Cipro 500 mg Tablets

Brand name

The drug is known in the pharmaceutical market under the trade name Cipro. This designation is assigned to it in official registers and is used by doctors, pharmacists and patients to identify the drug in clinical practice and pharmacy networks. The name has become widely recognized due to its use in the treatment of various infectious diseases that require effective antibacterial action. The history of this name goes back to the development of fluoroquinolones, when manufacturers sought to create a memorable and simple designation for one of the key representatives of this group.

International Nonproprietary Name (INN)

The international nonproprietary name of the medicine is ciprofloxacin. It indicates the chemical basis of the active substance, which belongs to the class of fluoroquinolones of the second generation. This term is adopted by the World Health Organization and is used worldwide to standardize the names of medicines, regardless of the brand or region of production. Ciprofloxacin as INN emphasizes its belonging to the group of synthetic antibiotics developed to combat a wide range of bacterial infections, which makes it a universal tool in the arsenal of modern medicine.

Form of release

The drug is available in several forms, which allows you to adapt its use to different clinical situations and patient needs. Among the available options:

• Film-coated tablets with dosages of 250 mg, 500 mg and 750 mg of the active substance. This form is most popular for oral administration due to its ease of use and dosing accuracy.
• Solution for intravenous infusions with a concentration of 2 mg/mL, supplied in ampoules or vials of 50 ml, 100 ml or 200 ml. It is intended for inpatient treatment of severe infections.
• Powder or granules for preparing an oral suspension (available in some countries), with a dosage of 250 mg per 5 mL after dilution. This form is convenient for patients with difficulty swallowing tablets.
• Eye and ear drops with a concentration of 0.3% used for the topical treatment of eye and ear infections.

Each form is tailored to the specific application: tablets are suitable for outpatient treatment, infusions for emergencies, and drops for topical application. The choice of form depends on the severity of the infection, the age of the patient and the availability of the drug in a particular region.

Composition

The main active ingredient is ciprofloxacin, a synthetic antibiotic from the group of fluoroquinolones, which has a powerful bactericidal effect. Auxiliary components differ depending on the form of release. In tablets, the following are used:

• Microcrystalline cellulose - an excipient that provides a stable tablet structure and uniform distribution of the active substance.
• Pregelatinized starch - a binder that contributes to the formation of a compact mass during production.
• Crospovidone - disintegrant, accelerating the disintegration of the tablet in the gastrointestinal tract for rapid release of the active substance.
• Magnesium stearate - a lubricating agent that facilitates the pressing process and prevents sticking to the equipment.
• The film coating consisting of hypromellose, titanium dioxide and polyethylene glycol protects the active substance from external factors and facilitates swallowing.

The infusion solution contains sodium chloride to maintain isotonicity, lactic acid to stabilize pH, and water for injection as a base. The suspension may include sucrose to improve taste, flavorings (e.g., orange), and xanthan gum to create a uniform consistency. The composition is carefully balanced to ensure that each form of the drug is stable and effective.

Pharmacologic Properties

Pharmacodynamics

The drug has a pronounced bactericidal action, which relies on suppressing the activity of two critical bacterial enzymes, DNA gyrase and topoisomerase IV. These enzymes are essential for the processes of DNA replication, transcription and repair in bacterial cells. By blocking their work, the drug disrupts the division and vital activity of microorganisms, which leads to their rapid death. This mechanism is especially effective against actively multiplying bacteria, which makes the drug indispensable in acute infections.

The spectrum of action covers a wide range of pathogens. Among Gram-negative bacteria it is active against Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella spp., Shigella spp. and Neisseria gonorrhoeae. Among Gram-positive microorganisms the drug is effective against Staphylococcus aureus (including some methicillin-sensitive strains) and Streptococcus pneumoniae, although activity against Gram-positive bacteria is somewhat lower than against Gram-negative bacteria. It also exhibits activity against intracellular pathogens such as Chlamydia trachomatis, Mycoplasma hominis, and Legionella pneumophila, expanding its use in the treatment of atypical infections.

The advantage is the low likelihood of rapid development of resistance when used correctly, although prolonged or irrational use may promote the emergence of resistant strains. The effect is rapid, which is particularly important in infections requiring immediate intervention, such as sepsis or complicated urinary tract infections.

Pharmacokinetics

Absorption

After oral administration, the active substance is absorbed predominantly in the small intestine due to its large surface area and optimal pH environment. The maximum concentration in blood plasma is reached 1-2 hours after administration. Bioavailability varies from 70 to 80%, which is due to partial metabolism during the first passage through the liver. The ingestion of food, especially foods high in calcium (milk, yogurt), magnesium or iron, slows absorption due to the formation of chelate complexes, reducing the rate of entry of the substance into the blood, although the total absorption remains virtually unchanged.

