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Ciproxin 500 Mg 10 Tablets

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WARNING:

Fluoroquinolones, including Ciproxin®, are associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart or lung transplants (see WARNINGS).

Fluoroquinolones, including Ciproxin, may exacerbate muscle weakness in persons with myasthenia gravis. Avoid Ciproxin in patients with known history of myasthenia gravis (see WARNINGS).

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Ciproxin Tablets and Ciproxin Oral Suspension and other antibacterial drugs, Ciproxin Tablets and Ciproxin Oral Suspension should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

DESCRIPTION

Ciproxin (ciprofloxacin hydrochloride) Tablets and Ciproxin (ciprofloxacin*) Oral Suspension are synthetic broad spectrum antimicrobial agents for oral administration. Ciprofloxacin hydrochloride, USP, a fluoroquinolone, is the monohydrochloride monohydrate salt of 1-cyclopropyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid. It is a faintly yellowish to light yellow crystalline substance with a molecular weight of 385.8. Its empirical formula is C17H18FN3O3•HCl•H2O and its chemical structure is as follows:

Ciprofloxacin Hydrochloride structural formula

Ciprofloxacin is 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid. Its empirical formula is C17H18FN3O3 and its molecular weight is 331.4. It is a faintly yellowish to light yellow crystalline substance and its chemical structure is as follows:

formula

Ciproxin film-coated tablets are available in 250 mg and 500 mg (ciprofloxacin equivalent) strengths. Ciprofloxacin tablets are white to slightly yellowish. The inactive ingredients are cornstarch, microcrystalline cellulose, silicon dioxide, crospovidone, magnesium stearate, hypromellose, titanium dioxide, and polyethylene glycol.

Ciprofloxacin Oral Suspension is available in 5% (5 g ciprofloxacin in 100 mL) and 10% (10 g ciprofloxacin in 100 mL) strengths. Ciprofloxacin Oral Suspension is a white to slightly yellowish suspension with strawberry flavor which may contain yellow-orange droplets. It is composed of ciprofloxacin microcapsules and diluent which are mixed prior to dispensing (See Instructions for Use/Handling). The components of the suspension have the following compositions:

Microcapsules – ciprofloxacin, povidone, methacrylic acid copolymer, hypromellose, magnesium stearate, and Polysorbate 20.

Diluent – medium-chain triglycerides, sucrose, lecithin, water, and strawberry flavor.

Five (5) mL of 5% suspension contains approximately 1.4 g of sucrose and 5 mL of 10% suspension contains approximately 1.3 g of sucrose.

CLINICAL PHARMACOLOGY

Absorption

Ciprofloxacin given as an oral tablet is rapidly and well absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability is approximately 70% with no substantial loss by first pass metabolism. Ciprofloxacin maximum serum concentrations and area under the curve are shown in the chart for the 250 mg to 1000 mg dose range.


Dose 
(mg)

Maximum 
Serum Concentration 
(mcg/mL)

Area 
Under Curve (AUC) 
(mcg•hr/mL)

 250

1.2

 4.8

 500

2.4

11.6

 750

4.3

20.2

1000

5.4

30.8

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 mcg/mL, respectively. The serum elimination half-life in subjects with normal renal function is approximately 4 hours. Serum concentrations increase proportionately with doses up to 1000 mg.

A 500 mg oral dose given every 12 hours has been shown to produce an area under the serum concentration time curve (AUC) equivalent to that produced by an intravenous infusion of 400 mg ciprofloxacin given over 60 minutes every 12 hours. A 750 mg oral dose given every 12 hours has been shown to produce an AUC at steady-state equivalent to that produced by an intravenous infusion of 400 mg given over 60 minutes every 8 hours. A 750 mg oral dose results in a Cmax similar to that observed with a 400 mg IV dose. A 250 mg oral dose given every 12 hours produces an AUC equivalent to that produced by an infusion of 200 mg ciprofloxacin given every 12 hours.

