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65 Cards in this Set

  • Front
  • Back
Chemical classes of Anxiolytic drugs
Benzodiazepines
Buspirone
Antidepressants
B-adrenergic agents
Most commonly prescribed Anxiolytic
Benzodiazepines
Benzodiazepines pharmocological action
Exert effects by actions on the GABA-A receptor
Benzodiazepines
onsets and PK
Widely variable half lives
Widely variable onsets
Reach peak levels in blood and brain after 1-2 hr
Metabolized extensively by CYPs
Benzodiazepines bioavailability and distribution
Well absorbed after oral admin
Food delays absorption
Highly bound to plasma proteins which affects Distrib.
Benzodiazepines CS class and properties
CS IV
Potential for physiological dependence
Shorter acting analogs esp.
Taper the dose
Benzodiazepine metabolism paths
Glucoronylation
CYP pathways
Benzodiazepines common metabolic intermediate
N-desmethyldiazepam (nordiazepam)
Half life 30-200 hr)
Benzodiazepine common side effects
Withdrawl and seizures
Drowsiness/sedation
Irritability
Memory impairment
Anterograde amnesia
Depression
Contraindications for Benzodiazepines
HTN
Glaucoma
Pregnancy (Cat D or X)
Benzodiazepine drug interactions
CNS depressants (ROH, antihistamines, narcotics, anti-psychotics)
CYP inhibitors (Cimetidine, oral contraceptives)
Alprazolam brand name
Xanax
Alprazolam indications
GAD
Panic disorder
Anxiety associated with depression
Alprazolam PK
Onset 1-2 hr
Half life 11 hr
Metabolism: CYP3A4
Alprazolam dosage forms
Oral (ER) and orally dissolving
Alprazolam chemical structure feature
Chloro at 7-position yields sedative properties
Chemical feature of benzodiazepines
7-Cl or 7-NO2 yields sedative/hypnotic properties
Clonazepam brand name
Klonopin
Clonazepam indications
Panic disorder
Clonazepam PK
Onset: 20-60 min FAST
Half life 19-50 hr
Metabolism: CYP3A4
Clonazepam chemical structure feature
7-NO2 group produces sedative effect
Diazepam brand name
Valium
Diazepam indications
Anxiety disorders
Ethanol withdrawl
Diazepam PK
Onset 15-30 min
Half life (parent) 20-50 hr
Half life Desmethyldiazepam 30-200 hr
Meatbolism: CYP2C19, CYP3A4
Lorazepam brand name
Ativan
Lorazepam indications
Anxiety disorders
Off label: Insomnia, EtOH withdrawl
Lorazepam PK
Onset 30 min
Half life 12 hr short
Metabolism: glucuronidation NOT CYP
Chlordiazepoxide brand name
Librium
Chlordiazepoxide indications
Anxiety disorders
EtOH withdrawl
Chlordiazepoxide PK
Onset 30-60 min
Half life 6-25 hr
Metabolism: CYP3A4
4 active metabolites
Chlordiazepoxide side effects
Drowsiness
Ataxia
Confusion
Clorazepate brand name
Tranxene
Clorazepate indications
GAD
EtOH withdrawl
Clorazepate side effects
Dizziness
GI nervousness
Clorazepate PK
Onset 1-2 hr
Half life 48-96 hr (parent)
Metabolism: CYP3A4
2 active metabolites
Oxazepam brand name
Serax
Oxazepam indications
Anxiety disorders
EtOH withdrawl
Oxazepam PK
Onset 2 hr
Half life 3-6hr Short!
Metabolism: glucuronidation
50% excreted unchanged
glucuronidation meatbolism yields what?
Inactive metabolites
Flumazenil brand name
Romazicon
Flumazenil indication
Benzodiazepine overdose
Flumazenil drug action/class
Benzo GABA-A antagonist
Binds to receptor normally bound by benzodiazopines
No effect on ROH overdose
Flumazenil warning
May result in seizures
Flumazenil PK
Onset: 6-10 min FAST
Half life 40-80 min
Flumazenil dosage form
I.V.
Multiple doses
hospital setting
Buspirone drug class
NOT a benzodiazepine
Buspirone DRUG ACTION
Doesn't bind GABA receptors
Anxiolytic
Serotonin based mechanism of action
Serotonin partial agonist
Same binding site as Sero
Buspirone advantages
No abuse potentil
No CNS depression
Buspirone brand name
BuSpar
Buspirone binds which receptor?
Serotonin 5-HT-1a
Buspirone indications
GAD
Buspirone not indicated for?
Panic attacks
OCD
PTSD
Buspirone phrmacological onset
4-6 weeks like antidepressants
Often prescribed with SSRIs
Not a good prn drug unlike benzos
Not as good long term as benzos
Buspirone key advantage over benzos
no sedative or hypnotic effects
Buspirone PK
Onset 30 min
Half life 2-11 hr
Metabolism: CYP3A4
Buspirone contraindicated for?
pregnancy (Cat B)
Patients taking SSRIs
Oxepam excretion
50% excreted unchanged
Generalized Anxiety Disorder Drugs (GAD)
Alprazolam/Xanax
Chlorazepate/Tranxene
Buspirone
GAD! Praise Clora's Bus!
Panic disporder drugs
Alprazolam/Xanax
Clonazepam/Klonepin

Al panics at the Clondike
Anxiety associated with depression drugs
Alprazolam/Xanax
EtOH withdrawl
Valium/diazepam
Lorazepam
Chloriazepoxide
Oxazepam CLOVes
CLOVes always help me be less anxious and stop drinking
Anxiety drugs
Diazepam/Valium
Lorezapam/Ativan
Chlordiazepoxide/Librium
Oxazepam/Serax
CLOVes
Benzodiazepine overdose drug
Flumazenil
CYP metabolized
Alprazolam
Clonazepam
Diazepam
Chlorazepate
Chlordiazepxide
Buspirone
Metabolized by Glucuronidation
Lorazepam 12 hr t1/2
Oxazepam 3-6h t1/2

Gluco LOx down the half life