Distribution

The component has an excellent ability to penetrate tissues and body fluids. High concentrations are achieved in urine, bile, lungs, kidneys, prostate, bones and soft tissues. Binding to plasma proteins is relatively low - 20-40%, which contributes to the free distribution of the active substance. The drug penetrates the placental barrier and is found in small amounts in breast milk, which is important to consider when prescribing to certain groups of patients. Concentrations in urine are tens of times higher than the minimum inhibitory concentration for most pathogens, which makes it particularly effective in urinary tract infections.

Metabolism

Metabolism is carried out in the liver with the participation of enzymes of the cytochrome P450 system, mainly CYP1A2. Several metabolites are formed, including oxociprofloxacin and sulfociprofloxacin, which have less antibacterial activity than the parent substance. About 20-35% of the administered dose undergoes metabolic transformation, and the remainder remains unchanged, retaining its therapeutic potency.

Excretion

The drug is excreted through the kidneys (50-70% in unchanged form) by tubular filtration and tubule secretion, as well as with bile and feces (15-30%). The elimination half-life in patients with normal renal function is 3-5 hours, but may increase to 8-12 hours in renal failure. High concentration in the urine persists for 24 hours after administration, which provides prolonged effect in infections of the urinary system.

Indications for Use

Medicament is used for the treatment of infectious diseases caused by microorganisms sensitive to it. The main indications include:

• Infections of the urinary tract: acute and chronic cystitis, pyelonephritis, urethritis, prostatitis. The high concentration in the urine makes the drug particularly effective in these cases.
• Infections of the respiratory tract: out-of-hospital pneumonia, exacerbation of chronic bronchitis, infections in cystic fibrosis caused by Pseudomonas aeruginosa.
• Infections of the skin and soft tissues: abscesses, phlegmons, infected wounds, burn infections.
• Infections of bones and joints: osteomyelitis, septic arthritis, especially with gram-negative etiology.
• Gastrointestinal infections: bacterial diarrhea, salmonellosis, shigellosis, typhoid fever.
• Systemic infections: sepsis, bacteremia, endocarditis caused by sensitive strains.
• Infections of the genital tract: gonorrhea, chlamydia.

The drug is also used for prophylaxis of infections in patients with neutropenia, after surgical interventions or in contact with anthrax pathogens. Prescribing requires accurate diagnosis and, ideally, determination of the sensitivity of bacteria to the antibiotic to avoid ineffective treatment and the development of resistance.

Contraindications

The use of the medicine is prohibited in the following cases:

• Individual intolerance to fluoroquinolones or auxiliary components.
• Childhood and adolescence under 18 years of age (except for special indications, such as cystic fibrosis or complicated urinary tract infections), due to the risk of damage to cartilage tissue.
• Pregnancy and breastfeeding period, because the active ingredient may adversely affect the development of the fetus and newborn.
• Epilepsy or a history of seizure syndrome, due to the risk of central nervous system stimulation.
• Tendinitis or tendon rupture associated with past administration of quinolones, because of the potential damaging effect on connective tissue.

The drug is prescribed with caution in atherosclerosis of cerebral vessels, psychiatric disorders, severe renal or hepatic insufficiency, and in patients with prolongation of the QT interval on ECG to avoid complications.

Method of Administration and Dosage

How to take

Tablets are taken orally, drinking enough water (at least 200 ml), preferably 1-2 hours before a meal or 2 hours after to avoid interaction with food containing calcium, magnesium or iron. Infusion solution is administered by intravenous drip over 60 minutes, pre-diluted in physiologic solution or 5% glucose. Eye or ear drops are used topically, following the instructions for the number of drops and frequency of application.

It is important to avoid concomitant administration with an antiplatelet.

It is important to avoid concomitant administration with antacids, sucralfate or iron preparations, as they reduce the absorption of the active substance. Patients are advised to drink more fluids during treatment to prevent crystalluria - formation of crystals in the urine.

Dosages for adults and children

Dosage is determined by the type of infection, its severity, and the patient's condition:

• Adults with uncomplicated infections (e.g., cystitis): 250 mg every 12 hours for 3-7 days.
• Adults with complicated infections (e.g., pyelonephritis, pneumonia): 500-750 mg every 12 hours, course 7-14 days, sometimes up to 21 days for osteomyelitis.
• Children (in exceptional cases such as cystic fibrosis): 10-20 mg/kg body weight every 12 hours, maximum daily dose - 750 mg, under strict medical supervision.
• Intravenous administration: 200-400 mg every 12 hours in severe infections, with possible transition to oral administration after stabilization of the condition.
• Anthrax prophylaxis: 500 mg every 12 hours for 60 days after exposure.

