AntiEmetics Flashcards by Iseoluwa Ojo

Emesis
The act of vomiting is a _______ of _____ contents through _____.

It is often preceded by ________ and may be _______

forceful evacuation

gastric; the mouth

nausea; retching

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Emesis

Vomiting can be a valuable but it is also an unwanted side effect of _________ as well as _____,__________ e.t.c.

cancer chemotherapy

opioids, general anaesthetics

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Vomiting can be a valuable

T/F

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Medications that often cause nausea and vomiting

Mention5

Cancer chemotherapy
Analgesics
Anti-arrythmics
Antibiotics
Oral contraceptives

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Medications that often cause nausea and vomiting

Cancer chemotherapy
e.g.____

Analgesics

e.g. _______,_______

Anti-arrythmics
e.g.,_______,_______

Antibiotics
e.g.,_________

Oral ________

cisplatin

opiates, NSAIDs

digoxin, quinidine

erythromycin

contraceptives

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Medications that often cause nausea and vomiting

_________

Anti- ________

Anti- _______

Anti- ________

________
________

Metformin

parkinsonians

convulsants

hypertensives

Theophylline
Anesthetic

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Medications that often cause nausea and vomiting

Anti-parkinsonians
e.g., ______,_______

Anti-convulsants

e.g.,________ ,_________

bromcryptine, L-DOPA

phenytoin, carbamazepine

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Neurotransmitter in Emesis

The neurotransmitters that have been implicated in vomiting include:

___________,________,_______,_______

Acetylcholine, Histamine, 5-HT, and Dopamine

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Neurotransmitter in Emesis

____________ found on the vestibular nuclei

_____________ are on the CTZ

_________ also on vomiting centre

H1R, AchMR

D2 R and 5-HT R

AchMR and 5-HT R

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CTZ is found in the ____________

vomiting centre is located in the ————

floor of the 4th ventricle

brain stem

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Chemoreceptor Trigger Zone (CTZ) is ______ the BBB

Outside

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In the event of swallowing a toxic agent, there could be a need to stimulate emesis

T/F

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Emetic drugs

__________ acts locally in the ______

Performs its irritant action via ———

Ipecacuanha

its constituents

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Ipecacuanha (_______ and _______)

emetine and cephaeline

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Serotonin 5 HT3 Antagonist

Potent antiemetics

Even though 5 HT3 receptors are present in _______ and ________ , the antiemetic action is restricted to emesis originating from the _____ and ———- .

vomiting centre & CTZ

gut and CNS

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Serotonin 5 HT3 Antagonist

(Low or High?) first pass metabolism

Excreted by _______________

Given ____________ daily – _____ or _____

High

liver & kidney

once or twice

orally or intravenously.

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Serotonin 5 HT3 Antagonist

No dose reduction in _____ insufficiency but needed in ______ insufficiency

renal

hepatic

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Drugs Available for Serotonin 5 HT3 Antagonist

________
_______
__________

Ondansetron Granisetron Dolasetron

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Serotonin 5 HT3 Antagonist

Used in Chemotherapy induced _______ and _______ – given at least _________. before chemotherapy.

Postoperative & postradiation nausea & vomiting

nausea & vomiting

30 min

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Serotonin 5 HT3 Antagonist

Adverse Effects
_________ safety profile

Headache & ________

All three drugs cause ______ of ______ interval, but more pronounced with ________.

Excellent

constipation

prolongation of QT

dolasetron

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Dopamine D2 Antagonist

Antagonise D2 receptors in ______.

CTZ

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Dopamine D2 Antagonist

Drugs available
___________
________

Both drugs are also ________ agents due to their 5HT4 agonist activity.

Metoclopramide
Domperidone

prokinetic

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Dopamine D2 Antagonist

Route of administration

Domperidone – _____

Metoclopramide – ________

oral

oral & i.v

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Which crosses the BBB

domperidone OR Metoclopramide

Metoclopramide crosses BBB but domperidone cannot.

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Which is a better antiemetic – Metoclopramide or Domperidone ?

As CTZ is outside BBB both have antiemetic effects. But as metoclopramide crosses BBB it has adverse effects like extrapyramidal side effects.. Domperidone is well tolerated.

CTZ Inside or outside BBB

Outside

metoclopramide _______ ____ it has adverse effects like ________ side effects..

crosses BBB extrapyramidal

Domperidone is poorly tolerated. T/F

F well

Phenothiazines & Butyrophenones List 3 under Phenothiazines

Prochlorperazine Promethazine (H1 antagonist) Chlorpromazine

Phenothiazines & Butyrophenones Phenothiazines are _______ with potent antiemetic property due to ____________

antipsychotics D2 antagonism.

Phenothiazines & Butyrophenones Butyrophenone Eg ___________

Droperidol

Phenothiazines & Butyrophenones Butyrophenone Droperidol used for post operative. _______ and ___________, but cause ____________

nausea & vomiting QT prolongation.

