1

UI  - 1

AU  - Bosnjak SM

AU  - Neskovic-Konstantinovic ZB

AU  - Radulovic SS

AU  - Susnjar S

AU  - Mitrovi LB

AD  - Institute for Oncology and Radiology of Serbia, Belgrade, Yugoslavia. bosnjaks@ncrc.ac.yu

TI  - High efficacy of a single oral dose of ondansetron 8 mg versus a metoclopramide regimen in the prevention of acute emesis induced by fluorouracil, doxorubicin and cyclophosphamide (FAC) chemotherapy for breast cancer.[In Process Citation]

AB  - The aim of our single-center, prospective, randomized, open study was to evaluate the antiemetic efficacy and tolerability of a regimen based on a single oral dose of ondansetron 8 mg in comparison with a metoclopramide-based regimen, for prevention of acute FAC (fluorouracil, doxorubicin and cyclophosphamide) chemotherapy-induced emesis. A total of 149 chemotherapy-naive, female outpatients, under 50 years of age and with no history of alcohol consumption, scheduled to receive their first cycle of FAC chemotherapy, were included. The patients received either oral ondansetron (8 mg) or metoclopramide (1.5 mg/kg, i.v.), both combined with dexamethasone (16 mg, i.v.) and alprazolam (0.5 mg t.i.d. orally). No antiemetic prophylaxis was given for delayed emesis. Complete control of acute vomiting was obtained in 69/74 (93%) of patients receiving ondansetron, and in 49/75 (65%) of those receiving metoclopramide (p=0.00003). Complete control of acute nausea was obtained in 58% of patients receiving ondansetron and in 36% of those receiving metoclopramide (p=0.007). Complete prevention of delayed vomiting/nausea was achieved in 73%/20% and 60%/16% of patients, respectively. Sedation was more frequent in the metoclopramide arm (p=0.04). As far as we know this is the first study that supports the efficacy of a regimen based on a single oral dose of ondansetron 8 mg in the prevention of acute FAC chemotherapy-induced emesis. The ondansetron regimen was highly effective in female patients and was superior to the metoclopramide based regimen

RP  - NOT IN FILE

NT  - UI - 21011474LA - engPT - Journal ArticleDA - 20001220IS - 1120-009XCY - ItalyJC - JCYAA - Author

UR  - PM:0011128567

SO  - J Chemother 2000 Oct ;12(5):446-453

 

2

UI  - 3

AU  - Ding P

AU  - Xu H

AU  - Wei G

AU  - Zheng J

AD  - Department of Pharmacy, Shenyang Pharmaceutical University, People's Republic of China. dingpt402@yahoo.com

TI  - Microdialysis sampling coupled to HPLC for transdermal delivery study of ondansetron hydrochloride in rats

AB  - The transdermal delivery of ondansetron hydrochloride (ON) solution in propylene glycol (PG) with a widely used penetration enhancer, oleic acid (OA), was studied in rats by a microdialysis sampling technique. Dialysate samples collected from the probe were directly injected into the HPLC system without any pre-treatment and no interference occurred in the blank sample. A good linearity between the standard concentrations and peak areas within the calibration range was achieved. In vivo recovery (32.52 +/- 1.8%) of the probe was assessed with the retrodialysis method, which was used to calculate the ON concentration in the dermis. Oleic acid at the concentrations of 2% and 5% (w/v) increased the steady-state delivery rate from 0.001 to 0.030 and 0.058 microg/h, respectively. OA proved to be an effective enhancer for transdermal delivery of ON in rats

MH  - Administration,Cutaneous

MH  - Animal

MH  - Antiemetics

MH  - administration & dosage

MH  - analysis

MH  - Chromatography,High Pressure Liquid

MH  - methods

MH  - Kinetics

MH  - Male

MH  - Microdialysis

MH  - Oleic Acid

MH  - Ondansetron

MH  - pharmacokinetics

MH  - Propylene Glycol

MH  - Rats

MH  - Serotonin Antagonists

MH  - Skin

MH  - chemistry

MH  - metabolism

MH  - Solutions

RP  - NOT IN FILE

NT  - UI - 20306788LA - EngRN - 0 (Antiemetics)RN - 0 (Serotonin Antagonists)RN - 0 (Solutions)RN - 112-80-1 (Oleic Acid)RN - 57-55-6 (Propylene Glycol)RN - 99614-02-5 (Ondansetron)PT - JOURNAL ARTICLEDA - 20000906IS - 0269-3879SB - MCY - ENGLANDJC - BIMAA - AuthorEM - 200011

