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Mand's Pharmacology > Anti-emetics > Flashcards

Anti-emetics Flashcards

1
Q

What is emesis?

A

An emetic is an agent that causes vomiting.

Stages of emesis are nausea, retching and vomiting.

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2
Q

What causes emesis?

A

Disease states- migraine, bacterial and viral infections.
Physiological status- pregnancy.
Unwanted side effects- CINV and PONV, opioids.

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3
Q

What are the components of the vomiting reflux?

A

Regulated in the medulla.
The Chemoreceptor trigger zone. This is the main site of action for antiemetic drugs.
Vagal pathway (sensory input)
Vestibular pathway (affected by disorientated motions).

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4
Q

What are the actions of antiemetics?

A

Neurotransmitter antagonists- block neurotransmitters preventing triggering of emetic response.

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5
Q

List the different anti-emetics that block neurotransmitter release. (6)

A 
5HT3 block serotonin
H1 block histamine
M block ACH
D2 blocks dopamine
NK1 blocks substance P.
Enkephalin.
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6
Q

What are the most commonly used anti-emetic drugs?

A

5HT3- Serotonin
M- ACH
H- Histamine.

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7
Q

What anti-emetic target the vomiting centre?

A

M
H
NK1
5HT3

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8
Q

What anti-emetics block the vestibular pathway?

A

M

H1

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9
Q

What anti-emetics block the vagal pathway?

A

5HT3

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10
Q

What antiemetic blocks the chemoreceptor trigger zone?

A

D2
5HT3
NK1

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11
Q

What are the actions of H1 antagonists?

A

They target the vestibular pathway. Are used to treat motion sickness, vestibular disease and GI irritants.
The side effects include drowsiness and sedation.

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12
Q

What are examples of H1 antagonists

A

Cyclizine- used to treat motion sickness.

Cinnarizine- Morning sickness.

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13
Q

What are the actions of H3 agonists?

A

Activate H-receptors in the blood vessels of the inner ear.

Reverses the underlying problems of endolymphatic hydrops causing vasodilator and increased permeability.

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14
Q

What are the side effects of H3 agonists?

A

GI disturbances, headache, rash, pruritus.

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15
Q

What are examples of H3 agonists?

A

Betahistamine

Hydrochloride (anti-vertigo drug).

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16
Q

Explain anti-emetic Muscuarinic receptor (ACH) antagonists.

A

A good general purpose drug due to its non selective features
The drug of choice for motion sickness.
Targets vestibular pathway

17
Q

What are the side effects of muscuarinic receptor antagonists

A

Dry mouth and blurred vision- however less sedative effects than histamine antagonists.

18
Q

What are examples of anti-emetic ACH drugs?

A

Hyscoine and scopolamine.

19
Q

Explain D2 receptor antagonists

A

Strong representation in the CTZ.
Most powerful anti-emetic drug.
Used to treat uraemia, opiod induced emesis, CINV, GI disorders and viral gastroentritis.

20
Q

What are phenothiazamines?

A

D2 receptor antagonists that are the drug of choice for morning sickness.
Side effects include sedation, hypotension, dystonia, dyskineasia.

21
Q

What is metoclopramide?

A

D2 receptor antagonist.
Penetrated blood barrier.
Acts on GIT to increase gut motility.
Side effects include movement disorders, spasmodic torticolitis and menstrual disturbances.

22
Q

What is domperidone?

A

D2 receptor antagonist.
Does not penetrate blood barrier so therefore has less central effectiveness however has fewer side effects.
Used to treat migraines, CINV and sickness due to emergency contraception.

23
Q

What are anti-emetic serotonin receptor antagonists?

A

Work on the vagal, CTZ and vomiting centre.

Used to treat CINV and PONV and radiation induced vomiting.

24
Q

What is ondansteron?

A 
5HT3 antagonist. 
Drug of choice for CINV and PONV. 
Side effects include headache and GI disturbances. 
Strands of drug end in steron. 
Granisteron
Palonosteron.
25
Q

What are NK1 antagonists?

A

They become active at the late phase of emesis with cytotoxic drugs.
Substance P antagonists that work on the CTZ and vomiting centre.

26
Q

What is aprepitant?

A

A type of NK1 antagonist.
Used for CINV and PONV.
Strands inlcude fosaprepitant.
Drugs that end in pitant.

27
Q

Explain the anti-emetic effects of cannabionoids?

A

Act as agonists of CB (brain stem) and CTZ.

E.g Nabilone and Marinol

28
Q

Explain the steroid effects of anti-emetics.

A

Dexamethasone.

Used to treat CINV in conjunction with D2 or 5HT3

29
Q

List some therapeutic uses of emetics

A

Syrup of ipecac and Apomorphine stimulate CTZ>

30
Q

Where does 5HT3 target

A

Vomiting centre, vagal pathway, CTZ

31
Q

Where do M target?

A

Vomiting centre, vestibular pathway

32
Q

Where do NK1 target?

A

Vomiting centre and the CTZ

33
Q

Where do D2 target?

A

CTZ

34
Q

Where do H target?

A

Vestibular pathway and the vomiting centre

Mand's Pharmacology (12 decks)

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