Opiates antidiarrheal

What are the side effects of opiate antidiarrheal medication ... 

Which opiate antidiarrheal is useful in inflammatory bowel disease ... 

Diphenoxylate Hydrochloride. l-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxyhc acidmonohydrochlorhydrate [3810-80-8] (Lomotil) (13) is a white, odorless, crystalline powder that melts at 220—226°C. It is soluble ia methanol, spariagly soluble ia ethanol and acetone, slightly soluble ia water and isopropyl alcohol, freely soluble ia chloroform, and practically iasoluble ia ether and hexane. The method of preparation for diphenoxylate hydrochloride is available (11). Diphenoxylate hydrochloride [3810-80-8] (13) is an antidiarrheal that acts through an opiate receptor. It has effects both on propulsive motility and intestinal secretion. Commercial forms are mixed with atropiae to discourage abuse. 

When an opiate is used as an antidiarrheal drug, the nurse records each bowel movement, as well as its appearance, color, and consistency. The nurse should notify the primary health care provider immediately if diarrhea is not relieved or becomes worse if die patient has severe abdominal pain or if blood in die stool is noted. 

These dm may produce withdrawal symptoms in those physically dependent on the narcotics. The patient must not have taken any opiate for the last 7 to 10 days. Naloxone may prevent die action of opioid antidiarrheals, antitussives, and analgesics. This drug is used cautiously during lactation. 

When AAD is mild, the best first step is to discontinue the inciting antibiotics. Most cases will resolve spontaneously. Some advocate restriction of dietary carbohydrate as well [60], More serious cases require specific therapy against the pathogen. Antidiarrheals and opiates should be avoided. 

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. 

Paregoric [Camphorated Tincture of Opium] [C lll] [Narcotic Antidiarrheal] Uses D, Pain neonatal opiate withdrawal synd Action Narcotic Dose Adults. 5—10 mL PO daUy-qid PRN Peds. 0.25-0.5 mL/kg daily-qid Neonatal withdrawal 3-6 gtt PO q3-6 h PRN to relieve Sxs x 3-5 d, then taper ovo 2-4 wk Caution [B (D w/ prolonged use/high dose near term, +]... 

There are many peripheral organs that possess enkephalin opiate receptors the ileum, the most distal part of the small intestine, and the vas deferens are the most significant. The receptors in the ileum are responsible for the antidiarrheal activity of opiates. This is also the explanation for the severe constipation that may occur when people use opiates for pain relief. 

Opiate preparations, usually given as paregoric, are effective and fast acting antidiarrheal agents. These agents are also useful postoperatively to produce solid stool following an ileostomy or colostomy. A meperidine derivative, diphenoxylate, is usually dispensed with atropine and sold as Lomotil. The atropine is added to discourage the abuse of diphenoxylate by narcotic addicts who are tolerant to massive doses of narcotic but not to the CNS stimulant effects of atropine. 

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],... 

Stomach ailments) more than 1 million ounces of quinine sulfate and its crade drug derivative cinchona (used for fevers) and some 2.3 million ounces of opiates (anodynes and antidiarrheals) among other items on the standard supply table. Even when physicians were doing surgery there was a pharmaceutical component, as seen in the essential anesthetics distributed—almost 3 million ounces of ether and over 1.1 million ounces of chloroform.n... 

Diphenoxylate is a synthetic compound designed to have the antidiarrheal effects of the opiates, but it also retains some less desirable opiate effects. It is generally combined with atropine, as co-phenotrope, which was originally added to the formulation in the hope of preventing misuse, although it can itself cause problems, especially if the combination is intentionally or accidentally used to excess. 

Although this quote may seem more a testament to the ignorance of medical problems of this age, certainly the remarkable analgesic (pain-relieving) properties of opium must have made it seem helpful for many disease states. In fact, opiate drugs do have special cough-suppressant and antidiarrheal properties in addition to their analgesic actions, and they are used in modern medicine for these purposes. 

Difenoxin, an opiate receptor agonist with antidiarrheal properties (2 mg p.o.), is indicated as an adjunctive treatment of acute nonspeciflc exacerbations of chronic functional diarrhea. 

Diphenoxylate is an opiate (schedule V) with antidiarrheal properties. It is usually dispensed with atropine and sold as Lomotil. The atropine is added to discourage the abuse of diphenoxylate by narcotic addicts who are tolerant to massive doses of narcotic but not to the CNS stimulant effects of atropine. Diphenoxylate shonld be used cautiously in patients with obstructive jaundice because of its potential for hepatic coma, and in patients with diarrhea cansed by pseudomembranous colitis because of its potential for toxic megacolon. In addition, it should be used cautiously in the treatment of diarrhea caused by poisoning or by infection by Shigella, Salmonella, and some strains of E. coli because expulsion of intestinal contents may be a protective mechanism. Diphenoxylate should be used with extreme caution in patients with impaired hepatic function, cirrhosis, advanced hepatorenal disease, or abnormal liver function test results, because the drug may precipitate hepatic coma. Because diphenoxylate is structurally related to meperidine, it may cause hypertension when combined with monoamine oxidase inhibitors. As a narcotic, it will augment the CNS depressant effects of alcohol, hypnotic-sedatives, and numerous other drugs, such as neuroleptics or antidepressants that cause sedation. 

L. What is a common characteristic of opiates used as antidiarrheals ... 

Opiates used as antidiarrheals generally do not cross the blood-brain barrier well. They therefore produce peripheral effects, such as slowing of the bowel, but central effects Ce.g.. euphoria and addiction) are not manifested at therapeutic doses. 

At therapeutic dosage, are the effects of atropine evident with opiate-atropine combination antidiarrheals ... 

Codeine, C]8H2i03N, is an opiate, has analgesic and antidiarrheal properties, and is widely used. In water, codeine is a weak base. A handbook gives pKa = 6.05 for protonated codeine, Ci8H2i03NH. Write the reaction for Ci8H2i03NH and calculate pKt for codeine. 

---