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CISAPRIDE (Veterinary—Systemic) CISAPRIDE (Veterinary—Systemic) There are no human- or veterinary-labeled commercial ELUS,CANDelayed gastric emptying (treatment)EL; or cisapride products in the United States or Canada. ELUS,CANSmall bowel motility disorders (treatment)EL— Although no feline studies are available, the Category: Gastrointestinal emptying adjunct; documented effects of cisapride in healthy dogs and peristaltic stimulant. other animals suggest it may have efficacy in disorders that benefit from stimulation of gastric, Indications small intestinal, or colonic motility and from Note: Cisapride is not specifically approved for shortened transit time in cats (Evidence rating: B- {R-2; 4-7; 21-24} veterinary use. In other USP information 2). monographs, the ELUS and ELCAN designations refer to uses that are not included in U.S. and Canadian Dogs product labeling; however, in this monograph Potentially effective they reflect the lack of commercial product ELUS,CANGastroesophageal reflux (treatment)EL; availability in the countries indicated. See also the ELUS,CANDelayed gastric emptying (treatment)EL; Regulatory Considerations section below in this ELUS,CANSmall bowel motility disorders (treatment)EL; or monograph. US,CAN EL Colonic motility disorders (treatment)EL — Classification as Accepted, Potentially effective, Although no studies of clinical disease states are or Unaccepted is an evaluation of reasonable use available, studies of the effects of cisapride in that considers clinical circumstances, including healthy dogs suggest it may have efficacy in the availability of other therapies. The quality of disorders that benefit from stimulation of gastric, evidence reviewed for an indication is shown by small intestinal, or colonic motility and from the evidence rating. shortened transit time (Evidence rating: B-2 [table 1][table 2][table3]).{R-4-7; 17; 21-24} Cats Accepted Note: There is no evidence that cisapride is effective in ELUS,CAN EL Constipation, chronic (treatment) ; or the treatment of megaesophagus in dogs. The US,CAN EL Megacolon, idiopathic (treatment)EL—Although canine esophagus is striated muscle, with no no studies of clinical disease cases are available, smooth muscle to directly respond to the cisapride may be used as part of a multifaceted medication; cisapride is not expected to aid in regimen in the treatment of chronic constipation canine esophageal emptying.{R-25} that has not responded to other therapies and in the treatment of idiopathic megacolon, based on in Horses vitro studies of its effects on colonic tissues {R-1-3} Accepted (Evidence rating: B-4,5). ELUS,CANIleus, post-operative (prophylaxis and treatment)EL—Based on evidence demonstrating the Potentially effective ELUS,CAN EL ability of cisapride to stimulate gastrointestinal Esophageal motility dysfunction (treatment) — motility and emptying in horses, as well as clinical The action of cisapride in stimulating esophageal studies suggesting it decreases the risk of post- motility in the cat may be useful in the treatment of {R-2; 20} operative ileus, cisapride may be used as part of a esophageal disorders (Evidence rating: B-4,5). US,CAN comprehensive regimen to prevent or treat post- EL EL {R-8-16; 26} Gastroesophageal reflux (treatment) ; operative ileus (Evidence rating: B-2,3,4,5). Evidence ratings Evidence Quality Evidence Type A Good evidence to support a recommendation for use 1 Species-specific evidence from at least one large randomized and B Moderate evidence to support a recommendation for use controlled trial (RCT) or multiple small RCTs C Insufficient evidence to support a recommendation for use 2 Species-specific evidence from a small RCT, disease models, D Moderate evidence to support a recommendation against use large case studies, pharmacokinetic studies using surrogate E Good evidence to support a recommendation against use endpoints, or evidence from well-designed trials in a different species that is considered appropriate for comparison 3 Dramatic results from either well-designed, species-specific trials without controls, controlled trials without randomization, or small case studies 4 Pharmacokinetic studies without surrogate endpoints or well designed pharmacodynamic studies in healthy animals 5 In vitro studies 6 Opinions of respected authorities on the basis of clinical experience or reports of expert committees © 2008 The United States Pharmacopeial Convention All rights reserved More research is needed to establish the relative Pharmacology/Pharmacokinetics efficacy of cisapride in comparison with other Note: See also Tables I and II at the end of this promotility agents and to demonstrate the types of monograph. gastrointestinal tissue injuries that are likely to benefit from prokinetic therapy. Mechanism of action/Effect: Cisapride is a prokinetic drug; it stimulates gastrointestinal smooth muscle Potentially effective motility and decreases transit time of gastrointestinal ELUS,CAN EL Gastroesophageal reflux (treatment) ; contents down the length of the tract.