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50 Cards in this Set
- Front
- Back
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BZ1
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Sedation, anticonvulsant
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Zolpidem
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BZ1
Hypnotic |
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BZ2
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Antianxiety
Cognitive impairment Antianxiolytics |
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Flumazenil
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BZD antagonist
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Rx for generalized anxiety
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Begin w/BZD + SSRI then withdraw BZD after few weeks
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BZD Uses
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Anxiolytic
Sedative-hypnotic Anticonvulsant Skeletal mm relaxant |
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BZD MOA
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Enhance GABA's inhibitory action @CNS by interacting w/BZD receptor on GABA-A complex
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BZD PK
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Highly bound to plasma proteins
Don't induce hepatic microsomal enzymes Decreased oxidative biotransformation @old age, hepatic damage, other drugs leads to accumulation and increased duration of axn |
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BZD AEs
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Sedation
Tolerance for sedative, anticonvulsant axns CP450 interaxns Physical dependence (Sx@withdrawal) Abuse |
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Diazepam Uses
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Anxiety, insomnia, pre-op, mm relaxer
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Diazepam Class
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BZD
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Diazepam PK
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Fast absorption
P450->active metabolites->glucuronidation Long t1/2 |
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Diazepam Metabolites
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Active:Desmethyl-diazepam
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Chlordiazepoxide Uses
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EtOH detox
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Chlordiazepoxide PK
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Int. absorption,
P450->Active met.->glucuronidation Active-desmethyldiazepam Long half life |
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Flurazepam Uses
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Insomnia
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Flurazepam PK
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Int absorption
P450-active metabolites-glucuronidation converted immediately |
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Clonazepam Uses
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Panic disorder
Anxiety Seizure |
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Clonazepam PK
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Int absorption
Inactive metabolite Short t1/2 |
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Alprazolam Uses
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Panic
Anxiety |
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Alprazolam PK
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Fast absorption
Active metabolite Short t1/2 |
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Temazepam Uses
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Insomnia
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Temazepam PK
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Slow Absorption
Active met Short t1/2 |
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Lorazepam Uses
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Anxiety
EtOH detox Seizures |
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Lorazepam PK
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Int absorption
Glucuronidation Inactive metabolites |
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Oxazepam Uses
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EtOH detox
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Oxazepam PK
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Slow absorption
Glucuronidation Inactive metabolites short t1/2 |
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Azapriones MOA
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Partial agonists @5HT1A receptors
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Buspirone class
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Azaprione
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Buspirone PK
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Highly bound to plasma proteins (>90%)
Metabolized by hepatic ox to 1-pyrimidinyl piperazine (active) T1/2<3 hr Therapeutic lag |
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Buspirone Uses
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Acute anxiety
Nonsedating Doesn't potentiate EtOH |
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Buspirone AEs
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Pts maintained on BZDs don't like them and discontinue use
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Citalopram
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SSRI
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Fluoxetine
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SSRI
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Fluvoxamine
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SSRI
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Paroxetine
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SSRI
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Sertraline
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SSRI
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Situational anxiety Rx
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Beta blockers
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OCD Rx
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TCAs
SSRIs SNRI BZDs |
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Chlorimipramine
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TCA
Halogenated derivative of imipramine, more potents as a serotonin reuptake inhibitor Significant activity inhibiting NE reuptake AE: cardiac tox associated w/TCAs |
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Clomipramine
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TCA
Halogenated derivative of imipramine, more potents as a serotonin reuptake inhibitor Significant activity inhibiting NE reuptake AE: cardiac tox associated w/TCAs |
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SSRIs in OCD
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Equally effective, safer
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Venlafaxine
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SNRI
Block 5-HT reuptake w/in usual Rx dose range |
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BZDs in OCD
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adjunct
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Panic disorder Rx
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SSRIs
TCAs MAOIs BZDs |
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SSRIs in Panic disorder
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Drug of choice
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Imipramine
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TCA for panic disorder
2nd line |
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Phenelzine
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MAO irreversible inhibitor
2nd line for panic disorder |
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Alprazolam in panic disorder
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BZD
2nd line Doses much higher than for generalized anxiety disorder |
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Phobia disorder Rx
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PsychoRx
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