Antidiarrhoeal

Antidiarrhoeal drugs are used for the symptomatic treatment of diarrhoea (the frequent passage of liquid... 

ABDULLAHI A L, AGHO M o, AMOS s, GAMANIEL K s, WAMBEBE c (2001) Antidiarrhoeal activity of the aqueous extract of Terminalia avicennoides roots. Phytother Res. 15 431-4. ALETOR V A (1993) Allelocheuiicals in plant foods and feedingstuffs 1. Nutritional, biochemical and physiopathological aspects in animal production. Vet Hum Toxicol. 35 57-67. 

Fiorentino F, Simioli F, Conte M, Postiglione A, Cinque F, Santaniello A Open study on the antidiarrhoeal effectiveness of the L 105 compound. Chemioterapia 1984 3 132-135. 

Mazzitelli M, Brega G, Dirani D, Andalo A Antidiarrhoeal effectiveness and tolerance in man of a local antibiotic Rifaximin. Comparative assessment using a control drug. Eur Rev Med Pharmacol Sci 1984 6 301-306. 

Imodium containing loperamide (antidiarrhoeal) is available as 2 mg capsules. 

Bisacodyl is a stimulant laxative that does not take long to act and is therefore useful in acute constipation. The bulk-forming laxative ispaghula husk takes longer to act when compared with bisacodyl but is useful for long-term administration. Lactulose, which is an osmotic laxative, has a lag time of about 48 hours before onset of action. Loperamide and kaolin and morphine mixture are antidiarrhoeals used in acute diarrhoea. 

Loperamide is an antidiarrhoeal drug indicated for use in adults and children over 12 years. Loperamide should not be administered in children under 4 years v/ho have diarrhoea. Children are more sensitive to the occurrence of the side-effect of respiratory depression. Fluid and electrolyte replacement are first-line treatments in diarrhoea. 

Haak H, Claeson ME. Regnlatory actions to enhance appropriate drng nse the case of antidiarrhoeal dmgs. Soc Sci Med 1996 42(7) 1011-9. 

Simple antidiarrhoeals are generally contra-indicated, they do not help to reduce mucosal efflux, and may, by reducing colonic transit, predispose to megacolon development. Despite the strong association between non-smoking and the occurrence of ulcerative colitis nicotine patch treatment has shown little evidence of value. 

Antidiarrhoeals are given for symptomatic relief of diarrhoea. The first step in treatment of acute diarrhoea is replacement of fluid and electrolytes. If due to diarrhoea there is severe dehydration, it requires immediate hospitalization for IV fluid and electrolyte replacement. Antidiarrhoeal drugs are administered for obtaining symptomatic relief in acute diarrhoea but have untoward effects. Alongwith antidiarrhoeal drugs, antispasmodics are administered in those patients who have diarrhoea with abdominal pain. 

Fixed dose combinations of antihistaminics with antidiarrhoeals. 

Antidiarrhoeal formulations containing kaolin or pectin or attapulgite or activated charcoal. 

Antidiarrhoeal formulations containing phthalyl sulfathiazole or sulfaguanidine or succinyl sulphathiazole. 

Antidiarrhoeal formulations containing neomycin or streptomycin or dihydrostreptomycin including their respective salts or esters. 

Liquid oral antidiarrhoeals or any other dosage form for paediatric use containing diphenoxylate or atropine or belladonna including their salts and esters or metabolites, hyoscyamine or their extracts or their alkaloids. 

Liquid oral antidiarrhoeals of any other dosage form for paediatric use containing halogenated hydroxyquinolines. 

Other activities on the gastrointestinal system included antidiarrhoeal and gastroprotective effects. Satureja hortensis and Aloysia triphylla EOs inhibited castor oil induced diarrhoea in rodents [225, 255]. The EO of lavender and its components (linalool, linalyl acetate) and the EO of Cryptomeria japonica (ter-pin-4-ol and elemol) showed protective activities against acute ethanol/aspirin-induced gastric ulcers in rodents [200,254]. 

The antidiarrhoeal drug ipecac, which was introduced into Europe from Brazil in 1658, contains the amoebicidal alkaloids emetine (12) and cephaeline. Emetine remained the major remedy for amoebic dysentery and amoebic hepatitis for many years. Cephaeline is less active and more toxic. ( j-2-Dehydroemetine, which is made by synthesis, is equiactive with (—)-emetine and less toxic, but other chemical modification has not yielded better amoebicides. From investigations of synthetic routes to the benzoquinolizine moiety the tranquilizer tetrabenazine (13a) was discovered. The very similar compound benzquinamide (13b) is also a tranquilizer and antiemetic. 

Morphine and other opium alkaloids affect the activity of the bowel and have long been used in antidiarrhoeal medicines. Pethidine has a similar effect, and the piperidine diphenoxylate (142) is effective in the treatment of diarrhoea in doses that do not produce any CNS effects. 

Despite the lack of studies correlating the antidiarrheic activity of crude drugs with the presence of flavonoids, these have been also studied as pure compounds in this regard. The most used assay of antidiarrhoeic activity is the castor oil test, in which diarrhea is induced by the oral administration of castor oil to mice. Different flavonoids have been shown to possess antidiarrheal activity in this test quercetin, kaempferol, morin, myricetin, rutin (i.p.) [117,118], quercitrin (p.o.) [114,119], and tematin (i.p.) [44], all showing a dose-dependent activity in the range between 25 and 100 mg/kg. However, flavonoids are not only able to exert a preventive antidiarrheal effect in this acute model of experimentally-induced diarrhea, but also in chronic models. Thus quercitrin showed beneficial effects in a model of lactose-induced chronic diarrhea in rats, since it reduced the diarrheal output and facilitated colonic mucosal repair in lactose fed [120]. 

Haskins, N. J., Ford, G. C., Grigson, S, J., and Waddell, K. A. (1978). A carrier effect observed in assays for antidiarrhoeal drug compounds. Biomed. Mass Spectrom. 5, 423-424. 

Beubler and Badhri (1990) used the PGE2-induced net fluid secretion in the jejunum and colon in the rat to evaluate the antisecretory effects of antidiarrhoeal drugs. Polyethylene catheters were placed into the jejunum and colon and Tyrode solution was instilled into the loops. Net fluid transfer rates were determined gravimetrically 30 min after instillation of Tyrode solution. 

Medical treatments of IBS are limited. Laxatives (particularly dietary fibre and bulking laxatives such as ispaghula) and antidiarrhoeals (loperamide and sometimes codeine) are prescribed to manage the symptoms of altered bowel habit. Colestyramine is of use in those with diarrhoea caused by bile salt... 

This can be controlled with the co-administration of standard antidiarrhoeal agents such as loperamide. All patients on FOLFOX chemotherapy (or any 5-fluorouracil-containing regimen) should be co-prescribed an antidiarrhoeal medication to use on an as required basis. The onset of diarrhoea should also indicate to the patient that they must increase their fluid intake to prevent dehydration. Patients must be warned that if the diarrhoea is not controlled (for example, within 48 hours of onset) then dehydration is a danger and they should be advised to contact their treating hospital or GP for advice. Severe manifestations may have to be managed by delay and/or dose modification of the patient s next cycle of chemotherapy. 

Many centres co-prescribe an antidiarrhoeal drug such as loparmide to use in case of diarrhoea. Mrs RP should be counselled to use this to treat diarrhoea should it occur again. 

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