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Drugs acting on GIT
*Drugs Acting on Gastro 
Intestinal Tract 
Presented by, 
ROSHNI ANN BABY 
Pharm. Chemistry 
M.Pharm Part I
*CONTENTS 
INTRODUCTION TO GI AGENTS 
EMETICS 
ANTIEMETICS 
DIARRHOEA AND ANTIDIARRHOEALS 
CONSTIPATION AND LAXATIVES 
MISCELLANEOUS DRUGS
*GASTRO INTESTINAL AGENTS 
Drugs acting on gastrointestinal tract gastrointestinal 
agents/drugs. 
Classified as – 
Drugs for peptic ulcer – Cimetidine, ranitidine, omeprazole, 
misoprostol, sucralfate etc. 
Emetics and anti emetics. 
Laxatives – lactulose, bisacodyl, liquid paraffin, castor oil etc.
Anti diarrhoeal drugs – Ispaghula, atropine, codeine, 
loperamide, sulfasalazine etc. 
Miscellaneous – Peppermint, cardamom, pepsin, papain, 
ursodiol, chenodiol etc
* EMETICS 
Emetics drugs used to evoke vomiting. 
Vomiting undesirable substances are ingested. 
At emergency powdered mustard suspension or strong salt 
solution may be used. 
CLASSIFICATION. 
Act on Chemoreceptor Trigger Zone(CTZ). 
eg: Apomorphine. 
Act reflexly and on CTZ. 
eg: Cephaeline.
Drugs acting on GIT
* APOMORPHINE. 
Mechanism of action(MOA) 
Acts centrally by stimulating the 
medullary CTZ connected with 
vomiting centre 
Uses 
As emetic. 
HO OH 
N 
H 
H3C
* CEPHAELINE 
MOA. 
Locally by irritating the gastric mucosa & centrally by 
stimulating the medullary CTZ to induce 
vomiting. 
Uses – as emetic. 
H3C 
O 
Chemically it is an alkaloid found in ipecac. 
CH3 
H 
H 
H3C 
O 
N 
HN 
O CH3 
OH
* ANTIEMETICS 
Anti emetics drugs used to prevent or suppress 
vomiting. 
CLASSIFICATION OF ANTI EMETICS 
Anticholinergics 
eg: Hyoscine,Dicyclomine. 
H1 antihistamines. 
eg: Promethazine, Diphenhydramine, Dimenhydrinate, 
Doxylamine, Cyclizine, Meclizine, Cinnarizine.
Neuroleptics or D2 blockers. 
eg: Chlorpromazine, Prochlorperazine, Haloperidol. 
Prokinetic drugs. 
eg: Metoclopramide, Domperidone, Cisapride, Mosapride, 
Tegaserod. 
5HT3 antagonists. 
eg: Ondansetron, Granisetron. 
 Adjuant antiemetics. 
eg: Dexamethasone, Benzodiazepine, Cannabinoids.
*ANTICHOLINERGICS 
HYOSCINE 
MOA 
Blocks conduction of 
nerve impulses across a 
cholinergic link in the pathway 
leading from the vestibular 
apparatus to the vomiting centre. 
Uses 
For motion sickness. 
CH3 
O 
O 
O 
N OH 
9-methyl-3-oxa-9-azatri 
cyclo[3.3.1.02,4]non-7-yl 
(2S)-3-hydroxy-2-phenyl 
propanoate
* DICYCLOMINE 
MOA 
Same as that of hyoscine. 
2-(diethyl amino)ethyl(bicyclohexane)- 
1- carboxylate. 
Uses 
As antiemetic, spasmolytic, in motion sickness, morning 
sickness. 
O 
O N 
CH3 
CH3
*H1 ANTIHISTAMINES. 
MOA OF ANTIHISTAMINES 
Act by both relaxing the smooth muscles and also act 
centrally to depress vomiting centres. 
They diminish vestibular stimulation & depress labyrinthine 
function. 
H1 antagonism.
* PROMETHAZINE 
Uses 
Antihistaminic 
Antiemetic 
sedative 
S 
N 
H3C 
10-(2-(dimethylamino)propyl) 
phenothiazine. 
CH3 
N 
CH3
S 
N 
H 
PHENOTHAIZINE 
S 
N 
NaNH2 
ClCH2CHN(CH3)2 
S 
N 
CH3 
N 
H3C 
H3C 
+
* DIPHENHYDRAMINE 
Uses 
Antihistaminic 
Antiemetic 
Antitussive 
2-(diphenylmethoxy) 
Sedative N,N-dimethylethanamine. 
CH3 
O 
N 
CH3
* MECLIZINE 
Uses 
Antihistaminic 
Antiemetic 
1-(p-chlorophenylbenzyl)-4- 
(m-methylbenzyl)piperazine. 
Cl 
N N 
CH3
* CYCLIZINE 
H 
N N CH3 
1-(diphenylmethyl)-4-methyl piperazine. 
