Sparfloxacin

Pharmacokinetics.

 


Sparfloxacin is well absorbed from the gastrointestinal tract following
oral administration with a reported bioavailability of about 90%. Peak
plasma concentrations are achieved 3 to 6 hours after a dose.
Sparfloxacin is widely distributed into body tissues and fluids,
including respiratory tissues, but is only about 45% bound to plasma
proteins. It is metabolised in the liver by glucuronidation and has an
elimination half-life of about 20 hours. It is excreted in equal amounts
in the faeces and urine as unchanged drug and as the glucuronide
metabolite.

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Indication
& Dosage

 


Oral

INFECTIONS CAUSED BY SUSCEPTIBLE ORGANISMS: RTI, UTI, SURGICAL
INFECTIONS; SKIN & SOFT TISSUE INFECTIONS; SALMONELLOSIS; PID;
UNCOMPLICATED GONORRHEA; CHLAMYDIAL INFECTIONS: Usually 400mg on day 1.
followed by 200mg OD up to “1-2 weeks depending on infection severtiy.
Children: Not recommended.

 

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Action




It has broad-spectrum of activity against Gram-positive &
Gram-negative bacteria, including anerobes especially Bacteroides
fragilis. It is reportedly more active than ciprofloxacin against
Strep.saprophyticus. Also effective against Enterobacter spp.,
Acinetobacter spp., pseudomonas cepacia, Xanthomonas maltophilia, &
flavobacterium; other sussceptible bacteria include H.influenzae,
Salmonella, K.pneumoniae, K.oxytoca, Moraxella Catarrhalis, E.coli,
P.mirabilis, P.vulgaris, Serratia marcescens, S.liquefaciens,
Moraganella morganii, Neisseria gonorrheae, citrobacter diversus,
citrobacter freundi & Aeromonas hydrophilia; chlmaydia trachomatis;
Mycobacterium spp. It acts by inhibiting the supercoiling activity of
DNA gyrase which is an enzyme essential for DNA replication.

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Interaction

 

As sparfloxacin may prolong the QT interval it should not be
administered concomitantly with other drugs known to have this effect
(such as the antihistamines astemizole and terfenadine, cisapride,
erythromycin, pentamidine, phenothiazines, or tricyclic
antidepressants).

Sparfloxacin does not appear to interact with theophylline or
caffeine, nor with warfarin or cimetidine. Probenecid does not alter the
pharmacokinetics of sparfloxacin.

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Adverse
Effect & Precautions





G.I. disturabances (nausea,
vomiting, abdominal pain, diarrhoea) cutaneous allergy, headache,
tremor, convulsions, hallucination, insomnia, paraeshtesia.



Precaution: Avoid exposure to sunligh, discontinue the drug if skinrash
occurs, epilepsy, cardiac disease, hypokalaemia, hypomagnesaemia,
concomitant use of anti-arrhythmic drugs.

Pregnancy: Contraindicated.

Breast Feeding: Contraindicated.

Man: May be used with caution.



 

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Brands
available in market

 

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