1
Q
Amitriptyline (Elavil®)
A
- tertiary amine
- Tricyclic Antidepressants (TCAs)
2
Q
Imipramine (Tofranil®)
A
- tertiary amine
- Tricyclic Antidepressants (TCAs)
3
Q
Nortriptyline (Pamelor®)
A
- secondary amine
- Tricyclic Antidepressants (TCAs)
4
Q
Desipramine (Norpramin®)
A
- secondary amine
- Tricyclic Antidepressants (TCAs)
5
Q
Phenelzine (Nardil®)
A
Monoamine Oxidase Inhibitors (MAOIs)
6
Q
Selegiline (Deprenyl®)
A
Monoamine Oxidase Inhibitors (MAOIs)
7
Q
Fluoxetine (Prozac®)
A
Selective Serotonin Reuptake Inhibitors (SSRIs)
8
Q
Paroxetine (Paxil®
A
Selective Serotonin Reuptake Inhibitors (SSRIs)
9
Q
Sertraline (Zoloft®)
A
Selective Serotonin Reuptake Inhibitors (SSRIs)
10
Q
Citalopram (Celexa®
A
Selective Serotonin Reuptake Inhibitors (SSRIs)
11
Q
Venlafaxine (Effexor®)
A
5-HT and NE Reuptake Inhibitors (SNRIs)
12
Q
Duloxetine (Cymbalta®)
A
5-HT and NE Reuptake Inhibitors (SNRIs)
13
Q
which neurotransmitter is responsible for reward, motivation, euphoria, and movement
A
dopamine
14
Q
which neurotransmitter is responsible for reward, arousal, alertness, decisions, and flight or fright
A
NE/noradrenaline
15
Q
which neurotransmitter is responsible for mood, emotion, memory, sleep, and cognition
A
serotonin (5-HT)
16
Q
what is the Monoamine Hypothesis of depression
A
- amine neurotransmitters are DA, NE, and serotonin
- depression results from abnormal or decressed neurotransmission of dopamine, norepinephrine and serotonin
17
Q
evidence for the Monoamine Hypothesis is that patients treated with Reserpine which depletes neurons of noradrenaline (NE) and serotonin (5-HT) developed what
A
- depression
* This suggested that depression had something to do with a deficit of NE and 5-HT.
18
Q
the antidepressant effect takes 2-3 weeks due to
A
neural plasticity
19
Q
differentiate between short term effects and long term effects of uptake inhibitors
A
- Normal - amine levels in synapse are modulated by reuptake and presynaptic inhibition
- short term Uptake inhibitors - amine levels in synapse are increased BUT so does feedback inhibition so synaptic amine levels are balanced
- Long-term - Antidepressants downregulate auto-receptors (which control firing rate of neuron by negative feedback); increasing firing rate of amine neurons
20
Q
MOA of tricyclic antidepressants
A
- inhibit re-uptake of NE and serotonin
- also block a-adrenergic, histamine and muscarinic receptors
21
Q
list uses of tricyclic antidepressants
A
- depression: not first line
- chronic pain (TMJ)
22
Q
List the tertiary amines TCA
A
- amitriptyline (Elavil®)
- imipramine (Tofranil®)
23
Q
MOA of tertiary amines. adverse effects?
A
- primarily inhibit serotonin re-uptake
- produce more seizures and are more sedating than secondary amines
24
Q
List the secondary amines TCA
A
- nortriptyline (Pamelor®)
- desipramine (Norpramin®)
25
MOA of secondary amine TCA
primarily block NE re-uptake
26
List the 4 dopamine pathways
1. nigrostriatal
2. mesolimbic
3. mesocortical
4. tubero-infundibular
27
TCAs are metabolized by
CYP2D6: thus drug interactions are very common
28
List the side effects of TCA
* weight gain
* histamine receptor blockade -\> sedation
* cholinergic blockade -\> blurred vision, tachycardia, constipation, dry mouth, impaired memory
* a1 receptor blockade -\> postural hypotension, reflex tachycardia
* analgesia
* SIADH -\> hyponatremia
* sexual dysfunction
* decrease in sz threshold
29
can TCAs be used in pregnant patients
yes
30
TCA toxicity can lead to what cardiac abnormality
* Torsades de pointes
* antidote: magnesium
31
Monoamine oxidase inhibitors and TCAs together can result in what condition? what are the signs of this condition?