Uses 
In postoperative and drug induced vomiting. 
In motion sickness. 
C 
C6H5
* 
HN NH + CH3COCl N NH 
H3C 
O 
CH3I 
-HI 
N N CH3 
H3C 
O 
HCl 
HN N CH3 + 
Cl 
N N CH3 
-HCl
*NEUROLEPTICS 
MOA – They block D2 receptors in the CTZ. 
CHLORPROMAZINE. 
Uses 
Antipsychotic 
Antiemetic 
Antitussive 
H3C 
N CH3 
N 
2-chloro-10-(3-(dimethylamino) 
propyl)phenothiazine. 
S 
Cl
* HALOPERIDOL 
O 
F N 
4-(4-(p-chlorophenyl)-4-hydroxy 
piperidone)-4-N-fluorobutyrophenone 
Uses 
Antipsychotic 
antiemetic 
CCH 2CH2CH2 
Cl 
OH
*PROCHLORPERAZINE 
2-chloro-10-[3-(4-methyl-1-piperazinyl) propyl ] 
phenothiazine 
Uses 
antiemetic 
S 
N Cl 
(CH2)3 N N CH3
+ H3C N N Cl 
* 
S 
N 
H 
Cl 
2 CHLORO PHENOTHAIZINE 
-HCl 
NaNH2/TOLUENE 
H3C N N 
S 
N Cl
*PROKINETIC DRUGS 
METOCLOPRAMIDE 
MOA 
D2 antagonism, 
5HT3 antagonism, 
5HT4 agonism in CTZ 
or NTS. 
Uses 
Cl 
Antiemetic 4-amino-5-chloro-N-(2-(diethyl-aminoethyl)- 
2-methoxy benzamide 
H2N 
O 
NH 
N 
CH3 
CH3 
O 
CH3
* DOMPERIDONE 
H 
5-chloro-1-(1-(3-(2-oxo2,3-dihydro-1H-benzo 
imidazol-1-yl)propyl)piperidin-4-yl)-1H-benzo 
imidazol-2(3H)-one. 
MOA – D2 antagonism in CTZ. 
Uses 
Antiemetic 
O 
N 
N 
O 
N 
N 
H 
N 
Cl
*5HT3 ANTAGONISTS 
ONDANSETRON 
Act via CTZ or NTS 
Uses 
In chemotherapy induced vomiting. 
In post operative vomiting. 
CH O 3 
N 
N N 
H3C 
9-methyl-3-[(2-methyl-1H-imidazol-1-yl) 
methyl]-1,2,3,9-tetrahydro-4H-carbazol- 
4-one
* GRANISETRON 
Has long half life compared to 
ondansetron. 
Uses 
In chemotherapy induced vomiting 
In post operative vomiting 
H3C 
O 
N 
H3C 
NH 
N 
N 
1-methyl-N-(9-methyl-9-azabicyclo 
[3.3.1]non-3-yl)-1H-indazole-3-carb 
oxamide
DIARRHOEA 
Loose bowel movements resulting into the frequent 
passage of watery,uniformed stools with or without 
mucous and blood. 
Classification 
Osmotic diarrhoea 
Something in the bowel draws water from the body into the 
bowel. 
Eg;Sorbitol is not absorbed by the body but draws water from 
the body into the bowel, resulting in diarrhoea.
Secretory diarrhoea 
Occurs when the body is releasing water into the bowel, 
many infections, drugs causes secretory diarrhoea. 
Exudative diarrhoea 
Diarrhoea with the presence of blood and pus in the stool. 
This occurs with inflammatory bowels disease (IBD), such as 
Crohn’s disease or ulcerative colitis etc.
Acute diarrhoea 
Sudden onset in a previously healthy person 
Lasts from 3 days to 2 weeks 
Self-limiting 
Resolves without sequels 
Chronic diarrhoea 
Lasts for more than 3 weeks. 
Associated with recurring passage of diarrhoeal stools, fever, 
loss of appetite, nausea, vomiting, weight loss, and chronic 
weakness
CAUSES OF DIARRHOEA 
Acute Diarrhoea 
Microbes 
Drug induced 
Nutritional 
Chronic Diarrhoea 
Tumours 
Diabetes 
Addison’s disease 
Hyperthyroidism 
Irritable bowel syndrome 
E. Coli bacteria Rotavirus
DRUG THERAPY 
i. Specific antimicrobial drugs 
ii. Non specific antidiarrhoeal drugs 
ORAL REHYDRATION 
THERAPY
Specific anti microbial drugs 
A. Antimicrobials are of no value 
Due to non infective causes such as 
Irritable bowel syndrome 
Colic disease 
Pancreatic enzyme deficiency etc 
Rota virus causes acute diarrhoea, specially in children
B. Antimicrobials are regularly useful 
cholera 
Tetracyclines, 
chloramphenicol 
etc 
Clostridium 
difficile 
Vancomycin, 
metronidazole etc 
amoebiasis 
Metronidazole, 
dioxonid 
furoate
NON SPECIFIC ANTIDIARROEALS 
1.Adsorbents 
Eg; kaolin, pectin, calcium carbonate. Etc 
2. Anti secretory drugs 
Eg; sulphasalazine, bismuth sub salicylate, 
atropine etc. 
