Anti-Emetic Drugs

ANTI-EMETIC DRUGS

Q. 1

Which of the following 5HT3 receptor blockers has highest receptor affinity

 A

Ondansetron

 B

Granisetron

 C

Dolasetron

 D

Palonosetron

Q. 1

Which of the following 5HT3 receptor blockers has highest receptor affinity

 A

Ondansetron

 B

Granisetron

 C

Dolasetron

 D

Palonosetron

Ans. D

Explanation:

Palonosetron [Ref. Katzung Pharma 10th/e p 1027] 5 HT3 subtypes of receptors are important for

– Emesis

– Gut peristalsis

– Bradycardia

– Transient hypotension

– Apnea

– Itch

5 HT3 receptor antagonists are:

Ondensetron – Granisetron – Pahmosetron

“Among the 5 HT3 receptor blockers palonosetron is a new i.v. agent that has greatest affinity for 5 HT3 receptor and has a long serum half life”.


Q. 2 Antiemetic used in vomiting induced by anticancer drugs is:
 A Ondansetron
 B Cisapride
 C Metoclopramide
 D Tritluopromazine
Q. 2 Antiemetic used in vomiting induced by anticancer drugs is:
 A Ondansetron
 B Cisapride
 C Metoclopramide
 D Tritluopromazine
Ans. A

Explanation:

Ondansetron


Q. 3

A 67-year-old woman is being treated for metastatic ovarian cancer with cisplatin and cyclophosphamide. To prevent nausea and vomiting, she is given an agent that selectively antagonizes 5-hydroxytryptamine-3 (5-HT3) receptors. Which of the following drugs is this patient most likely taking?

 A

Dimenhydrinate

 B

Dronabinol

 C

Metoclopramide

 D

Ondansetron

Q. 3

A 67-year-old woman is being treated for metastatic ovarian cancer with cisplatin and cyclophosphamide. To prevent nausea and vomiting, she is given an agent that selectively antagonizes 5-hydroxytryptamine-3 (5-HT3) receptors. Which of the following drugs is this patient most likely taking?

 A

Dimenhydrinate

 B

Dronabinol

 C

Metoclopramide

 D

Ondansetron

Ans. D

Explanation:

Cisplatin is an antineoplastic commonly used in the treatment of metastatic ovarian and testicular cancers, as well as advanced bladder cancer. This medication is associated with profound nausea and vomiting; in fact, it is considered to be one of the most emetogenic agents on the pharmaceutical market.

The selective 5-hydroxytryptamine-3 (5-HT3) receptor antagonists are potent anti nausea and anti emetogenic agents indicated for prevention of nausea and vomiting associated with cancer chemotherapy. Examples of 5-HT3 receptor antagonists include ondansetron, granisetron, and dolasetron.

Dimenhydrinate is an antihistamine with anticholinergic activity; it is indicated for the treatment of nausea and vomiting associated with motion sickness.
 
Dronabinol is the principal psychoactive substance present in Cannabis sativa (marijuana). The mechanism of its antiemetic action is largely unknown; it is indicated for the treatment of severe nausea and vomiting when conventional therapies are ineffective.
 
Metoclopramide is a prokinetic agent indicated for the treatment of gastroesophageal reflux disease and diabetic gastroparesis. Since this agent blocks dopaminergic receptors in the chemotrigger zone, it is also effective in the treatment of severe nausea and vomiting.

Quiz In Between


Q. 4

Fosaprepitant is used as:

 A

Anitidepressant

 B

Anitiemetic

 C

Antihypertensive

 D

Diuretic

Q. 4

Fosaprepitant is used as:

 A

Anitidepressant

 B

Anitiemetic

 C

Antihypertensive

 D

Diuretic

Ans. B

Explanation:

Neurokinin 1 (NK1)-receptor antagonists have antiemetic properties that are mediated through central blockade in the area postrema.
Aprepitant (an oral formulation) is a highly selective NK1-receptor antagonist that crosses the blood-brain barrier and occupies brain NK1 receptors. It has no affinity for serotonin, dopamine, or corticosteroid receptors.
Fosaprepitant is an intravenous formulation that is converted within 30 minutes after infusion to aprepitant.
 
