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LCRS 1 > Anti-Emetics > Flashcards

Anti-Emetics Flashcards

1
Q

State the 4 major classes of anti-emetic drugs.

A

H1 receptors
Dopamine (D2) receptor antagonists
Muscarinic receptor antagonists
Serotonin (5-HT3) receptor antagonists

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2
Q

What types of receptors in the stomach transmit signals to the vomiting centre and chemoreceptor trigger zone?

A

Chemoreceptors and Mechanoreceptors

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3
Q

What is special about the location of the CTZ and vomiting centre?

A

It is located in a part of the brain that has a very porous blood brain barrier
So the CTZ and vomiting centre act as an early warning system to protect the brain from toxin damage

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4
Q

What are the uses of promethazine?

A

Motion sickness

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5
Q

Give of example of dopamine receptor antagonists.

A

Metoclopramide

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6
Q

Give an example of a muscarinic receptor antagonist.

A

Hyoscine

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7
Q

What is the mode of action of muscarinic receptor antagonists in anti-emetics?

A

Act centrally on the CTZ, vestibular nuclei and vomiting centre to block the activation of the vomiting centre

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8
Q

What is hyoscine used for?

A

Prevention of MOTION SICKNESS

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9
Q

Give an example of a serotonin receptor antagonist.

A

Ondansetron

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10
Q

What is the mode of action of serotonin receptor antagonists?

A

Act to block transmission in visceral afferents and CTZ

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11
Q

What is the main use of serotonin receptor antagonists as an anti-emetic?

A

MAIN USE: preventing anti-cancer drug induced vomiting (especially cisplatin)

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12
Q

Example of treatment that can cause vomiting

A

Cisplatin for lung cancer-chemotherapy induced nausea and vomiting

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13
Q

Pathophysiology of cisplatin

A

Toxic to ECL cells in the stomach which cause release of free radicals. These free radicals cause an excessive serotonin release. The serotonin activates 5-HT3A receptors on nerve fibres to Chemoreceptor Trigger Zone

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14
Q

Effect of activation of CTZ

A

Activates fibres to vomiting centre which induces feeling of vomiting

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15
Q

Combined therapy for CINV

A

Ondensatron- 5HT3A antagonist
Glucocorticoids- reduce free radicals
Aprepitant- neurokinin 1 therapy

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16
Q

Common presentation of afro-carribean person for vomiting

A

Motion sickness

17
Q

Pathophysiology of motion sickness

A

Neural mismatch in the labyrinth which activates histamine receptors on vestibular nuclei. Vestibular nerve fibres then activate muscarinic receptoes on CTZ which activates muscarininc receptors in VC

18
Q

Treatment for motion sickness

A

Promethazine

Hyoscine

19
Q

What is promethazine

A

H1 receptor antagonist

20
Q

Pathophysiology of gastroparesis

A

Delayed emptying of the stomach and reduced stomach contraction.

21
Q

How does gastroparesis cause vomiting

A

Get an increase in 5-HT that activates 5-HT3A receptors on CTZ-> this activates muscarinic fibres on VC

22
Q

Treatment of gastroparesis

A

Metoclopramide

23
Q

What does metoclopramide do

A

D2 receptor antagonist

5-HT3A receptor antagonist - acts on CTZ

24
Q

How is a dopamine 2 receptor antagonist useful in vomiting treatment

A

Stimulates gastric opening

Inhibits D2 receptors in CTZ

25
Q

Where does CTZ recieve inputs from

A

Stomach

Vestibular nuclei

26
Q

Receptors associated with CTZ

A

Serotonin- 5HT3A
Muscarinc 1-2
Dopamine 2

27
Q

Receptor associated with vestibular nuclei

A

Histamine

28
Q

Receptor associated with VC

A

Muscarinic

29
Q

Main causes of vomiting

A 
Cytotoxic drugs
Motion sickness
Pregnancy
GI problems
Parkinsons treatment due to dopamine
30
Q

Side effects of muscarinic antagonists

A

Drowsiness

Dry mouth

31
Q

Side effects of H1 antagonist

A

Drowsiness

32
Q

Side effects of D2 receptor antagonists

A

Extra-pyramidal effects

Galactorrhoea

33
Q

Side effects of serotonin antagonists

A

Headaches

Constipation

LCRS 1 (58 decks)

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