UR  - PM:0010850615

SO  - Biomed Chromatogr 2000 May ;14(3):141-143

 

3

UI  - 9

AU  - Wilde MI

AU  - Markham A

AD  - Adis International Limited, Auckland, New Zealand

TI  - Ondansetron. A review of its pharmacology and preliminary clinical findings in novel applications

AB  - The use of ondansetron, a selective serotonin 5-HT3 receptor antagonist, is well established in patients with nausea and vomiting associated with cancer chemotherapy, radiotherapy or anaesthesia and surgery. The wide distribution of 5-HT3 receptors in the body and the role of these receptors in disease have provided the rationale for investigation of ondansetron in novel applications. Preliminary data have shown ondansetron to have clinical benefit in patients with nausea and vomiting associated with drug overdosage or poisoning, anti- infective or antidepressant therapies, uraemia or neurological trauma, and in patients with pruritus. Patients with gastrointestinal motility disorders (e.g. carcinoid syndrome, irritable bowel syndrome, diarrhoea associated with cryptosporidiosis or diabetes, and chronic refractory diarrhoea) have also shown some improvement when treated with ondansetron, as have patients with certain pain or CNS-related disorders [e.g. alcohol (ethanol) dependence, opiate withdrawal, vertigo, cerebellar tremor and Parkinson's disease treatment-related psychosis]. In contrast to conventional antiemetics, ondansetron is generally well tolerated with a lower incidence of sedation and only isolated case reports of extrapyramidal reactions. Furthermore, unlike dopamine receptor-blocking neuroleptics, ondansetron does not appear to worsen the symptoms of Parkinson's disease. Thus, in addition to its established indications, preliminary results suggest that ondansetron may be beneficial in a number of novel applications. This drug may represent a treatment alternative in patients with refractory disease, or an effective treatment of conditions for which current therapies are either poorly tolerated or not available. Further investigation of ondansetron in a range of potential new applications appears to be warranted

MH  - Animal

MH  - Antiemetics

MH  - therapeutic use

MH  - Brain

MH  - drug effects

MH  - Colonic Diseases,Functional

MH  - drug therapy

MH  - Drug Interactions

MH  - Drug Tolerance

MH  - Gastrointestinal System

MH  - Human

MH  - Malignant Carcinoid Syndrome

MH  - Nausea

MH  - Ondansetron

MH  - administration & dosage

MH  - pharmacology

MH  - Pain

MH  - Pruritus

MH  - Rats

MH  - Receptors,Serotonin

MH  - Serotonin Antagonists

MH  - Vomiting

RP  - NOT IN FILE

NT  - UI - 97081306LA - EngRN - 0 (Antiemetics)RN - 0 (Receptors, Serotonin)RN - 0 (Serotonin Antagonists)RN - 99614-02-5 (Ondansetron)PT - JOURNAL ARTICLEPT - REVIEWPT - REVIEW, ACADEMICDA - 19970422IS - 0012-6667SB - MCY - NEW ZEALANDJC - EC2AA - AuthorEM - 199706

UR  - PM:0009118822

SO  - Drugs 1996 Nov ;52(5):773-794

 

4

UI  - 11

AU  - Swift RM

AU  - Davidson D

AU  - Whelihan W

AU  - Kuznetsov O

AD  - Department of Psychiatry and Human Behavior, Brown University Medical School, Providence, Rhode Island, USA