Steady-state Pharmacokinetic Parameters Following Multiple Oral and IV Doses

aAUC 0-12h

bAUC 24h=AUC0-12h x 2

cAUC 24h=AUC0-8h x 3

Parameters

500 mg

400 mg

750 mg

400 mg

     

AUC (mcg•hr/mL)

q12h, P.O.
13.7a

q12h, IV
12.7a

q12h, P.O.
31.6b

q8h, IV
32.9c

     

Cmax (mcg/mL)

2.97

4.56

3.59

4.07

     

Distribution

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 humors of the eye.

Metabolism

Four metabolites have been identified in human urine which together account for approximately 15% of an oral dose. The metabolites have antimicrobial activity, but are less active than unchanged ciprofloxacin. Ciprofloxacin is an inhibitor of human cytochrome P450 1A2 (CYP1A2) mediated metabolism. Coadministration of ciprofloxacin with other drugs primarily metabolized by CYP1A2 results in increased plasma concentrations of these drugs and could lead to clinically significant adverse events of the coadministered drug (seeCONTRAINDICATIONS; WARNINGS; PRECAUTIONS: Drug Interactions).

Excretion

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 mcg/mL during the first two hours and are approximately 30 mcg/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/minute, exceeds the normal glomerular filtration rate of 120 mL/minute. Thus, active tubular secretion would seem to play a significant role in its elimination. Co-administration of probenecid with ciprofloxacin results in about a 50% reduction in the ciprofloxacin renal clearance and a 50% increase in its concentration in the systemic circulation. 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 feces within 5 days after dosing. This may arise from either biliary clearance or transintestinal elimination.

With oral administration, a 500 mg dose, given as 10 mL of the 5% Ciproxin Suspension (containing 250 mg ciprofloxacin/5mL) is bioequivalent to the 500 mg tablet. A 10 mL volume of the 5% Ciproxin Suspension (containing 250 mg ciprofloxacin/5mL) is bioequivalent to a 5 mL volume of the 10% Ciproxin Suspension (containing 500 mg ciprofloxacin/5mL).

Drug-Drug Interactions

When Ciproxin 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 rather than 1 hour whereas there is no delay observed when Ciproxin Suspension is given with food. The overall absorption of Ciproxin Tablet or Ciproxin Suspension, however, is not substantially affected. The pharmacokinetics of ciprofloxacin given as the suspension are also not affected by food. Concurrent administration of antacids containing magnesium hydroxide or aluminum hydroxide may reduce the bioavailability of ciprofloxacin by as much as 90%. (See PRECAUTIONS.)

The serum concentrations of ciprofloxacin and metronidazole were not altered when these two drugs were given concomitantly.

Concomitant administration with tizanidine is contraindicated. (See CONTRAINDICATIONS.) Concomitant administration of ciprofloxacin with theophylline decreases the clearance of theophylline resulting in elevated serum theophylline levels and increased risk of a patient developing CNS or other adverse reactions. Ciprofloxacin also decreases caffeine clearance and inhibits the formation of paraxanthine after caffeine administration. (See WARNINGS: PRECAUTIONS.)

Special Populations

Pharmacokinetic studies of the oral (single dose) and intravenous (single and multiple dose) forms of ciprofloxacin indicate that plasma concentrations of ciprofloxacin are higher in elderly subjects (> 65 years) as compared to young adults. Although the Cmax is increased 16-40%, the increase in mean AUC is approximately 30%, and can be at least partially attributed to decreased renal clearance in the elderly. Elimination half-life is only slightly (~20%) prolonged in the elderly. These differences are not considered clinically significant. (SeePRECAUTIONS: Geriatric Use.)

Patients withRenal Impairment

In patients with reduced renal function, the half-life of ciprofloxacin is slightly prolonged. Dosage adjustments may be required. (See DOSAGE AND ADMINISTRATION.)

Patients withHepatic Impairment

In preliminary studies in patients with stable chronic liver cirrhosis, no significant changes in ciprofloxacin pharmacokinetics have been observed. The kinetics of ciprofloxacin in patients with acute hepatic insufficiency, however, have not been fully elucidated.

