Digestive Flashcards
True choleretics
Phenobarbital
Hydrocholeretics
Ox bile extract, dehydrocholica acid, cynalra scolimus
Choleretics
drug which stimulate production of bile by the liver
Cholagogues/cholecystokinetics
decrease biliary stasis by stimulating flow of bile into duodenum
Real cholagogues
magnesium sulphate, olive oil, sunflower oil, yolk
Hydrocholeretics and cholagogues are administered in
biliary dyskinesia (contraindicated in gallstones)
Phenobarbital
anticonvulsant and sedative-hypnotic induces CYP450 to decrease serum bilirubin, used in neonatal hyperbilirubinemia, cholestasis, CONTRAINDICATIONS respiratory problem, lactation period
Hydrocholeretics
increase volume of diluted bile, do not stimulate secretion of biliary constituents, excreted through bile they act by an osmotic mechanism, stimulate antitoxic function of liver (choleric and cholecystokinetic), laxative, spasmolytic, anti-inflammatory effects. INDICATIONS : acute/chronic cholecystitis, liver cirrhosis, constipation
Gallstones
cholesterol component, not soluble in water, poorly soluble in bile, precipitation of biliary salts in biliary cholesterol supersaturation, risk factors are female, fat, fair, forty, fertile, family. Modifying bile composition, drugs dissolve gallstones prevent precipitation and favor dissolving. Pharmacological/surgical treatment prevent complications
Ursodeoxycholic acid
Replaces endogenous biliary acids (hydrophobic) with hydrophilic and nontoxic ones, suppresses cholesterol secretion and inhibits intestinal absorption of cholesterol, bile acids used gradually to dissolve small stones, no influence on calcium. INDICATIONS: biliary lithiasis with cholesterol (radiotransparent, small gallstones), primary biliary cholangitis (delated liver transplant). ADVERSE EFFECTS diarrhea, skin rash, CONTRAINDICATIONS cholecystitis, obstruction of biliary tract, biliary contraction disorder, pregnancy first trimester/;actating. At least 6 (to 24) months of treatment, success rate 60% after 6 months but resurrect is common, expensive and reserved for those unfit for surgery
Bilichol
decrease endogenous production of cholesterol, prevents formation of gall stones, increases biliary flow and antispastic, inhibits HMG-CoA reductase, desaturates bile. I: biliary duct dyskinesia, cholecystitis, chlelythiasis; 1-2 camps. 3 times/day, before meal
Rowachol
almost like Bilichol, but only in cholelythiasis
Constipation
hard/dry stool in elderly, sedentary, pregnancy, hypothyroidism, (diverticulitis, colorectal cancer, hernia, hemorrhoids, anal fissues), neurological (Parkinson, multiple sclerosis, spinal lesion).
Drugs responsible for constipation
opioids, anticholinergics, tricyclic antidepressants, neuroleptics, antihistaminic, spasmolytics
Laxative administration
before initiation: rich fiber diet, 1,5 to 2L liquid, physical exercise, empty intestinal content before colonoscopy and surgical interventions, painful anal lesions, avoid vascular complications due to increased intra-abdominal pressure, food/drug intoxications
Result of laxatives
normal stool, usually after 8-12 hours, sometimes days, high doses have a purgative effect, only 5-10% absorbed from GI tract, locally through different mechanisms, forbidden in ileum, abdominal pain, without detected cause, acute intestinal diseases. Caution in pregnancy and lactation period.
Purgatives
eliminate intestinal content through semisolid first then liquid stool with latency of 2-6 hours
Misuse/chronic administration of lazatives
dependence (reduced peristalsis), hydroelectric imbalance (hypokalemia, hyponatremia with secondary hypoaldosteronism) hypokalemia more sever with loop diuretics, thiazides, glucocoticoids, amphotericin b
Bulk forming agents- fibers - plant based foods
methylcellulose, psyllium seeds
Hyperosmotic agents
polyethylene glycol (peg macrogol), lactulose, magnesium or sodium salts
Laxatives and Purgatives
bulk forming agents, hyper osmotic agents, stool softeners, stimulant agents, new laxatives
Stool softeners
docusate, mineral oil
Stimulant agents
Senna, bisacodyl, castor oil
New laxatives
prucaloprid, linaclotid, methynaltrexone
Methylcellulose, psyllium seeds
resist enzymatic digestion, work locally by absorbing water, swelling and increasing bulk of stool, stimulating peristalsis and defecation, latency 12-36 hours, I: constipation (main therapy), AE: abdominal cramps, flatulence (fermentation), risk of ileum (not enough liq) CI: intestinal atony, obstruction, immobility; no laxative dependence, may take a few days to act fully
