Egleton: Anxiolytics

Question 1

Fluoxetine/ Sertraline: use and side effects

Answer 1

SSRIs
For PTSD and most anxiety disorders
Very slow onset of action (2-4 wks)
Jitters

Question 2

Venflaxine

Answer 2

SNRIs
Similar to SSRI + NE 
Treat depression 
Desensitize NE receptor, normalize amygdala activation and CSTC
PTSD
Slow onset (2-4wk)
Jitters

Question 3

Anti-jitters

Answer 3

Benzodiazepine

Question 4

Imipramine

Answer 4

TCA
Similar to SSRI and SNRI
More side effects
Second line GAD and Panic disorders
Slow onset (2-4wk)
Jitters

Question 5

Benzodiazepine: MoA

Answer 5

Enhance GABA binding to GABA A receptor
Increase frequency of channel opening
Increaser Cl flux into cell
Hyperpolarization
Inhibit cell activity

Question 6

Benzodiazepine: CNS effect

Answer 6

Relief of anxiety
Sleep induction
Anesthetic effects
(Tapers off before Coma and Death)

Question 7

Benzodiapine: considerations

Answer 7

Don’t give to pregnant/ breastfeeding mother (cross placenta/ secreted in milk/ lipophilic)
Antacid prevent absorption from gut

Question 8

Benzodiazepine: metabolism

Answer 8

Longer metabolite half life than parent
Hepatic metabolism
Phase I inhibited by Cimetidine

Question 9

Oxazepam/ Lorazepam

Answer 9

Benzodiazepine
Useful for liver disease patient and elderly
No metabolites
Short half life

Question 10

Benzodiazepine: side effects

Answer 10

Drowsiness and Confusion
Anterograde amnesia (1-3 hr after dose) for Anesthesia
Rebound
Interact with alcohol and other depressant= Resp. depression/ Coma

Question 11

Benzodiazepine: contra

Answer 11

COPD: Midazolam= worse with Asthma, Chronic bronchitis, Emphysema
Obstructive sleep apnea: aggravate sleep related breathing disorder
Liver disease: potentiated BDZ effects
Must reduce dose for elderly
Alcohol: overdose with respiratory depression
Pregnancy

Question 12

Benzodiazepine: tolerance/ dependence

Answer 12

No tolerance to anxiolytic effects (others do)

Physical dependence can occur if extended therapy

Question 13

Benzodiazepine: withdrawal

Answer 13

More severe for shorter half life
Anxiety, Insomnia
Seizure (rare){for treatment of seizure}

Question 14

Diazepam: unique property

Answer 14

BDZ

Direct muscle relaxant

Question 15

Alprazolam: unique property

Answer 15

BDZ

Antidepressant, Panic disorder, Agoraphobia

Question 16

Trizolam: unique property

Answer 16

BDZ

Rebound anxiety and Rebound insomnia

Question 17

Lorazepam: unique property

Answer 17

Antiemetic

Question 18

Flumazenil

Answer 18

BDZ antagonist
Antagonist for BDZ overdose
IV admin
May precipitate withdrawal/ cause seizure with BDZ use for anticonvulsant
ADR: dizziness, nausea, vomit, agitation

Question 19

Buspirone

Answer 19

Non-BDZ
Agonist of 5HT1A (post and presynaptic)
Treat GAD (generalized anxiety disorder)
Lack sedative= for pilots and doctors
No interaction with alcohol and other CND depressants
Good for elderly with substance abuse

Question 20

Pregabalin

Answer 20

Blocks Voltage sensitive Ca channels (VSCC)
Binds presynaptic N and P/Q channel
Prevent release of exitatory neurotransmitters in Amygdala/ CTSC
For GAD, Social generalized

Question 21

Meprobamate

Answer 21

Not as effective as BDZ
For anxiety
Contra: Porphyrias

Question 22

Propanolol

Answer 22

Nonselective beta-adrenergic blocker
Reduce somatic symptoms of anxiety (palpitation, sweating, tachycardia)
For short term Situational anxiety, stage/ exam fright

Question 23

Hydroxyzine

Answer 23

Antihistamine (H1 receptor antagonist)
Cause sedation
For GAD + insomnia

Question 24

Mirtazapine

Answer 24

5HT2 receptor angatonist
For GAD + insomnia
ADR: Weight gain and Sedation

Question 25

Fluoxetine/ Sertraline: general characteristics

Answer 25

SSRIs
1st line for anxiety disorders
Work on Amygdala, Prefrontal cortex, Striatum, Thalamus
{controlled by serotonin from Raphe nuclei
Normalize activation of Amygdala and CSTC loop