Intestinal fluid stimulant

The intestinal fluid stimulant [2] consisted of a solution of pancreatin. First potassium dihydrogen phosphate (KH2PO4) (6.8 g) was dissolved in distilled water (250 ml) in a 1 litre volnmetric flask. Then 0.2 M sodium hydroxide (190 ml), sodium taurocholate (0.5 g), and distilled water (around 400 ml) were added. A solution of pancreatin (10 g, USP) was prepared separately by gradually adding the enzyme into distilled water (150 ml) to avoid the formation of lumps, and it was then transferred into the volumetric flask with gentle shaking. The pH was adjusted to 7.5 0.1 with sodium hydroxide (0.2 M), and the resulting solution was diluted to 1 litre with distilled water. 

Opioids induce an inhibitory effect on gastrointestinal motility and fluid secretion (Kromer, 1990). The effect is peripherally and centrally mediated. The peripheral component is related to p- and K-receptors in intestinal organs, which are densely equipped with opioid receptors. They are located at parasympathic ganglia and inhibit the release of acetylcholine, which stimulates the contraction of smooth muscles. Inhibition of the intestinal fluid secretion is mediated via inhibition of adenylate cyclase. The intestinal effects of opioids extend to all parts of the gut and results in inhibition of stomach emptying and inhibition of secretion and motility of duodenum, jejunum, colon and rectum. 

The study was performed with a Class 1 member in the form of tablets. Changes in pH have no effects while changes in agitation intensity for USP apparatus II and IV have shown clear influences on the tablet erosion and subsequently on its release. Finally to simulate the fasted and fed state in vivo, fasted state stimulated intestinal fluid(Fassif) and fed state simulated intestinal fluid(Fessif) media were used. None of the USP traditional apparatus show a clear relationship with the in vivo results, especially in the fed conditions. In vitro data obtained by the ADS in the fasted state were consistent with those in vivo, as well as in the fed state after a slight time adjustment allowed in the FDA notes of guidance. A Level A of IVIVC was easily established with a good correlation coefficient in the fasted and fed states, respectively. The main results are presented in Fig. 13. 

Bismuth subsalicylate (BSS) is used widely in humans for treatment of diarrhea and is specifically recommended for the prevention of traveler s diarrhea. The precise mechanism of action remains undetermined and although the end result of treatment with BSS is reduction in diarrhea (Figueroa-Quintanilla et al 1993), its effect is probably not related to a direct antisecretory mechanism. Salicylates have been shown to stimulate intestinal fluid and electrolyte absorption per se but it is likely that, in many cases of colitis, resolution of inflammation and restoration of a normal surface epithelium is required to restore mucosal function. When used as pretreatment or coadministered, BSS significantly reduced the fluid secretory response to E. coli LT enterotoxin and cholera toxin in intestinal loops of rabbits and pigs (Ericsson et al 1990). However, when administered even 5 min after the enterotoxins, BSS had no significant effect on enterotoxin-stimulated intestinal secretion. These results suggest that BSS adsorbs or neutralizes bacterial enterotoxins but does not alter the effect of enterotoxins once they have bound to intestinal mucosa. BSS also modulates normal... 

Chemical cathartics stimulate intestinal fluid secretion by activating mucosal secretion. Some... 

Botella A, Vabre F, Fioramonti J et al 1993 In vivo inhibitory effect of lanreotide (BIM 23014), a new somatostatin analog, on prostaglandin- and cholera toxin-stimulated intestinal fluid in the rat. Peptides 14 297-301 Brzozowski T, Konturek S J, Sliwowski Z et al 1997 Role of L-arginine, a substrate for NO-synthase, in gastroprotection and ulcer healing. Journal of Gastroenterology 32 442-452... 

Diarrhea can cause dehydration and electrolyte imbalance because intestinal fluids are rich in water, sodium, potassium, and bicarbonate. To rehydrate and restore electrolyte imbalance, patients are administered Gatorade, Pedialyte, Ricelyte, and electrolytes given IV. Antidiarrheal medication decreases the hypermotility (increased peristalsis) that stimulates frequent bowel movements and should be administered for less than 2 days and not if the patient experiences a fever. There are four classifications of antidiarrheal medication. These are ... 

Stimulant laxatives work by stimulating enteric nerves (in the wall of the intestine), which results in smooth muscle contraction and an increase in peristalsis. At the same time they increase fluid secretion from the intestinal mucosa. Stimulant laxatives can cause abdominal cramps. 

CASTOR OIL An age-old home remedy seldom recommended now, castor oil (purge, NEOLOID, others) is derived from the bean of the castor plant, Ricinus communis, which contains two well-known noxious ingredients an extremely toxic protein, ricin, and an oil composed chiefly of the triglyceride of ricinoleic acid. The triglyceride is hydrolyzed in the small bowel by the action of lipases into glycerol and the active agent, ricinoleic acid, which acts primarily in the small intestine to stimulate secretion of fluid and electrolytes and speed intestinal transit. When taken on an empty stomach, as little as 4 mL of castor oil may produce a laxative effect within 1-3 hours however, the usual dose for a cathartic effect is 15-60 mL for adults. 

The story of the discovery and structure determination of these remarkable compounds began in 1930 when gynecologists Raphael Kurzrock and Charles Lieb reported that human seminal fluid stimulates the contraction of isolated uterine muscle. A few years later, Ulf von Euler in Sweden confirmed this report and noted that, when injected into the bloodstream, human seminal fluid also stimulates the contraction of intestinal smooth muscle and lowers the blood pressure. Von Euler proposed the name prostaglandin for the mysterious substance(s) responsible for these diverse effects, because it was believed at the time that they were synthesized in the prostate gland. Although we now know that prostaglandin production is by no means limited to the prostate gland, the name has stuck. 

