Loperamide antidiarrheal

One important analogue of morphine is fentanyl, a clinically used narcotic that is about 100 times more potent than morphine. Several analogues have been synthesised such as sufentanil, alfentanil, lofentanil and, even more interestingly, structurally related compounds with different activities such as astemizole (antihistaminic), droperidol (tranquillizing), loperamide (antidiarrheal) and lorcainide (antiarrhythmic) [50]. 

Antidiarrheals decrease intestinal peristalsis, which is usually increased when the patient has diarrhea. Examples of these drug s include difenoxin with atropine (Motofen), diphenoxylate witii atropine (Lomotil), and loperamide (Imodium). 

Antidiarrheal medications that reduce GI motility, such as loperamide, diphenoxylate/atropine, or codeine should be avoided in patients with active IBD due to the risk of precipitating acute colonic dilation (toxic megacolon). 

Bowel symptoms in MS patients can include both fecal incontinence and constipation. Fecal incontinence is difficult to treat. Some patients may have improvement if they use a regular schedule for emptying the bowel with laxative suppositories or enemas. Alternatively, antidiarrheal medications such as loperamide can be used.14... 

HT3 antagonist, prochlorperazine for emesis (avoid corticosteroids), H2 blocker for gastritis, antidiarrheal as needed (loperamide, diphenoxylate/atropine, codeine). 

L The answer is a. (Hardman, p 922) Lactulose is a synthetic disaccharide (galactose-fructose) that is not absorbed. In moderate doses, it acts as a laxative. In higher doses, it is capable of binding ammonia and other toxins that form in the intestine in severe liver deficiency and that are believed to cause the encephalopathy. Loperamide is an antidiarrheal opioid lorazepam is a CNS depressant loxapine is a heterocyclic antipsychotic. 

Opioids. Activation of opioid receptors in the enteric nerve plexus results in inhibition of propulsive motor activity and enhancement of segmentation activity. This antidiarrheal effect was formerly induced by application of opium tincture (paregoric) containing morphine. Because of the CNS effects (sedation, respiratory depression, physical dependence), derivatives with peripheral actions have been developed. Whereas diphenoxylate can still produce clear CNS effects, loperamide does not Lullmann, Color Atlas of Pharmacology... 

Loperamide is presently used more often as an antidiarrheal drug than as an analgesic, and it is also included in the list of over-the-counter drugs because of its insignificant action on the CNS. It reduces intestinal smooth muscle tone and motility as a result of binding to intestinal opiate receptors. It is used for symptomatic treatment of severe and chronic diarrhea of various origins. The most popular synonym for loperamide is imodium. 

Difenoxin is a metabolite of diphenoxylate with antidiarrheal effects similar to the parent drug. Loperamide Imodium) is a piperidine derivative of diphenoxylate, which acts both at the level of the gut and also in the CNS to reduce GI motility. Its use as an antidiarrheal and its potency are similar to those of diphenoxylate. 

The dangers of dependency and addiction clearly preclude the use of such compounds as morphine, meperidine, and methadone as treatment for diarrhea. Antidiarrheal specificity therefore is of paramount importance in choosing among the synthetic opioids and their analogues (e.g., diphenoxylate and loperamide). 

Pharmacological studies with selective agonists have shown that opioid control of intestinal electrolyte transport is predominantly mediated by delta opioid receptors [58], while the gastrointestinal propulsion is under the control of mu receptors [59,60]. The antidiarrheal effects of NEP inhibitors, such as acetorphan, the prodrug of thiorphan, have been compared to those of an opiate agonist, loperamide, in a model of castor oil-induced diarrhea in rats. When administered peripherally, they produced a delayed onset of diarrhea with no reduction in the gastrointestinal transit [61,62], as is commonly observed with loperamide [63],... 

In the N-oxide of loperamide (an antidiarrheal) the hydroxy group and the oxide oxygen have a trans relationship. Draw the structure in a chair form and determine whether the molecule is chiral. Which stereodescriptors must be added to the systematic name to exactly describe the configuration ... 

Loperamide is, therefore, the opioid antidiarrheal of first choice. The prolonged contact time for intestinal contents and mucosa may also improve absorption of fluid. With overdosage, there is a hazard of ileus. The drug is contraindicated in infants below age 2 years. 

The effects of a preparation containing berberine and the crude herb Geranii Herba on different diarrheal models in mice and the contractions of isolated guinea pig intestinal muscle were studied via comparison with a preparation containing creosote and loperamide. The results suggested that Geranii Herba exerted its antidiarrheal effect via the inhibition of intestinal movement, with the mechanism of action possibly differing from creosote and loperamide [257]. 

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