Ofloxacin

Ofloxacin is an antibiotic of the fluoroquinolones group, which has a broad spectrum of action and penetrates well into the tissues and fluids of the urogenital tract. It is effective against most Enterobacteriaceae, Staphylococcus saprophyticus, methicillin-sensitive strains of S. Aureus, Neisseria gonorrhoeae, Chlamydia trachomatis and Haemophilus ducreyi. Ofloxacin shows intermediate activity against Ureaplasma urealyticum and most enterococci, but limited or no activity against enterococci, Serratia marcescens, Pseudomonas aeruginosa, and many anaerobes. However, high concentrations in urine provide its activity against most pathogens causing urinary tract infections.

Ofloxacin has demonstrated consistent efficacy in a broad spectrum of urinary tract infections, achieving bacteriologic responses greater than 80% in uncomplicated and 70% in complicated infections. Ofloxacin efficacy was similar to that of all tested analogs, including other fluoroquinolones, cephalosporins and cotrimoxazole (trimethoprim/sulfamethoxazole).

Ofloxacin is also effective as a single-dose regimen for the treatment of uncomplicated gonorrhea, as a 7-day regimen for uncomplicated C. Trachomatis infections, and as monotherapy for uncomplicated pelvic inflammatory disease (PID). Again ofloxacin showed similar efficacy to alternative therapies for each type of infection. The availability of intravenous formulation and near complete oral bioavailability allow administration of ofloxacin as a sequential regimen without loss of activity.

The tolerability and drug interaction profile of ofloxacin is consistent with that of other fluoroquinolones. The most commonly reported side effects ofloxacin are associated with gastrointestinal, nervous system, and dermatologic reactions. It is associated with a lower incidence of photosensitivity and tendonitis and a higher incidence of some neurologic events than some other fluoroquinolones. Ofloxacin appears to have a lower propensity to interact with xanthines than other fluoroquinolones (Onrust, Lamb, & Barman Balfour, 2012).

Indications Ofloxacin

1. Urinary tract infections: Ofloxacin may be prescribed to treat cystitis (inflammation of the bladder), urethritis (inflammation of the urethra), and pyelonephritis (inflammation of the kidney cups and pelvis).
2. Respiratory infections: Including bronchitis (inflammation of the bronchi), pneumonia (inflammation of the lungs), and sinusitis (inflammation of the sinuses).
3. Skin and soft tissue infections: Ofloxacin can be used for various bacterial infections of the skin, such as cellulitis (inflammation of subcutaneous tissue), folliculitis (inflammation of hair follicles) and others.
4. Gastrointestinal Infections: Ofloxacin may be used to treat bacterial infections of the stomach and intestines, such as bacterial diarrhea or gastroenteritis.
5. Bone and joint infections: Including osteomyelitis (inflammation of the bone) and joint infections.

Release form

1. Oral tablets: This is the most commonly used form of ofloxacin for the systemic treatment of a wide range of bacterial infections. Tablets usually contain 200 to 400 mg of active ingredient and are intended to be taken once or twice daily.
2. Solution for intravenous administration: Used in hospital settings for treatment of severe or life-threatening infections when oral administration is impossible or ineffective. The solution ensures rapid achievement of therapeutic concentrations of the substance in the blood.
3. Eye drops: Used for the topical treatment of bacterial eye infections such as conjunctivitis or keratitis. The eye drops provide targeted action directly to the area of infection, minimizing systemic side effects.
4. Ear drops: Used to treat bacterial infections of the ear, including otitis media. Like eye drops, they allow the active ingredient to be delivered directly to the site of infection.

Pharmacodynamics

1. Inhibition of DNA gyrase: Ofloxacin binds to the enzyme DNA gyrase, which is required for the positioning and unwinding of DNA during its duplication. This causes ofloxacin to form a complex with the enzyme and inhibits its activity, which prevents DNA synthesis.
2. Bactericidal action: Since DNA synthesis is crucial for bacterial replication and survival, inhibition of DNA gyrase leads to the death of bacterial cells. Ofloxacin has bactericidal action, which means that it kills bacteria, not just inhibits their growth.
3. Broad spectrum of activity: Ofloxacin is active against a wide range of bacteria, including Gram-positive and Gram-negative bacteria. It can be used to treat infections caused by pathogens such as Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzae and others.
4. Mechanism of resistance: Although ofloxacin is an effective antibiotic, some bacteria can develop resistance to it by altering the structure of DNA gyrase or increasing outward release of the drug.

Pharmacokinetics

1. Absorption: Ofloxacin is usually well absorbed after oral administration. Its absorption may be delayed after a meal, but this usually does not affect its bioavailability.
2. Distribution: Ofloxacin is well distributed in tissues and organs of the body, including lungs, kidneys, liver, bladder, prostate and skin. It also penetrates the placental barrier and is excreted in breast milk.
3. Metabolism: Ofloxacin is metabolized in the body to a minor extent.
4. Excretion: Ofloxacin is excreted mainly by the kidneys, where it is partly excreted unchanged and partly as metabolites. A small amount is also excreted in the feces.
5. Half-life: The half-life of ofloxacin is approximately 3-5 hours, which usually ensures that the drug can be taken 1-2 times a day.
6. Effects on intestinal microflora: Ofloxacin may affect the composition of intestinal microflora, which may lead to the development of dysbacteriosis.

Dosing and administration

Here are general recommendations for the use of ofloxacin for adults:

Tablets for oral administration:

• Dosage for mild to moderate infections: 200 mg every 12 hours (twice daily) is usually recommended.
• Dosage in severe infections or infections caused by less sensitive microorganisms: May be increased to 400 mg every 12 hours.

Solution for intravenous injection:

• Dosage: Usually 200 to 400 mg every 12 hours, depending on the type and severity of infection. Intravenous administration is preferred in hospital settings.