3.Antimotility drugs 
Eg: codeine, loperamide, diphenoxylate etc
Functions of Antidiarrhoeal Drugs 
Decrease irritation to the intestinal wall 
Block GI muscle activity to decrease movement 
Affect CNS activity that cause GI spasm and stop 
movement 
Relief of symptoms and compensation of fluid & 
electrolyte loss
Non Specific Antidiarrhoeal Drugs 
Adsorbents 
 Coat the walls of the GI tract 
 Bind to the causative bacteria or toxin, which is then 
eliminated through the stool 
 Examples: bismuth subsalicylate, kaolin-pectin, activated 
charcoal.
Side Effects 
Increased bleeding time 
Constipation, dark stools 
Confusion 
Hearing loss, metallic taste, blue gums
Anti secretory drugs 
 Agents which reduce the secretion 
 Decrease intestinal muscle tone and peristalsis of GI tract 
 Result: slowing the movement of faecal matter through the 
GI tract 
 Examples: belladonna alkaloids, atropine, sulphasalazine, 
hyoscyamine
Side effects 
Urinary retention, impotence 
Headache, dizziness, confusion, anxiety, drowsiness 
Dry skin, rash, flushing 
Blurred vision, photophobia, increased intraocular 
pressure 
Hypotension, hypertension, bradycardia, tachycardia
Antimotility drugs 
Decrease bowel motility and relieve rectal spasms 
Decrease transit time through the bowel, allowing more 
time for water and electrolytes to be absorbed 
Examples: codeine, loperamide, diphenoxylate
Side effects 
Drowsiness, sedation, dizziness, lethargy 
Nausea, vomiting, anorexia, constipation 
Respiratory depression 
Bradycardia, palpitations, hypotension 
Urinary retention 
Flushing, rash, urticaria
O 
N 
N 
CH2 
C 
C CH2 
C 
O 
CH2 
H3C 
Diphenoxylate HCl
SYNTHESIS OF DIPHENOXYLATE HCL 
CH3 
H2C 
NH 
O 
O 
H2C 
H2C 
+ O 
CH3 
H2C 
N 
O 
O 
CH2 
CH2 
OH 
ethyl 4-phenylpiperidine-4-carboxylate ethyl 1-(2-hydroxyethyl)-4-phenylpiperidine-4-carboxylate 
CH3 
H2C 
N 
O 
O 
CH2 
CH2 
Cl 
H3C C 
H + 
N 
CH2 N 
O 
C CH2 
O 
CH2 
H3C 
C 
ethylene oxide
LOPERAMIDE 
H3C CH3 
N 
N 
CH2 
C CH2 
OH 
C 
Cl 
O
N 
HN 
O 
S 
N 
N 
HO 
O 
HO 
O 
SULPHASALAZINE
Synthesis of Sulphasalazine 
O 
OH 
OH 
H2N 
Cl 
N O 
OH 
OH 
N 
+ 
H 
S 
O 
N N 
O 
H2N 
H 
N 
N 
O 
S 
N 
N 
HO 
O 
HO 
O 
5-amino-2-hydroxybenzoic acid 
NaNO2/HCl 
5-[(Z)-chlorodiazenyl]-2-hydroxybenzoic acid 
4-amino-N-(pyridin-2-yl)benzenesulfonamide 
2-hydroxy-5-{(E)-[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl}benzoic acid
Metabolism of Sulphasalazine 
Sulphasalazine 
[H] 
Gut 
H2N 
O 
OH 
OH 
5- Amino salicylic acid 
+ 
H 
O 
S 
N 
O N 
N-(pyridin-2-yl)benzenesulfonamide 
Prodrug, having low solubility and poorly absorbed from 
ileum. 
 The azo bond split by colon bacteria into Sulfapyridine and 
5-amino salicylic acid. 
Blocks cyclooxgenase and lipooxygenase pathway and 
reduce mucosal secretion.
Laxatives
CONSTIPATION 
Constipation is the infrequent and/or unsatisfactory 
defecation fewer than 3 times per week. 
Abnormally infrequent and difficult passage of faeces through 
the lower GI tract 
Symptom, not a disease 
Disorder of movement through the colon and/or rectum
CAUSES OF CONSTIPATION 
Diet 
 Lack of exercise 
 Irregular bowel habits 
 Drug induced 
 Disease States/Conditions 
Spasm of colon 
Dysfunction of myenteric plexus
SYMPTOMS OF CONSTIPATION 
Infrequent defecation 
Nausea 
Vomiting 
Anorexia 
Feeling full quickly 
Stools that are small, hard, and/or difficult 
to evacuate 
Rectal bleeding 
Weight loss (in chronic constipation)
• Mild action, 
elimination of soft 
stools but formed 
stools. 
