Exam II Flashcards
This diagnosis is characterized by feelings of intense sadness and despair, mental slowing, loss of concentration, pessimistic worry, agitation and self-deprecation - what is it?
Major Depression
- an affective disorder, ie altered mood
What does the acronym SIGECAPS stand for?
changes noted in depression
S - sleep I - interest G - guilt E - energy C - concentration A - appetite P - psychomotor disturbance S - suicidal ideation
a chemical family including - dopamine - norepinephrine - serotonin what family is this and which drugs act on this family?
Monoamine neurotransmitters
- most antidepressants work on metabolism of these neurotransmitters and their receptor sites
All anti-depressants carry an increased risk of what?
Suicide*
black box warning on all antidepressants
can also lower the threshold for seizure
(especially in combination with alcohol)
These are:
- used less commonly than other anti-depressants (d/t serious side effect profile of: weakness, dizziness, severe HA, tremors and HYPERTENSIVE CRISIS)
what are they?
Monoamine Oxidase Inhibitors
- tranylcypromine / parmate
- phenelzine / nardil
- isocarcarboxazid / marplan
- selegiline
This amino acid has the ability to enter presynaptic terminals and inhibit serotonin, it can also do this in the blood vessels - it’s thought to displace NE from neuronal storage vesicles - which amino acid is it and why is this important?
tyramine
- MOAIs prevent breakdown of this AA which causes marked HTN with MAOIs
- found in all the good foods: cheese, soy, dried fruits, meat, wine - anyone on MAOIs must avoid these foods!
- fatal HTN emergencies have been reported when patients reported intake of tyramine containing foods with their MAOIs
Tyramine is thought to act directly as a neurotransmitter, through which recently discovered receptor?
TA1
a G protein-coupled receptor (high affinity for tyramine)
found in
- brain
- peripheral tissue
- kidney
The MOA is thought to
- diminish re-uptake of monoamine neurotransmitters, sp. Serotonin and NE (increasing amt of neurotransmitter in the synaptic cleft)
with subsequent down regulation of post-synaptic receptors (potentially the main action) - which drug class is this?
tricyclic antidepressants (TCAs)
amitriptyline / elavil
- generally taken at bedtime due to sedative effects.
- takes approx. 4 weeks to meet therapeutic dose (will not see results until this time)
The chief side effects of these are anti-cholinergic in nature - DRY MOUTH being one of the best known SEs, ALL have potential to be CARDIOTOXIC - which class is this?
tricyclic antidepressants (TCAs)
anti-cholinergic reminder:
- dry mouth
- constipation
- urinary hesitancy
- orthostatic hypotension
- sedation
What is most disconcerting about tricyclic and tetracyclic antidepressants?
dangerous in OVERDOSE
- 10x daily dose can be fatal
- generally due to prolongation of QT interval.
- a week’s supply taken at once can be fatal for many individuals.
this tricyclic antidepressant works primarily on the serotonin transporter, moderately on the NE transport to effectively increase both in synapse.
Generally taken PO or IM. Which drug is this and can it be stopped abruptly?
Amitriptyline/Elavil
- stopping treatment abruptly causes withdrawal-like symptoms:
N, HA, dizziness, lethargy, flu-like sx
ie - discontinuation syndrome
This tetracyclic is a potent antagonist of
- 5-HT2, 5-HT3 and Histamine (H1) receptors
- creates prominent sedative effects.
A moderate antagonist of peripheral alpha-1 adrenergeic receptors explaining a common side effected noted with it’s use - what drug is it and what’s the side effect?
Remeron / Mirtazapine
S/E: occasional orthostatic hypotension
Another common SE of TeCAs is WEIGHT GAIN
this tetracyclic works as a serotonin reuptake inhibitor and partial antagonist (decreases serotonin at pre-synaptic and increases at post-synaptic R sites)
- it’s an ANXIOLYTIC and induces sleep - which drug is this?
Trazodone / Desyrel
This TeCA has off-label indications for use with:
fibromyalgia, complex regional pain syndrome, control of nightmares, panic disorder, diabetic neuropathy, bulimia nervosa, OCD, alcohol withdrawal and - best yet - ERECTILE DYSFUNCTION - what drug is this and what significant SEs should be noted?
