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Pharmacology > Treatment of Nausea and Vomitting > Flashcards

Treatment of Nausea and Vomitting Flashcards

1
Q

Vomiting?

A

A physiological response that comes as a result of stimulation of the
chemoreceptor trigger zone (CTZ) and/or the vomiting centre in the
CNS.

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2
Q

Aetiology of N & V?

A
  1. GI mechanisms
  2. Cardiovascular disease
  3. Neurologic processes
  4. Metabolic Disorders
  5. Psychiatrist causes
  6. Therapy induced causes
  7. Drug withdrawl
  8. Other causes: pregnancy, noxious, poperative procedure
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3
Q

Chemical transmitters involved in N & V?

A

Dopamine-D2

Acetylcholine

Histamine

Serotonin

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4
Q

Antiemtics defintion?

A

Antiemetic drugs are medicines that ease nausea or vomiting

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5
Q

Antiemtics?

A

A. H 1Receptor Antagonists
B. Muscarinic Receptor Antagonists
C. D 2Receptor Antagonists
D. 5HT 3Receptor Antagonists
E. Substance P (NK1) Antagonists
F. Other

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6
Q

H 1Receptor Antagonists I?

A

*NV induced by any stimuli
*Vomiting produced by substances acting directly on
the CTZ
*Motion sickness, substances acting on the stomach

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7
Q

H 1Receptor Antagonists drugs?

A

Cyclizine
Cinnearizine
Buclizine
Doxylamine
Promethazine

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8
Q

H 1Receptor Antagonists MOA?

A

Mostly 1st generation anƟhistamines → enter
the CNS

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9
Q

Cyclizine MOA?

A

Inhibition H 1receptors in the VC (also has antimuscarinic action)

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10
Q

Cyclizine I?

A

Used for all types of vomiting including motion sickness

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11
Q

Cyclizine Kinetics?

A, D, M & E.

A

A=well orally
D=does not readily cross
BBB
M=extensively in liver, E=inactive
metabolites in urine, DOA=4‐6 hrs

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12
Q

Cyclizine AE?

A

Drowziness, xerostomia

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13
Q

Cyclizine CI?

A

closed‐angle glaucoma, urinary retention, prostatic hypertrophy, chronic pulmonary disease, acute asthma

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14
Q

Cyclizine DI?

A

CNS depressants,
anƟcholinergics➡️ ⬆️anƟcholinergic effects

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15
Q

Doxylamine MOA?

A

competes for H 1‐receptors sites on target
cells; has anƟcholinergic effects ➡️ depresses
labyrinthine function, blocks CTZ; diminishes
vestibular stimulation

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16
Q

Doxylamine I?

A

Used for all types of vomiting including motion sickness

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17
Q

Doxylamine Kinetics?

A

A=well absorbed orall, D=crosses BBB,
M=hepatic
E=urine
T 1/2=10‐12 hrs

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18
Q

Doxylamine AE?

A

tachycardia
urinary retention
constipation
drowsiness
blurred vision

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19
Q

Doxylamine CI?

A

children <12 yrs

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20
Q

Doxylamine DI?

A

CNS depressants,
anƟcholinergics➡️ ⬆️anƟcholinergic effects

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21
Q

Cinnarizine MOA?

A

Inhibition (‐) H 1receptors in the VC & vestibular
system (also has antimuscarinic action; CCB)

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22
Q

Cinnarizine I?

A

motion sickness, vestibular disorders
(Meniere’s)

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23
Q

Cinnarizine Kinetics?

A

A=fairly rapid
D=91% protein bound
M=extensively in liver
E=excreted unchanged in
faeces, metabolites in urine, t 1/23‐6 hrs ?

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24
Q

Cinnarizine AE?

A

extrapyramidal symptoms + depressive
feeling (with prolonged therapy), hypotension
(at high doses)

