Laxative#Hyperosmotic agents

Bulk-forming laxatives, also known as roughage, are substances, such as fiber in food and hydrophilic agents in over-the-counter drugs, that add bulk and water to stools so they can pass more easily through the intestines (lower part of the digestive tract).[http://www.cancer.gov/dictionary?CdrID=489403 Bulk-forming agent] entry in the public domain NCI Dictionary of Cancer Terms

Properties

• Site of action: small and large intestines
• Onset of action: 12–72 hours
• Examples: dietary fiber, Metamucil, Citrucel, FiberCon{{cite book|vauthors=Berardi M, Tietze KJ, Shimp LA, Rollins CJ, Popovich NG |title=Handbook of Nonprescription Drugs|date=2006|publisher=American Pharmaceutical Association|location=Washington, D.C.|isbn=978-1582120744|edition=15th}}

Bulk-forming agents generally have the gentlest of effects among laxatives, making them ideal for long-term maintenance of regular bowel movements.

Foods that help with laxation include fiber-rich foods. Dietary fiber includes insoluble fiber and soluble fiber, such as:{{cite web|title=The Facts About Fiber|url=http://www.aicr.org/assets/docs/pdf/brochures/facts-about-fiber.pdf|website=www.aicr.org|publisher=American Institute for Cancer Research|access-date=3 November 2014|archive-date=3 November 2014|archive-url=https://web.archive.org/web/20141103115438/http://www.aicr.org/assets/docs/pdf/brochures/facts-about-fiber.pdf|url-status=dead}}

• Fruits, such as bananas,{{cite journal|last=Das|first=JL|title=Medicinal and nutritional values of banana cv. NENDRAN|journal=Asian Journal of Horticulture|year=2010|volume=8|pages=11–14|url=http://www.cabdirect.org/abstracts/20103272020.html;jsessionid=2B9A2FDF37186F0DA0A347FF227D606D|access-date=2012-11-29|archive-date=2014-11-03|archive-url=https://web.archive.org/web/20141103120544/http://www.cabdirect.org/abstracts/20103272020.html;jsessionid=2B9A2FDF37186F0DA0A347FF227D606D|url-status=dead}} though this depends on their ripeness,{{Cite news|url=http://www.medicinenet.com/top_foods_that_cause_constipation/page2.htm|title=15 Foods That Cause Constipation (Caffeine, Chocolate, Alcohol)|work=MedicineNet|access-date=2017-12-12|language=en}} kiwifruits,{{cite journal |vauthors=Rush EC, Patel M, Plank LD, Ferguson LR | title = Kiwifruit promotes laxation in the elderly. | journal = Asia Pac J Clin Nutr | volume = 11 | issue = 2 | pages = 164–8 | year = 2002 | pmid = 12074185 | doi = 10.1046/j.1440-6047.2002.00287.x | s2cid = 15280086 }} prunes,{{cite journal |vauthors=Stacewicz-Sapuntzakis M, Bowen PE, Hussain EA, Damayanti-Wood BI, Farnsworth NR | title = Chemical composition and potential health effects of prunes: a functional food? | journal = Critical Reviews in Food Science and Nutrition | volume = 41 | issue = 4 | pages = 251–86 | year = 2001 | pmid = 11401245 | doi = 10.1080/20014091091814 | s2cid = 31159565 }} apples (with skin), pears (with skin), and raspberries
• Vegetables, such as broccoli, string beans, kale, spinach, cooked winter squash, cooked taro and poi, cooked peas, and baked potatoes (with skin)
• Whole grains
• Bran products
• Nuts
• Legumes, such as beans, peas, and lentils

Emollient laxatives, also known as stool softeners, are anionic surfactants that enable additional water and fats to be incorporated in the stool, making movement through the bowels easier.

Properties

• Site of action: small and large intestines
• Onset of action: 12–72 hours
• Examples: Docusate (Colace, Diocto), Gibs-Eze

Emollient agents prevent constipation rather than treating long-term constipation.

