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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 1 CHAPTER 49 Acid-Controlling Agents NDEG 26 A Pharmacology I Eliza Rivera-Mitu, RN, MSN
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 2 Types of Acid-Controlling Agents Antacids H 2 antagonists Proton pump inhibitors
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 3 Acid-Related Pathophysiology The stomach secretes: Hydrochloric acid (HCl) Bicarbonate Pepsinogen Intrinsic factor Mucus Prostaglandins
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 4 Glands of the Stomach Cardiac Pyloric Gastric* *The cells of the gastric gland are the largest in number and of primary importance when discussing acid control
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 5 Cells of the Gastric Gland Parietal Chief Mucoid Endocrine Enterochromaffin
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 6 Cells of the Gastric Gland (cont'd) Parietal cells Produce and secrete HCl Primary site of action for many acid-controller drugs
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 7 Cells of the Gastric Gland (cont'd) Chief cells Secrete pepsinogen, a proenzyme Pepsinogen becomes pepsin when activated by exposure to acid Pepsin breaks down proteins (proteolytic)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 8 Cells of the Gastric Gland (cont'd) Mucoid cells Mucus-secreting cells (surface epithelial cells) Provide a protective mucous coat Protect against self-digestion by HCl
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 9 Hydrochloric Acid Secreted by the parietal cells when stimulated by food Maintains stomach at pH of 1 to 4 Secretion also stimulated by: –Large fatty meals –Excessive amounts of alcohol –Emotional stress
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 10 Acid-Related Diseases Caused by imbalance of the three cells of the gastric gland and their secretions Most common: hyperacidity Lay terms for overproduction of HCl by the parietal cells –indigestion, sour stomach, heartburn, acid stomach
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 11 Acid-Related Diseases (cont'd) PUD: peptic ulcer disease GERD: gastroesophageal reflux disease Helicobacter pylori (H. pylori) –Bacterium found in GI tract of 90% of patients with duodenal ulcers, and 70% of those with gastric ulcers –Antibiotics are used to eradicate H. pylori (tetracycline)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 12 Antacids: Mechanism of Action Promote gastric mucosal defense mechanisms Secretion of: –Mucus: protective barrier against HCl –Bicarbonate: helps buffer acidic properties of HCl –Prostaglandins: prevent activation of proton pump
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 13 Antacids: Mechanism of Action (cont'd) Antacids DO NOT prevent the overproduction of acid Antacids DO neutralize the acid once it’s in the stomach
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 14 Antacids: Drug Effects Reduction of pain associated with acid- related disorders Raising gastric pH from 1.3 to 1.6 neutralizes 50% of the gastric acid Raising gastric pH 1 point (1.3 to 2.3) neutralizes 90% of the gastric acid Reducing acidity reduces pain
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 15 Antacids OTC formulations available as: –Capsules and tablets –Powders –Chewable tablets –Suspensions –Effervescent granules and tablets
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 16 Antacids (cont'd) Used alone or in combination Aluminum salts Magnesium salts Calcium salts Sodium bicarbonate
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 17 Antacids: Aluminum Salts Forms: carbonate, hydroxide Have constipating effects Often used with magnesium to counteract constipation Examples –Aluminum carbonate: Basaljel –Hydroxide salt: AlternaGEL –Combination products (aluminum and magnesium): Gaviscon, Maalox, Mylanta, Di-Gel
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 18 Antacids: Magnesium Salts Forms: carbonate, hydroxide, oxide, trisilicate Commonly cause diarrhea; usually used with other agents to counteract this effect Dangerous when used with renal failure—the failing kidney cannot excrete extra magnesium, resulting in accumulation
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 19 Antacids: Magnesium Salts (cont'd) Examples –Hydroxide salt: magnesium hydroxide (MOM) –Carbonate salt: Gaviscon (also a combination product) –Combination products such as Maalox, Mylanta (aluminum and magnesium)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 20 Antacids: Calcium Salts Forms: many, but carbonate is most common May cause constipation Their use may result in kidney stones Long duration of acid action may cause increased gastric acid secretion (hyperacidity rebound) Often advertised as an extra source of dietary calcium –Example: Tums (calcium carbonate)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 21 Antacids: Sodium Bicarbonate Highly soluble Buffers the acidic properties of HCl Quick onset, but short duration May cause metabolic (systemic) alkalosis when used excessively Sodium content may cause problems in patients with HF, hypertension, or renal insufficiency