Laxative or 
aperients 
• Stronger action 
resulting in more 
fluid evacuation. 
Purgative or 
cathartic 
LAXATIVES 
Drugs that promote evacuation of bowels. 
Based on intensity of action
Classification 
• Methyl cellulose, 
ispaghula,Agar, 
Psyllium seeds 
1. Bulk 
forming 
• Liquid paraffin, 
Glycerine, Olive oil 
2. Stool 
softener
Diphenyl 
methanes 
• Bisacodyl, phenolphthalein, sodium 
picosulphate. 
Anthraqui 
nones 
• Senna, cascara sagrada 
5HT4 
agonist • Tegaserod 
Fixed 
oil • Castor oil 
3. Stimulant 
purgative
4. Osmotic purgative 
Magnesium salts, lactulose 
etc 
Bulk Forming Laxatives 
Improve stool consistency and frequency with regular use 
Ensure good fluid intake to prevent faecal impaction 
Onset of action 2-3 days 
Side Effects may include bloating, flatulence, distension
Stool Softeners 
May be useful with anal fissures of haemorrhoids 
Liquid paraffin is not recommended for treatment of 
constipation 
- risk of aspiration and lipoid pneumonia 
- long term use may result in depletion of Vitamins 
A, D, E and K
Stimulant Laxatives 
 Increase intestinal motility by stimulating colonic nerves 
 Useful with opioids 
 Onset of action 8-12 hours 
 May develop tolerance 
 2nd line therapy in elderly due to risk of electrolyte 
disturbances 
Cramping, diarrhoea, dehydration
Osmotic Laxatives 
Increase fecal water content 
Result: bowel distention, increased peristalsis, and 
evacuation 
Improving stool frequency 
Onset of action – up to 48 hours 
Metabolized by bacteria  flatulence
O 
O 
N 
H O 3 C O 
CH3 
Bisacodyl 
Synthesis of Bisacodyl 
N O 
CH + 2C6H5OH 
H2SO4 
(CH3CO)2O 
N 
O 
O 
O 
C 
CH3 
CH3 
C 
O 
pyridine-2-carbaldehyde 
(pyridin-2-ylmethanediyl)dibenzene-3,1-diyl diacetate
O 
O 
OH 
OH 
Phenolphthalein 
O 
O 
O 
+ 
OH 
OH 
H2SO4 
 
O 
O 
OH 
OH 
phathalic anhydride 
phenol 
3,3-bis(4-hydroxyphenyl)-2-benzofuran-1(3H)-one 
phenolphthalein 
Synthesis of phenolphthalein
N 
- 
- 
Na S S 
Na 
O O 
O 
O 
O 
O O 
O 
sodium picosulphate 
-{(pyridin-2-ylmethanediyl)dibenzene-4,1-diyl bis[hydrogenato(2-)-O sulfate]}disodate(2-)
OH 
NH 
N NH 
NH 
Tegaserod CH3 
3-[(E)-{2-[(pentylamino)methyl]hydrazinylidene}methyl]-1H-indol-5-ol 
It is 5HT4 agonist used for the management of 
irritable bowel syndrome and constipation
*Contract stomach muscles and stimulate hunger 
N 
N 
3-phenyl-3,4-dihydroquinazoline( Orexin) 
Bitters – secretion of gastric juice 
Eg: Quassins
* 
*Disturbance of appestat – weight regulating 
mechanism in hypothalamus 
Eg: Dextro amphetamine 
NH2 
CH3 
NH2 
CH3 
H3C 
Aptrol
* 
*HCl 
*Pepsin 
O 
O 
CH3 
CH3 
O 
O 
OH 
CH3 
Florantyrone 
Si O 
CH3 
O 
CH3 
CH3 
Si CH3 
CH3 
CH3 
Si 
CH3 
H3C 
n 
Simethicone
* 
*Protect sensitive surface from irritation 
*Lozenges or gargles 
*Cohesive substances like colloids, dextrins, sugar, 
starches 
*Eg: Acacia 
Tragacanth 
Liquorice
* 
*PPI 
*H2 blockers 
*Sodium alginate 
*Prokinetic drugs 
*Antacids
* 
*Expulsion of gases 
*Eg: Sodium bicarbonate 
Peppermint oil 
Tincture of cardamom 
Oil of dill 
Tincture of ginger
* 
CH3 
CH3 
CH3 
NH 
N 
O O CH3 
Camylofin 
*Anticholinergics 
NH 
O 
CH3 
O 
CH3 
H3C O 
H3C O 
Dicycloverine
Liver protectants 
*Chenodiol ( chenodeoxy cholic acid) 
*Ursodiol ( Ursodeoxy cholic acid) 
Gall stone dissolving drugs 
*Metadoxine 
*L-Ornithine 
*L- Aspartase 
*Silymarin
* 
Proton pump inhibitor 
IL – YANG pharmaceuticals 
NH 
H 
N 
N 
S 
O 
H3C O CH3 
N 
Ilaprazole
Anti diarroheal 
HIV Assosiated 
NAPO pharmaceuticals 
O 
O 
HO 
OH 
HO 
HO 
HO 
OH 
OH 
HO 
OH 
OH 
O 
HO 
OH 
HO 
OH 
OH 
Crofelimer
Antiemetic drug 
Neurokinin receptor antagonist 
N 
N 
N 
F 
H3C 
O 
CH3 
N 
O 
CH3 
CH3 
CF3 
CF3 
Casopirant
REFERENCE 
1.Text Book of Medicinal Chemistry by V. Alagarsamy, 
1st edition volume-II, page no:1137 
2.Bently and Driver’s Text book of Pharmaceutical Chemistry 
8th edition, page No. 724, 625. 