H1 Antihistaminics Most effective drugs for __________ Drugs available List 5

motion sickness Meclizine Cyclizine Dimenhydrinate Diphenydramine Promethazine

H1 Antihistaminics Promethazine – Used in _______, used by NASA for ___________

pregnancy space motion sickness

Anticholinergics Scopolamine (_________) – used as ___________ for _________

hyoscine transdermal patch motion sickness

Cannabinoids Dronabinol – (it’s a ________ substance) used as adjuvant in _____________ inducing _________.

psychoactive chemotherapy induced vomiting

Cannabinoids Mention 2

Dronabinol Nabilone

Cannabinoids Nabilone : a synthetic cannabinoids acting on ____________ receptors.

both CB1 and CB2

Cannabinoids (nabilone): inhibit at ______

CTZ

Cannabinoids (nabilone): Orally (poorly or well ?) absorbed with half life of _______. Metabolites excreted in the ___________________

Well; 120min urine and faeces

Cannabinoids (nabilone): AE: Drowsiness, dizziness, ______, _____ changes, hallucinations. Treats vomiting caused by ________________

dry mouth ; mood cytotoxic anticancer drugs.

Anti-emetic Steroids (___________) used in combination with ________ or _______

dexamethasone ondansetron or chlopromazine.

A physician prescribed Tab.Ondansetron for prophylaxis of motion sickness. Even though ondansetron is a potent antiemetic it didn’t produce any effect in this patient. Can you explain why ?

Vestibular nuclei has only muscarinic and H1 histaminic receptors.

INPUT SITE of emesis Are sites in the body that receive stimuli Then transmit afferent signals to the Control center They include _______ __________ ________ ______

GIT CHEMORECEPTOR TRIGGER ZONE VESTIBULAR SYSTEM CEREBRAL CORTEX

CONTROL CENTER of emesis The control center for vomiting is called The ____________ or ________

VOMITING CENTRE or AREA POSTREMA

CONTROL CENTER of emesis Located in the _______ at the ______ It is involved in the integration of impulses of emesis

Rhomboid fossa Medulla

OUTPUT SITE of emesis The _____ is the final site of output of Emesis It receives efferent signals from the Control Center

GIT

PHENOTHIAZINE Examples _________,________,________ M.O.A _______________________ in the CNS Adverse Effect __________ symptoms _____tension

Prochlorperazine Promethazine Chlorpromazine Binds and block D2 receptors Extrapyramidal; Hypo

BUTYROPHENONES Examples ————-,————- M.O.A ___________________ in the CNS Indications ————- nausea __________ vomiting

Droperidol; Haloperidol Binds and blocks D2 receptors Post-operative; Post-operative

H1 ANTI-HISTAMINES Examples _________,______,______,_______,______ M.O.A Binds and blocks H1 receptors in either the ________ or ________ Indications ________ __________(most effective) Adverse Effect Drowsiness Confusion Dry mouth

Meclizine Cyclizine Dimenhydrinate Diphenhydramine Promethazine Vestibular system or Vomiting Center Pregnancy; Motion sickness

ANTI-CHOLINERGICS Examples ————-/________ M.O.A Binds and block M__ receptors at the _______ Indication ___________(Drug of Choice)

Scopolamine/Hyoscine 3; Vestibular nuclei Motion sickness

Motion sickness Drug of choice ? Most effective drug?

Hyoscine H1 antagonist

CANNABINOIDS Examples ————,———— M.O.A Acts directly by __________ Indication For ______________________ Emesis.

Dronabinol Nabilone inhibiting the CTZ Cancer chemotherapy induced

CORTICOSTEROIDS Examples _________,_______ M.O.A Enhances ___________________ Used in combination with __________ or ________ Adverse Effect ___________

Dexamethasone Methyl-prednisone 5-HT receptor antagonism ondansetron or chlorpromazine. Cushing syndrome

SEROTONIN 5HT3 ANTAGONIST Examples ————,———-,———,——— M.O.A Binds and blocks 5HT3 receptors; primarily in the ———

Ondansetron Granisetron Delasetron Palonosetron GIT

Which anti emetics cause QT prolongation

Butyrophenones and Serotonin antagonist

DOPAMINE ANTAGONIST (D2 ANTAGONIST) Examples __________,_______ M.O.A Binds and blocks D2 receptors in ______ Indication —————-

Metoclopramide Domperidone CTZ Pregnancy

NEUROKININ RECEPTOR ANTAGONIST Examples ————,———— M.O.A Binds and block __________ in the _________ in the __________ Indication For __________________ Nausea and Vomiting

Aprepitant Fosaprepitant NK1 receptors ; solitary nucleus; brain stem Chemotherapy Induced

Which anti-emetics is used for Chemotherapy Induced nausea and vomiting?

Canabinoids and NK-receptor antagonist

Atropine is anti-diarrheal T/F

Codeine is anti-diarrheal T/F

Codeine causes constipation T/F