting thing about barbituates is their duration and half lives are _______
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very different
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one interesting thing about barbituate metabolism in the liver is
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they enhance their own metabolism
"metabolic tolerance" |
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name 3 ultrashort barbs
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1. thiopental
2. thiamylal 3. methylhexital |
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thiopental onset of action
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5-8 mins.
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thiopental half life
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12 hours
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name 2 intermediate acting barbs
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1. secobarbital
2. pentobarbital |
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dangers of intermediate acting barbs
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-they open the chloride channel by itself therefore having a very narrow therapeutic index
-not really used anymore |
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name one long acting barb
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phenobarbital
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phenobarbital half life
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80-120 hrs
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phenobarb withdrawal symptoms looks like
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the opposite of the medication effect. That's why CNS depressant withdrawals are so DEADLY they can cause seizures.
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adverse effects barbs
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-sedation
-resp. depression -tolerance -dependence -abuse |
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drug interactions barbs
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other CNS depressants can have an additive effect (1+1=5)
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Benzodiazepine M of A
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1. binds to a specific site on GABAa (like barbs)
2. facilitates the actions of GABA (like barbs) 3. DOES NOT activate GABAa receptor directly (unlike barbs) |
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the fact that benzos do not activate the GABAa receptor directly makes them
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SAFER:
-you are not likely to die of resp. depression from a benzo. you would more likely die of starvation! |
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benzo clinical uses
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-anxiolytic
-sedative -muscle relaxant -anticonvulsant -anesthesia induction |
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adverse effects of benzos
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-sedation
-anterograde amnesia -resp. depression -tolerance -dependence -abuse |
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are withdrawals of benzos life threatening like for the barbs?
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YES.
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How much benzo does a pt have to take before they are dependent?
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even at therapeutic doses/levels
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do you have additive effects with benzos and other CNS depressants?
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YES
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benzos are also commonly given for
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alcohol withdrawal
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can you treat an overdose of phenobarb?
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no
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can you treat an overdose of benzo?
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yes
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benzo overdose treatment
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Flumazenil
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2 types of anxiety disorder
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1. Generalized Anxiety Disorder
2. Panic Disorder |
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4 treatment categories of anxiety disorders
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1. benzos
2. buspirone 3. antidepressants 4. beta blockers |
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the only benzo marketed for panic disorder
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alprazolam (xanax)
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buspirone M of A
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5HT 1a agonist
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How much benzo does a pt have to take before they are dependent?
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even at therapeutic doses/levels
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do you have additive effects with benzos and other CNS depressants?
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YES
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benzos are also commonly given for
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alcohol withdrawal
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can you treat an overdose of phenobarb?
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no
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can you treat an overdose of benzo?
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yes
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benzo overdose treatment
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Flumazenil
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2 types of anxiety disorder
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1. Generalized Anxiety Disorder
2. Panic Disorder |
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4 treatment categories of anxiety disorders
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1. benzos
2. buspirone 3. antidepressants 4. beta blockers |
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the only benzo marketed for panic disorder
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alprazolam (xanax)
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buspirone M of A
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5HT 1a agonist
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does buspirone relieve anxiety immediately?
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no has a long latency to obtain antianxiety effects.
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buspirone is generally used to treat
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mild anxiety disorder
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is buspirone used to treat panic disorder?
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no is not quick acting.
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adverse effects of buspirone
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-headache
-dizziness -nausea |
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what is the first choice for treatment of panic disorder?
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the Antidepressants:
1. SSRIs 2. tricyclics 3. MAOIs |
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beta blockers are used to treat
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performance anxiety
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what is the general first choice to treat anxiety?
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benzos
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5 causes of insomnia
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1. stress
2. aging 3. medical/psychiatric illness 4. drugs/alcohol 5. jet lag/sleep cycle disruption |
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5 treatment categories for insomnia
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1. benzos
2. non benzos ("z" drugs) 3. chloral hydrate 4. antidepressants 5. antihistamines |
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3 benzos used to treat insomnia
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1. triazolam
2. flurazepam 3. temazepam |
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are all of the benzos used to treat insomnia short acting?
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no, the only short acting one is triazolam with a half life of 3 hours
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nonbenzo M of A
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they bind to the Type 1 benzo binding site, so they have a benzo mech of action!
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the nonbenzos are known as being more _________
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selective (reduced muscle relaxation, reduced amnesia, etc.) They bind selectively to the Benzo 1 site.
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name 3 nonbenzos
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1. zolpidem
2. zaleplon 3. eszopiclone |
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what is the active ingredient in chloral hydrate?
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alcohol
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adverse effects of chloral hydrate?
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-cancer causing metabolite
-unstable kinetics (zero order) -NO ANTAGONIST |
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should we use chloral hydrate anymore?
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no, use versed instead
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example of an antihistamine used to treat insomnia
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hydroxyzine
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