3.Essentials of Medicinal Pharmacology by K D TRIPATHI, 
6th edition page No. 651 
4.Clinical Pharmacy and Therapeutics, by Roger Walker, 
Cate Whitelsia, 4th edition, Page No: 824- 832 
5. Foye’s principles of Medicinal Chemistry, 5th edition, 
page No: 474-475
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Drugs acting on GIT

  • 2. *Drugs Acting on Gastro Intestinal Tract Presented by, ROSHNI ANN BABY Pharm. Chemistry M.Pharm Part I
  • 3. *CONTENTS INTRODUCTION TO GI AGENTS EMETICS ANTIEMETICS DIARRHOEA AND ANTIDIARRHOEALS CONSTIPATION AND LAXATIVES MISCELLANEOUS DRUGS
  • 4. *GASTRO INTESTINAL AGENTS Drugs acting on gastrointestinal tract gastrointestinal agents/drugs. Classified as – Drugs for peptic ulcer – Cimetidine, ranitidine, omeprazole, misoprostol, sucralfate etc. Emetics and anti emetics. Laxatives – lactulose, bisacodyl, liquid paraffin, castor oil etc.
  • 5. Anti diarrhoeal drugs – Ispaghula, atropine, codeine, loperamide, sulfasalazine etc. Miscellaneous – Peppermint, cardamom, pepsin, papain, ursodiol, chenodiol etc
  • 6. * EMETICS Emetics drugs used to evoke vomiting. Vomiting undesirable substances are ingested. At emergency powdered mustard suspension or strong salt solution may be used. CLASSIFICATION. Act on Chemoreceptor Trigger Zone(CTZ). eg: Apomorphine. Act reflexly and on CTZ. eg: Cephaeline.
  • 8. * APOMORPHINE. Mechanism of action(MOA) Acts centrally by stimulating the medullary CTZ connected with vomiting centre Uses As emetic. HO OH N H H3C
  • 9. * CEPHAELINE MOA. Locally by irritating the gastric mucosa & centrally by stimulating the medullary CTZ to induce vomiting. Uses – as emetic. H3C O Chemically it is an alkaloid found in ipecac. CH3 H H H3C O N HN O CH3 OH
  • 10. * ANTIEMETICS Anti emetics drugs used to prevent or suppress vomiting. CLASSIFICATION OF ANTI EMETICS Anticholinergics eg: Hyoscine,Dicyclomine. H1 antihistamines. eg: Promethazine, Diphenhydramine, Dimenhydrinate, Doxylamine, Cyclizine, Meclizine, Cinnarizine.
  • 11. Neuroleptics or D2 blockers. eg: Chlorpromazine, Prochlorperazine, Haloperidol. Prokinetic drugs. eg: Metoclopramide, Domperidone, Cisapride, Mosapride, Tegaserod. 5HT3 antagonists. eg: Ondansetron, Granisetron.  Adjuant antiemetics. eg: Dexamethasone, Benzodiazepine, Cannabinoids.
  • 12. *ANTICHOLINERGICS HYOSCINE MOA Blocks conduction of nerve impulses across a cholinergic link in the pathway leading from the vestibular apparatus to the vomiting centre. Uses For motion sickness. CH3 O O O N OH 9-methyl-3-oxa-9-azatri cyclo[3.3.1.02,4]non-7-yl (2S)-3-hydroxy-2-phenyl propanoate
  • 13. * DICYCLOMINE MOA Same as that of hyoscine. 2-(diethyl amino)ethyl(bicyclohexane)- 1- carboxylate. Uses As antiemetic, spasmolytic, in motion sickness, morning sickness. O O N CH3 CH3
  • 14. *H1 ANTIHISTAMINES. MOA OF ANTIHISTAMINES Act by both relaxing the smooth muscles and also act centrally to depress vomiting centres. They diminish vestibular stimulation & depress labyrinthine function. H1 antagonism.