Pediatrics

Following a single oral dose of 10 mg/kg ciprofloxacin suspension to 16 children ranging in age from 4 months to 7 years, the mean Cmax was 2.4 mcg/mL (range: 1.5 – 3.4 mcg/mL) and the mean AUC was 9.2 mcg*h/mL (range: 5.8 – 14.9 mcg*h/mL). There was no apparent age-dependence, and no notable increase in Cmax or AUC upon multiple dosing (10 mg/kg TID). In children with severe sepsis who were given intravenous ciprofloxacin (10 mg/kg as a 1-hour infusion), the mean Cmax was 6.1 mcg/mL (range: 4.6 – 8.3 mcg/mL) in 10 children less than 1 year of age; and 7.2 mcg/mL (range: 4.7 – 11.8 mcg/mL) in 10 children between 1 and 5 years of age. The AUC values were 17.4 mcg*h/mL (range: 11.8 – 32 mcg*h/mL) and 16.5 mcg*h/mL (range: 11 – 23.8 mcg*h/mL) in the respective age groups. These values are within the range reported for adults at therapeutic doses. Based on population pharmacokinetic analysis of pediatric patients with various infections, the predicted mean half-life in children is approximately 4 - 5 hours, and the bioavailability of the oral suspension is approximately 60%.

MICROBIOLOGY

Mechanism of Action

The bactericidal action of ciprofloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV (both Type II topoisomerases), which are required for bacterial DNA replication, transcription, repair, and recombination.

Mechanism of Resistance

The mechanism of action of fluoroquinolones, including ciprofloxacin, is different from that of penicillins, cephalosporins, aminoglycosides, macrolides, and tetracyclines; therefore, microorganisms resistant to these classes of drugs may be susceptible to ciprofloxacin. Resistance to fluoroquinolones occurs primarily by either mutations in the DNA gyrases, decreased outer membrane permeability, or drug efflux. In vitro resistance to ciprofloxacin develops slowly by multiple step mutations. Resistance to ciprofloxacin due to spontaneous mutations occurs at a general frequency of between < 10-9 to 1x10-6.

Cross-Resistance

There is no known cross-resistance between ciprofloxacin and other classes of antimicrobials.

Ciprofloxacin has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section of the package insert for Ciproxin (ciprofloxacin hydrochloride) Tablets and Ciproxin (ciprofloxacin*) 5% and 10% Oral Suspension.

Gram-positive bacteria

Enterococcus faecalis (vancomycin-susceptible isolates only)

Staphylococcus aureus (methicillin-susceptible isolates only)

Staphylococcus epidermidis (methicillin-susceptible isolates only)

Staphylococcus saprophyticus

Streptococcus pneumoniae (penicillin-susceptible isolates only)

Streptococcus pyogenes

Gram-negative bacteria

Campylobacter jejuni

Proteus mirabilis

Citrobacter koseri (diversus)

Proteus vulgaris

Citrobacter freundii

Providenciarettgeri

Enterobacter cloacae

Providenciastuartii

Escherichia coli

Pseudomonas aeruginosa

Haemophilus influenzae

Salmonella typhi

Haemophilus parainfluenzae

Serratiamarcescens

Klebsiella pneumoniae

Shigella boydii

Moraxella catarrhalis

Shigella dysenteriae

Morganella morganii

Shigella flexneri

Neisseria gonorrhoeae

Shigella sonnei

 Ciprofloxacin has been shown to be active against Bacillus anthracis both in vitro and by use of serum levels as a surrogate marker (see INDICATIONS AND USAGE andINHALATIONAL ANTHRAX – ADDITIONAL INFORMATION).

The following in vitro data are available, but their clinical significance is unknown. At least 90 percent of the following bacteria exhibit an in vitro minimum inhibitory concentration (MIC) less than or equal to the susceptible breakpoint for ciprofloxacin (≤1 mcg/mL). However, the efficacy of ciprofloxacin in treating clinical infections due to these bacteria has not beenestablished in adequate and well-controlled clinical trials.