Lubricant laxatives are substances that coat the stool with slippery lipids and decrease colonic absorption of water so the stool slides through the colon more easily. Lubricant laxatives also increase the weight of stool and decrease intestinal transit time.{{cite book |title=Handbook of Nonprescription Drugs |vauthors=Berardi M, Tietze KJ, Shimp LA, Rollins CJ, Popovich NG |date=2006 |publisher=American Pharmaceutical Association |isbn=978-1582120744 |edition=15th |location=Washington, D.C.}}

Properties

• Site of action: colon
• Onset of action: 6–8 hours
• Example: mineral oil

Mineral oils, such as liquid paraffin, are generally the only nonprescription lubricant laxative available, but due to the risk of lipid pneumonia resulting from accidental aspiration, mineral oil is not recommended, especially in children and infants.{{Cite book |last=Krinsky |first=Daniel L. |url=https://pharmacylibrary.com/doi/book/10.21019/9781582123172 |title=Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care, 20th Edition |date=November 30, 2020 |publisher=The American Pharmacists Association |isbn=978-1-58212-317-2 |location=2215 Constitution Avenue, N.W. Washington, DC 20037-2985 |language=en |doi=10.21019/9781582123172.ch15}}{{Cite web |last=Bowles-Jordan |first=Jane |title=Constipation |url=http://proxycheck.lib.umanitoba.ca/libraries/online/proxy.php?http://www.e-therapeutics.ca/?p=mzLm9vCs3qxZyEUHPZaNJ7uOeM6sKtN-Az2x-dKQMNz0daKJqHkuaoQKNMbtytXe&logintype=auto&auto=true |access-date=March 20, 2020 |website=CPS}} Mineral oil may decrease the absorption of fat-soluble vitamins and some minerals.

===Hyperosmotic agents===

Hyperosmotic laxatives cause the intestines to hold more water, creating an osmotic gradient, which adds more pressure and stimulates bowel movement.{{cite book |title=Handbook of Nonprescription Drugs |vauthors=Berardi M, Tietze KJ, Shimp LA, Rollins CJ, Popovich NG |date=2006 |publisher=American Pharmaceutical Association |isbn=978-1582120744 |edition=15th |location=Washington, D.C.}}

Properties

• Site of action: colon
• Onset of action: 12–72 hours (oral), 0.25–1 hour (rectal)
• Examples: glycerin suppositories (Hallens), sorbitol, lactulose, and polyethylene glycol (PEG - Colyte, MiraLax)

Lactulose works by the osmotic effect, which retains water in the colon; lowering the pH through bacterial fermentation to lactic, formic, and acetic acids; and increasing colonic peristalsis. Lactulose is also indicated in portal-systemic encephalopathy. Glycerin suppositories work mostly by hyperosmotic action, but the sodium stearate in the preparation also causes local irritation to the colon.{{cn|date=March 2023}}

Solutions of polyethylene glycol and electrolytes (sodium chloride, sodium bicarbonate, potassium chloride, and sometimes sodium sulfate) are used for whole bowel irrigation, a process designed to prepare the bowel for surgery or colonoscopy and to treat certain types of poisoning. Brand names for these solutions include GoLytely, GlycoLax, Cosmocol, CoLyte, Miralax, Movicol, NuLytely, Suprep, and Fortrans. Solutions of sorbitol (SoftLax) have similar effects.{{cn|date=March 2023}}

Saline laxatives are nonabsorbable, osmotically active substances that attract and retain water in the intestinal lumen, increasing intraluminal pressure that mechanically stimulates evacuation of the bowel. Magnesium-containing agents also cause the release of cholecystokinin, which increases intestinal motility and fluid secretion. Saline laxatives may alter a patient's fluid and electrolyte balance.

