git drugs
TRANSCRIPT
GIT DRUGS-DR.AKIF A.B
STEP TO PG-MD/MS DR.AKIF A.B
PEPTIC ULCERDISEASE
STEP TO PG-MD/MS DR.AKIF A.B
H2 Receptor
M1Receptor
CCK2
Histamine A-ch Gastrin
G-Cell
Delta cell
Gastrin
ECL
+
+
+
Somatostatin
(-)
Activates H+ /K+ ATPase
HCl
Parietal cell
STEP TO PG-MD/MS DR.AKIF A.B
PROTON PUMPINHIBITORS
1) Most effective Antisecretory drug
2) Half life =30-120min
3) Duration of action = >24hrs
4) Even though PPIs have a short half life but their duration of action is more since they binds with receptors irreversibly and takes around 24hrs for new receptors to form. Thus these are known as Hit and Run Drugs
5) Should be given 30 minutes prior to taking food so that when food is ingested they should be available at the site of action.
STEP TO PG-MD/MS DR.AKIF A.B
PROTON PUMPINHIBITORS
Proton pump Inhibitors
PROTON PUMPINHIBITORS
DRUG FEATURESLansoprazole -PPI of choice in pregnancy
- Enzyme Inhibitor
Omeprazole - Both Enzyme inducer(CYP1A2) and Enzyme Inhibitor(CYP2C19)
PantoprazoleRabeprazole -most potent and fastest
acting.
STEP TO PG-MD/MS DR.AKIF A.B
PROTON PUMPINHIBITORS
-DOC in : 1) Peptic ulcer disease
2) Zollinger ELLison Sx
3) NSAIDs induced Ulcer
4) GERD
STEP TO PG-MD/MS DR.AKIF A.B
NSAIDs induced Ulcer-DOC = PPIs
-Most specific drug =Misoprostol
STEP TO PG-MD/MS DR.AKIF A.B
S/E of PROTON PUMPINHIBITORS
1) Acid is required for proper digestion of food. So when acid is decreased food is not digested properly and leads to:
1) Nausea
2) Flatulence
3) Constipation/ Diarrhoea
2) Pseudomembranous colitis :Decrease in acid leads to survival of bacterias and leads to infection.
3) Hypergastrinemia
STEP TO PG-MD/MS DR.AKIF A.B
Chronic S/E of PROTON PUMP INHIBITORS
-Decrease acid impairs absorption of calcium , Iron, Magnesium and Vitamin B12.
1)Osteoporosis
2)Anemia
3)Hypomagnesemia
STEP TO PG-MD/MS DR.AKIF A.B
DRUG INTERACTIONS OF PPIs
CYP2C9 enzyme activates clopidogrel
PPIs inhibits CYP2C9
Thus PPIs shouldn’t be combined with ClopidogrelSince it will decrease the activation of clopidogrelAnd its Antiaggregant effect.
PPIs + Clopidogrel
STEP TO PG-MD/MS DR.AKIF A.B
ENZYME INDUCERSG =Griseofulvin
P = Phenytoin
R = Rifampicin
S = Smoking
Cell = Carbamazepine
Phone = PhenobarbitoneSTEP TO PG-MD/MS DR.AKIF A.B
ENZYME INHIBITORSVitamin = Valproate
K =ketoconazole
Can = Cimetidine
Cause = Ciprofloxacin
Enzyme =Erythromycin
Inhibition =IsoniazidSTEP TO PG-MD/MS DR.AKIF A.B
1. Which of the following drugs is not used for H. pylori treatment? (LQ)
A Oxytetracycline
B Bismuth compounds
C Amoxicillin
D Mosapride
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Mosapride
Mosapride is a 5-HT4 agonist used in GERD. Rest of all drugs are used in H.Pylori
Drugs used against H. Pylori are:
1. Amoxicillin2. Clarithromycin3. Tetracycline4. Metronidazole /Tinidazole5. Bismuth subsalicylate6. Omeprazole/ LansoprazoleMonotherapy has failed in treatment of H. Pylori infections. Hence, multidrug regimens given for 7 -14 days are generally used.
