Exam 2- specific meds Flashcards
FDA approved first line meds for panic disorder and then preferred/why?
FDA approved SSRIs: fluoxetine (Prozac), paroxetine (Paxil, Pexeva) and sertraline (Zoloft)
FDA approved SNRI: venlafaxine
preferred: escitalopram, citalopram, sertraline bc lower drug/drug interactions and decreased SEs
Contraindications/considerations for TCAs
narrow angle glaucoma, BPH, cardiac (increases risk arrhythmias), elderly (falls/sedation/orthostasis), toxic in OD
Baseline ECG
Benefit SSRI w/ BZO augmentation in panic disorder
Accelerates speed of response
BZO adjunct for 3-4 weeks until SSRI works if compromising ability to function
Which BZOs indicated for panic disorder
alprazolam, clonazepam, diazepam, lorazepam
fluoxetine (class, indications, neurobiology, how long until works, best augmentation, SE)
class: SSRI
indications:
MDD, OCD, PMDD, *bulimia, panic disorder, bipolar (esp. w/ olanzazpine), social anxiety, PTSD)
neurobiology:
block serotonin re-uptake pump to increase 5-HT; desensitize 5-HT1A receptors; antagonizes 5HT2c receptors = increase NE & DA
how long until works:
2-4 weeks
best augmentation:
trazodone for insomnia
BZO for anxiety
hypnotics for insomnia
mood stabilizers or atypical antipsychotics for bipolar, tx resistant anxiety or depression
(olanzapine specifically)
SE:
increase anxiety/energy/activation early in tx (d/t 5HT2c antagonist properties)
insomnia & other CNS
GI
sexual dysfunction
autonomic (sweating)
rare- seizures
weight gain but not expected
bleeding/bruising
What to do if SSRI SE
wait
take in am if activating
*try another SSRI before augmenting
augment w/ meds for specific sx
decrease dose, if tolerated/effective increase again
escitalopram (indications, neurobiology, how long until works, best augmentation, SE, Pearls)
class: SSRI
indications:
MDD, GAD, panic disorder, OCD, PTSD, social anxiety, PMDD
neurobiology:
block serotonin re-uptake pump to increase 5-HT; desensitize 5-HT1A receptors
how long until works:
2-4 weeks
best augmentation:
trazodone for insomnia
BZO for anxiety
hypnotics for insomnia
mood stabilizers or atypical antipsychotics for bipolar, tx resistant anxiety or depression
SE:
all r/t serotonin reuptake blockade
insomnia & other CNS
GI
sexual dysfunction
autonomic (sweating)
rare- seizures
weight gain but not expected
hyponatremia in elderly
bleeding/bruising
Pearls:
one of best tolerated SSRI
paroxetine (class, indications, neurobiology, how long until works, best augmentation, SE, Pearls)
class: SSRI
indications:
MDD, OCD, social anxiety, panic disorder, PTSD, GAD, PMDD, vasomotor sx
neurobiology:
block serotonin re-uptake pump to increase 5-HT; desensitize 5-HT1A receptors
mild anticholinergic
mild NE reuptake blocking actions
how long until works:
for anxiety/insomnia may be early relief
2-4 weeks
best augmentation:
trazodone for insomnia
BZO for anxiety
hypnotics for insomnia
mood stabilizers or atypical antipsychotics for bipolar, tx resistant anxiety or depression
SE:
anticholinergic
GI
sexual dysfunction
autonomic (sweating)
rare- seizures
weight gain but not expected
hyponatremia in elderly
bleeding/bruising
Pearls:
more likely withdrawal effects
anticholinergic effects make anxiolytic/hypnotic effects more rapid but then cause anticholinergic SE
sertraline (class, indications, neurobiology, how long until works, best augmentation, SE, Pearls)
Class: SSRI
indications:
MDD, PMDD, panic disorder, PTSD, social anxiety, OCD, GAD
neurobiology:
block serotonin re-uptake pump to increase 5-HT; desensitize 5-HT1A receptors
block DA reuptake pump
binds at sigma 1 receptors
how long until works:
2-4 weeks
best augmentation:
trazodone for insomnia
commonly with bupropion
BZO for anxiety
hypnotics for insomnia
