Diphenoxylate/atropine Lomotil

Diphenoxylate + Atropine (Lomotil, Lonox) [C V] [Opioid Antidiarrheal] Uses D Action Constipating m CTidine congener, X GI motihty Dose Adults. Initial, 5 mg PO tid—qid until controlled, then 2.5-5 mg PO bid 20 mg/d max Peds >2 y. 0.3-0.4 mg/kg/24 h (of diphenoxylate) bid-qid, 10 mg/d max Caution [C, +] Contra Obstructive jaundice, D d/t bacterial Infxn children <2 y Disp Tabs, Liq SE Drowsiness, dizziness, xCTostomia, blurred vision, urinary retention, constipation Interactions T Effects W/ CNS depressants, opioids, EtOH, T risk HTN crisis W7 MAOIs EMS Monitor for Sxs of electrolyte disturbances and hypovolemia d/t D OD May cause Szs, hypotension, and anticholinergic effects (xerostomia [dry mouth], urine retention, flushed skin) activated charcoal may be effective for OD... 

Individuals on very small amounts of heroin are prescribed diazepam for anxiety, agitation or craving, zopiclone or zolpidem for insomnia, hyoscine butylbromide (Buscopan) for stomach cramps, and diphenoxylate/atropine (Lomotil) for diarrhoea, over a seven-day period. The medication schedule provided to the user explains which drug is for which symptoms, and the maximum doses of each that can be taken in a day, which for diazepam varies during the course. The basic medication regime is included in the Appendix. 

McCarron MM, Challoner KR, Thompson GA. Diphenoxylate-atropine (Lomotil) overdose in children an update (report of eight cases and review of the literature) Pediatrics 1991 87(5) 694-700. 

The total dose required to reverse the effects of the opioid is highly variable and is dependent on the concentration and receptor affinity of the opioid. Some drugs (eg, propoxyphene, diphenoxylate/atropine [Lomotil], buprenorphine, pentazocine, and the fentanyl derivatives) do not respond to usual doses of naloxone. However, if no response is achieved by a total dose of 10-15 mg, the diagnosis of opioid overdose should be questioned. 

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). 

Aluminum Hydroxide Magnesium Trisilicate (Gaviscon) Aluminum Hydroxide (Amphojel, ALtemaGEL) Aluminum Hydroxide + Magnesium Carbonate (Gaviscon Extra Strength, Liquid) Antidiarrheals Bismuth Subcitrate/ Metronidazole/ Tetracycline (Pylera) Bismuth Subsalicylate (Pepto-Bismol) Diphenoxylate w/ Atropine (Lomotil, Lonox)... 

Oral 1 mg (with 0.025 mg atropine sulfate) tablets Diphenoxylate (generic, Lomotil, others)... 

Diphenoxylate-atropine has been used in the past to treat cats with diarrhea, but toxicity has limited its usefulness. Lomotil should generally be avoided in cats. 

Diphenoxylate and Atropine (Lomotil) Diphenoxylate is an agonist at opiate receptors in Gl tract and atropine blocks muscarinic receptors. Both actions inhibit peristalsis. Diarrhea Few, minor side effects include constipation, abdominal and bowel distention, nausea. 

Diphenoxylate Lomotil) is a meperidine derivative used as an antidiarrheal. It exhibits no morphinelike effects at low doses, but it produces mUd opioid effects, such as sedation, euphoria, and dependence, at higher doses. Its salts are highly insoluble in water, which reduces recreational use. Preparations often include atropine. 

Diphenoxylate (marketed in combination with atropine as Lomotil in the United States) is chemically related to both analgesic and anticholinergic compounds. It is as effective in the treatment of diarrhea as the opium derivatives, and at the doses usually employed, it has a low incidence of central opioid actions. Diphenoxylate is rapidly metabolized by ester hydrolysis to the biologically active metabolite difenoxylic acid. Lomotil is recommended as adjunctive therapy in the management of diarrhea. It is contraindicated in children under 2 years old and in patients with obstructive jaundice. Adverse reactions often caused by the atropine in the preparation include anorexia, nausea, pruritus, dizziness, and numbness of the extremities. 

Diphenoxylate (not more than 2.5 mg and not less than 0.025 mg of atropine per dosage unit, as in Lomotil)... 

Opiates produce constipation by affecting receptors in the intestines. Opium extracts were used in this capacity to treat diarrhea. Today there are other related compounds on the market which accomplish the peripheral task without affecting the CNS because of their poor absorption from the Gl tract when taken orally. Imodium A-D , an OTC, contains loperamide. It is also available as a generic OTC. The prescription mixture of diphenoxylate and atropine is called Lomotil . 

Diphenoxylate Hydrochloride. l-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylic acid monohydrochlorhydrate [3810-80-8] (Lomotil) (13) is a white, ododess, crystalline powder that melts at 220—226°C. It is soluble in methanol, sparingly soluble in ethanol and acetone, slightly soluble in water and isopropyl alcohol, freely soluble in chloroform, and practically insoluble in 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 atropine to discourage abuse. 

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. 

Diphenoxylate Hydrochloride/Atropine Sulfate Brand name Lomotil Class Antidiarrheals... 

One of the commonest drugs usL d to treat intestinal cramps and diarrhea is Lomotil, a combination of a synthetic opiate called diphenoxylate and atropine, one ot the constituents of nigiushade plants. Both of these drugs reduce the movement of the intestines by paralyzing the nerves that control them. Diphenoxylate is a close chemical relative of meperidine (Demerol), one of the strong medical narcotics. Like its relative, diphenoxylate can cause depression ot the nervous system that may he intensified by simultaneous use of other depressants. It can also cause euphoria and dependence. Many patients who take Lomotil for intestinal upset experience narcotic effects on mood but have no idea they are using an opiate. 

Dryness of mucous membranes is a common side effect of anticholinergic drug use and is due to dose-dependent inhibition of glandular secretion. In one study, oral administration of atropine caused tear secretion to fall from 15 to 3 mcl/min.A similar dose of atropine given subcutaneously gave a nearly 50% reduction in lacrimal secretion. Scopolamine at a dose of 1 to 2 mg orally reduced tear secretion from 5 to 0.8 mcl/min. Atropine combined with diphenoxylate (Lomotil) has been reported to cause severe keratoconjimctivitis sicca in susceptible individuals. 

Novak E, Lee JG, Seckman CE, PhUhps JP, DiSanto AR. Unfavorable effect of atropine-diphenoxylate (Lomotil) therapy in lincomycin-caused diarrhea. JAMA 1976 235(14) 1451. ... 

Example Diphenoxylate with atropine Route Pregnancy Pharmacokinetic (Lomotil) Schedule V PO category C Well absorbed from GI tract metabolized in liver eliminated in feces... 

Jacutin, Kildane, Kwell, Kwildane, Lencid, Locion-V, Lomotil atropine sulfate, diphenoxylate... 

DIPHENOXYLATE HYDROCHLORIDE WITH ATROPINE SULFATE (Lomotil)... 

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