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 22 Antacids and Antiflatulents Antiflatulents: used to relieve the painful symptoms associated with gas Several agents are used to bind or alter intestinal gas and are often added to antacid combination products
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 23 Antacids and Antiflatulents (cont'd) OTC antiflatulents Activated charcoal Simethicone –Alters elasticity of mucus-coated bubbles, causing them to break –Used often, but there are limited data to support effectiveness
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 24 Antacids: Side Effects Minimal, and depend on the compound used Aluminum and calcium –Constipation Magnesium –Diarrhea Calcium carbonate –Produces gas and belching; often combined with simethicone
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 25 Antacids: Drug Interactions Adsorption of other drugs to antacids –Reduces the ability of the other drug to be absorbed into the body Chelation –Chemical binding, or inactivation, of another drug –Produces insoluble complexes –Result: reduced drug absorption
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 26 Antacids: Drug Interactions (cont'd) Increased stomach pH Increased absorption of basic drugs Decreased absorption of acidic drugs Increased urinary pH Increased excretion of acidic drugs Decreased excretion of basic drugs
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 27 Antacids: Nursing Implications Assess for allergies and preexisting conditions that may restrict the use of antacids, such as: –Fluid imbalances– Renal disease– HF –Pregnancy– GI obstruction Patients with HF or hypertension should use low-sodium antacids such as Riopan, Maalox, or Mylanta II
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 28 Antacids: Nursing Implications Use with caution with other medications due to the many drug interactions Most medications should be given 1 to 2 hours after giving an antacid Antacids may cause premature dissolving of enteric-coated medications, resulting in stomach upset
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 29 Antacids: Nursing Implications Be sure that chewable tablets are chewed thoroughly, and liquid forms are shaken well before giving Administer with at least 8 ounces of water to enhance absorption (except for the “rapid dissolve” forms) Caffeine, alcohol, harsh spices, and black pepper may aggravate the underlying GI condition
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 30 Antacids: Nursing Implications Monitor for side effects –Nausea, vomiting, abdominal pain, diarrhea –With calcium-containing products: constipation, acid rebound Monitor for therapeutic response –Notify heath care provider if symptoms are not relieved
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 31 Histamine Type 2 (H 2 ) Antagonists Reduce acid secretion All available OTC in lower dosage forms Most popular drugs for treatment of acid-related disorders –cimetidine (Tagamet)– nizatidine –famotidine (Pepcid) –ranitidine (Zantac)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 32 H 2 Antagonists: Mechanism of Action Block histamine (H 2 ) at the receptors of acid-producing parietal cells Production of hydrogen ions is reduced, resulting in decreased production of HCl
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 33 H 2 Antagonists: Drug Effect Suppressed acid secretion in the stomach
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 34 H 2 Antagonists: Indications GERD PUD Erosive esophagitis Adjunct therapy in control of upper GI bleeding Pathologic gastric hypersecretory conditions
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 35 H 2 Antagonists: Side Effects Overall, less than 3% incidence of side effects Cimetidine may induce impotence and gynecomastia May see: –Headaches, lethargy, confusion, diarrhea, urticaria, sweating, flushing, other effects
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 36 H 2 Antagonists: Drug Interactions cimetidine –Binds with P-450 microsomal oxidase system in the liver, resulting in inhibited oxidation of many drugs and increased drug levels –All H 2 antagonists may inhibit the absorption of drugs that require an acidic GI environment for absorption (Example: Ketoconazole)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 37 H 2 Antagonists: Drug Interactions (cont'd) SMOKING has been shown to decrease the effectiveness of H 2 blockers
