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Pharmacology Exam 2 (Year 2 sem 2) > Chapter 14: Serotonergics > Flashcards

Chapter 14: Serotonergics Flashcards

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1
Q

What is the number one inducer of depressive episodes?

A

stress

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2
Q

What is serotonin made from (including rate limiting enzyme) and where is it located?

A

tryptophan–(tryptophan hydroxylase)–> serotonin

  • in the raphe nuclei
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3
Q

what is norepinephrine made from (including rate-limiting enzyme) and where is it located?

A

tyrosine –(tyrosine hydroxylase)–> L-DOPA–>dopamine –>NE.

  • in locus ceruleus
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4
Q

what does MAO-A oxidize?

what does MAO-B oxidize?

A

MAO-A: 5-HT, NE, dopamine

MAO-B: dopamine

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5
Q

What are characteristics of bipolar I disorder, and what would be an adverse effect taking antidepressants concurrently?

A

only one manic episode not superimposed on schizophrenia and no past depressive episodes.
- life-threatening switches into mania

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6
Q

What effect do transmitters have on the 5;HT2(A,C) receptors?

A

excitatory (increase IP3, DAG)

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7
Q

What effect do 5-HT4,6,7 receptors have?

A

excitatory (increase cAMP)

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8
Q

What is the monoamine hypothesis?

A

States that decreased serotonin and/or NE levels cause mood disorders

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9
Q

What are characteristics of typical depression, and what is the first line agent?

A

depressed mood w/ no cause 2+ weeks, early awakening/sleep disturbance, decreased appetite with weight loss, social disengagement, NO MANIC EPISODES.
- SSRIs

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10
Q

What are characteristics of atypical depression, and what are effective treatments?

A

hypersomnia, increased appetite, sensitivity, engagement in pleasure-seeking behaviors.
- bupropion, venlafaxine, methylphenidate, 2nd/3rd line = MAOIs

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11
Q

What are characteristics of bipolar II disorder?

A

1+ depressive episodes, 1+ hypomanic episodes, no manic or mixed episodes

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12
Q

What experimental drug induces depression by inhibiting transport of 5-HT, NE, and DA?

A

reserpine

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13
Q

What are the acute vs. chronic effects of treatment with antidepressants?

A

Acute: decreased neuronal firing, decreased 5-HT and NE.

Chronic(3+ weeks): downregulation of inhibitory autoreceptors, leading to enhancement of neurotransmission

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14
Q

What selective 5-HT2a/2c agonist prodrug is converted into mCPP used mostly for insomnia?

A

trazodone

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15
Q

What drug displaces 5-HT,dopamine, and NE from their storage vesicles in presynaptic nerve terminals, and is used as a 2nd line agent for atypical depression and depression in the elderly?

A

modafinil

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16
Q

What drugs that treat ADHD displace 5-HT,dopamine, and NE from their storage vesicles in presynaptic nerve terminals?

A

dextroamphetamine, lisdexamfetamine

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17
Q

What drug for ADHD has side effects of sudden death, hyperthermia, CNS stimulation, and psychotic disorder, and should not be used with CV disease or with MAO-Is?

A

dextroamphetamine

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18
Q

What drug for ADHD has side effects of sudden death, MI, ventricular hypertrophy, stroke, Gilles de la Tourette syndrome, seizure, and Stevens-Johnson syndrome, and should not be used with CV disease or with MAO-Is?

A

lisdexamfetamine

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19
Q

What drugs inhibit MAO (serotonin degradation) to treat depression, and are irreversible and nonselective so have the worst tyramine toxicity?

A

iproniazid, phenelzine, isocarboxazid (all Z)

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20
Q

What drugs that inhibit MAO-A are reversible, and have less tyramine toxicity than the irreversible drugs of their class?

A

moclobemide, befloxatone, brofaromine (mo, flo, bro)

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21
Q

What drug, as a transdermal patch, will have a decreased risk of tyramine induced crisis? It inhibits MAO-B at low doses and MAO-A at high doses.

A

selegiline

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22
Q

What 2 things should always be done prior to starting tricyclic antidepressant treatment

A

ECG to rule out conduction system disease, and make sure they’re not taking MAO-Is

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23
Q

What inhibits reuptake of serotonin to treat depression, anxiety, & OCD (1st line), post-traumatic stress disorder, and pain syndromes?

A

SSRIs (citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)

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24
Q

What drugs will cause side effects of sexual dysfunction and GI distress, and when taken with MAO-Is, cause hyperthermia, muscle rigitity, myoclonus, and mental status fluctuations?

A

SSRIs (citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
((the group of symptoms with MAO-Is is called “serotonin syndrome”!))

