ANTIEMETICS

PRINCIPLES
Used only when
cause is known.[if not
symptom masking]
Not needed when
cause is corrected.
Eg. DKA,
Drug depends on the
cause of vomiting
ANTIHISTAMINES
Act by inhibiting the H1 receptor
Use:
Vomiting due to vestibular
disorders[vertigo]
Vomiting in pregnancy[Promethazine]
Drugs:
Sedative Promethazine
Non sedative Cinnarizine, Cyclizine
DOPAMINE RECEPTOR ANTAGONISTS
Act on the CTZ and gut.
Antagonist of D2 receptors.
Metoclopramide[ most frequently asked drug in exam]
MOA: Centrally - Antagonize D2 receptors in CTZ
Peripherally [Prokinetic effect] Enhance action of Ach
at muscarinic receptors in gut causing,
Increased tone of LES
Relax pyloric antrum
Increase peristalsis and emptying on upper GIT
PK :Metabolized in liver, t1/2 =4hrs
USES:
Nausea and vomiting due to GI disorders, drugs,
migraine
Prokinetic effect used to empty gut before anesthesia
and labour.
CI: GI obstruction, perforation or haemorrhage,3-4 days after GI
Sx, Phaeochromocytoma
Hepatic and renal disease: Reduce dose
Not known to be harmful in pregnancy, avoid in breast feeding
SE: Extrapyramidal dystonia due to crossing of BBB and action
on basal ganglia [torticollis,facial spasms, trismus] / more in
younger females and children
Gynaecomastia and galactorrhoea
Dose: 10mg tds

Domperidone: Similar to metoclopromide except CI .
T1/2 = 7hrs
Poor BBB cross dystonic reactions are uncommon
CI: Prolactinoma
Dose: 10 20 mg 3-4 times a day
ANTIMUSCARINICS
Inhibit muscarinic receptor activation in
vomiting centre and gut.
Use:
Vomiting due to any cause due to action
at vomiting center.
Treatment of motion sickness
Drugs: Hyosine hydrobromide
SE : Drowsiness, blurred vision, urinary
retention, dry mouth
Dose:150 300 microgram, 30-60 mins before
travelling repeated 6 hrly[max 900ug daily]
5HT3 ANTAGONISTS
Drugs: Ondansetron, Granisetron
Effective for drug induced vomiting [chemo and
radio therapy]
Act centrally through CTZ and peripherally by
reducing action of serotonin in gut and CNS
[cancer drugs cause serotonin production by
enterochromaffin cells in gut.]
Ondansetron
SE: Constipation, headache, flushing
CI: congenital long QT syndrome
CORTICISTEROIDS
Drugs: Dexamethasone
Use: Adjuvant therapy in drug
induced vomiting.
SYNTHETIC CANNABINOIDS
Use: To relieve nausea or vomiting due to cytotoxic
drugs which is non responsive to other drugs.
Drugs : Nabilone

ANTIPSYCHOTIC DRUGS
1]Phenothiazines : block D2 receptor in CTZ, H1
receptor & muscarinic receptor in vomiting
center.
Eg:Prochlorperazine used in vertigo
2]Haloperidol
POST OPERATIVE VOMITING PREVENTION
Prochlorperazine : Deep IM or suppository
Metoclopramide IM or IV injections and oral