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1)Anticholinergics – hyoscine, dicyclomine
2)H1 antihistaminics – promethazine
diphenhydramine
cyclizine
cinnarizine etc
3)D2 receptors
antagonists – droperidol
metoclopramide
chlorpromazine
4)Prokinetic drugs - metoclopramide
domperidone
cisapride
mosapride
5)5HT 3 receptors
antagonists – ondensetron
granisetron
dolasetron
palonosetron
6)Adjuvants - dexamethasone
benzodizepines
Anticholinergics
- Inhibits muscurinic receptors in vestibular
apparatus
-Blocks the conduction of impulses from
vestibular apparatus to vomitting centre
-More effective against motion sicknes
- Side effects : dry mouth ,
blurred vision
constipation
urinary retention
Hyoscine : also known as scopolamine
most effective for motion sickness
transdermal patch which works for
3 days can be useful for prevention
of postdischarge nausea and
vomiting in an ambulatory patient
Atropine : not a primary antiemetic
less incidence of post operative
nausea and vomiting when used with
neostigmine to reverse neuromuscular
blockade than glycopyrrolate
probably because of its central action
-Effective in motion sickness
-Highly sedative
-May delay the recovery when given
before the end of anaesthesia
-More useful in treating allergic rhinitis
And chronic urticaria
e.g. promethazine, diphenhydramine
cinnarazine , cyclizine
-D2 Receptors are located in CTZ and in the gut wall
-Morphine induces vomiting through these receptors
-Antagonists more useful for opioid induced vomiting
-Less effective in motion sickness as vestibular
pathway does not involve dopaminergic link
METOCLOPRAMIDE :
- Antidopaminergic and prokinetic actionc
-prokinetic action more helpful during
emergency anaesthesia for patient with
inadequate starvation
-Dose more than 10mg is avoided – can cause
dystonia
-Dystonia can be prevented by adminstration
of benzodizepine during anaesthesia
Droperidol :
- Highly sedative
- short half life of 3 hrs
- supplimentation with morphine loaded
PCA (patient controlled analgesia) pump
highly effective in preventing opioid
induced vomitting
- anticonvulsive property
SIDE EFFECTS :
-Extra pyrimidal – dystonia,
restlessness,
dyskinesia etc.
-Galectorrhorea
- Dysphorea
- QT prolongation ( droperidol)
-Antagonism of D2 receptors in the gut wall
-Enhancing Ach release from myentric motor
neurons
-Increases gastric persistalsis and LES tone
-This action is helpful in patient who is full
stomach and to be induced in emergency
-Enhances gastric emptying in diabetic
patients with autonomic neuropathy
METOCLOPROMIDE :
-central as well as GI action
DOMPERIDONE :
- blocks D2 receptors in
upper GI
- no central action
- less extrapyrimidal side effects
CISAPRIDE :
- Prokinetic action mainly through
Ach release from myentric
neurons
- no extrapyrimidal side effects
- prolong QT syndrome
-5HT3 receptors in the gut are linked with CTZ
via afferent vagus
-cytotoxic drugs , radiation release serotonin
from enterocromaffin cells which acts on 5HT3
receptors
-triggers CTZ via vagus causing emesis
-5HT3 antagonists most effective against
chemotherapy induced vomiting
-Also effective against PONV
-Advantages : no extrapyrimidal or sedative side
effects like previous antiemetics
ONDENSETRON:
-1ST drug introduced in this group
-Dose 0.1 mg/kg
-Plasma half life of 4hrs
-metabolism by cyto P450 enzyme
-genetic polymorphism of this enzyme leads to
decreased efficacy due to ultrarapid metabolism
-Effective when given at the end of the surgery
-- effective in treatment of pruritus caused by
neuraxial opioid adminstration
GRANISETRON :
-Half life twice as that of ondensetron
-Requires less frequent dosing
-Dose 20 mcg/kg
OTHER 5HT3 antagonists :
dolasetron
palanosetron ( longest acting)
These drugs enhances antiemetic property of
Primary drugs
DEXAMETHASONE:
-Supposedly has action on nucleus tractus solitarius
-Onset of action is slow , better to be given at the
begining of surgery during general anaesthesia
- Dose : 4mg is effective
BENZODIZEPINES:
-They help by relieving anxiety, anticipatory
vomiting
-produce amnesia for unpleasant procedure
-also supress dystonic side effects of
metoclopramide
PROPOFOL:
Antiemet
-ic dose : 10-15 mg
Antiemetics in anaesthesia

