Pharm Section 12

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Prostaglandins: indications

Affect GI motility and gastric secretions - reduce complications from NSAID ulcers Can be taken in conjunction with NSAIDS to prevent ulcers

Risk factors for reflux and heartburn (pyrosis) include:

Alcohol Hiatal hernia (part of the stomach moves above the diaphragm) Obesity Pregnancy Scleroderma Smoking

Doug is 78-years-old and complains about not have a daily bowel movement. What do you tell him about laxative use?

Answer: Laxatives should only occasionally be used for constipation. You should find out more about what is causing constipation: New medication? Change in exercise or diet? Other symptoms? Some older people feel that they should have a daily BM; however, it is not necessary if they do not feel constipated. If Doug is taking an opioid or anticholinergic or TCA, he may experience constipation and a stool softener or bulk-forming agent may be necessary. But also teach him about the need to eat a high fiber diet, drink plenty of liquids, and exercise routinely.

Bulk-Forming Laxatives:

Bulk-forming agents used to treat constipation contain plant matter that absorbs water and softens the stool.

Continue your review of treatment of H. pylori-induced peptic ulcers. Triple therapy for eradication of H. pylori may include _________

2 antibiotics that are effective against the bacteria (selected from tetracyclines, amoxicillin, metronidazole) and colloidal bismuth.

Osmotic Laxatives: patient tips

Can take 24-48 hours for results since they will not work until they reach the colon. Do not take another dose or other laxative while waiting for effects. Eat a high-fiber diet, eat regularly, get regular exercise, and drink 8 glasses (8 oz) of water daily

Prostaglandins: contraindications and interactions

Cannot be used in pregnant women (may induce labor) or lactating women

Stool Softeners: indications

For ease of bowel movements, and prophylactically for those who should avoid straining.

The majority of both gastric and duodenal ulcers is caused by ______.

H. pylori

proton Pump Inhibitors (PPI): adverse effects/warnings

Headache, dizziness, fatigue, abdominal pain, rash Rare - hematuria

proton Pump Inhibitors (PPI): mechanism of action

Hydrogen ions (protons) in parietal cells are necessary for hydrochloric acid formation. These drugs block the enzymes that produce hydrochloric acid - antisecretory action.

What Are the Common Drug Actions for GI Disorders?

Increase or decrease function of GI tract ---Change muscle tone ---Change secretions Increase or decrease emptying time ---Delay emptying of the stomach ---Change rate of peristalsis Replace enzyme deficiencies.

Prostaglandins: mechanism of action

Inhibit gastric acid and gastrin production; stimulates mucin release and secretion of bicarbonate - antisecretory action

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: indications

Irritable and inflammatory bowel disease

Antiemetics: mechanism of action

Largely unknown, but thought to relax brain center responsible for muscles used in vomiting Prokinetic agents - increase gastric motility

Among the most misused gastrointestinal drugs are ___.

Laxatives are among the most misused drugs to treat constipation or, in many cases, "perceived" constipation.

Drugs used to treat constipation include bulk-forming agents and the stimulants and cathartics. Osmotic or stimulant laxatives are considered first-line therapy for chronic constipation. Prokinetics and secretagogues are the next step when osmotics or stimulants do not control chronic constipation.

Laxatives can also be useful in patients with irritable bowel syndrome, constipation , and opioid-induced constipation.

Recommendations for Correct Use of Antacids:

Liquid antacids should be shaken well before pouring the dose. Do not drink any liquids after taking the liquid antacid so as not to dilute the medication. Chewable tablets should be chewed thoroughly followed by a glass of water or milk to increase absorption. Antacids are not indicated for long-term use, but for the relief of acute symptoms of pyrosis. If symptoms continue, then further evaluation and diagnosis of underlying cause should be done to identify more appropriate treatment. Chronic use of antacids produces acid rebound so that the person may experience increased gastric acid production and pyrosis.

Laxative Stimulants: patient tips

Chronic use causes dependence by disrupting normal reflex activity of colon and rectum Eat a high fiber diet, eat regularly, get regular exercise, drink 8 glasses (8 oz) of water daily

________ enters the duodenum and mixes with bile and pancreatic juices. These substances are secreted by the liver and pancreas, respectively, into the small intestine to help digest fats and carbohydrates.

Chyme

Stool Softeners: mechanism of action

Detergent like properties retain water in stool - these can take several days to work

Vomiting is controlled by the medulla and mediated by serotonin, dopamine, and acetylcholine.

Dopamine antagonists and anticholinergics or antihistamines are frequently used to treat nausea, vomiting and motion sickness.

Antiemetics: LIST OF DRUGS/ROUTE OF ADMINISTRATION

Dopamine antagonists: haloperidol (Haldol) - PO, chlorpromazine (Thorazine) - PO, IM, IV, perphenazine (Perphenazine Tablets) - PO, prochlorperazine (Compazine) - PO IM IV rectal, promethazine (Phenergan) - PO IM IV rectal, thiethylperazine (Torecan) - PO IM rectal Antihistamines: dimenhydrinate (Dramamine) - PO IM IV, diphenhydramine (Benadryl) - PO IM IV, hydroxyzine (Atarax, Vistaril) - PO IM, and meclizine (Antivert) - PO Anticholinergics: scopolamine (Transderm-Scop) - transdermal, trimethobenzamide (Tigan) - PO, rectal Prokinetic agents - metoclopramide (Reglan) - PO IM rectal Serotonin Receptor Antagonists - granisetron (Kytril) - PO IV, ondansetron (Zofran) - PO IV

Stool Softeners: adverse effects and warnings

Mild abdominal cramps, diarrhea, nausea, bitter taste

Bulk-Forming Laxatives: patient tips

Some contain sodium and natural sugars and/or artificial sweeteners - can interfere with individuals on low-sodium or low-calorie diet Can cause appetite suppression

Many people will have diarrhea once or twice each year. It typically lasts two to three days and can be treated with OTC medicines.