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25
Cinnarizine CI?
hypersensitivity to the drug
26
Cinnarizine DI?
CNS depressants, anticholinergics, antihistamines, MAOIs, tricyclic antidepressants
27
Buclizine (long‐acting) MOA?
(‐) H 1receptors in the VC & vestibular system (also has anticholinergic properties)
28
Buclizine (long‐acting) I?
motion sickness, radio/chemo‐induced NV
29
Buclizine (long‐acting) A/E?
sedation dizziness headache anxiety hypotension tight chest dry mouth urinary retention
30
Buclizine (long‐acting) CI?
asthma, pulmonary disease, bladder neck obstruction, closed‐angle glaucoma
31
Buclizine (long‐acting) DI?
CNS depressants
32
Promethazine HCL MOA?
(‐) D 2, muscarinic and H 1receptors, crosses BBB
33
Promethazine HCL I?
all types of vomiting including severe morning sickness in pregnancy (only if absolutely essential), prevention of motion sickness
34
Promethazine Kinetics?
A=well orally D=crosses BBB, M=extensively in liver, E=inactive conjugates in urine, T 1/2= 10‐14hrs
35
Promethazine Kinetics A/E?
strong sedative effect dizziness Fatigue, incoordination extrapyramidal symptoms
36
Promethazine CI?
children <2yrs
37
Promethazine DI?
CNS depressants, anticholinergic agents
38
Hyoscine MOA?
(‐) M receptors, blocks impulses from the CTZ to the vomiting centre (act directly on the VC)
39
Hyoscine I?
motion sickness, nausea as a result of labyrinth disturbances
40
Hyoscine Kinetics? A, D, M & E?
A=poor orally D=unclear M=in liver, E=in urine
41
Hyoscine AE?
drowsiness dry mouth dry skin blurred vision, urine retention (at high doses) constipation dementia
42
Hyoscine CI?
glaucoma GI obstruction porphyria
43
Hyoscine DI?
tricyclic antidepressants, antihistamines, antipsychotics
44
D2 Receptor Antagonists drugs?
Domperidone [(CTZ), peripheral actions] Droperidol(butyrophenone, (‐) GIT) Metoclopramide [(‐) CTZ & GIT] Prochlorperazine (phenothiazine, (‐) CTZ)
44
D2 Receptor Antagonists drugs?
Domperidone [(CTZ), peripheral actions] Droperidol(butyrophenone, (‐) GIT) Metoclopramide [(‐) CTZ & GIT] Prochlorperazine (phenothiazine, (‐) CTZ)
45
D2 Receptor Antagonists I?
NV caused by motion sickness or other labyrinth disturbances *Chemotherapy induced NV (CINV) *Post Operative NV (PONV) *Radiation Induced NV (RINV)
46
D2 Receptor Antagonists A/E?
sedation dizziness dyskinesia dystonias
47
Domperidone MOA?
(‐) D 2receptors in the CTZ, to prevent the action of circulation emetic agents
48
Domperidone I?
post‐operative NV, NV of central/peripheral origin
49
Domperidone Kinetics? A, D, M & E?
A=well absorbed orally, D=limited entry into the CNS (poor lipid‐solubility) M=in liver by CYP3A4 enzymes, E=65% in faeces and 35% in urine (as metabolites), T 1/2=7‐8 hrs
50
Domperidone A/E?
Extrapyramidal symptoms (⬇️), drowsiness, headache, reversible galactorrhoea
51
Domperidone CI?
hepatic impairement, GI obstruction or perforation, GI haemorrhage, cardiovascular disease
52
Domperidone DI?
CYP3A4 inhibitors potassium depleting agents, macrolides antacids anticholinergics protease inhibitors
53
Droperidole ?
(‐) D 2receptors at the CTZ
54
Droperidole I?
prevention of PONV where other treatments are ineffective or inappropriate
55
Droperidole Kinetics? D & M
D=rapid crosses BBB M=in liver, T 1/2=2‐3 hrs
56
Droperidole A/E?
Extrapyramidal symptoms, drowsiness, hypotension blurred vision, anxiety
57
Droperidole CI?
electrolyte imbalance, Parkinson’s, severe depression, pregnancy
58
Droperidole DI?
alcohol, K‐depleting diuretics, glucocorticoids, CNS depressants, opioids, Bromocriptine, levodopa, CYP3A4/1A2 inhibitors➡️⬆️ risk of QT prolongaƟon
59
Metoclopramide MOA?
(‐) D 2receptors in the CTZ and VC, also has a stimulant effect on the GIT (facilitates emptying of the stomach, relaxes the pylorus and increases GI motility)
60
Metoclopramide I?
vomiting caused by uraemia, radiation GIT disorders drug related NV (cytotoxic drugs) PONV
61
Metoclopramide CI?
epilepsy phaeochromocytoma, mechanical bowel obstruction intestine perforation
62
Metoclopramide Kinetics? A, D & M.
A=rapid oral absorption; bioavailability 30‐100% due to first‐pass metabolism D=widely distributed and readily crosses BBB M=in the liver, E=85% unchanged in urine, T 1/2=4‐6 hrs
63
Metoclopramide A/E?