Properties

• Site of action: small and large intestines
• Onset of action: 0.5–3 hours (oral), 2–15 minutes (rectal)
• Examples: sodium phosphate (and variants), magnesium citrate, magnesium hydroxide (milk of magnesia), and magnesium sulfate (Epsom salt)

Stimulant laxatives are substances that act on the intestinal mucosa or nerve plexus, altering water and electrolyte secretion.[http://www.mayoclinic.com/health/drug-information/DR602359 Laxative (Oral Route)] from Mayo clinic. Last updated: Nov. 1, 2012 They also stimulate peristaltic action and can be dangerous under certain circumstances.{{cite journal |vauthors=Joo JS, Ehrenpreis ED, Gonzalez L, Kaye M, Breno S, Wexner SD, Zaitman D, Secrest K | title = Alterations in colonic anatomy induced by chronic stimulant laxatives: the cathartic colon revisited | journal = J Clin Gastroenterol | volume = 26 | issue = 4 | pages = 283–6 | year = 1998 | pmid = 9649012 | doi = 10.1097/00004836-199806000-00014 }}

File:Cassia senna Ypey80-cropped.jpg

Properties

• Site of action: colon
• Onset of action: 6–10 hours
• Examples: senna, bisacodyl

Prolonged use of stimulant laxatives can create drug dependence by damaging the colon's haustral folds, making users less able to move feces through their colon on their own. A study of patients with chronic constipation found that 28% of chronic stimulant laxative users lost haustral folds over the course of one year, while none of the control group did.{{cite journal |last1=Joo |first1=Jae Sik |last2=Ehrenpreis |first2=Eli D. |last3=Gonzalez |first3=Leopoldo |last4=Kaye |first4=Mark |last5=Breno |first5=Susan |last6=Wexner |first6=Steven D. |last7=Zaitman |first7=Daniel |last8=Secrest |first8=K. |title=Alterations in Colonic Anatomy Induced by Chronic Stimulant Laxatives: The Cathartic Colon Revisited |journal=Journal of Clinical Gastroenterology |date=June 1998 |volume=26 |issue=4 |pages=283–286 |doi=10.1097/00004836-199806000-00014 |pmid=9649012 }}

Castor oil is a glyceride that is hydrolyzed by pancreatic lipase to ricinoleic acid, which produces laxative action by an unknown mechanism.

Properties

• Site of action: colon, small intestine (see below) {{citation needed|date=September 2018}}
• Onset of action: 2–6 hours
• Examples: castor oil

Long-term use of castor oil may result in loss of fluid, electrolytes, and nutrients.

These are motility stimulants that work through activation of 5-HT₄ receptors of the enteric nervous system in the gastrointestinal tract. However, some have been discontinued or restricted due to potentially harmful cardiovascular side effects.

Tegaserod (brand name Zelnorm) was removed from the general U.S. and Canadian markets in 2007, due to reports of increased risks of heart attack or stroke. It is still available to physicians for patients in emergency situations that are life-threatening or require hospitalization.{{cite web|url=https://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm103223.htm|title=Postmarket Drug Safety Information for Patients and Providers - Zelnorm (tegaserod maleate) Information|first=Center for Drug Evaluation and|last=Research|website=www.fda.gov|access-date=14 April 2018}}

Prucalopride (brand name Resolor) is a current drug approved for use in the EU since October 15, 2009,{{cite web|url=http://www.emea.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/001012/WC500053995.pdf|title=European Medicines Agency EPAR summary for the public|website=europa.eu|access-date=14 April 2018|archive-date=14 April 2018|archive-url=https://web.archive.org/web/20180414233759/http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/001012/WC500053995.pdf|url-status=dead}} in Canada (brand name Resotran) since December 7, 2011,{{cite web|url=http://www.hc-sc.gc.ca/dhp-mps/prodpharma/sbd-smd/drug-med/sbd_smd_2012_resotran_141157-eng.php#a2|title=Health Canada, Notice of Decision for Resotran|website=hc-sc.gc.ca|access-date=14 April 2018|archive-url=https://web.archive.org/web/20170318120956/http://www.hc-sc.gc.ca/dhp-mps/prodpharma/sbd-smd/drug-med/sbd_smd_2012_resotran_141157-eng.php#a2|archive-date=18 March 2017|url-status=dead}} and in the United States since December 2018.

Lubiprostone is used in the management of chronic idiopathic constipation and irritable bowel syndrome. It causes the intestines to produce a chloride-rich fluid secretion that softens the stool, increases motility, and promotes spontaneous bowel movements.

