T/F: Some adverse effects of Buspar (Buspirone) are tolerance, dependency, CNS depression, & sedation.
False. Buspar does not cause tolerance or dependency, and it does not have any anticonvulsive or muscle relaxant qualities that would lead to depression or sedation.
What is Buspar (buspirone) indicated for?
Generalized anxiety disorder (mild to moderate intensity)
Depression w/overlay of anxiety or agitation (give with SSRI or SNRI)
Situational anxiety that is long-lasting
Buspar contraindications?
Benzodiazepine withdrawal
Unable to adhere to multiple daily dosing
Serotonin syndrome risk w/MAOIs & SSRIs
Panic ATTACKS (prolonged onset of 2-6weeks)
Anxiety ATTACKS
Renal or hepatic disease (severe)
What is the MOA for Buspar (Buspirone)?
partial serotonin receptor agonist
(Serotonergic Anxiolytic)
Buspirone acts as an agonist at presynaptic serotonin receptors, opens channel & permits serotonin binding (inhibits neuron firing)
T/F: Buspar (Buspirone) is good for those with a history of substance abuse.
True.
T/F: Although Buspar (Buspirone) does not lead to tolerance or dependency, it has a lot of side effects, and is not well tolerated.
False. The side effects are few and resolve with continued use.
Light-headedness, HA, insomnia, nausea, nervousness, & dry mouth
RARE - akathisia & involuntary movements
Why is Buspar (Buspirone) not used with panic attacks?
A metabolite has noradrenergic (norepi) effects
What type of drug is Alprazolam (Xanax)?
short-acting anxiolytic of Benzodiazepine drug class, "gaba-ergic"
decreases neuronal excitation by increasing the action of GABA (an inhibitory NT)
T/F: Xanax (alprazolam) is likely to cause dependency.
True. High potency & rapid action make it likely.
Over time, need higher dosage. Abrupt withdrawal causes anxiety/panic (so taper off).
Xanax (alprazolam) is indicated for treatment of...
anxiety and insomnia (main one)
Alprazolam also possesses sedative, hypnotic, skeletal muscle relaxant, anticonvulsant, and amnestic properties.
· muscle relaxant
· pre-anesthesia sedation
· prevention & tx of panic attacks
· acute agitaion
· dystonia
· emergency tx of uncontrollable seizures
· tx of RLS
What do benzodiazepine drugs do?
work on chloride ion channels of GABAA receptors. They enhance GABA neurotransmission which lengthens hyperpolarization and slows down responses.
T/F: Withdrawal symptoms occur within 1-2 days after last dose of Xanax (alprazolam).
True.
S&S of WD: insomnia, agitation, anxiety, & rarely seizures
What are contraindications for benzodiazepines? (Xanax, Serax, Klonopin)
Pregnancy & Lactation
Hepatic or Renal Disease
Children <6
Acute narrow-angle glaucoma
T/F: Benzodiazepines (xanax, serax, klonopin) can be prescribed for an elderly patient.
Yes, but remember to decrease the dose (decreased metabolism)
What are the major adverse effects of Benzodiazepines (xanax, serax, klonopin)?
· additive effects with other CNS depressants (barbituates, alcohol, antihistamines, neuroleptics)
Benzodiazepines (Xanax, Klonopin, Serax) can cause increased drug levels of
TCAs or digitalis
Labs needed to monitor for Xanax
Liver function, CBC
What drug will increase Haldol levels due to competitive metabolism?
Buspar (buspirone)
What might happen if you give Buspar (buspirone) with Trazadone?
increased ALT
In what drug class is Prozac (fluoxetine)?
SSRI
What is Prozac (fluoxetine) indicated for?
Bulimia
Major depression
Premenstrual dysphoric disorderOCDPanic disorder
T/F: You should see results of antidepressants in less than 3 weeks.
False. Response in <3 weeks is a placebo effect.
How long does it take Prozac (fluoxetine) to reach steady state?
~1 month
What do antidepressants have a black box warning for?
antidepressants may increase the risk of suicide in people younger than 25
most likely to occur in first 2 months of tx
MOA for Prozac?
SSRI
NE (0), 5-HT (+++++), ACh (+), H (+), a1 (+)
Metabolism of Prozac (fluoxetine)?
Liver via cytochrome P450
caution in elderly, liver dysfunction
Half-life of Prozac (fluoxetine)?
2-7d (longest for SSRIs)
slow elimination distinguishes it from other antidepressants
ONLY SSRI THAT DOES NOT REQUIRE SLOW TAPER OF DOSE
T/F: You have to taper Prozac gradually when stopping treatment, as it can result in abrupt withdrawal syndrome if stopped suddenly .
False. Side effects of the fluoxetine discontinuation are uncommon and mild. One of the recommended strategies for the management of discontinuation syndrome with other SSRIs is to substitute fluoxetine for the original agent, in cases where tapering off the dose of the original SSRI is ineffective
What pregnancy category is Prozac?
C (epocrates), B (ppt slide)
(not recommended during lactation)
T/F: It is best to give Prozac before bed due to the sedation side effect.
Fasle. It will cause insomnia, so it is best to take it in the morning.
Major contraindication for fluoxetine (Prozac)?
MAOI - either concurrent or within 14 days
What is a fatal side effect of Prozac?
Serotonin syndrome if given with triptans, tramadol or other serotonergic agents (antidepressants, dopamine agonists, analgesics)
What are some S&S of serotonin syndrome and when do you see them?