mood stabilizers or atypical antipsychotics for bipolar, tx resistant anxiety or depression
SE:
increase anxiety/energy/activation early in tx
anticholinergic
GI
sexual dysfunction
autonomic (sweating)
rare- seizures
weight gain but not expected
rare- hyponatremia in elderly
rare- hypotension
bleeding/bruising
Pearls:
activating
best cardiovascular safety in class
sigma 1 receptor binding may enhance anxiolytic effects
more GI effects esp. diarrhea
venlafaxine (class, indications, neurobiology, how long until works, best augmentation, SE, Pearls)
class: SNRI
indications:
depression, GAD, social anxiety, panic disorder
non FDA: PTSD, PMDD
neurobiology:
blocks NE, 5HT, DA reuptake pumps so increases them; desensitizes 5ht1a receptors and beta adrenergic receptors; increase DA in frontal cortex
how long until works:
2-4 weeks
best augmentation:
*mirtazapine (powerful dual 5HT and NE combo; can activate bipolar or SI)
trazodone for insomnia
BZO for anxiety
hypnotics for insomnia
mood stabilizers or atypical antipsychotics for bipolar, tx resistant anxiety or depression
SE:
dose-dependent increase BP
HA, nervousness, insomnia, sedation
nausea, diarrhea, decreased appetite
sexual
asthenia, sweating
hyponatremia
SIADH
rare- weight gain & sedation
Pearls:
check/monitor BP before/during tx
OD lethal
withdrawal more common/severe
caution in cardiac, lower dose w/ renal/hepatic
alprazolam (class, indications, neurobiology, how long until works, best augmentation, tests, SE, Pearls)
class: benzo/GABA positive allosteric modulator
indications:
FDA approved: GAD and panic disorder
not: other anxiety disorders, PMDD, IBS, insomnia, adjunct for acute mania/psychosis, catatonia
neurobiology:
binds to benzo receptors at GABA-A ligand-gated Cl channel complex (increases GABA inhibitory effect); inhibits neuronal activity in amygdala-centered fear circuits
how long until works:
immediate relief w/ first dosing
several weeks with daily dosing
should only be short-term or PRN
best augmentation:
benzos used to augment SSRI/SNRI in psychotic/bipolar disorders
used to augment SSRI/SNRI in anxiety
could augment w/ gbapentin or pregabalin
Tests:
concomitant medical illness, long-term meds, seizures- periodic LFTs and blood counts prudent
SE:
sedation, fatigue, depression
dizziness, ataxia, slurred speech, weak
forgetful, confusion
hyperexcitability, nervousness
rare- hallucinations, hypotension, hypersalivation, dry mouth, respiratory depression, hepatic or renal dysfunction
Pearls:
short half life
dependence in tx > 12 weeks
seizures upon abrupt discontinuation esp. > 4mg
clonazepam (class, indications, neurobiology, how long until works, best augmentation, tests, SE, Pearls)
class: benzo/GABA positive allosteric modulator
indications:
FDA approved: GAD, panic disorder (w/ or w/o agoraphobia), Lennox-Gastaut syndrome, Akinetic, seizure, myoclonic seizure, absence seizure
not: other seizure disorders, insomnia, adjunct for acute mania/psychosis, catatonia
neurobiology:
binds to benzo receptors at GABA-A ligand-gated Cl channel complex (increases GABA inhibitory effect); inhibits neuronal activity in amygdala-centered fear circuits
how long until works:
immediate relief w/ first dosing
several weeks with daily dosing
should only be short-term or PRN
best augmentation:
benzos used to augment SSRI/SNRI in psychotic/bipolar disorders
used to augment SSRI/SNRI in anxiety
could augment w/ gbapentin or pregabalin
Tests:
concomitant medical illness, long-term meds, seizures- periodic LFTs and blood counts prudent
SE:
sedation, fatigue, depression
dizziness, ataxia, slurred speech, weak
forgetful, confusion
hyperexcitability, nervousness
rare- hallucinations, hypotension, hypersalivation, dry mouth, respiratory depression, hepatic or renal dysfunction
Pearls:
long half life
