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73 Cards in this Set
- Front
- Back
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What are drugs that control gastric acid secretion and treat peptic ulcer disease?
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Antacids
H2 receptor antagonists Proton pump inhibiots (PPI) Mucosal protective agents Helicobartor pylori Therapy |
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Prokinetics
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-Cholinomimetic agentsbethanechol
-Metoclopramide -Serotonin agonist (Cisapride,Tegaserod) -Macrolides (erythoromycin) -Ghrelin agonists |
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Drugs to treat constipation
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Stimulant laxatives
Bulk Forming Laxatives Stool Softeners Prokinetics Chloride Channel Activator |
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Antidiarrheal Drugs
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Diphenoxylate
Loperamine Kaolin and Pectin Bismuth Subsalicylate |
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Drugs to treate IBD
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Immunosuppressants
Salicylates azathioprine, mercaptopurine, cyclosporine |
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Drugs to treat IBS
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Anticholinergics (atropine like)
Alosteron Tegaserod |
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Antiemetic Drugs
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Ondanstron
H-1 Antihistamines Anticholinergics - scopolamine Benzo Cannabinoid Corticosteroids |
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Three modulators of gastric ATPase?
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Histamine, Acetylcholine, Gastrin - last two act thorough Ca2+, first cAMP
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Two endogenous agents that inhibit gastric acid secretion?
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Prostaglandins
Somatostatin |
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Patho of peptic ulceration
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breakdown of mucoal barrier
excess acid secretion Pepsin Drugs, NSAIDS |
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Breakdown of Mucoal barrier
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Alcohol
high salt concentration bile acids |
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Offensive forms that destory mucosal barrier
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Acid
Pepsin Bile Alcohol NSAIDS |
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Defensive protection of mucosal barrier
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Mucus
Bicarb protaglandins epithelial cell layer mucosal blood flow |
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Antacids
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neutralize HCL to form water and salt
generally large doses (7X/day) Basic compounds Mg, Al, Ca, Na hydroxide, carbonate, bicarb,citrate |
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Aluminum Compunds
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wide variability in solution
CONSTIPATION weak, binds phosphates decrease absorb of some drugs toxic in renal disease? |
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Calcium Compunds
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Rapid onset
CHALKY taste may lead to alkylosis decreases bioavalibility of some drugs |
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Magnesium Compounds
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Reacts promptly
POORly absorbed DIARRHEA + osmotic, increase in perstalsis of ENS decreases absorb of digoxin, prednison, tetracycline, cimtidine |
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Sodium Compunds
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Highly soluable
rapidly absorbed from gut systemic alkalosis, fluid retention not for LONG TERM |
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Theraputic Uses of Antiacids
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GU and DU
GERD prophylaxis of stress ulcers antidiarrheal agent, AL |
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Gastric ATPase Inhibitors (PPI)
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Final step in acid secretion, irreversibly inhibits gastric proton pump
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Omeprazole
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prodrug, concentrats in secreatory caniculli - non competitive binding - 10X as potent as cimetidine
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Cancer?
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Carcinoid gastric mucosa - rats
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Clinical uses
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GU, reflux esophagitis, Z-E syndrome (where gastrin levels are high, because of tumors which secrete)
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Hypergastrinemia
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if you block acid, gastrin levels rise and you get hyperplasia of mucosa wall
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Prostaglandins
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PGE - produced by gastric mucosa
Potent inhibitors of basal and nocturnal acid secretion "cytoprotective" |
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PGE
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stimulate Cl- secretion, increase mucous secretion, increase bicarb, increase blood flow
increases phospholipids |
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Misoprostol
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synthetic PGE, gastric antisecretory and mucosal properties
SE: diarrhea, uterine contractions Combined with NSAID to reduce GI toxicity |
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Sucralfate
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Coating agent - AL
binds to protein, inactivates pepsin, and allows crater to heal increase mucus and PGE prod REQUIRES ACID TO BE ACTIVE |
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Helocobacter pylori
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gram negative found in stomach
lives by creating alkaline environment infection causes GU/DU treat - 2 antibiotics, 1 PPI |
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GERD - Progression
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GERD with normal mucosa
Erythema of mucosa Erosions of mucosa Esophagitis Strictures Barrett's Esophagus |
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GERD - Causes
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Hiatal hernia (increase LES relax)
smoking, large meals, fatty, obesity Abnormal LES Delayed Emptying (Diabetics) |
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GERD - Symptoms
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Heartburn, regurgitation, Dysphagia, orodynophagia, non cardiac chest pain
Also: asthma, cough, hoarsness, vocal cord polyps, dental erosions |
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GERD - Treat
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step wise - behavioral changes (food)
Relieve symptoms - antacids etc Treat underlying motility disorder Mucosal Protection |
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Strictures
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narrowing of esophagal lumen
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Prokinetics
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drugs that augment GI tract motor activity
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Bethanechol - cholinergic agonists
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Stimulates uncoordinated motility