Figure 106,2. Opioid-induced bowel dysfunction (OBD). Opioids increase intestinal fluid absorption, inhibit intestinal secretions and peristalsis, and block propulsive movements in the colon. Constipation and other symptoms associated with OBD occur in 15-90% of cancer patients and may be more distressful and debilitating than pain. Tolerance rarely develops to these symptoms and traditional therapy including stimulants, lubricants, arxf bulk laxatives may not be effective.

Okadaic acid is a powerful tumor promoter of a nonphorbol ester type that inhibits protein phosphatase-1 and -2A in vitro (Haystead et al., 1989). Okadaic acid directly stimulates smooth muscle contraction (Haystead et al., 1989) and probably causes diarrhea, either by stimulating the phosphorylation of proteins controlling sodium secretion by intestinal cells or by increasing phosphorylation of elements that regulate permeability to solutes, resulting in a passive loss of fluids (Aune and Yndestad, 1993). 

Enterotoxigenic E. coli (ETEC) is the main cause of TD in Latin America, whereas in Asia it is reported in only 15% of cases. Enteroinvasive E. coli (EIEC) strains are recorded with even less frequency. ETEC is isolated in 0 to 5% of cases. Symptoms of poisoning develop after 16 hours from consumption of contaminated water, salads, cheeses, or meats. The outgrowth of ETEC rods takes place in a patient s gastrointestinal tract, where they produce thermostable and thermolabile toxins that imitate Vibrio cholerae infections. Stimulation of intestinal guanylcyclase and interruption of ion transport leads to watery stools, which do not require medical treatment or only need simple replacement of fluids and salts by means of multielectrolyte solutions. If a co-infection with EIEC strains occurs, the symptoms of enteritis will develop, with the presence of leukocytes, erythrocytes, and mucous in stools due to a cytotoxic influence of bacteria (Butterton and Claderwood, 2001). 

ADP ribosylation results in inhibition of GTPase activity and hence maintains the a-subunit in the active form. The constant activity of the G-protein results in an increase in adenyl cyclase activity and therefore a chronic increase in the cychc AMP level. This stimulates an ion channel in the enterocyte which results in a loss of Na ions and hence water from the cells into the intestine. This leads to diarrhoea and a massive loss of fluid from the body which can be sufficiently severe to result in death. Since 2000 there have been epidemics in South America and parts of central Africa. Infection is usually caused by drinking water contaminated with faecal matter. Treatment consists of hydration with rehydration fluids (Chapter 5). 

Gastrointestinal tract. Serotonin released from myenteric neurons or enterochromaffin cells acts on 5-HT3 and 5-HT4 receptors to enhance bowel motility and enteral fluid secretion Cisapride is a proldnetic agent that promotes propulsive motor activity in the stomach and in small and large intestines. It is used in motility disorders. Its mechanism of action is unclear, but stimulation of 5HT4 receptors may be important... 

IgE-mediated allergic reactions (p. 72) involve mast cell release of histamine (p. 114) and production of other mediators (such as leukotrienes, p. 196). Resultant responses include relaxation of vascular smooth muscle, as evidenced locally by vasodilation (e.g., conjunctival congestion) or systemically by hypotension (as in anaphylactic shock) enhanced capillary permeability with transudation of fluid into tissues— swelling of conjunctiva and mucous membranes of the upper airways ( hay fever ), cutaneous wheal formation contraction of bronchial smooth muscle-bronchial asthma stimulation of intestinal smooth musde—diarrhea. 

In general, ethanol in low to moderate amounts, is relatively benign to most body systems. A moderate amount of ethanol causes peripheral vasodilation, especially of cutaneous vessels, and stimulates the secretion of salivary and gastric fluids the latter action may aid digestion. On the other hand, ethanol consumption in high concentrations, as found in undiluted spirits, can induce hemorrhagic lesions in the duodenum, inhibit intestinal brush border enzymes, inhibit the uptake of amino acids, and limit the absorption of vitamins and minerals. In addition, ethanol can reduce blood testosterone levels, resulting in sexual dysfunction. 

Mechanism of Action A laxative prepared from the bean of the castor plant but the exact mechanism of acfion is unknown. Acts primarily in the small intestine. Maybe hydrolyzed to ricinoleicacid which reduces net absorption of fluid and electrolytes and stimulates peristalsis. Therapeutic Effect Increases peristalsis, promotes laxative effect. 

Misoprostol has both acid inhibitory and mucosal protective properties. It is believed to stimulate mucus and bicarbonate secretion and enhance mucosal blood flow. In addition, it binds to a prostaglandin receptor on parietal cells, reducing histamine-stimulated cAMP production and causing modest acid inhibition. Prostaglandins have a variety of other actions, including stimulation of intestinal electrolyte and fluid secretion, intestinal motility, and uterine contractions. 

Chloride channel activator Lubiprostone, prostanoic acid derivative, stimulates chloride secretion into intestine, increasing fluid content... 

Stimulant laxatives Bisacodyl, 5-15 mg daily. Senna, dosage varies, consult product labeling Correctol, Dulcolax, Ex-Lax, Senokot, various generic Stimulant laxative actions include direct irritation of intestinal mucosa or stimulation of the myenteric plexus, resulting in peristalsis. These agents may also cause alteration of fluid and electrolyte absorption, resulting in luminal fluid accumulation and bowel evacuation. 

The chief herb is Da Huang. It is bitter and cold, can vigorously stimulate the intestines, purge the heat accumulation and move the stool. With the salty and cold Mang Xiao as deputy, which can increase the fluid of the intestines and soften the stool, the function of purging the stool is increased. 

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