ciprofloxacin

Action and Spectrum

Actions and Spectrum: 

ciprofloxacin is a broad-spectrum fluoroquinolone antibiotic that is active against a wide range of gram-negative and gram-positive bacteria. It works by inhibiting the bacterial DNA gyrase and topoisomerase IV enzymes, which are essential for DNA replication and cell division. This leads to bacterial death and clearance of the infection. 

The spectrum of activity of ciprofloxacin includes: 

• Gram-negative bacteria: ciprofloxacin is effective against many gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae, Proteus species, Pseudomonas aeruginosa, Salmonella species, Shigella species, and Haemophilus influenzae. 

• Gram-positive bacteria: ciprofloxacin is active against some gram-positive bacteria, including Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis. 

• Atypical bacteria: ciprofloxacin is also effective against some atypical bacteria, such as Mycoplasma pneumoniae and Chlamydia trachomatis. 

• Anaerobic bacteria: ciprofloxacin has limited activity against anaerobic bacteria. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Nausea  

Abdominal pain  

Diarrhea  

Increased aminotransferase levels  

Vomiting  

Headache  

Increased creatinine  

Rash 

Restlessness  

<1% 

Acidosis 

Allergic reaction 

Angina pectoris 

Anorexia 

Arthralgia 

Ataxia 

Back pain 

Bad taste 

Blurred vision 

Breast pain 

Bronchospasm 

Diplopia 

Dyspnea 

Flushing 

Foot pain 

Hallucinations 

Hiccups 

Hypertension 

Hypotension 

Insomnia 

Irritability 

Joint stiffness 

Lethargy 

Palpitation 

Photosensitivity 

Polyuria 

Syncope 

Tachycardia 

Tinnitus 

Tremor 

Urinary retention 

Vaginitis 

Black Box Warning

fluoroquinolones, including ciprofloxacin, have been associated with some serious adverse reactions, and the FDA has issued warnings regarding their use. These include: 

• Tendinitis and tendon rupture: fluoroquinolones can increase the risk of tendinitis and tendon rupture, particularly in elderly patients and those with renal impairment. The risk is higher for patients who receive concomitant corticosteroid therapy. Patients experiencing any signs of tendinitis or tendon rupture, such as pain, swelling, or inflammation of a tendon, should discontinue the use of fluoroquinolones immediately and seek medical attention. 

• Peripheral neuropathy: fluoroquinolones have been associated with an increased risk of peripheral neuropathy, which can manifest as pain, burning, tingling, numbness, and weakness, predominantly in the sensory or motor nerves of the limbs. The risk of peripheral neuropathy is higher for elderly patients, those with renal impairment, and those receiving concomitant treatment with corticosteroids. 

• Central nervous system (CNS) effects: fluoroquinolones can cause CNS effects such as seizures, anxiety, agitation, confusion, hallucinations, and depression, particularly in patients with a history of CNS disorders. These effects can occur even after a single dose, and patients should discontinue the use of fluoroquinolones and seek medical attention if they experience any of these symptoms. 

Contraindication / Caution

ciprofloxacin is contraindicated in patients with a history of hypersensitivity to ciprofloxacin or any other fluoroquinolone antibiotics. It is also contraindicated in patients who have experienced tendonitis or tendon rupture with fluoroquinolone use, as well as in children and adolescents under 18 years of age (except for the treatment of certain specific infections). 

ciprofloxacin should be used with caution in the following populations: 

• Elderly patients: The risk of tendonitis and tendon rupture, as well as CNS effects, may be increased in elderly patients. 

• Patients with renal impairment: ciprofloxacin is excreted primarily by the kidneys, and its elimination may be impaired in patients with renal impairment. The dose of ciprofloxacin may need to be adjusted in these patients. 

• Patients with hepatic impairment: ciprofloxacin is metabolized in the liver, and its elimination may be impaired in patients with hepatic impairment. The dose of ciprofloxacin may need to be adjusted in these patients. 

• Patients with a history of seizures: ciprofloxacin can lower the seizure threshold and should be used with caution in patients with a history of seizures. 

• Patients receiving concomitant treatment with theophylline: ciprofloxacin can increase serum theophylline levels, which can lead to toxicity. Theophylline levels should be monitored closely in patients receiving concomitant treatment with ciprofloxacin. 

• Patients receiving concomitant treatment with warfarin: ciprofloxacin can increase the anticoagulant effect of warfarin, and INR levels should be monitored closely in patients receiving concomitant treatment with ciprofloxacin. 

• Pregnant and breastfeeding women: ciprofloxacin should be used with caution in pregnant and breastfeeding women, as its safety has not been well established in these populations. 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnant females can take this medication on the advice of a physician. 

Breastfeeding warnings: lactating females should not breastfeed during the treatment. 

Continue breastfeeding after the two half-lives of the last dose. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 

• Category B: There is no affirmation of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women. 

• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a product in humans; Pregnant women must take care of the potential risks. 

• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergency cases for potential benefits. 

• Category X: Drugs listed in this category outweigh risks over benefits. The drug is not for pregnant women. 

• Category N: No data is available for the drug under this category. 

