APROCIN

Ciprofloxacin

Description:

Aprocin (Ciprofloxacin) is a synthetic quinolone antibacterial agent having broad-spectrum activity. In vitro studies have shown that the antibacterial action of ciprofloxacin results from the inhibition of bacterial DNA gyrase. This mode of action differs from that of penicillins, cephalosporins, aminoglycosides and tetracyclines and therefore, organisms resistant to these antibiotics are generally sensitive to ciprofloxacin. It is active against most gram-negative aerobic bacteria including Enterobacteriaceae and Pseudomonas aeruginosa. Ciprofloxacin is also active against gram-positive aerobic bacteria including penicillinase producing, non-penicillinase-producing and methicillin resistant staphylococci, although many strains of streptococci are relatively resistant to the drug.

Following oral administration it is rapidly and well absorbed from the GI tract. It is widely distributed into body tissues and fluids. The half-life is about 3.5 to 4.5 hours. About 30 to 50% of an oral dose of Ciprofloxacin is excreted in the urine within 24 hours as unchanged drug and biologically active metabolite.

Composition:

Aprocin: Each film coated tablet contains Ciprofloxacin USP 250 mg as hydrochloride.

Aprocin-500: Each film coated tablet contains Ciprofloxacin USP 500 mg as hydrochloride.

Aprocin Powder for Suspension: After reconstitution each 5 ml suspension contains Ciprofloxacin USP 250 mg as hydrochloride.

Indications:

Aprocin is used in adults for the treatment of urinary tract infections, lower respiratory tract infections and skin structure infections, bone and joint infections, and G.I. infections (enteric fever, infectious diarrhoea) caused by susceptible gram-negative and gram-positive aerobic bacteria. It is also used for the treatment of uncomplicated urethral gonorrhoea caused by penicillinase and non-penicillinase-producing Neisseria gonorrhoea.

Dosage & administration:

In the majority of other infections, 500-750 mg twice daily should be administered.

Duration of treatment: The duration of treatment depends upon the severity of infection, clinical response and bacteriological findings. For acute infections the usual treatment period is 5 to 10 days with Aprocin. Generally treatment should be continued for 3 days after the signs and symptoms of the infection have disappeared.

Cystic fibrosis: In adults with pseudomonal infections of the lower respiratory tract, the normal dose is 750 mg twice daily. As the pharmacokinetics of Ciprofloxacin remain unchanged in patients with cystic fibrosis, the low body weight of these patients would be fallen into consideration when determining dosage.

Impaired renal function: Dosage adjustment are not usually required except in patients with severe renal impairment (serum creatinine>265 micro mol/L or creatinine clearance <20ml/minute). If adjustment is necessary, this may be achieved by reducing the total daily dose by half, although monitoring of drug serum levels provide the most reliable basis for dose adjustment.

Elderly: Although higher Ciprofloxacin serum levels are found in the elderly, no adjustment of dosage is necessary.

Adolescents and children: As with other drugs in its class, Ciprofloxacin has been shown to cause arthropathy in weight bearing joints of immature animals. Although the relevance of this to man is unknown. Its use in children, growing children and growing adolescents is not recommended. However, where the benefit of using ciprofloxacin is considered to outweigh this potential risk, the dosage should be 7.5-15 mg/Kg/day depending upon the severity of infection, administered in two divided doses.

Contraindication:

Ciprofloxacin is contraindicated in patients who have shown hypersensitivity to ciprofloxacin or other quinolones.

Warning and Precaution:

Ciprofloxacin should be used with caution in patients with a history of convulsive disorders. Crystalluria related to the use of Ciprofloxacin has been observed very rarely. Patients receiving Ciprofloxacin should be well hydrated and excessive alkalinity of the urine should be avoided.

Drug Interactions:

Concurrent administration of Ciprofloxacin with theophylline may lead to elevated plasma concentration of theophylline and prolongation of its elimination half-life. This may result in increased risk of theophylline related adverse reactions. If concomitant use can not be avoided plasma levels of theophylline should be monitored and dosage adjustments are made as appropriate.

Antacids containing magnesium, hydroxide or aluminium, hydroxide may interfere with the absorption of Ciprofloxacin resulting in serum and urine levels lower than desired, concurrent administration of these agents with Ciprofloxacin should be avoided. Probenecid interferes with renal tubular secretion of ciprofloxacin and produces an increase in the level of ciprofloxacin in the serum. This should be considered if patients are receiving both drugs concomitantly. As with other broad spectrum antibiotics, prolonged use of ciprofloxacin may result in overgrowth of nonsusceptible organism. Repeated evaluation of the patient’s condition and microbial susceptibility testing are essential. If superinfection occurs during therapy, appropriate measures should be taken.

Other Information:

Patients should be advised that Ciprofloxacin may be taken with or without meals. The preferred time of dosing is two hours after a meal. Patients should also be advised to drink fluid liberally and not take antacid containing magnesium or aluminium concomitantly or within two hours after dosing. Ciprofloxacin may cause dizziness or lightheahedness, therefore patients should know how they react to this drug before they operate an automobile or machinery or engage in activities requiring mental alertness or condition.

Use in Pregnancy and Lactation:

Reproduction studies performed in mice, rats and rabbits using parenteral and oral administration did not reveal any evidence of teratogenicity, impairment of fertility or impairment of peri/post natal development. However as with other quinolones, Ciprofloxacin has been shown to cause arthropathy in immature animals and therefore its use during pregnancy is not recommended. Studies in rats have indicated that ciprofloxacin is secreted in milk; administration to nursing mothers is thus not recommended.

Overdosage:

No information on overdosage is available. Routine measures such as gastric lavage should be performed as soon as possible after ingestion of Aprocin. Serum levels os ciprofloxacin are reduced by dialysis.

Side-effects:

Gastrointestinal disturbances e.g. nausea, diarrhoea, vomiting, dyspepsia, abdominal pain. Disturbance of the central nervous system e.g. dizzines, headache, tiredness, confusion, convulsions. Hypersensitivity reactions e.g. skin rashes, pruritus and possible systemic reactions. The following other reactions have also been reported : joint pain, mild photosensitivity and transient increase in liver enzymes (particularly in patients with previous liver damage), serum bilirubin, urea or creatinine levels.

Packing:

Aprocin: Box containing 5x4's film coated tablets in blister pack.

Aprocin-500: Box containing 2x10's/ 3x10's film coated tablets in blister pack.

Aprocin Powder for Suspension: Each bottle contains dry powder for reconstituting 60 ml suspension.