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 38 H 2 Antagonists: Nursing Implications Assess for allergies and impaired renal or liver function Use with caution in patients who are confused, disoriented, or elderly Take 1 hour before or after antacids For intravenous doses, follow administration guidelines
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 39 Proton Pump The parietal cells release positive hydrogen ions (protons) during HCl production This process is called the “proton pump” H 2 blockers and antihistamines do not stop the action of this pump
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 40 Proton Pump Inhibitors: Mechanism of Action Irreversibly bind to H + /K + ATPase enzyme This bond prevents the movement of hydrogen ions from the parietal cell into the stomach Result: achlorhydria—ALL gastric acid secretion is blocked –In order to return to normal acid secretion, the parietal cell must synthesize new H + /K + ATPase
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 41 Proton Pump Inhibitors: Drug Effect Total inhibition of gastric acid secretion –lansoprazole (Prevacid) –omeprazole (Prilosec)* –rabeprazole (Aciphex) –pantoprazole (Protonix) –esomeprazole (Nexium) *The first in this new class of drugs
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 42 Proton Pump Inhibitors: Indications GERD maintenance therapy Erosive esophagitis Short-term treatment of active duodenal and benign gastric ulcers Zollinger-Ellison syndrome Treatment of H. pylori–induced ulcers; usually combined with antibiotic such as clarithromycin (Biaxin)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 43 Proton Pump Inhibitors: Side Effects Safe for short-term therapy Incidence low and uncommon
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 44 Proton Pump Inhibitors: Nursing Implications Assess for allergies and history of liver disease pantoprazole is the only proton pump inhibitor available for parenteral administration, and can be used for patients who are unable to take oral medications May increase serum levels of diazepam, phenytoin, and cause increased chance for bleeding with warfarin
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 45 Proton Pump Inhibitors: Nursing Implications Instruct the patient taking omeprazole: It should be taken before meals The capsule should be swallowed whole, not crushed, opened, or chewed It may be given with antacids Emphasize that the treatment will be short term
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 46 Other Drugs sucralfate (Carafate) misoprostol (Cytotec)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 47 sucralfate (Carafate) Cytoprotective agent Used for stress ulcers, erosions, PUD Attracted to and binds to the base of ulcers and erosions, forming a protective barrier over these areas Protects these areas from pepsin, which normally breaks down proteins (making ulcers worse)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 48 sucralfate (Carafate) (cont'd) Little absorption from the gut May cause constipation, nausea, and dry mouth May impair absorption of other drugs, especially tetracycline Binds with phosphate; may be used in chronic renal failure to reduce phosphate levels Do not administer with other medications
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 49 misoprostol (Cytotec) Synthetic prostaglandin analog Prostaglandins have cytoprotective activity –Protect gastric mucosa from injury by enhancing local production of mucus or bicarbonate –Promote local cell regeneration –Help to maintain mucosal blood flow
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 50 misoprostol (Cytotec) (cont'd) Used for prevention of NSAID-induced gastric ulcers Doses that are therapeutic enough to treat duodenal ulcers often produce abdominal cramps, diarrhea
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 51 CHAPTER 50 Antidiarrheals and Laxatives
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 52 Diarrhea Abnormal frequent passage of loose stools or Abnormal passage of stools with increased frequency, fluidity, and weight, or with increased stool water excretion
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 53 Diarrhea (cont'd) Acute diarrhea Sudden onset in a previously healthy person Lasts from 3 days to 2 weeks Self-limiting Resolves without sequelae
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 54 Diarrhea (cont'd) Chronic diarrhea Lasts for more than 3 weeks Associated with recurring passage of diarrheal stools, fever, loss of appetite, nausea, vomiting, weight loss, and chronic weakness