STEP TO PG-MD/MS DR.AKIF A.B
Anti-H.pylori AgentsTriple Therapy Quadruple
therapyPPI OD PPI BD
Clarithromycin Metronidazole
Metronidazole or Amoxicillin or Tetracycline
Tetracycline
Bismuth Subsalicylate
- Given for 14days
STEP TO PG-MD/MS DR.AKIF A.B
2. All are antiemetic except (DNB Dec 2009)
A Domperidone
B Metoclopramide
C Cinnarizine
D Ondansetron
STEP TO PG-MD/MS DR.AKIF A.B
Ans. C Cinnarizine
Cinnarizine is used for treatment of vertigo.
STEP TO PG-MD/MS DR.AKIF A.B
Class of emetics Example
Anticholinergics Hyoscine, Dicyclomine
H1 antihistaminicsPromethazine, Diphenhydramine, Meclizine,Dimenhydrinate, Cyclizine,
Neuroleptics
Chlorpromazine, Prochlorperazine, Haloperidol,etc.
Prokinetic drugsMetoclopramide, Domperidone, Ciaspride, Mosapride
5-HT 3 antagonists Ondansetron, GranisetronSubstance-P/Neurokinin Receptor Antagonist (used inchemotherapy induced vomitting)
Aprepitant
Adjuvant antiemetics Dexamethasone, Benzodiazepines, Cannabinoids
STEP TO PG-MD/MS DR.AKIF A.B
3. Most potent anti-emetic is: (DNB June 2010)
A Ondansetron
B Granisetron
C Dolasetron
D Palonosetron
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Palonosetron
5HT3 antagonist potency sequence {Mnemonics: PGOD}: Palonosetron>Granisetron>Odansetron>Dolasetron
-5HT3 Receptor is present at CTZ area and its inhibition prevents vomiting
STEP TO PG-MD/MS DR.AKIF A.B
ANTI-EMETICS DOC
Type of vomiting DOC
Early onset chemotherapy Induced vomiting
Ondansetron
Late onset chemotherapy Induced vomiting
Aprepitant
Motion sickness Scopalamine >Hyoscine/Dicyclomine
Morning Sickness Pyridoxine + Doxylamine
STEP TO PG-MD/MS DR.AKIF A.B
4. We have two patients. One requires suppression of emesis caused by an anticancer drug that causes a high incidence and severity of vomiting (highly emetogenic drug). Another patient has severe diabetic gastroparesis and gastroesophageal reflux, which requires relief. Which one drug would be suitable for both indications (assuming no specific contraindications)? (LQ)
A Diphenoxylate
B Dronabinol
C Loperamide
D Metoclopramide
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Metoclopramide
a. Metoclopramide has clinically useful antiemetic and prokinetic actions and would be suitable for either of the patients described in the question.
b. The antiemetic effect arises from blockade of dopamine (and, probably, serotonin) receptors in the brain’s chemoreceptor trigger zone (CTZ).
c. The enhanced gastric and upper intestinal motility probably reflects an enhancement of the expected effects of ACh on muscarinic receptors found on longitudinal smooth muscle in the GI tract.
d. Metoclopramide raises the lower esophageal sphincter tone and relaxes the pyloric sphincter, which hastens gastric emptying.
e. This helps explain its beneficial effects in both gastroparesis and GERD. Importantly, the drug should not be given along with atropine because of its cholinergic properties.
STEP TO PG-MD/MS DR.AKIF A.B
PROKINETICS-Acts by stimulating A-ch which increases motility and peristalsis of GIT
-A-ch stimulates GI Motility
-Dopaminergic(D2) and serotonergic (5HT4) neurons acts by forming synapse with cholinergic neurons
-D2 is an Inhibitory neuron
-5HT4 is an stimulatory neuron.
-CCK and motilin are other receptors which increases GI motility
-Prokinetics acts by inhibiting D2 receptor and stimulating 5HT4, Motilin and CCK.