Ref: Katzung 11th edition Chapter 60.

Q. 5

All of the following is used as antiemetic, EXCEPT:

 A

Granisetron

 B

Dolasetron

 C

Palonosetron

 D

Alosetron

Q. 5

All of the following is used as antiemetic, EXCEPT:

 A

Granisetron

 B

Dolasetron

 C

Palonosetron

 D

Alosetron

Ans. D

Explanation:

Alosetron is a 5-HT3 antagonist that has been approved for the treatment of patients with severe IBS with diarrhea.
Four other 5-HT3 antagonists (ondansetron, granisetron, dolasetron, and palonosetron) have been approved for the prevention and treatment of nausea and vomiting (see Antiemetics); however, their efficacy in the treatment of IBS has not been determined.
The differences between these 5-HT3 antagonists that determine their pharmacodynamic effects have not been well studied
 
Ref: Katzung 11th edition Chapter 60.

Q. 6

Aprepitant is used as:

 A

Anitidepressant

 B

Antiemetic

 C

Antihypertensive

 D

Diuretic

Q. 6

Aprepitant is used as:

 A

Anitidepressant

 B

Antiemetic

 C

Antihypertensive

 D

Diuretic

Ans. B

Explanation:

The actions of substance P and neurokinins A and B are mediated by three G protein-coupled tachykinin receptors designated NK 1, NK 2, and NK 3.

Several nonpeptide NK1 receptor antagonists have been developed.

These compounds are highly selective and orally active, and enter the brain.

Recent clinical trials have shown that these antagonists may be useful in treating depression and other disorders and in preventing chemotherapy-induced emesis.

The first of these to be approved for the prevention of chemotherapy-induced nausea and vomiting is aprepitant.

Ref: Katzung, 11th edition, Chapter 17.

Quiz In Between


Q. 7

Antiemetic acting on H2 receptors –

 A

Promethazine

 B

Metoclopramide

 C

Ondansetron

 D

Amiodarone

Q. 7

Antiemetic acting on H2 receptors –

 A

Promethazine

 B

Metoclopramide

 C

Ondansetron

 D

Amiodarone

Ans. A

Explanation:

Ans. is ‘a’ i.e., Promethazine

Promethazine is an antihistaminic antiemetic.


Q. 8

Metoclopramide is useful for all except –

 A

Motion sickness

 B

Chemotherapy induced vomiting

 C

Antiemetic

 D

All

Q. 8

Metoclopramide is useful for all except –

 A

Motion sickness

 B

Chemotherapy induced vomiting

 C

Antiemetic

 D

All

Ans. A

Explanation:

Ans. is ‘a’ i.e., Motion sickness

o Metoclopramide can be used as an antiemetic in postoperative, drug induced, disease associated, radiation sickness,

but is less effective in motion sickness.

o It should not be used to augment lactation. Though the amount secreted in milk is small, but suckling infant may develop loose motions, dystonia, myoclonus.


Q. 9

The statement that is NOT true of domperiodone is that-

 A

It rarely causes extrapyramidal side effects

 B

It is a DO receptor antagonist

 C

Its antiemetic efficacy is higher than metoclopramide

 D

It causes loose stool

Q. 9

The statement that is NOT true of domperiodone is that-

 A

It rarely causes extrapyramidal side effects

 B

It is a DO receptor antagonist

 C

Its antiemetic efficacy is higher than metoclopramide

 D

It causes loose stool

Ans. C

Explanation:

Ans. is ‘c’ i.e., Its antiemetic efficacy is higher than metoclopramide

Domperidone is a selective dopamine D2 receptor antagonist which dose not cross BBB and therefore, does not cause extrapyramidal side effects or hyperprolactinemia.

o It has moderate efficacy as an antiemetic agent, which is less than metoclopramide.

o There are more chances of diarrhea because of slightly greater action on lower GIT.

Quiz In Between


Q. 10

Granisetron is used in?

