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Cisapride
drug data and news
Cisapride drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Cisapride | ||
| Brand Names/Synonyms | Acenalin; Prepulsid; Propulsid; Propulsin; Alimix; Enteropride; Syspride; Pridesia; Kinestase; Cipril; Propulsid Quicksolv; R 51619; Risamal | ||
| Indication | For the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Cisapride is a parasympathomimetic which acts as a serotonin 5-HT4 agonist. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. Cisapride stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. Cisapride increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder. Cisapride does not induce muscarinic or nicotinic receptor stimulation, nor does it inhibit acetylcholinesterase activity. | ||
| Mechanism Of Action | Cisapride acts through the stimulation of the serotonin 5-HT4 receptors which increases acetylcholine release in the enteric nervous system (specifically the myenteric plexus). This results in increased tone and amplitude of gastric (especially antral) contractions, relaxation of the pyloric sphincter and the duodenal bulb, and increased peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. | ||
| Cisapride News (When available) |
Roche to Focus Resources on Availability of Invirase, Now ... Feb 6, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... Feb 9, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... 09 Feb 2006 Roche to Focus Resources on Availability of Invirase, Now ... Feb 6, 2006 FDA Approves EMEND(R) (aprepitant), in Combination with Other ... Jan 11, 2006 Bristol-Myers Squibb and Gilead Announce Data Supporting ... Jan 9, 2006 Companies Anticipate Filing New Drug Application in Second Quarter ... Jan 9, 2006 FDA Approves EMEND® (aprepitant), in Combination with Other ... Jan 11, 2006 Lexiva for the treatment of HIV infection in adults in combination ... Jan 19, 2006 FDA Approves Updated Labeling for LEXIVA Nov 18, 2005 New Data Show a Kaletra(R) (Lopinavir/Ritonavir)-Based Regimen ... Nov 18, 2005 Boehringer Ingelheim Announces 48-Week Results from Aptivus(R) ... Nov 21, 2005 Invasive aspergillosis survival, Voriconazole may be better than ... Nov 19, 2005 Former FDA Commissioner’s Ownership of Stock in Regulated ... Oct 30, 2005 New analysis supports starting with VFEND for life-threatening ... Oct 29, 2005 Erythromycin Antagonizes the Deceleration of Gastric Emptying By ... Jul 10, 2005 Omeprazole better than other drugs for indigestion Jul 26, 2005 Kaletra ® may provide convenient dosages in HIV treatment regime Jul 31, 2005 New Study Results Find That Patients Treated With Boosted INVIRASE ... Jul 25, 2005 Study Results Presented on Pharmacokinetics of Once-Daily HIV ... Jul 26, 2005 Abbott Statement on Agreement With Brazilian Government for ... 11 Jul 2005 Erythromycin Antagonizes the Deceleration of Gastric Emptying By ... Jul 10, 2005 Lucrative Drug, Danger Signals and the FDA Jun 10, 2005 Lucrative Drug, Danger Signals and the FDA Jun 10, 2005 Antifungal Vfend® provides significant cost advantages when used ... Jun 1, 2005 Committee for Medicinal Products for Human Use Post-authorisation ... May 27, 2005 MedWatch - The FDA Safety Information and Adverse Event Reporting ... Jun 10, 2005 Banned drugs available in medical shops Jun 2, 2005 News For Your Web Site Apr 19, 2005 EMEND® (aprepitant) Helps Prevent Nausea/Vomiting for Breast ... Apr 19, 2005 Black box, black hole Apr 10, 2005 FDA List Serve ~ Important Information About Sustiva (efavirenz) ... Mar 31, 2005 Bad Medicine Mar 9, 2005 Axcan Pharma expects sales of new product Itax will double ... Feb 17, 2005 Banned drugs aplenty in Karnataka Feb 11, 2005 Fair of face, foul of heart - cardiotoxicity and drug development Mar 6, 2005 WHO to fund adverse drug reaction monitoring system Feb 12, 2005 | ||
| Dosage Forms | SUSPENSION; TABLET | ||
| Drug_Category | Gastrointestinal Agents; Anti-ulcer Agents; Prokinetic Agents; Serotonin Agonists; ATC:A03FA02 | ||
| Absorption | Cisapride is rapidly absorbed after oral administration. The absolute bioavailability of cisapride is 35-40%. | ||