For adults, a randomized controlled trial found PEG (MiraLax or GlycoLax) 17 grams once per day to be superior to tegaserod at 6 mg twice per day.{{cite journal |vauthors=Di Palma JA, Cleveland MV, McGowan J, Herrera JL | title = A randomized, multicenter comparison of polyethylene glycol laxative and tegaserod in treatment of patients with chronic constipation | journal = Am. J. Gastroenterol. | volume = 102 | issue = 9 | pages = 1964–71 | year = 2007 | doi = 10.1111/j.1572-0241.2007.01365.x | pmid = 17573794 | s2cid = 32055676 }} A randomized controlled trial found greater improvement from two sachets (26 g) of PEG versus two sachets (20 g) of lactulose.{{cite journal |vauthors=Attar A, Lémann M, Ferguson A, Halphen M, Boutron MC, Flourié B, Alix E, Salmeron M, Guillemot F, Chaussade S, Ménard AM, Moreau J, Naudin G, Barthet M | title = Comparison of a low dose polyethylene glycol electrolyte solution with lactulose for treatment of chronic constipation | journal = Gut | volume = 44 | issue = 2 | pages = 226–30 | year = 1999 | pmid = 9895382 | pmc = 1727381 | doi = 10.1136/gut.44.2.226 }} 17 g per day of PEG has been effective and safe in a randomized, controlled trial for six months.{{cite journal |vauthors=Dipalma JA, Cleveland MV, McGowan J, Herrera JL | title = A randomized, multicenter, placebo-controlled trial of polyethylene glycol laxative for chronic treatment of chronic constipation | journal = Am. J. Gastroenterol. | volume = 102 | issue = 7 | pages = 1436–41 | year = 2007 | doi = 10.1111/j.1572-0241.2007.01199.x | pmid = 17403074 | s2cid = 10946562 }} Another randomized, controlled trial found no difference between sorbitol and lactulose.{{cite journal |vauthors=Lederle FA, Busch DL, Mattox KM, West MJ, Aske DM | title = Cost-effective treatment of constipation in the elderly: a randomized double-blind comparison of sorbitol and lactulose | journal = Am J Med | volume = 89 | issue = 5 | pages = 597–601 | year = 1990 | pmid = 2122724 | doi = 10.1016/0002-9343(90)90177-F }}

For children, PEG was found to be more effective than lactulose.{{cite web |url=http://www.bestbets.org/cgi-bin/bets.pl?record=00901 |title=BestBETs: Is polyethylene glycol safe and effective for chro... |access-date=2007-09-06 }}

Some of the less significant adverse effects of laxative abuse include dehydration (which causes tremors, weakness, fainting, blurred vision, kidney damage), low blood pressure, fast heart rate, postural dizziness and fainting; however, laxative abuse can lead to potentially fatal acid-base, and electrolyte imbalances. For example, severe hypokalaemia has been associated with distal renal tubular acidosis from laxative abuse. Metabolic alkalosis is the most common acid-base imbalance observed. Other significant adverse effects include rhabdomyolysis, steatorrhoea, inflammation and ulceration of colonic mucosa, pancreatitis,{{cite journal |vauthors=Brown NW, Treasure JL, Campbell IC | title = Evidence for long-term pancreatic damage caused by laxative abuse in subjects recovered from anorexia nervosa | journal = International Journal of Eating Disorders | volume = 29 | issue = 2 | pages = 236–238 | year = 2001 | pmid = 11429987 | doi = 10.1002/1098-108X(200103)29:2<236::AID-EAT1014>3.0.CO;2-G }} kidney failure,{{cite journal | author = Copeland PM | title = Renal failure associated with laxative abuse | journal = Psychother Psychosom | volume = 62 | issue = 3–4 | pages = 200–2 | year = 1994 | pmid = 7531354 | doi = 10.1159/000098619 | last5 = Alaminos | last4 = MacIas | last7 = Teijeiro | last6 = Alvarez | last3 = Ohye | last2 = Molina | last9 = Ortega | last8 = Muñoz | first8 = J. | first9 = I. | first2 = H. | first3 = Ch. | first4 = R. | first5 = A. | first6 = L. | first7 = J. }}{{cite journal |vauthors=Wright LF, DuVal JW | title = Renal injury associated with laxative abuse | journal = South Med J | volume = 80 | issue = 10 | pages = 1304–6 | year = 1987 | pmid = 3660046 | doi = 10.1097/00007611-198710000-00024 }} factitious diarrhea{{cite journal |vauthors=Oster JR, Materson BJ, Rogers AI | title = Laxative abuse syndrome | journal = Am. J. Gastroenterol. | volume = 74 | issue = 5 | pages = 451–8 | date = November 1980 | pmid = 7234824 }} and other problems.{{cite journal | vauthors = Roerig JL, Steffen KJ, Mitchell JE, Zunker C | title = Laxative abuse: epidemiology, diagnosis and management | journal = Drugs | volume = 70 | issue = 12 | pages = 1487–1503 | year = 2010 | pmid = 20687617 | doi = 10.2165/11898640-000000000-00000 | s2cid = 29007249 }} The colon will need more quantities of laxatives to keep functioning, this will result in a lazy colon, infections, irritable bowel syndrome, and potential liver damage.

