AntiEmetics Flashcards
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
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
Vomiting can be a valuable
T/F
T
Medications that often cause nausea and vomiting
Mention5
Cancer chemotherapy
Analgesics
Anti-arrythmics
Antibiotics
Oral contraceptives
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
Medications that often cause nausea and vomiting
_________
Anti- ________
Anti- _______
Anti- ________
________
________
Metformin
parkinsonians
convulsants
hypertensives
Theophylline
Anesthetic
Medications that often cause nausea and vomiting
Anti-parkinsonians
e.g., ______,_______
Anti-convulsants
e.g.,________ ,_________
bromcryptine, L-DOPA
phenytoin, carbamazepine
Neurotransmitter in Emesis
The neurotransmitters that have been implicated in vomiting include:
___________,________,_______,_______
Acetylcholine, Histamine, 5-HT, and Dopamine
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
CTZ is found in the ____________
vomiting centre is located in the ————
floor of the 4th ventricle
brain stem
Chemoreceptor Trigger Zone (CTZ) is ______ the BBB
Outside
In the event of swallowing a toxic agent, there could be a need to stimulate emesis
T/F
T
Emetic drugs
__________ acts locally in the ______
Performs its irritant action via ———
Ipecacuanha
its constituents
Ipecacuanha (_______ and _______)
emetine and cephaeline
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
Serotonin 5 HT3 Antagonist
(Low or High?) first pass metabolism
Excreted by _______________
Given ____________ daily – _____ or _____
High
liver & kidney
once or twice
orally or intravenously.
Serotonin 5 HT3 Antagonist
No dose reduction in _____ insufficiency but needed in ______ insufficiency
renal
hepatic
Drugs Available for Serotonin 5 HT3 Antagonist
________
_______
__________
Ondansetron Granisetron Dolasetron
Serotonin 5 HT3 Antagonist
Used in Chemotherapy induced _______ and _______ – given at least _________. before chemotherapy.
Postoperative & postradiation nausea & vomiting
nausea & vomiting
30 min
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
Dopamine D2 Antagonist
Antagonise D2 receptors in ______.
CTZ
Dopamine D2 Antagonist
Drugs available
___________
________
Both drugs are also ________ agents due to their 5HT4 agonist activity.
Metoclopramide
Domperidone
prokinetic
Dopamine D2 Antagonist
Route of administration
Domperidone – _____
Metoclopramide – ________
oral
oral & i.v
Which crosses the BBB
domperidone OR Metoclopramide
Metoclopramide crosses BBB but domperidone cannot.
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
T
Codeine is anti-diarrheal
T/F
T
Codeine causes constipation
T/F
T