STEP TO PG-MD/MS DR.AKIF A.B
PROKINETICSD2 Antagonists 5HT4 agonists MotilinReceptor
Agonists
Metoclopromide Cispride Erythromycin
Domperidone Tegaserod
Levosulpiride Mosapride
Itopride
STEP TO PG-MD/MS DR.AKIF A.B
D2 Antagonists-Prokinetic effect
-Extra effects : 1) Antiemetic : Due to D2 antagonist effect at CTZ area
2) Increases Lower Esophageal Sphincter
3) Increases Gastric motility and emptying
4) Increases small intestinal motility
5) No effect on Large Intestine
STEP TO PG-MD/MS DR.AKIF A.B
METOCLOPROMIDE- Prokinetic agent
-D2 Antagonist
-Also 5HT3 antagonist and 5HT4 agonist
-Uses : 1) Gastroparesis : Since it increases Gastric motility
2) GERD : Since it increases LES pressure
3) Post op Ileus : Since it increases motility of small intestine
4) Hiccups
-It is lipid soluble drug. Hence easily crosses BBB and due to D2 Antagonism it causes Hyperprolactinemia, Extrapyramidal S/E.
STEP TO PG-MD/MS DR.AKIF A.B
DOMPERIDONE-Exclusively D2 receptor Antagonism
-Lipid insoluble drug. Hence doesn’t crosses BBB
-Doesn’t cause Hyperprolactinemia, Extrapyramidal S/E.
-Uses similar to Metoclopromide
STEP TO PG-MD/MS DR.AKIF A.B
5. A patient presents with severe abdominal pain. Endoscopy reveals several benign ulcers in the antral mucosa of the stomach. When therapy is started, which will provide the fastest relief of the discomfort with just a single dose? (AIPG 2010)
A Antacids
B Ranitidine
C Misoprostol
D Omeprazole
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Antacids
a. The typical symptoms of acid-peptic disease are caused by acid.
b. Although antacids seem to have no ability to accelerate ulcer healing, they act almost instantaneously to neutralize acid (provided adequate dosages are given), thereby relieving pain and other discomforts that are due to the acid in a matter of a minute or so.
c. All the other drugs can, to varying degrees, suppress gastric acid secretion and ultimately get the patient near or to a “no acid, no pain” state. However, it takes some time (variable, but clearly longer than it takes for an antacid to work) for other medications to be absorbed and reach blood levels sufficient to suppress acid production and then reduce symptoms.
STEP TO PG-MD/MS DR.AKIF A.B
ANTACIDSTraditional and obsolete Now being used
Calcium carbonate Combination of Aluminium and Magnesium salt
Sodium bicarbonate
- Calcium carbonate and Sodium bicarbonate is not being used due to risk of MILK-ALKALI Syndrome.
-Aluminium salts causes Constipation and Magnesium salts causes Diarrhoea. Hence both are combined to counteract their extra effects.
-Aluminium hydroxide is absolutely C.I in Renal failure
-Magnesium hydroxide can decrease absorption of fat soluble vitamins. Hence should be avoided in elderly patients.
STEP TO PG-MD/MS DR.AKIF A.B
MILK-ALKALI SYNDROMEALKALOSIS
+
HYPOCALCEMIA
+
RENAL FAILURE
STEP TO PG-MD/MS DR.AKIF A.B
6. Which of the following drug is not a gastrokinetic drug:
A Erythromycin
B Domperidone
C Cisapride
D Ampicillin
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Ampicillin
GASTROKINETIC DRUGS:Metoclopramide DomperidoneCisapride Erythromycin (via motilin receptors)
*Prokinetic drugs act by promoting gastric motility, increase gastric emptying, prevent the retention and reflux of gastric contents and thus provide symptomatic relief.
STEP TO PG-MD/MS DR.AKIF A.B
7. Misoprostol is a: (DNB June 2012)
A Prostaglandin E1 analogue B Prostaglandin E2 analogue C Prostaglandin antagonist D Antiprogestin
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Prostaglandin E1 analogue
Prostaglandin Analogues:MOAIt is a synthetic analogue of PGE1. It produces significant reduction of basal and food stimulated acid secretion. It is rapidly absorbed undergoes extensive first pass metabolism. Peak effect seen in 60 min and lasts for 3 hours.
INDICATIONThe primary use of PG analogue is in the prevention of NSAID associated gastrointestinal injury and blood loss. Especially in patients in which NSAIDS can not be stopped.
