Antidepressants Flashcards

Selective serotonin reuptake inhibitor
Terms Definitions
Venlafaxine
SNRI
zoloft
sertraline
Citalopram
SSRI
paroxetine
PAXIL
Serzone
Nefazodone
depression
*priapism*
Elavil
Amitriptyline
Pamelor
nortriptyline
Fluvoxamine
Luvox-SSRI
Paroxetine
Paxil-SSRI
Mirtazepine
Antidepressant
Serotonin agent
weight gain
cymbalta
atypical antidepressant
Amitriptyline
TCA.Tertiary amines.
Effexor
venlafaxine (SSRI)
Lithium Salts
Bipolar disorder
name SNRIs
venlafaxine, duloxetine
Imipramine
TCA. Tertiary amines.
Imipramine
First Gen - TCA
Mirtazapine
adverse effects
Sedation (H1-mediated)
increased appetite/weight
occasional ortho hypo (alpha-1 block peripherally)
OD: safe
 
buproprion indications
smoking cessation, ADHD
Atypical antipsychotic + SSRI
Bipolar disorder
MAOI time to therapy
2-4 weeks
Name heterocyclic antidepressants.
Nefazadone, mirtazapine, venlafaxine.
Trazodone (Desyrel)
bloceks postsynaptic seotonin recetpors in addition to blocking the reuptake for serotonin. At high doses - 5HT receptor agonist
Venlafaxine
Mech/adverse/pkin/other
M: 5-HT reuptake inhibitor, NE reuptake @ higher dose
P: short T1/2
name serotonin antagonist and RIs
trazodone, nefazodone
_________ are used for treating depression and obsessive compulsive disorder
SSRIs
Trimipram
Unique mechanism! No alteration of reuptake or either serotonin or NE. Highly sedating.
Clomipramine
MOST selective for inhibition of serotonin reuptake. Indicated for Depression, and OCD. Adverse effect: Orthostatic hypotension
name TCA secondary amines
norepinephrine increase (desipramine, nortryptiline, amoxapine)
what are the MAOI antidepressants?
isocarboxazid, moclobemide, phenelzine, and tranylcypromine
how long do antidepressant drugs take to see a clinical effect?
4-6wks
Desipramine is the prototype for what group of Antidepressants?
Tricyclic
SSRI's
first line treatment for depression! Includes: Citalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline
Reversible inhibitor of MAO-A...? RIMA
Moclobemide (Manerix)
what are the serotonin norepinephrine reuptake inhibitors?
desvenlafaxine, duloxetine, mirtazapine, minacipran, and venlafaxine
Antidepressants whose effects no seen for weeks.
TCA and SSRI.
A group of mental illnesses that include depresson and manic-depression (bipolar disorder)
Affective disorders
What are MAOI side effects?
Orthostatic hypotension, hypertensive crisis, anorexia, dry mouth & impotence.
Irreversible inhibition of MAO A and B?
Phenelzine (Nardil)
TCA's contraindications.....
within 2 weeks of MAOI therapy, recovery following MI, lowers seizure threshold, potentiation of CNS depressants
Bupropion (wellbutrin/zyban)
weakly blocks NE reuptake and hight affinity for the dopamine transporter. USES: depression and smoking cessation. DO NOT use with seizure disorders
what are the selective serotonin reuptake inhibitors (decreased 5HT uptake >>> decreased NE uptake)?
citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline, and tianeptine
do not prescribe more than 1 wk supply of __
TCA
1. inhibits MAO, an enzyme that breaks down norepinephrine, dopamine and serotonin. ->allowing these neurotransmitters to accumulate at the synapse=leading to increased activation of postsynaptic receptors2. Inhibit oxidases responsi
Monoamine Oxidase(MAO)Inhibitors Mechanism of Action
What are they used for?
Affective disorder - depression, smoking cessation - Wellbutrin.
Sertraline (Zoloft)
might be less likely to have metabolic drug interactions
Serotonin Syndrome
causes, sx
Cause: too much serotonin due to combo of SSRIs/tricyclics with other drugs, St. John's Wort
Sx: Seizures, CV instability, hyperthermia, myoclonus
what are the anticholinergic ADRs associated w/TCAs?
blurred vision, paralysis of accommodation (may precipitate glaucoma attack in pts w/narrow-angle glaucoma), constipation, urinary retention, dry mouth.
What are the OT Implications (3 parts)?
Antimuscarinic effects:Dry mouth=need water, blurred vision=color code,constipation=increase fiber intake, urinary retentionCVS:cardiac arrhythmias=monitor BP, orthostatic hypotension=avoid sudden mvmt, reflex tachycardia=decrease exercise stressCNS:sedation and headache=time tx for time pt has decreased effects
Norepinephrine selective reuptake inhibitors (NRI's)
Less likely to trigger mania, or seizures. Atomoxetine (Strattera) Uses: ADHD and off label for depression. Adverse: GI and CNS - diarrhea, abdominal pain, drowsiness, fatigue
what is the effect of TCA administration?
alpha-1 adrenergic blocking activity, anticholinergic (greater w/tertiary TCAs), blockade of presynaptic reuptake: primarily 5HT for tertiary TCAs and primarily NE for secondary TCAs.
SE: sexual problem (loss of desire, impaired arousal, delayed/impaired ejaculation or orgasm)
All SSRI. Venlafaxine.Paroxetine has highest rate.Can be minimized by "drug holidays" (skip one day dose and resume in 2 days. Could reduce efficacy or lead to serotonin withdrawal symptoms (dizziness, depressed, nausea, confusion).
what are the CNS ADRs associated w/TCAs?
confusion, delirium, sedation (> 30% in pts >50 y/o - more likely w/tertiary TCAs), dizziness, hypomanic/manic excitement (switch process), seizures (more w/maprotiline), tremors (10%)
What are SSRI & 2nd generation side effects?
Insomnia, weight gain, sexual dysfunction, GI symptoms, Serotonin syndrome - delirium, agitation, tachycardia, sweating, myoclonus - involuntary twitching & shivering.
Which MAO treats what illness?MAO A treats__________MAO B treats__________
MAO A =for depressionMAO B =for Parkinson's
Duloxetine
SNRI
lexapro
escitalopram
Fluoxetine
SSRI
Fluvoxamine
SSRI
*TCAs
ElavilDeserylTrofanilAnafranil
Celexas
Citalopram
Depression
*sedation*
(SSRI)
Klonopin
Clonazepam
Remeron
Mirtapine
Prozac
fluoxetine
Citalopram
Celexa-SSRI
Nefazodone
Heterocyclics.3rd generation.
Parnate
Trancylcypromine
Depression
*insomnia, hypotension, hypertensive crisis*
MAO inhibitors
Celexa
citalopram (SSRI)
Fluoxetine
Prozac
SSRI
s/e: nausea, sexual
OCD medical treatment
clomipramine
Bupropion
Heterocyclics.2nd generation atypicals.
Amoxapine
Second Gen - TCA
Trazodone, nefazodone
Mech/adverse/pkin/ddi/other
M:presynaptic 5-HT receptor antagonist, histamine antagonist, weak 5-HT reuptake inhibitor
A: strong hypnotic, priapism, limited sex dysfxn, OD: hypotension, excessive sedation, seizure for nefazodone
Pkin/DDI: Short t1/2, substrate/inhibitor of CYP
Other: trazodone best to induce sleep,
Nefazodone effective as SSRIs, less sexual dysfxn, more hypnotic
 
