Anxiolytics Drugs - Egleton Flashcards
what part of the brain is involved with fear
amygdala
what part of the brain is involved with worry
cortico-striato-thalamo-cortico loop circuit
what are the first line of drugs to treat anxiety
SSRI
what are the 2nd line of drugs to treat anxiety
TCA
Benzodiazepines
SSRI is commonly used in what medical condition
depression
What is SSRI used for
- treatment of anxiety disorders
- PTSD: reduces flashbacks, arousal, and avoidance
what is the onset of action for SSRI
2-4 weeks
slow
what are sides effects of SSRI
Jitters potentially some increased anxiety initially
name a SNRI drug
Venflaxine
what are SNRI commonly used to treat
depression
what is a difference between SNRI and SSRI
SSRI: serotonin
SNRI: serotonin and NE
what is SNRI used for
treatment of most anxiety disorders
PTSD: reduce flashbacks, arousal, and avoidance
Co-morbid pain disorders
what is the onset for SNRI to start working
very slow
2-4 weeks
what is a side effect of SNRI
jitters, potentially some increased anxiety initially
what are jitters
paradoxical increase in anxiety, restlessness, insomnia in first weeks of drugs
how can jitter problem be fixed with SSRI and SNRi
take with Benzodiazepine for short term
Name two SSRI drugs
Fluoxetine
Sertraline
Imipramine is used when and what type of drug
second line
TCA ( tricyclic antidepressant)
What is Imipramine used for
GAD
panic disorders if SNRI and SSRI are ineffective
Benzodiazepines MOA
enhance GABA binding to GABA receptor
- increase frequency of opening channel
- increases Cl- flux into cell
- hyper polarizes
- inhibition of cell acitivity
GABA initiates signaling from where
amygdala
cortico-striato-thalamo-cortico-loop
Benzodiazepines have different levels of CNS effects. what are they
- relief of anxiety
- sleep induction
- anesthetic effects
- coma and death
when is coma and death seen with Benzodiazepines
in conjunction with other depressants like Alcohol
At what dose does Benzodiazepines have respiratory effects
Anesthetic dose
what does Benzodiazepines have cardiovascular effects
none, except at high doses
Benzodiazepines are very soluble in what
lipids
how does Benzodiazepines work in the GI
completely absorbed
- antacids prevent absorption
how does Benzodiazepines effect pregnant women
crosses placenta
secreted into breast milk
how does the hepatic metabolism impact Benzodiazepines
- active metabolites generated
- 1/2 life of active metabolites is higher then parent compound
explain phase I , II, III of active metabolism of Benzodiazepones
I: initial oxidation step, quickest reaction.Inhibited by cimetidine.
II: Hydroxylation at R3 to yield another active metabolite, slowest reaction
III: Glucuronidation followed by urinary excretion
Which Benzodiazepones are useful for patients with liver disease
Oxazepam
Lorazepam
what are the most common side effects of Benzodiazepones
Drowsiness and confusion
what is a anesthesia side of effect of Benzodiazepones
anterograde amnesia
forget experience 1-3 hours after dose
what is a side effect of Benzodiazepone
rebound… dose tapering required for short half-life drugs
Benzodiazepone have what drug interaction and can this lead to
alcohol and other depressants
- respiratory depression and death
what Benzodiazepone drugs should be given to elderly and why
Lorazepam and Oxazepam
1/3 or 1/2 dose should be given
What Benzodiazepone drugs should not be given to COPD patients
Midazolam
how does Benzodiazepone drug impact obstructive sleep apnea
muscle relaxant of Benzodiazepone
what happens in alcohol and Sedative-hypnotic mixed withBenzodiazepone
respiratory depression
what Benzodiazepone drugs should not be given to pregnant women
Chlordiazepoxide
diazepam
what kind of dependence can occur with Benzodiazepone
physcial
what are frequent withdrawal symptoms of benzodizepone
anxiety
insomnia
what are rare withdrawal symptoms for Benzodiazepone
siezures
benzodizepone: Diazepam
direct muscle relaxant
benzodizepone: alprazolam
panic disorder
benzodizepone: triazolam
rebound anxiety and insomnia
benzodizepone: antiemetic
antimemetic – prevent vomiting
what is Flumazenil
BDZ antagonist
what is Flumazenil used for
BDZ overdose
what is the disadvantage for using Flumazenil
may precipitate withdrawal; may cause seizures if BDZ is used to control seizure activity
mechanism of action for Buspirone
agonist for 5-HT (post and presynaptic)
what is Buspirone used for
treatment of GAD
what are 3 characteristics of Buspirone
- lacks sedative, anticonsuvlsants and muscle relaxant effects
- no interaction with alcohol or other CNS depressans
- good for substance abuse patients
what is the mechanism of action for Pregabalin
blocks voltage sensitive calcium channels
- binds to presynaptic N and P/Q channel alpha2gamma
- prevents release of excitatory neurotransmitters in amygdala and CTSC
what is Pregabalin used for
GAD
social generalized
compare the effectivness of Meprobamate and BDZ
Not as effective as BDZ’s
what caution needs to be taken for Meprobamate
contraindicated in prophyrias
how does Propanolol work
nonselective beta-adrenergic blocker
what is Propanolol used for
short term anxiety
what is Hydroxyzine
antihistamine
H1 receptor antagonist
what is Mirtazapine
5HT2 receptor antagonist
side effects of Mirtazapine
weight gain and sedation
