Antidepressants and Mood Stabilizers-Craviso Flashcards
1
Q
Currently available drugs are based on the (blank) hypothesis of depression
A
monoamine
2
Q
All the antidepressants cause immediate effects on synaptic (blank) levels
A
monoamine
3
Q
How long does it take for antidepressants to kick in? Why?
A
one or more weeks
-due to slow increase in expression of BDNF that promotes synaptogenesis
4
Q
Which antidepressant class is superior?
A
there isnt one
5
Q
At least (blank) percent of all depressed patient are refractory to multiple different antidepressants at adequate doses
A
20%
6
Q
What are the four major classes of antidepressant drugs?
What is the first line drug?
A
- SSRI
- SNRI
- MAOis
- New drugs
SSRI and SNRIs are first line drugs
7
Q
What do SSRIs work?
A
block 5-HT reuptake
8
Q
What are serotonin-norepinephrine reuptake inhibitors?
A
- newer “selective” inhibitors - block NE and 5-HT reuptake
- older, less selective inhibitors-tricyclics (TCA) that exert antagonist effects on a variety of receptors
9
Q
How do the newer antidepressants work?
A
- inhibit reuptake of dopamine
- agonist/antagonist activities at certain types of 5-HT and NE receptors
10
Q
How do Monamine oxidase inhibitors work?
A
inhibit the metabolism of NE and 5-HT
11
Q
What AA does serotonin come from?
What AA does NE come from?
A
tryptophan
tyrosine
12
Q
What are the five famous SSRIs (first line drugs)?
A
- Fluoxetine (prozac)
- Sertraline (Zoloft)
- Paroxetine (Paxil)
- Citalopram (Celexa)
- Escitalopram (Lexapro)
13
Q
How are SSRIs metabolized?
A
in the liver
14
Q
What are SSRIs potent inhibitors of?
A
several cytochrom P-450 enzymes (CYP2D6)
15
Q
Fluoxetine and Paroxetine are (low/high potential) cytochrome P450 inhibitors?
A
High potential
16
Q
Citalopram (celexa) and Escitalopram (lexapro) are (low/high potential) cytochrome P450 inhibitors?
A
low potential
17
Q
What are the adverse side effects of SSRIs?
A
- Signif sexual dysfunction
- Gi disturbance
- Insomnia, restlessness
- anorexia and weight loss (early treatment)
- Weight gain (long term)
18
Q
What SSRI can give you QT prolongation?
A
Citalopram
19
Q
Use of (blank) during pregnancy linked to an increased risk for cardiovascular
A
paroxetine
20
Q
How can you get 5-HT syndrome when giving SSRIs?
A
You give them with MAO inhibitors or other drugs that enhance 5-HT neurotransmission
21
Q
WHy dont you want to give antidepressants to children, adolescents and young adults really?
A
because it can worsen their depression (suicide)
22
Q
What is the only SSRI approved for use in children and adolescents?
A
Fluoxetine
23
Q
What is an SSRI approved for use in adolescents?
A
escitalopram
24
Q
What can you use SSRIs for other than treatment for depression?
A
- anxiety
- seasonal affective disorder
- bulimia nervosa
- migraine prophylactic
- PMS and PMDD, hot flashes
25
What SSRI do you give for seasonal affective disorder?
paroxetine
26
What SSRI do you give for bulimia nervosa?
fluoxetine
27
What SSRI do you give for PMS and PMDD (most); hot flashes?
paroxetine
28
What are the 2 newer "selective" inhibitors (SNRIs)?
Venlafaxine (effexor, effexor ER)
| Duloxetine (Cymbalta)
29
What does Venlafaxine do?
block reuptake of both NE and 5-HT
| -weakly inhibits DM uptake
30
What are the adverse SEs of Venlafaxine (effexor)?
resemble those of SSRIs (sexual dysfunction, GI, restlessness, insomnia)
31
What are some additional uses of Venlafaxine?
anxiety disorders
| -treatment of neuropathic pain
32
What are the adverse side effects of Duloxetine (cymbalta)?
contraindicated for those with chronic liver disease or hepatic insufficiency
33
What are some additional uses of Duloxetine (cymbalta)?
- management of fibriomyalgia
- management of diabetic peripheral neuropathy
- long term treatmetn of generalized anxiety disorder (GAD)
34
What do tricyclic antidepressants do ?
THey are old SNRIs and block the reuptake of both NE and 5-HT to varying degrees
35
What are the three important tricyclic antidepressants?
nortriptyline (aventyl, pamelor)
impiramine (tofranil)
amitriptyline (elavil)
36
What does nortriptyline (aventyl, pamelor) block mostly?
Norepinephrine (mostly) and seritonin (a little)
37
What does imipramine (tofranil) and amitryiptyline (Elavil) block mostly?
seritonin (mostly) and NE (a little)
38
Why arent tricyclic antidepressants first line drugs anymore?
- can be fatal in overdose
- are cardiotoxic
- lower seizure threshold
- have signif antagonist activity at several types of neurotransmitter receptors
39
WHo do you give tricyclic antidepressants to?
patients who do not respond or tolerate more widely-prescribed antidepressants.
