Anti-Anxiety Drugs Flashcards
What are three characteristics of anxiety?
Adaptive
Pathological
Anticipatory
3 main types of anxiety
Gen anxiety disorder
Panic disorder
Phobias
What are 4 proposed treatments for GAD?
Antidepressants, especially SSRIs
Benzodiazepines (eg. Diazepam)
Beta blockers (propranolol) if somatic
Buspirone (5-HT1A partial agonist)
What are 2 proposed treatments for Panic Disorder?
Benzodiazepines
Antidepressants
What are the proposed treatments for social and specific phobias?
Social - beta blockers
Specific - Therapist sessions
What is the comorbidity of GAD?
Other anxiety disorders and Major Depression
Who gets GAD?
Everyone
Diazepam has similar distribution patterns to which kind of receptor?
GABA-A
Diazepam _____ GABA receptors’ affinity to GABA
Increases
GABA and GABA agonists ______ Diazepam binding
Increase
What three parameters describe GABA-A receptor activity?
Probability of opening
Open time
Conductance
Benzodiazepines mainly do what to GABA receptors?
They increase the probability of the channel opening
Barbiturates do what to GABA receptors?
Prolong channel opening
True/False? GABA-A receptors have only one binding site
False
True/False? All Benzodiazepines have roughly the same pharmacokinetics
False
What properties to Benzodiazepines share? (4)
Rapid brain entry, slow redistribution (IV diazepam)
Active metabolites
Binding to plasma proteins
Enterohepatic recycling
What is the main active metabolite in benzodiazepines?
Nordiazepam
Why do Benzodiazepines have a long duration of action?
Clearance is reduced due to plasma protein binding
What are the three main effects of benzodiazepines? What receptors are affected?
Sedation
Muscle relaxation
Anticonvulsant
GABA-A receptors presenting alpha 1 subunit
Which receptors produce anxiolytic effects when affected?
Noradrenergic alpha 2 receptors
What determines the anxiolytic action of diazepam?
alpha2-containing GABA-A receptors
What is the difference in therapeutic delay for buspirone and Benzodiazepines?
Buspirone: 1-3 weeks
BZs: 15 min-2 hrs
True/False? buspirone helps with panic attacks
False
True/False? buspirone has hardly any side effects
True (slight sedation)
Is Buspirone’s effect on 5-HT transmission predictable? Why (not)?
No.
- 5-HT1A receptors have opposing effects on 5-HT transmission (they inhibit 5-HT cell firing and release, but also mimic a postsynaptic action of 5-HT)
- Partial agonists can have agonist-like or antagonist-like actions, depending on 5-HT tone
What is the stereotypical beta blocker?
Propranolol
What are the endogenous agonists at beta-adrinergic receptors? (2)
Noradrenaline and adrenaline
Where are beta adrenergic receptors found?
Heart
Blood vessels in muscle
Bronchi
Brain
What does the effect of beta blockade depend on?
sympathetic tone
What are 5 unwanted effects of Propranolol?
Bronchoconstriction in asthma Cardiac failure in heart disease Blocks signs of hypoglycemia in diabetic patients Physical fatigue Bad dreams
True/False? Diazepam reduces somatic and psychic anxiety.
True
True/False? Propranolol reduces somatic and psychic anxiety.
False, just somatic
Which drugs work best for GAD?
Benzodiazepines ~ buspirone ~ SSRIs
Choice of drugs depends need of rapid onset and adverse effects
Beta blockers are widely used but not proven to work long term (considered second line)
What are 2 examples of animal models?
Elevated plus maze
Fear-potentiated startle response
True/False? Acute buspirone helped rats spend more time in the open arms of the elevated plus mase
False
What is the fear-potentiated startle response?
- Pavlovian conditioning to associate light with shock
- startle in dark, measure response
- startle in light, measure response
- and 2. have different responses
What are three advantages of the fear-potentiated startle response?
- Detects broad range of anxiolytics
- Not only order drugs, but newer ones (buspirone)
- Reveals brain mechanisms
True/False? Anxiety has many components
True
