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pharmacology GI > Drugs and motility in the GI tract - Anti-Emetics > Flashcards

Drugs and motility in the GI tract - Anti-Emetics Flashcards

1
Q

what is the function of anti-emetics

A

they act centrally to inhibit or prevent nausea or vomiting

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2
Q

Give two examples phenothiazine anti-emetics

A

1) Chlorpromazine

2) Acepromazine

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3
Q

What receptor to Chlorpromazine and Acepromazine act on?

A

D2 receptor antagonist

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4
Q

Where in the brain do Chlorpromazine and Acepromazine act?

A

In the chemical trigger zone

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5
Q

When are Chlorpromazine and Acepromazine used?

A

Good at preventing vomiting by agents that directly stimulate the CTZ.
Its sedative side effects is useful for treating motion sickness

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6
Q

What are the side effects of Chlorpromazine and Acepromazine?

A

sedation
hypotension (due to dilation of blood vessels) platelet dysfunction
Ataxia (movement disorder)

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7
Q

why cant pregnant or nursing mothers have Chlorpromazine and Acepromazine?

A

They can cross placenta and get into foetus, and can get to baby via breast milk
The breakdown of phenothiazines is slower in foetus so causes respiratory problems for the baby

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8
Q

Give other examples of a anti-emetics that are NOT phenothiazines

A

Metoclopramide

Ondasetron

nabilone

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9
Q

What receptors does Metoclopramide act on?

A

D2 and 5-HT3 receptor antagonist

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10
Q

Where in the brain does Metoclopramide act?

A

It acts in the chemical trigger zone

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11
Q

What is the mechanism of action of Metoclopramide?

A

increases muscle tone in the lower oesophageal sphincter to prevent vomiting

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12
Q

What are the side effects of Metoclopramide?

A

disorders of movement

prolactin release

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13
Q

What receptor does Ondasetron and nabilone act on?

A

5-HT3 receptor antagonists

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14
Q

Where in the brain does Ondasetron and nabilone act?

A

It acts in the chemical trigger zone

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15
Q

When is Ondasetron used?

A

particularly useful in chemotherapy or radiation induced vomiting

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16
Q

When is nabilone used?

A

Used in cytotoxic induced vomiting

Only used of conventional drugs dont work

17
Q

what are the side effects of Ondasetron and nabilone?

A

Euphoria

drowsiness

18
Q

Give an example of an anit-emetic that is a 5HT-4 receptor agonist

A

Cisapride

19
Q

Why is Cisapride no linger used?

A

no longer used in medicine due to long-QT, still used in vetinary

20
Q

Where in the brain does Cisapride act?

A

chemical trigger zone and visceral afferents

21
Q

What is the mechanism of action of Cisapride?

A

Acts peripherally to increase gastro-oesophageal sphincter contraction and GI motility.

22
Q

What are the side effects of Cisapride?

A

Long QT-syndrome

Diarrhoea

Abdominal cramp

23
Q

Give an example of a corticosteroid that is an anti-emetic

A

Dexamethasone

24
Q

At which receptor does Dexamethasone act?

A

5HT3 receptor antagonists

25
Q

Where in the brain does Dexamethasone act?

A

chemical trigger zone and visceral afferents

26
Q

What is the mechanism of action of Dexamethasone?

A

It decreases prostaglandin activity in the brain, increases endorphin release and potentiating effects of other anti-emetics.

27
Q

When is the corticosteroid Dexamethasone used?

A

Used as a single agent against mild to moderate emetogenic chemotherapy.
For highly emetogenic chemotherapy it works well with 5HT3 receptor antagonists preventing post operative nausea and vomiting.

28
Q

Give 3 examples of anti-emetics that are H1 histamine receptor antagonists and mACh receptor antagonists?

A

Diphenhydramine

Cyclizine

Promethazine

29
Q

Where do Diphenhydramine, Cyclizine, and Promethazine act in the brain?

A

Vestibular nuclei
Nucleus of solitary tract
Voimiting centre

30
Q

When are Diphenhydramine, Cyclizine, and Promethazine used?

A

Highly effective in motion sickness and against stimuli acting locally in the stomach

31
Q

What are the side effects of Diphenhydramine, Cyclizine, and Promethazine?

A

side effects include drowsiness and sedation as they are dirty drugs that have anti-muscarinic activity

32
Q

Give an example of an anti-emetic that is an mACh receptor antagonist

A

Hyoscine

scopolamine

33
Q

Where does hyoscine act in the brain?

A

Vestibular nuclei
Nucleus of solitary tract
Voimiting centre

34
Q

When is Hyoscine used and not used

A

effective in motion sickness

not effective against substances acting directly on the CTZ eg chemotherapy

35
Q

What are the side effects of

A

drowsiness
blurred vision
dry mouth

pharmacology GI (9 decks)

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