This slide is based upon prokinetic agents with detailed descriptions of their dosage to be taken with their respective usage in conditions and effects to be careful. I hope you will get the best of your knowledge from the respective material.
2. Pro-Kinetic Agents
Drugs that….
enhance gastro-duodenal motility and
hasten the gastric motility
Metoclopramide
Domperidone
Cisapride
Mosapride Dr.Khalid Ghaznavi
(DPT)
3. --METOCLOPRAMIDE--
Actions GIT:
Promotes forward movement of upper GIT
Speeds up gastric emptying
Prevents reflex esophagitis
Slightly increase intestinal motility/peristalasis.
CNS Actions:
Acts as anti-emetic by
actions on CTZ and
by speeding up the gastric emptying
Dr.Khalid Ghaznavi
(DPT)
4. Mechanism of action of Metoclopramide
By Blocking dopamine receptors in the gut
By Enhancing acetylcholine release from the cholinergic neurons in the
gut
By Blocking the D2 receptors in the CTZ-responsible for anti-emetic
action
Dr.Khalid Ghaznavi
(DPT)
5. Adverse effects of Metoclopramide
Sedation
Dystonia
Diarrhea
Gynecomastia
Galactorrhea
Parkinsonism (extra-pyramidal symptoms) can occur on long term
use due to blockade of dopamine receptors.
Dr.Khalid Ghaznavi
(DPT)
6. Uses of Metoclopramide
Reflux esophagitis
Heart burn due to reflex of acid into esophagus is benefited by prokinetic
agents.
As anti-emetic
In post-operative period and vomiting due to anti-cancer drugs.
As pre-anesthetic medication
To promote gastric emptying before induction of general anesthesia in
emergency.
In Endoscopy
to assist the passage of tubes into duodenum
Dr.Khalid Ghaznavi
(DPT)
7. --DOMPERIDONE--
Similar to metoclopramide;
Except it does not cross Blood Brain Barrier
Hence does not cause extra-pyramidal side effects
Side effects include;
✓ Headache
✓ Dryness of mouth
✓ Diarrhea
✓ Rashes
Domperidone can be used in place of metoclopramide.
Dr.Khalid Ghaznavi
(DPT)
8. --CISAPRIDE--
Enhance gastric motility by promoting the release of
acetylcholine in gut wall
Promotes colonic motility which may result in diarrhea
Used in reflux esophagitis
But not being used because of their adverse effects now a days
Dr.Khalid Ghaznavi
(DPT)
10. Emetics
“A protective reflex that
serves to rid the stomach and intestine of toxic substances and
prevent their further ingestion.”
Occurs due to stimulation of the
emetic/vomiting center situated in the medulla oblongata
Dr.Khalid Ghaznavi
(DPT)
11. Multiple pathways can
elicit vomiting
Vomiting center receives
afferents impulses arising from
◼ CTZ ,
◼ GI Tract,
◼ throat ,
◼ vestibular apparatus and
◼ other viscera
CTZ is also accessible;
blood borne drugs,
mediators,
hormones,
toxins etc.
Dr.Khalid Ghaznavi
(DPT)
12. Emetics –centrally acting Apomorphine
Derivative of morphine.
Given S.C/I.M -6mg
Causes vomiting within 5-10 min
Vomiting is often accompanied by sedation
Act by stimulating CTZ
Dr.Khalid Ghaznavi
(DPT)
13. Emetics –peripherally acting Mustard:
It is safe and easily available
Dose -1 tp in water Sodium chloride
Given orally
Causes reflex emesis
Dr.Khalid Ghaznavi
(DPT)
14. Emetics –both Ipecacuanha (Emetine):
Contains an alkaloid emetine.
Given as syrup (15-20ml) it produces vomiting in 15 min.
It is safe even in children.
Acts by irritating gastric mucosa as well as through CTZ
Dried root of ipecacuanha contains emetine
Takes 15 min or more for the effect
Used as syrup ipecac for inducing vomiting
15-20ml adults
10-15ml children
5ml infants
Dr.Khalid Ghaznavi
(DPT)
17. --Metoclopramide--
Introduced in early 1970s as a ‘gastric hurrying agent’
Widely used anti-emetic Actions
Act centrally by blocking dopamine D2 receptors on the CTZ
Increases the tone of lower esophageal sphincter
Enhance gastric peristalsis
Dr.Khalid Ghaznavi
(DPT)
18. Uses
In nausea and vomiting due to gastrointestinal disorders
Migraine
Post-operative period
Vomiting due to anti-cancer drugs and radiotherapy
Vomiting due to pregnancy
Dr.Khalid Ghaznavi
(DPT)
20. --Hyoscine--
Most effective for motion sickness/travelling sickness
Due to overstimulation of vestibular apparatus along
with psychological and environmental factors
Dr.Khalid Ghaznavi
(DPT)
21. 0.4 -0.6mg oral, I.M
Take 30 min before journey
Acts for 6 hours
Suitable for short brisk journeys
Dose should be repeated if journey is longer
Produces sedation and other anticholinergic side effects
Transdermal patch 1.5mg applied behind the ear
To be delivered over 3 days
Suppresses motion sickness
Have only mild side effects
Dr.Khalid Ghaznavi
(DPT)
22. --DICYCLOMINE--
10-20mg oral
Used for prophylaxis of motion sickness and for morning
sickness
It has been cleared of teratogenic potential
Dr.Khalid Ghaznavi
(DPT)
24. H1 Anti-Histamines
Some anti-histaminics are anti-emetic
They are useful mainly in motion sickness and
Lesser extent in morning sickness, post-operative and some other
forms of vomiting
Their antiemetic effect appears to be based on anti-cholinergic,
anti-histaminic and sedative properties
Also Used in pregnancy Dr.Khalid Ghaznavi
(DPT)
26. H1 antihistamines Cont..
All antimotion drugs are more effective when taken ½ -1
hr before commencing journey
Once sickness has started, it is more difficult to control
Dr.Khalid Ghaznavi
(DPT)
28. --Ondansetron--
5-hydroxytryptamine released in the gut is an important
transmitter of emesis
Ondansetron blocks 5-hydroxytryptamine 3 receptors in
GIT and CTZ and prevents vomiting
Dr.Khalid Ghaznavi
(DPT)
29. Ondansetron
Used in:
Postoperative period
Vomiting due to anti-cancer drugs and radiotherapy
Drug induced vomiting
Dr.Khalid Ghaznavi
(DPT)
31. --Neuroleptics--
Potent antiemetics
Act by blocking D2 receptors in the CTZ
Antiemetic dose is much lower than antipsychotic doses
These agents should not be administered until the cause of
vomiting has been diagnosed
Dr.Khalid Ghaznavi
(DPT)
32. Neuroleptics Cont…
Broad spectrum antiemetic , effective in;
Drug induced and post-anesthetic nausea and vomiting
Disease induced vomiting
Chemotherapy induced (mildly emetogenic)
Dr.Khalid Ghaznavi
(DPT)
