Anti-anxiety Flashcards
What class of drugs treats anxiety?
Benzodiazapines (BNZ).. Use the long acting ones
MOA of benzos?
Allosteric GABA agonist; requires endogenous GABA ligand (does not directly activate receptor)
Where do benzos bind on the GABA receptor?
Unique site from flumanezil (competitive antagonist) and GABA (endogenous agonist –> Cl- influx = polarization)
All benzos (except which ones) are metabolized to what?
Nordiazepam (long half life)
-except: Alprazolam, Lorazepam, Oxazepam (rapidly eliminated in urine)
what are the long duration benzos?
Chlordiazepoxide, Clorazepate, Prazepam, Diazepam, Flurazepam
*Clor’s + PDF
Rapid onset?
Clorazepate & Diazepam
Slow onset?
Oxazepam & Prazepam
ADEs of benzos?
Sedation, Teratogen, Tolerance, Dependence
Describe the sedation ADE of benzos?
can lead to respiratory depression; esp in combo w/ other drugs/alcohol in elderly
Describe the tolerance ADE of benzos?
Tolerance develops to sedativeness > anticonvulsant»_space;»> rarely ever to anxiolytic
Mechanism of tolerance?
- Receptor uncoupling
- Receptor-subunit down regulation
- Sensitization of glutamatergic system
- Cross talks b/t other G-protein receptor systems
Dependence is worse with short or long acting drugs?
Short.. must taper
Withdrawal symptoms?
Autonomic: tremor, sweating, insomnia, abdominal discomfort, tachycardia, HTN, muscle twitching
Which benzo is a muscle relaxant?
Diazepam
Clinical uses of benzos? (4)
- Anxiety
- Panic attacks (Alprazolam)
- Muscle relaxant (Diazepam)
- Alcohol withdrawal (Chlordiazepoxide, Lorazepam)