 A

Motion sickness

 B

Sedation in endoscopy

 C

Chemotherapy induced nausea & vomiting

 D

Gastroesophageal reflux disease

Q. 10

Granisetron is used in?

 A

Motion sickness

 B

Sedation in endoscopy

 C

Chemotherapy induced nausea & vomiting

 D

Gastroesophageal reflux disease

Ans. C

Explanation:

Ans. is ‘c’ i.e., Chemotherapy induced nausea & vomiting

5-HT3 blockers (e.g. ondansetron, granisetron etc) are the drugs of choice for chemotherapy induced nausea and vomiting.


Q. 11

Which drug is given in delayed vomiting after chemotherapy –

 A

Metoclopramide

 B

Hyoscine

 C

Domperiodone

 D

Aprepitant

Q. 11

Which drug is given in delayed vomiting after chemotherapy –

 A

Metoclopramide

 B

Hyoscine

 C

Domperiodone

 D

Aprepitant

Ans. D

Explanation:

Ans. is ‘d’ i.e., Aprepitant

o Cisplatin can induce vomiting within 24 hours or after 2 days. DOC for the early vomiting is ondensetron while for delayed vomiting is aprepitant (substant P antagonist).


Q. 12

All of the following are effective against cytotoxic drug induced emesis except –

 A

Dexamethasone

 B

Hyoscine

 C

Metoclopramide

 D

Ondansetron

Q. 12

All of the following are effective against cytotoxic drug induced emesis except –

 A

Dexamethasone

 B

Hyoscine

 C

Metoclopramide

 D

Ondansetron

Ans. B

Explanation:

Ans. is ‘b’ i.e., Hyoscine

Quiz In Between


Q. 13

All of the following drug may be used for motion sickness except –

 A

Hyoscine

 B

Dicyclomine

 C

Domperidone

 D

Scopolmine

Q. 13

All of the following drug may be used for motion sickness except –

 A

Hyoscine

 B

Dicyclomine

 C

Domperidone

 D

Scopolmine

Ans. C

Explanation:

Ans. is ‘c’ i.e., Domperidone

o Drugs used are :

a)         Anticholinergics —> Hyoscine (Scopolamine), Dicyclomine.

b)      Hl-antihistaminic —> Promethazine, cyclizine, meclizine, cinnarizine, etc.

o Hyoscine (scopolamine) is the most effective drug for motion sickness.

About option ‘c’

o Domperidone is a prokinetic drug and acts by D2 blockade. It is ineffective in motion sickness as vestibular pathway does not involve dopaminergic link.


Q. 14

Most potent antiemitic agent used in preoperative period

 A

Glycopyrolate

 B

Hyoscine

 C

Atropine

 D

Metochlorpromide

Q. 14

Most potent antiemitic agent used in preoperative period

 A

Glycopyrolate

 B

Hyoscine

 C

Atropine

 D

Metochlorpromide

Ans. D

Explanation:

D i.e. Metochlopromide

  • Metochlopramide increases lower esophageal sphinter tone, speeds gastric emptying & lowers gastric fluid volume & decreases risk for aspiration pneumonia due to antiemetic effect

Q. 15

Drugs indicated in drug induced vomiting are all except: 

March 2012

 A

Metoclopramide

 B

Hyoscine

 C

Ondansteron

 D

Chlorpromazine

Q. 15

Drugs indicated in drug induced vomiting are all except: 

March 2012

 A

Metoclopramide

 B

Hyoscine

 C

Ondansteron

 D

Chlorpromazine

Ans. B

Explanation:

Ans: B i.e. Hyoscine

Anti-emetic drugs

  • Metoclopramide is an effective and popular drug for many types of vomiting – postoperative, drug induced, disease associated (migraine), radiation sickness, etc.
  • Hyoscine is the most effective antiemetic drug for motion sickness and is not effective in vomiting of other etiologies
  • Ondansetron belongs to a new class of antiemetic drugs developed to control cancer chemotherapy/radiotherapy induced vomiting
  • Neuroleptics/antipsychotics have broad spectrum antiemetic action effective in drug induced and post-anaesthetic nausea and vomiting etc.