40
What can amitriptyline be used for other than depression?
migraine prophylactic
41
Tricyclic antidepressants (TCAs) have more effects than blocking 5-HT and NE reuptake. What are the three other receptors that TCAs block?
mACh, alpha 1, histamine 1
42
What TCA blocks the mACh, alpha 1 and histamine 1 receptors the most?
amitriptyline (elavil)
43
What TCA blocks the mACh, alpha 1 and histamine 1 receptors the least?
nortriptyline (aventyl, pamelor)
44
What will blocking of mACh receptors cause?
- sedation
- cognitive impairment
- confusion
- delirium
- blurred vision
- dry mouth
- tachycardia
- urinary retention
45
What will blocking of alpha 1 receptors cause?
orthostatic hypotension
| sedation
46
What will blocking of histamine 1 receptors cause?
sedation
47
At therapeutic doses all TCAs can cause what SEs?
lowering of seizure threshold
sexual dysfunction
weight gain
48
So what is the worst TCA?
amitriptyline (elavil) (it can block too many things)
49
At toxic doses what can TCAs cause?
cardiotoxicity-(cardiac conduction delays Q-T prolongation, ventricular block, arrhythmias (ventricular tachycardia)
50
The therapeutic index for TCAs is (blank) and some patients may develop cardiotoxicity at therapeutic doses
low
51
Acute overdose of TCAs is often life-threatening due to .....?
- hyperpyrexia
- hypertension
- tachycardia
- arrhythmias
- severe anticholinergic effects
- convulsions
52
What drugs can cause drug interactions with TCAs?
- MAO inhibitors
- anticholinergics
- antihistamines
- CNS depressants
53
If you take a TCA with an MAOI at the same time, what can happen?
severe hypertension, rick of 5-HT syndrome
54
If you take a TCA with an anticholinergic or antihistamine, what can happen?
an additive effect due to blockade of mACH and H1 receptors by TCA
55
If you take a TCA with a CNS depressant, what can happen?
sedation
56
What is a well known dopamine reuptake inhibitor?
bupropion (wellbutrin)
57
Dopamine reuptake inhibitors such as bupropion can possibly block the reuptake of (blank and blank)
NE
| 5-HT
58
What are the adverse SEs of bupriopion (wellbutrin)?
- restlessness, insomnia, anxiety
- risk of seizure activity (dose-related)
- can precipitate psychotic episodes
59
What patients is buproprian (wellbutrin) contraindicated in?
patients with a history of seizures and eating disorders
60
How come bupropion (wellbutrin) can precipitate psychotic episodes?
excessive dopamine in susceptible individuals
61
Does bupropion (wellbutrin) have more or less sexual side effects compared to other antidepressants?
less
62
(blank) can be used as an aid in smoking cessation.
bupropion (sustained release formulation -Zyban)
63
What is the mechanism of action of Mirtazapine (Remeron)?
antagonist of central presynaptic alpha-2 adrenergic autoreceptors (receptors that mediate negative feedback for NE and 5-HT release i.e increase NE and 5-HT release)
-blockades 5HT2 an 5HT3 receptors
64
What are the adverse side effects of Mirtazapine (remeron)?
- sedation, somnolence
- dizziness
- stimulates appetite, signif weight gain
65
Does mirtazapine (remeron) have a lot of sexual side effects?
no
66
How does trazodone work?
blocks 5 ht reuptake
| -antagonist at 5HT2 receptors and partial agonist at 5HT1 receptors
67
What are some adverse SEs associated with Trazodone (Desyrel)?
- signif drowsiness and dizziness
- GI upset (nausea and vomiting)
- orthostatic hypotension
- protracted erection (priapism)
68
What is the mechanism of action of Vilazodone (Vibryd)?
a SSRI and a partia agonist at 5-HT1a receptors
69
What are the adverse effects of Vilazodone (vibryd)?
insomnia
| GI disturbances
70
Does Vilazodone (vibryd) cause sexual side effect and weight gain?
no
71
What are the three drugs with agonist/antagonist activities at certain types of 5-HT and NE receptors?
Vilazodone (Vibryd)
Trazodone (Desyrel)
Mirtazapine (Remeron)
72
What is MAO?
enzyme in nerve terminals that converts the monoamine neurotransmitters NE, 5-HT, and dopamine into inactive products
73
THere are 2 types of MAO, what does MAO-A metabolize?
NE and 5-HT
74
THere are 2 types of MOA, what does MAO-B metabolize?
dopamine
75
What is the last choice antidepressant? Why?
MAOI
| risk of hypertensive crisis in response to ingestion of certain foods (tyramine) and drugs during MAOI use.
76
What can you use MAOIs to treat other than depression?
Parkinson's disease
77
What happens if you are on an MAOI and then you eat tyramine?
tyramine will displace norepinephrine and you will get a hypertensive crisis
78
What is a MAOI that is a reversible inhibitor?
