Anti-Anxiety Drugs - Lauden Flashcards
What is the mechanism of action of benzodiazepines?
GABA agonist (works on a different ligand site on the same receptor as barbiturates and alcohol)
Causes a higher chloride influx
Bz1 receptors more related to sleep (those that act here have less side effects)
Bz2 more related to motor movement, concentration and cognition
Can be contraindicated by flumazenil in case of overdose (competitive receptor antagonist)
What are the different variations of bezodiazapines and how are their pharmacokinetics different?
3ִ hydroxy- oxazepam, Lorazepam (only one given IM), Temazepam-metabolized directly to
glucoronic acid- Short T1/2 (sleep aid)
Lipid soluble- Diazepam, Alprazolam- Fast acting but long lasting
2ִ keto group- Diazepam, Prazepam, Halzepam, Flurazepam, +/_
Clonazepam, chlordiazpoxide- Metabolized slowly to desmethyldiazepam- to
Oxazepam (active metabolites) to Glucoronic acid- resulting in long T1/2 (30-100 hours)
Short acting- alprazolam, estazolam, lorazepam, oxazepam,
temazepam, triazolam, brotizolam- most of them-no active
metabolite, average half lifetime: 2- 17 hours (underlined 2-7hours)
Long acting- chlordiazpoxide, clonazepam, clorazepate,
diazepam, flurazepam, halazepam (used for anxiety or to wean off short acting)
What are the indications for benzodiazepines?
Fast Anxiety relief- panic symptoms, situational, agitation,
Anxiety blockade until SSRI action- 2-4 weeks
Anxiety disorders- first line for GAD
Other psych disorders with anxiety- schizophrenia, bipolar,
personality disorders, low anxiety tolerance, Catatonia,
Sleep disturbances- depression, schizo, PTSD, other
Insomnia- preferably short duration – to 1 month
Zolpidem (Ambien) BZ1 agonist– less change in
sleep architecture, less cognitive disturbance
Alcohol withdrawal (chlordiazepoxide, lorazepam,
valium, then gradually lower)
Anesthesia induction (midazolam – i.v., rapid acting, increase in amnesia)
Akathisia (motor restlessness due to antipsychotics)
Seizures – status epilepticus, (to stop seizures)
Muscle relaxant – less commonly used but effective, LBP
Catatonia (high doses, but then treat underlying cause)
Pain augmentation (reduces muscle stiffness and anxiety)
What are the withdrawal signs and symptoms of benzodiazepines?
Increased anxiety (“rebound anxiety”) or panic attacks (even in patients with no anxiety to begin with)
Restlessness, dysphoria and irritability
Tremor, muscle twitching, shaking
Insomnia
Diaphoresis, tachycardia and elevations in BP
Dizziness
Sensory disturbances (paresthesias)
Flu-like illness with headache, muscle tension, cramping
Concentration difficulties, abnormal perception of movement, depersonalization
Nausea, low appetite
Depressed mood
Seizures
Confusion/delirium
Psychosis
Memory impairment
What are the medications used for anxiety?
Antihistamines- promethazine, Phenergan, preferred
for “high abuse potential patients”
Beta blockers- performance anxiety
TCA related- Trazadone
Benzodiazepines
