Loperamide chemical structure
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Loperamide

Loperamide, usually as hydrochloride, is a drug effective against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically under brand names such as Lopex®, Imodium®, Dimor® and Pepto® Diarrhea Control. more...

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Mode of action

Loperamide is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids.

It works by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.

Loperamide does not cross the blood-brain barrier and has no analgesic properties or addictive potential. Tolerance in response to long-term use has not been reported.

Contraindications

Treatment should be avoided in the presence of fever or if the stool is bloody. Treatment is not recommended for patients who could suffer detrimental effects from rebound constipation. If there is a suspicion of diarrhea associated with organisms that can penetrate the intestinal walls, such as E. coli O157:H7 or salmonella, loperamide is contraindicated.

Side-effects

Side effects can include the following: drowsiness, constipation, abdominal pain or discomfort, dry mouth, fatigue, and in rare cases toxic megacolon.

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Gut feeling: irritable bowel syndrome affects up to 20 percent of Americans. Herbs, supplements, nutrition, and hypnosis can get your insides back on track
From Natural Health, 11/1/05 by Kathleen Doheny

IT'S 2005, AND WE'LL TALK about anything. From fetishes to toenail fungus, maximum frankness pervades chat shows and chat rooms. Yet only about half of Americans with irritable bowel syndrome discuss their symptoms with their doctors, says gastroenterologist G. Richard Locke, M.D., professor of medicine at the Mayo Clinic College of Medicine in Rochester, Minn. When they do, it's because the constipation, diarrhea, or pain has gotten so disruptive that it's affecting their ability to function on the job, dine out, or exercise.

"Some people don't find their IBS symptoms bothersome or unusual, and some may be a little shy about talking to a doctor about bowel problems," Locke says. These silent sufferers remain unaware there's a growing array of strategies to help them achieve inner peace.

do you have IBS?

IRRITABLE BOWEL SYNDROME is a combination of symptoms that may consist of abdominal pain, cramps, bloating, flatulence, mucus in the stools, food intolerances, and constipation or diarrhea (often alternating between the two). The diagnostic criteria include having abdominal pain or discomfort for at least 12 weeks out of the previous 12 months, not necessarily consecutively. Generally, pain is relieved after a bowel movement; the frequency of bowel movements alters when pain or discomfort begins; and/or there are changes in the form or appearance of the stool.

"For most people, symptoms occur now and then, a couple of days a week or so," says Locke. "To meet the definition of IBS, you have to have the symptoms 25 percent [or more] of the time."

IBS isn't caused by structural or biochemical abnormalities. Instead, it appears to be a functional disorder stemming from a disturbance in the interaction between the digestive tract, the brain, and the autonomic nervous system. As a result, the motility of the colon may be disrupted: It can move too fast, resulting in diarrhea, or too slow, resulting in constipation; sometimes it's spasmodic.

"IBS used to be called spastic colon or spastic colitis, but those terms are not accurate," says Lin Chang, M.D., an associate professor of medicine in the division of digestive diseases at UCLA's David Geffen School of Medicine, and a member of the advisory board of the nonprofit International Foundation for Functional Gastrointestinal Disorders. "'Colitis' means inflammation of the colon, and that's not true in IBS."

IBS is also confused with a category of conditions known as inflammatory bowel disease. (See "What's Happening Down There?" on page 59.) The good news is that IBS has not been linked to more serious bowel problems; nor does it raise the risk of colon cancer.

"IBS is not a life-threatening condition, but it is a nuisance," says Keith Bruninga, M.D., a gastroenterologist at Rush University Medical Center in Chicago. And it can take a financial and emotional toll, with patients reporting missed workdays, feelings of nervousness or hopelessness, sleep problems, low energy, and reduced sexual interest.

"You don't know when it's going to come on," notes Chang. "You don't know how long it's going to last, and you don't know what might trigger it. It's constant anticipation."

No one can say for sure why one person gets IBS and another escapes it. R affects more women than men, and chronic stress seems to be a factor, including a history of physical, sexual, or verbal abuse; parental divorce; or parental alcoholism. "We think there is this early, adverse life event [that boosts IBS risk]," says Chang.