TI  - Ondansetron alters human alcohol intoxication

AB  - There is considerable evidence that serotonin-3 (5-HT3) receptor antagonists modulate some of the behavioral effects of alcohol, and may decrease alcohol consumption. To better clarify the mechanism of action of 5-HT3 antagonists on these behaviors, we investigated the effects of the 5-HT3 antagonist, ondansetron, on several subjective and objective measures of alcohol intoxication in social drinkers. Twelve nonalcoholic, social drinkers received either 8 mg ondansetron, p.o., or placebo during one of two test sessions in a crossover, double-blind protocol. Both conditions were followed by a standard, intoxicating dose of alcohol. Subjective and objective measures of intoxication including mood, physical sensations, performance changes, and alcohol pharmacokinetics were determined. To control for ondansetron effects, 10 additional subjects received either ondansetron or placebo, followed by a nonintoxicating, "placebo" dose of alcohol during a second crossover double-blind protocol. Ondansetron was found to augment certain stimulant, sedative, and discriminant effects of alcohol, without affecting psychomotor performance or alcohol pharmacokinetics. Ondansetron had minimal effects on subjects receiving placebo alcohol. These data suggest that the reductions in alcohol consumption observed in animals and humans treated with ondansetron may be mediated by increases in subjective intoxication, and/or increases in the aversive effects of alcohol

MH  - Adult

MH  - Affect

MH  - drug effects

MH  - Aged

MH  - Alcohol Drinking

MH  - drug therapy

MH  - psychology

MH  - Alcoholic Intoxication

MH  - Blood Pressure

MH  - Central Nervous System Depressants

MH  - pharmacokinetics

MH  - Cross-Over Studies

MH  - Double-Blind Method

MH  - Drug Interactions

MH  - Ethanol

MH  - Female

MH  - Human

MH  - Male

MH  - Middle Age

MH  - Ondansetron

MH  - therapeutic use

MH  - Psychomotor Performance

MH  - Pulse

MH  - Serotonin Antagonists

MH  - Support,Non-U.S.Gov't

RP  - NOT IN FILE

NT  - UI - 97033814LA - EngRN - 0 (Central Nervous System Depressants)RN - 0 (Serotonin Antagonists)RN - 64-17-5 (Ethanol)RN - 99614-02-5 (Ondansetron)PT - CLINICAL TRIALPT - JOURNAL ARTICLEPT - RANDOMIZED CONTROLLED TRIALDA - 19970203IS - 0006-3223SB - MCY - UNITED STATESJC - A3SAA - AuthorEM - 199704

UR  - PM:0008879472

SO  - Biol Psychiatry 1996 Sep 15 ;40(6):514-521

 

5

UI  - 14

AU  - Sellers EM

AU  - Toneatto T

AU  - Romach MK

AU  - Somer GR

AU  - Sobell LC

AU  - Sobell MB

AD  - Mental Health Unit, University of Toronto, Ontario, Canada

TI  - Clinical efficacy of the 5-HT3 antagonist ondansetron in alcohol abuse and dependence

AB  - Medications that act on the serotonergic system have been found to be of benefit in the treatment of alcohol-dependent individuals. In a randomized, placebo-controlled study, the efficacy of 6 weeks of ondansetron, a 5-HT3 antagonist (0.25 mg bid or 2.0 mg bid), in the treatment of 71 nonseverely alcohol-dependent males was tested. The results showed reduction of drinking differences were steadily increasing toward the end of the treatment period approached significance at week 7 in the 0.25 mg group (p = 0.06). Twice as many patients in this group showed > or = 2 standard deviations decrease in drinking compared with the other groups. When patients drinking > 10 drinks/drinking day at baseline (n = 11) were excluded from the analysis, significant group differences were found at both treatment and follow-up, with the lower ondansetron dose producing the greatest reduction from baseline (i.e., 2.8 standard drinks; -35% compared with baseline and -21% compared with placebo; p < 0.02-0.001). Within this group, there was an almost 4-fold greater number of patients showing a clinically meaningful decrease in drinking. Lower baseline drinking and higher level of education were significant and strong predictors of drinking reduction during treatment. Ondansetron was very well tolerated; hence, further long-term studies with 5-HT3 antagonists alone or in combination with other treatment components may offer promise for treatment of alcoholism

MH  - Adult

MH  - Alcoholism

MH  - rehabilitation

MH  - Dose-Response Relationship,Drug

MH  - Double-Blind Method

MH  - Follow-Up Studies

MH  - Human

MH  - Male

MH  - Middle Age

MH  - Ondansetron

MH  - administration & dosage

MH  - adverse effects

MH  - Receptors,Serotonin

MH  - classification

MH  - drug effects

MH  - Support,Non-U.S.Gov't

RP  - NOT IN FILE

NT  - UI - 95068751LA - EngRN - 0 (Receptors, Serotonin)RN - 99614-02-5 (Ondansetron)PT - CLINICAL TRIALPT - JOURNAL ARTICLEPT - RANDOMIZED CONTROLLED TRIALDA - 19941220IS - 0145-6008SB - MCY - UNITED STATESJC - 35XAA - AuthorEM - 199502