easier to taper
less abuse potential
dependence in tx but less than others
“longer-acting alprazolam-like anxiolytic”
trazodone (class, indications, neurobiology, how long until works, best augmentation, SE, Pearls)
class: SARI (serotonin 2 antagonist/reuptake inhibitor)
indications:
FDA: depression
not: insomnia, anxiety
neuro:
potently block 5HT2a receptors; blocks 5HT reuptake pump
also works on alpha 1 receptors
how long until works:
in insomnia= immediate
2-4 weeks
best augmentation:
can be combined w/ benzos in difficult insomnia
can boost many other antidepressants
SE:
**sedation d/t anthistamine
block **alpha 1 adrenergic receptors= dizziness, sedation, hypotension (anticholinergic)
n/v, edema, blurred vision, HA
hypotension, syncope
sinus bradycardia
rare- **priaprism, seizure, mania
Pearls:
SSRIs may raise levels
not dependence-forming
no sexual (rare) or weight gain SE
social anxiety disorder tx (non pharm, FDA & non-FDA approved, first line, second line, adjunct)
non pharm: CBT
FDA:
SSRIs first line- paroxetine, sertraline, fluvoxamine. SNRI- venlafaxine
Non FDA:
fluoxetine, escitalopram, citalopram
adjunct:
*clonazepam, alprazolam,
2nd/3rd line: MAOI phenelzine, beta adrenergic blocker propranolol, buspirone, gabapentin & pregabalin, atypical antipsychotics olanzapine & quetiapine
What SE concerns with SSRIs in elderly? what SSRIs preferred in elderly/why?
SE concerns: impaired gait, GI bleed, bone loss, low Na levels
preferred= sertraline & escitalopram d/t safer SE profile
concerns with pregabalin and benzos in elderly
increased risk of falls d/t dizziness/sedation
benzos= decreased respiratory drive, auto accidents
All SSRIs/SNRIs are category C pregnancy risk except which one that is category D and why?
paroxetine= atrial septal defects
Should you use antidepressants like SSRIs in bipolar depression with comorbid anxiety? Why/why not?
NO even though GAD rates higher in bipolar
especially if rapid cycling/mixed because of greater mood destabilization
What meds are recommended for bipolar depression & then what meds in addition for comorbid GAD?
Bipolar depression:
lithium
quetiapine
lurasidone
lamotrigine
GAD with bipolar add:
hydroxyzine
pregabalin
benzos
MOA of benzos
GABA-a allosteric modulator; therefore doesn’t directly bind to GABA which then modulates the GABA-a receptor, increases *frequency of Cl channel opening
What are ZZZ drugs & what are they used for? MAO?
ZZZ drugs are hypnotics used for sleep; they’re modified benzos that are agonists on BZ-1 binding site & selective alpha 1 GABA-a receptors
zolpidem (Ambien), zaleplon, eszopiclone (Lunesta)
how do ZZZ drugs differ from benzos?
ZZZ drugs target alpha 1 subunit of GABA-a receptors & don’t have the anticonvulsant, anxiolytic, muscle-relaxant effects of benzos
SE of ZZZ drugs
residual am sleepiness, amnesia, abuse potential
drowsiness, HA, dizziness, GI
What med for benzo OD? SE concern? What if mixed with other substances?
Flumazenil
antagonist at GABA-a receptor
can precipitate withdrawal and cause seizures
If mixed with other substances (alcohol, opioids, barbiturates) it won’t reverse respiratory depression
barbiturates MAO, use, SE, & meds
low dose > facilitate GABA binding
high dose > directly opens GABA
use= mostly for seizures & w/ anesthesia; RARELY for anxiety/sedation
SE= withdrawal causes seizures more than benzos
CNS depression
tolerance, dependence, abuse
Ton of drug interactions
long acting= phenobarbital
short/intermediate= pentobarbital, secobarbital
ultra short= thiopental, methohexital
buspirone (MAO, use, SE)
5-HT1A partial agonist
adjunct for anxiety
SE: palpitations, tachycardia, GI, pupillary constriction
*NO sedation/abuse potential; minimal tolerance
Ramelteon (MAO & use/sleep onset or maintenance?)
