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Topic
Drugs for Peptic Ulcer
Antiametic Drugs
by:
Dr. Nirav Shah, Dr. Prashant M.D.
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VOMITING
Vomiting occurs due to stimulation of the emetic (vomiting) center situated in medulla oblongata.
ANTIEMETICS
These are drugs used to prevent or suppress vomiting.
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CLASSIFICATION :
1.Anticholinergics Hyoscine, Dicyclomine
2. H1 antihistaminics Promethazine,
Diphenhydramine,
Cyclizine, Meclozine,
Cinnarizine
3. Neuroleptics Chlopromazine,
Prochlorperazine,
Haloperidol etc.
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4.Prokinentic drugs Metoclopramide,
Domperidone,
Cisapride, Mosapride
5. 5-HT3 antagonists Ondansetron,
Granisetron
6. Adjuvant antimetics Dexamethasone,
Benzodiazepines,
Cannabinoids.
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ANTICHOLINEGRICS
1. most effective drug for motion sickness.
2. brief duration of action.
3. Produces sedation and other anticholinergic side effects.
4. Suitable only for short brisk journies.
5. It acts probably by blocking conduction of nerve impulses across a cholinergic pathway from the vestibular apparatus to the vomiting center.
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6. It is non effective in vomiting of other etiologies.
7. Applied behind the pinna, it suppresses motion sickness while producing only mild side effects.
8. Dicyclomine – It has been used for prophylaxis of motion sickness and for morning sickness.
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H1 ANTHIHISTAMINICS
1. Some antihistaminics are antiemetic.
2. They are useful mainly in motion sickness and morning sickness, postoperative and some other forms of vomiting.
3. Their antiemetic effect appears to be based on anticholinergic, antihistaminic and sedative properties.
a.They afford protection of motion sickness.
b.They produce sedation and dryness of mouth.
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Cycline meclozine
1. These are less sedative and less anticholinergic.
2. Meclozine is long acting, protects against sea sickness.
3. It is also protective for motion sickness.
4. All antimotion sickness drugs are more effective when taken ½ -1 hour before journey.
5. It is better to avoid them for morning sickness.
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NEUROLOPTICS
1. These are potent antiemetics.
2. Drug induced and postanesthetic nausea and vomiting.
3. Disease induced vomiting: gastroenteritis, liver disease, migraine etc.
4. Radiation sickness vomiting.
5. Morning sickness.
6. They are not effective in motion sickness.
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7. Produce significant degree of sedation.
8. Used primarily as an antiemetic rather than as antipsychotic.
9. Extrapyramidal side effects are the most important limiting features.
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Prokinetic drugs
1. Drugs which promote gastrointestinal transit and speed gastric emptying.
2. Widely used antiemetic.
Actions
1. More prominent effect on upper g.i.t., increases gastric peristalsis.
2. Speeds gastric emptying, specially if it was slow.
3. It also increases intestinal peristalsis.
4. But has no significant action on colonic motility and gastric secretion.
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CNS
1. Metoclopramide is an effective antiemetic.
2. Gastrokinetic action may contribute to the antiemetic effect.
3. Not useful as an antipsychotic.
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D2 antagonism
1. Dopamine is an inhibitory transmitter in g.i.t.
2. Normally acts to delay gastric emptying when food is present in stomach.
3. It also appears to cause gastric dilation and LES relaxation.
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4. Metoclopramide blocks D2 receptors and has an opposite effect.
5. Hastening gastric emptying and enhancing LES tone.
6. The central antidipaminergic (D2) action of metoclopramide on CTZ is clearly responsible for its antiemetic property.
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5-HT4 agonism
1. It acts in the g.i.t. to enhance ACh release.
2. Results from 5-HT4 receptor activation.
3. Which promote ACh release from,
4. The gastric hurrying and LES tonic effects are mainly due to this action.
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PHARMACOKINETICS
1. Metoclopramide is rapidly absorbed orally, crosses placenta and is secreted in milk.
2. it. enters brain,
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INTERACTIONS
1. It hastens the absorption of many drugs, e.g. aspirin, diazepam.
ADVERSE EFFECTS
1. Extrapyramidal side effects,diarrhoea, muscle dystonias are the main side effects.
parkinsomism and gynaecomastia.