T/F: You can start an MAOI in someone that has been off Prozac as long as it has been at ≥ 2 weeks.
No, 5-6 weeks should elapse after discontinuing a SSRI and starting a MAOI
T/F: Prozac (fluoxetine) is not associated with GI disturbances.
False. GI disturbances are common.
With Prozac, treatment usually works well at first, but as side effects develop the efficacy diminishes.
False. Side effects come first (onset in hours to days) and therapeutic effects can take up to 4 to 6 weeks.
Is Prozac (fluoxetine) indicated for mania or bipolar disorder?
No. It can make them manic! Have to be careful because hypomania can mimic depression.
(S&S: hx of lots of energy, no sleep, risky behavior)
T/F: You should encourage pts to take NSAIDs for pain control when on Prozac (fluoxetine), as acetaminophen is a bad option due to additive liver side effects.
False! NSAIDs increase bleeding risk.
Also should not take ASA, Vit E, anticoagulants...
What drug class is escitalopram (Lexapro)?
SSRI
selectively inhibits serotonin reuptake
With Prozac, treatment usually works well at first, but as side effects develop the efficacy diminishes.
No. It can make them manic! Have to be careful because hypomania can mimic depression.
(S&S: hx of lots of energy, no sleep, risky behavior)
How do you d/c escitalopram (Lexapro)?
Titrate down slowly. ↓ by 50% for 3-4 days, then another 50% for 3/4 days.
How long will abrupt withdrawal syndrome last without intervention?
a couple of weeks
T/F: Routine vital signs and lab reports are needed in SSRI treatment for healthy individuals.
False. Need to watch electrolytes in the elderly.
T/F: Since antidepressants require an adequate trial of up to maximum dosing of 8 weeks, the first prescription should be written for 8 weeks.
False. Never give >4 weeks for the first perscription. You want to see them in 4 weeks to assess the response of the medication.
T/F: SSRI's (like Prozac or Lexapro) increase the risk of thromboemboli.
False. They increase the risk of bleeding.
2x the volume of blood loss during surgery
4x higher risk for blood transfusions
T/F: Escitalopram (Lexapro) causes sedation.
False. Insomnia.
What antidepressant do you avoid if sexual dysfunction is a concern?
SSRIs
70% of pts on Prozac develop sexual dysfunction
What drug class is phenelzine (Nardil) in?
MAOI
(MAO is an enzyme that metabolize dopamine, NE, 5HT)
Who should prescribe MAOIs (Nardil/phenelzine)?
a psychiatrist
low safety margin/potential lethal effects
What dietary problems result from MAOIs?
tyramine, phenylethylamine... ↑ HTN
Avoid tyramine-rich foods (yeast, yogurt, cheese, fish or meat, caviar, figs, bananas, raisins, avocados, wine, soy sauce)
Avoid foods with vasopressors too (fava beans, caffeine, chocolate, alcohol)
What is the big risky side effect of MAOIs (like Nardil)?
HTN/sympathomimetic crisis with concurrent anticholinergic, sympathomimetics, & stimulants
DO NOT GIVE WITH PROZAC
MAOIs are first-line treatment for depression but have a long half-life.
No. SSRIs or SNRIs are first-line treatment.
relatively SHORTER half-life
Treatment for MAOI HTN crisis?
Regitine (phentolamine)
Monitor what lab test for MAOIs?
LFTs, d/c if abnormal
Take their BP too!
Common ADRs of MAOIs
insomnia, anxiety, agitation (due to dopamine)
Anticholinergic SE (can't see, can't spit, can't pee, can't shit)
dizziness, HA, insomnia, restlessness, orthostatic hypotension
Your patient on Nardil (phenelzine) was just diagnosed with CAD on his 60th birthday. Also, he says, "Now that I'm 60, I'm gonna do whatever I want!". What's next?
MAOIs are contraindicated in arteriosclerotic disease or CHF, age ≥60, and in the impulsive, cognitively impaired, and those unable to follow the diet. Need to d/c, but need to taper down. Consult with psychiatrist.
PS- it's also CI for liver or kidney disease
What is the MOA of Klonopin (clonazepam)?
binds to benzodiazepine receptors; enhances GABA effects
What is clonazepam (Klonopin) indicated for and what class is it in?
a benzodiazepine drug (gaba-ergic)
Clonazepam (Klonopin) has anxiolytic, anticonvulsant, muscle relaxant, sedative, and hypnotic properties
Does clonazepam (Klonopin) cause dependency?
Yes. Tolerance, dependence, & withdrawal syndrome occur in 1/3 of people on clonazepam for > 4 weeks
PS-APN, what is clonazepam (Klonopin) used to treat?
Panic disorder
Seizure disorder
Anxiety
Periodic leg movement
Neuralgia
Major adverse reactions for clonazepam (Klonopin)?
Drowsiness and other CNS effects
Depression
"hangover effect" - long half life
sexual side effects
elevated LFTs
Contraindications of clonazepam (Klonopin)?
contraindicated if liver disease
pregnancy C
do not drink alcohol
In what drug class is oxazepam (Serax)?
Benzodiazepine (gaba-ergic)
What is an advantage of clonazepam (Klonopin)?
long half life means daily dosing
What is an advantage of Serax (oxazepam)?
good for detox, easy on liver
First-line therapy for anxiety?
SSRIs
Regarding SSRIs, which s/s resolve first (anxiety versus depression)?
Anxiety resolves earlier, but higher doses are needed for anxiety than for depression.
When is the full therapeutic effect of SSRIs realized?