extrapyramidal symptoms, light sedation, consƟpaƟon ⬆️ prolacƟn release➡️ galactorrhoea
64
MetoIclopramide D
antipsychotic agents, CNS depressants, digoxin, paracetamol, ampicillin, tetracyclines
65
Prochlorperazine MOA?
(‐) D 2receptors in the CTZ, also (‐) cholinergic and ∝‐adrenergic receptors➡️sedation, muscle relaxation, hypotension.
66
Prochlorperazine I?
vomiting due to uraemia, radiation, oncotherapy viral gastroenteritis severe morning sickness (if absolutely essential)
67
Prochlorperazine CI?
CNS depression coma bone‐marrow suppression
68
Prochlorperazine kinetics? A ,D, M & E?
A=well absorbed orally D=well distributed including CNS M=extensively metabolised in liver E=excreted in urine and bile, DOA=3‐4 hrs
69
Prochlorperazine A/E?
extrapyramidal constipation, dry mouth, drowsiness, blurred vision, hypotension, reflex tachycardia
70
Prochlorperazine DI?
CNS depressants anti‐Parkinson’s agents, metoclopramide(↑extrapyramidal SE)
71
5HT 3Receptor Antagonists Drugs?
Granisetron Ondansetron Palonosetron
72
5HT 3Receptor Antagonists I?
Vomiting caused by cytotoxic anti‐cancer drugs, post‐operative NV radiation‐induced NV (oncotherapy)
73
5HT 3Receptor Antagonists A/E?
headache Dizziness muscle pains GIT upsets constipation
74
Granisetron MOA?
(‐) 5HT 3in vagal nerve terminals and centrally in CTZ (selecƟve) → anƟemesis
75
Granisetron I?
Post‐cytotoxic chemo‐/radiotherapy NV, PONV
76
Granisetron CI?
hypersensitivity to any of the ingredients
77
Granisetron Kinetics?
A=rapid and complete orally, bioavailability 60% due to first‐pass effect D=extensively; 65% plasma protein binding M=in liver E=predominantly by hepatic metabolism, unchanged in urine, some in faeces, T 1/2= 9 hrs
78
Granisetron DI?
QT prolonging agents, serotonergic agents, cardiotoxic drugs, phenobarbital
79
Granisetron AE?
headache dizziness muscle pains GIT upsets constipation
80
Ondansetron MOA?
(‐) 5HT 3in vagal nerve terminals and centrally in CTZ (selecƟve) → anƟemesis
81
Ondansetron Kinetics? A, D, M & E.
A=well absorbed orally; bioavailability slightly enhanced by food D=extensively distributed; slowly crosses BBB M&E=extensively metabolised and excreted in the urine and faeces
82
Ondansetron I?
Post‐cytotoxic chemo‐/radiotherapy NV, PONV
83
Ondansetron AE?
headache flushing Constipation, dry mouth sedatio hypersensitivity reactions, seizures CVS effects (arrhythmia, bradycardia, hypotension), fatique
84
Ondansetron CI?
congenital long QT syndrome, concomitant use of apomorphine
85
Ondansetron DI?
tramadol, rifampicin, carbamazepine, phenytoin
86
Palonosetron MOA?
selectively (‐) 5HT 3receptors both peripheral and CNS with primary effects in GIT
87
Palonosetron Kinetics? A, D, M & E
A=low oral bioavailability D=widely distributed (62% protein bound) M=in liver (CYP2D6, CYP3A, CYP1A2) E=urine (80‐93%), faeces (5‐8%), T 1/2=40 hrs
88
Palonosetron I?
Post‐cytotoxic chemo‐/radiotherapy NV, PONV
89
Palonosetron A/E?
AE: anxiety, dizziness, headache, weakness, consƟpaƟon, pruritus, hyperkalaemia, ↑LFTs
90
Palonosetron CI?
CI: hypersensitivity to drug, coadministration with apomorphine ➡️profound hypotension and loss of consciousness
91
Palonosetron DI?
DI: serotonergic agents, SSRIs, SNRIs, anti‐ arrythmic agents, QT‐prolonging agents, agents resulting in electrolyte abnormalities
92
Aprepitant/fosaprepitant MOA?
selecƟve ⬆️‐affinity (‐) of human substance P/neurokinin 1 (NK1) receptors; little or no affinity for 5HT 3, D 2, and corticosteroid receptors
93
Aprepitant/fosaprepitant I?
adjunct to other antiemetics for prevention of acute or delayed CINV, PONV
94
Aprepitant/fosaprepitant CI?
hypersensitivity concomitant Pimozideor Cisapride use
95
Aprepitant/fosaprepitant Kinetics? A, D, M & E.
A=well absorbed orally bioavailability 60‐65%, D=crosses BBB; 95% protein bound M=hepatic CYP3A4 (major); CYP1A2, CYP2C19 (minor)Fosaprepitant (IV) rapidly converted into Aprepitant in vivo E=(IV admin): 57% urine; 45% faeces
96
Aprepitant/fosaprepitant DI?
CYP3A4 substrates, ketoconazole, rifampicin, corticosteroids, benzodiazepines, warfarin, oral contraceptives
97
N&V drugs to treat pregnancy?
*Sucrose/Phosphoric acid *Dicyclomine/Doxylamine succinate/Pyridoxine

Pharmacology (44 decks)

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