Antiemetics Amoebiasis

Antiemetics
1. Write the most appropriate antiemetic drug for each of the following conditions.
Choose the most appropriate antiemetic for the following conditions. Explain the reasons for your
choice of drugs
(a) Motion sickness –hyoscine

(b) Vomiting due to cytotoxic drug - ondansetron
(c) Morning sickness -promethazine
(d) Vertigo –cinnarazine
a) Motion sickness –hyoscine

- anticholinergic
Mechanism of action: blocks central muscarinic receptor on VC and gut (relaxation of GIT)
- Given one hour before journey, lasts for 4-6 hours
- Alternatively, hyoscine may be administered as dermal patch
(b) Vomiting due to cytotoxic drug - ondansetron

- 5HT3 antagonist
- block 5HT3 receptors both centrally (CTZ, Solitary Tract Nucleus) and peripherally in the
gastrointestinal tract
- highly effective for cytotoxic drug induced & radiation induced vomiting
- For severe vomiting, ondansetron plus dexamethasone with or without lorazepam (all given IV)
(c) Morning sickness -promethazine

- antihistamine
- block H1 receptors at VC
- is preferable for hyperemesis gravidarum
(d) Vertigo –cinnarazine or cyclizine

- antihistamine
- block H1 receptors at VC, antiemetic action
- may be used to relieve an acute attack
1. Metoclopramide: (TTFTF)
a) is useful for diabetic gastroparesis
b) is a prokinetic agent which increases gastrointestinal motility
c) cause no extrapyramidal side effects
d) is D2 receptor antagonist at CTZ
e) It cannot cross the blood brain barrier
2. Match the following drugs and their uses: (TFTTF)

a) apprepitant / vomiting due to cytotoxic drugs
b) meclizine / vomiting due to morphine
c) diphenhydramine /Meniere’s disease
d) hyoscine / motion sickness
e) ondansetron /hyperemesis gravidarum
3. Metoclopramide: (TFTFF)
a) is potent antidoperminergic with cholinomimetic properties
b) is used in vomiting and diarrhoea (Side effect-diarrhoea)
c) is used in vomiting due to cytotoxic drugs
d) is also used in motion sickness
e) It is used to promote post-partum lactation (domperidone)
4. Check the followings:(FFTT)
a) Ondansetron is most appropriate antiemetic for motion sickness.
b) Antacids are no longer recommended for the treatment of peptic ulcer.
c) Domperidone and omeprazole combination relieve gastroesophageal reflux
disorders.
d) Liquid paraffin is a fecal softener.
5. Ondansetron:(FTFFT)
a) is a prokinetic agent
b) used for prevention of vomiting due to radiation therapy
c) best used for pregnancy induced vomiting (morning sickness)
d) anti-emetic effect is through blockade on histamine receptor
e) more efficacious than metoclopramide
6. Domperidone: (TTFTT)
a) is a prokinetic and anti-emetic drug
b) is a D2 antagonist
c) can cross the blood brain barrier
d) is used to promote post partum-lactation
e) is used in non-ulcer dyspepsia
7. Metoclopramide: (FTTT)
a) decreases gut peristalsis
b) relaxes pyloric antrum and duodenal cap
c) is used to empty stomach before emergency anesthesia and labour
d) is used in gastrooesophageal reflux disease
8. Antiemetics which block dopamine D2 receptors include:(TFFTF)

a) domperidone
b) ondansetron
c) hyoscine
d) metoclopramide
e) cyclizine
Amoebiasis
1. Describe the drug treatment (rational therapy) of symptomatic intestinal amoebiasis. (acute amoebic
deysentry)
Pathogenesis--- Causal organism – Entamoeba histolytica, ingestion of quadrinucleated cyst of E.
histolytica from fecally contaminated food or water
Objectives
1. Curative -To kill the tissue invading trophozoites
2. Prophylaxis - To eradicate cysts in the lumen
Drug treatment according to objectives

