GI * Flashcards
H pylori tx *
First line quadruple therapy - bismuth subsalicylate, metronidazole, tetracycline and PPI
Triple therapy- PPI with amoxicillin (metronidazole for PCN allergy) and clarithromycin
Usually antibiotic +H2/PPI + protective agent
H2 receptor antagonist*
Drugs-cimetidine (tagemet), famotidine (Pepcid), nizatidine (axid)
MOA- Histamine H2 receptor antagonist acts selectively on h2 receptors in the stomach without effects on h1 receptors they are competitive antagonist of histamine are fully reversible
Uses-PUD, heart burn, decreased since use of PPI
-PUD- all drugs equally effective for this disease, if NSAIDs induced should use PPI,
-stress ulcers-IV infusion associated in critical care settings
-GERD-decrease acid secretion may not relieve heart burn synths for up to 45 minutes
ADE-cimedtidine can have endocrine effects like gynecomastia and galactorrhea acts as a non steroidal antiandrogen, confusion, AMS in elderly in IV infusion
D-D interactions- may reduce efficacy of drugs that require an acidic environment for absorption, cimetidine inhibits several cytochrome P450 and interferes with warfarin, clopidogrel, phenytoin
Inhibitors of H/K ATPase proton pump *
Drugs- dexlansoprazole (Dexilant) esomeprazole (nexium) landoprazole( prevacid) omeprazole (prilosec) pantoprazole (protonix), rabeprazole (aciphex)
MOA- prodrug with an acid resistant enteric coating to protect them from premature degradation by gastric acid, inhibit both basal and stimulated gastric acid secretion by more than 90%
Uses- GERD, erosive esophagitiis, active duodenal ulcer, Zollinger-Ellison syndrome, reduce risk of bleeding ulcers by NSAIDs, stress ulcer prophylaxis, h pylori
Kinetics- take 30-60 minutes before breakfast or largest meal, dexlansoprazole is ER esomeprazole and pantoprazole are in IV form
ADE-increase risk of fractures, for greater than 1 year use, prolonged acid suppression, low vitamin b12, diarrhea, c.diff
D-D- clopidogrel-
Prostaglandins *
Drug- misoprostol (cytotec)
Produced by gastric mucosa
Inhibits secretin of acid and bicarbonate
Decrease in prostaglandins is thought to be a cause of PUD
Misoprostol is approved for Prevention of NSAIDs induced gastric ulcers, for those who have NSAIDs and are moderate to high risk for ulcers
Contradicted in pregnancy
Can cause diarrhea
Antacids*
Drugs- aluminum hydroxide, calcium carbonate (tums), magnesium hydroxide (milk of magnesia)
Weak bases that react with gastric acid and diminish gastric acidity, making water and salt
Efficacy depends on capacity to neutralize gastric HCL and if stomach is empty or full
Food delays stomach emptying allowing more time for antacid to react and prolong duration of action
Systemic absorption can cause metabolic alkalosis
Uses-PUD, GERD, heartburn
Administer after meals for optimal effectiveness
ADE-aluminum can cause constipation, magnesium can cause diarrhea, can cause issues in renal impaired patients, sodium based antacids can cause issues in HTN or CHF pts
Bismuth*
-bismuth subsalicylate (peptide bismol) uses- component of quadruple therapy for h pylori related ulcers, antimicrobial actions,
MOA- inhibits pepsin, increases secretion of mucus and interacts with glycoproteins in necrotic mucosal tissue to coat and protect ulcer
Contraindicated in pregnancy, coagulation disorder, GIB, renal impairment
ADE- Reye’s syndrome
bismuth subsalicylate (pepto bismol) can also be used for Prevention and treatment of travelers diarrhea
MOA- decreases fluid secretion in bowel
ADE- black tongue and black stools (salicylate content)
Phenothiazines *
Drugs-prochlorperazine
MOA-acts by blocking dopamine receptors in chemoreceptor trigger zone
Uses-effective for chemo induced NV or breakthrough NV
ADE-dose limited
5 HT3 receptor antagonist *
Drugs- dolasetron (anzemet), granisetron (sancuso, sustol), ondansetron (zofran), palanosetron (aloxi)
MOA- block 5 HT3 decors in peripheral and in central
Uses-CINV, superior efficacy and longer duration of action, palanosetron has longest half life so repeated dose not recommended, post operative NV
Dose adjustments in liver patients needed
ADE-prolong QT with high doses
Substance P/neurokinin 1 receptor antagonist *
Drugs- aprepitant, fosaprepiant (emend), netupitant, fosnetupitant (akynzeo), rolapitant (varubi)
MOA- targets neuokinin receptor in the vomiting center and blocks the action of substance P
Uses- highly or moderately emetogenic chemotherapy, usually administer with dexamethasone, and 5HT3 antagonist
Drug-drug- st johns wort, CYP3A4 metabolism and liver metabolism
ADE-fatigue, diarrhea, abd pain, hiccups
Corticosteroids *
Drugs-dexamethasone (decadron)
Used with mildly to moderately emetogenic chemo
Used in combo with 5 HT3 receptor anatomist or P/neuokinin 1 receptor for prevention of moderate to high CINV
MOA- ? Block prostaglandins
Second generation antipsychotics *
Drugs-olanzapine (zyprexa)
MOA-blocks 5 HT2 receptor, dopamine, histamine 1 and alpha 1 receptors
Used in prevention of CINV in combo with 5HT3 receptor antagonist (or PN1 receptor antagonist), and corticosteroids, for moderate to highly emetogenic chemo
Substituted benzamides *
Drugs- metoclopramide (reglan)
MOA- inhibits dopamine
Uses- high dose emetogenic like cisplatin, less effective compared to other agents, should be reserved for those with inadequate response to 5HT3 receptors antagonist or P/neurokinin receptor antagonist, for breakthrough NV, gastroparesis
ADE- extra pyramidal symptoms, limit long term high dose use
BLACK BOX WARNING FOR USE FOR MORE THAN 12 WEEKS DUE TO TARDIVE DYSKINESIA
Butyrophenones *
Drugs- droperidol, haloperidol (haldol)
MOA-block dopamine receptors
Uses- moderate CINV, breakthrough CINV, reserve for patients with NV post op or inadequate other agents
ADE- prolong QT
Benzodiazepines *
Drugs- alprazolam (Xanax), lorazepam (ativan )
Uses- low potency, beneficial effect may be sedative, anxiolytic, amnesia
Alcohol increase effects and CNS depression
Anti motility agents *
Drugs- diphenoxylate with atropine (lomotil) and loperamide (imodium)
MOA- analogs of meperidine and opioid like action in gut, activate pre synaptic opioid receptors and decrease peristalsis, at normal doses lack analgesic effects
Uses- diarrhea, travelers diarrhea
High doses and overuse of loperamide have been observed in patients trying to obtain euphoria or prevent withdrawal of opioids
BLACK BOX WARNING REGARDING IMPORTANCE OF FOLLOWING RECOMMENDED DOSAGES TO AVOID SEVERE ADE
Contraindications-active UC, young children due to respiratory depression, cardiac events, coma death
Patients with severe or infectious diarrhea should avoid as self treatment