  • 15. * PROMETHAZINE Uses Antihistaminic Antiemetic sedative S N H3C 10-(2-(dimethylamino)propyl) phenothiazine. CH3 N CH3
  • 16. S N H PHENOTHAIZINE S N NaNH2 ClCH2CHN(CH3)2 S N CH3 N H3C H3C +
  • 17. * DIPHENHYDRAMINE Uses Antihistaminic Antiemetic Antitussive 2-(diphenylmethoxy) Sedative N,N-dimethylethanamine. CH3 O N CH3
  • 18. * MECLIZINE Uses Antihistaminic Antiemetic 1-(p-chlorophenylbenzyl)-4- (m-methylbenzyl)piperazine. Cl N N CH3
  • 19. * CYCLIZINE H N N CH3 1-(diphenylmethyl)-4-methyl piperazine. Uses In postoperative and drug induced vomiting. In motion sickness. C C6H5
  • 20. * HN NH + CH3COCl N NH H3C O CH3I -HI N N CH3 H3C O HCl HN N CH3 + Cl N N CH3 -HCl
  • 21. *NEUROLEPTICS MOA – They block D2 receptors in the CTZ. CHLORPROMAZINE. Uses Antipsychotic Antiemetic Antitussive H3C N CH3 N 2-chloro-10-(3-(dimethylamino) propyl)phenothiazine. S Cl
  • 22. * HALOPERIDOL O F N 4-(4-(p-chlorophenyl)-4-hydroxy piperidone)-4-N-fluorobutyrophenone Uses Antipsychotic antiemetic CCH 2CH2CH2 Cl OH
  • 23. *PROCHLORPERAZINE 2-chloro-10-[3-(4-methyl-1-piperazinyl) propyl ] phenothiazine Uses antiemetic S N Cl (CH2)3 N N CH3
  • 24. + H3C N N Cl * S N H Cl 2 CHLORO PHENOTHAIZINE -HCl NaNH2/TOLUENE H3C N N S N Cl
  • 25. *PROKINETIC DRUGS METOCLOPRAMIDE MOA D2 antagonism, 5HT3 antagonism, 5HT4 agonism in CTZ or NTS. Uses Cl Antiemetic 4-amino-5-chloro-N-(2-(diethyl-aminoethyl)- 2-methoxy benzamide H2N O NH N CH3 CH3 O CH3
  • 26. * DOMPERIDONE H 5-chloro-1-(1-(3-(2-oxo2,3-dihydro-1H-benzo imidazol-1-yl)propyl)piperidin-4-yl)-1H-benzo imidazol-2(3H)-one. MOA – D2 antagonism in CTZ. Uses Antiemetic O N N O N N H N Cl
  • 27. *5HT3 ANTAGONISTS ONDANSETRON Act via CTZ or NTS Uses In chemotherapy induced vomiting. In post operative vomiting. CH O 3 N N N H3C 9-methyl-3-[(2-methyl-1H-imidazol-1-yl) methyl]-1,2,3,9-tetrahydro-4H-carbazol- 4-one
  • 28. * GRANISETRON Has long half life compared to ondansetron. Uses In chemotherapy induced vomiting In post operative vomiting H3C O N H3C NH N N 1-methyl-N-(9-methyl-9-azabicyclo [3.3.1]non-3-yl)-1H-indazole-3-carb oxamide
  • 29. DIARRHOEA Loose bowel movements resulting into the frequent passage of watery,uniformed stools with or without mucous and blood. Classification Osmotic diarrhoea Something in the bowel draws water from the body into the bowel. Eg;Sorbitol is not absorbed by the body but draws water from the body into the bowel, resulting in diarrhoea.
  • 30. Secretory diarrhoea Occurs when the body is releasing water into the bowel, many infections, drugs causes secretory diarrhoea. Exudative diarrhoea Diarrhoea with the presence of blood and pus in the stool. This occurs with inflammatory bowels disease (IBD), such as Crohn’s disease or ulcerative colitis etc.
