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.

1. Pro-Kinetic Agents
Dr. Khalid Ghaznavi
Doctor of Physiotherapy
(USA)

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)

9. Emetics & Anti-emetics
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)

15. Classification: Anti-emetics
1. Dopamine D2 Antagonists-Prokinetic drugs:
Metoclopramide, Domperidone, Cisapride, Mosapride
2.Anti-cholinergics/ muscarinics:
Hyoscine, Dicyclomine
3. H1 anti-histaminics:
Promethazine, Diphenhydramine, Cyclizine
4. 5HT3 –Antagonists:
Ondansetron, Granisetron, Dolasetron, Tropisteron.
5. Adjuvant anti-emetics:
Corticosteroids, Benzodiazepines, Cannabinoids
6. Neuroleptics:
Chloropromazine, Prochlorperazine, haloperidol
7. Other agents:
Cisapride, Corticosteriods.
Dr.Khalid Ghaznavi
(DPT)

16. Pro-kinetic drugs
DOPAMINE D2
ANATAGOINST
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)

19. Anti-Cholinergics
ANTI-MUSCARINICS
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)

23. H1 Anti-Histamines
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)

25. Drugs available
1. Meclizine
2. Cyclizine
3. Diphenhydramine
4. Promethazine
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)

27. 5HT3 –Antagonists
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)

30. Adjuvant Anti-Emetics
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)

33. .From.
Dr.Khalid Ghaznavi
(DPT)