Term
Barbiturates
What neurons of the CNS does it affect and how?
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Definition
Barbiturates are allosteric agonists of GABA-A neurons
When barbituate is bound, GABA binding will cause the Cl channel to remain open for longer (barbiDURATEs = longer duration) ---> causes increased hyperpolarization, thus decreased neuronal firing
(but at higher doses, GABA is not needed to open the channel)
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Term
Original clinical indications? (3)
What are 6 reasons that barbituates are no longer used to treat anxiety?
How to treat barbiturate OD?
What are 3 medical uses of barbiturates today? |
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Definition
Original Indications: Sedative for
Anxiety
Seizures
Insomnia
Adverse affects:
1. Causes CNS depression
2. decreases respiratory drive
(both additive effects w/ EtOH, which also binds GABA-A receptors)
3. Low therapeutic index
4. Has high abuse potential
5. Overdose/suicide risk
6. Drug interactions, increases cytochrome p450 activity
Must simply manage the symptoms of a barbiturate OD (assist respiration, increase BP)
Current uses:
1. to induce anesthesia
2. anticonvulsant
3. In some pain meds |
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Term
| Benzodiasepines: Balancing Potency and Half-Life |
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Definition
If you're using the benzo to treat insomnia, you want it to last thru the night, so you want a longer half-life (sacrifice speed/potency)
If you're using benzo to treat panic attacks, you prefer something that works quickly and leaves the system quickly (Alprazolam, aka Xanax) |
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Term
| Glucuronidated Benzodiazepines; how are they diff than regular benzo? |
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Definition
| glucuronidated version avoid phase I metabolism, which is safer for patients w/ impaired liver function |
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Term
Benzodiazepine receptor agonists
Give an example
What are 2 specific receptors they act on? Effects?
Are these any better than just straight benzo?
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Definition
Zolpidem (Ambien) -- can cause amnesia if not allowed a full night's sleep
Benzo receptor 1 found in cortex and cerebellum, agonist causes sedation
Benzo R 2 found in striatum, hippcampus, and spinal cord - agonists cause anxiolysis and muscle relaxation
The increases specificity provided by the benzo receptor agonists may increase the safety of the drug:
less OD risk
less addiction potential
less withdrawal symptoms |
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Term
Anxiolytics: Buspirone
What is it?
How does it compare to benzo?
Drawbacks?
Indication? |
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Definition
Its a Serotonin 1A receptor partial agonist (Not at all structurally related to benzo)
- nonsedating
- no abuse potential, no tolerance or withdrawal
Has no immediate effects, takes 2-4 weeks (benzo takes 1-2 weeks)
Indicated for treatment of GAD
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Term
Anxiolytics: Buspirone
Side effects? (4)
Any condraindications? |
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Definition
Side effects:
Dizziness
drowsiness
headaches
nausea
Well tolerated and few drug interactions, just dont mix w/ MAOI's |
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