Gram-positive bacteria

Staphylococcus haemolyticus (methicillin-susceptible isolates only)

Staphylococcus hominis (methicillin-susceptible isolates only)

Bacillus anthracis

Gram-negative bacteria

Acinetobacterlwoffi

Pasteurellamultocida

Aeromonashydrophila

Salmonella enteritidis

Edwardsiellatarda

Vibrio cholerae

Enterobacteraerogenes

Vibrio parahaemolyticus

Klebsiellaoxytoca

Vibrio vulnificus

Legionella pneumophila

Yersinia enterocolitica

Susceptibility Test Methods

When available, the clinical microbiology laboratory should provide the results of in vitro susceptibility test results for antimicrobial drug products used in resident hospitals to the physician as periodic reports that describe the susceptibility profile of nosocomial and community-acquired pathogens. These reports should aid the physician in selecting an antibacterial drug product for treatment.

Dilution Techniques: Quantitative methods are used to determine antimicrobial minimum inhibitory concentrations (MICs). These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized test method (broth and/or agar).1, 3,4 The MIC values should be interpreted according to criteria provided in Table 1.

Diffusion Techniques: Quantitative methods that require measurement of zone diameters can also provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. The zone size provides an estimate of the susceptibility of bacteria to antimicrobial compounds. The zone size should be determined using a standardized test method.2, 3, 4 This procedure uses paper disks impregnated with 5 mcg ciprofloxacin to test the susceptibility of bacteria to ciprofloxacin. The disc diffusion interpretive criteria are provided in Table 1.

Table 1: Susceptibility Test Interpretive Criteria for Ciprofloxacin

S=Susceptible, I=Intermediate, and R=Resistant.

 

MIC (mcg/mL)

Zone Diameter (mm)

Bacteria

S

I

R

S

I

R

Enterobacteriaceae

≤1

2

≥4

≥21

16-20

≤15

Enterococcus faecalis

≤1

2

≥4

≥21

16–20

≤15

Staphylococcus aureus

≤1

2

≥4

≥21

16–20

≤15

Staphylococcus epidermidis

≤1

2

≥4

≥21

16–20

≤15

Staphylococcus saprophyticus

≤1

2

≥4

≥21

16–20

≤15

Pseudomonas aeruginosa

≤1

2

≥4

≥21

16–20

≤15

Haemophilus influenzae

≤1

   

≥21

   

Haemophilus parainfluenzae

≤1

   

≥21

   

Salmonellatyphi

0.06

0.12–0.5

≥1

≥31

21–30

20

Streptococcus pneumoniae

≤1

2

≥4

≥21

16–20

≤15

Streptococcus pyogenes

≤1

2

≥4

≥21

16–20

≤15

Neisseria gonorrhoeae

≤0.06

0.12–0.5

≥1

≥41

28–40

≤27

Bacillus anthracisa

≤0.25

         

1.

A report of “Susceptible” indicates that the antimicrobial is likely to inhibit growth of the pathogen if the antimicrobial compound reaches the concentrations at the site of infection necessary to inhibit growth of the pathogen. A report of “Intermediate” indicates that the result should be considered equivocal, and, if the microorganism is not fully susceptible to alternative, clinically feasible drugs, the test should be repeated. This category implies possible clinical applicability in body sites where the drug is physiologically concentrated or in situations where high dosage of drug can be used. This category also provides a buffer zone that prevents small uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that the antimicrobial is not likely to inhibit growth of the pathogen if the antimicrobial compound reaches the concentrations usually achievable at the infection site; other therapy should be selected.

Quality Control: Standardized susceptibility test procedures require the use of laboratory controls to monitor the accuracy and precision of supplies and reagents used in the assay, and the techniques of the individuals performing the test.1,2,3,4 Standard ciprofloxacin powder should provide the following range of MIC values noted in Table 2. For the diffusion technique using the ciprofloxacin 5 mcg disk the criteria in Table 2 should be achieved.