Some people have diarrhea more often because of irritable bowel syndrome or other chronic diseases of the large intestine.

Antidiarrheals: indications

Treatment of diarrhea

________ is a disease of the colon that includes characteristic ulcers. The main symptom of active disease is usually constant diarrhea mixed with blood, of gradual onset.

Ulcerative colitis (Colitis ulcerosa, UC)

Antacids LIST OF DRUGS/ROUTE OF ADMINISTRATION

aluminum hydroxide (Amphojel), magnesium hydroxide (Milk of Magnesia), magnesium hydroxide or aluminum hydroxide +simethicone (Maalox Plus), calcium carbonate (Tums, Titralac), sodium bicarbonate (aka baking soda - Alka-Seltzer)

Bulk-Forming Laxatives: LIST OF NAMES/ROUTE OF ADMINISTRATION

calcium polycarbophil (FiberCon, Mitrolan) PO psyllium hydrophilic mucilloid (Metamucil) PO

The GI system begins with the mouth and ends at the anus. The process of digestion is the act of _________

converting food into chemical substances that are used by the body.

If this sphincter muscle doesn't close well, food, liquid, and stomach acid can leak back into the esophagus. This is called reflux or gastroesophageal reflux. Reflux may just cause symptoms, or it can _________

damage the esophagus

According to the Mayo Clinic (Links to an external site.) about 50% of people in world-wide get an H.pylori infection; however, usually the infection is dormant. The lifetime risk of developing peptic ulcers in persons with the bacteria is about 10-20%. How does the infection contribute to the development of peptic ulcers?

damages the lining of the stomach and duodenum

Bulk-forming laxatives absorb free water in which of the following sections of the GI tract?

large intestine

When you eat, food passes from the throat to the stomach through the esophagus. Once food is in the stomach, a ring of muscle fibers prevents food from moving backward into the esophagus. These muscle fibers are called the __________

lower esophageal sphincter, or LES

Prostaglandins: NAME AND ROUTE OF ADMINISTRATION

misoprostol (Cytotec) PO

ch 34

p 592-610

emetics

p 605

antiemetics

p 606

Antacids neutralize hydrochloric acid and decrease the production of ___.

pepsin

Laxative Stimulants: indications

Temporary relief of constipation Prevent straining with bowel movements

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: patient education

Do not take with antacids Contact health care provider if IBD symptoms worsen

Laxative Stimulants: contraindications and interactions

Do not use in patients with abdominal pain, appendicitis, GI bleeding, fecal impaction, GI obstruction Do not use if pregnant or lactating Do not use in those with congestive heart failure, caution with diabetes and renal impairment

Osmotic Laxatives: contraindications and interactions

Do not use with renal impairment or hypertension because of potential for sodium accumulation

tony Jones is 18-years-old and has always suffered from motion sickness, especially when flying. He is going to fly to Cancun for spring break. He usually waits to take his oral medication until he feels nauseated because it makes him drowsy. When do you advise him to take his oral antiemetic?

30 minutes before flying to avoid development of nausea

Laxatives are often misused because people may think they are constipated when in fact they are not - called "perceived constipation". Laxatives are also abused by patients with bulimia nervosa or anorexia nervosa. Overuse of laxatives can cause volume depletion and electrolyte imbalances especially in older adults.

A healthy diet filled with fresh fruits, vegetables, and whole-grain products, regular exercise, and drinking at least 8 cups of water a day can help prevent constipation in most people.

Bulk-Forming Laxatives: mechanism of action

Absorbs free water in intestinal tract, opposes dehydration by forming gelatinous mass (bulk)

Be sure to read about GERD on the NIDDKD Web site (Links to an external site.) and your lecture notes and select all true statements.

Antacids and OTC or prescribed PPIs or H2-blockers may be used for treatment of symptoms. Lifestyle changes in diet and timing of food intake at bedtime can be as important as medication. Gastroesophageal reflux occurring more than 2x per week for several weeks may be GERD. GERD may be caused by medications; e.g., calcium channel blockers, certain asthma medications (e.g., bronchodilators), antihistamines, painkillers, sedatives, and antidepressants. Stomach acid may leak upward into the esophagus when the lower esophageal spincter does not close completely causing symptoms, such as pyrosis.

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: mechanism of action

Anti-inflammatory

Antidiarrheals: drug interactions

Anticoagulants (Pepto-Bismol), digoxin, thiazides, penicillins, tetracyclines, propranolol, thyroid replacement, folic acid, oral hypoglycemics, synthetic opioids, alcohol CNS depressants, MAOIs Adsorbents may interfere with absorption of drugs in GI tract

Antacids: MECHANISM OF ACTION

As bases (alkaline), they neutralize hydrochloric acid and decrease pepsin production by increasing the pH so pepsinogen isn't converted to pepsin - antisecretory action

Antiemetics: patient tips

Avoid driving/using heavy machinery - due to drowsiness Avoid in pregnancy, especially in first trimester - teratogen For motion sickness, take 30 minutes prior to travel

Based on your understanding of the lecture notes and WebMD information, select all true statements about Crohn disease (Links to an external site.).