CONTRAINDICATIONInflammatory bowel disease
ADVERSE EFFECTSN/V, diarrhea, abdominal cramps. It can cause bleeding and abortion in pregnancy
STEP TO PG-MD/MS DR.AKIF A.B
NSAIDs induced Ulcer-DOC = PPIs
-Most specific drug =Misoprostol
STEP TO PG-MD/MS DR.AKIF A.B
8. Which one of the following drugs increases gastrointestinal motility? (LQ)
A Glycopyrrolate
B Atropine
C Neostigmine
D Fentanyl
STEP TO PG-MD/MS DR.AKIF A.B
Ans. C Neostigmine
Anticholinesterase drugs increase the level of ACh by protecting it from hydrolysis.Neostigmine is an anticholinesterase drug.
Fentanyl:a. It is an opioid analgesic which leads to constipation by:b. Direct action on GIT/CNS increases tone and segmentation but decreases propulsive movement.c. Spasm of pyloric / ileo-caecal and anal sphincters.d. Decrease in all GIT secretions.f. Central action causing inattention to defecation reflex.
Glycopyrrolate :a. Anticholinergic drug. Hence decreases Gastric motilityb. Potent anti secretoryc. Potent antibradycardia drugd. Lack of central actione. Used in preanesthetic medication
STEP TO PG-MD/MS DR.AKIF A.B
ANTICHOLINERGICSANTICHOLINERGICS IN PEPTIC ULCER DISEASE1) Pirenzepine2) Telenzepine
-Decreases Acid secretion by Inhibiting M1 Receptors
-Not being used much because of other better drugs.
STEP TO PG-MD/MS DR.AKIF A.B
9. Drug implicated for prolonging QT interval in a premature baby is: (AIIMS Nov 2010)
A Domperidone
B Metoclopramide
C Cisapride
D Omeprazole
STEP TO PG-MD/MS DR.AKIF A.B
Ans. C Cisapride
Drugs causing prolonged QT interval / Torsades de pointes
Antiarrhythmic
Antihistaminics
CYP 3A4 inhibitors
Others
QuinidineAmiodaroneProcainamideDisopyramide
TerfenadineAstemizole
KetoconazoleFluconazole
ImipramineAmitriptylineErythromycinHaloperidolCisapride
STEP TO PG-MD/MS DR.AKIF A.B
10. Which of the following is false regarding metoclopramide: (AIIMS May 2009)
A Extrapyramidal side effects
B Promotes gastric motility
C Milk secretion
D Stimulates chemo trigger zone
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Stimulates chemo trigger zone
b. It speeds gastric emptying by increasing gastric peristalsis and relaxing pylorus and first part of duodenum. It directly acts on CTZ and blocks it.
c. It is a dopamine (D2) receptor blocker and produces extrapyramidal side effects and hyperprolactinemia.
STEP TO PG-MD/MS DR.AKIF A.B
11) Dimethyl polysiloxane acts as: (LQ)
A Defoaming agent
B Local antacids
C Systemic antacids
D Ulcer healing agents
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Defoaming agent
Dimethyl Polysiloxane (Simethicone) is a silicon polymer, which reduces surface tension and collapses the froth (antifoaming agent).
It is not absorbed from intestine and is pharmacologically inert.
It reduces flatulence.
STEP TO PG-MD/MS DR.AKIF A.B
12) Proton pump inhibitors are most effective when: (LQ)
A Given after prolonged fasting B Along with an H2 blocker C Given with meals D Given before meals
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Given before meals ‘
Proton pump inhibitors are most effective when taken immediately before a meal, preferably with the morning meal.
STEP TO PG-MD/MS DR.AKIF A.B
PROTON PUMPINHIBITORS
1) Most effective Antisecretory drug
2) Half life =30-120min
3) Duration of action = >24hrs
4) Even though PPIs have a short half life but their duration of action is more since they binds with receptors irreversibly and takes around 24hrs for new receptors to form. Thus these are known as Hit and Run Drugs
5) Should be given 30 minutes prior to taking food so that when food is ingested they should be available at the site of action.
STEP TO PG-MD/MS DR.AKIF A.B
13. Ondansetron is a potent: (DNB Dec 2012) AAntiemeticBAnxiolytic CAnalgesicDAntidepressant
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Antiemetic
a. Ondansetron is a competitive, highly selective antagonist of 5-hydroxy tryptamine (serotonin) subtype-3 (5HT3) receptors.
b. Ondansetron is indicated for the prevention of nausea and vomiting associated with initial and repeat courses of moderately of highly emetogenic cancer chemotherapy, including high-dose cisplatin.