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 55 Causes of Diarrhea Acute Diarrhea Bacterial Viral Drug induced Nutritional Protozoal Chronic Diarrhea Tumors Diabetes Addison’s disease Hyperthyroidism Irritable bowel syndrome
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 56 Antidiarrheals: Mechanism of Action Adsorbents Coat the walls of the GI tract Bind to the causative bacteria or toxin, which is then eliminated through the stool Examples: bismuth subsalicylate (Pepto-Bismol), kaolin-pectin, activated charcoal, attapulgite (Kaopectate)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 57 Antidiarrheals: Mechanism of Action (cont'd) Anticholinergics Decrease intestinal muscle tone and peristalsis of GI tract Result: slowing the movement of fecal matter through the GI tract Examples: belladonna alkaloids (Donnatal), atropine (Lomotil), hyoscyamine
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 58 Antidiarrheals: Mechanism of Action (cont'd) Intestinal flora modifiers Bacterial cultures of Lactobacillus organisms work by: –Supplying missing bacteria to the GI tract –Suppressing the growth of diarrhea- causing bacteria Example: L. acidophilus (Lactinex)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 59 Antidiarrheals: Mechanism of Action (cont'd) Opiates Decrease bowel motility and relieve rectal spasms Decrease transit time through the bowel, allowing more time for water and electrolytes to be absorbed Examples: paregoric, opium tincture, codeine, loperamide (Imodium), diphenoxylate Although an opiate, dependence has not been reported
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 60 Antidiarrheal Agents: Side Effects Adsorbents Increased bleeding time Constipation, dark stools Confusion, twitching Hearing loss, tinnitus, metallic taste, blue gums
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 61 Antidiarrheal Agents: Side Effects (cont'd) Anticholinergics Urinary retention, hesitancy, impotence Headache, dizziness, confusion, anxiety, drowsiness Dry skin, rash, flushing Blurred vision, photophobia, increased intraocular pressure Hypotension, hypertension, bradycardia, tachycardia
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 62 Antidiarrheal Agents: Side Effects (cont'd) Opiates Drowsiness, sedation, dizziness, lethargy Nausea, vomiting, anorexia, constipation Respiratory depression Bradycardia, palpitations, hypotension Urinary retention Flushing, rash, urticaria
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 63 Antidiarrheal Agents: Interactions Adsorbents decrease the absorption of many agents, including digoxin (Lanoxin), clindamycin, quinidine, and hypoglycemic agents Adsorbents cause increased bleeding time when given with anticoagulants Antacids can decrease effects of anticholinergic antidiarrheal agents
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 64 Antidiarrheal Agents: Nursing Implications Obtain thorough history of bowel patterns, general state of health, and recent history of illness or dietary changes, and assess for allergies DO NOT give bismuth subsalicylate to children younger than age 16 or teenagers with chickenpox because of the risk of Reye’s syndrome
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 65 Antidiarrheal Agents: Nursing Implications Use adsorbents carefully in geriatric patients or those with decreased bleeding time, clotting disorders, recent bowel surgery, confusion Anticholinergics should not be administered to patients with a history of glaucoma, BPH, urinary retention, recent bladder surgery, cardiac problems, myasthenia gravis
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 66 Antidiarrheal Agents: Nursing Implications Teach patients to take medications exactly as prescribed and to be aware of their fluid intake and dietary changes Assess fluid volume status, I&O, and mucous membranes before, during, and after initiation of treatment
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 67 Antidiarrheal Agents: Nursing Implications Teach patients to notify their physician immediately if symptoms persist Monitor for therapeutic effect
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 68 Laxatives
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 69 Constipation Abnormally infrequent and difficult passage of feces through the lower GI tract Symptom, not a disease Disorder of movement through the colon and/or rectum Can be caused by a variety of diseases or drugs
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 70 Laxatives: Mechanism of Action Bulk forming Emollient Hyperosmotic Saline Stimulant
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 71 Laxatives: Mechanism of Action (cont'd) Bulk forming High fiber Absorbs water to increase bulk Distends bowel to initiate reflex bowel activity Examples: –psyllium (Metamucil) –methylcellulose (Citrucel) –polycarbophil