UR  - PM:0007978099

SO  - Alcohol Clin Exp Res 1994 Aug ;18(4):879-885

 

6

UI  - 16

AU  - Johnson BA

AU  - Rue J

AU  - Cowen PJ

AD  - MRC Unit of Clinical Pharmacology, Littlemore Hospital, Oxford, UK

TI  - Ondansetron and alcohol pharmacokinetics

MH  - Adult

MH  - Cross-Over Studies

MH  - Double-Blind Method

MH  - Ethanol

MH  - blood

MH  - pharmacokinetics

MH  - Human

MH  - Male

MH  - Middle Age

MH  - Ondansetron

MH  - pharmacology

MH  - Support,Non-U.S.Gov't

RP  - NOT IN FILE

NT  - UI - 95175795LA - EngRN - 64-17-5 (Ethanol)RN - 99614-02-5 (Ondansetron)PT - CLINICAL TRIALPT - JOURNAL ARTICLEPT - RANDOMIZED CONTROLLED TRIALDA - 19950329IS - 0033-3158SB - MCY - GERMANYJC - QGIEM - 199506

UR  - PM:0007871005

SO  - Psychopharmacology (Berl) 1993  ;112(1):145

 

7

UI  - 18

AU  - Costall B

AU  - Jones BJ

AU  - Kelly ME

AU  - Naylor RJ

AU  - Onaivi ES

AU  - Tyers MB

AD  - Postgraduate Studies in Pharmacology, School of Pharmacy, University of Bradford, U.K

TI  - Ondansetron inhibits a behavioural consequence of withdrawing from drugs of abuse

AB  - The ability of the selective 5-HT3 receptor antagonist ondansetron to influence the behavioural consequences of withdrawal from chronic treatment with ethanol, nicotine or cocaine was investigated in the light/dark exploration test in the mouse and social interaction test in the rat. In both tests acute and chronic (7 days) treatments with ondansetron (0.01-1.0 microgram.kg-1 IP) disinhibited suppressed behaviour; withdrawal from chronic treatment (0.1 mg/kg IP b.i.d.) did not exacerbate the behavioural suppression. Chronic treatment for 14 days with ethanol (8% w/v in the drinking water), nicotine (0.1 mg/kg b.i.d.) or cocaine (1.0 mg/kg b.i.d.) released suppressed behaviour in the mouse and rat tests. Behavioural suppression was increased following withdrawal from ethanol, nicotine and cocaine. The administration of ondansetron (0.01 mg/kg IP b.i.d.) during the period of ethanol, nicotine and cocaine withdrawal prevented the exacerbation in suppressed behaviour. It is concluded that ondansetron potently reduces behavioural suppression during acute and chronic treatments in the rodent models, does not cause a rebound exacerbation of behavioural suppression following withdrawal, and is a highly effective inhibitor of the increased behavioural suppression following withdrawal from the drugs of abuse: ethanol, nicotine and cocaine

MH  - Animal

MH  - Cocaine

MH  - toxicity

MH  - Ethanol

MH  - Exploratory Behavior

MH  - drug effects

MH  - Imidazoles

MH  - pharmacology

MH  - therapeutic use

MH  - Male

MH  - Mice

MH  - Nicotine

MH  - Rats

MH  - Rats,Inbred Strains

MH  - Receptors,Serotonin

MH  - antagonists & inhibitors

MH  - Social Behavior

MH  - Street Drugs

MH  - Substance Withdrawal Syndrome

MH  - prevention & control

RP  - NOT IN FILE

NT  - UI - 90287934LA - EngRN - 0 (Imidazoles)RN - 0 (Receptors, Serotonin)RN - 0 (Street Drugs)RN - 50-36-2 (Cocaine)RN - 54-11-5 (Nicotine)RN - 64-17-5 (Ethanol)RN - 99614-02-5 (Ondansetron)PT - JOURNAL ARTICLEDA - 19900720IS - 0091-3057SB - MCY - UNITED STATESJC - P3QAA - AuthorEM - 199009

UR  - PM:0002141423

SO  - Pharmacol Biochem Behav 1990 Jun ;36(2):339-344