STEP TO PG-MD/MS DR.AKIF A.B
14. Which one of the following drugs has been shown to offer protection from gastric aspiration syndrome in a patient with symptoms of reflux? (LQ) A Ondansetron
B Metoclopramide
C Sodium citrate
D Atropine
STEP TO PG-MD/MS DR.AKIF A.B
Ans. B Metoclopramide
a. Metoclopramide has been used in patients with gastroesophageal reflux disease (GERD); it can produce symptomatic relief without necessarily promoting healing of associated esophagitis.
b. Metoclopramide is indicated more often in symptomatic patients with gastroparesis, in whom it may cause mild to moderate improvement in gastric emptying.
STEP TO PG-MD/MS DR.AKIF A.B
15. The two most common ingredients in over-the-counter antacid combination products are a magnesium salt and an aluminum salt. The rationale for this particular combination is that: (LQ) A. Al salts counteract the gastric mucosal-irritating effects of Mg salts
B. Al salts require activation by an Mg-dependent enzyme
C. Mg salts cause a diuresis that helps reduce systemic accumulation of the Al salt by increasing renal Al excretion
D. Mg salts tend to cause a laxative effect that counteracts the tendency of an Al salt to cause constipation
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Mg salts tend to cause a laxative effect that counteracts the tendency of an Al salt to cause constipation.
a. Magnesium salts used alone tend to cause a laxative effect. (Indeed, at dosages higher than those used for acid neutralization, magnesium salts are used for their laxative or cathartic effects.) Aluminum (and calcium) antacids, given alone, tend to cause constipation. Combining a magnesium salt with an aluminum (and/or calcium antacid) is an often successful approach to minimizing antacid-induced changes of net gut motility
STEP TO PG-MD/MS DR.AKIF A.B
16. A 55-year-old woman with insulin-dependent diabetes of 40 years' duration complains of severe bloating and abdominal distress, especially after meals. Evaluation is consistent with diabetic gastroparesis. The drug you would be most likely to recommend is (AIPG 2011) A.DocusateB.Dopamine C.LoperamideD.Metoclopramide E.Sucralfate
STEP TO PG-MD/MS DR.AKIF A.B
Ans. D Metoclopramide
Of the drugs listed, only metoclopramide is considered a prokinetic agent, i.e. one that increases propulsive motility in the gut.
STEP TO PG-MD/MS DR.AKIF A.B
METOCLOPROMIDE- Prokinetic agent
-D2 Antagonist
-Also 5HT3 antagonist and 5HT4 agonist
-Uses : 1) Gastroparesis : Since it increases Gastric motility
2) GERD : Since it increases LES pressure
3) Post op Ileus : Since it increases motility of small intestine
4) Hiccups
-It is lipid soluble drug. Hence easily crosses BBB and due to D2 Antagonism it causes Hyperprolactinemia, Extrapyramidal S/E.
STEP TO PG-MD/MS DR.AKIF A.B
17.A patient who must take verapamil for hypertension and angina has become severely constipated. Which of the following drugs would be most suitable as a cathartic? (LQ) AAluminum hydroxideBDiphenoxylate CMagnesium hydroxideDMetoclopramide EMineral oil
STEP TO PG-MD/MS DR.AKIF A.B
Ans. C) Magnesium hydroxide
A cathartic that mildly stimulates the gut would be most suitable in a patient taking a smooth muscle relaxant drug such as verapamil.
Magnesium hydroxide, by holding water in the intestine, provides additional bulk and stimulates increased contractions.
STEP TO PG-MD/MS DR.AKIF A.B
18. Your cousin is planning a three-week trip overseas and asks your advice regarding medications for traveler's diarrhea. A drug suitable for noninfectious diarrhea is AAluminum hydroxideBDiphenoxylate CMagnesium hydroxideDMetoclopramide EMineral oil
STEP TO PG-MD/MS DR.AKIF A.B
Ans. B Diphenoxylate Diphenoxylate and Ioperamide are the traditional traveler's antidiarrheal drugs.
Diphenoxylate requires a prescription in the USA but is less expensive than loperamide.