name TCAs
amitriptyline, imipramine, clomipramine, nortriptyline
Lamotrigine
Decreased glutamate release and modulation of voltage-gated calcium/sodium channels; Anticonvulsant; used with bipolar depression as well (w/o mania); SLOW titration and contraindicated in pregnancy (fast titration = SJ syndrome)
mirtazapine main advantage
no sexual dysfunction
Venlafaxine: MOA
Heterocyclic class.5-HT reuptake inhibitor at low dose (like SSRI), but NE reuptake inhibitor at high doses.
Other uses of TCs
Clomipramine - OCD
Anxiety
Enuresis
Chronic Pain
ADHD (Atomoxetine [Straterra])
Smoking Cessation
AE: rash, steven johnson syndrome (10%)
lamotrigine
Monoamine Oxidase(MAO)Inhibitors:Administration?Onset of action?Contraindications?
1. Active orally2. Slow onset...minimum of 2 weeks3. Pts should avoid high tyramine foods(i.e. cheese, salami, chocolate, wine, beer, chicken liver, yogurt, etc) because of risk of hypertensive crisis
Monoamine Oxidase Inhibitors
Phenelzine (Nardil), Tranylcypromine (parnate) Moclobemide (Manerix), Selegiline (for parkinsons)
serotonin rebound
from abrupt cessation of SSRIs (discontinuation syndrome), common in paroxetine and venlafaxine
what are possible drug interactions for MAOI pts?
amphetamine/cocaine/buspirone/L-dopa (increased risk of HTN), meperidine/related narcotics (increased risk of hyperpyrexia), dextromethorphan (increased risk of psychosis), alcohol/anticholinergics/antihistamines (increases peak/duration of effect)
Selective for MAO-B and also an antiparkinsonism agent.
Selegiline.
Common Comorbid Conditions with Bipolar
substance abuseOCDpanic disorderbulimia
Reversibly inhibits MAO A and B...?
Tranylcypromine (Parnate)
Heterocyclics, 3rd generation includes:
Mirtazapine and venlafaxine (effexor)
what are possible clinical consequences of blocking alpha 1 adrenergic receptors?
potentiation of antihypertensive effect of labetalol etc, postural hypotension, dizziness, reflex tachycardia
Name 3 specific TCA's worth knowing
 