Quiz In Between


Q. 16

Which of the following anaesthetic agent also has anti-emetic property:           

September 2006

 A

Ketamine

 B

Thiopentone

 C

Propofol

 D

Nitrous oxide

Q. 16

Which of the following anaesthetic agent also has anti-emetic property:           

September 2006

 A

Ketamine

 B

Thiopentone

 C

Propofol

 D

Nitrous oxide

Ans. C

Explanation:

Ans. C: Propofol

Anaesthetics with anti-emetic property:

  • Midazolam given at the onset of anaesthesia has been shown in to be as effective as ondansetron
  • Propofol is versatile; the drug can be given for short or prolonged sedation as well as for general anaesthesia. It is an anti-emetic.

Q. 17

Most effective agent to prevent motion sickness is‑

 A

Ephedrine

 B

Nedocromil

 C

Cyproheptidine

 D

Hyoscine

Q. 17

Most effective agent to prevent motion sickness is‑

 A

Ephedrine

 B

Nedocromil

 C

Cyproheptidine

 D

Hyoscine

Ans. D

Explanation:

Ans. is `d’ i.e., Hyoscine

Motion sickness is more easily prevented than cured.

Transdermal hyoscine (scopolamine) is the best agent for the prevention of /notion sickness.

Antihistamines can also be used for prevention.


Q. 18

All are antiemetic except ‑

 A

Ondansetran

 B

Metoclopramide

 C

Chlorpromazine

 D

Bismuth

Q. 18

All are antiemetic except ‑

 A

Ondansetran

 B

Metoclopramide

 C

Chlorpromazine

 D

Bismuth

Ans. D

Explanation:

Ans. is ‘d’ i.e., Bismuth

Antiemetic drugs

  1. Anticholinergics → Hyoscine, Dicyclomine.
  2. H1 antihistaminics → Promethazine, cyclizine, Cinnarizine, etc.
  3. Neuroleptics (D2 blockers) → Chlorpromazine, Haloperidol, Droperidole etc.
  4. Prokinetics drugs → Metoclopramide, Domperidone, cisapride, Mosapride, Tegaserod.
  5. 5-HT3 antagonists → Ondansetron, Granisetron.
  6. Adjuvant antiemetics → Dexamethasone, BZDs, Cannabinoids, Clonidine & ephedrine.

Quiz In Between


Q. 19

Best anti – Emetic for patient treated with radiotherapy –

 A

Clonidine

 B

Metoclopromide

 C

Ondansetron

 D

Cisapride

Q. 19

Best anti – Emetic for patient treated with radiotherapy –

 A

Clonidine

 B

Metoclopromide

 C

Ondansetron

 D

Cisapride

Ans. C

Explanation:

Ans. is ‘c’ i.e., Ondansetron

Chemotherapy induced nausea and vomiting:

Cytotoxic drugs and radiation cause cellular damage which leads to release of 5-HT from intestine and activation of emetogenic 5-HT3 receptors. Therefore, 5-HT3 receptor antagonists (e.g. ondenstron) are the DOC for this condition.

Cisplatin is the most common culprit causing chemotherapy induced nausea and vomiting.

Drugs used to treat chemotherapy induced nausea and vomiting are:

i)  5-HT3 antagonists (drug of choice): Ondansetron, dolasetron, palonosetron, granisetron.

ii) Other drugs: Dexamethasone, methylprednisolone, metoclopramide, BZDs (lorazepam) and aprepitant.

Cisplatin can induce vomiting within 24 hours or after 2 days. DOC for the early vomiting is ondensetron while for delayed vomiting is aprepitant (substant P antagonist).