STEP TO PG-MD/MS DR.AKIF A.B
ANTI-DIARRHEA DRUGSOPIOIDS SOAMTOSTATIN
ANALOGSBILE ACID BINDING RESINS
Loperamide Octreotide Cholestyramine
Diphenoxylate Colesevalam
Colestipol
STEP TO PG-MD/MS DR.AKIF A.B
LOPERAMIDE-Opioid
-Mu receptor antagonist
-Decreases intestinal motility
-Increases anal sphincter pressure
-DOC in : 1) Irritable Bowel Sx
2) Ironitecan induced Diarrhea
-Also used in Traveller’s Diarrhea
-C.I : 1) Children <2yrs
2) Inflammatory Bowel Sx
STEP TO PG-MD/MS DR.AKIF A.B
OCTREOTIDE-Somatostatin analog
-Inhibits secretion of various hormones in GIT like Serotonin, Gastrin ,VIP etc. which leads to decrease GI Secretion and Motility.
-DOC in: HIV associated Diarrhea
-Other uses : 1) Secretory diarrhea
2) chemotherapy induced diarrhea
STEP TO PG-MD/MS DR.AKIF A.B
19. Which of the following drugs or drug groups is not useful in the prevention of nausea and vomiting induced by cancer chemotherapy (LQ) ADexamethasone BDronabinol CKetanserin DOndansetron EPhenothiazines
STEP TO PG-MD/MS DR.AKIF A.B
Ans. C Ketanserin
Ketanserin is an inhibitor of 5-HT 2 receptors and has no antiemetic action. All of the other drugs listed are useful in preventing chemotherapy-induced nausea and vomiting.
STEP TO PG-MD/MS DR.AKIF A.B
Class of emetics Example
Anticholinergics Hyoscine, Dicyclomine
H1 antihistaminicsPromethazine, Diphenhydramine, Meclizine,Dimenhydrinate, Cyclizine,
Neuroleptics
Chlorpromazine, Prochlorperazine, Haloperidol, Phenothiazinesetc.
Prokinetic drugsMetoclopramide, Domperidone, Ciaspride, Mosapride
5-HT 3 antagonists Ondansetron, GranisetronSubstance-P/Neurokinin Receptor Antagonist (used inchemotherapy induced vomitting)
Aprepitant
Adjuvant antiemetics Dexamethasone, Benzodiazepines,
Cannabinoids Dronabinol , Nabilone
20. On your way to an examination you experience that vulnerable feeling that an attack of diarrhea is imminent. If you stopped at a drugstore, you could buy this antidiarrheal drug without a prescription even though it is related chemically to the strong opioid-analgesic meperidine (AIPG 2009) AAluminum hydroxideBDiphenoxylate CLoperamideDMagnesium hydroxide EMetoclopramide
STEP TO PG-MD/MS DR.AKIF A.B
Ans. C Loperamide
a. Aluminum hydroxide is constipating but is not related chemically to meperidine; magnesium hydroxide is a strong laxative.
b. The two antidiarrheal drugs that are structurally related to opioids are diphenoxylate and loperamide.
c. Loperamide is available over-the-counter; diphenoxylate is mixed with atropine alkaloids, and the product (Lomotil, others) requires a prescription.
STEP TO PG-MD/MS DR.AKIF A.B
21. PPI with CYPP450 enzyme inhibiting activity (LQ) AOmeprazoleBRabeprazole CEsomeprazoleDPantoprazole
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Omeprazole
a. Omeprazole has maximum enzyme inhibiting action on CYPP450 among PPI. The drug can inhibit metabolism of warfarin and therefore can lead to bleeding. Pantoprazole is claimed to have lesser possibility of drug interactions and stable pharmacokinetics.
b. Rabeprazole has best 24 hours pain relief and the drug has marginally better efficacy than other proton pump inhibitors. Esomeprazole is an optical isomer of omeprazole
STEP TO PG-MD/MS DR.AKIF A.B
22) Which of the following drug is wrong about proton pump inhibitors (AIIMS Nov 2010)
APro-drugs BShort acting CLong acting DHigh first pass metabolism
STEP TO PG-MD/MS DR.AKIF A.B
Ans. B Short acting
a. These act by blocking the enzyme Na+K+ ATPase.
b. The drugs are well absorbed orally and in the apex of parietal canaliculi; these drugs get converted into their active moiety.
b. The drugs have high first pass metabolism. They form a covalent bond with their target. Perhaps, that is the reason of their long duration of action.
