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65 Cards in this Set
- Front
- Back
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Chemical classes of Anxiolytic drugs
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Benzodiazepines
Buspirone Antidepressants B-adrenergic agents |
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Most commonly prescribed Anxiolytic
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Benzodiazepines
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Benzodiazepines pharmocological action
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Exert effects by actions on the GABA-A receptor
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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 |
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Benzodiazepines bioavailability and distribution
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Well absorbed after oral admin
Food delays absorption Highly bound to plasma proteins which affects Distrib. |
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Benzodiazepines CS class and properties
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CS IV
Potential for physiological dependence Shorter acting analogs esp. Taper the dose |
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Benzodiazepine metabolism paths
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Glucoronylation
CYP pathways |
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Benzodiazepines common metabolic intermediate
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N-desmethyldiazepam (nordiazepam)
Half life 30-200 hr) |
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Benzodiazepine common side effects
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Withdrawl and seizures
Drowsiness/sedation Irritability Memory impairment Anterograde amnesia Depression |
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Contraindications for Benzodiazepines
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HTN
Glaucoma Pregnancy (Cat D or X) |
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Benzodiazepine drug interactions
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CNS depressants (ROH, antihistamines, narcotics, anti-psychotics)
CYP inhibitors (Cimetidine, oral contraceptives) |
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Alprazolam brand name
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Xanax
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Alprazolam indications
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GAD
Panic disorder Anxiety associated with depression |
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Alprazolam PK
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Onset 1-2 hr
Half life 11 hr Metabolism: CYP3A4 |
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Alprazolam dosage forms
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Oral (ER) and orally dissolving
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Alprazolam chemical structure feature
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Chloro at 7-position yields sedative properties
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Chemical feature of benzodiazepines
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7-Cl or 7-NO2 yields sedative/hypnotic properties
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Clonazepam brand name
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Klonopin
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Clonazepam indications
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Panic disorder
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Clonazepam PK
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Onset: 20-60 min FAST
Half life 19-50 hr Metabolism: CYP3A4 |
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Clonazepam chemical structure feature
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7-NO2 group produces sedative effect
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Diazepam brand name
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Valium
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Diazepam indications
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Anxiety disorders
Ethanol withdrawl |
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Diazepam PK
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Onset 15-30 min
Half life (parent) 20-50 hr Half life Desmethyldiazepam 30-200 hr Meatbolism: CYP2C19, CYP3A4 |
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Lorazepam brand name
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Ativan
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Lorazepam indications
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Anxiety disorders
Off label: Insomnia, EtOH withdrawl |
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Lorazepam PK
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Onset 30 min
Half life 12 hr short Metabolism: glucuronidation NOT CYP |
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Chlordiazepoxide brand name
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Librium
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Chlordiazepoxide indications
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Anxiety disorders
EtOH withdrawl |
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Chlordiazepoxide PK
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Onset 30-60 min
Half life 6-25 hr Metabolism: CYP3A4 4 active metabolites |
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Chlordiazepoxide side effects
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Drowsiness
Ataxia Confusion |
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Clorazepate brand name
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Tranxene
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Clorazepate indications
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GAD
EtOH withdrawl |
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Clorazepate side effects
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Dizziness
GI nervousness |
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Clorazepate PK
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Onset 1-2 hr
Half life 48-96 hr (parent) Metabolism: CYP3A4 2 active metabolites |
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Oxazepam brand name
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Serax
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Oxazepam indications
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Anxiety disorders
EtOH withdrawl |
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Oxazepam PK
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Onset 2 hr
Half life 3-6hr Short! Metabolism: glucuronidation 50% excreted unchanged |
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glucuronidation meatbolism yields what?
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Inactive metabolites
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Flumazenil brand name
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Romazicon
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Flumazenil indication
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Benzodiazepine overdose
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Flumazenil drug action/class
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Benzo GABA-A antagonist
Binds to receptor normally bound by benzodiazopines No effect on ROH overdose |
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Flumazenil warning
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May result in seizures
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Flumazenil PK
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Onset: 6-10 min FAST
Half life 40-80 min |
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Flumazenil dosage form
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I.V.
Multiple doses hospital setting |
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Buspirone drug class
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NOT a benzodiazepine
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Buspirone DRUG ACTION
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Doesn't bind GABA receptors
Anxiolytic Serotonin based mechanism of action Serotonin partial agonist Same binding site as Sero |
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Buspirone advantages
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No abuse potentil
No CNS depression |
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Buspirone brand name
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BuSpar
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Buspirone binds which receptor?
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Serotonin 5-HT-1a
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Buspirone indications
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GAD
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Buspirone not indicated for?
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Panic attacks
OCD PTSD |
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Buspirone phrmacological onset
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4-6 weeks like antidepressants
Often prescribed with SSRIs Not a good prn drug unlike benzos Not as good long term as benzos |
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Buspirone key advantage over benzos
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no sedative or hypnotic effects
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Buspirone PK
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Onset 30 min
Half life 2-11 hr Metabolism: CYP3A4 |
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Buspirone contraindicated for?
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pregnancy (Cat B)
Patients taking SSRIs |
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Oxepam excretion
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50% excreted unchanged
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Generalized Anxiety Disorder Drugs (GAD)
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Alprazolam/Xanax
Chlorazepate/Tranxene Buspirone GAD! Praise Clora's Bus! |
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Panic disporder drugs
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Alprazolam/Xanax
Clonazepam/Klonepin Al panics at the Clondike |
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Anxiety associated with depression drugs
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Alprazolam/Xanax
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EtOH withdrawl
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Valium/diazepam
Lorazepam Chloriazepoxide Oxazepam CLOVes CLOVes always help me be less anxious and stop drinking |
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Anxiety drugs
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Diazepam/Valium
Lorezapam/Ativan Chlordiazepoxide/Librium Oxazepam/Serax CLOVes |
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Benzodiazepine overdose drug
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Flumazenil
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CYP metabolized
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Alprazolam
Clonazepam Diazepam Chlorazepate Chlordiazepxide Buspirone |
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Metabolized by Glucuronidation
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Lorazepam 12 hr t1/2
Oxazepam 3-6h t1/2 Gluco LOx down the half life |
