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Respected sir,
I am post graduate student in veterinary
pharmacology . I am working on pharmacokinetics of Sparfloxacin in
calves by antiboitic assay method.
using E.coli. as test organisms. I request you to send me
information regarding references of pharmacokinetics of sparfloxacin
and the laboratory protocol if any, of the method.
sir, I also request you for any precautions to be taken
during the research.
your help will be highly appriciated.
yours sincerly
- Dr N.suresh Babu
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[A few replies - db]
Date: Wed, 22 Mar 2000 01:29:29 -0700 (MST)
X-Sender: ml11439.-at-.pop.goodnet.com
To: PharmPK.-a-.boomer.org
=46rom: ml11439.at.goodnet.com (Michael J. Leibold)
Subject: Re: PharmPK Pharmacokinetics of Sparfloxacin
Dear Mr.Babu,
Here are a few references:
Good luck!
Mike Leibold, PharmD, RPh
ML11439.-at-.goodnet.com
<1>
Unique Identifier
97400244
Authors
Zix JA. Geerdes-Fenge HF. Rau M. Vockler J. Borner K. Koeppe P. =
Lode H.
Institution
Department of Pulmonary and Infectious Diseases, City Hospital
Zehlendorf-Heckeshorn, Freie Universitat Berlin, Germany.
Title
Pharmacokinetics of sparfloxacin and interaction with
cisapride and sucralfate.
Source
Antimicrobial Agents & Chemotherapy. 41(8):1668-72, 1997 Aug.
Abstract
In an open, randomized, triple crossover study, the effects of=
cisapride and
sucralfate on the pharmacokinetics of sparfloxacin were
assessed. Fifteen healthy volunteers received 400 mg of
sparfloxacin as a single oral dose on day 0. In a random
order, concomitant doses of 10 mg of cisapride three times daily from=
day -2
to day 2 and 1 g of sucralfate four times daily from day -2 to day 0 we=
re
administered. Sparfloxacin concentrations were measured by
bioassay and high-performance liquid chromatography. Pharmacokinetic
parameters for sparfloxacin alone were as follows (mean +/-
standard deviation): maximum concentration of drug in serum (C(max)), 1=
=2E27
+/- 0.39 microg/ml; time to C(max) (T(max)), 4.1 +/- 1.9 h; area under =
the
concentration-time curve (AUC), 35.0 +/- 9.7 microg x h/ml; mean reside=
nce
time, 28.5 +/- 5.7 h; half-life (t1/2), 20 +/- 4 h; urinary recovery=
(UR x
f), 11.0% +/- 2.7%; and metabolite-sparfloxacin ratio in
urine, 2.6. For the cisapride group there was a significant decrease in=
the
sparfloxacin T(max) (1.9 +/- 2.1 h) and a significant
increase in C(max) (1.74 +/- 0.73 microg/ml). The QTc interval for pati=
ents
receiving sparfloxacin and cisapride was prolonged by 7.7%
compared to the QTc interval during medication-free periods. Significan=
t
differences in the values for the group receiving sucralfate compared=
to the
values for the group receiving sparfloxacin alone were
found: C(max), 0.77 +/- 0.31 microg/ml; AUC, 18.6 +/- 5.8 microg x h/ml=
;
t1/2, 26 +/- 10 h; and UR x f, 5.8 +/- 1.8%. Concomitant adminstration =
of
cisapride accelerates the absorption and increases the peak=
concentration of
sparfloxacin without having a significant effect on the
extent of bioavailability. Coadministration of sucralfate leads to a 44=
%
decrease in the bioavailability of sparfloxacin.
<2>
Unique Identifier
97253224
Authors
Goa KL. Bryson HM. Markham A.
Institution
Adis International Limited, Auckland, New Zealand.
Title
Sparfloxacin. A review of its antibacterial activity,
pharmacokinetic properties, clinical efficacy and tolerability in lower
respiratory tract infections. [Review] [150 refs]
Source
Drugs. 53(4):700-25, 1997 Apr.
