Intestinal antiseptic

Various other properties intestinal antiseptic (932, 933), fungicide (934, 935), insecticide (895. 898), coccidiostatic activity (936), car-cinolytic activity (937), radioprotective activity (938), antimutagenic activity (939, 940). 

Over 30 years ago, the three major requirements for an effective intestinal antiseptic were outlined (1) rapid, highly bactericidal activity against gastrointestinal pathogenic organisms, (2) low local and systemic toxicity, and... 

The /V4-acylatcd sulfonamides, succinylsulfathiazole (4.124) and phtha-lylsulfathiazole (4.125), are poorly absorbed by the gastrointestinal tract. These compounds, which were once used as intestinal antiseptics, are inactive in vitro and must be activated by hydrolysis to sulfathiazole by bacterial hydrolases in the large intestine [78],... 

Phenyl salicylate (salol) is manufactured by heating salicylic acid and phenol in the presence of phosphoms oxychloride for 4—5 hours at 110—115°C. The molten product is separated, mixed with water, dried, and distilled under vacuum. Another process involves the transesterification of a salicylate such as methyl, with phenol in the presence of an alkali or alkaline-earth phenate. Medicinally, phenyl salicylate was formerly used as an intestinal antiseptic. However, the main applications of phenyl salicylate have been related to the ability to absorb uv light over the wavelengths of 290—325 nm. As an effective uv-light absorber, phenyl salicylate was incorporated in alkyd paints, waxes, and polishes, but has been largely replaced in this application by less extractable, more effective compounds. The May 1996 price was 10.60/kg (18). 

To deliver drugs intended for local action in the intestine (e.g., intestinal antiseptics could be delivered to their site of action) in a concentrated form... 

D-Glucuronolactone has recently been found to be of clinical value as an intestinal antiseptic. The substance was said to suppress the enteric flora257 and to lengthen the effective period of sterilization by streptomycin.258 It was reported that this combination does not diminish indican excretion269 or induce hypoprothrombinemia.260... 

A number of zinc compounds with organic constituents (e.g., zinc salts of organic acids) have therapeutic uses. These include antidandruff zinc pyridinethione, antifungal zinc undecylenate used to treat athlete s foot, zinc stearate and palmitate (zinc soap), and antibacterial zinc bacitracin. Zinc naphthenate is used as a low-toxicity wood preservative, and zinc phenolsulfonate has insecticidal properties and was once used as an intestinal antiseptic. The inhalation of zinc soaps by infants has been known to cause acute fatal pneumonitis characterized by lung lesions similar to, but more serious than, those caused by talc. Zinc pyridine thione (zinc 2-pyridinethiol-l-oxide) has been shown to cause retinal detachment and blindness in dogs this is an apparently species-specific effect because laboratory tests at the same and even much higher dosages in monkeys and rodents do not show the same effect. 

Diiodo-8-quinolinol widely used as an intestinal antiseptic, especially as an antiamebic agent. It is also used topically in other infections and may cause CNS and eye damage. It is known by very many similar trade names worldwide. 

See also Amide ions Anions Carboca-tions and Radical intermediates Intestinal antiseptic, 152 Intramolecular reactivity, see Heterocycliza-tione... 

Dose. As an intestinal antiseptic, up to 12 g of neomycin sulphate daily, by mouth it is also applied topically. 

Salol is used as an intestinal antiseptic. It is prepared by heating salicylic acid alone to 160° to 240°. In this case one molecule loses carbon dioxide yielding phenol which then esterifies with another molecule of the acid yielding the phenyl ester. 

Berggren L, Hansson O. Absorption of intestinal antiseptics derived from 8-hydroxyquinolines. Clin Pharmacol Ther 1968 9(l) 67-70. 

Another active principle soon extracted from plants was salicylic acid. Salicin, extracted from the willow tree, has been launched in 1876 by a Scottish physician, Thomas John McLogan It was in extensive competition with Cinchona bark and quinine and never became a very popular treatment for fever or rheumatic symptoms. The Italian chemist Raffaele Piria, after having isolated salicylalde-hyde (1839) in Spireae species, prepared salicylic acid from salicin in Dumas laboratory in the Sorbonne, Paris. This acid was easier to use and was an ideal step before future syntheses. Its structure was closely related to benzoic acid, an effective preservative useful as an intestinal antiseptic for instance in typhoid fever. Acetylsalicylic acid has been first synthesized by Charles Frederic Gerhardt in 1853 and then, in a purer form, by Johann Kraut (1869). Acetylsalicylic acid synthesis with carbolic acid and carbon dioxide was improved by Hermann Kolbe in1874, but in fact nobody noticed its pharmacological interest. 

FIGURE 91 Sulfonamides that are poorly absorbed include succinylsulfathiazole, phthalylsulfathiazole, and sulfasalazine and they are used as intestinal antiseptics. 

The snlfonamides are structurally related to p-aminoben-zoic acid. The presence of a free p-amino gronp is essential for the antibacterial action. Succinylsulfathiazole (sulfasuxi-dine) and phthalysnlfathiazole (sulfathalidine) are agents with a snbstitnted p-amino group. These intestinal antiseptics are slowly hydrolyzed in the intestine, releasing sulfathiazole, which exerts antiseptic effects against the coliform and clostridial organisms. 

Sulfonamides that are poorly absorbed. These agents include succinylsulfathiazole (Sulfasux-ide), phthalylsulfathiazole (Sulfathalidine), and sulfasalazine (Azulfldine) they are used as intestinal antiseptics. Sulfasalazine is used especially in the therapy of regional enteritis and ulcerative colitis (Figure 91). 

The recommended dose is 10,000 to 20,000 units given intramuscularly every 6 hours and accompanied by careful studies of the renal function i " . In this way bacitracin is absorbed readily from the site of injection although pain and some injury may be observed there. It has been used in the treatment of staphylococcal bacteremias, osteomyelitis, bacterial endocarditis, and in the control of urinary tract infections either alone or in combination with other drugs . Local injection into circumscribed areas, such as furuncles and abscesses, has also been successful. Orally, bacitracin has been used either alone or in combination with other antibiotics as an intestinal antiseptic i, for example in the pre-operative sterilization of the bowel. Because of the poor absorption from the gastro-intestinal tract, no special precautions are necessary. 

THERAP CAT (VET) Has been used in dusting powders, as an insecticide and internally as an intestinal antiseptic and ver -micide. 

THERAP cat (vet) Has been used as an intestinal antiseptic, and externally to promote healing of ulcers, slowly granulating wounds. 

Potassium guaiacosulphonate is employed both as an expectorant in bronchitis and also as an intestinal antiseptic. 

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