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Nausea and vomiting Flashcards

1
Q

Chemical transmitters involved in vomiting

A

Dopamine: D2 receptors
ACh: MR in vomiting center
Histamine: H1 receptors
Serotonin: 5HT3 receptors

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2
Q

Indications of H1 R antagonists

A

N&V induced by any stimuli.
Vomiting produced by substance acting directly on CTZ
Motion sickness, substances acting on stomach

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3
Q

H1 R antagonist drugs are

A

Cyclizine
Cinnarizine
Buclizine
Doxylamine
Promethazine

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4
Q

Sedation in H1 R antagonist

A

Promethazine and Doxylamine
Cyclizine
Cinnarizine

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5
Q

MOA of Cyclizine

A

inhibits H1 R in VC
also has antimuscarinic activity

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6
Q

I of Cyclizine

A

for all types of vomiting including motion sickness

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7
Q

DOA of cyclizine

A

4-6 hrs

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8
Q

AE of Cyclizine

A

Drowsiness
Xerostomia

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9
Q

CI of Cyclizine

A

Closed angle Glaucoma
Urinary retention
Prostatic hypertrophy
Chronic pulmonary disease
acute asthma

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10
Q

DI of Cyclizine

A

CNS depressants
Anti-cholinergics: incr. their effects

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11
Q

MOA of Cinnarizine

A

inhibits H1 R in VC and vestibular system
also has antimuscarinic activity

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12
Q

I of Cinnarizine

A

motion sickness
Vestibular disorders (meniere’s)

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13
Q

Half-life of Cinnarizine

A

3-6 hrs

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14
Q

AE of Cinnarizine

A

Extrapyramidal symptoms
Depressive feeling (with prolonged therapy)
Hypotension (high doses)

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15
Q

CI of Cinnarizine

A

Hypersenstivity to drug

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16
Q

DI of Cinnarizine

A

CNS depressants
Anti cholinergics
Anti histamines
MAOi
TC antidepressants

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17
Q

MOA of Doxylamine

A

competes for H1 R sites on target cells
has anti-cholinergic effects= depresses labyrinthine function, blocks CTZ, diminishes vestibular stimulation

