Anxiolytics Flashcards
Fight or Flight response has a peripheral noradrenergic response mediated via ____ and a central adrenergic reaction mediated via ______.
- NA/NE
2. adrenaline/epinephrine
The stress response involves the ____ axis and secretion of ______
- Hypothalamus-pituitary-adrenal(HPA)axis
2. cortisol (stress hormone)
Therapeutic rationale of sedatives is to cause _____ and ______. (Patient is still conscious)
sedation
relaxation
Therapeutic rationale of _____ is to induce drowsiness, sleep and may have amnestic effects.
Hypnotics
Anxiolytics reduce _____.
anxiety
The same anxiolytic can have more than one action depending on dose.
- Low dose = _______
- Higher doses = _______
- Even higher doses = ________
- anxiolytic and sedative effects
- hypnotic
- can cause anesthesia, used for surgery
Benzodiazepines can be used as anxiolytics/sedatives (i.e. ________).
diazepam, lorazepam
Benzodiazepines that can be used as hypnotics (i.e. _________, _________, _________).
- diazepam
- triazolam
- temazepam
Benzodiazepines can be used as _______ (i.e. diazepam, midazolam).
pre-anaesthetics
Benzodiazepines can have anti-convulsant effects (i.e. ______).
diazepam
Benzodiazepines can have anti-convulsant effects (i.e. ______).
diazepam
Non-BZDs include Barbiturates (eg _________), _______, ________ and Propranolol etc.
- phenobarbital
- Buspirone
- Zolpidem
BZD binding potentiates the binding of ______ receptor binding site, making GABA-A open more easily, Potentiates __________ leading to _______= neurons not firing
- GABA to GABA-A
- influx of Cl-ions
- Hyperpolarization
GABA binding, enhanced by BZDs leads to ______ (limbic system), ______ (reticular activating system) and ________ (motor cortex).
- altered mood
- drowsiness
- relaxed muscles
The longer acting BZDs are more appropriate for ______ to reduce dose frequency and have a duration of ______.
- chronic conditions
2. 1-3 days
The Short acting BZDs are more appropriate for ______ and can last ______.
- General anesthesia induction
2. 3-8hrs
The intermediate acting BZDs can last ______.
10-20hrs
BZDs can cause _________, especially used concurrently with alcohol.
severe respiratory depression
Treatment of BZD overdose is using ______, a benzodiazepine antagonist
flumazenil
Side effects of BZDs are related to CNS depression and include: ______, _______, _______. and impaired muscle co-ordination (which is why we must counsel pts _______).
- Drowsiness
- confusion
- amnesia
- Not to operate heavy machinery
BZD tolerance depends on ______ of use. Therefore, tolerance develops ______for epilepsy than use to induce sleep.
- frequency
2. faster
Dependence for BZDs can develop and BZDs have abuse potential. Withdrawal effects include: _____, rebound _____, tremor and ______.
- disturbed sleep
- anxiety
- convulsions
A key strategy to avoid BZD dependence is to ______.
Withdraw gradually
Zolpidem has the ______ but different _____ compared to BZDs. It is ____effective than anxiolytics.
- same MOA
- structure
- less
Zolpidem has a good _____ effect and is primarily used to treat ________.
- hypnotic
2. insomnia
Buspirone is a _____ receptor partial agonist that also binds _____ receptors.
- 5-HT1A
2. dopamine
Buspirone is indicated for GAD but anxiolytic effects require ______. It also lacks anti-convulsant and _______ properties.
- take 1-2 wks
2. muscle relaxant
Barbiturates have the same ______ but different _______ compared to BZDs. At anesthetic doses, barbiturates (i.e. phenobarbital) can _____________ as well as block Na+ channels.
- MOA
- binding site
- directly open CL- channels (no longer potentiates)
Barbiturate use as a sedative-hypnotic has largely been replaced by BZDs due to barbiturate’s increased tendency to ________. Flumazenil is _____ in treating Barbiturate overdose.
- develop tolerance and dependence
2. not effective
Barbiturates have _____ withdrawal symptoms.
severe
Long acting barbiturates meant for anti-convulsant use have a duration of action of 1-2 _____. (i.e. _____)
- days
2. phenobarbital
Short acting barbiturates meant for sedative and hypnotic use have a duration of action of 3-8 _____. (i.e. _____ and ______)
- hrs
- pentobarbital
- amobarbital
Ultra-short acting barbiturates meant for induction of anesthesia have a duration of action of 20 _____. (i.e. _____ )
- mins
2. thiopental
BZDs are ____ likely to cause respiratory depression compared to barbiturates.
less
At higher doses, barbiturates cause _____ depression and can even result in _____.
- medullary
2. coma
Pregabalin acts by _______, resulting in hyperpolarization. It also acts on _____channels.
- increasing synaptic GABA
2. voltage gated Ca2+
Pregabalin has ______effects and is used in treatment of _____ but may be associated with emergence or worsening of ______.
- anticonvulsant
- GAD
- suicidal thoughts
Hydroxyzine is a 1st gen anti-histamine with effects on _____ and ______ receptors. Its anxiolytic effects are due to antagonism of ______ receptors. It can also help with _____ due to its anti-histamine activity.
- serotonergic
- α-adrenergic
- serotonergic
- itching/nausea related anxiety
Hydroxyzine has ____ addictive potential compared to BZDs and barbiturates.
lower
Propranolol can be used for treating _________ and _____ phobias. It reduces the physical symptoms associated with adrenergic activation i.e. tachycardia and _______.
- performance anxiety
- social
- muscle tremors
Propranolol is Contraindicated in patients with _____ and ______ conditions. (including predisposition)
- asthma
2. heart
Many other depressants also serve as anxiolytics as the 2 conditions may share the same chemical basis. They include _______ (NaSSA), _______ (TCA), Fluoxetine, citalopram, sertraline, paroxetine (____) and Venlafaxine, duloxetine (_____).
- Mirtazapine
- Clomipiramine
- SSRI
- SNRIs