How long does it take for the TCA's to have therapeutic effects?
Amitriptyline (Elavil)
Clomipramine (Anafranil)
Nortriptyline (Pamelor)
 
Therapeutic effect begins only after 3-4 weeks of administration
TCA antidepressant MOA.
Inhibits reuptake of NE and 5-HT
Lithium salts work well but take time to kick in so be sure to ______ pt. closely
watch
Cetalopram (Celexa)
may be good for menopausal hot flashes
Tricyclic antidepressants
now considered 2nd line agents, are related to the antipsychotic phenothiazines. All agents have adrenergic, histamininc and muscarinic side effects. (ie: dry mouth, sedation, urinary retention, constipation, hpyotension and cardiac arrhthmias
Venlafaxine (effexor)
works as SSRI. Low activity at histamine , muscarinic or adrenergic recptors. Can cause N sweating dizziness and somnolence
SSRI other uses, Discontinuation
PMDD - fluoxetine
OCD - fluoxetine, fluvoxamine
GAD & Phobia - paroxetine
Bulimia Nervosa - fluoxetine
Discontinuation - grip of side effects for 1-several weeks
MOA of...
1. trazodone
2. buproprion
3. venlafaxine
4. SSRIs
1. trazodone: blocks 5-HT2 receptors and reuptake
2. buproprion: blocks NE and DA reuptake
3. venlafaxine: blocks NE and 5-HT reuptake
4. SSRIs: blocks NE and 5-HT reuptake
Clinical depression is characterized by:
Intense feelings of sadness, hoplessness, despair and the inability to find pleasure in usual activities
Fluoxetine (Prozac)
only one FDA approved for peds. also used for depression, anxiety, OCD, bulimia, panic, PMDD, PTSD. Do not give within 2 weeks of MAOI therapy, of the thioredazine
Treatment of a HTN crisis....
5 mgs of phentolamine IV
anti-depressants and increased suicide?
yes, but does not make people suicidal; just gives them the motivation to carry out the act
Lithium salts (Lithobid, Lithonate)Mechanism of action?Helps with...Administration?Side Effects?
1. EXACT Mech of Action is UNKNOWN2.relief from signs and symptoms of Mania *stabilizes mood 3. Active orally4. Ataxia, tremors, confusion and convulsions***HAS A NARROW THERAPEUTIC INDEX
what actions do SSRIs have less of?
histamine, muscarinic, and alpha-1 blocking action - but these are not necessary to tx depression and the lack thereof may make SSRIs more attractive to some pts.
Side effect of Imipramine (and most TCA).
Excessive sedation; 2ndary amines cause less sedation than tertiary amines.Antichoinergic: blurred vision, dry mouth, urinary retention, constipation, agigation, tachycardia, sweating (amitriptyline produces the most severe anticholinergic effects).Alpha1 blockade: Postural hypotension, tachycardia.Additive depression of CNS w/ ethanol, barbiturates.OD:resp depression, convulsion, arrhythmias, coma.
SARIs
 
What is it, and how is it different from an SSRI?
 
Indications
Adverse effects
Serotonin Antagonist & Reuptake Inhibitors
 
Its an SSRI that also blocks the 5HT2A-R (overall, its less activating and more sedating than the SSRI's)
 
Used to treat depression, anxiety, insomnia
AND no associated weight gain OR sexual dysfunction!
 
Adverse:  Sedation, orthostatic hypotention, priapism (rare)
 
Yet its rarely used, not 1st line
what characterizes duloxetine - an SNRI?
strong inhibitor of both 5-HT and NE, weak inhibition of DA reuptake, and low affinity for histamine and muscarinic receptors. indicated for depression *and stress urinary incontinence and pain related to DM neuropathy. t1/2: 10-15 hrs.
1. MAO-A metabolizes __2. MAO-B metabolizes __
1. A -> 5-HT, tyramine2. B -> NE, epi
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