Although some patients with eating disorders such as anorexia nervosa and bulimia nervosa abuse laxatives in an attempt to lose weight, laxatives act to speed up the transit of feces through the large intestine, which occurs after the absorption of nutrients in the small intestine is already complete. Thus, studies of laxative abuse have found that effects on body weight reflect primarily temporary losses of body water rather than energy (calorie) loss.{{cite journal |vauthors=Lacey JH, Gibson E | title = Controlling weight by purgation and vomiting: A comparative study of bulimics | journal = Journal of Psychiatric Research | volume = 19 | issue = 2–3 | pages = 337–341 | year = 1985 | pmid = 3862833 | doi = 10.1016/0022-3956(85)90037-8 }}{{Cite web|url=http://www.uptodate.com/contents/acid-base-and-electrolyte-abnormalities-with-diarrhea-or-ureteral-diversion|title=Acid-base and electrolyte abnormalities with diarrhea|website=www.uptodate.com|access-date=2017-12-12}}

Physicians warn against the chronic use of stimulant laxatives due to concern that chronic use could cause the colonic tissues to get worn out over time and not be able to expel feces due to long-term overstimulation.{{cite journal |vauthors=Joo JS, Ehrenpreis ED, Gonzalez L, Kaye M, Breno S, Wexner SD, Zaitman D, Secrest K | title = Alterations in colonic anatomy induced by chronic stimulant laxatives: the cathartic colon revisited | journal = Journal of Clinical Gastroenterology | volume = 26 | issue = 4 | pages = 283–6 | date = June 1998 | pmid = 9649012 | doi = 10.1097/00004836-199806000-00014 }} A common finding in patients having used stimulant laxatives is a brown pigment deposited in the intestinal tissue, known as melanosis coli.{{citation needed|date=October 2012}}

Laxatives, once called "physicks" or "purgatives", were used extensively in historic medicine to treat many conditions for which they are now generally regarded as ineffective in evidence-based medicine.{{Cite journal|last=Stolberg|first=Michael|date=2003|title=[The miraculous effects of taking laxatives. Success and failure of pre-modern medical treatment from the patients' perspective]|journal=Wurzburger Medizinhistorische Mitteilungen|volume=22|pages=167–177|issn=0177-5227|pmid=15641192}} Likewise, laxatives (often termed colon cleanses) may be promoted in alternative medicine for various conditions of quackery, such as "mucoid plaque".{{Cite book|title=Illustrated medical pharmacology|last=M.|first=Raju, S.|isbn=9789350906552|oclc=870530462|date = 2013-09-30|publisher=JP Medical }}

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• ATC code A06
• Bowel management
• Cathartic
• Dietary fiber
• Diuretic
• Maltitol
• Enema
• Suppository
• Transanal irrigation

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{{Commons category|Laxatives}}

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{{Laxatives}}

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Category:Gastroenterology