Vertigo, Hearing Loss & N/V-Drugs Flashcards

1
Q

name 3 major classes of drugs that have ototoxicity

A

aminoglycosides
cisplatin
loop diuretics

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2
Q

name the drug class: causes ototoxicity that is usually not reversible; possible improvement w/ N-acetylcysteine; dose dependent

A

aminoglycosides

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3
Q

which class of drugs produces irreversible ototoxicity?

A

cytostatic drugs (cisplatin)

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4
Q

is the ototoxicity with loop diuretics reversible?

A

can be irreversible

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5
Q

are most of the drugs that cause ototoxicity reversible or irreversible?

A

reversible

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6
Q

which drug class enters into outer hair cell –> cell death by either caspase-dependent or caspase independent mechanisms?

A

aminoglycoside

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7
Q

which drug enters outer hair cells and results in cell death, which appears to be primarily caspase-dependent?

A

cisplatin

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8
Q

how do the loop diuretics cause ototoxicity?

A

interfering with the production and maintenance of endolymph in the stria vascularis

  • upset the fluid balance & this results in edema & loss of function
  • the effect is dose-rate dependent (the concentration gradient is an important factor in the penetration of drugs into this area of the body)
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9
Q

meclizine, diphenhydramine, & promethazine all work to treat vertigo via which two types of receptors?

A

H1 & M1 receptors

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10
Q

which drug is useful for nausea arising from higher brain centers mediating fear, emotion, anticipation?

A

diazepam

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11
Q

which drug used to treat vertigo has the longest duration of action?

A

scopolamine

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12
Q

diphenhydramine & promethazine are inhibitors of what CYP enzyme?

A

CYP2D6

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13
Q

what are the general adverse effects of the drugs that treat vertigo?

A

drowsiness, dizziness

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14
Q

scopolamine is an antagonist at what receptor?

A

M1

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15
Q

diphenhydramine, meclizine, & promethazine all block which 2 receptors in the treatment of vertigo?

A

H1 & M1

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16
Q

which drug used to treat vertigo has a BBW for use by injection?

A

promethazine

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17
Q

which drug used to treat vertigo has an adverse effect of fatal respiratory depression in <2 y/o?

A

promethazine

18
Q

all 4 drugs to treat vertigo (diphenhydramine, meclizine, promethazine, & scopolamine) are all inappropriate in what pt population?

A

geriatric

19
Q

the vomiting process appears to be coordinated by what center in the lateral retcular formation of the mid-brainstem adjacent to both the CTZ in the area postrema at the bottom of the 4th ventricle & the solitary tract nucleus?

A

central emesis center

20
Q

the lack of a BBB allows the CTZ to monitor blood & CSF constantly for toxins & to relay info to what center to trigger nausea and vomiting?

A

emesis center

21
Q

other than the CTZ, what are four other inputs to the emesis center?

A
  1. vagus nerve (via solitary tract nucleus)
  2. splanchnic afferents via the spinal cord
  3. cerebral cortex
  4. vestibular apparatus
22
Q

the CTZ has high concentrations of what 3 receptors?

A

serotonin (5-HT3), Dopamine (D2), Opioids

23
Q

the solitary tract nucleus has what 4 types of receptors?

A

Enkephalin
histamine
ACh
5-HT3

24
Q

what is the efferent component for the emesis center?

A

sends efferents to nuclei responsible for respiratory, salivary, vasomotor activity, and striated & smooth muscle involved in act of vomiting

25
Q

what is the only 5HT-3 antagonists that has to be adjusted in hepatic disease?

A

ondansetron

26
Q

all the 5HT-3 antagonists have what cardiac adverse effect?

A

QT-prolongation

27
Q

ECG monitoring is recommended in pts taking which two 5HT-3 antagonists?

A

dolasetron or Ondansetron

28
Q

what are the most common adverse effects of the 5-HT3 antagonists?

A

headache
constipation
diarrhea

29
Q

the serotonin antagonists are used for CINV & PONV prophylaxis, often with what other drug class?

A

corticosteroid

30
Q

which two D2 receptor antagonists are considered general purpose anti-nausea & anti-emetic drugs?

A

prochlorperazine

Chlorpromazine

31
Q

Prochlorperazine & Chlorpromazine are D2 receptor antagonists and have what two other functions?

A
  1. antihistaminic
  2. anticholinergic
    (used in other forms of Nausea, such as motion sickness)
32
Q

chronic use of D2 receptor antagonists can have what adverse effect?

A

bone marrow suppression / blood dyscrasias

33
Q

co-administration of D2 receptor antagonists with what other drug class may cause increased CNS adverse effects?

A

antipsychotics

34
Q

phenothiazines (prochlorperazine, chlorpromazine) are associated with what cardiac adverse effect?

A

risk of QT prolongation w/ Torsades de pointes

35
Q

what is the MOA for aprepitant?

A

substance P/NK-1 receptor antagonist

  • central action (solitary tract) essential
  • peripheral effects (vagal terminals in GI tract) also contribute
36
Q

Aprepitant is metabolized by what CYP enzyme?

A

CYP3A4

37
Q

what is the name of the pro-drug substance P / NK-1 receptor antagonist that is activated by extra-hepatic metabolism?

A

fosaprepitant

38
Q

MOA dronabinol

A

G-protein coupled decreased neuronal activity in the medullary vomiting center & solitary tract nucleus

  • oppose 5-HT3 mediated stim of vagal afferents
  • appetite stim. via CB receptors in lateral hypothalamus (lower doses than for antiemetic action)
39
Q

emesis is most likely from what 6 anti-neoplastic drugs?

A
cisplatin
mechlorethamine
streptozotocin
cyclophosphamide
carmustine
dacarbazine
40
Q

what is the treatment of choice for prophylaxis against acute emesis?

A

serotonin receptor antagonist + corticosteroid & possibly NK-1 antagonist

41
Q

how do corticosteroids help reduce emesis caused by antineoplastic drugs?

A

corticosteroids act on steroid receptors in solitary tract nucleus (reduced release o serotonin has been proposed)