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House Pharmacology > AntiEmetics > Flashcards

AntiEmetics Flashcards

1
Q

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

It is often preceded by ________ and may be _______

A

forceful evacuation

gastric; the mouth

nausea; retching

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2
Q

Emesis

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

A

cancer chemotherapy

opioids, general anaesthetics

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3
Q

Vomiting can be a valuable

T/F

A

T

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4
Q

Medications that often cause nausea and vomiting

Mention5

A

Cancer chemotherapy
Analgesics
—Anti-arrythmics
Antibiotics
Oral contraceptives

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5
Q

Medications that often cause nausea and vomiting

Cancer chemotherapy
e.g.____

Analgesics
—
e.g. _______,_______

Anti-arrythmics
— —e.g.,_______,_______

Antibiotics
e.g.,_________

Oral ________

A

cisplatin

opiates, NSAIDs

digoxin, quinidine

erythromycin

contraceptives

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6
Q

Medications that often cause nausea and vomiting

_________

Anti- ________

Anti- _______
— —
Anti- ________

________
________

A

Metformin

parkinsonians

convulsants

hypertensives

Theophylline
Anesthetic

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7
Q

Medications that often cause nausea and vomiting

Anti-parkinsonians
e.g., ______,_______

Anti-convulsants
— —
e.g.,________ ,_________

A

bromcryptine, L-DOPA

phenytoin, carbamazepine

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8
Q

Neurotransmitter in Emesis

The neurotransmitters that have been implicated in vomiting include:
—
___________,________,_______,_______

A

Acetylcholine, Histamine, 5-HT, and Dopamine

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9
Q

Neurotransmitter in Emesis

____________ found on the vestibular nuclei

_____________ are on the CTZ

_________ also on vomiting centre

A

H1R, AchMR

D2 R and 5-HT R

AchMR and 5-HT R

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10
Q

CTZ is found in the ____________

vomiting centre is located in the ————

A

floor of the 4th ventricle

brain stem

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11
Q

Chemoreceptor Trigger Zone (CTZ) is ______ the BBB

A

Outside

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12
Q

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

T/F

A

T

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13
Q

Emetic drugs

__________ acts locally in the ______
—
Performs its irritant action via ———

A

Ipecacuanha

its constituents

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14
Q

Ipecacuanha (_______ and _______)

A

emetine and cephaeline

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15
Q

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 ———- .

A

vomiting centre & CTZ

gut and CNS

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16
Q

Serotonin 5 HT3 Antagonist

(Low or High?) first pass metabolism

Excreted by _______________

Given ____________ daily – _____ or _____

A

High

liver & kidney

once or twice

orally or intravenously.

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17
Q

Serotonin 5 HT3 Antagonist

No dose reduction in _____ insufficiency but needed in ______ insufficiency

A

renal

hepatic

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18
Q

Drugs Available for Serotonin 5 HT3 Antagonist

________
_______
__________

A

Ondansetron Granisetron Dolasetron

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19
Q

Serotonin 5 HT3 Antagonist

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

Postoperative & postradiation nausea & vomiting

A

nausea & vomiting

30 min

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20
Q

Serotonin 5 HT3 Antagonist

Adverse Effects
_________ safety profile

Headache & ________

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

A

Excellent

constipation

prolongation of QT

dolasetron

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21
Q

Dopamine D2 Antagonist

Antagonise D2 receptors in ______.

A

CTZ

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22
Q

Dopamine D2 Antagonist

Drugs available
___________
________

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

A

Metoclopramide
Domperidone

prokinetic

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23
Q

Dopamine D2 Antagonist

Route of administration

Domperidone – _____

Metoclopramide – ________

A

oral

oral & i.v

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24
Q

Which crosses the BBB

domperidone OR Metoclopramide

A

Metoclopramide crosses BBB but domperidone cannot.

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25
Q

Which is a better antiemetic – Metoclopramide or Domperidone ?

A

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.

26
Q

CTZ

Inside or outside BBB

A

Outside

27
Q

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

A

crosses BBB

extrapyramidal

28
Q

Domperidone is poorly tolerated.

T/F

A

F

well

29
Q

Phenothiazines & Butyrophenones

List 3 under Phenothiazines

A

Prochlorperazine
Promethazine (H1 antagonist) Chlorpromazine

30
Q

Phenothiazines & Butyrophenones

Phenothiazines are _______ with potent antiemetic property due to ____________

A

antipsychotics

D2 antagonism.

31
Q

Phenothiazines & Butyrophenones

Butyrophenone

Eg
___________

A

Droperidol

32
Q

Phenothiazines & Butyrophenones

Butyrophenone

Droperidol used for post operative. _______ and ___________, but cause ____________

A

nausea & vomiting

QT prolongation.

