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Local
Emetics
Central
Emetics &
antiemetics
Anticholinergic
Anti-diarrhoeal
agents
Antihistamine
Laxative and
cathertics
Antiemetics
D2 receptor
antagonist
5HT3 receptor
antagonist
Cannabinoids
Pathophysiology N&V
Vomiting center loosely organized neuronal region & coordinates act of vomiting thru
interactions w/ CN VIII,CN X & NTS
Sources afferent input to vomiting center:
1. Chemoreceptor trigger zone (CTZ) which is outside the BBB & accessible to
emetogenic stimuli in blood / CSF. It rich in dopamine D2 receptor & opiod
receptors, serotonin 5HT3 & NK1 Receptors
2. Vestibular system motion sickness via CN VIII & rich in muscarinic M1 &
histamine H1 receptors
3. Vagal & spinal afferent nerves from GIT rich in 5 HT3 receptors. Irritation of GIT
by chemotherapy, distention, acute infectious gastroenteritis release mucosal
serotonin & activation of the receptors stimulate vagal afferent input to
vomiting center & CTZ
4. CNS: psychiatric disorders, stress
1.
2.
3.
4.
5.
6.
Types
Local
mustard & water
warm hypertonic solution of
salt
salts of heavy metals
1% Cupric sulphate
1% Zinc sulphate
Ipecac*** (alkaloid) syrup
Central
1. Apomorphi
ne selective
action on
CTZ
2. Ipecacuanh
a - locally
irritates the
gut &
centrally
acts on
CTZ
Emetics
Indications
1. Acute
1.
poisoning
by noncorrosive
substances
2.
2. Acute
indigestion
due to
3.
excessive
intake of
4.
food
CI
Poisoning by corrosives - cause scarring
eg, strong acids & alkalis - gastric perforation & damage
to esophagus
petroleum distillates - chemical pneumonitis due to
inhalation
Comatose, stuporous or delirious patients d/t
asphyxiation & aspiration pneumonia d/t lack of coughing
reflex
Pregnancy, hernias, advanced PU & other GI erosions d/t
intra-abdominal pressure is dangerous
Cardiac decompensated patient & hypertensive patient
d/t BP
5. Young children, debilitated patient d/t BP
Antiemetics
Drugs
1. Anticholinergics: Hyoscine
Classification
Site of action
Vomiting center &
Drugs
4. 5HT3 receptor
Site of action
CTZ & gut
MOA
Act either on Vomiting
Center(VC) / on CTZ
2. Anti-histamine:
Cinnarizine
Cyclizine
Meclizine
Diphenhydramine (Benedryl)
Dimenhydrinate (Dramamine)
Promethazine (Phenergan)
3. D2 receptor antagonists Phenothiazines:
o Chlorpromazine(Buromazine)
o Prochlorperazine (Stemetil)
o Perphenazine
Butyrophenone : Haloperidol
Metoclopramide
Domperidone (Motilium)
Hyoscine
(Scopolamine)
Cyclizine &
Meclizine
Promethazine
gut
Vomiting center
and gut
antagonists
Ondansetron
Tropisetron
Granisetron
5. Cannabinoids:
Nabilone
Pronabilol
Dronabinol
CTZ
Anti-emetic effect
1. VC anticholinergic
action, antihistaminic
action
2. CTZ - antidopaminergic /
5HT3 antagonist action
CTZ
CTZ
CTZ & gut
CTZ & gut
MOA
block central muscarinic receptor on VC & gut
(relaxation of GIT)
PK / Dosage
0.65 - 0.75 mg
IM
1. Cyclizine shortest
DOA, 50
mg TDS
2. Meclizine longest
DOA, 24
hrs / more,
single dose
50 mg
Dose- 25 mg
BD
Uses
motion sickness (given 1
hr b4 journey, lasts for 4
- 6 hrs)
Meclizine: motion
sickness & Rx vertigo d/t
labryth dysfx
morning sickness
CI / DI
Diphenhydram
ine &
dimenhydrinat
e
Phenothiazine
&
chlorpromazin
e
Prochlorperazi
ne &
perphenazine
Metochlopromi
de
Sedating properties
Dose- 50 - 100
mg TDS
Drowsiness (common)
Phenothiazine: potent
antiemetic & sedative
Dose - 25 - 50
mg 8 hourly IM
*structurally related to procainamide (lacks LA &
antiarrhythmic action)
Actions
1. antiemetic action
2. prokinetic action lower esophageal sphincter tone
gut peristalsis & emptying ,relaxation of
pyloric antrum & duodenal cap
MOA:
1. Central: inhibits dopamine D2 r/c on CTZ
2. Peripheral All these facilitate ACh release
from enteric neurons
may be d/t 5HT4 r/c agonistic action
5HT3 r/c antagonist action
D2 r/c blocking action on cholinergic enteric
neurones
rapidly &
completely
absorbed
1st pass
metabolism
present
Bioavailabil
ity 75%
T : 4-6 hr
Dose: 10
mg 8
hourly oral,
IM, IV
drowsiness,hypotensi
on, extrapyramidal
effects
A/E
1. extrapyramidal
dystonia: >
common in
children & young
adults w/ high
dose fatigue,
motor restless,
spasmodic
torticollis
(involuntary
twisting of neck),
occulogyric crises
(involuntary
upward eye
movement)
2. gynaecomastia,
galactorrhoea (due
to prolactin
secretion),
menstrual disorder
3. somnolence,
drowsiness,
dizziness,
diarrhoea
CI
1. intestinal
obstruction
2. perforation
3. haemorrhage
Domperidone
MOA
1. blocks dopamine receptor in CTZ (D2)
2. activation of dopamine receptor inhibit
cholinergic smooth muscle activation
blockade of D2 receptor oeso & gastric
contraction
Actions
1. tone in lower esophageal sphincter
2. Relax pyloric sphincter
3. Not penetrate well into BBB (no CNS effects)
4. Antagonise D2 in pituitary (prolactin level)
5. block adrenoreceptor increase motility by
relaxation
Ondansetron
Nabilone
dose 8 mg
TDS
Motion sickness
Hyoscine
best for motion
sickness, short
lasting
Other drugs:
o Cinnarazine
o Cyclizine
o Dimemhydrinate
o Promethazine
For prophylaxis, an
antiemetic is best
taken 1 hr before
exposure to the
motion
Once motion sickness
has started, IM, SC or
rectal routes are
required
Alternatively,
hyoscine may be
administered as a
dermal patch
Management
Vomiting d/t cytotoxic drug
Vomiting after
general anaesthesia
Metoclopramide
5HT3 receptor antagonist
or
(ondansetron) effective
5HT3 receptor
For severe vomiting,
antagonist
ondansetron plus
(ondansetron)
dexamethasone w/ or w/o
or
lorazepam (all given IV)
butyrophenone
most effective combination &
(haloperidol,
well tolerated
droperidol)
Metoclopramide may be
substituted for ondansetron
Occurs at 10-11
weeks & usually
resolves by 13-14
weeks of gestation
By reassurance that
the problem is
transient &
discussion of diet*
Rarely, decision is
taken to take a drug
H1 receptor
antagonist or
phenothiazine (eg,
promethazine) is
preferable
Pyridoxine deficiency
may occur in
hyperemesis
gravidarum which
requires IV fluids &
multivitamin
supplement
Vertigo
Antimuscarinics
&
phenothiazines
are generally
preferable
Cyclizine /
prochlorperazine
may be used to
relieve an acute
attack
Betahistine (a
histamine
analogue) used to
improve blood
circulation to the
inner ear in
Menieres disease;
also cinnarazine