and gastric acid secretion SE:cramps, increased acid increase tone of LES |
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Metoclopramide - DA antagonist
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peripheral and central effects
promotes gastric emptying increased Ach release from post ganglionic no effect on ACID/Gastric secretion Central antiemetic action |
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Metoclopramide - clinical indications
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Upper GI motility disorders
Diabetic gastroparesis Reflux refractory to H2 blocker Facilitate passage of diag tools antiemetic, cancer chemotherapy pseudo-obstruction |
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Metoclopramide - SE
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common at theraputic doses
drowsiness, EPS (tardative dyskinesia Prolactin (galactorrhea, mentration) |
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Domperidone
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D2 antagonist, upper GI only
peripherally acting, enhances antroduodenal coordination |
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Domperidone - Clinical
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Upper Gi motility disorders
Diabetic Gastroparesis SE: hyperprolactin, no EPS |
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Cisapride - MOA
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5-HT3 antagonist, 5-HT4 agonist
augments ACH reslease peripherally enhances gastric acid clearance Coordinates gastric/duodental motil Limited antiemetic |
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Cispride - SE
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fatal ventricular arrythmias - no longer avalible
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Erythromycin (macrolides)
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motilin agonist
increase LES tone (useful in GERD) speeds up GI transit IV Admin |
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Erythromycin - Clinical/SE
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Clinical - diabetic gastroparesis
SE- abdominal cramping and diarrhea |
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Tegaserod -
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partial 5HT4 agonist/ 5HT2B antagonist
augments peristalsis, peripherally no central activity, no BBB similar efficacy as cisapride |
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Tegsaerod - SE
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cardiotoxicity, angina/heart attacks
women under 55 with consipation-IBS SE - diarrhea |
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Constipation
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dysmotility, dietary, congenital, cancer chemo, chronic laxative abuse, drug induced (opioid) metabolic, POI- post operative ileus
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Laxatives
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dietary fiber, bulk forming
saline and osmotic laxatives Irritatn or stimulant laxatives Stool softening - docustates |
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Bran, Psyllium
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dietary/bulk forming laxative
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Magnesium salts, lactulose, glycerin, sorbitol
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saline and osmotic lax
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Bisacodyl, phenophalein, senna, cascara, castor oil
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Irritant or stimulant laxatives
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docusates, colace
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stool softening
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Indication for laxatives
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Bed ridden parients
cardiovascualr disease, straining parients with hemorrhoids patients receiving morphine |
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Chloride Channel Activators
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Lubiprostone - C-IBS
selevtive CL activator, but not CFTR no effect on sodium/K in blood crypt cell Cl channels |
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Alvimopan
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postoperative ileus - IV
high number of myocardial infarctions |
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Methylnaltrexone
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opioid induced bowel dysfunction
sub-CT SE: abdominal pain.flatulence |
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Diarrhea
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infections/noninfections, toxins, parasites,malabsorption, food allergy, drug induced, mucosal defect (celiac disease), rapid gastric emptying, IBD, IBS
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Opioids
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diphenoxylate CNS and peripheral
Loperamine - peripherally |
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Anticholinergic agents
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Atropine like drugs, fell out of favor
scopolamine |
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Sympathetic agonists
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clonidine alpha 2
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Indications for antidiarrheals
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rapid gastric emptying
IBS infections diarrhea |
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IBD - autoimmunity
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chrons -transmural inflamm
ulcerative colitis - mucosal inflamm |
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Therapeutic
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corticoteroids
sulfasalasine, other 5-ASA, olsalazine, mesalamine infliximab - monoclonal directed at TNF cytotoxic, cyclosporin |
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Budesonide
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corticosteroid with decreased sideeffects
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IBS
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functional bowel disorder, NOT inflam
dyspepsia, non cardiac chest pain no structural/biochemical disorder more common in females |
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IBS symptoms
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abdominal pain, abnormal bowel habits, anxiety, stress, depression
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IBS - Therapy
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Anticholinergics, antispasmodics (dicyclomine, hyoscyamine
Serotonin |
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Alosetron
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5-HT3 receptor antagonist
restricted use - female IBS patients with diarrhea - IBS, rapidly absorbed, increases transit time SE: ischemic colitis, constipation |
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Tegaserod
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stated earlier, but this is used for IBS
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N and V
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infections, toxic, mechanical/pseudo obstruction, cancer chemo -5-HT3, sensory perception - motion sickness
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Theraputics N&V
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H1 receptor antagnoists - diphenhydramine
Metoclopramide - DA antag Corticosteroids - dexamethazone Cannabinoids Serotonin - ondansetron - 5HT3 antagnoist |
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Indications for usage
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motion sickness - scopolamine
Cancer chemo - serotonin 5HT3 antagnoists - effects enhanced by corticosteroids |
