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Ciprofloxacin
DESCRIPTION
Pharmaniaga Ciprofloxacin tablet 250 mg.
White, round film-coated tablet, plain on one side and scored on the other.
Pharmaniaga Ciprofloxacin tablet 500 mg.
White, oblong film-coated tablet (8 x 17 mm in dimension) plain on one side
and scored on the other.
Pharmaniaga Ciprofloxacin tablet 750 mg.
White, oblong film-coated tablet (21.5 x 10 mm in dimension) plain on one
side and scored on the other.
COMPOSITION
Pharmaniaga Ciprofloxacin tablet 250 mg. Each film-coated tablet contains:
Ciprofloxacin (as Hydrochloride) 250 mg.
Pharmaniaga Ciprofloxacin tablet
500 mg. Each film-coated tablet contains: Ciprofloxacin (as Hydrochloride)
500 mg.
Pharmaniaga Ciprofloxacin tablet 750 mg. Each film-coated tablet
contains: Ciprofloxacin (as Hydrochloride) 750 mg.
ACTIONS
Ciprofloxacin is a fluoroquinolone antibacterial agent with a strong
antibacterial activity against a broad spectrum of bacteria. These
substances are also known as gyrase inhibitors. It prevents transcription by
the chromosome (genetic material) of the information needed for the normal
metabolism of bacteria. This leads to a rapid decrease in the ability of
bacteria to reproduce. Ciprofloxacin is also characterised by the
fact that, as a result of its particular mode of action, it does not
generally exhibit parallel resistance to any other antibiotic outside the
gyrase inhibitor group. Therefore, Ciprofloxacin is highly effective against
bacteria which are resistant, eg to aminoglycosides, penicillins,
cephalosporins, tetracyclines and other antibiotics.
Ciprofloxacin has been shown to be active against most strains of the
following microorganisms, both in vitro and in clinical infections.
Aerobic Gram-positive microorganisms
Enterococcus faecalis
(Many strains are only moderately susceptible)
Staphylococcus aureus (methicillin
susceptible)
Staphylococcus epidermidis
Staphylococcus saprophyticus
Streptococcus pneumoniae
Streptococcus pyogenes
Aerobic Gram-negative microorganisms
Campylobacter jejuni
Citrobacter
diversus
Citrobacter freundii
Enterobacter cloacae
Escherichia coli
Haemophilus
influenzae
Haemophilus parainfluenzae
Klebsiella pneumoniae
Moraxella
catarrhalis
Morganella morganli
Neisseria gonorrhoeae
Proteus mirabilis
Proteus vulgaris
Providencia rettgeri
Providencia stuartii
Pseudomonas
aeruginosa
Salmonella typhi
Serratia marcescens
Shigella boydii
Shigella
dysenteriae
Shigella flexneri
Shigella sonnei
Ciprofloxacin given as an oral tablet is rapidly and well absorbed from the
gastro-intestinal tract after oral administration. The absolute
bioavailability is approximately 70% with no substantial loss by first pass
metabolism. Maximum serum concentrations are attained 1 to 2 hours after
oral dosing. Mean concentrations 12 hours after dosing with 250, 500 or 750
mg are 0.1, 0.2 and 0.4 µg/ mL, respectively. The serum elimination
half-life in subjects with normal renal function is approximately 4 hours.
The serum elimination half-life in subjects with normal renal function is
approximately 4 hours. Approximately 40 to 50% of an orally administered
dose is excreted in the urine as unchanged drug. After a 250 mg oral dose,
urine concentrations of ciprofloxacin usually exceed 200 mg/ mL during the
first 2 hours and are approximately 30 mg/ mL, at 8 to 12 hours after
dosing. The urinary excretion of ciprofloxacin is virtually complete within
24 hours after dosing. The renal clearance of ciprofloxacin which is
approximately 300 mL/ minutes, exceeds the normal glomerular filtration rate
of 120 mL/ minute. Thus, active tubular secretion would seem to play a
significant role in its elimination. Although
bile concentrations of ciprofloxacin are several fold higher than serum
concentrations after oral dosing, only a small amount of the dose
administered is recovered from the bile as unchanged drug.
An additional 1 to 2 % of the dose is recovered from the bile in the form of
metabolites. Approximately 20 to 35% of an oral dose is recovered from the
faeces within 5 days after dosing. This may arise from either biliary
clearance or trans-intestinal elimination. Four metabolites have
antimicrobial activity, but are less active than unchanged ciprofloxacin.
When ciprofloxacin tablet is given concomitantly with food there is a delay
in the absorption of the drug, resulting in peak concentrations that occur
closer to 2 hours after dosing.
The binding of ciprofloxacin to serum proteins is 20 to 40 which is not
likely to be high enough to cause significant protein binding interactions
with other drugs. After oral administration, ciprofloxacin is widely
distributed throughout the body. Tissue concentrations often exceed serum
concentrations in both men and women, particularly in genital tissue
including the prostate. Ciprofloxacin is present in active form in the
saliva, nasal and bronchial secretions, mucosa of the sinuses, sputum, skin
blister fluid, lymph, peritoneal fluid, bile and prostatic secretions.
Ciprofloxacin has also been detected in lung, skin, fat muscle, cartilage
and bone. The drug diffuses into the cerebrospinal fluid (CSF): however, CSF
concentrations are generally less than 10% of peak serum concentrations. Low
levels of the drug have been detected in the aqueous and vitreous humor of
the eye.
INDICATIONS
Uncomplicated and complicated infections caused by
ciprofloxacin-sensitive pathogens:
Infections of the
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respiratory tract. Ciprofloxacin can be regarded as an advisable treatment
for pneumonias caused by Klebsiella, Enterobacter, Proteus, Pseudomonas,
Haemophilus, Branhamella, Legionella, and Staphylococcus.
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Middle ear (otitis media), of the paranasal sinuses (sinusitis), especially
if these are caused by Gram-negative organisms including Pseudomonas or by
Staphylococcus.
- Eyes
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Kidneys and / or urinary tract.
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Genital organs, including adnexitis, gonorrhoea and prostatitis.
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Abdominal cavity (e.g. bacterial infections of the gastrointestinal tract,
biliary tract, peritonitis).
- Skin and soft tissue
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Bones and joints
Septicaemia
Ciprofloxacin is also indicated for prophylaxis against infection in
elective upper gastro-intestinal surgery and endoscopic procedures where
there is an increased risk of infection. Infections or imminent risk of
infection (prophylaxis) in patients whose immune system has been weakened
(e.g. patients on immunosuppressants or in state of neutropenia). Selective
intestinal decontamination in immunosuppressed patients.
CONTRAINDICATIONS
Ciprofloxacin must not be used in cases of hypersensitivity to ciprofloxacin
or other quinolone chemotherapeutics. Ciprofloxacin must not be prescribed
for children, adolescents, pregnant women, or nursing mothers, since there
is no experience on the drug's safety in these patient groups and since on
the basis of animal studies, it is not entirely improbable that the drug
could cause damage to articular cartilage in the immature organism.
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