CIPROFLOXACIN 200 mg / 100 mL SOLUTION FOR INJECTION

Jesse O'Neil

 

For the use of a Registered Medical Practitioner or a Hospital or a Laboratory only.

ALCIPRO

Composition

Each 100 mL contains:

  • Ciprofloxacin — 200 mg

  • Sodium Chloride — 900 mg

  • Water for Injection — q.s.

INDICATION

Ciprofloxacin Solution for Injection is a broad-spectrum antibiotic indicated for the treatment of a wide variety of infections caused by the susceptible strains of gram-positive and gram-negative bacteria, including mixed infections caused by two or more organisms.

Ciprofloxacin Solution for Infusion is indicated for the treatment of the following infections caused by susceptible bacteria:

  • Respiratory tract infections;

  • Bronchopneumonia;

  • Acute exacerbation of chronic bronchitis;

  • Lung infections in patients with cystic fibrosis;

  • Urinary tract infections;

  • Chronic bacterial prostatitis;

  • Skin and skin structure infections;

  • Bacterial gastrointestinal infections.

CLINICAL PHARMACOLOGY

Mechanism of Action

Ciprofloxacin is an antibiotic belonging to the group of fluoroquinolones.

Pharmacokinetics

Absorption

Following an intravenous infusion of ciprofloxacin, the mean maximum serum concentrations were achieved at the end of infusion.

Pharmacokinetics of ciprofloxacin were linear over the dose range up to 400 mg administered intravenously.

Comparison of the pharmacokinetic parameters for a twice-a-day and three-times-a-day intravenous dose regimen indicated no evidence of drug accumulation for ciprofloxacin and its metabolites.

A 60-minute intravenous infusion of 200 mg ciprofloxacin or the oral administration of 250 mg ciprofloxacin, both given every 12 hours, produced an equivalent area under the serum concentration-time curve (AUC).

A 60-minute intravenous infusion of 400 mg ciprofloxacin every 12 hours was bioequivalent to a 500 mg oral dose every 12 hours with regard to AUC.

The 400 mg intravenous dose administered over 60 minutes every 12 hours resulted in a Cmax similar to that observed with a 750 mg oral dose.

A 60-minute infusion of 400 mg ciprofloxacin every 8 hours is equivalent with respect to AUC to 750 mg oral regimen given every 12 hours.

Distribution

Protein binding of ciprofloxacin is low (20–30%).

Ciprofloxacin is present in plasma largely in a non-ionised form and has a large steady-state distribution volume of 2–3 L/kg body weight.

Ciprofloxacin reaches high concentrations in a variety of tissues such as lung (epithelial fluid, alveolar macrophages, biopsy tissue), sinuses, inflamed lesions (cantharides blister fluid), and the urogenital tract (urine, prostate, endometrium), where total concentrations exceeding those of plasma concentrations are reached.

Biotransformation

Low concentrations of four metabolites have been reported, which were identified as:

  • Desethyleneciprofloxacin (M1)

  • Sulphociprofloxacin (M2)

  • Oxociprofloxacin (M3)

  • Formylciprofloxacin (M4)

The metabolites display in-vitro antimicrobial activity but to a lower degree than the parent compound.

Ciprofloxacin is known to be a moderate inhibitor of the CYP450 1A2 iso-enzymes.

Elimination

Ciprofloxacin is largely excreted unchanged both renally and, to a smaller extent, faecally.

Renal clearance is between 180–300 mL/kg/h and the total body clearance is between 480–600 mL/kg/h.

Ciprofloxacin undergoes both glomerular filtration and tubular secretion.

Severely impaired renal function leads to increased half-lives of ciprofloxacin of up to 12 hours.

Non-renal clearance of ciprofloxacin is mainly due to active trans-intestinal secretion and metabolism.

1% of the dose is excreted via the biliary route.

Ciprofloxacin is present in the bile in high concentrations.

DOSAGE AND ADMINISTRATION

The dosage is determined by:

  • The indication;

  • The severity and the site of the infection;

  • The susceptibility to ciprofloxacin of the causative organism(s);

  • The renal function of the patient; and

  • In children and adolescents, the body weight.

The duration of treatment depends on the severity of the illness and on the clinical and bacteriological course.

InfectionDoseFrequencyUsual Duration
Urinary Tract Infection200 mg to 400 mgevery 12 to every 8 hours7–14 days
Lower Respiratory Tract Infection400 mgevery 12 to every 8 hours7–14 days
Nosocomial Pneumonia400 mgevery 8 hours10–14 days
Skin and Skin Structure Infections400 mgevery 12 to every 8 hours7–14 days
Bone and Joint Infection400 mgevery 12 to every 8 hours4 to 8 weeks
Complicated Intra-Abdominal Infection400 mgevery 12 hours7–14 days
Acute Sinusitis400 mgevery 12 hours10 days
Chronic Bacterial Prostatitis
400 mgevery 12 hours
28 days

ADVERSE EFFECT

Hypersensitivity and skin reactions have been associated with ciprofloxacin and other fluoroquinolones.

The most commonly reported adverse reactions are:

  • Nausea;

  • Diarrhea;

  • Vomiting;

  • Transient increase in transaminase;

  • Rash; and

  • Injection site reactions.

PRECAUTION

Ciprofloxacin should be used with caution in patients with epilepsy or a history of CNS disorders.

Ciprofloxacin and related fluoroquinolones have, like nalidixic acid, been shown to cause degenerative changes in the cartilage of young animals.

It has been suggested that these compounds should not be used in children, adolescents, pregnant women or breast-feeding mothers.

Care is necessary in patients with renal function, glucose-6 phosphate dehydrogenate deficiency or myasthenia gravis.

Exposure to strong sunlight or lamps should also be avoided.

The ability to drive or operate machinery may be impaired by ciprofloxacin, especially when alcohol is also taken.

CONTRAINDICATIONS

Ciprofloxacin is contraindicated in patients with hypersensitivity to quinolones, in children below 18 years old, in pregnancy and lactation.

WARNING

The drug may cause hypoglycemia (low blood sugar levels) and mental health related side effects.

Hypoglycemia can lead to coma.

The mental health side effects are more prominent and more consistent across the systemic fluoroquinolone drug class.

The mental health side effects to be added to or updated across all the fluoroquinolones are:

  • Disturbances in attention;

  • Disorientation;

  • Agitation;

  • Nervousness;

  • Memory impairment; and

  • Serious disturbances in mental abilities called delirium.

STORAGE

Store at a temperature not exceeding 30°C.

Avoid freezing and exposure to light.

SHELF LIFE

3 Years

CAUTION

Foods, Drugs, Devices & Cosmetics Act prohibits dispensing without prescription.

PACK SIZE

100 mL of the solution for Injection in LDPE bottle.

Manufactured in Ghana by

Atlantic Lifesciences Limited
Plot No: 16/01, Larkpleku,
Tema-Aflao Road,
Greater Accra, Ghana.

Date of publication: Jan, 2021

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