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PPNP drugs > Antiemetics: drugs used in nausea & vomiting > Flashcards

Antiemetics: drugs used in nausea & vomiting Flashcards

1
Q 
Vomiting is caused by noxious stimulation of 1 or more of 4 of the sites which can trigger the vomiting centre:
1. 
2.
3. 
4.
A
  1. Chemoreceptor trigger zone
  2. GI tract & heart
  3. Vestibular system (motion sickness)
  4. CNS (pain, repulsive smells, etc)
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2
Q

What are the drugs to prevent ACUTE nausea & vomiting & LOW risk of emetic?

A
  • serotonin 5-HT3 antagonists (1st line)
  • corticosteroids
  • dopamine receptor antagonists: substituted benzamides
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3
Q

Examples of serotonin 5-HT3 antagonists

A

Ondansetron (half life 4-9hrs)
Granisetron
Palonosetron

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4
Q

Serotonin 5-HT3 antagonists act at _______primarily in the _______

A

they act at 5-HT3 receptors primarily in the GI tract

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5
Q

Serotonin 5-HT3 antagonists’ efficacy is enhanced by

A

combining with a corticosteroid & NK1-receptor antagonist

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6
Q

Administering serotonin 5-HT3 antagonists:

  • when (IV & oral)
  • why
A

IV, 30 mins before OR
Orally, 1h before
chemo

Why: to prevent acute chemotherapy-induced vomiting

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7
Q

With serotonin 5-HT3 antagonists, there is a small risk of:
1.
2.

A
  1. cardiac arrhythmia (in pts with cardiac abnormalities)

2. orofacial malformations (in early pregnancy) (eg. cleft lips)– (ondansetron)

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8
Q

Examples. of corticosteroids

A

Dexamethasone

methylprednisolone

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9
Q

Corticosteroids mimic effects of _______

A

endogenous cortisol

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10
Q

Higher doses/ long term use (>2 wks) of corticosteroids may cause _________.
Symptoms include:

A

may cause iatrogenic Cushing’s syndrome

Symptoms:

  • mood swings
  • weight gain
  • facial flushing
  • impaired wound healing
  • thinning of skin, easy bruising
  • osteoporosis
  • immunosuppression
  • muscle wasting, dysphonia
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11
Q

Example of dopamine receptor antagonist

A

metoclopramide

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12
Q

Dopamine receptor antagonists act at the _______, and they are also used as _______ to stimulate ________.

A

chemoreceptor trigger zone;
used as prokinetics;
to stimulate GI motility

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13
Q

Concerns of dopamine receptor antagonists
1.
2.

A
  1. Extrapyramidal symptoms (EPS)
    - restlessness
    - dystonia
    - parkinsonian symptoms
    - long term: tardive dyskinesia can develop
  2. Elevated prolactin levels can cause:
    - menstrual disorders
    - galactorrhea
    - gynaecomastia
    - impotence
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14
Q

Can dopamine receptor antagonists be used long-term?

A

NOOOO

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15
Q

What are the drugs to prevent ACUTE nausea & vomiting & HIGH risk of emetic?

A

neurokinin receptor antagonists (substance P antagonists)

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16
Q

Examples of neurokinin receptor antagonists

A
  • aprepitant (oral)

- fosaprepitant (IV)

17
Q

Neurokinin receptor antagonists act at ____________ in ________

A

act at Neurokinin 1 receptors in area postrema

18
Q

Signs and symptoms of neurokinin receptor antagonists

  1. Common
  2. Severe
A
  1. Common:
    - fatigue
    - dizziness
    - constipation/diarrhoea
    - anorexia
    - hiccups
  2. Severe:
    - dehydration
    - peripheral neuropathy
    - blood dyscrasias
    - pneumonia
19
Q

Neurokinin receptor antagonists inhibit the CYP3A4 enzyme that is responsible for the _______ and ______ of many drugs. Accordingly, NK-1 receptor antagonists such as aprepitant can result in ____________ concentrations of drugs.

A

metabolism and elimination;

elevated plasma

20
Q

What are the drugs to prevent DELAYED nausea & vomiting & HIGH risk of emetic?