3. It should not be used lactation. Though the amount secreted in milk is small, but suckling infant may develop loose motions, dystonia, myoclonus.
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USES
1. Antiemetic.
2. Gastrokinetic
3. Dyspepsia.
4. Gastroesophageal reflux disease.
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CISAPRIDE
1. cisapride-It is a prokinetic
3. Facilitates motility throughout g.i.t. including colon.
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4. Oral bioavailability of cisapride is ~33%.
5. Cisapride is a prokinetic drug without antidopaminergic side effects, but abdominal cramps and diarrhoea can occur.
6. Primary indication of cisapride has been GERD.
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5-HT3 ANTAGONISTS
Ondansetron
1-It controls cancer chemotherapy/radiotherapy induced vomiting .
2-highly effective in postoperative nausea and vomiting as well.
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Pharmacokinetics
Oral bioavailability of ondansetron is % due to first pass metabolism. .
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CARMINATIVES
These are drugs which promote the expulsion of gases from the . GIT and give a feeling of warmth and comfort in the epigastrium.
DIGESTANTS
These are substances intended to promote digestion of food. As appetite stimulants and health tonics.
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Q.1 Name three H2 Antihistaminic drugs?
A. Cimitidine, Ranitidine, Roxatidine, Loxatidine, Femotidine.
Q.2 Name three Proton pump inhibitor drugs?
A. Omeprazole, Lensoprazole, Pantoprazole, Robeprezole.
Q.3 Name two Anticholinergics used in treatment of Peptic ulcer?
A. Piranzepine, Oxypnenonium.
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Q.4 Name of two Prostaglandin Analogues used in Peptic ulcer?
A. Misoprosol, Enprostil, Rioprostil.
Q.5 Name two systemic Antacids?
A. Sodium bi carbonate, sodium citrate.
Q.6 What is Magaldrate?
A. Nonsystemic antacids.
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Q.7 Name one Ulcer healing Agents ?
A. Carbenoxolone sod .
Q.8 Name three drugs regime for H.pylori treatment ?
A. Tebacudine, Tenidacole, rnetrunidawle, Arnaxialin, claritnromvcin
Q.9 Name two side effects of cimetidine
A. Headache, dry mouth, rashes dizziness CMS effect conational state convulsion coma.
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Q.10 Name two Ulcer prote ctive drugs ?
A. Collidal Bismuth Subcitrate, Sucral Fate
Q11. Name five uses of H.Blockers ?
A. Tetracycline Tenedazole Amoxycylene
Q12. Name two drawbacks of Magnesium Antacids ?
A. Poorly absorbed, in soluble, diarhhoea
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Q13. Name two side effects of Aluminum Antacids ?
A. Weak & slowly reacting
Q14.Name two side effects of Colloidal Bismutli Sub citrate ?
A. Diarrhoea, dizyness, Headache
Q15. Name two contraindications of Emetics?
A. Acid Poisoning, CNS stimulant
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Q16. Name two emetics ?
A. Epomorphin
Q17. Name two Antichrolinergic ?
A. Hyoscine, dicyclomine
Q18. Name two Antihistaminic Anticmetic ?
A. Promethazine, cyclizine
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Q19. Name two Narcoleptics ?
A. Chlorpromazine, Haloparidol
Q20. Name two Prokinetic drugs ?
A. Metoclopramide, Domperidon
Q21. Name two 5HT3 Antagonists ?
A. Granisetrom, Ondancitron
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Q22. Name DOC of Motion sickness ?
A. Hyosine,
Q23. What is the mechanism of action of metoclopromide ?
A. D2 antogonism, 5HT4 & 5HT3 antogonism
Q24. DOC for chemotnerapy induced vomiting ?
A. Ondansetron.
Q25. Name two gall stone dissolving drugs ?
A. Chemodiol, Ursodiol
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