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pathopharm exam 4


GI Drugs Antiemetics Antidiarrheals Drugs for irritable bowel syndrome Drugs for inflammatory bowel disease
Antiemetics ARE? Many antiemetics interact with one or more of the receptors suppress nausea and vomiting Emetic response Complex reflex that occurs after activation of vomiting center in the medulla oblongata receptors SEROTONIN, glucocorticoids, substance P, neurokinin1, dopamine, acetylcholine, histamine
Serotonin receptor antagonists ? •Blocks type 3 serotonin receptors on afferent vagal nerve •More effective when used with dexamethasone Ondansetron [Zofran] 1ST APPROVED chemotherapy-induced nausea and vomiting (CINV) •prevent nausea and vomiting DUE TO radiotherapy and anesthesia ADR= Headache, diarrhea, dizziness, prolonged QT interval, risk of torsades de pointes
Glucocorticoids Unknown mechanism of action (MOA) as antiemetic Dexamethasone Commonly used to suppress CINV; however, this is not an application approved by the U.S. Food and Drug Administration (FDA) Effective alone and in combination with antiemetics
Benzodiazepines? Lorazepam [Ativan] Used in combination regimens to suppress CINV Three primary benefits: •Sedation •Suppression of anticipatory emesis •Production of anterograde amnesia
Dopamine antagonists Phenothiazines: Prochlorperazine Block dopamine2 receptors in CTZ •Surgery, cancer, chemotherapy, and toxins •Side effects Extrapyramidal reactions Anticholinergic effects Hypotension and sedation
Cannabinoids Dronabinol [Marinol] Related to marijuanaCINV MOA with emesis unclear Potential for abuse and psychotomimetic effects
Management of Chemotherapy-Induced Nausea and Vomiting Three types of emesis: Anticipatory •Occurs before drugs are given Acute •Onset within minutes to a few hours Delayed •Onset 1 day or longer after drug administration
Management of Chemotherapy-Induced Nausea and Vomiting Antiemetics are more effective in preventing CINV than in suppressing CINV in progress Give before chemotherapy drugs Monotherapy and combination therapy may be needed
Nausea and Vomiting of Pregnancy First-line therapy consists of a two-drug combination: Doxylamine plus vitamin B6 Hyperemesis gravidarum: Dehydration, ketonuria, hypokalemia, and loss of 5% or more of body weight Nondrug measures
LAST-LINE OF DEFENSE Prochlorperazine, metoclopramide, and ondansetron; methylprednisolone may be tried as a last resort, but only after 10 weeks’ gestation-acupuncture, ginger, snacks
Drugs for Motion Sickness Scopolamine Muscarinic antagonist Patch goes behind the ear Side effects•Dry mouth•Blurred vision•Drowsiness
Drugs for Motion Sickness S/E-Sedation (H1 receptor blocking) •Dry mouth, blurred vision, urinary retention, constipation (muscarinic receptor blocking) Antihistamines Dimenhydrinate, meclizine, cyclizine Considered anticholinergics; block receptors for acetylcholine and histaminE
Diarrhea Characterized by stools of excessive volume and fluidity and increased frequency of defecationSymptom of GI disease Causes-Infection, maldigestion, inflammation, functional disorders of the bowel Complications Dehydration and electrolyte depletion
Diarrhea Management Diagnosis and treatment of underlying disease Replacement of lost water and salts Relief of crampingReducing passage of unformed stools Two major groups of antidiarrheals Specific antidiarrheal drugs Nonspecific antidiarrheal drugs
Nonspecific Antidiarrheal Agents Most commonly used: Diphenoxylate [Lomotil] and loperamide [Imodium] •Decrease secretion of fluid into small intestine and increase absorption of fluid and salt Opioids Most effective antidiarrheal agents Activate opioid receptors in GI tract •Reduce intestinal motility •Slow intestinal transit• Allow more fluid to be absorbed
Diphenoxylate [Lomotil] Formulated with atropine to discourage abuse •Opioid used only for diarrhea •High doses can elicit typical morphine-like subjective responses
Loperamide [Imodium] Structural analog of meperidine •Used to treat diarrhea and to reduce the volume of discharge from ileostomies •Little or no potential for abuse
Management of Infectious Diarrhea Many cases require no treatment Variety of bacteria and protozoa can be responsible Infections are usually self-limited Antibiotics should be used only when clearly indicated: Salmonella, Shigella, Campylobacter, or Clostridium infectionsTraveler’s diarrheaEscherichia coli: Usually self-limitingCiprofloxacin, norfloxacin
Irritable Bowel Syndrome (IBS) Most common disorder of GI tract Affects 20% of Americans Incidence in women is 3 times higher than in men Characterized by cramping abdominal pain (may be severe) that cannot be explained by structural or chemical abnormalities
Irritable Bowel Syndrome (IBS) American College of Gastroenterology has concluded there is no proof of clinical benefit for most of these agents: May occur with diarrhea, constipation, or bothConsidered IBS when symptoms have been present for 12 weeks over the past year Four groups of drugs historically used Antispasmodics •Bulk-forming agents •Antidiarrheals •Tricyclic antidepressants
IBS-Specific Drugs Alosetron [Lotronex] For Diarrhea-predominant IBS Potentially hazardous drug; approved for women only GI toxicities can cause complicated constipation, leading to perforation and ischemic colitis Risk management programDrug interactions
IBS-Specific Drugs Lubiprostone [Amitiza] Approved for constipation-predominant IBS (IBS-C) in women age 18 years or olderModest benefits
nflammatory Bowel Disease (IBD) Caused by exaggerated immune response to normal bowel flora Crohn’s disease Usually affects terminal ileum (can affect all parts of GI tract) Ulcerative colitis Inflammation of the mucosa and submucosa of the colon and rectumMay cause rectal bleeding May require hospitalization
Drugs for IBD Not curative; may control disease process 5-Aminosalicylates (sulfasalazine) Glucocorticoids (budesonide) Immunosuppressants/Immunomodulators(mercaptopurine/infliximab)
5-Aminosalicylates Sulfasalazine [Azulfidine] 5-ASA reduces inflammation; it also suppresses prostaglandin synthesis and migration of inflammatory cells into affected region Most effective against acute episodes of mild to moderate ulcerative colitisAdverse effects
Glucocorticoids Budesonide mild to moderate Crohn’s disease that involves the ileum and ascending colonProlonged use of glucocorticoids can cause severe : ADR= adrenal suppression, osteoporosis, increased susceptibility to infection, and a cushingoid syndrome
Immunosuppressants Reserved for patients who have not responded to traditional therapy Azathioprine [Imuran] and mercaptopurine [Purinethol] Induce and maintain remission in both ulcerative colitis and Crohn’s disease Onset of effects may be delayed for up to 6 monthsADR= pancreatitis and neutropenia
A patient is experiencing chemotherapy-induced nausea. Which prescribed medication would be most effective for this patient? Ondansetron is a serotonin receptor antagonist and is the most effective drug available for suppressing nausea and vomiting caused by chemotherapy.
A patient with irritable bowel syndrome is prescribed alosetron [Lotronex]. Before this drug is administered, it is most important for the nurse to do what? Ask the patient about any problems with constipation. Patients should not take alosetron if constipation develops. Impaction, bowel obstruction, and perforation can occur.
Created by: Seka_nurse
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