Selegiline (Eldepryl)
79
What is a MAOI that is an irreversible inhibitor?
Phenelzine (Nardil)
80
What is Ensam?
it is selegiline that is available transdermally
81
Why would you want to give selegiline transdermally (Ensam)?
so it can bypass the gut and inhibit central MAO enzymes wihile reducing the chance of hypertensive reactions caused by tyramine
82
What are the adverse side effects of phenelzine (nardil)?
- Anorgasmia or sexual impotence
- CNS stimulation (restlessness, insomnia)
- sleep disturbances (inhibit REM sleep)
- weight gain
- Orthostatic hypotension
83
You get drug interactions with MAOI when you take them with
- indirect acting sympathomimetics and tyramine-containing food (hypertensive crisis)
- SSRIs and 5-HT receptor agonists (5-HT syndrome)
84
If you see drug names with 2 Es and a ZINE or a LINE at the end what kind of drugs are they?
MAOIs
85
What characterizes a manic episode?
- exaggerated optimism and self-confidence
- decreased sleep w/out experiencing fatigue
- grandiose delusions, inflated sense of self-importance
- excessive irritability; aggressive behavior
- racing speech, flight of ideas
- easily distracted
- impulsiveness, poor judgement
- reckless behavior
86
Depressive and manic episodes last for several weeks to several months, often with (blank) in between swings
normal mood
87
What is considered rapid cycling in bipolar disorder?
more than 4 full cycles per year (rare)
88
What is the first line drug for acute mania and long-term maintenance therapy to avert manic and depressive episodes in patients with bipolar disorder?
lithium
89
What are the 2 types of lithium you can give?
```
lithium carbonate (Eskalith-CR)
lithium citrate (Cibalith-S)
```
90
Why dont you want to give antidepressants to a bipolar patient?
can trigger mood swings
91
What isn't effective for rapid cyclers?
lithium
92
Sometimes you will combine lithium with (blank) in bipolar patients initially during depressive episodes but use caution
SSRI
93
The mechanism behind lithium is unknown but it involves long-term (blank) changes
neuroplastic
94
What are the immediate effects of lithium?
- inhibition of recycling of inositol substrates
| - altering the function of G-proteins associated with Beta-adrenergic and M1 ACh receptors
95
How does lithium distribute in the body?
into total body water
96
When do you get peak plasma levels of lithium?
1-2 hours standard prep
| 4 hours with slow release formula
97
How does lithium get eliminated and what is its half-life?
kidney
| 20-24 hours
98
Renal clearance is proportional to (blank) concentration
plasma
99
What all can increase lithium levels?
renal problems, CHF, dehydration, advanced age
100
When you take lithium, you willl retain lithium at the expense of what ion?
sodium
101
Lithium clearance is decreased by what 3 drugs?
NSAIDs
loop and thiazide diuretics
ACE inhibitors
102
Lithium clearance is increased with what four drugs?
caffeine
osmotic diuretic
acetazolamide
theophylline
103
What do you use acetazolamide for?
Edema-> its a diuretic
104
What is the therapeutic plasma level of lithium?
0.5-1.5 mEq/l
105
What are the adverse SEs of lithium at therapeutic levels?
- drowsiness, slowed mentation and forgetfullness
- GI disturbances (nausea, vomiting, diarrhea)
- polyuria and thirst (decreased response of kidney to ADH)
- weight gain
- mild tremor (principally in the fingers)
106
What are the adverse SEs of lithium with long-term use?
- degenerative changes in the kidney (interstitial nephritis)
- depression of thyroid function (goiter) due to interference with iodine use in the thyroid
107
When shouldnt you take lithium and why?
pregnancy and breast feeding
| -> can cause Ebstein's anomaly
108
Lithium has a (blank) therapeutic index so serum levels must be carefully monitored
low (always monitor for conditions that my decrease clearance or volume of distribution)
109
Above 2.5 mEq/ lithium produces.....(4)?
- ataxia
- gross tremor
- cardiac arrhythmias
- coma and convulsions (can cause death)
110
When can you see toxicity of lithium in the blood?
you can see toxicity at any blood level
111
What is valproic acid (depakote, depakote ER)?
an antiepileptic drug (AED) and used to treat mania and mixed states
112
Whats the downside of treating bipolar disorder with valproic acid (depakote)?
shows good efficacy relative to lithium in the acute and long-term BUT can be more sedating than lithium
113
What is carbamazepine (tegretol, tegretol XR, equetro)?
antiepileptic drug (AED) used to treat mania and mixed states
114
What are the 6 atypical antipsychotics?
- quetiapine (seroquel)
- aripiprazole (abilify)
- olanzapine (zyprexa)
- lurasidone (latuda)
- asenapine (saphris)
- risperidone (risperdal)
115
What do you give lurasidone (latuda) for?
bipolar depression
116
What are the 2 famous benzodiazepines?
Lorazepam (ativan)
| Clonazepam (klonopin)
117
What is a new AED used also for bipolar depression?
Lamotrigine (lamictal)
