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31 Cards in this Set
- Front
- Back
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Benzodiazepines
Mech |
inc frequency of GABA stimulated cl channel opening
bind to site between alpha and gamma subunits; GABA bines site between alpha and beta hyperpolerize cell - shift response curve to left |
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Benzodiazepines
Indications ANXIETY 6 |
1. anxiety - ssri and snri and propanolol also used - SHORT TERM
panic disorder - alprazolam |
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Alprazolam
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panic disorder
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diazepam
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muscle relax
status epileticus (with lorazepam) and toxin induced seizures withdrawal symptoms (with Chlrodiazepoxide) |
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Benzodiazepines
Pharmaco |
rapidly and completely absorbed
Clorazepate - first decarboxylated in gastric juice to active metabolite |
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Benzodiazepines
Pharmaco Duration |
highly lipid soluble; rapid distribution
duration depends on rate of biotrans |
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Benzodiazepines
Pharmaco Biotransformation |
1. n-dealkylation
2. aliphatic hydroxylation (CYP3A4) 3. conjugation |
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Benzodiazepines
Pharmaco N-dealkylation |
leads to long acting half life of metabolite
desmethyldiazepam (50 hr) |
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Benzodiazepines
Side E |
sedation, drowsiness, ataxia, confusion
anterograde amnesia COPD worsening |
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Benzodiazepines
Tolerance |
occurs and cross-tol with other sedative and alcohol
abuse potential low withdrawal - severe anxiety and insomnia |
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Benzodiazepines
Drug interactions |
CNS depressant - can be deadly with alcohol
Cimetidine - CYP3A4 inhibitor grapefruit juice |
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Benzodiazepines
Buspirone Mech |
nonBZ that acts on BZ receptor.
5HT1a partial agonist |
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Benzodiazepines
Buspirone Indication |
chronic generalized anxiety disorder
no sedation hypnosis or dependance |
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Benzodiazepines
Buspirone Side E |
nervousness, restlessness
tachycardia, GI |
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Benzodiazepines
Buspirone Pharmaco |
slow onset of action (week), limits use to treatment
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Benzodiazepines
Zolpiden, Zaleplon Mech |
nonBZ
inc Cl conductance stimulated by GABA by binding to GABA receptor with alpha1 subunit |
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Benzodiazepines
Zolpiden, Zaleplon Pharmaco |
metab by CYP3A4
rapid onset and short duration |
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Benzodiazepines
Zolpiden, Zaleplon Indications |
short term treatment of insomnia
littlle m. relaxation/anticonvulant minimal tolerane and dependance less amnesia/sedation |
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Benzodiazepines
Flumazenil Mech |
BZ receptor antag
competitive |
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Benzodiazepines
Flumazenil indications |
BZ overdose or to speed recovery from anesthetics
frequent admin b.c short half life can have withdrawal symptoms |
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Sedatives for nonselective, dose dependant CNS depression
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barbituates
phenobarbital - anticonvulsant thiopental - anesthesia |
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Sedatives for nonselective, dose dependant CNS depression
barbituates Mech - low dose |
los doses - prolong GABA induced opening of cl channels; leading to enhanced GABA inhib activity
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Sedatives for nonselective, dose dependant CNS depression
barbituates Mech - high dose |
higher dose direction action on GABA receptor (open channel ind of GABA)
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Benzos
Indications Insomnia |
2. insomnia
lorazepam and triazolam for induction and ramelton temazepam and flurazepam for maintenance |
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Benzos
Indications Others 5 |
3. status epilepticus/seizure
4. muscle relaxation 5. preanesthetic amnesea 6. dependance 7. acute mania/bipolar |
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Benzos
Ramelton Mech |
antag at MT1/MT2 in brain
no GABA receptor effect |
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Benzos
Ramelton Action |
help falling asleep
antag. MT1/MT2 in brain no GABA-R effect |
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Benzos
Pharmaco Shorter action b.c conjugation of drug only |
lorazepam and triazolam
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Physical Dependance/Withdrawal
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Chlrodiazepoxide
Diazepam |
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Status epileticus
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Lorazepam
Diazepam |
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Preanesthetic
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midazolam
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