STEP TO PG-MD/MS DR.AKIF A.B
PROTON PUMPINHIBITORS
1) Most effective Antisecretory drug
2) Half life =30-120min
3) Duration of action = >24hrs
4) Even though PPIs have a short half life but their duration of action is more since they binds with receptors irreversibly and takes around 24hrs for new receptors to form. Thus these are known as Hit and Run Drugs
5) Should be given 30 minutes prior to taking food so that when food is ingested they should be available at the site of action.
STEP TO PG-MD/MS DR.AKIF A.B
S/E of PROTON PUMPINHIBITORS
1) Acid is required for proper digestion of food. So when acid is decreased food is not digested properly and leads to:
1) Nausea
2) Flatulence
3) Constipation/ Diarrhoea
2) Pseudomembranous colitis :Decrease in acid leads to survival of bacterias and leads to infection.
3) Hypergastrinemia
STEP TO PG-MD/MS DR.AKIF A.B
Chronic S/E of PROTON PUMP INHIBITORS
-Decrease acid impairs absorption of calcium , Iron, Magnesium and Vitamin B12.
1)Osteoporosis
2)Anemia
3)Hypomagnesemia
STEP TO PG-MD/MS DR.AKIF A.B
23. Drug used in irritable bowel syndrome with consti- pation is (AI 2012)
A Lubiprostone
B Loperamide
C Alosetron
D Clonidine
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Lubiprostone Lubiprostone acts by stimulating Cl channel opening in the intestine, increasing liquid secretion in gut and decreasing transit time, therefore used for chronic constipation.
It has also been approved for constipation dominant irritable bowel syndrome in women.
STEP TO PG-MD/MS DR.AKIF A.B
IRRITABLE BOWEL SYNDROME
Constipation Visceral painDiarrhea
Polyethylene Glycol
Loperamide
LubiprostoneAlosetron
Tricyclic Antidepressants
No response
No response
STEP TO PG-MD/MS DR.AKIF A.B
LAXATIVESProbiotics Bifidobacterium
SaccharomycesLactobacillus
Prebiotics Psyllium husk, bran, methyl cellulose
Symbiotics Combination of Pro and Prebiotics
Stimulants Bisacodyl, cascara , senna
Osmotic agents Lactulose, sorbitol, mannitol
Stool softeners Docusate sodium and calcium
Mineral oilsChloride secretory drugs Lubiprostone, Linaclotide
STEP TO PG-MD/MS DR.AKIF A.B
PROBIOTICS-Live organisms that provides benefit to health when taken in adequate amounts.
BifidobacteriumSaccharomycesLactobacillus
STEP TO PG-MD/MS DR.AKIF A.B
PREBIOTICS-Food ingredients that is composed of oligosaccharides, not digestable by humans, but has a beneficial effect on growth of organisms.
Psyllium husk
Bran
methyl cellulose
STEP TO PG-MD/MS DR.AKIF A.B
BRAN
STEP TO PG-MD/MS DR.AKIF A.B
STIMULANTSBisacodyl
cascara
senna
-These irritates colon by inducing inflammation and thus leads to water and solute accumulation.
-Takes 5-6hrs to act
-Absolutely C.I in Intestinal Obstruction
-Cascara and senna can cause Melanosis coli
STEP TO PG-MD/MS DR.AKIF A.B
OSMOTIC AGENTSLactulose
Sorbitol
mannitol
-These are non digestible sugars metabolised into short chain fatty acids which are Osmotic and draws water into intestinal lumen.
-Lactulose when metabolised into Short chain fatty acids makes intestinal pH acidic which turns ammonia into polar ammonium and facilitates its excretion. Hence used in Hepatic Encephalopathy.
STEP TO PG-MD/MS DR.AKIF A.B
STOOL SOFTENERS1) Docusate sodium and calcium ; These are surfactants and softens stools by decreasing Surface tension
2)Mineral oils : They directly enters stools and softens them.