The condition isn't "all in your head," but stress and emotions can affect the colon, since its many nerves connect it to the brain. "People who are prone to anxiety, who hold stress in, tend to be more likely to have problems with IBS," says Peter Galier, M.D., chief of staff at Santa Monica UCLA Medical Center.

mix-and-match strategies

NO SINGLE METHOD works for everyone, so treatment responses are multifaceted. "The initial management of IBS is really about managing your lifestyle," says Locke. "People need to pay attention to stress in their lives." Regular exercise is recommended; "it also tends to help if you eat smaller amounts of food frequently rather than large meals," Locke adds.

After that, treatment is based on whether diarrhea or constipation is predominant. For mild symptoms, you can self-treat, says Locke, using milk of magnesia for constipation and nonprescription Imodium (loperamide) for diarrhea. If symptoms worsen, consider the following options:

Pull the triggers. Steer clear of foods that exacerbate your symptoms. Among the common culprits are greasy foods, milk products, alcohol, chocolate, and caffeinated beverages. "Up to 50 percent of patients will relate a worsening of symptoms to specific foods," Chang says.

Fiber up. It might sound counterintuitive, but increasing fiber aids both diarrhea-predominant and constipation-predominant IBS. "Fiber has water-holding capacity, so it bulks up the stool," Bruninga says, explaining how it can ease diarrhea. "And it can also help bring fluid into the bowel," lessening constipation.

Focus on fiber-rich foods, like fruits and vegetables, or consider adding a fiber supplement. "Take Metamucil or Fibercon twice a day," advises Galier. Since taking too much fiber too quickly can cause bloating, start small and gradually work your way up to the dosage recommended on the package.

Go pro(biotics). These microorganisms, believed to make the intestinal environment friendlier by populating it with "good" bacteria, may be worth a try, especially if abdominal bloating is a problem, says H. Jae Kim, M.D., an assistant professor of medicine at the Mayo Foundation in Scottsdale, Ariz. In a placebo-controlled study on the probiotic formula VSL#3, funded by the supplement maker and published in Alimentary Pharmacology and Therapeutics, Kim gave patients with diarrhea-predominant IBS supplements containing 225 billion bacteria twice a day for eight weeks. While the probiotics had no effect on abdominal pain, flatulence, or bowel urgency, there was significant improvement in bloating. "Improvement was noted within the first week," he reports.

Kim believes the amount used in the study would be a reasonable dose for people to try, since there were no significant side effects among the participants. However, typical probiotic formulas deliver only 1 to 4 billion bacteria per day. "Whether 1 billion or 2 billion is as good as 450 billion, I don't know," says Kim. "Without having a controlled trial, you can't conclude anything from using low doses." (To get the formula used in the study, go to vsl3.com.)

Root up ginger. Ginger is often recommended as a general aid for digestion and remedy for diarrhea and stomach upset. For indigestion, take either a daily dose of 2 to 4 grams of the fresh root, 0.25 to 1 gram of the powdered root, or 1.5 to 3 milliliters of tincture.

Think mint. Taking capsules of peppermint off reduces gas and abdominal pain and distension, according to a study in the Journal of Gastroenterology. Participants took one peppermint capsule three to four times a day about 30 minutes before meals for one month; 79 percent of them reported reduction of abdominal pain, compared to 43 percent of those on a placebo. The mint group also experienced less gas and bloating, as well as a decrease in stool frequency.

"Peppermint oil has been very effective for a lot of patients with IBS," says Drew Francis, O.M.D., a licensed medical herbalist and owner of the Golden Cabinet Medical Healing Center in Los Angeles. Francis suggests trying two 200-milligram capsules three times a day before meals. Look for enteric-coated capsules, which target the intestine more effectively, he adds.

Order Chinese. In a study published in the Journal of the American Medical Association, researchers gave IBS patients a Chinese herbal formula containing licorice, ginger, and 18 other ingredients; a similar mix tailored to specific symptoms; or a placebo. Seventy-six percent of those taking the standard blend and 64 percent of those on the tailored blends said their symptoms improved after four months of use, compared to 33 percent of the placebo group.