Abstract
Sparfloxacin is a fluoroquinolone antibacterial agent with
activity against a broad range of Gram-negative and Gram-positive organ=
isms
including Streptococcus pneumoniae, one of the main pathogens in
community-acquired pneumonia. In this infection,
sparfloxacin has shown efficacy similar to that of
amoxicillin, erythromycin, roxithromycin, amoxicillin/clavulanic acid a=
nd
amoxicillin plus ofloxacin, producing clinical cure rates of 80 to 84%
assessed by intention-to-treat analyses in European or multinational tr=
ials.
US studies showed similar results for sparfloxacin to those
for erythromycin and cefaclor. Sparfloxacin was also as
effective as all other comparator drugs in patients with other lower
respiratory tract infections, usually acute exacerbations of chronic
obstructive pulmonary disease (COPD). The profile of adverse effects fo=
r
sparfloxacin is generally similar to that of other
quinolones: gastrointestinal discomfort and CNS effects are
the most common in clinical trials. Sparfloxacin causes
fewer gastrointestinal disturbances than agents such as amoxicillin and
erythromycin and doses not interact with theophylline, an important
consideration when treating patients with respiratory disease. Its long
elimination half-life permits once-daily dosage regimens. On the other =
hand,
there are infrequent reports of prolonged QTc interval (3% increase) du=
ring
sparfloxacin therapy. Photosensitivity occurs more
frequently than with the other fluoroquinolones (2% of
patients in an ongoing postmarketing study and 7.9% of those in US tria=
ls),
and requires ongoing surveillance. In summary, the good activity of
sparfloxacin against S. pneumoniae and other respiratory
pathogens supports its use in lower respiratory tract infections,
particularly community-acquired pneumonia. Its profile of good efficacy=
,
once-daily dosage, good gastrointestinal tolerability and lack of inter=
action
with theophylline are advantageous, but clinicians and patients must be=
alert
to the possibility of photosensitivity reactions. On this basis,
sparfloxacin, when appropriately prescribed, can provide the
clinician with a useful alternative treatment option for these common
infections. [References: 150]
---
Date: Wed, 22 Mar 2000 01:38:32 -0700 (MST)
X-Sender: ml11439.-at-.pop.goodnet.com
To: PharmPK.at.boomer.org
=46rom: ml11439.at.goodnet.com (Michael J. Leibold)
Subject: Re: PharmPK Pharmacokinetics of Sparfloxacin
Mr.Babu,
Here are a few more:
Mike Leibold, PharmD,RPh
ML11439.at.goodnet.com
<1>
Unique Identifier
99113646
Authors
Johnson RD. Dorr MB. Talbot GH. Caille G.
Institution
Rhone-Poulenc Rorer Pharmaceuticals, Collegeville, Pennsylvania 19426-0=
800,
USA.
Title
Effect of Maalox on the oral absorption of sparfloxacin.
Source
Clinical Therapeutics. 20(6):1149-58, 1998 Nov-Dec.
Abstract
Sparfloxacin is a broad-spectrum oral
fluoroquinolone antimicrobial agent with a long elimination
half-life (t(1/2)). Concurrent treatment with antacids has demonstrated=
a
reduction in the oral absorption of many quinolones. This study was
undertaken to determine an optimal time for dosing antacids in relation=
to
sparfloxacin administration to minimize antacid-induced
reduction in sparfloxacin bioavailability. This open-label,
single-dose, randomized, four-way crossover study was conducted in 20 h=
ealthy
male volunteers between the ages of 18 and 38 years. Treatments=
consisted of
single 400-mg oral doses of sparfloxacin alone and with
Maalox 30 mL given 2 hours before, 2 hours after, and 4 hours after ora=
l
administration of sparfloxacin. All 20 subjects completed
the study. A 400-mg single oral dose of sparfloxacin was
well tolerated both given alone and with Maalox. Maalox given 4 hours a=
fter
sparfloxacin administration was the only regimen that did
not cause a statistically significant reduction in the rate and extent =
of
sparfloxacin absorption. The 90% confidence intervals
comparing sparfloxacin alone with the preceding regimen in
terms of area under the concentration-time curve from zero to infinity
(AUC(0-infinity)) and maximum plasma concentration (Cmax) were within t=
he
range 80% to 125%. Administration of Maalox 2 hours before, 2 hours aft=
er,
and 4 hours after sparfloxacin caused mean decreases in
AUC(0-infinity) of 23%, 17%, and 5%, respectively. Corresponding=
decreases in
mean Cmax values were 29% with Maalox administered 2 hours before
sparfloxacin and 13% with Maalox administered 2 hours after
sparfloxacin. The mean Cmax value was un affected when
Maalox was administered 4 hours after sparfloxacin
administration. The 90% confidence intervals for these comparisons with
sparfloxacin alone were outside the 80% to 125% range and
did not include 100%. Time to Cmax and t(1/2) were similar for all four
regimens. The elimination rate of sparfloxacin was
unaffected by concomitant administration with Maalox in healthy male
volunteers.