33
Q

H1 Antihistaminics

Most effective drugs for __________

Drugs available

List 5

A

motion sickness

Meclizine
Cyclizine
Dimenhydrinate
Diphenydramine
Promethazine

34
Q

H1 Antihistaminics

Promethazine – Used in _______, used by
NASA for ___________

A

pregnancy

space motion sickness

35
Q

Anticholinergics

Scopolamine (_________) – used as ___________ for _________

A

hyoscine

transdermal patch

motion sickness

36
Q

Cannabinoids

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

A

psychoactive

chemotherapy induced vomiting

37
Q

Cannabinoids

Mention 2

A

Dronabinol

Nabilone

38
Q

Cannabinoids

Nabilone : a synthetic cannabinoids acting on ____________ receptors.

A

both CB1 and CB2

39
Q

Cannabinoids (nabilone): inhibit at ______
—

A

CTZ

40
Q

Cannabinoids (nabilone):

— Orally (poorly or well ?) absorbed with half life of _______.

Metabolites excreted in the ___________________

A

Well; 120min

urine and faeces

41
Q

Cannabinoids (nabilone):

— AE: Drowsiness, dizziness, ______, _____ changes, hallucinations.
— Treats vomiting caused by ________________

A

dry mouth ; mood

cytotoxic anticancer drugs.

42
Q

Anti-emetic

Steroids (___________) used in combination with ________ or _______

A

dexamethasone

ondansetron or chlopromazine.

43
Q

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 ?

A

Vestibular nuclei has only muscarinic and H1 histaminic receptors.

44
Q

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

_______
__________
________
______

A

GIT
CHEMORECEPTOR TRIGGER ZONE VESTIBULAR SYSTEM
CEREBRAL CORTEX

45
Q

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

A

VOMITING CENTRE or AREA POSTREMA

46
Q

CONTROL CENTER of emesis

Located in the _______ at the ______

It is involved in the integration of impulses of emesis

A

Rhomboid fossa

Medulla

47
Q

OUTPUT SITE of emesis

The _____ is the final site of output of Emesis

It receives efferent signals from the Control Center

A

GIT

48
Q

PHENOTHIAZINE

Examples
_________,________,________

M.O.A
_______________________ in the CNS

Adverse Effect
__________ symptoms
_____tension

A

Prochlorperazine
Promethazine
Chlorpromazine

Binds and block D2 receptors

Extrapyramidal; Hypo

49
Q

BUTYROPHENONES
Examples
————-,————-

M.O.A
___________________ in the CNS

Indications
————- nausea
__________ vomiting

A

Droperidol; Haloperidol

Binds and blocks D2 receptors

Post-operative; Post-operative

50
Q

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

A

Meclizine
Cyclizine
Dimenhydrinate
Diphenhydramine
Promethazine

Vestibular system or Vomiting Center

Pregnancy; Motion sickness

51
Q

ANTI-CHOLINERGICS

Examples
————-/________

M.O.A
Binds and block M__ receptors at the _______

Indication
___________(Drug of Choice)

A

Scopolamine/Hyoscine

3; Vestibular nuclei

Motion sickness

52
Q

Motion sickness

Drug of choice ?

Most effective drug?

A

Hyoscine

H1 antagonist

53
Q

CANNABINOIDS

Examples
————,————

M.O.A
Acts directly by __________

Indication
For ______________________ Emesis.

A

Dronabinol
Nabilone

inhibiting the CTZ

Cancer chemotherapy induced

54
Q

CORTICOSTEROIDS

Examples
_________,_______

M.O.A
Enhances ___________________
Used in combination with __________ or ________

Adverse Effect
___________

A

Dexamethasone
Methyl-prednisone

5-HT receptor antagonism

ondansetron or chlorpromazine.

Cushing syndrome

55
Q

SEROTONIN 5HT3 ANTAGONIST

Examples
————,———-,———,———

M.O.A
Binds and blocks 5HT3 receptors; primarily in the ———

A

Ondansetron
Granisetron
Delasetron
Palonosetron

GIT

56
Q

Which anti emetics cause QT prolongation

A

Butyrophenones and Serotonin antagonist

57
Q

DOPAMINE ANTAGONIST (D2 ANTAGONIST)

Examples
__________,_______

M.O.A
Binds and blocks D2 receptors in ______

Indication
—————-

A

Metoclopramide
Domperidone

CTZ

Pregnancy

58
Q

NEUROKININ RECEPTOR ANTAGONIST

Examples
————,————

M.O.A
Binds and block __________ in the _________ in the __________

Indication
For __________________ Nausea and Vomiting

A

Aprepitant
Fosaprepitant

NK1 receptors ; solitary nucleus; brain stem

Chemotherapy Induced

59
Q

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

A

Canabinoids and NK-receptor antagonist

60
Q

Atropine is anti-diarrheal

T/F

A

T

61
Q

Codeine is anti-diarrheal

T/F

A

T

62
Q

Codeine causes constipation

T/F

A

T

House Pharmacology (50 decks)

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