| Interactions | Interactions for Cisapride: Cisapride is metabolized mainly via the cytochrome P450 3A4 enzyme. In some cases where serious ventricular arrhythmias, QT prolongation, and torsades de pointes have occurred when cisapride was taken in conjunction with one of the cytochrome P450 3A4 inhibitors, elevated blood cisapride levels were noted at the time of the QT prolongation. Antibiotics: In vitro and/or in vivo data show that clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride, which can result in an increase in plasma cisapride levels and prolongation of the QT interval on the ECG. Anticholinergics: Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be expected to compromise the beneficial effects of cisapride. Anticoagulants (Oral): In patients receiving oral anticoagulants, the coagulation times were increased in some cases. It is advisable to check coagulation time within the first few days after the start and discontinuation of cisapride therapy, with an appropriate adjustment of the anticoagulant dose, if necessary. Antidepressants: In vitro data indicate that nefazodone inhibits the metabolism of cisapride, which can result in an increase in plasma cisapride levels and prolongation of the QT interval on the ECG. Antifungals: In vitro and/or in vivo data indicate that fluconazole, itraconazole, and oral ketoconazole markedly inhibit the metabolism of cisapride, which can result in an increase in plasma cisapride levels and prolongation of the QT interval on the ECG. Human pharmacokinetic data indicate that oral ketoconazole markedly inhibits the metabolism of cisapride, resulting in a mean eight-fold increase in AUC of cisapride. A study in 14 normal male and female volunteers suggests that coadministration of cisapride and ketoconazole can result in prolongation of the QT interval on the ECG. H2 Receptor Antagonists: Cimetidine coadministration leads to an increased peak plasma concentration and AUC of cisapride, there is no effect on cisapride absorption when it is coadministered with ranitidine. The gastrointestinal absorption of cimetidine and ranitidine is accelerated when they are coadministered with cisapride. Protease Inhibitors: In vitro data indicate that indinavir and ritonavir markedly inhibit the metabolism of cisapride which can result in an increase in plasma cisapride levels and prolongation of the QT interval on the ECG. Other: Coadministration of grapefruit juice with cisapride increases the bioavailability of cisapride and concomitant use should be avoided. Cisapride should not be used concomitantly with other drugs known to prolong the QT interval: certain antiarrhythmics, including those of Class IA (such as quinidine and procainamide) and Class III (such as sotalol); tricyclic antidepressants (such as amitriptyline); certain tetracyclic antidepressants (such as maprotiline); certain antipsychotic medications (such as sertindole); astemizole, bepridil, sparfloxacin, and terodiline. The preceding lists of drugs are not comprehensive. The acceleration of gastric emptying by cisapride could affect the rate of absorption of other drugs. Patients receiving narrow therapeutic ratio drugs or other drugs that require careful titration should be followed closely; if plasma levels are being monitored, they should be reassessed. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidyl]-2-methoxy-benzamide | ||
| Chemical Formula | C23H29ClFN3O4 | ||
| Molecular Weight | 465.945 g/mol | ||
| Smiles String | COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F | ||
| Melting Point | 110 °C | ||
| Water Solubility | 2.71 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 3.802 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | extensively metabolized via cytochrome P450 3A4 enzyme | ||
| Half Life | 6-12 hours | ||
| Protein Binding [%] | 97.50% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Cisapride.html http://www.rxlist.com/cgi/generic/cisap.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00454 | ||
| CAS Registry Number | 81098-60-4 | ||
| KEGG Compound ID | C06910 | ||
| PubChem ID | SID:192212 | ||
| PharmGKB ID | PA449011 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2054817 |
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