1. To kill the tissue invading trophozoites, Following tissue amoebicides can be used
Nitroimidazole- metronidazole, tinidazole
Dehydroemetine
Chloroquine
Nitroimidazole is the drug of choice
Metronidazole
MOA- The nitro group of metronidazole is able to serve as an electron acceptor, forming reduced
cytotoxic compounds that bind to proteins and DNA, resulting in cell death.
PA- It kills trophozoites but not cysts of E. histolytica and effectively eradicates intestinal and
extraintestinal tissue infections
***Metronidazole plus a luminal amoebicide is the treatment of choice for amebic colitis and dysentery.
This combination provides cure rates of greater than 90 percent
Dose- 800mg tds for 10 days
Alternative
Dehydroemetine
MOA- inhibit protein synthesis, affects almost all tissues
Systemic amoebicidal (to control severe symptoms), Dehydroemetine may be less toxic
Should not be taken for more than 5 days and needs close clinical observations.
2. To eradicate cysts in the lumen, following luminal amoebicides can be used

- Diloxanide furoate
- Iodoquinol, clioquinol
- Paromomycin, erythromycin, tetracycline
Diloxanide furoate-DOC
Mechanism of action - unknown
- after oral ingestion, the ester is largely hydrolysed in the lumen or mucosa of the intestine to
diloxanide and furoic acid; only diloxanide appears in the systemic circulation
- the blood concentration of diloxanide peaks within 1hr, 60-90% excreted in urine as glucuronide forms
within 48 hrs, with no cumulative effect
- the unabsorbed diloxanide is the active anti-amoebic substance and is not attacked by gut bacteria
Pharmacological action- direct amoebicidal action, affecting the amoebae before encystment
Dose-500mg tds for 10 days
Alternative
Paromomycin
- related to aminoglycoside
Mechanism of action – irreversibly inhibits 30s ribosomal subunit - inhibits protein synthesis, bactericidal
Pharmacological action- direct luminal amoebicidal action and also has antibacterial activity against
normal and pathogenic organism in GIT
Used for asymptomatic and mild intestinal infection, eradication of cysts
2.Describe the drug treatment of asymptomatic intestinal amoebiasis.
Pathogenesis
Causal organism – Entamoeba histolytica
Objective –to eradicate cysts in the lumen
Drug treatment
Luminal amoebiasis is usually treated with luminal amoebicides
Luminal amoebicides are
1. Diloxanide furoate
2. Iodoquinol, clioquinol
3. Paromomycin, erythromycin, tetracycline
Each drug eradicates carriage in about 80- 90% of patients with a single course of treatment
Diloxanide furoate
Mechanism of action - unknown
- after oral ingestion, the ester is largely hydrolysed in the lumen or mucosa of the intestine to
diloxanide and furoic acid; only diloxanide appears in the systemic circulation
- the blood concentration of diloxanide peaks within 1hr, 60-90% excreted in urine as glucuronide forms
within 48 hrs, with no cumulative effect
- the unabsorbed diloxanide is the active anti-amoebic substance and is not attacked by gut bacteria
Pharmacological action
- direct amoebicidal action, affecting the amoebae before encystment
Drug of choice for asymptomatic patients
Iodoquinol
Pharmacological action - direct amoebicidal effect (both motile and cyst forms)
Effective against organisms in the bowel lumen but not against trophozoites (Asymptomatic cyst passers)
Paromomycin
- related to aminoglycoside
Mechanism of action – irreversibly inhibits 30s ribosomal subunit - inhibits protein synthesis, bactericidal
Therapeutic uses - asymptomatic and mild intestinal infection, eradication of cysts
Erythromycin
Macrolide antibiotic, bacteriostatic
reversibly inhibits 50s ribosomal subunit -> inhibits protein synthesis
indirect luminal amebicides
Tetracycline
bacteriostatic, reversibly inhibits 40s ribosomal subunit -> inhibits protein synthesis
indirect luminal amoebicides
if there is sign and symptoms of invasive intestinal amoebiasis -> tissue amoebicide – metronitazole

Antiemetics Amoebiasis

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Antiemetics

(a) Motion sickness –hyoscine

a) Motion sickness –hyoscine

(b) Vomiting due to cytotoxic drug - ondansetron

(c) Morning sickness -promethazine

(d) Vertigo –cinnarazine or cyclizine

2. Match the following drugs and their uses: (TFTTF)

8. Antiemetics which block dopamine D2 receptors include:(TFFTF)

Drug treatment according to objectives

2. To eradicate cysts in the lumen, following luminal amoebicides can be used

2.Describe the drug treatment of asymptomatic intestinal amoebiasis.

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