Polyethylene Glycol (Macrogol)
not absorbed, local osmotic pressure retains water in colon, laxative effect at low doses and purgative at high doses; I: chronic constipation (predictable effect, directly related to dose and adm. of electrolytes, long administration possible), before colonoscopy/intestinal surgery; AE: flatulence(rare)
Lactulose
synthetic disaccharide (galactose +fructose) not absorbed, having laxative effect through osmosis, broken by colonic bacteria to lactic, acetic, and organic acids, decrease local pH, reduce ammonia absorption, beneficial effect in PT with liver disease (prevent encephalopathy); I: elderly, liver encephalopathy; AE: abdominal pain, flatulence, diarrhea
Sodium/Magnesium sulphate
decrease viscosity of feces by inc. water content; I: rare (before radiology/surgery, though enema (30 min latency) or oral (2-5 hour latency), Sodium sulphate (Glauber salt) was used before as purgative in intoxication but not anymore due to adm of activated charcoal, see adverse effects and contraindications in lecture
Docusate, mineral oil
stool softeners, lubricate and soften stool by adding water and fats, risk of lipid aspiration pneumonia
Irritant purgative agents
irritant action increases accumulation of water and electrolytes in lumen of colon and enhances peristalsis by local reflexes
Senna
irritant purgative, partially absorbed (risk of uterine contraction), passes in milk (diarrhea in baby), 8-10 hour latency, pro kinetic and secretory properties, laxative tea. I: constipation (second line, short adm.), AE: abdominal cramps (each dose), electrolyte imbalance, melanosis coli (reversible, no carcinoma risk), laxative dependence, dehydration, atony of bowel (chronic use), CI: pregnancy, lactation, obstruction
Bisacodyl
6-8 hours (oral) and 30-60 minutes (suppository), small doses decreases water abs in intestine, large doses increases water absorption in intestine; I: constipation (surgery, myocardial infarction, stroke), hemorrhoids, anal tissues, before diagnostic procedures; AE: abdominal pain (each dose), electrolyte imbalance, bowel atony (adm more than 1o days)
Castor Oil
riconoleic acid irritates small intestine mucosa, increasing peristalsis, latency 1-3 Hours, I:empty bower before surgery/diagnostic (not first choice); AE: bad taste, abdominal pain, diarrhea, hydroelectric imbalance; CI: obstruction, intoxication (increases absorption), pregnancy (uterine contraction)
Prucaloprid
new laxative, 5ht4 antagonist with pro kinetic effect; I: women with chronic constipation who do not respond to conventional laxatives (or intolerance)
Linaclotid
new laxative, agonist of guanitlcyclase C, stimulates intestinal secretion of water and chloride; I: irritable colon syndrome w/constipation, chronic constipation (small doses), well tolerated (no adv. effects)
Methylnaltrexone
new laxative, peripheral opioid antagonist, without inhibiting central analgesia, advantage over Naltrexone; I: constipation caused by opioids (palliative tmt.) AE: intestinal perforation (increased in association with chemotherapy)
Diarrhea
elimination of 3 or more semisolid/liquid stools per day, symptom, only treated if etiology isk know. Acute: self limiting read more
Symptomatic antidiarrheal drugs
Opioids (Opium, morphine, loperamide), Antidiarrheal microorganisms (saccharomyces boulardii), mucoprotecting agents (diosmectite), anticholinergic drugs (atropine)
Etiologic antidiarrheal drugs
Ciprofloxacin (C. jejune, Salmonella, shigella, v. cholerae), Metronidazole (C. difficile), Ampicillin (L. Monocytogenes), Vancomycin (S. aureus)
Opioids
reduce peristalsis, increase sphincter tone by stimulating opiod receptors in bowel, elimination of toxins/infectious factors inhibited (strict ind.), CI in ulcerous colitis/enterocolitis caused by antibiotics
Loperamide
opioid, well abs. oral, first hepatic passage with poor bioavailability, does not pass through BBB, no analgesic effect, no risk of dependence decrease in peristalsis allows absorptions of fluids and consolidation of stool. AE: constipation, CI: ileus, constipation, Children, diarrhea (w/fever/blood), ulcerous, pseudomembranous colitis.
Opium tincture
opioid, I: ileostomy, colonostomy; AE: high risk of dependence, CI: intestinal occlusion/subocclusion, ulcerous colitis, toxic dilation of colon.