MAO= melatonin agonist
use= circadian rhythm sleep disorders (often in patients who are blind & can’t regulate circadian rhythm)
*good for sleep ONSET
narcolepsy tx
modafinil
sleep tx 1st, 2nd, 3rd, last line
1st= non pharm/sleep hygiene
2nd= antihistamine, melatonin
3rd= trazodone, ZZZ drugs
Last= benzos
Management of nightmares in PTSD
r/o or manage other causes of sleep disturbance
first line= prazosin
prazosin (indication, MAO, effect)
first-line tx for PTSD symptoms including nightmares
alpha 1 antagonist; cross blood-brain barrier
Prazosin is thought to help by blocking the alpha1 receptor for norepinephrine
*non sedating
PTSD patient on prazosin, doing well with nightmares but still has trouble falling asleep. What do you consider first?
trazodone
eszopliclone (Lunesta)- class, indication, onset, dietary note, short or long term?
GABA-PAM (positive allosteric modulator)
- helps stay asleep
- onset within 1 hour
-high fat meals may slow absorption
- controlled med but not significant tolerance/dependence, can be used long term
zaleplon (Sonata)- class, indication, onset, short or long term?
- GABA-PAM, alpha 1 agonist GABA-A
- Approved for short term insomnia
- Onset less than 1 hour but short half-life
- Dependence with longer term tx, not intended for longer term use
Zolpidem (Ambien)- class, short or long term, SE, black box warning, dietary note
- Selectively binds to Omega-1 receptor on GABA-A receptor (responsible for sedation)
- Should be used for short-term of insomnia
- Less tolerance/dependence occurs with prolonged use (can still occur)
- Reports of anterograde amnesia, hallucinations, parasomnias (sleep walking, sleep eating) increased fall risk and GI effects
-** FDA Black Box Warning nighttime complex behaviors - *** take on empty stomach
ramelteon (Rozerem)- class, tolerance/dependence?
- Selective Melatonin (MT1 and MT2 agonist)
- Effective and safe sleep aid d/t no tolerance or dependence.
- DOES NOT Act on benzodiazepine receptors
Do non-benzo hypnotics affect REM sleep?
NOTE: Non-benzo hypnotics do not generally affect REM sleep.
Ramelteon SEs and notable drug/drug interaction
Interacts with fluvoxamine d/t CYP 1A2
SE: fatigue, dizziness, somnolence, mild elevation in prolactin w/ females, decrease in testosterone in males
no respiratory depression in mild-mod OSAH or mod COPD
Doxepin SE (low dose and high dose)
low dose: somnolence/sedation, nausea, URI
high dose: anticholinergic SE (so contraindicated in urinary retention or narrow-angle glaucoma), hypotension, dose-dependent cardiotoxicity
What are the FDA approved hypnotics?
Benzodiazepines (estazolam, flurazepam, quazepam, temazepam, triazolam)
The so-called “Z drugs” (eszopiclone, zaleplon, zolpidem)
A tricyclic antidepressant (doxepin)
Melatonin receptor agonists (ramelteon, tasimelteon)
Z drugs for sleep onset/initiation and short term/long term?
Zolpidem (ER can also treat sleep maintenance)
Zaleplon
*Short term use only
Z drugs for sleep maintenance and short term/long term?
Eszopiclone, can be used long term
Zolpidem ER can be used for onset and maintenance short term. SL can be taken at middle of the night awakenings as long as they can sleep 4 more hours
Doxepin drug class, used for sleep onset or maintenance?
TCA
insomnia with sleep maintenance
Are BZO usually for sleep onset or maintenance?
BOTH
FDA approved drugs for panic disorder
SSRIs: paroxetine, sertraline, fluoxetine
but all drugs in class have equal efficacy
SNRI: venlafaxine
What SSRIs may be preferred regardless of FDA approval due to lower SE profiles?
escitalopram, citalopram, sertraline
Drugs FDA approved for social anxiety disorder
SSRI: paroxetine, sertraline, fluvoxamine
SNRI: venlafaxine
Special SE considerations with SSRIs in social anxiety disorder
the SE sweating and sexual dysfunction may already be an issue in SAD and therefore, maybe exacerbated by SSRI
Most effective benzo for SAD (although NOT FDA approved)
clonazepam
What meds FDA approved for GAD?
SSRIs: Escitalopram (Lexapro) and paroxetine (Paxil) are FDA approved to treat GAD
However, all others in class can be used off label/same efficacy
Meds with FDA approval for PTSD
SSRIs: sertraline and paroxetine
what kind of drugs are gabapentin and pregabalin
alpha 2 ligands