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18
Q

Doxyalmine can be used

A

alone or with Pyridoxine and dicyclomine

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19
Q

Half-life of doxylamine

A

10-12 hrs

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20
Q

AE of Doxylamine

A

Tachycardia
urinary retention
constipation
drowsiness
blurred vision

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21
Q

CI of doxylamine

A

children <12 years

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22
Q

DI of doxylamine

A

CNS depressants
Anti-cholinergics= incr. their effects

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23
Q

MOA of Buclizine

A

inhibits H1 R in VC and vestibular system
also has anti-cholinergic properties

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24
Q

I of Buclizine

A

Motion sicness
radio/chemo induced NV

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25
AE of Buclizine
sedation dizziness headache anxiety hypotension dry mouth-xerostomia tight chest urinary retention
26
CI of Buclizine
Asthma Pulmonary disease bladder neck obstruction Closed angle Glaucoma
27
DI of Buclizine
CNS depressants
28
MOA of Promethazine HCL
inhibits D2 R, MR and H1 R crosses BBB
29
I of Promethazine HCL
all types of vomiting including: severe morning sickness (only if essential) Prevention of motion sickness
30
HAlf-life of Promethazine HCL
10-14hrs
31
AE of Promethazine HCL
strong sedative effect dizziness fatigue incoordination Extrapyramidal symptoms
32
CI of Promethazine HCL
children <2years
33
DI of Promethzine HCL
CNS depressants ANti-cholinergic agents
34
MR antagonists are
Hyoscine
35
MOA of hyoscine
inhibits MR blocks impulses from CTZ to vomiting center (acts direct in VC)
36
I of Hyoscine
motion sickness nausea as a result of labyrinthine disturbances
37
AE of Hyoscine
Drowsiness Xerostomia Dry skin blurred vision Urinary retention (high doses) Constipation dementia
38
CI of Hyoscine
Glaucome GI obstruction Prophyra
39
DI of Hyoscine
TCA Antihistamines Antipsychotics
40
Indictations of D2 R antagonists
NV caused by nausea/labyrinthine disturbances Chemo-induced NV Post-op NV Radiation-induced NV
41
D2 R antagonist drugs are
Domperidone (CTZ: peripheral actions) Droperidol (butyrophenone, inhibits GIT) Metocloopramide (inhibits CTZ and GIT) Prochlorperazine (phenothiazine, inhibits CTZ
42
MOA of Domperidone
Inhibits D2 R in CTZ, to prevent circulation action of emetic drugs
43
I of Domperidone
Post-op NV NV of central/peripheral origin
44
Half-life of Domperidone
7-8hrs
45
AE of Domperidone
Extrapyramidal symptoms (decr) Drowsiness Headache Reversible Galactorrhoea
46
CI of Domperidone
Hepatic impairment GI obstruction/Perforation CVS disease
47
DI of Domperidone
CYP34A inhibitors K-depleting agents Macrolides Antacids Anticholinergics Protease inhibitors
48
MOA pf Droperidol
inhibits D2 R at CTZ
49
I of Droperidol
Prevention of Post-op NV where other treatments are ineffective/inappropriate
50
Half-life of Droperidol
2-3hrs
51
AE of Droperidol
EXtrapyramidal symptoms Drowsiness Hypotension Blurred vision anxiety
52
CI of Droperidol
Electrolyte imbalance Parkinson's severe depression pregnancy
53
DI of Droperidol
alcohol K-depleting diuretics Glucocorticoids CNS depressants Opioids Bromocriptine Levodopa CYP34A/1A2 inhibitors: incr. risk of QT prolongation
54
MOA of Metoclopramide
Inhibtis D2 R in CTZ and VC Has stimulant effect on GIT (facilitates emptying of stomach, relaxes pylorus and incr. GI motility)
55
I of Metoclopramide
V caused by: uraemia radiation GIT disorders Drug-related NV(cytotoxic drugs) Post-op NV
56
CI of Metoclopramide
Epilepsy Pheochromocytma Mechanical bowel obstruction Intestine perforation
57
Half-life of Metoclopramide
4-6 hrs
58
AE of Metoclopramide
Extrapyramidal symptoms Light sedation Constipaion Incr. prolactin release=galactorrhoea
59
DI of Metoclopramide
Antipsychotic agents CNS depressants Digoxin Paracetamol Ampicillin Tetracyclines
60
MOA of Prochlorperazine
inhibits D2 R in CTZ inhibits Cholinergic and a adrenergic R =sedation, muscle relaxation, hypotension
61
I of Prochlorperazine
V due to: uraemia Radiation Oncotherapy Viral gastroenteritis severe morning sickness(if essential only)
62
DOA of Prochlorperazine
3-4hrs
63
AE of Prochlorperazine
Extrapyramidal symptoms Constipation dry mouth Hypotension Reflex tachycardia blurred vision drowsiness
64
DI of Prochlorperazine
CNS depressants Anti-Parkinsons's agents Metoclopramide (Incr. extrapyramidal SEs)
65
I of 5HT3 R anatgonists
V caused by: Cytotoxic anti-cancer drugs Post-op NV Radiation-induced NV (oncotherapy)
66
AE of 5HT3 R antagonists
Headache dizziness muscle pain GIT upsets Constipation
67
Which are the 5HT3 R antagonists
Granisetron Ondansetron Palonosetron
68
MOA of Granisetron
inhibits 5HT3 in vagal n. terminal and centrally in CTZ (selective)=antiemesis
69
I of Granisetron
Post-cytotoxic chemo/radi NV Post-op NV
70
CI of Granisetron
Hypersenstivity to any of ingredients
71
Half-life of Granisetron
9 hrs
72
DI of Granisetron
QT prolonging agents Serotonergic agents Cardiotoxic drugs Phenobarbital
73
MOA of Ondansetron
inhibits 5HT3 in vagal n. terminal and centrally in CTZ (selective)=antiemesis
74
I of Ondansetron
Post-cytotoxic chemo/radio NV Post-op NV
75
AE of Ondansetron
headache flushing constipation dry mouth sedation Hypersensitivity rxns Seizures CVS effects: arrythmia, bradycardia, hypotension Fatigue
76
CI of Ondansetron
Congenital long QT syndrome Concomitant use of Apomorphine
77
DI of Ondansetron
Tramadol Rifampicin Carbamazepine Phenytoin
78
MOA of Palonosetron
selectively inhibits 5HT3 R both in peripheral and CNS with primary effects in GIT
79
I of Palonosetron
Post-cytotoxic chemo/radio NV Post-op NV
80
Half-life of Palonosetron
40hrs
81
AE of Palonosetron
Anxiety dizziness headache weakness constipation pruritus Hyperkalemia
82
CI of Palonosetron
Hypersensitivity to drug Coadministration with ampomorphine= prolonged hypotension and loss of consiousness
83
DI of Palonosetron
Serotonergic agents SSRIs SSNRis anti-arrythmic agents QT-prolonging agents agents resulting in electrolyte abnormalities
84
Which are the Substance P (NK1) antagonists
Aprepitant/Fosaprepitant

Pharmacology (50 decks)

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