The standard formula used in the study, called IBS-F, is made by Brion Herbs (brionherbs.com) and is available only through healthcare professionals. To find a practitioner of Chinese medicine in your area, log on to aaom.org. Francis, who is familiar with the study, says the dose used--five capsules three times a day--is ideal.

Take a stab at needles. Using acupuncture for IBS has shown conflicting results. In one small study published in Hepatogastroenterology, participants reported significant improvement in well-being and reduction of bloating symptoms. Yet a study published in Digestion found no improvement in patients given acupuncture at the LI-4 colonic meridian or a placebo. Chang remains open to the idea, and to combining acupuncture with medication.

Psych out tension. "Stress reduction helps," says Locke, who recommends that IBS patients enroll in the stress-management classes offered by community hospitals. "They can evaluate how you respond to stress and teach you techniques for dealing with it."

Hypnosis might be the most effective tool for relaxation and soothing symptoms, asserts Olafur Palsson, Psy.D., an associate professor of medicine in the division of gastroenterology and hepatology at the University of North Carolina at Chapel Hill. Citing several published studies, Palsson says the response rate to hypnosis is 80 percent or better. On his public information Web site, IBShypnosis.com, he offers a list of practitioners. (For a do-it-yourself hypnosis technique, see "Visualize Inner Peace" on page 52.)

Mull over medications, Like other treatments, IBS drug protocols are tailored to whether cases are diarrhea-predominant or constipation-predominant. For the latter, Zelnorm (tegaserod maleate) has been approved by the FDA. For diarrhea, Lotronex (alosetron hydrochloride), previously pulled off the market for its association with decreased blood flow to the colon and constipation, has been re-approved for women who have not responded to conventional treatments. Lotronex should be "cautiously prescribed" due to these potential side effects, Locke says.

Antispasmodic medications, such as hyoscyamine sulfate (Anaspaz, Levsin, Levbid), can help if bowel spasms occur, adds Locke. A low dose of antidepressants may be useful as well, not by lifting depression, but because they block the brain's perception of gut pain.

In the search for the right mix of treatments, persistence and patience pay off. You may have to go through a period of trial and error, but chances are good that you can lead a normal, productive life. As Locke says, "You don't have to suffer with IBS."

VISUALIZE INNER PEACE

Hypnosis is effective for improving the signs of IBS, says Olafur Palsson, Psy.D. He offers this visualization technique for DIY relief:

1. Sit comfortably in a chair in a quiet place. Look all the way up into your eyebrows, as far up as your eyes can comfortably go.

2. Hold your eyes in this position and let your eyelids close slowly. Inhale deeply and hold your breath for a few moments.

3. Relax your eyes (which stay closed), exhale slowly, and concentrate on the feeling of sinking deep into your chair as your whole body relaxes.

4. Breathe slowly and regularly. With every exhalation, imagine yourself sinking further into the chair, as if your body is gradually deflating.

5. When you are relaxed, begin to visualize your intestines as a river flowing through your body at a smooth, steady pace--no matter what's happening on the surrounding banks. Picture it as vividly as you can; dwell on the image for a while.

6. To finish, count back slowly in your mind from 3 to 1, imagining your body waking with each inhalation and filling with energy that will make you feel good for the rest of the day. At the count of 1, open your eyes and say to yourself, "Wide awake!" This will bring you into an alert state.

WHAT'S HAPPENING DOWN THERE?

Irritable bowel syndrome (IBS) is often confused with other intestinal conditions. Here's a quick glossary:

IBD Inflammatory bowel disease is a category encompassing more serious conditions than IBS. It includes ulcerative colitis, which causes ulcers and inflammation in the inner lining of the colon and the rectum, and Crohn's disease, where inflammation in the small intestine can extend through the bowel wall. Both are accompanied by sometimes-bloody diarrhea and may require surgery.

Diveticulitis Small pouches in the colon called diverticula become irritated or infected. Symptoms include abdominal pain, bloating, gas, fever, chills, and nausea.

Celiac disease Also called celiac sprue, this autoimmune disorder is marked by the inability to digest a gluten protein found in wheat, oats, barley, and rye. Its presence triggers an attack on the small intestine, blocking the absorption of nutrients.

COPYRIGHT 2005 Weider Publications
COPYRIGHT 2005 Gale Group

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