Azathioprine and methotrexate are immunosuppressants that may be prescribed if corticosteroids do not attain remission. The main symptoms of Crohn disease include abdominal pain, diarrheal stool (possibly bloody) 10-20 times a day, weight loss, and less frequently, mouth sores, bowel blockages, anal fissures and fistulas. Diagnostic tests include barium x-ray, colonoscopy, biopsy of diseased tissue (rule out cancer or other disease), and stool analysis (rule out infection). Aminosalicylates (sulfasalazine or mesalamine) are used to manage symptoms caused by inflammation.

Antacids: CONTRAINDICATIONS AND INTERACTIONS

Calcium containing products should not be used in patients with hypercalcemia or hyperparathyroidism, severe renal disease, ventricular fibrillation, or pregnancy Caution should be taken with patients who are elderly, lactating, or on kidney dialysis Calcium products decrease absorption of tetracycline and ciprofloxacin

Stool Softeners: patient tips

Consume plenty of fluids, eat a high-fiber diet, exercise regularly, eat meals regularly Not for prolonged dietary management

A lower GI anti-inflammatory agent, olsalazine is indicated treatment for UC and other chronic IBDs. Look up olsalazine sodium (Dipentum) (Links to an external site.) in the PDR and select all true statements.

Contraindications/precautions include 5-aminosalicylate hypersensitivity, colitis and inflammatory bowel disease, renal disease/failure/impairment, and pregnancy/breast-feeding. This drug is to be taken orally with food. Some moderate adverse effects include stomatitis, colitis, leukopenia, eosinophilia, anemia, neutropenia, hepatitis, jaundice, and cholestasis. Olsalazine sodium is a salicylic acid derivative used to maintain remission of UC in patients, who can not tolerate sulfasalazine.

Antacids: indications

Counteract hyperacidity in the stomach, protect from ulcers, and promote ulcer healing

_______ primarily causes abdominal pain, diarrhea (which may be bloody if inflammation is at its worst), vomiting (can be continuous), or weight loss, but may also cause complications outside the gastrointestinal tract such as skin rashes, arthritis, inflammation of the eye, tiredness, and lack of concentration.

Crohn's disease

_______ describes bowel movements (stools) that are loose and watery and frequent in occurrence. It is very common and usually not serious, and is most often caused by infection, toxins, or drugs. Bacterial or parasitic diarrhea should be treated with the appropriate agent for the infection. Drug-induced diarrhea should be treated by discontinuation of the drug - if possible.

Diarrhea

Laxative Stimulants: mechanism of action

Directly increase peristaltic movements of the intestines Cathartic

H2 Receptor Antagonists: patient tips

Do not smoke or drink alcohol - decrease effectiveness of medication Avoid taking this drug with other medications

Antiemetics: contraindications and interactions

Don't use antiemetics when use may prevent or delay diagnosis Not to be used routinely Hypersensitivity

Antidiarrheals: patient tips

Drink plenty of clear fluids, take on an empty stomach (1-2 hrs after meals) Shake liquids well before use Avoid taking with other medications Use precautions when operating machinery Do not drink alcohol Antibacterials may be prescribed if a bacterial infection is the cause of diarrhea: some common ones are macrolides (erythromycin, azithromycin), fluoroquinolones (Cipro, rifaximin)

The following also raises the risk for peptic ulcers:

Drinking too much alcohol Caffeine consumption Regular use of aspirin, ibuprofen, naproxen, or other nonsteroidal anti-inflammatory drugs (NSAIDs) Smoking cigarettes or chewing tobacco Being very ill - e.g., ventilator-dependent Having radiation treatments

Prostaglandins: patient tips

Ensure females of childbearing age are using contraception because this drug may produce spontaneous abortion. Diarrhea may occur in first month and then should resolve.

H2 Receptor Antagonists: adverse effects/warnings

GI disturbances, headache, drowsiness, agitation and confusion, hallucinations, reversible impotence Large doses should be avoided as they can cause cardiac arrhythmias and arrest.

Treatment for UGI disorders include lifestyle changes, medications, and potentially surgery. What classes of medications may be used to treat PUD or GERD? Mark all that apply.

H2 blockers, PPIs, antacids

Ulcers are sometimes caused by the bacterium ________. In these cases, an antibiotic is prescribed. When two antibacterial medications are combined with colloidal bismuth (which increases mucus production and appears to be bactericidal to H. pylori), it is known as triple therapy.

Helicobacter pylori

If you haven't done so already, go to this site - DHHS National Digestive Disease Information Clearinghouse (Links to an external site.) - and learn more about peptic ulcer disease and H. pylori. What statements are true about this condition?

Helicobacter pylori is a major cause of peptic ulcers, and individuals who contract it are more likely to develop PUD. It is theorized that the bacteria may be spread via contaminated food, water or utensils, and possibly, from person to person from saliva or other body fluids of an infected person. The urea breath test and stool test can detect H. pylori.

H2 Receptor Antagonists: contraindications and interactions

Hypersensitivity to medication They should not be used in children <16 yrs or pregnant/lactating women Cimetidine - warfarin, phenytoin, diazepam, chlormethiazole, propranolol, lidocaine, and others Cimetidine binds to CYP450 - therefore, adverse drug interactions with drugs transformed via the CYP450 system are common.

Stimulant laxatives are the most commonly abused laxative and Chronic use can result in ...

Impaired function of intestines - loss of normal muscle tone and nerve response - cannot contract and evacuate stool normally Rebound constipation - alternating constipation, diarrhea, and gas - becomes trapped in the intestines Dehydration - too much fluid lost due to diarrhea Electrolyte abnormalities - sodium potassium, and chloride losses Blood in stool - irritation of the colon Rectal prolapse - inside of the intestines protrudes through the anal opening

The most common cause of diarrhea is a virus that infects the gut. The infection usually lasts for 2 days and is sometimes called "intestinal flu" or "stomach flu". Diarrhea may also be caused by:

Infection by bacteria (the cause of most types of food poisoning) or by other organisms Eating foods that upset the digestive system; e.g., spicy foods Allergies to certain foods Medications Radiation therapy Diseases of the intestines (Crohn disease, ulcerative colitis) Malabsorption (where the body is unable to adequately absorb certain nutrients) Hyperthyroidism Some cancers Laxative abuse Alcohol abuse Digestive tract surgery Diabetes mellitus Competitive running Diarrhea may also follow constipation, especially for people who have irritable bowel syndrome.

Antacids can decrease the absorption of other drugs because they change the stomach and duodenal pH. They can also bind to drugs and block absorption - aluminum salts often are the culprit. Antacids also have systemic effects.

Magnesium salts can cause hypermagnesemia and aluminum slats can cause hypophosphatemia

Antacids: adverse effects/warnings

Magnesium-containing products commonly cause diarrhea Calcium and aluminum products commonly cause constipation Sodium bicarbonate - nausea, bloating gas (neither diarrhea or constipation) Less common adverse effects, often due to overuse, include ---aluminum-containing antacids - anorexia, weakness, bone pain, tremors ---hypermagnesemia - nausea/vomiting, confusion, renal calculi, metabolic alkalosis, headache ---calcium products - excessive use can lead to kidney stones and acid rebound ------acid rebound - paradoxical increase of gastric secretions causing increased symptoms of heartburn ---sodium bicarbonate - more serious effects - swelling lower extremities, weight gain

Antiemetics: adverse effects and warnings

Main adverse effect - drowsiness Other effects include - dizziness, headache, restlessness, blurred vision, skin, dry mouth, hypotension

___________ begins the process by mechanically breaking down the food into smaller pieces. Taste buds detect the chemicals that make up the food being eaten — carbohydrate, protein, fat — so that appropriate enzymes are produced and secreted throughout the system.

Mastication

H. Pylori Treatment Protocols -

Most recent drug regimens for H. pylori include triple therapy (2014 Medscape News) for 10-14 days with - ---PPI, amoxicillin, and clarithromycin; or ---bismuth subsalicylate, metronidazole, and tetracycline. Wolters Kluwer "UpToDate" treatment regimen (June 2015) states that first-line therapy should include a - ---PPI (like lansoprazole, omeprazole, or esomeprazole) with amoxicillin and clarithromycin for 7-14 days. Quadruple therapy may be indicated when the patient has been exposed to clarithromycin or metronidazole or when there is known resistance (>15%) in the region.

Bulk-Forming Laxatives: adverse effects and warnings

Nausea and vomiting, abdominal cramping, and diarrhea (with chronic use)

Osmotic Laxatives: adverse effects and warnings

Nausea, vomiting, abdominal cramping, diarrhea, lethargy, electrolyte imbalance. Can also cause hypotension, bradycardia, depression and coma

Antidiarrheals: adverse effects

Nausea, vomiting, agitation, drowsiness, tachycardia Opioids - recall that opioids are CNS depressants, so with high doses - respiratory depression, coma, dependence

proton Pump Inhibitors (PPI): contraindications and interactions

Not for long term use of duodenal ulcers or GERD Avoid using in those with GI bleeding Not recommended for those who are pregnant or children <18 yrs

Antidiarrheals: LIST OF NAMES/ROUTE OF ADMINISTRATION (primarily PO)

Opioids - camphorated opium tincture (paregoric) diphenoxylate hydrochloride with atropine sulfate(Lomotil), difenoxin hydrochloride with atropine sulfate, loperamide (Imodium, Maalox Anti Diarrheal) Adsorbents: bismuth subsalicylate (Pepto-Bismol), kaolin, pectin, activated charcoal, attapulgite (aluminum silicate

Antidiarrheals: mechanism of action

Opioids - decrease intestinal motility by relaxing smooth muscles of the intestine. Slowing down forward gut movement allows for more re-absorption Adsorbents - antimicrobial, antisecretory, and anti-inflammatory effects

Osmotic Laxatives: mechanism of action

Osmosis of sodium or magnesium ions to attract water into the stool and increase pressure and volume inside the intestines that stimulates the defecation reflex

Doctors classify diarrhea as osmotic, secretory, or exudative.

Osmotic diarrhea means that something in the bowel is drawing water from the body into the bowel. A common example of this is "dietetic candy" or "chewing gum" diarrhea, in which a sugar substitute, such as sorbitol, is not absorbed by the body but draws water from the body into the bowel, resulting in diarrhea. Secretory diarrhea occurs when the body is releasing water into the bowel when it's not supposed to. Many infections, drugs, and other conditions cause secretory diarrhea. Exudative diarrhea refers to the presence of blood and pus in the stool. This occurs with inflammatory bowel diseases, such as Crohn disease or ulcerative colitis - as well as several infections.

One treatment of inflammatory bowel disease is the use of anti-inflammatory/anti-irritant agents like mesalamine or olsalazine. What is the usual route of administration for these agents? Mark all that apply.

PO, RETENSION ENEMA, suppository

proton Pump Inhibitors (PPI)

PPIs inhibit the H+-K+-ATPase enzyme of the parietal cell to reduce acid secretion. These drugs are superior to H2 antagonists in suppressing acid and healing of peptic ulcers.

If you haven't already done so, read about peptic ulcer disease on the WebMD (Links to an external site.) site and study your lecture notes and text to select all true statements about PUD.

PUD is diagnosed by a history of symptoms and may be confirmed with an upper endoscopy; doctors may choose to treat ulcers empirically. Symptoms of PUD are gnawing or burning pain in the middle or upper stomach between meals and at night, bloating, pyrosis, n/v, and potentially severe symptoms of GI bleeding. While there is no single cause for peptic ulcers, they are an end result of an imbalance between digestive juices in the stomach and the duodenum. Alcohol use and long-term NSAID use can contribute to peptic ulcer disease.

_________, also in the pancreatic juice, continues to break down carbohydrates into disaccharides. Disaccharidases further break down disaccharide molecules into monosaccharides that can be absorbed through the cells lining the small intestines. At this point in digestion, carbohydrates and fats are in their simplest forms in the small intestines.

Pancreatic amylase

Antiemetics: indications

Prevent or treat nausea/vomiting - it's easier to prevent nausea/vomiting than it is to treat Commonly used to prevent motion sickness and radiation/chemotherapy vomiting Prokinetic - gastroparesis (slowed gastric motility), relieves symptoms of nausea, vomiting, heartburn, a feeling of fullness after meals, and loss of appetite

proton Pump Inhibitors (PPI): indications

Promote healing of active gastric and duodenal ulcers Reduction of gastroesophageal reflux symptoms Palliation of esophagitis symptoms (i.e., acid regurgitation and heartburn) Prevention of stress-related ulcers in critically ill patients

H2 Receptor Antagonists: mechanism of action

Reduce gastric acid secretion in the stomach by blocking H2 receptors preventing histamine-induced acid release - antisecretory action

Bulk-Forming Laxatives: indications

Relieves both diarrhea and constipation Chronic spastic constipation or constipation associated with rectal disorders/surgeries

Antidiarrheals: contraindications and warnings

Renal or hepatic impairment, chronic diarrhea or diarrhea caused by toxic substances, ulcerative colitis

Osmotic Laxatives: indications

Short term treatment of occasional constipation

H2 Receptor Antagonists: indications

Short term treatment of peptic ulcer disease, (at reduced doses also for prevention of recurrence) Short term treatment of gastric ulcers and heartburn

Bulk-Forming Laxatives: contraindications and interactions

Should not be used in those with GI obstruction, nausea and vomiting or undiagnosed abdominal pain. Caution with use in children younger than 2 years, pregnancy and lactation Interacts with antibiotics, warfarin, digoxin, salicylates, nitrofurantoin

T/F: Many people will experience diarrhea a couple times a year and generally it can be treated with OTC medications.

T

T/F: The most common use of antiemetics is to prevent and/or treat nausea and vomiting associated with motion sickness and post-radiation/chemotherapy.

T

Antacids: patient tips

Take 1-3 hours after meals and at bedtime Avoid taking within 1-2 hours of other oral medications - so it does not interfere with absorption Do not overuse and increase fluid intake to prevent kidney stones (calcium products) or acid rebound. [Acid rebound is the paradoxical increase of gastric secretions after eating or drinking that occur when antacids are taken in high doses and over a long period of time.] Alternate between aluminum and calcium products to prevent constipation and diarrhea - or use products that are pre-mixed (aluminum hydroxide + magnesium hydroxide). If gas is also a problem, simethicone can also be added (aluminum hydroxide + magnesium hydroxide + simethicone). The medications are for symptom relief - if pain persists for several days, contact physician.

Antidiarrheals:

The antidiarrheal agents are classified as opioid or synthetic opioid medications and adsorbents. The opioids relax smooth muscle and decrease peristalsis. The adsorbents coat the walls of the GI tract, bind to acids, and absorb toxic substances, which are then excreted in the stool.

The Big Picture

The digestive system includes the mouth, pharynx, esophagus, stomach, small intestine, large intestine, rectum and anus. Accessory organs include salivary glands, liver, pancreas, and gallbladder. This system does mechanical and chemical digestion, absorption of nutrients and elimination of waste. Many common GI conditions have medicines available OTC and have a high risk of being misused and/or abused. GI medications can increase/decrease muscle tone, increase/decrease digestive secretions, and impact the rate of peristalsis and gastric emptying. Ulcers are treated by decreasing irritants (acid production, NSAID use, pepsin, H. pylori) and increasing protectants (mucous, bicarbonate, bile, pancreatic juices). These are used at a higher dose to promote healing and then at a lower dose for prevention. The antisecretory drugs are H-2 receptor antagonists, antacids, prostaglandins, and proton pump inhibitors. If there are bacterial causes (H. pylori), antibiotics will be utilized. Overuse of calcium antacids can result in kidney stones and acid rebound. Diarrhea is often able to be controlled with OTC medications. For more severe cases, opioids can be very effective, but should not be used long term. Constipation may be treated with laxatives. Bulk forming laxatives add fiber to increase stool volume. Osmotic laxatives with osmosis (magnesium and sodium) to draw water back to the intestine. Laxative stimulants act directly in the intestinal wall to increase peristalsis. Laxatives can be overused and result in dependence for defecation or electrolyte imbalance in elderly Caution should be used with taking opioid GI medications, particularly in the elderly, as they can decrease blood pressure. Antiemetics can also cause CNS depression and the elderly should be closely monitored.

Laxative Stimulants:

The stimulants used to treat constipation increase water and electrolytes in the feces and increase motility.

Stimulant laxatives are the most commonly abused laxative ...

They stimulate the nerves in the walls of the large intestines and cause intestinal contractions as well as fluid and electrolyte changes. These can be dangerous, despite the fact that they are non-prescription medications. They can be habit-forming, and tolerance develops so that higher and higher doses are needed to obtain the same effect.

Stool Softeners: contraindications and interactions

Those with atonic constipation, GI obstruction or perforation Caution should be used in those with congestive heart failure, diabetes Can interact with mineral oil which is sometime used as a lubricant in constipation

proton Pump Inhibitors (PPI): patient tips

Treatment is only short-term and should be limited to 4-8 weeks Avoid taking with other medications

there are two more enzymes in the pancreatic juice that help digest proteins. Like pepsin, their inactive forms are secreted and they become activated in the cavity of the small intestines. The inactive forms are trypsinogen and chymotrypsinogen._________ are the active forms that do the work of breaking apart peptide fragments. ________ then break the peptides into individual absorbable amino acids.

Trypsin and chymotrypsin, Aminopeptidases

Based on your text, lecture notes and the National Digestive Diseases Information Clearinghouse Web site information, select all true statements about ulcerative colitis

While blood tests might identify inflammation (high WBCs) or anemia (decreased hemoglobin) and include stool tests to rule out infection, flexible sigmoidoscopy or colonoscopy are the most accurate methods for diagnosing UC and ruling out other s/s causes. Ulcerative colitis is a chronic disease with characteristic inflammation and ulceration of the inner lining of the colon and rectum, generally occurring in people between the ages of 15-30, and may be a cause or a result of an immune system disorder. Treatment of UC includes aminosalicylates, immunomodulators and/or anti-TNF biologic. The most common symptoms of UC are abdominal discomfort and blood or pus in diarrheal stool.

Although ulcerative colitis has no known cause, there is a genetic component to susceptibility to this condition. The disease may be triggered in a susceptible person by environmental factors.

While dietary modification may reduce the discomfort of a person with the disease, ulcerative colitis is not thought to be caused by dietary factors.

As the stomach continues to churn the food particles, hydrochloric acid breaks down the peptide bonds in proteins. The resultant semisolid mixture, or chyme, enters the duodenum through the pylorus. Periodic opening and closing of the pyloric sphincter allows _________ at any given time.

a small portion of chyme into the duodenum

Nerve endings in the stomach secrete _________ which directly on the parietal cells and mediate the secretion of gastrin from G cells as well as histamine-2.

acetylcholine and gastrin-releasing peptide

Indications for laxatives are to treat constipation or to clear the bowel for testing (e.g., radiologic imaging or colonoscopy) or bowel surgery. Laxatives contain chemicals that

act on the bowel to increase motility, bulk, and/or frequency

Gastric acid is a digestive fluid produced by the parietal cells in the lining of the stomach and is comprised of hydrochloric acid, potassium chloride, and sodium chloride. What is the primary purpose of gastric acid in the digestive process?

activates digestive process

Inflammatory bowel disease is generally divided into Crohn's disease and ulcerative colitis. For both of these disease consideration needs to be given to induction of remission and maintenance of remission. Sometimes the same drugs are used for both, but not always. The main drugs used for these conditions are -

aminosalicylates corticosteroids immunosuppressants TNF inhibitors integrin receptor antagonists antibacterials

The drug cards for treating gastroesophageal reflux disease (GERD), peptic ulcer disease (PUD), and nausea and vomiting are include below:

antacids H2-receptor antagonists proton pump inhibitors prostaglandins anticholinergics. These drugs act by either preventing cell destructive effects or promoting cell protective effects.

The drugs that treat common GI disorders, like GERD and PUD, include ___________. Antiemetics are not used for GERD and PUD specifically, but used to treat nausea and vomiting

antacids, H2-receptor antagonists (H2 blockers), and proton pump inhibitors (PPIs)

Ulcerative colitis is treated as an autoimmune disease. Treatment options are individualized and dependent on the disease and symptom severity. The goals of therapy are to induce and maintain remission and to improve quality of life. Treatment includes -

anti-inflammatory drugs ---aminosalicylates - sulfasalazine (Azulfidine) ---glucocorticoids - prednisone, methylprednisone, or hydrocortisone immunosuppressants immunomodulators - azathioprine or methotrexate biological therapy targeting specific components of the immune response - infliximab (anti-tumor necrosis factor). Colectomy (partial or total removal of the large bowel through surgery) may be necessary, but is not a cure for the disease

Kim is flying to Europe in 2 weeks. She has had motion sickness during previous air trips and does not want to be nauseated on this long flight. She asks Dr. Merry if there is a medication she can take to prevent nausea. From what overall medication category would Dr. Merry choose to prescribe?

antiemetics

Digestion ends in the small intestines and the residual from this process moves into the large intestines. Electrolytes and excess fluids are reabsorbed into the body to maintain fluid balance - what remains are feces. Feces are then eliminated from the body through the ______

anus

Crohn's disease is caused by interactions between environmental, immunological and bacterial factors in genetically susceptible individuals. This results in a chronic inflammatory disorder, in which the body's immune system attacks the gastrointestinal tract possibly directed at microbial antigens. Crohn's disease has traditionally been described as an _________

autoimmune disease, but recent investigators have described it as an immune deficiency state.

Lifestyle changes to reduce or eliminate the occurrence of pyrosis include -

avoid foods that increase secretion of stomach acids; e.g., alcohol, colas, acid juices, coffee, chocolate and spices, as well as fried or fatty foods eat smaller, more frequent meals reduce weight since excess weight contributes to a variety of stomach problems other strategies include smoking cessation, avoid eating within 2 hours of bedtime, and elevating the head of the bed 6-8 inches.

Laxative Stimulants: NAMES AND ROUTES OF ADMINISTRATION

bisacodyl (Dulcolax, Apo-Bisacodyl) - PO rectal; cascara sagrada (Cascara Sagrada Aromatic extract, Cascara Sagrada Fluid Extract) - PO, senna (Black Draught, Senokot) - PO

Antibacterial medication used to eradicate H. pylori include - tetracycline, amoxicillin, clarithromycin, and metronidazole. Combination medications include ______

bismuth-tetracycline-metronidazole (PO) and bismuth ranitidine (Tritec, PO).

H2 Receptor Antagonists DRUG NAMES/ADMINISTRATION

cimetidine (Tagamet) - PO IM IV (prototype), famotidine (Pepcid) - PO, nizatidine - PO, ranitidine (Zantac) - PO IV recognizable by the "-tidine" ending

Prostaglandins: adverse effects and warnings

diarrhea stomach pain, nausea, flatulence vaginal bleeding or spotting, menorrhagia (heavy menstrual flow), menstrual cramps

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: drug interactions

digoxin, oral hypoglycemia, warfarin, varicella vaccine, fluvoxamine

Stool Softeners: NAMES AND ROUTES OF ADMINISTRATION

docusate calcium (Surfak) PO, docusate potassium (Dialose) PO, docusate sodium (Colace) PO, rectal, glycerin (Glycerol, Osmoglyn) rectal

proton Pump Inhibitors (PPI): names and route of administration

esomeprazole (Nexium) PO, lansoprazole (Prevacid) PO, omeprazole (Prilosec) PO, pantoprazole (Protonix) PO IV, rabeprazole (AcipHex) PO recognizable by the "-azole" ending (however, don't confuse with the azole antifungal agents)

Disorders of the esophagus, stomach, and duodenum arise from ________

excess secretion or regurgitation of gastric acids and enzymes

Bile salts emulsify fats, and lipase, an enzyme in pancreatic juice, breaks apart fat molecules into _______

fatty acids and glycerol

Gastric ulcers are usually caused by defective mucous production and take longer to heal than duodenal ulcers. Gastric ulcers are often chronic. Duodenal ulcers are mainly caused by excessive acid production. This makes the treatment for the two slightly different. We used to believe that all ulcers were caused by too much stress or spicy foods. Stress-related ulcers are more likely to be _________

gastric and occur as a result of stress-induced trauma; however, everyday stress is not likely to cause ulcers

An increase in the production of gastric acid secretions to neutralize antacids, also known as ______, can occur when antacids have been taken for a prolonged period of time.

gastric rebound

Prostaglandins are used to prevent the effects of NSAID-induced ___.

gastric ulcers

The most common cause of inflammation and ulceration is infection of the stomach by a bacterium called Helicobacter pylori (H. pylori) - 70% of gastric and 85% of duodenal ulcers are caused by this _________ While most people with peptic ulcers have these bacteria living in their gastrointestinal (GI) tract, many do not develop an ulcer.

gram-negative bacterium.

Gastroesophageal reflux disease (GERD) is a condition in which the stomach contents (food or liquid) leak backward from the stomach into the esophagus. This action can irritate the esophagus, causing heartburn and other symptoms. This is the most common disorder of the esophagus and often caused by an incompetent lower esophageal sphincter. The regurgitation of gastric acid and pepsin into the esophagus causes mucosal damage. Common signs/symptoms include ___________

heartburn (pyrosis) and pain on swallowing (due to ulcerative esophagitis)

Constipation can also be an adverse effect of medications like narcotics, anticholinergics, and tricyclic antidepressants. While a __________ can counteract this adverse effect, a stool softener or bulk-forming laxatives may also be necessary.

higher fiber diet, water, and exercise

The release of ___________ is the most important positive regulation mechanism of the secretion of gastric acid in the stomach. Its release is stimulated by gastrin and acetylcholine, and then, inhibited by somatostatin.

histamine-2

Production of gastric acid is regulated by both the autonomic nervous system and several hormones. Gastric acid is a digestive fluid produced by the parietal cells in the gastric glands of the stomach - it's composed of ________ which activates the digestive enzymes.

hydrochloric acid, potassium chloride, and sodium chloride.

Most ulcers occur in the first layer of the inner lining. A hole that goes all the way through the stomach or duodenum is called a perforation. Ulceration results from an ________

imbalance between the cell destructive effects (gastric acid, pepsin, H. pylori, NSAIDs) and cell protective effects (mucus, bicarbonate, pancreatic juices and bile).

The lining of the stomach and small intestines is protected against the irritating acids produced by the stomach. However, if this protective lining stops working correctly and the lining breaks down, it may result in _________

inflammation (gastritis) and a potential ulcer.

Nausea and vomiting are fairly common symptoms that can accompany almost any illness. There are numerous causes of nausea and vomiting such as _____

it is most common adverse effect of medications and many illnesses (infection/inflammation), radiation therapy, and chemotherapy for malignancies, noxious stimuli, physical or mental stress, inner ear disorders, and motion sickness.

Osmotic Laxatives: NAMES AND ROUTE OF ADMINISTRATION

lactulose (Cephulac) PO, magnesium citrate (Citrate of magnesia, Citroma) PO,magnesium hydroxide (Milk of Magnesia) PO, magnesium sulfate (Epsom Salt) PO

A common adverse effect of laxative stimulants is abnormal dark pigmentation of the colon, referred to as ____.

melanosis

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: NAMES OF DRUGS/ROUTE OF ADMINISTRATION

mesalamine (Rowasa, Pentasa), sulfasalazine (Azulfidine), olsalazine (Dipentum), balsalazide (Colazal), alosetron (Lotronex) - PO, SUPP, retention enema

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: adverse effects

mesalamine - abdominal pain, cramping, headache, weakness, dizziness sulfasalazine - nausea, fever, joint pain, rashes olsalazine - abdominal cramping, diarrhea, dyspepsia, joint pain, anorexia alosetron - constipation, bloody diarrhea, heartburn, nausea, vomiting

Since the aluminum salts and calcium carbonate antacids cause constipation and the magnesium salts cause diarrhea, they can be ________

mixed into one compound or alternated

The tongue pushes the bolus of food to the back of the throat where it is swallowed down the esophagus to the stomach. As salivary amylase action ends, _________ take over.

molecules and enzymes in the stomach

Finally, after several hours in the digestive system, the carbohydrates, fats, and proteins all are in their smallest components: ___________. They are absorbed from the small intestines and used for body processes.

monosaccharides (glucose), fatty acids and glycerol, and amino acids

What is the action and benefit of schedule III opioids (e.g., paregoric) in the treatment of diarrhea? There is more than one response.

most effective drug for controlling diarrhea stimulation of opioid receptors in GI tract to increase segmentation or mixing movement of the gut decrease peristaltic movements to slow forward movement and reabsorption

One of the ways in which drugs work on GI disorders is through the increase or decrease of function to change ______ in the GI tract. Drugs for GI disorders may also increase or decrease ____ as food passes through the stomach or change the rate of ____.

muscle tone and/or secretions emptying time; peristalsis

Laxative Stimulants: adverse effects and warnings

nausea, abnormally loose stools, rebound constipation, melanosis discoloration of urine, hypokalemia

Other cells in the stomach produce bicarbonate and mucus to protect the stomach lining. Cells in the duodenum produce large amounts of bicarbonate to _________

neutralize gastric acid that passes further down the digestive tract

laxatives come in tablets, capsules, liquids, suppositories, and enemas. Suppositories and enemas work faster than ______

oral medications

antacids

p 596

H-2 receptor antagonists including cimetidine

p 597

proton pump inhibitors (PPIs)

p 597

prostaglandins

p 598

opioid and synthetic opioid drugs

p 599-600

adsorbents

p 600

osmotic laxatives

p 602

stool softeners aka emollients aka surfactants including docusate sodium

p 603

bulk-forming laxatives including psyllium hydrophilic mucilloid and polycarbonphil

p 604

laxative stimulants including sagrada and senna

p 604

an ulcer is an open sore on an external or internal surface of the body, caused by a break in the skin or mucous membrane that fails to heal on its own. A peptic ulcer is an erosion in the lining of the stomach (peptic ulcer) or the first part of the small intestine (duodenal ulcer) - the condition of having ulceration in the stomach and/or the duodenum is _________

peptic ulcer disease (PUD)

Ulcerative colitis is an intermittent disease, with _________. Symptoms of ulcerative colitis can sometimes diminish on their own, however, the disease usually requires treatment to go into remission.

periods of exacerbated symptoms, and periods that are relatively symptom-free

____ is the progressive wavelike involuntary movement that moves food and waste materials through the gastrointestinal tract.

peristalsis

When the bolus enters the stomach, pepsin breaks down __________. Proteins are hydrolyzed causing the long protein chains (polypeptides) to be broken down further into smaller dipeptides or peptides.

proteins into smaller chains of amino acids

The ________ increases gastric pH - so proton pump inhibitors target this enzyme and cause decreased stomach acidity in diseases that have excess acid. H2antagonists indirectly decrease gastric acid production. Antacids neutralize existing acid.

proton pump enzyme

What enzyme increases gastric pH?

proton pump enzyme

Crohn's disease, also known as_________, is a type of inflammatory bowel disease that may affect any part of the GI from mouth to anus, causing a wide variety of symptoms.

regional enteritis

The goal of Crohn disease treatment is to ___________. Aminosalicylates (sulfasalazine or mesalamine) are used to manage symptoms caused by inflammation. Azathioprine and methotrexate are immunosuppressants (immunomodulator drugs) that may be prescribed if corticosteroids do not attain remission

relieve symptoms, promote healing of damaged tissues, attain remission, prevent exacerbations, and postpone need for surgery

Gastrointestinal Anti-Inflammatory and Anti-Irritant Agents: warnings and precautions

renal impairment hepatic failure in pre-existing liver disease elderly

In addition to mastication, _______ is secreted during mastication to split the bonds between glucose molecules into long chains of starches.

salivary amylase

In addition, _________ is secreted continuously in the mouth (not just during mastication) and accumulates in the stomach between meals. Approximately 10-30% of dietary fat is hydrolyzed in the stomach by this enzyme

salivary lipase


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