  • 31. Acute diarrhoea Sudden onset in a previously healthy person Lasts from 3 days to 2 weeks Self-limiting Resolves without sequels Chronic diarrhoea Lasts for more than 3 weeks. Associated with recurring passage of diarrhoeal stools, fever, loss of appetite, nausea, vomiting, weight loss, and chronic weakness
  • 32. CAUSES OF DIARRHOEA Acute Diarrhoea Microbes Drug induced Nutritional Chronic Diarrhoea Tumours Diabetes Addison’s disease Hyperthyroidism Irritable bowel syndrome E. Coli bacteria Rotavirus
  • 33. DRUG THERAPY i. Specific antimicrobial drugs ii. Non specific antidiarrhoeal drugs ORAL REHYDRATION THERAPY
  • 34. Specific anti microbial drugs A. Antimicrobials are of no value Due to non infective causes such as Irritable bowel syndrome Colic disease Pancreatic enzyme deficiency etc Rota virus causes acute diarrhoea, specially in children
  • 35. B. Antimicrobials are regularly useful cholera Tetracyclines, chloramphenicol etc Clostridium difficile Vancomycin, metronidazole etc amoebiasis Metronidazole, dioxonid furoate
  • 36. NON SPECIFIC ANTIDIARROEALS 1.Adsorbents Eg; kaolin, pectin, calcium carbonate. Etc 2. Anti secretory drugs Eg; sulphasalazine, bismuth sub salicylate, atropine etc. 3.Antimotility drugs Eg: codeine, loperamide, diphenoxylate etc
  • 37. Functions of Antidiarrhoeal Drugs Decrease irritation to the intestinal wall Block GI muscle activity to decrease movement Affect CNS activity that cause GI spasm and stop movement Relief of symptoms and compensation of fluid & electrolyte loss
  • 38. Non Specific Antidiarrhoeal Drugs Adsorbents  Coat the walls of the GI tract  Bind to the causative bacteria or toxin, which is then eliminated through the stool  Examples: bismuth subsalicylate, kaolin-pectin, activated charcoal.
  • 39. Side Effects Increased bleeding time Constipation, dark stools Confusion Hearing loss, metallic taste, blue gums
  • 40. Anti secretory drugs  Agents which reduce the secretion  Decrease intestinal muscle tone and peristalsis of GI tract  Result: slowing the movement of faecal matter through the GI tract  Examples: belladonna alkaloids, atropine, sulphasalazine, hyoscyamine
  • 41. Side effects Urinary retention, impotence Headache, dizziness, confusion, anxiety, drowsiness Dry skin, rash, flushing Blurred vision, photophobia, increased intraocular pressure Hypotension, hypertension, bradycardia, tachycardia
  • 42. Antimotility drugs Decrease bowel motility and relieve rectal spasms Decrease transit time through the bowel, allowing more time for water and electrolytes to be absorbed Examples: codeine, loperamide, diphenoxylate
  • 43. Side effects Drowsiness, sedation, dizziness, lethargy Nausea, vomiting, anorexia, constipation Respiratory depression Bradycardia, palpitations, hypotension Urinary retention Flushing, rash, urticaria
  • 44. O N N CH2 C C CH2 C O CH2 H3C Diphenoxylate HCl
  • 45. SYNTHESIS OF DIPHENOXYLATE HCL CH3 H2C NH O O H2C H2C + O CH3 H2C N O O CH2 CH2 OH ethyl 4-phenylpiperidine-4-carboxylate ethyl 1-(2-hydroxyethyl)-4-phenylpiperidine-4-carboxylate CH3 H2C N O O CH2 CH2 Cl H3C C H + N CH2 N O C CH2 O CH2 H3C C ethylene oxide
  • 46. LOPERAMIDE H3C CH3 N N CH2 C CH2 OH C Cl O
  • 47. N HN O S N N HO O HO O SULPHASALAZINE
  • 48. Synthesis of Sulphasalazine O OH OH H2N Cl N O OH OH N + H S O N N O H2N H N N O S N N HO O HO O 5-amino-2-hydroxybenzoic acid NaNO2/HCl 5-[(Z)-chlorodiazenyl]-2-hydroxybenzoic acid 4-amino-N-(pyridin-2-yl)benzenesulfonamide 2-hydroxy-5-{(E)-[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl}benzoic acid
  • 49. Metabolism of Sulphasalazine Sulphasalazine [H] Gut H2N O OH OH 5- Amino salicylic acid + H O S N O N N-(pyridin-2-yl)benzenesulfonamide Prodrug, having low solubility and poorly absorbed from ileum.  The azo bond split by colon bacteria into Sulfapyridine and 5-amino salicylic acid. Blocks cyclooxgenase and lipooxygenase pathway and reduce mucosal secretion.