* **serotonin syndrome**
* severe CNS toxicity
* fever
* convulsions
* coma
32
List the Selective Serotonin Reuptake Inhibitors (SSRIs)
* Fluoxetine (Prozac®)
* Paroxetine (Paxil®)
* Sertraline (Zoloft®)
* Citalopram (Celexa®)
33
Escitalopram (Lexapro)
SSRI
34
obsessive compulsive disorder and social anxiety are usually treated with what SSRI
* Paroxetine (Paxil)
35
of the SSRIs, which is the most likely to inhibit CYP450 enzymes? specially which enzymes?
* Fluoxetine
36
SSRI drug of choice in an elderly patient? why?
* sertraline (zoloft)
* due to shorter half life of 26 hours
* least likely to interact with other drugs
37
DOC for depression
* **SSRI**
* specifically Citalopram
38
MOA of SSRIs
selectively inhibits serotonin reuptake
39
list the side effects of SSRIs
* mild side effects
* sexual dysfunction
40
fluoxetine has what drug interaction with codeine
* it inhibits the conversion of codeine to morphine
41
SSRIs + MAOI will cause
serotonin syndrome
42
SSRI + St johns wart or amphetamines will cause
serotonin syndrome
43
SSRI/MAOI/ or TCA + tramadol can cause
* tramadol is a mu agonist
* inhibits NE/serotonin uptake and can cause seizures and serotonin syndrome
44
MOA of serotonin-norepinephrine reuptake inhibitors
* inhibit reuptake of NE and 5-HT reuptake
45
side effect of venlafaxine
may increase blood pressure
46
side effects of duloxetine
* hepatotoxicity
* bilateral acute angle-closure glaucoma
47
MOA of Monoamine oxidase inhibitors
irreversibly inhibit MAOs which metabolize NE, DA, and serotonin -\> get increased amounts of these
48
MOA of **MAO-A**
* metabolize NE, DA, and serotonin in **both** the CNS and periphery (**GI tract**)
49
MOA of **MAO-B**
* selectively metabolizes **DA** in the **CNS** but not the GI tract
50
MOA of Phenelzine
* inhibits both MAO-A and MAO-B
* increases NE, serotonin, and DA
* **drug of last choice**
51
MOA of Selegiline
* selectively inhibits MAO-B
* increases DA
* fewer side effects
52
side effects of Phenelzine
* hypertensive crisis
53
with what medication should you avoid use with tyramine? why
* MAOI: phenelzine
* foods with tyramine: red wine, beer, aged cheese
* MAO-A is inhibited in GI tract, tyramine causes release of amines and with limited metabolism by MAO-A can get severe hypertension
54
MAOI + SSRIs or TCAs can lead to
serotonin syndrome
55
MAOI + OTC cold and cough medication containing sympathomimetic amines (ephedrine or amphetamines) can lead to
severe hypertension
56
MAOIs affect on 2D6
inhibit 2D6
57
MOA of Buproprion (wellbutrin)
* inhibits DA reuptake
58
when is Buproprion (wellbutrin) used
* ADHD
* alcoholism (reduces craving)
59
side effects of Buproprion (wellbutrin)
* seizures: CI in patients with h/o sz
* anxiety, insomnia, tremor
* tachycardia
* **sexual dysfunction rare**
60
MOA of Mirtazapine
* blocks presynaptic alpha 2 receptors which inhibits release of NE and 5-HT
* increases relase of NE and 5-HT
61
side effects of Mirtazapine
* blocks histamine receptors -\> **drowsiness**
62
good drug to use in patient who is depressed with insomnia or anxiety
Mirtazapine
63
MOA of Atomoxetine
* selective inhibitor of NE reuptake
64
use of Atomoxetine
* ADHD
* does not cause euphoria so good for addicts
65
MOA and use of Trazodone
* 5-HT receptor antagonist
* sedating -\> more often used as sleep aid and pain management
66
St. johns wort may be effective in mild depression but it should not be combined with what
* other antidepressants
* will cause **serotonin syndrome**
67
Side effect of Trazodone
Liver failure
pharm III exam 1
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