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Antiemetics in anaesthesia

  • 1. 1)Anticholinergics – hyoscine, dicyclomine 2)H1 antihistaminics – promethazine diphenhydramine cyclizine cinnarizine etc 3)D2 receptors antagonists – droperidol metoclopramide chlorpromazine 4)Prokinetic drugs - metoclopramide domperidone cisapride mosapride
  • 2. 5)5HT 3 receptors antagonists – ondensetron granisetron dolasetron palonosetron 6)Adjuvants - dexamethasone benzodizepines
  • 3. Anticholinergics - Inhibits muscurinic receptors in vestibular apparatus -Blocks the conduction of impulses from vestibular apparatus to vomitting centre -More effective against motion sicknes - Side effects : dry mouth , blurred vision constipation urinary retention
  • 4. Hyoscine : also known as scopolamine most effective for motion sickness transdermal patch which works for 3 days can be useful for prevention of postdischarge nausea and vomiting in an ambulatory patient Atropine : not a primary antiemetic less incidence of post operative nausea and vomiting when used with neostigmine to reverse neuromuscular blockade than glycopyrrolate probably because of its central action
  • 5. -Effective in motion sickness -Highly sedative -May delay the recovery when given before the end of anaesthesia -More useful in treating allergic rhinitis And chronic urticaria e.g. promethazine, diphenhydramine cinnarazine , cyclizine
  • 6. -D2 Receptors are located in CTZ and in the gut wall -Morphine induces vomiting through these receptors -Antagonists more useful for opioid induced vomiting -Less effective in motion sickness as vestibular pathway does not involve dopaminergic link
  • 7. METOCLOPRAMIDE : - Antidopaminergic and prokinetic actionc -prokinetic action more helpful during emergency anaesthesia for patient with inadequate starvation -Dose more than 10mg is avoided – can cause dystonia -Dystonia can be prevented by adminstration of benzodizepine during anaesthesia
  • 8. Droperidol : - Highly sedative - short half life of 3 hrs - supplimentation with morphine loaded PCA (patient controlled analgesia) pump highly effective in preventing opioid induced vomitting - anticonvulsive property
  • 9. SIDE EFFECTS : -Extra pyrimidal – dystonia, restlessness, dyskinesia etc. -Galectorrhorea - Dysphorea - QT prolongation ( droperidol)
  • 10. -Antagonism of D2 receptors in the gut wall -Enhancing Ach release from myentric motor neurons -Increases gastric persistalsis and LES tone -This action is helpful in patient who is full stomach and to be induced in emergency -Enhances gastric emptying in diabetic patients with autonomic neuropathy
  • 11. METOCLOPROMIDE : -central as well as GI action DOMPERIDONE : - blocks D2 receptors in upper GI - no central action - less extrapyrimidal side effects CISAPRIDE : - Prokinetic action mainly through Ach release from myentric neurons - no extrapyrimidal side effects - prolong QT syndrome
  • 12. -5HT3 receptors in the gut are linked with CTZ via afferent vagus -cytotoxic drugs , radiation release serotonin from enterocromaffin cells which acts on 5HT3 receptors -triggers CTZ via vagus causing emesis -5HT3 antagonists most effective against chemotherapy induced vomiting -Also effective against PONV -Advantages : no extrapyrimidal or sedative side effects like previous antiemetics
  • 13. ONDENSETRON: -1ST drug introduced in this group -Dose 0.1 mg/kg -Plasma half life of 4hrs -metabolism by cyto P450 enzyme -genetic polymorphism of this enzyme leads to decreased efficacy due to ultrarapid metabolism -Effective when given at the end of the surgery -- effective in treatment of pruritus caused by neuraxial opioid adminstration
  • 14. GRANISETRON : -Half life twice as that of ondensetron -Requires less frequent dosing -Dose 20 mcg/kg OTHER 5HT3 antagonists : dolasetron palanosetron ( longest acting)
  • 15. These drugs enhances antiemetic property of Primary drugs DEXAMETHASONE: -Supposedly has action on nucleus tractus solitarius -Onset of action is slow , better to be given at the begining of surgery during general anaesthesia - Dose : 4mg is effective
  • 16. BENZODIZEPINES: -They help by relieving anxiety, anticipatory vomiting -produce amnesia for unpleasant procedure -also supress dystonic side effects of metoclopramide PROPOFOL: Antiemet -ic dose : 10-15 mg

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