The duration of the course is determined by the doctor, and it is not recommended to interrupt treatment early to avoid relapse or development of bacterial resistance.

Dose adjustment for certain conditions

In renal impairment, dosage is adjusted based on creatinine clearance:

• Clearance 30-50 mL/min: 250-500 mg every 12 hours.
• Clearance 5-29 mL/min: 250-500 mg every 24 hours.
• Patients on hemodialysis: 250-500 mg after dialysis session.

In hepatic insufficiency, correction is usually not required, as the drug is excreted predominantly by the kidneys. However, in case of combined renal and hepatic dysfunction, the dose is reduced individually under medical supervision.

Side Effects

The use of the drug may be accompanied by a number of adverse reactions, which vary in frequency and severity:

• Gastrointestinal disorders: nausea, vomiting, diarrhea, epigastric pain, decreased appetite, sometimes pseudomembranous colitis.
• Nervous system: dizziness, headache, insomnia, anxiety, rarely - convulsions, confusion, hallucinations.
• Musculoskeletal system: arthralgia, myalgia, tendonitis, in rare cases - rupture of tendons, especially in the elderly or in combination with corticosteroids.
• Skin reactions: rash, itching, photosensitivity (hypersensitivity to sunlight), rarely - severe allergic manifestations such as Stevens-Johnson syndrome.
• Cardiovascular: prolongation of the QT interval, tachycardia, especially in patients with predisposition.
• Hematologic: leukopenia, thrombocytopenia, eosinophilia (rare).
• Renal: crystalluria, increase in blood creatinine.

Most side effects are reversible after discontinuation, but if serious symptoms (tendonitis, cramps, allergic reactions) occur, medical attention should be sought immediately.

Overdose

Symptoms of overdose

Exceeding the recommended dose may result in acute toxicity, including nausea, vomiting, severe dizziness, seizures, confusion, oliguria (decreased urine volume), and in severe cases, acute renal failure or heart rhythm disturbances.

First aid measures

If you suspect an overdose, you should:

• Stop taking the drug immediately.
• Rinse the stomach if it has been less than 1-2 hours from the time of ingestion, or induce vomiting.
• Provide copious drinking to stimulate diuresis and prevent crystalluria.
• Seek medical attention to monitor the condition (ECG, blood tests) and provide symptomatic therapy.

Hemodialysis or peritoneal dialysis is ineffective in eliminating the active ingredient, so the focus is on supportive care.

Drug Interactions

Influence on the effects of other drugs

The drug may alter the pharmacokinetics or pharmacodynamics of other drugs:

• Theophylline and caffeine: increase their concentration in the blood due to inhibition of CYP1A2, which increases the risk of toxicity (tachycardia, seizures).
• Barfarin and other anticoagulants: intensification of their effect, increased risk of bleeding.
• Antacids, iron preparations, sucralfate: decreased absorption of the active substance due to chelation, requires an interval of at least 2 hours between doses.
• Non-steroidal anti-inflammatory drugs (except aspirin): increased risk of seizures when coadministered.
• Cyclosporine: increased nephrotoxicity with combined use.

Compatibility with alcohol and food

Alcohol has no direct interaction with the active ingredient, but its consumption during infection increases the burden on the liver and may delay recovery, so it is recommended to abstain. Foods, especially those rich in calcium (dairy products), magnesium or iron, reduce the rate of absorption, so it is better to take it on an empty stomach. Acidic foods (citrus juices) have no significant effect.

Special Precautions

Use in pregnancy and breastfeeding

Use during pregnancy is contraindicated (category C according to FDA), as the active substance penetrates through the placenta and may affect the development of cartilage tissue of the fetus. During lactation, the drug is excreted with breast milk in small amounts, which requires temporary cessation of breastfeeding during treatment to avoid potential effects on the child.

Allergen's effects on the baby

Effects on driving and driving mechanisms

Side effects such as dizziness, tremor, or confusion may make it difficult to drive or operate dangerous machinery. Patients should refrain from such actions until individual reaction to therapy is clarified.

Particularities of use in the elderly and children

In elderly patients more often occur side effects associated with tendons (tendonitis, ruptures) and renal function, so careful monitoring and, if necessary, dose reduction is required. In children, the drug is used only in exceptional cases (e.g. cystic fibrosis or complicated urinary tract infections), as it may damage growing cartilage. Dosage in such cases is strictly calculated according to body weight, and treatment is carried out under the supervision of a specialist.