{R-40} Cisapride US,CAN EL Delayed gastric emptying (treatment)EL; acts by enhancing the release of acetylcholine from ELUS,CANSmall bowel motility disorders (treatment)EL; or postganglionic nerve endings at the myenteric ELUS,CANColonic motility disorders (treatment)EL— plexus. Studies have demonstrated effects at Studies of the effects of cisapride in horses suggest it serotonin (5-hydroxytryptamine) receptors (as an may have efficacy in disorders other than post- agonist at 5-HT4 and 5-HT2; and an antagonist at 5- operative ileus that would benefit from stimulation HT3 and 5-HT1); however, there appear to be of gastric, small intestinal, or colonic motility and differences among species in action at these from shortened transit time (Evidence rating: B-2 receptors.{R-40-42; 49} [table 1][table 2]).{R-10-14; 27-32} In the dog, cisapride increases plasma motilin concentration while stimulating motility during the Regulatory Considerations interdigestive phase but during digestion, it U.S. and Canada— stimulates motility without affecting plasma {R-6} Commercial cisapride products labeled for human motilin. use were withdrawn from the United States and Cisapride has no central antiemetic effect and does not Canadian markets in 2000 due to reports of significantly affect secretion of gastric acid, {R-23; 50} adverse events.{R-34} Because there are no pancreatic enzymes, or bile secretion. commercial cisapride products, medicinal or analytic grade cisapride must be purchased from Absorption: an approved source and compounded for Oral bioavailability—In cats, dogs, horses, and human veterinary use. In the United States, refer to the beings, oral bioavailability appears to be low to {R-2; 12} Animal Medicinal Drug Use Clarification Act, moderate (30 to 60%). This is generally Food and Drug Administration regulations attributed to extensive first-pass metabolism in the pertaining to compounding (CFR 21 Part intestinal wall or liver of many species but may also {R-2; 12} 530.13), and the current Food and Drug be affected by poor drug dissolution. In fasted {R-18} Administration’s Compliance Policy Guide on rats, cisapride is almost completely absorbed. Compounding of Drugs for Use in Animals.{R-35- Availability may vary among members of the same {R-12} 37} In Canada, refer to the Health Canada Health species. Products and Food Branch’s Manufacturing and Rectal absorption—Horses: Absorption of rectally Compounding Drug Products in Canada.{R-38} administered cisapride has been investigated using aqueous, propylene glycol, and dimethylsulfoxide Chemistry formulations; at best, only half of horses achieved measurable plasma cisapride concentrations. Chemical group: Substituted piperidinyl Bioavailability appears to be low and extremely benzamide.{R-40} variable by this route.{R-10; 11; 13} Chemical name: Benzamide, 4-amino-5-chloro-N-[1- [3-(4-fluorophenoxy)propyl]-3-methoxy-4- {R-39} Distribution: piperidinyl]-2-methoxy-, cis-. {R-39} Dogs—Beagles given cisapride daily for a year showed Molecular formula: C23H29ClFN3O4. {R-39} no evidence of significant accumulation in tissues, Molecular weight: 465.95. even when given 40 mg/kg daily. Relative tissue Description: Cisapride monohydrate—White or almost drug concentrations twenty-four hours after the last white powder. dose were: colon > liver, kidney, stomach, ileum, Ionization: Weak base with a pKa1 of 7.8 and pKa2 of {R-17} {R-55} lung, pancreas > brain, skeletal muscle. 1.7. Rats—Cisapride is quickly absorbed and distributed, to Solubility: Cisapride monohydrate—Freely soluble in peak in the tissues at 15 to 30 minutes, with the dimethylformamide, soluble in methylene chloride; highest concentrations in the liver, stomach, and sparingly soluble in methanol, practically insoluble small intestine. Of a 10-mg/kg dose, 42% can reach in water (water solubility of 2.7 mg per liter). the contents of the small intestine within 2 to 4 © 2008 The United States Pharmacopeial Convention All rights reserved 2 hours. Cisapride also reaches the brain, but at levels Fertility significantly less than in plasma.{R-17} Rats: When administered at oral doses of up to 160 mg/kg a day, cisapride was found to have no effect Protein binding: on fertility in male rats. Female rats given oral doses Human beings—97.5 ± 0.2%.{R-19} of ≥ 40 mg/kg a day and the female offspring of Dogs—95.0 ± 1.5 %.{R-19} female rats given 10 mg/kg a day were found to need {R-43} Rats—91.6 ± 0.3%.{R-19} a prolonged breeding interval for impregnation. Sheep—89.0.{R-54} Pregnancy
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