Anxiety - Steve Fitzjohn

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Degree Neuropharmacology Fichas sobre Anxiety - Steve Fitzjohn, creado por Anna mph el 15/12/2015.
Anna mph
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What is anxiety? Anticipation of fear in the absence of external stimuli
What is an anxiolytic? Takes a state of increased arousal back to normal
What is a sedative? Takes nervous system from normal level to lower (i.e. for surgery)
What is a hypnotic? Takes nervous system from normal level and dampens down even further, sends individual to sleep
What classes of drugs can be used as anxiolytics? (6) Antidepressants Benzodiazepines 5-HT1a receptor agonists Some antiepileptic drugs Anti-psychotics B-adrenoreceptor agonists
Which class of drugs can be used to subdue a panic attack but shouldn't be used long term due to their addictive nature? Benzodiazepines
Which drugs are anxiolytic, sedative and hypnotic? Benzodiazepines Zopiclone (Potentiates GABAa) Barbituates
Which drugs are just anxiolytic? Antidepressants Buspirone B adrenoreceptor antagonists (eg propanolol)
Which drug is just hypnotic? Antihistamine
What are the two mainly used types of anti-depressants? SSRIs (Selective serotonin re-uptake inhibitors) SNRIS (Selective noradrenaline re-uptake inhibitors)
What is the onset time period for anti-depressants? (SSRIs and SNRIs) 6 weeks
Give an example of an SSRI Citalopram
Give an example of a SNRI Venlafaxine
What are the clinical uses of benzodiazepines? anti-anxiety sedative hypnotic anti-convulsant antieplieptic (some eg diazepam) Muscle relaxant
What are the side effects of benzodiazepines? (6) Drowsiness Amnesia Confusion Impaired motor function Lack of depth perception Reduced REM
Give an example of a benzodiazepine used to treat anxiety? Nitrazepam
What happens if you mix benzodiazepines with alcohol? Respiratory depression
What are the half lives of these drugs and what are they (hypnotic, anxiolytic, anticonvulsant) (5) (more important are *) Zolpidem 1-2h Hypnotic
Triazolam 2-4h Hypnotic
Loprazolam 6-12h Anxiolytic and Hypnotic
*NITRAZEPAM 16-40h Anxiolytic and Hypnotic
Diazepam 10-40h Anticonvulsant & Anxiolytic
Tolerance in benzodiazepine is ? in Anticonvulsants Anxiolytics Hypnotics High Medium Low
How does tolerance vary with half life of the drug? Shorter the half life the less likely tolerance occurs
What are the physical dependence withdrawal symptoms? Anxiety Dizziness Tremor Tinnitus Weight loss Sleep disturbances
How do benzodiazepines work? (2) 1) Increase affinity of GABA to receptor 2) Increase probability of channel opening
What effect does BCCE (ethyl-B-carboline-3-carboxylate) and diazepam binding inhibitors have? Cause conformational change to GABA receptor making it harder for benzodiazepines to bind.
What is the point of benzodiazepine antagonists? Reverse effects of benzodiazepines eg. excessive drowsiness
What happens if you give someone a benzodiazepine antagonist if they have no benzodiazepines in their system? Induce anxiety
Give an example of a benzodiazepine antagonist Flumazenil
What is phenobarbitone? Barbituate
What type of receptors do barbituates potentiate the action of? GABAa
Which ligand gated ion channel do they inhibit? AMPA
Why are benzodiazepines used more commonly than barbiturates? Harder to cause anaesthesia and death in overdose when using benzodiazepines
How do low and high concentrations of barbiturates interact with GABA receptors? 1) Low conc. prolong opening of R in presence of GABA 2) High conc. can open receptor without GABA present
What is Buspirone 5HT-1a receptor partial agonist
How does Buspirone differ to benzodiasepines in terms of sedation and motor in-coordination? Less
What are the side effects of Buspirone and how do they relate to benzodiazepines? Headaches Nausea Dizziness Restlessness ALL LESS THAN IN BENZODIAZEPINES
What are the pros of Buspirone (1) 1) No tolerance or physical dependence
What are the cons of Buspirone? 1) Doesn't help withdrawal from Benzos. 2) Takes days to weeks to work but only licensed for short term use 3) Don't help with panic attacks/severe anxiety 4) May increase anxiety initially
What are 5-HT1a receptors and where are they located? Somatodendritic autoreceptors Serotenergic neurons in the Raphe nucleus
What effect does the prolonged presence of buspirone have on the 5-HT1a receptors (and seretonin release)? Initially receptors are activated causing a decrease in seretonin release. Receptors desensitise, seretonin release increases.
Why are B adrenoreceptors antagonists not a good anxiety treatment? Treat symptoms not anxiety itself
Which symptoms of anxiety do B adrenoreceptor antagonists treat? Peripheral symptoms - Palpitations Sweating Tremor
Give an example of an B adrenoreceptor antagonist Propanolol
What can antipsychotics be used to treat? GAD, PTSD
Why are antipsychotics not generally used? Greater incidence of side effects than other anxiolytics
What can zopiclone and zolpidem be used for? Insomnia treatment
Where do Zopiclone and zolpidem bind? Same place and benzodiazepines (ay interface)
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