anxiolytics Flashcards
uses of low/high/even higher doses of Benzodiazepines and Barbiturates
low dose –> anxiolytic, sedation
high dose –> hypnotic
even higher dose –> anesthesia
what is 1 similarity and 1 difference btw benzodiazepines and barbiturates
similarity: bind to GABA –> so GABA can bind better to Cl-
- -> potentiate GABA-mediated Cl channel –> Cl- can come in more –> m is hyperpolarised, harder to depolarise –> decrease neural excitability
but both bind at different site
list some benzodiazepines
diazepam (long acting)
Alprazolam (xanax)
clonazepam
lorazepam
midazolam, triazolam (short acting: for anesthetic)
list uses of diazepam
sedation, anxiolytics, hypnotic, anti-epileptic, anesthetics
SE of BZD
1. abuse, tolerance (if use more frequently esp for epilepsy bzd (those bzd has longer t1/2 than sleeping bzd also)) and dependence (withdrawal: rebound anxiety, rebound insomnia, tremour and may even go into fits) -> withdraw gradually*
- overdose: resp depression (esp with alcohol)
- GA: sedation, amnesia, confusion
- impair muscle co-ordination*
Important counselling point for BZD
- dont take with alcohol –> higher risk of overdose –> higher risk of severe resp depression
- taper slowly to reduce withdrawal sx (rebound anxiety, rebound insomnia, tremor, convulsion)
- dont operate machinery as this medication impair manual skills
barbiturates
SE
higher risk of developing dependence (more severe withdrawal sx) and tolerance than BZD
- overdose –> resp collapse, fatal
- high dose will be anesthetic
What is the use flumazenil?
BZD antagonist to reverse overdosing of BZD.
not for barbiturates bc flumazenil bind at a site different from BZD.
list some barbiturates
(ultra short DOA: in IV induction of anesthetic)
thiopental
(short DOA: anxiolytic, sedative, hypnotic)
amobarbital
pentobarbital
(long DOA: in anti epileptic)
phenobarbital
Propanolol
hydroxyzine
propanolol can decrease physical szx associated with anxiety (e.g. tachycardia) –> treat social phobias, performance anxiety
Hydroxyzine: help with itching, anti-histamine, serotonergic and a-adrenergic activity
other anxiolytic
TCA, SSRI, NASSA, SNRI
TCA: clonipramine
SSRI: fluoxetine, citalopram, sertaline, paroxetine
SNRI: venlafaxine, duloxetine
NASSA: mirtazapine
what is pregabalin
GABA analogue –> cause more GABA to be released –> trigger Cl- channel to open more –> hyperpolarisation
uses of pregabalin
for generalised anxiety disorder
adjunct for partial epileptic
SE of pregabalin
suicidal thoughts
sedation
Buspirone
MOA
Uses
MOA: 5-HT1 receptor partial agonist and bind to dopamine receptor
Use: for generalized anxiety disorder, lack anti-epileptic and muscle relaxant properties.