Hypnotics Flashcards
Contraindications for zopiclone
Unstable myasthenia gravis
Severe sleep apnoea
Breastfeeding
Respiratory failure
Side effects of zopiclone
Metallic taste
Heartburn
Lightening of sleep on withdrawal
Mechanism of action of flumazenil
Selective competitive GABA A receptor antagonist
Administration method of flumazenil
IV
Half-life of flumazenil
60 minutes
Agents blocked by flumazenil
Benzodiazepines
Zopiclone
Duration of effect of flumazenil
20-50 minutes
Long acting benzodiazepines
Diazepam
Chlordiazepoxide
Clonazepam
Flurazepam
Short acting benzodiazepines
Lorazepam
Oxazepam
Temazepam
Alprazolam
Very short acting benzodiazepine
Triazolam
Use for triazolam
Used in anaesthesia
Side effect profile of short vs. long acting benzodiazepines
Short acting have more severe withdrawal phenomena, rebound insomnia, and anterograde amnesia
Long acting have more daytime sedation
Z drug which is known for having a hangover effect due to its active metabolites
Zopiclone
Z drug which is used for sleep maintenance rather than sleep initiation issues
Zopiclone
Z drugs which are used for sleep initiation issues rather than maintenance of sleep
Zolpidem
Zaleplon
Absorption of benzodiazepines
Complete
Time to peak concentration of diazepam after a single dose
30-90 minutes
Protein binding of benzodiazepines
70-99%
Impact of benzodiazepines on sleep cycle
Suppress REM sleep
Amnesia which can be caused by benzodiazepines
Anterograde amnesia
Paradoxical reaction seen with benzodiazepine use
Aggressive behaviour Sexual disinhibition Hyperactivity Hostility Vivid dreams
Drug factors increasing the risk of a paradoxical reaction with benzodiazepine use
Benzodiazepine with a short half life
High dose
IV administration
Patient factors increasing the risk of a paradoxical reaction with benzodiazepine use
Extremes of age
Learning disability
History of aggression or poor impulse control
Teratogenic effect of diazepam
Cleft lip and palate
Effect of pregabalin on GABA
None - it is a GABA analogue
Time to steady state for pregabalin
24-48 hours
Bioavailability of pregabalin
High
Most toxic benzodiazepine in overdose
Alprazolam
Antiepileptic medication licensed for treatment of generalised anxiety disorder
Pregabalin
Protein binding of diazepam
98%
Subunit of the GABA receptor benzodiazepines and Z drugs act on
Omega 1 subunit
Subunit of voltage gated calcium channels pregabalin acts on
Alpha-2-delta subunit
Time to maximum plasma concentration for pregabalin
1 hour
Binding of pregabalin to plasma proteins
Does not bind
Effect of prolonged use on the euphoric effects of pregabalin
Disappear with prolonged use
Impact of flumazenil on risk of seizures
Increases risk
Risk factors for developing a paradoxical reaction to benzodiazepines
Learning disability
Extremes of age
History of aggression or poor impulse control
Use of a benzodiazepine with a short half life
IV administration
Use of a high dose
