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

Chapter 14: Serotonergics Flashcards

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
Q

What drugs block reuptake of 5-HT and NE by GENERALLY blocking their transporters, enhancing post-synaptic responses, and what do they generally treat

A 
tricyclic antidepressants (-pramine/-ptyline)
- depression, pain syndromes
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26
Q

What SSRI causes a side effect of constipation?

A

paroxetine

27
Q

What tricyclic antidepressant treats OCD?

A

clomipramine

28
Q

What are the major side effects with tricyclic antidepressants?

A

heart block, arrythmia, MI, conduction delays, AV block & BBB, orthostatic hypotension in elderly, agranulocytosis, suicidal thoughts, antihistaminergic effects (sedation, weight gain, confusion)

29
Q

What should always be done prior to starting tricyclic antidepressant treatment

A

ECG to rule out conduction system disease

30
Q

What inhibits reuptake of serotonin to treat depression, anxiety, OCD, post-traumatic stress disorder, and pain syndromes?

A

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

31
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)

32
Q

What SSRI causes a side effect of diarrhea?

A

sertraline

33
Q

What SSRI causes a side effect of constipation?

A

paroxetine

34
Q

What happens if you stop administration of citalopram, fluoxetine, fluvoxamine, paroxetine, or sertraline?

A

serotonin discontinuation syndrome (anxiety, dysphoria, GI/flu-like symptoms, insomnia, hypomania)

35
Q

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?

A

duloxetine

36
Q

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?

A

venlafaxine, duloxetine

37
Q

What depression medications will give you neuroleptic malignant syndrome and hepatitis?

A

venlafaxine, duloxetine

38
Q

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?

A

desvenlafaxine

39
Q

What drug is used for fibromyalgia that causes abnormal bleeding and serotonin syndrome, and what is its class?

A

milnacipran (SNRIs)

40
Q

What drug that selectively blocks NE transporter treats ADHD?

A

atomoxetine

41
Q

What is the benefit of atomoxetine over amphetamines in treating ADHD, and what side effects remain?

A

lower abuse potential, but still can have MI, prolonged QT, sidden cardiac death, liver injury, suicidal thoughts, psychotic disorder, dyskinesia

42
Q

What is the treatment for atypical depression and smoking cessation and what does it inhibit?

A

buproprion: inhibits 5-HT, dopamine, and NE reuptake

43
Q

What is the biggest side effect with buproprion?

A

seizure

44
Q

What are the biggest pros of buproprion over other antidepressants?

A

fewer sexual effects and less mania

45
Q

What drug blocks 5-HT2a, 5-HT2c, and alpha-2 adrenergic receptors, decreasing 5-HT neurotransmission while increasing NE neurotransmission?

A

mirtazapine

46
Q

What is a potent somnorific and appetite stimulant in the elderly, but can cause agranulocytosis?

A

mirtazapine

47
Q

What blocker of post-synaptic 5-HT2 receptors causes a side effect of priapism?

A

trazodone

48
Q

What blocker of post-synaptic 5-HT2 receptors causes a side effect of liver failure and orthostatic hypotension?

A

nefazodone

49
Q

What atypical antidepressant drug should not be administered with MAO-I, pimozide, triazolam, or carbamazepine?

A

nefazodone

50
Q

What drug is a 5-HT1a agonist for anxiety with nonaddictive properties?

A

buspirone

51
Q

What serotonin receptor do the “triptans” for acute migraines work on?

A

5-HT1B, 5-HT1D

52
Q

What should never be taken with “triptans”?

A

ergot agent or MAO-Is

53
Q

What serotonin antagonist is used to treat glaucoma and HTN, and on which serotonin receptor?

A

ketanserin (“Ket smokes pot”), on 5-HT2a/2c

54
Q

What serotonin antagonist is used for nausea in cancer chemotherapy, and on which serotonin receptor?

A

odansetron, on 5-HT3

55
Q

What serotonin antagonist is used for IBS with constipation, and on which serotonin receptor?

A

tegaserod, prucalopride (“ROD up butt, PRIDE = stick up yer ass”), on 5-HT4

56
Q

What serotonin antagonist is used for IBS with diarrhea, and on which serotonin receptor?

A

alosetron (“losing lots of stool/water”), on 5-HT3

57
Q

What 2 contraindications should you check for before prescribing tegaserod or prucalopride?

A

history of bowel obstruction, gallbladder disease

58
Q

What contraindications should you check for before prescribing alosetron?

A

constipation, fluvoxamine use, IBD, diverticulitis, hypercoaguable history

59
Q

What is a treatment for irritability and impulsivity?

A

valproic acid

60
Q

What are treatments for bipolar disorder?

A

lithium (major), carbamazepine, lamotrigine

61
Q

What are 4 mechanisms of action of lithium?

A

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
Q

What are side effects of lithium?

A

intoxication (nausea, diarrhea, ataxia, tremor, confusion), hyperkalemia, hypotension, bradyarrythmia, pseudotumor cerebri, increased ICP/papilledema, polyuria, nephrogenic DI, hypothyroidism, goiter, ECG/EGG abnormalities

63
Q

What are contraindications of lithium?

A

CV disease, hyponatremia/nephrogenic DI, renal impairment, lactation

64
Q

What drugs & electrolyte state increase lithium absorption in the proximal tubules?

A

NSAIDs & hyponatremia

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

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