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25
What drugs block reuptake of 5-HT and NE by GENERALLY blocking their transporters, enhancing post-synaptic responses, and what do they generally treat
``` tricyclic antidepressants (-pramine/-ptyline) - depression, pain syndromes ```
26
What SSRI causes a side effect of constipation?
paroxetine
27
What tricyclic antidepressant treats OCD?
clomipramine
28
What are the major side effects with tricyclic antidepressants?
heart block, arrythmia, MI, conduction delays, AV block & BBB, orthostatic hypotension in elderly, agranulocytosis, suicidal thoughts, antihistaminergic effects (sedation, weight gain, confusion)
29
What should always be done prior to starting tricyclic antidepressant treatment
ECG to rule out conduction system disease
30
What inhibits reuptake of serotonin to treat depression, anxiety, OCD, post-traumatic stress disorder, and pain syndromes?
SSRIs (citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
31
What drugs will cause side effects of sexual dysfunction and GI distress, and when taken with MAO-Is, cause hyperthermia, muscle rigitity, myoclonus, and mental status fluctuations?
SSRIs (citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
32
What SSRI causes a side effect of diarrhea?
sertraline
33
What SSRI causes a side effect of constipation?
paroxetine
34
What happens if you stop administration of citalopram, fluoxetine, fluvoxamine, paroxetine, or sertraline?
serotonin discontinuation syndrome (anxiety, dysphoria, GI/flu-like symptoms, insomnia, hypomania)
35
What is the best drug for pain syndromes in the elderly/fragile or in patients where citalopram, fluoxetine, fluvoxamine, paroxetine, or sertraline did not work?
duloxetine
36
What drugs that block 5-HT reuptake and NE reuptake in a CONCENTRATION-dependent manner (low = 5-HT, high = NE) treat depression, anxiety, and panic disorders?
venlafaxine, duloxetine
37
What depression medications will give you neuroleptic malignant syndrome and hepatitis?
venlafaxine, duloxetine
38
What drug that blocks 5-HT reuptake and NE reuptake in a concentration dependent manner (low = 5-HT, high = NE) treats major depressive disorder, and has unique side effects like hyponatremia, GI hemorrhage/bleeding, interstitial lung disease, and pulmonary eosinophilia?
desvenlafaxine
39
What drug is used for fibromyalgia that causes abnormal bleeding and serotonin syndrome, and what is its class?
milnacipran (SNRIs)
40
What drug that selectively blocks NE transporter treats ADHD?
atomoxetine
41
What is the benefit of atomoxetine over amphetamines in treating ADHD, and what side effects remain?
lower abuse potential, but still can have MI, prolonged QT, sidden cardiac death, liver injury, suicidal thoughts, psychotic disorder, dyskinesia
42
What is the treatment for atypical depression and smoking cessation and what does it inhibit?
buproprion: inhibits 5-HT, dopamine, and NE reuptake
43
What is the biggest side effect with buproprion?
seizure
44
What are the biggest pros of buproprion over other antidepressants?
fewer sexual effects and less mania
45
What drug blocks 5-HT2a, 5-HT2c, and alpha-2 adrenergic receptors, decreasing 5-HT neurotransmission while increasing NE neurotransmission?
mirtazapine
46
What is a potent somnorific and appetite stimulant in the elderly, but can cause agranulocytosis?
mirtazapine
47
What blocker of post-synaptic 5-HT2 receptors causes a side effect of priapism?
trazodone
48
What blocker of post-synaptic 5-HT2 receptors causes a side effect of liver failure and orthostatic hypotension?
nefazodone
49
What atypical antidepressant drug should not be administered with MAO-I, pimozide, triazolam, or carbamazepine?
nefazodone
50
What drug is a 5-HT1a agonist for anxiety with nonaddictive properties?
buspirone
51
What serotonin receptor do the "triptans" for acute migraines work on?
5-HT1B, 5-HT1D
52
What should never be taken with "triptans"?
ergot agent or MAO-Is
53
What serotonin antagonist is used to treat glaucoma and HTN, and on which serotonin receptor?
ketanserin ("Ket smokes pot"), on 5-HT2a/2c
54
What serotonin antagonist is used for nausea in cancer chemotherapy, and on which serotonin receptor?
odansetron, on 5-HT3
55
What serotonin antagonist is used for IBS with constipation, and on which serotonin receptor?
tegaserod, prucalopride ("ROD up butt, PRIDE = stick up yer ass"), on 5-HT4
56
What serotonin antagonist is used for IBS with diarrhea, and on which serotonin receptor?
alosetron ("losing lots of stool/water"), on 5-HT3
57
What 2 contraindications should you check for before prescribing tegaserod or prucalopride?
history of bowel obstruction, gallbladder disease
58
What contraindications should you check for before prescribing alosetron?
constipation, fluvoxamine use, IBD, diverticulitis, hypercoaguable history
59
What is a treatment for irritability and impulsivity?
valproic acid
60
What are treatments for bipolar disorder?
lithium (major), carbamazepine, lamotrigine
61
What are 4 mechanisms of action of lithium?
1) enters via Na+ channels, inhibiting inositol phosphates that makes IP2 -->IP1-->inositol, which blocks PIP regeneration 2) increases 5-HT 3) decreases NE, DA 4) inhibit adenylyl cyclase
62
What are side effects of lithium?
intoxication (nausea, diarrhea, ataxia, tremor, confusion), hyperkalemia, hypotension, bradyarrythmia, pseudotumor cerebri, increased ICP/papilledema, polyuria, nephrogenic DI, hypothyroidism, goiter, ECG/EGG abnormalities
63
What are contraindications of lithium?
CV disease, hyponatremia/nephrogenic DI, renal impairment, lactation
64
What drugs & electrolyte state increase lithium absorption in the proximal tubules?
NSAIDs & hyponatremia

Pharmacology Exam 2 (Year 2 sem 2) (7 decks)

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