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LEARNING ACTIVITY NO. 11

ANTI-EMETIC DRUGS

INTRODUCTION

Nausea and vomiting may be manifestations of a wide variety of conditions,

including adverse effects from medications; systemic disorders or infections;
pregnancy; vestibular dysfunction; central nervous system infection or increased
pressure; peritonitis; hepatobiliary disorders; radiation or chemotherapy; and
gastrointestinal obstruction, dysmotility, or infections.

LEARNING CONTENT

Anti-emetic Drugs

Considering the complexity of the mechanisms involved in emesis, it is not

surprising that antiemetic represent a variety of classes and offer a range of efficacies.
Anticholinergic drugs, especially the muscarinic receptor antagonist, scopolamine, and
H1-receptor antagonists, such as dimenhydrinate, meclizine, and cyclizine, are very
useful in motion sickness but are ineffective against substances that act directly on
the chemoreceptor trigger zone.

Pathophysiology of Nausea and Vomiting

The brainstem vomiting center is located in the lateral medullary reticular

formation and coordinates the complex act of vomiting through interactions with
cranial nerves VIII and X and neural networks in the nucleus tractus solitarius that
control respiratory, salivatory, and vasomotor centers. High concentrations of
muscarinic M1, histamine H1, and serotonin 5-HT3 receptors have been identified in
the vomiting center.

There are five sources of afferent input to the vomiting center:

1. The chemoreceptor trigger zone is located in the fourth ventricle in the area
postrema. This is outside the blood-brain barrier and is accessible to emetogenic
stimuli in the blood or cerebrospinal fluid. The chemoreceptor trigger zone is rich in
dopamine D2 receptors, serotonin 5-HT3 receptors, neurokinin 1 (NK1), and opioid
receptors.

2. The vestibular system is important in motion sickness via cranial nerve VIII. It is
rich in muscarinic and histamine H1 receptors.

3. Irritation of the pharynx, innervated by the vagus nerve, provokes a prominent gag
and retch response.

4. Vagal and spinal afferent nerves from the gastrointestinal tract are rich in 5-HT3
receptors. Irritation of the gastrointestinal mucosa by chemotherapy, radiation
therapy, distention, or acute infectious gastroenteritis leads to release of mucosal
serotonin and activation of these receptors, which stimulate vagal afferent input to the
vomiting center and chemoreceptor trigger zone.

5. The central nervous system plays a role in vomiting due to psychiatric disorders,
stress, and anticipatory vomiting prior to cancer chemotherapy.
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LEARNING OUTCOMES

At the end of the activity, the student is expected to:

1. Determine the anti-emetic effect of the substances to be tested

2. Compare the anti-emetic effect of the substances tested by means of

statistical analysis

3. Discuss the mechanism of nausea and vomiting and the means that drugs
available in the market can decrease the tendency of nausea and vomiting.

MATERIALS

Blue Vitreol (CuSO4.5H2O)

Mature Frogs (4 each group)

Tween 80

Earthworm/meal worm

Chlorpromazine, Meclizine, Granisetron, Metoclopramide

PROCEDURE

1. The frogs are divided into groups consisting of 2 each

2. Each frog is orally fed with earthworms 1 hr before the experiments.

3. The test samples are suspended in 5% Tween 80 and administered orally at

doses of 500 mg/kg body weight.

4. The control group of frogs receives only 5% Tween 80 solution

5. The frogs are allowed to stand for 30 min to stablize their conditions.

6. The copper sulfate pentahydrate (emetic agent) is administered orally and the
first emesis (emetic latency) is recorded for 60 min.

7. The results are judged by the prolongation of the emetic latency.

8. A significant prolongation of emetic latency is the sign of an anti-emetic

action of the test sample.

9. All numerical data are expressed as the means of ±S.E. The statistical
significance of the difference is determined by an unpaired student’s t-test

LEARNING EVALUATION

1. Why is there a need to prevent the emetic response of the body?

2. Discuss the different mechanisms of action of the different anti-emetics

available in the market

3. Discuss when a patient is in need of anti-emetic therapy.

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WORKSHEET

Name: Date:

Group No: Score:

LEARNING ACTIVITY NO. 11

ANTI-EMETIC AGENTS

DOCUMENTATION

Weighing of Frogs Administration of Earthworms

Administration of Blue Vitreol Observation of Emetic Latency

DATA AND RESULTS

Frog Weight (g) Amount of Volume of Emetic

Earthworms Blue Vitreol Latency
Given (g) Given (mL) (min.)
G1F1
G1F2
G2F1
G2F2
G3F1
G3F2
G4F1
G4F2
G5F1
G5F2
G6F1
G6F2
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LEARNING EVALUATION

1. Why is there a need to prevent the emetic response of the body?

2. Discuss the different mechanisms of action of the different anti-

emetics available in the market

3. Discuss when a patient is in need of anti-emetic therapy.

CONCLUSIONS: