Pharmacology, Intravenous Therapy & Nutrition Flashcards
What are antacids
Antacids commonly prescribed have at least one of the following elements as their main ingredient:
1. Aluminum salts
2. Calcium carbonate
3. Magnesium salts
The ingredient alginate is not an antacid but may provide barrier protections
Are available OTC
What is the mechanism of action of antacids
- Antacids have no direct effect on gastric acid secretin and do not coat or protect the mucous lining.
- Instead, antacids neutralize gastric acid, reducing the total acid load in the GI tract and leading to a transient rise of gastric pH.
- This decreases pepsin activity because pepsin is rendered inactive in alkaline conditions.
- It also increases LES tone, reducing reflux
- Aluminum ions inhibit smooth muscle contraction and gastric emptying. This action is counterproductive because in gastroesophageal reflux disease (GERD), prompt gastric emptying is beneficial
What are the indications for antacids
Antacids are indicated in the treatment of:
1. Hyperacidity—heartburn (pyrosis)
2. Gastroesophageal reflux disease (GERD)
3. Acid indigestion
4. Hyperacidity associated with peptic ulcer disease
- Research studies demonstrate that antacids are clearly superior to placebos in healing gastric ulcers
Because antacids leave the stomach rapidly, they are best used for intermittent symptoms.
Taken on an empty stomach, the effects of antacids last less than 1 hour.
After meals, the buffering effect may last as long as 3 hours
For optimal effect, antacids should be given about 1 hour after meals or feedings and during periods of acid rebound
What are adverse effects of antacids
- Prolonged use of magnesium or calcium containing antacids may cause systemic absorption of toxic quantities of these ions.
- Excessive use of aluminum containing antacids my lead to hypophosphatemia
- Aluminum and calcium preparations tend to be constipating, whereas magnesium preparations tend to produce a laxative effect
- In chronic patients with renal failure, administration of aluminum-containing antacids is best at mealtime
- Antacids containing sodium can precipitate edema in patients with cirrhosis, hypertension, or renal or congestive heart failure
What are contraindications of use of antacids
- In patients taking tetracycline, iron, or H2-receptor antagonists
—Calcium binds and prevents absorption of tetracycline, whereas antacids decrease the absorption of iron and H2blockers - Magnesium containing antacids can precipitate hypermagnesemia in patients with chronic renal failure and should be avoided in these patients, as central nervous system depression, skin irritation, and rarely, muscle paralysis with respiratory failure can occur
What are examples of antacids
- Aluminum hydroxide gel
- Calcium carbonate (Alkaline-Seltzer, Tums)
- Magnesium hydroxide (Milk of Magnesia)
- Gaviscon, Gelusil, Maalox, Mylanta, Rolaids
- Pepto-Bismol
What are antibiotics
- May be prescribed for pediatric and adult patients
- The nurse needs to have a basic knowledge of mechanism of action, antimicrobial spectrum, typical uses, and toxicity of commonly used antibiotics
- Cost and dosing schedules must be considered in the decision-making process when prescribing, in order to enhance patient compliance
- Knowledge of patient drug allergies, recommended dosages, and bacterial taxonomy is of critical importance for GI nurses in order to provide safe medical care and promote patient and family education
What is the mechanism of action for antibiotics
- Antibiotics are antimicrobial agents
- The specific antibiotic drug selection depends on the pathogen, drug adverse-effect profile, patient drug allergies, age of the patient, and any comorbid illness
What are the indications for antibiotics
For infectious agents found in the GI tract
- Mouth infections
- Gastroenteritis
- Traveler’s diarrhea
- Severe diarrhea
- Diverticulitis
- Gastritis and ulcers
What are indications of using antibiotics for prophylaxis
- Prosthetic cardiac valves, including trans catheter implanted prostheses and homografts
- Prosthetic material used for cardiac valve repair such as annuloplasty rings and chords
- previous IE (infectious endocarditis)
- Unrepaired cyanotic congenital heart disease or repaired congenital heart disease with residual shunts or valvular regurgitation at the site of or adjacent to the site of a prosthetic patch or prosthetic device
- Cardiac transplant with valve regurgitation due to a structurally abnormal valve
What are adverse effects of antibiotics
- Side effects may vary depending on agent given and can include nausea, vomiting, diarrhea, rash, urticaria, headache, and anaphylaxis
- The administering provider should be familiar with the medication, its potential side effects and their contraindications prior to drug administration
What are contraindications of antibiotics
Contraindications include a known sensitivity to the antibiotic agent
What are examples of antibiotics
- Clindamycin
- Ampicillin
- Tetracycline
- Ciprofloxacin
- Levofloxacin
- Moxifloxacin hydrochloride
- Metronidazole
- Azithromycin
- Clarithromycin
- Trimethoprim-sulfamethoxazole (TMP-SMX)
- Vancomycin
What are Anticholinergic
Substances that block the action of the neurotransmitter called acetycholine at synapses in the central and peripheral nervous system
What is the mechanism of action for Anticholinergic drugs
- Inhibit gastric acid secretions at its source by blocking the acetylcholine receptor on gastric parietal cells
- Decrease the output of pepsin and block vagal stimulation of the smooth muscle, thus decreasing GI tone and motility
- They also decrease gastric emptying tome, presumably through their inhibition of vagal and cholinergic-mediated motility
What are indications for Anticholinergic medications
In treatment for:
- Diffuse esophageal spasm
- Peptic ulcer disease
- IBS
- Diverticulitis
- Hypermotility disorders
- Ulcerative colitis
Can be use to relived the gastric distress caused by gastric spasms, hyperperistalsis, and rapid emptying of the stomach
Because of their side effects they are primarily used as an adjunctive therapy for peptic ulcer disease in combination with antacids or H2 blockers
Best given approximately 1 hour after meals, when food-stimulated acid is at its peak
Their effects persist for 4-5hours
What are adverse effects of Anticholinergics
- Dry mouth, nose and throat
- Hoarseness
- Tachycardia
- Blurred vision
- Urinary hesitancy or retention
- Flushing of the skin
- Constipation
What are contraindications of anticholinergics
In patients who experience bleeding or who have tachycardia, closed angle glaucoma, Achalasia, obstruction, or suspected toxic mega colon
What are examples of Anticholinergic drugs
- Atropine sulfate
- Hyoscyamine
- Dicyclomine hydrochloride (Bentyl)
- Lomotil
What are cholinergic drugs
Mimic the action of acetycholine and/or butrylcholine
What is the mechanism of action for cholinergic drugs
- In contrast to Anticholinergic agents, they increase GI tone and motility
- Produce the same effects as stimulation of the parasympathetic nervous system, thereby stimulating GI secretion and motility
What are indications for the use of cholinergic drugs
- Bethanechol may be used to increase LES pressure in patients suffering from GERD
- also used in children with GERD who are unresponsive to metoclopramide (reglan)
- Domperidone is a peripheral dopamine antagonist that has a safety profile similar to reglan, used to enhance gastric emptying. - not FDA approved in the US
- Cisapride used to relieve symptoms of reflux esophagitis by increasing contractions in the stomach to improve stomach emptying - removed from the market in late 2000
What are adverse effects of cholinergic medications
Cause the same parasympathetic symptoms as anticholinergics, which may include diaphoresis and bladder contractions
What are contraindications of cholinergic medications
Peptic ulcers or possible GI obstruction
What are examples of cholinergic medications
Bethanechol (urecholine, duvoid)
What are antidiarrheals
Agents used for symptomatic relief of diarrhea
What is the mechanism of action for antidiarrheals
Include drugs that decrease intestinal motility and drugs that decrease the fluid content of the stool or inhibit intestinal secretions
What are indications for antidiarrheals
Opium alkaloids may be used as antidiarrheal agents in addition to anticholinergics to inhibit intestinal motility
Bismuth subsalicylate is useful for mild diarrhea and upset stomach; may be used in combination with an antibiotic for the treatment of H.pylori
What are adverse effects of antidiarrheals
Continued use of antidiarrheal agents over an extended period of time is not recommended. If it is not possible to control diarrhea promptly, diagnostic tests should be ordered.
Because opium alkaloid drugs may be habit-forming patients must be cautioned not to exceed the recommended dosage
What are contraindications of antidiarrheals
- Fever, or bloody diarrhea or in patients younger than 2
- Agents that inhibit intestinal motility may cause toxic mega colon in patients suffering from pseudomemranous enterocolitis, acute dysentery, and acute ulcerative colitis
- Should be used in acute exacerbation of IBD only after an infectious cause for the symptoms has been ruled out
- Opium alkaloids are contraindicated in patients with toxic causes of diarrhea and should be used cautiously by patients with asthma, liver disease, prostatic hypertrophy and narcotic dependence
What are examples of antidiarrheals
- Lomotil
- Pepto-bismol
- Imodium
- Acidophilus
What are antiemetics
Produce symptomatic relief of nausea and vomiting
What is the mechanism of action for antiemetics
- Phenothiazines - appear to exert their effects on the cells of the chemoreceptor trigger zone (CTZ) located in the medulla of the brain stem, preventing vomiting center from being activated
- Certain antihistamines - act on the CTZ to suppress centrally mediated nausea and vomiting
- Trimethobenzamide hydrochloride - has a mechanism of action that is unknown, but it may act on the CTZ
- Ondansetron is a selective 5-HT3 antagonist antiemetic, a subtype of serotonin receptor capable of controlling nausea and vomiting by acting on receptors within the vagus nerve and CTZ, without the sedation that accompanies phenothiazines
- Reglan may also be considered an antiemetic drug as a result of its antagonism of central and peripheral dopamine receptors
What are indications for antiemetics
- Phenothiazines—effective in relieving vomiting associated with gastroenteritis, radiation sickness, and drug therapy, but they do not relieve motion sickness
- Antihistamine—suppresses nausea and vomiting associated with motion sickness, drug or radiation therapy, or following surgery
- Trimethobenzamide hydrochloride—effective for the treatment of postoperative nausea and vomiting and nausea associated with gastroenteritis
- Ondansetron—a preferable choice for long term use such as chemotherapy
What are adverse effects of antiemetics
- Phenothiazines—sedation, hypotension, restlessness, dry mouth, blurred vision, constipation, and muscle twitching, they should be used only when non-drug antiemetic measures or other drugs fail
- Antihistamines—drowsiness
- Trimethobenzamide hydrochloride—dizziness, headache, rash, Parkinson-like symptoms, muscle cramps and seizures
- Ondansetron—headache, drowsiness, diarrhea, fatigue, dystonia, hypotension, cardiac arrhythmias, atrioventricular (AV) block, and Steven-Johnson syndrome
- Metoclopramide has been associated with an increased risk of extrapyramidal movement disorders such as tardive dyskinesia
What are contraindications of antiemetic drugs
- Phenothiazine—asthma, benzyl alcohol hypersensitivity, phenothiazine hypersensitivity, sulfate hypersensitivity, CNS depression, leukopenia, seizure disorder, tardive dyskinesia, a history of urinary retention, and previous coronary disease, liver disease, or pulmonary disease
- Antihistamine—renal and liver disease, a history of urinary retention, coronary disease, hypertension, seizure disorder, narrow angle glaucoma, bowel obstruction, hyperthyroidism, asthma or COPD
- Trimethobenzamide hydrochloride—renal failure and impairment, hepatic disease, pregnancy, breastfeeding, encephalopathy, fever, Reye’s syndrome, or in geriatric or pediatric populations
- Ondansetron—hepatitis, liver disease, phenylketonuria, GI obstruction, coronary artery disease, electrolyte imbalance, alcoholism, bradycardia, or hypertension
- Metoclopramide—CHF, seizure disorder, tardive dyskinesia, Parkinson’s disease, GI bleeding, hypertension, pheochomocytoma, G6PD deficiency, or breast cancer (prolactin is increased by metoclopramide which may enhance tumor growth)
What are examples of antiemetic drugs
- Phenothiazines—chlorpromazine, thioridazine, fluphenazine, promazine
- Antihistamine—diphenhydramine
- Trimethobenzamide hydrochloride—Tigan
- Ondansetron
What are antiflatulent medications
Used to relieve painful symptoms of excess gas in the GI tract
What is the mechanism of actin for antiflatulent medication
These agents act by dispersing and preventing the formation of mucus-surrounded air or gas pockets in the GI tract
What are indications for antiflatulent medications
Relieve gas that may be caused by
1. Air swallowing
2. Postoperative gaseous distention
3. Peptic ulcer
4. Spastic or irritable colon
5. Diverticulosis
6. Infantile colic
What are adverse effects of antiflatulent medications
- Stool discoloration
- Diarrhea
- Nausea
What are contraindications of antiflatulent medications
Simethicone should not be taken with oral thyroid medications, as simethicone chelates with oral thyroid medications reducing thyroid absorption in the GI tract
Patients with phenylketouria must check for the presence of aspartame in the chosen drug preparation
What are examples of antiflatulent agents
Simethicone
What are antiparasitic agents
Combat the effects of intestinal parasites
What is the mechanism of action for antiparasitic agents
Metronidazole demonstrates antimicrobial activity with antibacterial, antiprotozoal, and anti inflammatory effects against a wide variety of bacterial and protozoan infections
What are indications for antiparasitic medications
1.Metronidazole is effective in treating bacterial and protozoan infections, including Bacterioides fragils (B.fragilis) infections and C.Diff-associated colitis, and as surgical prophylaxis.
2. Indications for uses of metronidazole in Crohn’s disease include perianal disease, Crohn’s colitis and sulfasalazine intolerance or allergy
3. Metronidazole has shown no benefit in the therapy of Ulcerative Colitis
4. Nitazoxanide (Alinia) is another drug effective in the treatment of Cryptosporidiosis or giardiasis caused by cryptosporidium parvum or Giardia lamblia. It has been used effectively for rotavirus, C.Diff and the eradication of H.pylori
What are adverse effects of antiparasitic agents
- Nitazoxanide—headache, nausea, diarrhea, abdominal pain, and sinus tachycardia
- Metronidazole—headache, nausea, Pruritus, candidia, Stevens-Johnson syndrome, seizures, elevated liver function tests (LFTs) and cardiac arrhythmias
What are contraindications of antiparasitic agents
- Metronidazole—us with caution in patients with liver and renal failure and a history of alcoholism or in patients on corticosteroid therapies. Patients with a history of CAD, arrhythmia, electrolyte imbalance, sodium restriction, and newly diagnosed primary malignancy should be monitored carefully
- Nitazoxanide—use with caution in patients with renal and hepatic or biliary disease. Insufficient data is available regarding use in pregnancy, breastfeeding, and pediatric and geriatric populations
What are some examples of antiparasitic agents
- Metronidazole
- Nitazoxanide
What are antifungal agents
They combat the effects of fungal infections
What are indications of antifungal agents
Effective against
1. Oropharynx
2. Esophageal
3. Vaginal
Fungal infections
Patients may be predisposed due to disease and drugs
What are some examples of antifungal agents
- Nystatin—available as an oral tablet or suspension and topical cream, powder, or ointment
- Clotrimazole—available OTC as topical cream or solution, oral lozenge, or vaginal cream
- Ketoconazole—available as an oral tablet and topical cream, foam, gel, or shampoo
- Itraconazole—available as an oral solution or tablet
- Amphotericin-B—available as an injectable
- Fluconazole—available as an oral table or suspension
What are anti-ulcer agents
The classes of drugs used as antiulcer agents include:
1. Antacids
2. Anticholinergics agents
3. H2 blockers
4. Sucralfate (Carafate)
5. Prostaglandins
6. Proton Pump Inhibitors (PPIs)
What is the mechanism of action for anti-ulcer agents
Promote healing by reducing gastric acid secretion, buffering secreted gastric acid, and/or enhancing intrinsic mucosal defenses
- H2 blockers—reduce the secretion of gastric acid by blocking histamine’s action on the H2 receptors in the parietal cells
- Sucralfate (Carafate)—is a basic aluminum salt of sucrose octasulfate, which forms a viscous adhesive gel that adheres to the ulcer crater, preventing further digestive action by both acid and pepsin
- Synthetic prostaglandins have both antisecretory and cytoprotective effects
- Proton Pump Inhibitors (PPIs)—provide more complete control of acid than H2 blockers. PPIs are prodrugs and need to be administered 30 minutes prior to eating in order to maximally activate proton pump blockade
What are the indications for antiulcer agents
- H2 Blockers—reduce the secretion of gastric acid and may also be used to reduce gastric acidity in patients with upper GI bleeding that stems from a peptic ulcer
- Sucralfate—has been approved for the treatment of duodenal ulcers but not for gastric ulcers
- Prostaglandins—may be used to prevent the gastric ulcers and mucosal injury that have been associated with the use of non steroidal anti-inflammatory drugs (NSAIDs)
- PPIs—are the most effective agents in the therapy of GERD. Use of these agents is indicated for the treatment of patients with erosive esophagitis or active duodenal ulcers. Long-term treatment may be indicated in some hypersecretory conditions such as Zollinger-Ellison syndrome, systemic mastocytosis, chronic erosive esophagitis, and Barrett’s esophagus
- omeprazole and Lansoprazole may be used in combination with Clarithromycin and amoxicillin in patients with positive H.pylori infection
What are adverse effects of anti-ulcer agents
- H2 blockers—the most common side effects of H2 blockers are diarrhea, headaches, dizziness, fatigue, muscle pain, rash, impotence, mild gynecomastia, leukopenia, and thrombocytopenia
- Sucralfate—the main side effect of sucralfate is constipation, which occurs in approximately 2% of patients who take this drug. Other rare side effects include dizziness, vertigo, sleepiness, dry out, skin rashes, Pruritus, back pain, diarrhea, nausea, gastric discomfort and indigestion
- Prostaglandins—the most common side effect of prostaglandins is diarrhea, followed by abdominal pain
- PPIs—patients taking anticoagulants, anticonvulsants, or diazepam along with a PPI will require special monitoring because of potential drug-drug interactions
- adverse reaction to PPIs may include—abdominal pain, asthenia, constipation, diarrhea, nausea, vomiting and headaches
-although rare—several severe adverse reactions have been attributed to long term use and include an increased risk of fractures, hypomagnesemia, thrombocytopenia, vitamin B12 deficiency (especially in patients with Ellison-Zollinger Syndrome), interstitial nephritis, enteric infections (including C.Diff) and neoplasm
-there is some concern that prolonged use may contribute to increased cardiovascular risk and dementia
What are contraindications for the use of anti-ulcer agents
- Increases in H2 blocker drug therapy may increase or produce a confused state in women who are breastfeeding, patients with renal and hepatic disease, and the geriatric population
- Sucralfate is contraindicated in patients with renal failure and in patients with dysphagia where aspiration is a potential risk. It should be used with caution in patients with diabetes due to the glucose content of the drug
- Because of its abortifacients properties, Misoprostol is contraindicated in pregnant women and generally is not recommended for women of child-bearing age
- PPIs should be used with caution in patients with known liver disease, osteoporosis, vitamin B12 deficiency and hypomagnesemia
What are examples of anti-ulcer agents
- H2 blockers—cimetidine (Tagamet HB), famotidine (Pepcid, Pepcid AC), Nizatidine (Axid AR), and ranitidine (Zantac) depending on the drug they are available OTC or at prescription doses
- Sucralfate (Carafate)
- Prostaglandins —Misoprostol (cytotec)
- Proton Pump Inhibitors (PPIs)—omeprazole (Prilosec), Lansoprazole (Prevacid), Pantoprazole (Protonix), Rabeprazole (AcipHex), Esomeprazole (Nexium), and Dexlansoprazole (Dexilant). Many of these PPIs are now available OTC
What are corticosteroids
Are used in gastroenterology practice primarily for their anti-inflammatory properties
What are indications for corticosteroids
- Treatment of inflammatory conditions, such as IBD, autoimmune hepatitis, collagenous sprue, severe cases of celiac disease, collagenous colitis, and radiation injury
- Possible relief of dysphagia in patients with benign esophageal strictures of various causes following intralesional injection therapy
- Crohn’s disease, including proctitis or distal colitis
What are adverse effects of corticosteroids
- Patients on prolonged corticosteroid therapy should be monitored for signs of Cushing’s syndrome, which is characterized by rapidly developing adipose deposition of the face, neck and trunk; kyphosis; hypertension; diabetes mellitus; amenorrhea, hypertrichosis; impotence; osteoporosis, bruising, mood alteration; insomnia; muscular wasting and weakness
- Because of the immunosuppressive nature of corticosteroids, patients must be monitored for infection and cautioned to avoid exposure to infectious disease. The physician should be notified of such exposures (such as chicken pox). The physician should be consulted before the patient considers receiving immunizations prepared with live virus (e.g., measles, mumps, rubella, varicella, and oral polio vaccines and nasal flu vaccine)
What are contraindications of corticosteroids
- Should not be used in patient with concurrent bacterial or viral infection, communicable disease (varicella, measles, tuberculosis), myasthenia gravis, or recent acute myocardial infarction, or while on anticholinesterase agents
What are examples of corticosteroids
- Hydrocortisone
- Prednisone
- Synthetic analogs such as prednisolone and methylprednisolone (Medrol, Solu-Medrol injectable, Depo-Medrol injectable, and Medrol oral tabs)
- Triamcinolone acetonide (Kenalog, Trisence injectable) and triamcinolone hexacetonide (Aristospan)
What are immunomodulators
Medications used to regulate or normalize the immune system in an effort to promote disease control or remission
They are immunosuppressants that weaken the immune response, which appears to be overactive in patients with IBD
What is the mechanism of action for immunomodulators
- Have a “steroid sparing” effect, allowing the patient to eventually discontinue the use of corticosteroids
What are the indications for use of immunomodulators
- Used in IBD when the patient is unable to wean or discontinue corticosteroids without exacerbation symptoms
- Cyclosporine has a more rapid onset of action Than Mercaptopurine or Azathioprine. Tacrolimus and cyclosporine have been effective in treating severe ulcerative colitis until either one of the slower immunomodulators begins to work or surgery is performed
- Tacrolimus is often used in Crohn’s disease when corticosteroids proved ineffective or fistula development is present
What are adverse effects of immunomodulators
- Because of the tendency for immunomodulator medications to suppress bone marrow activity, it is vital that patients be instructed to keep all follow-up appointments with their physician and to have laboratory studies drawn when requested
- Patients on an immunomodulator regimen should avoid exposure to communicable illness and should see a physician promptly when ill. Annual flu shots are a must for people who take these medications. Other immunizations should be discussed with the physician because immunizations prepared with live virus should be avoided. Parents who are taking immunomodulators should check with their child’s pediatrician before their child receives oral polio vaccine because the virus is shed in stool and urine for a period of time following immunization
What are contraindications of immunomodulators
- Some immunomodulator agents have a teratogenic effect
- Women considering pregnancy should consult their physician while taking these drugs
What are examples of immunomodulator agents
- Mercaptopurine
- (6-MP, Purinethol)
- Azathioprine (Imuran)
- Cyclosporine
- Methotrexate
- Tacrolimus (Prograf)
What are agents used in diagnostic tests
A number of different pharmacological agents may be used in the diagnosis of GI disorders
What is the mechanism of action of agents used in diagnostic tests
These agents are used in a variety of ways to improve data collection and visualization during the diagnostic and therapeutic exams
What are indications for agents used in diagnostic tests
- Penagastrin - stimulates gastric acid secretion
- Secretin (chirhostim-secretin) stimulates pancreatic secretions to aid in the diagnosis of pancreatic exocrine dysfunction. It can be used to stimulate gastric secretions to aid in the diagnosis of Gastrinomas
- Edrophonium chloride (Enron injectable), a cholinergic agent, is used for provocative testing in patients with non cardiac chest pain
- Glucagon is used in diagnostic tests and therapeutic procedures, primarily to reduce GI motility
- Sincalide (Kinevac), the GI hormone cholecystokinin, is given by exogenous administration and may be used in diagnostic procedures in which gallbladder contraction is desired
What are adverse effects of agents used in diagnostic tests
Adverse effects vary by medication
- Pentagastrin—often produces nausea, vomiting, increased gastric distress, and abdominal cramping
- Secretin—nausea, vomiting, GI distress, and flushing
- Edrophonium—watery eyes, muscle twitching, nausea, vomiting, and diarrhea
- Glucagon—rash, urticaria, and respiratory distress
- Sincalide—cramping, nausea, headache, shortness of breath, and flushing
What are contraindications of agents used in diagnostic tests
- Pentagastrin—concurrent medication use, especially antacids, anticholinergics, H2-receptor antagonist, or PPIs and acute bleeding peptic ulcer
- Secretin—patients with a history of liver disease, as they may be hyper reactive to secretin. Patients with a history of IBD or vagotomy may be hyporeactive to secretin, giving a false positive to testing. Alternative diagnostic testing should be considered
- Edrophonium—bowel or urinary obstruction, narrow angle glaucoma, and pyloric stenosis
- Glucagon—Insulinoma and pheochromocytoma
- Sincalide—Cholelithiasis, as this can lead to common bile duct (CBD) obstruction
What are gallstone therapeutic agents
- Ursodexycholic acid or ursodiol (Actigall, Urso 250, Urso Forte) is an agent that may dissolve cholesterol gallstones
- Urso 250 and Urso Forte oral tabs are available in different strengths
What is the mechanism of action for gallstone therapeutic agents
- Ursodiol decreases the rate of secretion of cholesterol into bile, thus causing the bile to become desaturated with cholesterol
- This unsaturated bile dissolves cholesterol molecules from gallstones and holds them in micellar or vesicular solution until gallbladder contraction discharges them into the duodenum
- Therapy must be continued until the stones dissolve completely, typically in 6-24 months
What are indications for gallstone therapeutic agents
- The efficacy of medical dissolution therapy differs according to the size of the gallstone and length of therapy
- Studies show the disappearance of stones with a diameter of less than 5mm in about 90% of cases, whereas the chance of dissolution is approximately 40-50% for larger or multiple stones
- Ursodeoxycholic acid studies have shown clinical significance in treatment of postcholecystectomy microlithiasis, also referred to as sludge, biliary San, and biliary sediment, and reversible Cholelithiasis
- Clinical conditions associated with the formation of microlithiasis are prolonged fasting, total Parenteral nutrition (TPN), rapid weight loss, pregnancy, and chronic illness
What are adverse effects to gallstone therapeutic agents
- Abdominal pain
- Diarrhea
- Headache
- Fatigue
What are contraindications of gallstone therapeutic agents
- Ursodiol is contraindicated for patients without patent cystic ducts
- Women who are or may be pregnant
- Patients with radiopaque(pigment) stones
- Cholangitis
- Biliary obstruction
- Biliary-gastrointestinal fistula
- Stones that are larger than 15mm in diameter
What are laxatives
Laxatives are classified into six primary categories
1. Bulk
2. Stool softener
3. Osmotic
4. Saline
5. Enema
6. Stimulant
What is the mechanism of action for bulking agent laxatives
- Hold on to water and soften stool, making it easier to pass, which is particularly important in patients with Anorectal disorders
- These agents are also used to relieve chronic constipation
- The best example of a bulking agent is the nonabsorbable complex carbohydrate called fiber
- Other examples including bulking agents that contain processed husk glom psyllium (Metamucil, Konsyl); agents based on methylcellulose, a synthetic fiber (e.g. Citrucel); and a complex nonabsorbable starch-calcium polycarbophil (Fibercon)
- The addition of natural fiber from fruits and vegetables to the diet has the same bulking effect
What is the mechanism of action for stool softener and emollients
Lubricating agents prevent the stool from becoming compacted and dry by:
1. Lowering the surface tension, thus allowing the fecal mass to be penetrated by intestinal fluid
2. Acting as surfactants that soften the fecal mass by facilitating the mixture of aqueous and fatty substances
3. Inhibiting fluid and electrolyte reabsorption by the intestine
