Ciprofloxacin

FORMULATION
Each film-coated tablet contains:
Ciprofloxacin Hydrochloride USP
equivalent to Ciprofloxacin …. 500 mg

DESCRIPTION
Ciprofloxacin is a synthetic 4-quinolone derivative with bactericidal activity against wide range of Gram- negative and Gram-positive organisms.

MODE OF ADMINISTRATION
To be taken orally.

MECHANISM OF ACTION
Ciprofloxacin is bactericidal and kills bacteria rapidly. It acts via inhibition of bacterial DNA gyrase, ultimately resulting in interference with DNA function. Ciprofloxacin is highly active against a wide range of Gram- positive and Gram-negative organisms and has shown activity against some anaerobes, Chlamydia spp. and Mycoplasma spp. Killing curves demonstrate the rapid bactericidal effect against sensitive organisms and it is often found that minimum bactericidal concentrations are in the range of minimum inhibitory concentrations. Ciprofloxacin has been shown to have no activity against Treponema pallidum and Urea plasma urealyticum. Nocardia asteroids and Enterococcus faecium are resistant.

INDICATIONS
It has been used in the treatment of a wide range of infections including biliary-tract infections, infected bites and stings (animal bites), bone and joint infections, brucellosis, cat scratch disease, chancroid, exacerbations of cystic fibrosis, gastroenteritis (including traveller’s diarrhoea and campylobacter enteritis, cholera, salmonella enteritis, and shigellosis), gonorrhea, infections in immunocompromised patients (neutropenia), legionnaires disease, meningitis (meningococcal meningitis prophylaxis), otitis externa, otitis media, peritonitis, Q fever, lower respiratory-tract infections (including pseudomonas infections in cystic fibrosis, but excluding infections in cystic fibrosis, infections due to Streptococcus pneumoniae such as Pneumococcal Pneumonia), septicaemia, skin infections (including soft-tissue infections) spotted fevers, surgical infection prophylaxis, typhoid and paratyphoid fever, typhus and urinary-tract infections.

DOSAGEANDADMINISTRATION
The usual adult dose of ciprofloxacin ranges from 250 mg – 750 mg twice daily usually depending on the severity and nature of the infection. A dose of 100 mg twice daily by mouth is recommended in women with acute uncomplicated cystitis. Single oral doses of 250 or 500 mg are used for the treatment of gonorrhea, depending upon patterns of resistance. A single oral dose of 500 mg is suggested for meningococcal meningitis prophylaxis. A single oral dose of 750 mg is suggested for surgical infection prophylaxis, given 60 to 90 minutes before the procedure. Ciprofloxacin is not generally recommended for other uses in children and adolescents but, if considered essential, doses of 5 to 15 mg per kg body-weight twice daily by mouth or 4 to 8mg per kg twice daily intravenously have been suggested. Or as prescribed by the physician.

CONTRAINDICATIONS
Ciprofloxacin is contraindicated in patients who have shown hypersensitivity to ciprofloxacin or any of the excipients, or other quinolone anti-infectives. Studies have indicated that ciprofloxacin is secreted in breast milk. Administration to nursing mothers is thus, not recommended.

PRECAUTIONS
In the event of hypersensitivity, which in some instances can occur after the first administration, therapy should be discontinued. Ciprofloxacin should be used with caution in epileptics and patients with a history of CNS disorders and only if the benefits of treatment are considered to outweigh the risk of possible CNS side effects. CNS side effects have been reported after first administration of ciprofloxacin in some patients. Treatment should be discontinued if the side effects, depression or psychoses lead to self-endangering behaviour. Crystalluria related to the use of ciprofloxacin has been reported. Patients receiving ciprofloxacin should be well hydrated and excessive alkalinity of the urine should be avoided.

PHARMACOKINETICS
Ciprofloxacin is rapidly and well absorbed from the gastrointestinal tract. Oral bio availability is approximately 70% and a peak plasma concentration of about 2.5 g per mL is achieved I to 2 hours after a dose of 500 mg by mouth. Absorption may be delayed by the presence of food, but it is not substantially affected overall. The plasma half-life is about 3.5 to 4.5 hours and there is evidence of modest accumulation. Half-life maybe prolonged in severe renal failure (a value of 8 hours has been reported in end stage renal disease) and to some extent in the elderly. There is limited information on the effect of liver dysfunction; in one study the half- life of ciprofloxacin was slightly prolonged in patients with severe cirrhosis of the liver. With one or two exceptions, most studies have shown the pharmacokinetics of ciprofloxacin to be not markedly affected by cystic fibrosis. Plasma protein binding ranges from 20 to 40%. Ciprofloxacin is widely distributed in the body and tissue penetration is generally good. It appears in the CSF, but concentrations are only about 10% of those in plasma when the meninges are not inflamed. Ciprofloxacin is eliminated principally by urinary excretion, but non-renal clearance may account for about a third elimination and includes hepatic metabolism, biliary excretion, and possibly transluminal secretion across the intestinal mucosa. At least 4 active metabolites have been identified. Oxociprofloxacin appears to be the major urinary metabolite and sulphociprofloxacin the primary faecal metabolite. Urinary excretion is by active tubular secretion as well as glomerular filtration and is reduced by probenecid; it is virtually complete within 24 hours. About 40-50% of an oral dose is excreted unchanged in the urine and about 15% as metabolites. Up to 70% of a parenteral dose may be excreted unchanged within 24 hours and 10% as metabolites. Faecal excretion over 5 days has accounted for 20 – 35% of an oral dose and 15% of an intravenous dose.

ADVERSE EFFECTS
Gastrointestinal disturbances include nausea, vomiting, diarrhea, abdominal pain, and dyspepsia and are the most frequent adverse effects. Pseudomembranous colitis has been reported rarely. Headache, dizziness, and restlessness are among the most common effects on the CNS. In addition to rash and pruritis, hypersensitivity type reactions affecting the skin have included, rarely, vasculitis, erythema multiforme. Stevens Johnson syndrome, and toxic epidermal necrolysis. Photosensitivity has occurred, and may be more frequent with some newer fluoroquinolones such as lomefloxacin and sparfloxacin. Anaphylaxis has been reported. As with other quinolone antibacterial reversible arthralgia has sometimes occurred and joint erosions have been documented in immature animals. Tendon damage has been reported. Other adverse effects reported with ciprofloxacin include transient increases in serum creatinine or blood urea nitrogen and, occasionally, acute renal failure secondary to interstitial nephritis; crystalluria; elevated liver enzyme values, jaundice, and hepatitis; haematological disturbances including eosinophilia, leukopenia, thrombocytopenia and very rarely, haemolytic anemia or agranulocytosis; myalgia; gynaecomastia; and cardiovascular effects including tachycardia.

DRUG INTERACTION
Concomitant administration of tizanidine and ciprofloxacin is contraindicated. The hypotensive and sedative effects of tizanidine are potentiated. As with other quinolones, concurrent administration of ciprofloxacin with theophylline may lead to elevated serum concentrations of theophylline and prolongation of its elimination half-life. This may result in increased risk oftheophylline related adverse reactions.

CAUTION
Foods, Drugs, Devices, and Cosmetics Act prohibits dispensing without prescription.

STORAGE CONDITION
Store at temperatures not exceeding 300C.

Keep all medicines out of children’s reach.

Price/SRP:

• SRP 9.00 per tablet

“For suspected adverse drug reaction, report to the FDA: www.fda.gov.ph“.