Anxiolytics and Hypnotics Flashcards
Anxiety disorders types
Panic disorders
Phobias
Social anxiety disorder
Generalised anxiety disorder
Stress disorder
PTSD
OCD symptoms
Thoughts a terrible event will occur, need for perfection with repetitive ritualistic behaviour
Sleep disorder types
Insomnia:
transient - noise/shift work/jet lag
Intermediate - illness/emotional episode
Chronic - psychiatric disorder
Anxiety and stress disorder treatments aim to
increase inhibition in limbic system as these are associated with increased glutamatergic activity
BDZ MOA
Binds to BDZ receptor on GABA-A receptors, potentiates GABA action and more chloride passing through
BDZ SE
Drowsiness Agitation Ataxia Addiction Interact with depressants
BDZ uses
Short term anxiety e.g. bereavement
Sedation/amnesia so traumatic awake surgical procedures
BDZ antagonist
Flumazenil short duration of action, used to reverse benzo activity
Midazolam duration and uses
4 hr
Amnesic, pre-med surgery e.g. endoscopy
Lorazepam, oxazepam, temazepam duration and uses
15 hr
Anxiolytic, hypnotic
Alprazolam, nitrazepam duration and uses
24 hr
Anxiolytic, panic attacks
Chlordiazepoxide, diazepam duration and uses
48 hr
Anxiolytic, muscle relaxant
Diazepam is anticonvulsant
Clonazepam, Flurazepam duration and uses
60 hr
Anticonvulsant, anxiolytic
flunitrazepam use
Roofies, rohypnol
Z drugs use
Zolpidem, zopiclone, zaleplon and eszopiclone preferred as hypnotics
Pagoclone, suproclone used as anxiolytic
Z drugs MOA
Zolpidem, zopiclone, zaleplon act at BDZ binding site but not BDZ
Natural anxiolytics
Neurosteroids derived from progesterone/corticosterone such as allopregnanolone made in neurones and GABA cells
Diazepam binding inhibitor protein, binds at BDZ site in thalamic reticular nucleus
Serotonergic system and anxiety
5HT1A receptors are inhibitory auto receptors, when activated reduces 5HT and increases anxiety
Buspirone treatment MOA
Partial 5HT1A agonist, acutely causes less 5HT release but eventually desensitises receptors and lots of 5HT released after a few weeks
Beta blockers MOA
Propranolol reduces physical manifestations of anxiety e.g. sweating, tremor, tachycardia by blocking beta-2
Anti-depressants used in anxiety
SSRIs (fluoxetine, paroxetine) and SNRIs (venlafaxine, duloxetine) used in GAD, SAD, PTSD, phobias
Anti-convulsants used in anxiety
Ca channel blockers (gabapentin, pregabalin), GABA uptake blocker (tiagabine) and GABA metaboliser (valproate) used for GAD
Anti-psychotics used in anxiety
D2 antagonist (olazapine, linked to Gi so inhibits adenylate cyclase) and risperidone used for GAD, PTSD
Chlormethiazole use
Hypnotic which potentiates GABA receptors, used for elderly as no hangover effect which could cause confusion/falls
Is a barbiturate
Advice for hypnotic use
short term treatment preferred
tolerance develops over 2 weeks
withdrawal over a few weeks, rebound insomnia, vivid dreams
Barbiturates MOA
Thiopental, amylobarbitone, secobarbital, butobarbital, phenobarbitone, clomethiazole acts via GABA-A receptor even in absence of GABA
Barbiturates use
no longer used, except sometimes as anticonvulsants (phenobarbital) and even more rarely as anaesthetic (thiopental)
Barbiturates SE
Resp depression
Easy to OD so natural antagonists
Dependence
Meprobamate use
No longer used as less potent than BDZ but more toxic
Non-prescription anxiolytics/sedatives
Antihistamines (diphenhydramine, promethazine)
Valarian extract potentiates GABA receptor function
