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