Pharmacology

ciprofloxacin is a broad-spectrum synthetic antibacterial agent of the fluoroquinolone class. It exerts its antibacterial activity by inhibiting bacterial DNA gyrase and topoisomerase IV enzymes, which are responsible for DNA replication, repair, and transcription. This results in inhibition of bacterial DNA synthesis and cell division, leading to bacterial cell death. 

ciprofloxacin has activity against a wide range of gram-negative and gram-positive bacteria, as well as atypical organisms such as Mycoplasma and Chlamydia. It is effective against many organisms that are resistant to other antibiotics, such as penicillins, cephalosporins, and aminoglycosides. 

ciprofloxacin is rapidly and well absorbed after oral administration, with peak plasma concentrations occurring within 1-2 hours. The bioavailability of oral ciprofloxacin is approximately 70%, and it is not significantly affected by food. ciprofloxacin has a large volume of distribution, indicating good tissue penetration, and it is widely distributed throughout the body, including the lungs, kidneys, prostate, and bile. 

ciprofloxacin is extensively metabolized in the liver, and approximately 50% of an oral dose is excreted unchanged in the urine within 24 hours. The elimination half-life of ciprofloxacin is approximately 3-5 hours in patients with normal renal function, but it may be prolonged in patients with renal impairment or hepatic dysfunction. 

ciprofloxacin is available in oral, intravenous, and ophthalmic formulations, and is used to treat a variety of bacterial infections, including urinary tract infections, respiratory tract infections, skin and soft tissue infections, bone and joint infections, gastrointestinal infections, and sexually transmitted infections. 

Pharmacodynamics: 

The pharmacodynamics of ciprofloxacin involve its concentration-dependent bactericidal activity, which means that higher concentrations of the drug result in greater bacterial killing. 

ciprofloxacin exerts its antibacterial effect by inhibiting the activity of bacterial DNA gyrase and topoisomerase IV enzymes, which are essential for bacterial DNA replication, transcription, and repair. By inhibiting these enzymes, ciprofloxacin prevents bacteria from replicating and leads to bacterial cell death. 

The bactericidal activity of ciprofloxacin is concentration-dependent, with a post-antibiotic effect that persists even after the drug concentration has fallen below the minimum inhibitory concentration (MIC) for the target bacteria. This means that higher doses of ciprofloxacin result in longer periods of bacterial suppression and may be particularly important for the treatment of infections caused by bacteria with high MICs. 

Pharmacokinetics: 

Absorption 

Bioavailability due to oral absorption is 50-85% 

Peak plasma concentration is achieved in 0.5-2 hours for immediate-release and 1-2.5 hours for extended-release 

Distribution 

The pharmacodynamics of ciprofloxacin involve its concentration-dependent bactericidal activity, which means that higher concentrations of the drug result in greater bacterial killing. 

ciprofloxacin exerts its antibacterial effect by inhibiting the activity of bacterial DNA gyrase and topoisomerase IV enzymes, essential for bacterial DNA replication, transcription, and repair. Ciprofloxacin prevents bacteria from replicating and leads to cell death by inhibiting these enzymes. 

The bactericidal activity of ciprofloxacin is concentration-dependent, with a post-antibiotic effect that persists even after the drug concentration has fallen below the minimum inhibitory concentration (MIC) for the target bacteria. This means that higher doses of ciprofloxacin result in more extended periods of bacterial suppression and may be significant for treating infections caused by bacteria with high MICs. 

Metabolism 

The drug is metabolized in the liver by enzyme inhibitors, CYP1A2 

Elimination and Excretion 

The half-life of the drug is 2-5 hours (for children) and 3-5 hours (for adults) 

(30-50%) of the drug is excreted in the urine and (15-43%) feces  

Adminstartion

ciprofloxacin can be administered orally, intravenously, or as an ophthalmic solution. The specific administration route and dosage of ciprofloxacin depend on the type and severity of the infection and the patient’s age and renal function. 

Oral Administration: ciprofloxacin tablets should be taken orally with a full glass of water, either with or without food. Drinking plenty of fluids while taking ciprofloxacin is essential to prevent dehydration. The dosage and duration of treatment depend on the type and severity of the infection, but a typical adult dose ranges from 250 to 750 mg every 12 hours. 

Intravenous Administration: ciprofloxacin can be administered as an intravenous infusion over 60 minutes. The treatment dosage and duration depend on the infection’s type and severity and the patient’s renal function. A typical adult dose ranges from 200 to 400 mg every 12 hours. 

Ophthalmic Administration: ciprofloxacin is available as an ophthalmic solution, which can be used to treat bacterial conjunctivitis or corneal ulcers. The solution is typically administered as one or two drops into the affected eye(s) every 2 to 4 hours for up to 7 days. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ciprofloxacin 

Pronounced: Cip-roh-floks-a-cin 

Why do we use ciprofloxacin? 

Some of the conditions that ciprofloxacin is commonly used to treat include: 

• Urinary tract infections (UTIs): ciprofloxacin is often prescribed to treat bladder and urinary tract bacterial infections. 

• Respiratory infections: ciprofloxacin can be used to treat bacterial infections of the lungs, including pneumonia and bronchitis. 

• Skin and soft tissue infections: ciprofloxacin can be used to treat bacterial skin infections such as cellulitis, as well as infections of the soft tissue. 

• Bone and joint infections: ciprofloxacin can be used to treat bacterial infections of the bones and joints, such as osteomyelitis.