Eye drops:

• Dosage in bacterial conjunctivitis and other superficial eye infections: Normally, one drop is injected into the affected eye 2-4 times a day. During the first two days of therapy, the dosage can be increased to every 2 hours during the day.

Ear drops:

• Dosage for ear infections: Drops 5 drops into the affected ear 2-3 times a day.

General Recommendations:

• Tablets should be taken 1 hour before a meal or 2 hours after a meal to maximize absorption.
• It is important to complete a full course of treatment, even if symptoms have disappeared before, to avoid a recurrence of the infection.
• Do not stop taking the drug without consulting your doctor, even if you feel improvement.

Use Ofloxacin during pregnancy

The use of ofloxacin during pregnancy is generally not recommended, especially in the first trimester, as data on its safety for the fetus are limited.

Fluoroquinolones may have adverse effects on cartilage development in the fetus, which may result in joint and tissue damage. Therefore, the use ofloxacin during pregnancy is generally considered inappropriate unless the potential benefits of treatment significantly outweigh the potential risks to the fetus.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to ofloxacin, other fluoroquinolones, or any of the ingredients of the drug should not use it because of the risk of allergic reactions.
2. Epilepsy and other CNS disorders: Ofloxacin may cause central nervous system (CNS) side effects such as increased excitability or seizures, therefore its use may be contraindicated in patients with epilepsy or other CNS disorders.
3. Severe renal impairment: The drug may accumulate in the body in case of renal impairment, therefore its use may be limited in patients with severe renal impairment.
4. Pediatric age: The use of ofloxacin in children and adolescents may be limited as this drug may have adverse effects on developing joints and bone tissues.
5. Pregnancy and breastfeeding: The safety ofloxacin use during pregnancy and breastfeeding has not been established and its use in these cases should be evaluated and recommended by a physician.
6. Diabetes mellitus: Ofloxacin may affect blood glucose levels, so its use may require caution in patients with diabetes mellitus.
7. Patients with a history of vomiting or diarrhea: Special caution may be required in patients with a previous history of vomiting or diarrhea caused by taking ofloxacin or other antibiotics.

Side effects Ofloxacin

1. Gastrointestinal disorders: Including nausea, vomiting, diarrhea, or dyspepsia (digestive disorders). These symptoms may be temporary and may go away after you stop taking the drug.
2. Nervous system disorders: Headache, dizziness, drowsiness, sleepiness, insomnia or more serious symptoms such as anxiety, depression or even hallucinations may occur. Rarely, convulsions may develop.
3. Skin reactions: Allergic reactions such as urticaria, itching, skin rash or angioedema (swelling of the skin, subcutaneous tissue or mucous membranes) may occur.
4. Dry mouth: This is a fairly common side effect that can cause discomfort.
5. Gutdysbiosis: Antibiotic use can change the gut microflora, which can lead to diarrhea or candidiasis (fungal infection of the gut).
6. Increased sensitivity to sunlight: In rare cases, ofloxacin may increase sensitivity to sunlight, which may cause sunburn or other skin reactions with prolonged exposure to sunlight.

Overdose

1. Increased side effects: Overdose ofloxacin may result in increased intensity and frequency of side effects such as headache, dizziness, nausea, vomiting, diarrhea, and drowsiness or insomnia.
2. Increased toxic effects on the central nervous system: In the case of a severe overdose, more serious symptoms such as seizures, anxiety, nervousness, and changes in perception or state of consciousness may occur.
3. Increased cardiotoxicity: Heart rhythm disturbances or other cardiac complications may occur in case of overdose.
4. Potentially dangerous allergic reactions: In case of severe overdose, serious allergic reactions such as anaphylactic shock or anaphylactic reactions may occur.

Interactions with other drugs

1. Drugs containing magnesium, aluminum, iron, or zinc: These metals may decrease the absorption ofloxacin, so drugs containing them (e.g., antacids, vitamins, or iron preparations) should be taken at least 2 hours before or after taking ofloxacin.
2. Anti-acids containing magnesium or aluminum: These may slow the absorption of ofloxacin from the gastrointestinal tract.
3. Drugs thatincrease the pH of the gastric contents: Drugs that increase the pH of the gastric contents (e.g. Proton pumps or antacids) may decrease the absorption of ofloxacin.
4. Drugs depressing the CNS: Ofloxacin may increase the effect of drugs depressing the central nervous system (e.g., some antidepressants or narcotic analgesics), which may lead to an increased risk of undesirable effects.
5. Drugs depressing the cardiovascular system: Co-administration of ofloxacin with drugs depressing the cardiovascular system (e.g. Antiarrhythmic drugs or beta-adrenoblockers) may increase the risk of arrhythmias.
6. Drugs prolonging the QT interval: Ofloxacin may increase the prolongation of the QT interval on electrocardiogram when used concomitantly with other drugs that may also cause this side effect (e.g. Antiarrhythmic drugs or some antidepressants).

Storage conditions

Ofloxacin, like most medications, requires proper storage conditions to maintain its stability and effectiveness. Generally, the storage recommendations for Ofloxacin are as follows:

1. Temperature: Store the drug at room temperature, which is usually 15 to 30 degrees Celsius (59 to 86 degrees Fahrenheit). Avoid overheating the drug as well as freezing.
2. Light: Store Ofloxacin in the original package or dark container to prevent exposure to direct sunlight, which may adversely affect the stability of the drug.
3. Humidity: Ensure dry storage conditions for the drug to avoid exposure to moisture, which may lead to the destruction or degradation of the drug.
4. Children: Keep Ofloxacin out of the reach of children to prevent accidental use.
5. Packaging: Follow the storage instructions given on the product package or in its instructions for use. Some manufacturers may have their own storage recommendations.