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 72 Laxatives: Mechanism of Action (cont'd) Emollient Stool softeners and lubricants Promote more water and fat in the stools Lubricate the fecal material and intestinal walls Examples: –Stool softeners: docusate salts (Colace, Surfak) –Lubricants: mineral oil
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 73 Laxatives: Mechanism of Action (cont'd) Hyperosmotic Increase fecal water content Result: bowel distention, increased peristalsis, and evacuation Examples: –polyethylene glycol (GoLYTELY) – Used before diagnostic or surgical bowel procedures –sorbitol –glycerin –lactulose (Chronulac)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 74 Laxatives: Mechanism of Action (cont'd) Saline Increase osmotic pressure within the intestinal tract, causing more water to enter the intestines Result: bowel distention, increased peristalsis, and evacuation
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 75 Laxatives: Mechanism of Action (cont'd) Saline laxative examples: –magnesium sulfate (Epsom salts) –magnesium hydroxide (MOM) –magnesium citrate –sodium phosphate (Fleet Phospho-Soda, Fleet enema)
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 76 Laxatives: Mechanism of Action (cont'd) Stimulant Increases peristalsis via intestinal nerve stimulation Examples: –castor oil –senna –cascara –bisacodyl
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 77 Laxatives: Indications Laxative Group Bulk forming Emollient Use Acute and chronic constipation Irritable bowel syndrome Diverticulosis Acute and chronic constipation Softening of fecal impaction; facilitation of BMs in anorectal conditions
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 78 Laxatives: Indications (cont'd) Laxative Group Hyperosmotic Saline Use Chronic constipation Diagnostic and surgical preps Constipation Diagnostic and surgical preps Removal of helminths and parasites
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 79 Laxatives: Indications (cont'd) Laxative Group Stimulant Use Acute constipation Diagnostic and surgical bowel preps
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 80 Laxatives: Side Effects Bulk forming –Impaction –Fluid overload Emollient –Skin rashes –Decreased absorption of fat-soluble vitamins A, D, E, & K Hyperosmotic –Abdominal bloating –Rectal irritation
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 81 Laxatives: Side Effects (cont'd) Saline –Magnesium toxicity (with renal insufficiency) –Cramping –Diarrhea –Increased thirst Stimulant –Nutrient malabsorption –Skin rashes –Gastric irritation –Rectal irritation –Can cause dependence if overused
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 82 Laxatives: Side Effects (cont'd) All laxatives can cause electrolyte imbalances!
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 83 Laxatives: Nursing Implications Obtain a thorough history of presenting symptoms, elimination patterns, and allergies Assess fluid and electrolytes before initiating therapy Patients should not take a laxative or cathartic if they are experiencing nausea, vomiting, and/or abdominal pain
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 84 Laxatives: Nursing Implications A healthy, high-fiber diet and increased fluid intake should be encouraged as an alternative to laxative use Long-term use of laxatives often results in decreased bowel tone and may lead to dependency All laxative tablets should be swallowed whole, not crushed or chewed, especially if enteric coated
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 85 Laxatives: Nursing Implications Patients should take all laxative tablets with 6 to 8 ounces of water Patients should take bulk-forming laxatives as directed by the manufacturer with at least 240 mL (8 ounces) of water
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 86 Laxatives: Nursing Implications Bisacodyl and cascara sagrada should be given with water due to interactions with milk, antacids, and H 2 blockers Patients should contact their physician if they experience severe abdominal pain, muscle weakness, cramps, and/or dizziness, which may indicate possible fluid or electrolyte loss
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 87 Laxatives: Nursing Implications Monitor for therapeutic effect
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 88 CHAPTER 51 Antiemetic and Antinausea Agents
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 89 Definitions Nausea –Unpleasant feeling that often precedes vomiting Emesis (vomiting) –Forcible emptying of gastric, and occasionally, intestinal contents Antiemetic agents –Used to relieve nausea and vomiting