A

antipsychotics: mixed dopamine/muscarinic receptor antagonists +/ antihistamines

21
Q

Examples of antipsychs

  1. Dopamine receptor antagonist & muscarininc antagonists & antihistamine
  2. Dopamine receptor antagonist
  3. Atypical antipsychotics
A
  1. Promethazine, prochlorperazine
  2. Droperidol
  3. Olanzapine
22
Q

Atypical antipsychotics such as OZP helps to _________ in delayed nausea.

A

decrease risk of EPSEs

23
Q

Promethazine & prochlorperazine are useful in nausea & vomiting caused by GIT eg. _________ or ________

A

small bowel obstruction or cholecystitis

24
Q

Muscarinic antagonism helps to 1. ______________ and also useful as 2. ________. This can suppress 3. __________ along the GI tract.

A
  1. block the vomitting output
  2. anti-spasmodic
  3. motility & movement
25
Q

Dopamine receptor antagonists work by ______________ in the __________.

A

work by blocking dopamine receptors in the chemoreceptor trigger zone

26
Q

Muscarinic antagonists work by __________ and inhibit cholinergic transmission from the ________ to the ________

A

blocking muscarinic receptors;

vestibular nuclei to the vomiting center

27
Q

Main concerns of antipsychotics: mixed dopamine/muscarininc receptor antagonists and/or antihistamines

A
  • sedative
  • EPSEs
  • hypotension
  • Droperidol: increase risk of cardiac arrhythmia due to prolongation of QT interval
28
Q

What are the drugs to prevent ANTICIPATORY nausea & vomiting?

A

Benzodiazepines (BZPs)

29
Q

Examples of BZPs

A

lorazepam

diazepam

30
Q

BZPs bind to _______ on ______. (this increases activity of GABA). Hence,
This increases __________.

A

allosteric site on GABA receptors;

chloride conductance

31
Q

BZPs are used as _______ to reduce anticipatory vomiting caused by anxiety.

A

anxiolytics

32
Q

Main concerns of BZPs

A
  • sedative
  • additive effects with antidepressants, alcohol, opioids
  • avoid during pregnancy!! esp 1st tri (risk of cleft palate)
33
Q

What are the drugs to prevent motion sickness?

A
  • muscarinic receptor antagonists (Anticholerginic)

- mixed H1 histamine + muscarinic receptor antagonists

34
Q

Examples of :

  1. muscarinic receptor antagonists (Anticholerginic)
  2. mixed H1 histamine + muscarinic receptor antagonists
A
  1. Hyoscine (Scopolamine)

2. Diphenhydramine

35
Q

Main concerns of muscarinic receptor antagonists (Anticholerginic).

Usually we administer the drugs by _______ because when given ______, will have high incidence of adverse effects.

A

anticholinergic adverse effects: dry mouth, blurring vision, constipation

by transdermal patch; when given orally

36
Q

Main concerns of diphenhydramine

A
  • anticholinergic adverse effects: dry mouth, blurring vision, constipation
  • sedative
37
Q

List at least 5 management of nausea & vomiting in pregnancy

A
  1. lifestyle changes first, then if needed, pharmaco
  2. avoid having empty stomach, must eat!!
  3. avoid overly full stomach (take food in small amts every 1-2hrs)
  4. avoid coffee, high-fat, acidic or very sweet food
  5. take giner-containing foods
  6. high-protein food

Pharmaco (only if needed):

  • pyridoxine (vit.B6)
  • doxylamine (only if pyridone doesnt work)
38
Q

List management of nausea & vomiting in infants & kids

  1. Gastroparesis
  2. Post-op
  3. Chemo induced
A

let it run normally : maintain fluid and electrolyte balance

Pharmaco (only if persistent):

  1. Gastroparesis– prokinetic agents eg metoclopramide
  2. Post-op – 5-HT3 antagonists eg. ondansetron, granisetron
  3. Chemo induced– 5-HT3 antagonists & neurokinin 1 antagonist eg. aprepitant

PPNP drugs (7 decks)

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