Table 2: Acceptable Quality Control Ranges for Ciprofloxacin

Bacteria

MIC range (mcg/mL)

Zone Diameter (mm)

Enterococcus faecalisATCC 29212

0.25–2

-

Escherichia coli ATCC 25922

0.004–0.015

30–40

HaemophilusinfluenzaeATCC 49247

0.004–0.03

34–42

Pseudomonas aeruginosa ATCC 27853

0.25–1

25–33

Staphylococcus aureus ATCC29213

0.12–0.5

-

Staphylococcus aureus ATCC25923

-

22–30

Neisseria gonorrhoeae ATCC 49226

0.001–0.008

48–58

Campylobacter jejuniATCC 33560

0.06–0.25 and 0.03–0.12

-

INDICATIONS AND USAGE

Ciproxin is indicated for the treatment of infections caused by susceptible isolates of the designated microorganisms in the conditions and patient populations listed below. Please seeDOSAGE AND ADMINISTRATION for specific recommendations.

Adult Patients

Urinary Tract Infections caused by Escherichia coli, Klebsiellapneumoniae, Enterobacter cloacae, Serratia marcescens, Proteus mirabilis, Providencia rettgeri, Morganella morganii, Citrobacter koseri (diversus), Citrobacter freundii, Pseudomonas aeruginosa, methicillin-susceptible Staphylococcus epidermidis, Staphylococcus saprophyticus, or vancomycin-susceptibleEnterococcus faecalis.

Acute Uncomplicated Cystitis in Females caused by Escherichia coli or Staphylococcus saprophyticus.

Chronic Bacterial Prostatitis caused by Escherichia coli or Proteus mirabilis.

Lower Respiratory Tract Infections caused by Escherichia coli, Klebsiellapneumoniae, Enterobacter cloacae, Proteus mirabilis, Pseudomonas aeruginosa, Haemophilus influenzae, Haemophilus parainfluenzae, or penicillin-susceptible Streptococcus pneumoniae.* Also, Moraxella catarrhalis for the treatment of acute exacerbations of chronic bronchitis.

*Ciprofloxacin is not a drug of first choice in the treatment of presumed or confirmed pneumonia secondary to Streptococcus pneumoniae.

Acute Sinusitis caused by Haemophilusinfluenzae, penicillin-susceptible Streptococcus pneumoniae, or Moraxella catarrhalis.

Skin and Skin Structure Infections caused by Escherichia coli, Klebsiellapneumoniae, Enterobacter cloacae, Proteus mirabilis, Proteus vulgaris, Providenciastuartii, Morganellamorganii, Citrobacterfreundii, Pseudomonas aeruginosa, methicillin-susceptible Staphylococcus aureus, methicillin-susceptible Staphylococcus epidermidis, or Streptococcus pyogenes.

Bone and Joint Infections caused by Enterobacter cloacae, Serratiamarcescens, or Pseudomonas aeruginosa.

Complicated Intra-Abdominal Infections (used in combination with metronidazole) caused by Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Klebsiellapneumoniae, orBacteroidesfragilis.

Infectious Diarrhea caused by Escherichia coli (enterotoxigenic isolates), Campylobacter jejuni, Shigella boydiiShigella dysenteriae, Shigella flexneri or Shigella sonnei† when antibacterial therapy is indicated.

Although treatment of infections due to this organism in this organ system demonstrated a clinically significant outcome, efficacy was studied in fewer than 10 patients.

Typhoid Fever (Enteric Fever) caused by Salmonella typhi.

NOTE: The efficacy of ciprofloxacin in the eradication of the chronic typhoid carrier state has not been demonstrated.

Uncomplicated Cervical and Urethral Gonorrhea due to Neisseria gonorrhoeae.

Pediatric Patients (1 to 17 years of age)

Complicated Urinary Tract Infections and Pyelonephritis due to Escherichia coli.

NOTE: Although effective in clinical trials, ciprofloxacin is not a drug of first choice i

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Ciproxin 500 Mg 10 Tablets

  • Brand: Bayer
  • Product Code: 8699546692262
  • Availability: In Stock
  • $16.00

Tags: Ciproxin 500 Mg 10 Tablets, Bayer, All Products, Antibiotics