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FPT > Pharmacology of Nausea and Vomiting > Flashcards

Pharmacology of Nausea and Vomiting Flashcards

1
Q

the tendency to vomit or as a feeling in the throat of epigastric region alerting an individual that vomiting is imminent

A

nausea.

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2
Q

the ejection or expulsion of gastric contents through the mouth. often requiring a forceful event.

A

vomiting.

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3
Q

list the 10 common causes of nausea?

A

1- chemotherapy.
2- general anesthesia.
3- viral gastroenteritis.
4- gastroparesis.
5- migraine.
6- motion sickness.
7- overdose of alcohol.
8- vertigo.
9- rotavirus.
10- pregnancy.

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4
Q

VOMIT stands for?

A

V- Vestibular.
O- Obstruction or drugs like Opiates.
M- Mind (dysmotility).
I- Infection (irritation of gut).
T- Toxins (taste and other senses).

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5
Q

list agonists and antagonists of antiemetics?

A

Antagonist: 5-HT3 RAs
agonist: 5-HT3.

antagonist: promethazine.
agonist: H1.

antagonist: atropine.
agonist: M.

antagonist: domperidol.
agonist: D2.

antagonist: NK1-RA
agonist: Substance P.

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6
Q

common condition of nausea and vomiting are?

A

1- motion sickness.
2- pregnancy.
3- hepatitis.

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7
Q

chemotherapeutic agents can directly activate what?

A

CTV or vomiting center.

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8
Q

chemotherapeutic agents can also act peripherally by what?

A

causing cell damage in the gastrointestinal tract and releasing serotonin from the enterochromaffin cells of the small intestinal mucosa serotonin activates 5-HT3 receptors.

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9
Q

uncontrolled vomiting can produce what?

A

1- dehydration.
2- metabolic imbalances.
3- nutrient depletion.

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10
Q

give example of a drug effective in motion sickness that works as a M1 receptor antagonists?

A

hyoscine (scopolamine) (transdermal scop).

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11
Q

give examples of a drug effective in motion sickness that works as a H1 receptor antagonists?

A

1- dimenhydrinate (dramamine).
2- diphenhydramine (dramenex).
3- cyclizine (emetrex).
4- meclizine (navidoxine).

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12
Q

list the properties of H1 and M1 receptor antagonists?

A
  • very useful in motion sickness.
  • ineffective against substances that act directly on the CTZ.
  • they don’t work once vomiting has started.
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13
Q

list drugs that are D2 receptor blocker?

A

1- phenothiazine compounds: prochlorperazine (emadrotec).
2- substituted benzamides: metoclopramide (primperan).
3- butyrophenones: droperidol (inapsine), haloperidol (haldol).
4- domperidone (motilime).

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14
Q

what is the first group of drugs shown to be effective antiemetic agents?

A

phenothiazine compounds.

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15
Q

what are the side effects of prochlorperazine?

A

1- hypotension, restlessness, extrapyramidal symptoms and sedation.
2- effective against moderately emetogenic chemotherapeutic agents.

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16
Q

which drug prevents emesis in 30-40% and reducing emesis in the majority?

A

metoclopramide (primperan)

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17
Q

what are the side effects of metoclopramide (primperan)?

A
  • anti-dopaminergic side effects, including sedation, diarrhea and extrapyramidal symptoms, limit its high dose use.
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18
Q

what are the uses of Doperidol (inapsine) and Haloperidol (haldol)?

A
  • moderately active anti-emetics.
  • high doses of haloperidol effective in preventing cisplatin (anticancer drugs) induced emesis).
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19
Q

what are the uses of Domperidone (motilime)?

A
  • nausea and vomiting (block D2 receptors are found in CTZ).
  • restore motility and tone to the upper GIT and facilitate gastric emptying regulates and duodenal function.
20
Q

what are the side effects of Domperidone (motilime)?

A
  • anti-dopaminergic side effect and increase level of prolactin hormone.
21
Q

list drugs that are 5-HT3 receptor blockers?

A

1- ondansetron (zofran).
2- granisetron (kytril).
3- tropisetron (navoban).
4- dolasetron (anzemet).
5- palonosetron (aloxi).

22
Q

how do we administer 5-HT3 receptor blockers?

A

IV and orally.

23
Q

what are the uses of 5-HT3 receptor blockers?

A
  • prevention of nausea and vomiting associated with surgery and cancer chemotherapy.
24
Q

what are the side effects of 5-HT3 receptor blockers?

A

headache and diarrhea.

25
Q

benzodiazepine target which receptor?

A

GABA A

26
Q

give examples of benzodiazepine that can be used as antiemtics?

A

1- lorazepam (ativan).
2- alprazolam (xanax).

27
Q

list the properties of benzodiazepines?

A
  • their antiemetic potency is low (not useful).
  • their beneficial effects may be due to their sedative and anxiolytic properties.
  • useful in treating anticipatory vomiting.
28
Q

give examples of corticosteroids that can be used as antiemetics?

A

1- methyl-prednisolone (depo-medrol).
2- dexamethasone (epidron).

29
Q

corticosteroids are effective against what?

A

moderately emetogenic chemotherapy.

30
Q

what is corticosteroids mechanism of action?

A

not known, may involve blockade of prostaglandins.

31
Q

give examples of cannabinoids used as antiemtics?

A

1- dronabinol.
2- nabilone.

32
Q

cannabinoids are effective against?

A

moderately emetogenic chemotherapy.

33
Q

why aren’t cannabinoids used?

A

due to serious side effects, including:
1- hallucinations.
2- sedation.
3- vertigo.
4- disorientation.

34
Q

give an example of NK1 receptor blocker?

A

aprepitant (depo-medrol).

35
Q

NK1 receptor blocker is a new class of drugs called?

A

substance P antagonists (SPA).

36
Q

NK1 receptor blockers mediates its effect by?

A

blocking the neurokinin 1 (NK1) receptor.

37
Q

aprepitant is metabolized primarily by what?

A

CYP3A4

38
Q

aprepitant can affect the metabolism of what?

A

other drugs such as warfarin.

39
Q

what are the side effects of NK1 receptor blocker?

A

constipation and fatigue.

40
Q

antiemetic drugs are often combined to?

A

increase antiemetic activity or decrease toxicity.

41
Q

dexamethasone increase antiemetic activity when given what what?

A

metoclopramide or a 5-HT3 antagonist.

42
Q

diphenhydramine is combine with?

A

metoclopramide to reduce extrapyramidal side effects.

43
Q

what is the first line therapy for morning sickness during pregnancy?

A

pyridoxine (vit B6)

44
Q

what to give to pregnant women for morning sickness is symptoms persist (after pyridoxine)?

A

addition of antihistaminic such as meclizine.
(meclizine + pyridoxine)

45
Q

what antiemetics are used in children?

A

corticoadrenal extract + pyridoxine

46
Q

what antiemetics come from natural sources?

A

ginger extract for prophylaxis of motion sickness.

FPT (17 decks)

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