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SULTAMICILLIN tosylate
SULTAMICILLIN
UNASYNTM
375 mg tablet
750 mg tablet
UNASYNTM
250 mg / 5 mL
Powder for Oral Suspension
PHARMACOLOGIC CATEGORY
Antibacterial
2.0
DESCRIPTION
Sultamicillin is a double ester in which ampicillin and the beta-lactamase inhibitor
sulbactam are linked via a methylene group. Chemically sultamicillin is the
oxymethylpenicillinate sulphone ester of ampicillin and has a molecular weight of 594.7.
3.0
FORMULATION
Unasyn 375 mg Film-Coated Tablet: Each tablet contains 375 mg sultamicillin (as
tosylate) which is a mutual prodrug of sulbactam and ampicillin yielding the equivalent of
147 mg sulbactam and 220 mg ampicillin.
Unasyn 750 mg Film-Coated Tablet: Each tablet contains 750 mg sultamicillin (as
tosylate) yielding the equivalent of 294 mg sulbactam and 440 mg ampicillin.
Unasyn 60 mL Powder for Oral Suspension: Per 5 mL contains 250 mg sultamicillin
4.0
CLINICAL PARTICULARS
4.1 Therapeutic Indications
Sultamicillin is indicated for infections caused by susceptible micro-organisms. Typical
indications are upper respiratory tract infections including sinusitis, otitis media and
tonsillitis; lower respiratory tract infections including bacterial pneumonias and
bronchitis; urinary tract infections and pyelonephritis; skin and soft tissue infections;
intra-abdominal infections and gonococcal infections.
Tablets: Patients with rare hereditary problems of galactose intolerance, the Lapp lactase
deficiency or glucose-galactose malabsorption should not take this medicine.
Powder for Oral Suspension: Patients with rare hereditary problems of fructose
intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should
not take this medicine.
Adverse reactions associated with use of ampicillin alone may be observed with
sultamicillin. Adverse reactions associated with the use of ampicillin and/or
sulbactam/ampicillin IM/IV include:
4.9 Overdose
Limited information is available on the acute toxicity of ampicillin sodium and sulbactam
sodium in humans. Overdosage of the drug would be expected to produce manifestations
that are principally extensions of the adverse reactions reported with the drug. The fact
that high CSF concentrations of -lactam antibiotics may cause neurologic effects,
including seizures, should be considered. Because ampicillin and sulbactam are both
removed from the circulation by hemodialysis, these procedures may enhance elimination
of the drug from the body if overdosage occurs in patients with impaired renal function.
5.0
PHARMACOLOGICAL PROPERTIES
5.1
Pharmacodynamic Properties
5.2
Pharmacokinetics Properties
While reversible glycogenosis was observed in laboratory animals, this phenomenon was
dose- and time-dependent and is not expected to develop at the therapeutic doses and
corresponding plasma levels attained during the relatively short periods of combined
ampicillin/sulbactam therapy in man.
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Long-term studies in animals have not been performed to evaluate carcinogenic potential.
The individual components of sultamicillin (ampicillin/sulbactam) tested negative for
mutagenicity.
Reproduction studies have been performed in mice and rats, and rabbits at doses in excess
of the human dose and have revealed no evidence of impaired fertility or harm to the fetus
due to sultamicillin. There are, however, no adequate and well controlled studies in
pregnant women.
6.0
PHARMACEUTICAL PARTICULARS
6.1 Directions for Reconstitution
Add water until the red line to the contents of this bottle to get a volume of 60 mL. Shake
until the powder is well suspended. When reconstituted, each 5 mL contains 250 mg
sultamicillin.Once reconstituted, store under refrigeration. Discard unused suspension
after 14 days.
6.2 Shelf-Life
Please see outer packaging for shelf-life data.
6.3 Special Precaution and Storage
375 mg Tablet: Store at a temperatures not exceeding 300C.
250 mg/5mL Powder for Oral Suspension and 750 mg Tablet: Store at temperatures not
exceeding 250C.
The reconstituted oral suspension must be stored under refrigeration and discarded
after 14 days.
Keep out of reach of children.
6.4 Availability
375 mg Tablets: White, capsular-shaped film-coated tablets available in box of 100s.
750 mg Tablets: A white to off-white, capsular-shaped film-coated tablets available in
box of 8s.
250 mg/5mL Powder for Oral Suspension: White to off-white powder for reconstitution
in 60 mL bottle.
Manufactured by:
375 mg Tablet
Pfizer Japan Inc.
5-Gochi, Taketoyo-Cho
Chita-Gun, Aichi-Ken, Nagoya, Japan
750 mg Tablet and 250mg/5mL Powder for Oral Suspension:
Haupt Pharma Latina S.r.l.
Strada Statale 156 Km 47,600
04010 Borgo San Michele, Latina Italy
Imported by: Pfizer, Inc.
23/F Ayala Life-FGU Center
6811 Ayala Avenue, Makati City, Philippines
Under the authority of Pfizer Inc., New York, New York, U.S.A.
References:
1) Letter from FDA issued 29 September 2006 (received 10 October 2006).
2) Wysowski DK. Increase in deaths related to enterocolitis due to Clostridium difficile in
the United States, 1999-2002. Public Health Reports 2006;121:361-362.
3) Clostridium difficile: deaths increase in 2005. Deaths: Office for National Statistics,
England and Wales. Available at: http://www.statistics.gov.uk/cci/nugget.asp?id=1735
Accessed May, 2007.
4) McDonald LC, Killgore GE, Thompson A, Owens RC Jr, Kazakova SV, Sambol SP, et
al. An epidemic, toxin gene-variant strain of Clostridium difficile. N Engl J Med
2005;353:2433-2441.
5) Loo VC, Poirier L, Miller MA, Oughton M, Libman, MD, Michaud S, et al. A
predominantly clonal multi-institutional outbreak of Clostridium difficile-associated
diarrhea with high morbidity and mortality. N Engl J Med 2005;353:2442-2449.
6) Chernak E, Johnson CC, Weltman A, McDonald LC, Wiggs L, Killgore G, et al. Severe
Clostridium difficile-associated disease in populations previously at low risk---four states,
2005. Morbidity and Mortality Weekly Report 2005;54(47);1201-1205.
Revision Number:3
Revision Date: 17 January 2012
Reference Document: CDS ver 4
Reference Date: 02 September 2011
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