Trazodone / Desyrel
- HYPOTENSION - fatalities are rare
- possible MANIA in patients w/ bipolar
Appears to be safer than TCAs and MAOIs
This class of drugs has been helpful in 50-70% of patients with major depression, it’s the most commonly prescribe anti-depressant - their full effect takes 3-8 weeks or more before a patient finds relief - what drug class is this and what two neuro-protective proteins increase as the hypothesized “downstream” effect of their action?
SSRIs
increases in serotonin lead to increased neuro-protective proteins:
- Brain-Derived Neurotrophic Factor (BDNF) and
- Bc1-2
Many users of SSRIs complain of apathy, lack of motivation, emotional numbness, feelings of detachment and indifference to surroundings - SSRIs, SNRIs and serotonergic TCAs can all cause this to varying degrees - what is the term for this notorious side effect?
mood anesthesia
- ie emotional blunting
- All SSRIs also come with the side effect of
sexual dysfunction
This SSRI decreases serotonin re-uptake at presynaptic cleft allowing for increased serotonin in the synapse and at post-synaptic R sites
- it is the antidepressant drug of choice for CHILDREN and TEENS. This drug is generally given PO, with a half life of 48-72 hours - what drug is this?
Fluoxetine / Prozac
- kid friendly, mother approved?
- SE: Serotonin syndrome (fever, agitation, diarrhea, HTN)
Painkillers of what family may interfere and reduce the efficiency of SSRIs and may compound the increased risk for GI bleed caused by SSRI use - these agents are?
NSAIDs
- aspirin
- ibuprofen
- naproxen (aleve)
The effects of this SNRI drug are dose-dependent
- low dose (<150 mg/day) acts on serotonergic transmission
- moderate dose (>150mg/day) acts on serotonergic and noradrenergic systems
- high doses (>300mg/day) they affect dopaminergic neurotransmission
What drugs is this?
venlafaxine / effexor
- first and MC used SNRI
This SNRI is C/I for use in patients with heavy alcohol use OR chronic liver disease (can cause ACUTE HEPATITIS**) - used mainly for major depressive disorder, general anxiety disorder, painful peripheral neuropathy and fibromyalgia.
- approved in Canada and Europe for stress urinary incontinence, not approved by the US due to concern of liver toxicity and suicidal events.
What drug is this?
Duloxetine / Cymbalta
(SNRI)
- don’t forget
antidepressants increase the risk of suicidal thinking and behavior in children, adolescents and young adults (Black Box)
This SNRI the active metabolite of venlafaxine - evidence suggests a lower efficacy when using this compared to venlafaxine and duloxetine - what drug is this?
Desvenlafaxine / Pristiq
This NDRI (NE and dopamine) and nicotine receptor antagonist - is indicated for depression, bipolar disorder and ADD - however, under a separate brand name it also aids in smoking cessation. What drug is this? What is its separate brand name?
Bupriopion / Wellbutrin
As a smoking cessation drug:
Bupriopion / Zyban
- approved for up to 6 months to prevent relapse for those quitting.
Takes 5-7 days to reach steady state blood levels
- 150mg/day x 3 days
then bid each day to follow
This drug is
- a partial nicotine agonist indicated for smoking cessation
- has a serious SE profile of neuropsychiatric events such as mood disturbances, psychosis and hostility - occurring in those W and W/OUT PRE-EXISTING psychiatric disease.
In combination with nicotine withdrawal - incidence of neuropsychiatric events increases - what is the name of this drug that is NOT recommended, ever.
Varenicline / Chantix
“No chance you’ll prescribe Chantix” (cheesy, deal with it)
Marketed in the US as a “medical food.”
- indicated for management of suboptimal folate levels in depressed patients
- assumed MOA w- acts as a trimonoamine modulator (TMM) enhancing synthesis of:
dopamine, NE and serotonin
- boosts efficacy of antidepressants.
What is the name of this active form of folic acid, and what is the medical food brand name?
Levomefolic acid / Deplin
Activated name:
Levomefolic acid / methyltetrahydrofolate / 5-MTHF
Medical food name: Deplin
- substantial evidence suggests deficiency in folic acid is associated with depression