S54 - Pharmacology of Anxiety Disorders Flashcards
_____________ are the most effective and safe (relatively) for rapid relief of anxiety symptoms.
Benzodiazepines
BZD's clobazam (Onfi®) clonazepam (Klonopin®) clorazepate (Tranxene®) diazepam (Valium®) lorazepam (Ativan®)
_________ is an optional treatment in patients without comorbid depression or other anxiety disorders.
Buspirone (Buspar)
First Line therapy for Generalized Anxiethy Disorder (GAD)
Duloxetine (Cymbalta) Escitalopram (Lexapro) Paroxetine (Paxil) Sertraline (Zoloft) Venlafexine XR (Effexor)
First Line therapy for Panic Disorder
SSRI’s
- fluoxetine (Prozac)
- sertraline (Zoloft)
- paroxetine (Paxil)
- citalopram (Celexa)
- escitalopram (Lexapro)
- vortioxetine (Trintellix)
Venlafexine XR (Effexor)
First Line Therapy for Social Anxiety Disorder
Escitalopram (Lexapro) Paroxetine (Paxil) Sertraline (Zoloft) Venlafexine XR (Effexor) Fluvoxemine CR
Aytpical antipsychotics low-dose have been used for GAD –
Quetiapine 150 mg = paroxetine 20 mg/day.
Pregabalin is used in Europe as a first-line agent for GAD.
Off-label at best in the USA.
Not included into treatment algorithms.
Antidepressants are considered the first-line agents in GAD.
Duloxetine (Cymbalta) Escitalopram (Lexapro) Paroxetine (Paxil) Sertraline (Zoloft) Venlafexine XR (Effexor)
FDA approved for Generalized Anxiety Disorder (GAD)
Response is delayed 2-4 weeks.
paroxetine (Paxil)
duloxetine (Cymbalta)
venlafaxine (Effexor)
escitalopram (Lexapro)
________ is FDA approved for PD with or without agoraphobia.
Alprazolam (Xanax)
FDA Approved agents for acute anxiety
Alprazolam (Xanax) clonazepam (Klonopin®) clorazepate (Tranxene®) diazepam (Valium®) lorazepam (Ativan®) chlordiazepoxide (Librium) Oxazepam (Serax)
IM administration of diazepam and chlordiazepoxide should be AVOIDED –
erratic absorption and painful.
Which BZD’s are glucuronidated?
Only lorazepam and oxazepam are glucuronidated
Clonazepam undergoes
nitroreduction.
Diazepam is also metabolized by
CYP 2C19
__________ is a prodrug converted to DMDZ in the GI tract under acidic pH. Watch out for antacid use!
Clorazepate
Long-acting BZ are metabolized to desmethyldiazepam (DMDZ) – active metabolite.
BZ efficacy – 65-75% response rate within 2 weeks.
Only effective for the
somatic symptoms.
Unique to benzodiazepines where patient can become highly agitated and increased BZD’s increases agitation.
Disinhibition syndrome
_________ _________ – rebound anxiety with Increased symptoms greater than baseline.
Benzodiazepine discontinuation
BZD’s have drug interactions with:
CYP3A4 inhibitors (ketoconazole) and inducers (carbamazepine).
__________ – nonBZ without anticonvulsant, hypnotic, motor impairment or dependence .
Buspirone (Buspar)
2nd line agent for GAD.
Delayed onset > 2 weeks.
MOA: 5-HT1A partial agonist activity at presymaptic neurons ↓ firing of 5-HT neurons.
Do not use with MAOI’s for concern of serotonin syndrome.
Pregnancy avoids
Antidepressants (SSRI’s and TCA’s) are preferred agents for pregnant pts. except paroxetine.
Benzodiazepines (BZs) associated with cleft lip and cleft palate in babies.
Clinicians avoid BZs during the 1st trimester.
BZs use in the 3rd trimester: sedation, withdrawal and “floppy baby syndrome.”
Alprazolam and lorazepam reported to cause neonatal withdrawal symptoms.
Panic Disorder (PND)
SSRI’s are considered first-line due to safety and tolerability.
Combination of psychotherapy and drug therapy.
CBT is used 16-20 hrs over 4 months
Panic Disorder (PND) treatment duration
Acute phase TX. : 1-3 months, therapy altered if no response found 6-8 weeks.
Maintenance Tx. : 12-24 months, drug dc’d over 4-6 months.
Monitor for various issues – BZ dependence, SSRI withdrawal syndrome and etc