<2>
Unique Identifier
99075494
Authors
Kamberi M. Kotegawa T. Tsutsumi K. Nakamura K. Nakano S.
Institution
Department of Clinical Pharmacology and Therapeutics, Oita Medical
University, Japan. Marika.aaa.Oita-med.ac.jp
Title
Sparfloxacin pharmacokinetics in healthy volunteers: the
influence of acidification and alkalinization.
Source
European Journal of Clinical Pharmacology. 54(8):633-7, 1998 Oct.
Abstract
OBJECTIVE: To investigate the effect of acidification and=
alkalinization on
the pharmacokinetics of sparfloxacin in healthy subjects.
METHODS: A single 200-mg oral dose of sparfloxacin was given
to nine healthy Japanese volunteers on three separate occasions under
different conditions of urinary pH. Acidic and alkaline conditions were
achieved by repeated oral doses of ammonium chloride and sodium bicarbo=
nate,
respectively. The concentrations of sparfloxacin and its
metabolite in plasma and urine were determined by high-performance liqu=
id
chromatography assays. RESULTS: The difference between treatments for C=
max,
AUCinfinity, and CL x f(-1) were found to be significant. The relative
bioavailability of sparfloxacin was 84.4% and 122.3% after
ammonium chloride and sodium bicarbonate treatments, respectively. The =
amount
of unchanged sparfloxacin in urine samples collected 0-48 h
after sparfloxacin administration represented 10.1% of the
dose in the control, 14.3% of the dose in urine acidification and 8.4%=
of the
dose with alkalinization of urine. Renal clearance was found to depend =
on
urinary pH. However, the plasma elimination and the metabolism of
sparfloxacin were not significantly altered by acidification
or alkalinization of the urine. CONCLUSION: The urinary pH dependence=
of the
renal clearance of sparfloxacin will be of minor clinical
importance with regard to the low contribution of renal excretion to the
overall elimination of sparfloxacin. On the other hand, the
alteration in the environmental pH in the gastrointestinal tract, produced by
the concomitant ingestion of ammonium chloride or sodium bicarbonate,
influences the absorption and bioavailability of
sparfloxacin. This effect is likely to be clinically
significant.
---
X-Originating-IP: [194.27.136.195]
=46rom: "=F7zlem =ABukurlu"
To: PharmPK.-a-.boomer.org, nsuresh.at.gau.guj.nic.in
Subject: Re: PharmPK Pharmacokinetics of Sparfloxacin
Date: Wed, 22 Mar 2000 07:44:45 PST
Dear Dr N. suresh Babu,
=46or the antibiotic assay methods of Sparfloxacin , i recommend you to
make a medline search. The useful sites i offer you are :
www.medscape.com , www.healthgate.com and www.biomednet.com.
Registeration is a necessity so make sure to register first.
Sincerely ,
=D6zlem =C7ukurlu
Istanbul University
Faculty of Pharmacy
PharmPK Discussion List Archive Index page
Copyright 1995-2010 David W. A. Bourne (david@boomer.org)