4. Increasing the secretion of water, both in the small bowel and the colon
These agents include mineral oil, docusate sodium (colace) and a combination of fiber and mineral oil in emulsion form (Kondremul)
The absorption of the fat-soluble vitamins A,D,E, and K appear to be moderately reduced with prolonged use of mineral oil, but there appears to be no significant clinical significance when used in limited quantities as directed
What is the mechanism of action for osmotic laxatives
- Osmotic laxatives are largely nonabsorbable sugars, thus making sugar a high concentration in the bowel
- Water from the tissues moves into the bowl to equalize the osmotic pressure and increase the bulk
- This results in increased colonic peristalsis
- Types of osmotic laxatives include:
- lactulose (enulose, kristalose)—most osmotic laxatives are disaccharides
- sorbitol—a non-soluble sugar
- sodium phosphate mono basic mono hydrate (osmo-prep)—often referred to as the pill prep. It lost favor because of documented cases of renal failure associated with its use
-Glycerin—a naturally occurring trivalent alcohol suppository that acts via hyperosmotic action and a local irritation and lubrication
- Polyethylene glycol (CoLyte, GoLytely, NyLytely)—an example of a polyethylene glycol 3350 (PEG-3350) and electrolytes colon lavage preparation that may be administered orally or by nasogastric tube infusion. Miralax, Plenvu, and MoviPrep also contain PEG-3350
- Sodium sulfate, potassium sulfate, and magnesium sulfate (Suprep)—an osmotic laxative intended for cleansing the colon prior to colonoscopic exam
- Clenpiq (sodium picosulfate, magnesium oxide, and anhydrous citric acid) oral solution—a stimulant and osmotic laxative intended for colon preparation prior to procedure
What is the mechanism of action for saline laxatives
- Increase the intraluminal pressure by attracting and retaining water in the small intestine and colon and inducing contractions
- The most common saline laxative is magnesium salts—magnesium hydroxide (milk of magnesia) and magnesium citrate
- Magnesium hydroxide also stimulates the release of cholecystokinin, which increases intestinal secretion and stimulates peristalsis and transit
What is the mechanism of action of enemas
- Primarily work by inducing evacuation as a response to colonic distention and by lavage
- They soften the stool by preventing colonic reabsorption of fecal fluid resulting from creation of a barrier between the feces and the colon
- They also have a lubricant effect that eases the passage of feces through the intestines
- Mineral oil retention enemas also work by lubricating the rectum and colon
- Soap sud enemas provide an irritant action that stimulates peristalsis
What is the mechanism of action of stimulant laxatives
- Work by directly signaling the muscles and nerve plexus of the intestines to contract and expel their content
- These laxatives include:
- a derivative of the senna leaf (Senokot)
- alkaloid chemicals such as bisacodyl (Ducolax)
- a combination of sodium picosulfate, magnesium oxide, and anhydrous citric acid (Prepopik), an oral stimulant laxative intended for the preparation of the colon prior to a diagnostic exam
What are the indications for use of laxatives
Laxatives vary in indication. They may be used to:
1. Cleanse the bowel before Radiographic examination, colonoscopy, flexible or rigid sigmoidoscopy, or surgery
2. Eliminate a substance from the GI tract
3. Prevent straining
4. Obtain a stool specimen
5. Treat constipation
For patients who experience irritable bowel syndrome with constipation (IBS-C) and for whom laxatives and bulking agents are ineffective, medications such as linaclotide(Linzess) may be trialed.
Linaclotide is a guanylate cyclase-C agonist
What are adverse effects of laxatives
- None of the bulking or lubricating agents or osmotic laxatives carries long-term side effects. Results vary from 5 minutes to several days
- Side effects of osmotic preparations include headache, nausea, vomiting, bloating, electrolyte imbalance, and dehydration
- Stimulant laxatives may be habit forming, necessitating increasingly higher doses to produce the same stimulation effect
- Side effects of Prepopik include headache, nausea, vomiting, bloating, electrolyte imbalance, and dehydration
- The most significant side effect of Linaclotide is diarrhea