STEP TO PG-MD/MS DR.AKIF A.B
26) Which of the following agents are useful in medical treatment of variceal bleeding? (AI 2011) AOctreotideBPantoprazole CSomatotropinDDexamethasone Flip
STEP TO PG-MD/MS DR.AKIF A.B
Ans. A Octreotide
Management of Variceal Bleeding
A. Prevention of re-bleeding· Non-selective beta blockers (e.g. propanolol)· Variceal band ligation
B. Management of acute bleed· Stabilize with fluids and blood· Octreotide· Vasopressin (Not preferred now)· Balioon tamponade:1. Sengstaken-Blackmore2. Minnesota Tube· Variceal ligation· Variceal sclerotherapy
STEP TO PG-MD/MS DR.AKIF A.B
SUCRALFATE-Made of Sucrose + Aluminium Hydroxide
-acid stimulates its cross linking which produces a polymer which covers the ulcer site
-Given on empty stomach before meals
-Antacids shouldn’t be given along with it since acid is required for its function. Thus a minimum of 30 minutes gap should be maintained between antacids and sucralfate.
-S/E : MC: Constipation
STEP TO PG-MD/MS DR.AKIF A.B
BISMUTH COMPOUNDSThese physically binds with ulcer and promotes mucin and bicarbonate production.
-Uses : 1) Anti H.pylori agent
2) Anti secretory hence used in Traveller’s diarrhea
-S/E : constipation and black discolration of tongue and stools
STEP TO PG-MD/MS DR.AKIF A.B
H2 BLOCKERS-Ranitidine
-Cimetidine = Shortest acting
-Famotidine = Longest acting
-DOC for Prophylaxis of Aspiration Pneumonia in patients undergoing Surgery.
- Maximum ulcer healing effect is seen after 8 weeks.
STEP TO PG-MD/MS DR.AKIF A.B
CIMETIDINE S/E1) Enzyme Inhibitor
2) Anti androgenic actions
3) Gynecomastia and impotence in males
4) Hyperprolactnemia
5) Galactorrhea in females
6) Tolerance
7) hepatotoxicity
STEP TO PG-MD/MS DR.AKIF A.B
CANNABINOID RECEPTORAGONISTS
-Dronabinol
-Nabilone
-Antiemetics
-S/E : Conjunctival congestion
STEP TO PG-MD/MS DR.AKIF A.B
Anti integrin drugs
Anti –TNF drugs +/-
Azathioprine
Mesalamine
Cyclosporine Azathioprine
Resistance Dependence
Steroids
MesalamineSevereMild/
Moderate
MaintenanceInduction
Ulcerative colitis
NR
NR
NR
STEP TO PG-MD/MS DR.AKIF A.B
Anti integrin drugs
Anti –TNF drugs +/-
AzathioprineSteroids
SevereMild/
Moderate
MaintenanceInduction
Crohn’s disease
Anti TNF@
NR
NR –No Response
STEP TO PG-MD/MS DR.AKIF A.B
STEP TO PG-MD/MS DR.AKIF A.B
STEP TO PG-MD/MS DR.AKIF A.B
ANTI-TNF @ DRUGS ANTI INTEGRIN DRUGS
Infliximab Netolizumab
Golimumab Vedolizumab
Certolizumab
Adalimumab
STEP TO PG-MD/MS DR.AKIF A.B
Condition DOCAcute bleeding gastric ulcer PPIs
Acute colonic pseudoobstruction (Ogilvie Sx)
Neostigmine
Aspiration pneumonia prophylaxis in surgical patients
H2 blockers
Dyspepsia PPIs
Gastrinoma PPIs
GERD PPIs
NSAID induced ulcer PPIs
Peptic ulcer disease PPIs
Zollinger ellison Sx PPIs
Stress ulcer PPIs
STEP TO PG-MD/MS DR.AKIF A.B
CONDITION DOC
GERD in pregnancy Antacids or sucralfate
Hemochromatosis Deferoxamine
Hiccups Chlorpromazine
HIV associated secretory diarrhea Octreotide
Irritable bowel Sx diarrhea Loperamide
Irritable bowel Sx constipation Polyethylene glycol
Whipples disease Cotrimoxazole
Xerostomia Cevimeline >pilocarpine
Wilson disease without heaptic decompensation or neuropsychiatric features
Zinc
With hepatic decompensation Zinc +Trientene
With neuropsychiatric features tetrathiomolybdate
STEP TO PG-MD/MS DR.AKIF A.B
STEP TO PG-MD/MS DR.AKIF A.B