Saccharomyces Boulardii
antidiarrheal microorganism, dried yeast, contains living microorganisms, forbidden with hot or cold drinks, bind to pathogenic bacteria (slows growth), decrease enterotoxic effects of E. coli and C. difficile, I: acute diarrhea, traveller’s diarrhea, AE: allergy, stool testing (false positive), CI: severe diarrhea, immunodepressed, children
Diosmectite
mucus protecting agent, natural aluminosilicate that increases viscosity and quantity of mucus layer and neutralizes pathogens (virus, bacteria, biliary salt, chemical agent); I: acute diarrhea, irritable bowel, well tolerated, even in children
Drugs for infl. bowel (ulcerative colitis, Crohn’s)
resolve acute episodes and prolong remissions, treatment also involves correction of any nutritional deficiency and surgery (complications)
Corticosteroids
anti-inflammatory drugs, act by inhibiting synthesis of prostaglandin and leukotriene, used systemically in severe acute attacks (prednisolone, hydrocortisone), locally (enema) for less severe acute attacks involving large bowel, maintenance therapy
Azathioprine, ciclosporin
anti-inflammatory, used occasionally
infliximab
anti-inflammatory, monoclonal antibody, inhibit action of inflammatory cytokine TNF-a, I: refractory Crohn’s, rheumatoid arthritis
Aminosalicylates Classification
Sulfasalazine (complex of suphonamide, sulfapyridine, 5-ASA); Mesalazine (5-ASA), Olsalazine (two molecules of 5-ASA)
Aminosalicylates
5-ASa is the active drug that blocks prostaglandins and leukotriene synthesis by inhibiting COX enzyme and lipooxygenase; I: ulcerative colitis, Crohn’s disease, rheumatoid arthritis, see adverse effects, can be adm orally, rectally, enema
gastric ulcers
read in lecture
Antiaggressive drugs - Antacids
Aluminium salts, magnesium salts, calcium salts, sodium salts
Antisecretory drugs - Histamine receptor antagonists
Cimetidine, ranitidine, famotidine, nizatidine, roxatidine
Antisecretory drugs - Proton pump inhibitors
Omeprazole, lansoprazole, esomeprazole, pantoprazole, rabeprazole
Antisecretory drugs - Anticholinergic drugs
pyrenzepine
Antisecretory drugs - prostaglandin agonists
misoprostol
Protective drugs - coating agents
bismuth salts, sucralfate
Antihelicobacter pylori drugs - Antibiotics
amoxicillin, clarithromycin, tetracycline
Anti H.pylori chemotherapeutics
metronidazole, tinidazole, furazolidone
Anti H.pylori protective drugs
bismuth salts
Anti H. Pylori antisecretory drugs
omeprazole, lansoprazole, esomeprazole, pantoprazole, rabeprazole
Antacids
read more
Aluminium and magnesium salts
aluminum compounds cause constipation, magnesium compounds cause diarrhea, toxicity can occur in patients with renal failure.
Sodium bicarbonate
dyspepsia, not recommended because it can cause systemic alkalosis in large amounts
histamine receptor agonists
read
Cimetidine
read
Ranitidine, famotidine, nizatidine
No CNS effects, no inhibition of drug metabolism, no antiandrogenic effect
Proton pump r
read
pyrenzipine
read
Misoprostol
read
Coating agents
increase protection of mucosa, form protective coating over ulcer crater allowing healing underneath, stimulate local prostaglandin release
Bismuth salts
only oral, minimum absorption and local effect, protection of mucosa, activity against H. Pylori, I: duodenal ulcer, GORD, diarrhea; AE: metallic taste, black stool, ecephalopathy
Sucralfate
read
Treatment against H pylori
read
Antiemetic drugs - dopamine receptor antagonists - substituted benzamides
metoclopramide
Antiemetic - dra - benzimidazol derivative
domperidon
Antiemetic - dra - phenothiazines
prochroperazine, thiethylperazine
Antiemetic - dra - butirophenone
droperidol, haloperidol
Antiemetic - antihistamine H1
dimenhydrinat, hydroxyzine, meclisine, promethazine
Antiemetic - anticholinergic drugs
scopalamine
Antiemetic - 5ht3 receptor antagonists
granisetron,ondansetron,tropisetron,palonosetron
Antiemetic - canabinoid
nabilone, dronabinol, cannbidiol
Antiemetic - neurokinin 1 antagonists
aprepitant, fosaprepitant
Metoclopramide
read
Domperidon
similar to metoclopramide but less likely to cause extrapyramidal
Prochlorperazine
read
Droperidol
temporarily withdrawn from market in 2008 because of severe CV side effects (arrhythmia, cardiac arrest)
Antihistamines H1
act on H1 receptors in vomiting center, weak anticholinergic and sedating effect; I: motion sickness, vestibular disease (inappropriate in elderly); AE: sedation, atropine effects
Scopalamine
anticholinergic, act on vomiting center and GI tract directly; I: motion sickness, AE: dry mouth, confusion, fatigue, agitation, one patch applied to hairless area of skin behind ear 5-6 hours before travel, can prevent sickness for up to 3 days
5HT3 receptor antagonists
block serotonin receptors in CNS and digestive; I: severe nausea and vomitting after chemotherapy, radiotherapy, postoperatively; AE: constipation, headache, in cases where other drugs ineffective
Canabinoids
act on CB1 distributed through CNS and PNS, also in enterochromfinlike cells and vagus; I: control delayed chemotherapy - induced nausea and vomiting, superiority compared to DOPA antagonists
Neurokinin 1 Antagonist
aprepitant is a selective human substance P and NK1 receptor antagonist that inhibits chemotherapy induced nausea and vomiting centrally in chemoreceptor trigger zone, antidepressant, anxiolytic; I: prophylaxis of acute and delayed phases of chemotherapy induced nausea and vomiting; AE: loss of appetite, headache , administered together with glucocorticoid and a 5ht3 receptor antagonist,