Anti-anxiety Flashcards
GABA receptor :
Barbituates
Rxs
Phenobarbital
Melatonin congener
Ramelteon ROZEREM
5-HT1a receptor agonist
(a1, a2, D2)
Rx
Non-sedative anxiolytic:
*Buspirone BUSPAR
Sedative hypnotics
Graded-dose response
Low dose - anxiolytic sedative
High dose - sleep/hypnosis
Benzos vs older (alcohol, barbituates, chloral hydrate)
Benzos = safer
Older - linear dose response curve
Anxiety Tx
Panic disorder
Antidepressants
Alprazolam XANAX
Anxiety Tx
Agoraphobia
Alprazolam, XANAX
ADDs
Sedative drugs
- **BARBITUATES
- **BENZODIAZEPINES
- Antipsycs
- Antidepressants
- Antihistimines
GABAa Receptor
- major inhibitory neurotrans in brain
* binding sites vary among drugs, some different from GABA site
Barbituates
Rx
Phenobarbital
Schedule III/IV
*many are sched II
ABUSE POTENTIAL FOR ALL
Barbituates + older
Mechanism
Up DURATION Gaba -mediated Cl flux
- neuronal inhbition
- at higher concentrations - DIRECTLY OPEN Gaba a Cl channel
Barbituates + older
Absorption
Phenobarb - longer
Barbituates + older
S.E.
High dose - CNS /respiratory depression
*Low T.E. - OD
Bartituates + older
Drug interactions
*+ ETOH = CNS depression
- INDUCE Cyp enzymes
- Dependence, addiction
Barbituates + Older sedatives
Uses
- rarely used today
- Anesthesia
- seizures = Phenobarbital
Anxiety Tx
Social phobia
Clonazepam KLONOPIN
ADDs, B-blockers
Anxiety Tx
Generalized Anxiety Disorder
1st line - ADD
- Buspirone BUSPAR
- Benzos = short-term relief
Axiolytic
CUT ANXIETY
*not all anxiolytics are sedatives, treated w/ non-sedatives
Sedative-hypnotics
- CNS depressants
- sedative = calming effect
- ideally - minimal effect on motor function or mental status
- some hypnotics are NOT sedative
Benzos
Rx list
- Alprazolam XANAX
- Clonazepam KLONOPIN
- Diazepam VALIUM
- Midazolam VERSED
- Triazolam HALCION
- Rohypnol - date rape drug
Benzos
Receptor mechanism
Bind to Gaba a
Facilitate GABA Cl influx
NO DIRECT OPENING - need GABA present
Benzos
Full agonists
NOT DIRECT, NEED GABA
Diazepam VALIUM
Alprazolam XANAX
Zolpidem AMBIEN
Benzos
Inverse agonist
INHIBIT GABA OPENING
Experimental drugs
-induce anxiety, seizure
Bezos
Antagonists
Flumazenil
*Compete with full ags (benzo) + hypnotics (zolpidem AMBIEN) + inverse ags
Benzos
CNS effect
Sedation
- higher dose - cognitive impairment
- amnesia
- anticonvulsant - clonazepam KLONOPIN, diazepam VALIUM)
Benzos
MSK effects
Relaxation - high dose
Benzos
Cardio effects
DOWN BP
UP HR