Q. 20

Antiemetic action is through ‑

 A

Chemoreceptor triggrezone (CTZ)

 B

H1 agonist

 C

Diantagonist

 D

Olfactory apparatus

Q. 20

Antiemetic action is through ‑

 A

Chemoreceptor triggrezone (CTZ)

 B

H1 agonist

 C

Diantagonist

 D

Olfactory apparatus

Ans. A

Explanation:

Ans. is ‘a’ i.e., .LCTZ

Pathophysiologv of vomiting

  • Useful vomiting occurs as a protective mechanism for eliminating irritant or harmful substances from upper GIT.
  • The act of emesis is controlled by vomiting (emetic) centre in the medulla.
  • Close to vomiting centre are other visceral centre, including those for respiration, salivation and vascular control, which give rise to the prodromal sensations of vomiting.
  • The vomiting centre does not initiate, but rather it coordinate the act of emesis on receiving stimuli from various sourse, e.g.‑
  1. The chemoreceptor trigger zone (CTZ) – most important.
  2. The vestibular system
  3. The periphery, e.g. distension or irritation of the gut, myocardial infarction, biliary or renal stone.
  4. Cortical centres
  • Vomiting centre and nucleus of tractus solitarius contain muscarinic cholinergic and histamine H1 receptors.
  • CTZ is located in area postrema (outside BBB) and contains Dopamine D2, opioid & serotonine 5-HT3 receptors.
  • So, antiemetic that act on vomiting centre have antimuscarinic and antihistaminic action can alleviate vomiting from any cause.
  • Drugs acting on CTZ have Dopamine D2 antagonistic and 5-HT3 antagonistic action → effective only in vomiting mediated by stimulation of chemoreceptors (by morphine, cytotoxic drugs, digoxin).

Note: CTZ is accesible to blood-borne drugs, mediators, hormone, toxins etc. because it lies outside the blood brain barrier.

  • 5HT4 agonistic (cisapride) action promotes gastrointestinal transient → prokenetic action (not antiemetic action). Antiemetic action of these drugs (cisapride) is due to weak 5-HT3 antagonistic action.

Q. 21

Antiemetic Phenothiazine with labrynthine suppressant activityused for vertigo is ‑

 A

Prochlorperazine

 B

Cinnarazine

 C

Hyoscine

 D

Promethazine

Q. 21

Antiemetic Phenothiazine with labrynthine suppressant activityused for vertigo is ‑

 A

Prochlorperazine

 B

Cinnarazine

 C

Hyoscine

 D

Promethazine

Ans. A

Explanation:

Ans. is ‘A’ i.e., Prochlorperazine

Labyrinthine suppressants used in vertigo

They suppress end organ receptors or inhibit central cholinergic pathways in vestibular nuclei.

These are :‑

  1. Antihistaminics (with anticholinergic action) – cinnarizine, cyclizine, dimenhydrinate, diphenhydramine, promethazine.
  2. Anticholinergics- atropine, hyoscine.
  3. Antiemetic phenothiazines-prochlorperazine, thiethylperazine.

Quiz In Between


Q. 22

All drugs are available as transdermal patches in India, except 

 A

Fentanyl

 B

Nitroglycerine

 C

Hyoscine

 D

Nicotine

Q. 22

All drugs are available as transdermal patches in India, except 

 A

Fentanyl

 B

Nitroglycerine

 C

Hyoscine

 D

Nicotine

Ans. C

Explanation:

Ans. is ‘c’ i.e., Hyoscine 

“Transdermal patches ofNTG, fentanyl, nicotine and estradial are available in India, where as those of isosorbide dinitrate, hyoscine and clonidine are marketed elsewhere”. — KDT


Q. 23

Which drug is used in treatment of vertigo

 A

Cinnarizine

 B

Metoclopramide

 C

Cisapride

 D

None

Q. 23

Which drug is used in treatment of vertigo

 A

Cinnarizine

 B

Metoclopramide

 C

Cisapride

 D

None

Ans. A

Explanation:

Ans. is ‘a’ i.e., Cinnarizine

  • Vertigo is due to labyrinthine disorder and the impulse utilizes cholinergic muscarinic and H1 histamic receptors (similar to motion sickness).
  • So, the drugs used are antimuscarinic, phenothiazines (phenothiazines have anticholinergic property) and antihistaminics.
  • Cinnarizine (act by inhibiting influx of Ca” into endolymph) and betahistine. (a histamine) analogue improve blood circulation to the inner ear can be used in Meniere’s disease.

Quiz In Between



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