  • 51. CONSTIPATION Constipation is the infrequent and/or unsatisfactory defecation fewer than 3 times per week. Abnormally infrequent and difficult passage of faeces through the lower GI tract Symptom, not a disease Disorder of movement through the colon and/or rectum
  • 52. CAUSES OF CONSTIPATION Diet  Lack of exercise  Irregular bowel habits  Drug induced  Disease States/Conditions Spasm of colon Dysfunction of myenteric plexus
  • 53. SYMPTOMS OF CONSTIPATION Infrequent defecation Nausea Vomiting Anorexia Feeling full quickly Stools that are small, hard, and/or difficult to evacuate Rectal bleeding Weight loss (in chronic constipation)
  • 54. • Mild action, elimination of soft stools but formed stools. Laxative or aperients • Stronger action resulting in more fluid evacuation. Purgative or cathartic LAXATIVES Drugs that promote evacuation of bowels. Based on intensity of action
  • 55. Classification • Methyl cellulose, ispaghula,Agar, Psyllium seeds 1. Bulk forming • Liquid paraffin, Glycerine, Olive oil 2. Stool softener
  • 56. Diphenyl methanes • Bisacodyl, phenolphthalein, sodium picosulphate. Anthraqui nones • Senna, cascara sagrada 5HT4 agonist • Tegaserod Fixed oil • Castor oil 3. Stimulant purgative
  • 57. 4. Osmotic purgative Magnesium salts, lactulose etc Bulk Forming Laxatives Improve stool consistency and frequency with regular use Ensure good fluid intake to prevent faecal impaction Onset of action 2-3 days Side Effects may include bloating, flatulence, distension
  • 58. Stool Softeners May be useful with anal fissures of haemorrhoids Liquid paraffin is not recommended for treatment of constipation - risk of aspiration and lipoid pneumonia - long term use may result in depletion of Vitamins A, D, E and K
  • 59. Stimulant Laxatives  Increase intestinal motility by stimulating colonic nerves  Useful with opioids  Onset of action 8-12 hours  May develop tolerance  2nd line therapy in elderly due to risk of electrolyte disturbances Cramping, diarrhoea, dehydration
  • 60. Osmotic Laxatives Increase fecal water content Result: bowel distention, increased peristalsis, and evacuation Improving stool frequency Onset of action – up to 48 hours Metabolized by bacteria  flatulence
  • 61. O O N H O 3 C O CH3 Bisacodyl Synthesis of Bisacodyl N O CH + 2C6H5OH H2SO4 (CH3CO)2O N O O O C CH3 CH3 C O pyridine-2-carbaldehyde (pyridin-2-ylmethanediyl)dibenzene-3,1-diyl diacetate
  • 62. O O OH OH Phenolphthalein O O O + OH OH H2SO4  O O OH OH phathalic anhydride phenol 3,3-bis(4-hydroxyphenyl)-2-benzofuran-1(3H)-one phenolphthalein Synthesis of phenolphthalein
  • 63. N - - Na S S Na O O O O O O O O sodium picosulphate -{(pyridin-2-ylmethanediyl)dibenzene-4,1-diyl bis[hydrogenato(2-)-O sulfate]}disodate(2-)
  • 64. OH NH N NH NH Tegaserod CH3 3-[(E)-{2-[(pentylamino)methyl]hydrazinylidene}methyl]-1H-indol-5-ol It is 5HT4 agonist used for the management of irritable bowel syndrome and constipation
  • 65. *Contract stomach muscles and stimulate hunger N N 3-phenyl-3,4-dihydroquinazoline( Orexin) Bitters – secretion of gastric juice Eg: Quassins
  • 66. * *Disturbance of appestat – weight regulating mechanism in hypothalamus Eg: Dextro amphetamine NH2 CH3 NH2 CH3 H3C Aptrol
  • 67. * *HCl *Pepsin O O CH3 CH3 O O OH CH3 Florantyrone Si O CH3 O CH3 CH3 Si CH3 CH3 CH3 Si CH3 H3C n Simethicone
  • 68. * *Protect sensitive surface from irritation *Lozenges or gargles *Cohesive substances like colloids, dextrins, sugar, starches *Eg: Acacia Tragacanth Liquorice
  • 69. * *PPI *H2 blockers *Sodium alginate *Prokinetic drugs *Antacids
  • 70. * *Expulsion of gases *Eg: Sodium bicarbonate Peppermint oil Tincture of cardamom Oil of dill Tincture of ginger
  • 71. * CH3 CH3 CH3 NH N O O CH3 Camylofin *Anticholinergics NH O CH3 O CH3 H3C O H3C O Dicycloverine
  • 72. Liver protectants *Chenodiol ( chenodeoxy cholic acid) *Ursodiol ( Ursodeoxy cholic acid) Gall stone dissolving drugs *Metadoxine *L-Ornithine *L- Aspartase *Silymarin
  • 73. * Proton pump inhibitor IL – YANG pharmaceuticals NH H N N S O H3C O CH3 N Ilaprazole
  • 74. Anti diarroheal HIV Assosiated NAPO pharmaceuticals O O HO OH HO HO HO OH OH HO OH OH O HO OH HO OH OH Crofelimer
  • 75. Antiemetic drug Neurokinin receptor antagonist N N N F H3C O CH3 N O CH3 CH3 CF3 CF3 Casopirant
  • 76. REFERENCE 1.Text Book of Medicinal Chemistry by V. Alagarsamy, 1st edition volume-II, page no:1137 2.Bently and Driver’s Text book of Pharmaceutical Chemistry 8th edition, page No. 724, 625. 3.Essentials of Medicinal Pharmacology by K D TRIPATHI, 6th edition page No. 651 4.Clinical Pharmacy and Therapeutics, by Roger Walker, Cate Whitelsia, 4th edition, Page No: 824- 832 5. Foye’s principles of Medicinal Chemistry, 5th edition, page No: 474-475