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 90 VC and CTZ Vomiting center (VC) Chemoreceptor trigger zone (CTZ) –Both located in the brain –Once stimulated, cause the vomiting reflex
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 91 Table 51-1 Neurotransmitters involved in nausea and vomiting
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 92 Mechanism of Action Many different mechanisms of action Most work by blocking one of the vomiting pathways, thus blocking the stimulus that induces vomiting
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 93 Indications Specific indications vary per class of antiemetics General use: prevention and reduction of nausea and vomiting
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 94 Mechanism of Action and Indications Anticholinergic agents (ACh blockers) –Bind to and block acetylcholine (ACh) receptors in the inner ear labyrinth –Block transmission of nauseating stimuli to CTZ –Also block transmission of nauseating stimuli from the reticular formation to the VC –scopolamine –Also used as a transdermal patch for motion sickness
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 95 Mechanism of Action Antihistamine agents (H 1 receptor blockers) –Inhibit ACh by binding to H 1 receptors –Prevent cholinergic stimulation in vestibular and reticular areas, thus preventing N&V –dimenhydrinate, diphenhydramine, meclizine, promethazine –Also used for nonproductive cough, allergy symptoms, sedation
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 96 Mechanism of Action (cont'd) Neuroleptic agents –Block dopamine receptors on the CTZ –Chlorpromazine, perphenazine, triflupromazine, prochlorperazine (Compazine) –Also used for psychotic disorders, intractable hiccups
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 97 Mechanism of Action (cont'd) Prokinetic agents –Block dopamine in the CTZ –Cause CTZ to be desensitized to impulses it receives from the GI tract –Also stimulate peristalsis in GI tract, enhancing emptying of stomach contents –Metoclopramide (Reglan), cisapride –Also used for GERD, delayed gastric emptying
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 98 Mechanism of Action (cont'd) Serotonin blockers –Block serotonin receptors in the GI tract, CTZ, and VC –dolasetron, granisetron, ondansetron (Zofran) –Used for N&V for patients receiving chemotherapy and postoperative nausea and vomiting
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 99 Mechanism of Action (cont'd) Tetrahydrocannabinoids –Major psychoactive substance in marijuana –Inhibitory effects on reticular formation, thalamus, cerebral cortex –Alter mood and body’s perception of its surroundings
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 100 Mechanism of Action (cont'd) Tetrahydrocannabinoids (cont'd) –dronabinol (Marinol) –Used for N&V associated with chemotherapy, and anorexia associated with weight loss in AIDS patients
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 101 Side Effects Vary according to agent used Zofran = headache Stem from their nonselective blockade of various receptors
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 102 Nursing Implications Diphenidol hydrochloride, an antinausea agent used mainly for treatment of Meniere’s inner ear disease, should be administered with food, water, or milk to decrease GI upset and should not be used with alcohol or CNS depressants Scopolamine patches should be changed every 3 days
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 103 Nursing Implications Assess complete nausea and vomiting history, including precipitating factors Assess current medications Assess for contraindications and potential drug interactions
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 104 Nursing Implications Many of these agents cause severe drowsiness; warn patients about driving or performing any hazardous tasks Taking antiemetics with alcohol may cause severe CNS depression Teach patients to change position slowly to avoid hypotensive effects
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 105 Nursing Implications For chemotherapy, antiemetics are often given ½ to 3 hours before a chemotherapy agent Monitor for therapeutic effects Monitor for adverse effects
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Mosby items and derived items © 2005, 2002 by Mosby, Inc. 106 Nursing Implications Neuroleptic agents, such as Prochlorperazine (Compazine), if taken simultaneously with quinidine, may cause adverse cardiac effects Antihistamines, such as Meclizine, when taken with barbiturates, opioids, hypnotics, TCAs, and alcohol cause increased CNS depression
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