Pefloxacin

Pefloxacin is an antibiotic from the fluoroquinolones group that is used to treat a wide range of bacterial infections. Like other fluoroquinolones, pefloxacin works by inhibiting DNA gyrase and topoisomerase IV, enzymes necessary for DNA replication, transcription, repair, and recombination in bacteria. As a result of inhibition of these enzymes, the process of DNA division is impaired, leading to the death of bacterial cells.

Pefloxacin is effective against a variety of Gram-positive and Gram-negative bacteria and can be used to treat the following conditions:

• Urinary tract infections (UTIs), including cystitis and pyelonephritis.
• Respiratory infections such as chronic bronchitis and pneumonia.
• Skin and soft tissue infections.
• Abdominal infections.

However, as with any antibiotics, there is a risk of bacterial resistance to pefloxacin, so its use should be based on the sensitivity of the pathogen and the recommendations of the doctor. It is important to take pefloxacin strictly according to the doctor's prescription, without interrupting the course of treatment and without changing the dosage without consulting a specialist.

The use of pefloxacin, like other fluoroquinolones, may be accompanied by certain side effects, including gastrointestinal disturbances, headache, dizziness, allergic reactions, and rarely - effect on tendons. Therefore, before starting treatment with pefloxacin, you should read the instructions for use and discuss possible risks and side effects with your doctor.

Indications Pefloxacin

1. Urinary tract infections: Inflammatory processes in the urinary system such as cystitis, urethritis, pyelonephritis and prostatitis caused by bacterial infection.
2. Respiratory infections: Including bronchitis, pneumonia and other respiratory tract infections caused by bacterial flora.
3. Skin and soft tissue infections: For example, boils, abscesses, pyoderma and other skin infections caused by bacterial infection.
4. Gastrointestinal Infections: Such as acute gastroenteritis, diverticulitis, salmonellosis and other bacterial infections of the gastrointestinal tract.
5. Bone and joint infections: Osteomyelitis, arthritis and other bacterial infections of bones and joints.
6. Prevention of infections in immunocompromised patients: Immunocompromised patients, e.g. After organ transplantation or in the presence of immunodeficiency conditions, to prevent the development of bacterial infections.

Release form

1. Oral tablets: This is the most common form of pefloxacin for the systemic treatment of infections. Tablets offer convenience of administration and are suitable for outpatient treatment. They are usually available in a variety of dosages, allowing the course of treatment to be tailored to the specific needs of the patient.
2. Solution for intravenous administration: It is used in hospital conditions for treatment of severe or complicated infections, when it is necessary to quickly achieve therapeutic concentration of antibiotic in the blood. Intravenous administration of pefloxacin provides direct delivery of the active substance to the site of infection.
3. Eye drops: In some cases, pefloxacin may be available in the form of eye drops for topical treatment of anterior eye infections such as bacterial conjunctivitis.

Pharmacodynamics

1. DNA gyrase inhibition: Pefloxacin acts by inhibiting the enzyme DNA gyrase, which is responsible for DNA unraveling during replication. This leads to disruption of DNA synthesis and stops bacterial growth and reproduction.
2. Inhibition of topoisomerase IV: In addition to inhibiting DNA gyrase, pefloxacin also inhibits the enzyme topoisomerase IV, which is involved in DNA separation and repair. This further contributes to the DNA breakdown of the bacterial cell.
3. Bactericidal effect: Pefloxacin has a bactericidal effect, which means that it kills bacteria, not just inhibits their growth. This is especially important in the treatment of severe infections, when complete elimination of pathogens is necessary.
4. Broad spectrum of activity: Pefloxacin is active against a variety of Gram-positive and Gram-negative bacteria, including pathogens such as staphylococci, streptococci, pneumococci, escherichia, Escherichia coli, salmonella, gonococci, and others.

Pefloxacin is a broad-spectrum antibiotic from the fluoroquinolone class that is active against a variety of bacterial pathogens. Here are some of the most common bacteria that pefloxacin is active against:

1. Gram-positive bacteria:

   • Staphylococcus aureus (including methicillin-resistant MRSA strains)
   • Streptococcus pneumoniae
   • Streptococcus pyogenes
   • Enterococcus faecalis

2. Gram-negative bacteria:

   • Escherichia coli
   • Klebsiella pneumoniae
   • Proteus mirabilis
   • Haemophilus influenzae
   • Pseudomonas aeruginosa
   • Neisseria gonorrhoeae
   • Moraxella catarrhalis

3. Atypical bacteria:

   • Mycoplasma pneumoniae
   • Legionella pneumophila
   • Chlamydia pneumoniae

4. Others:

   • Enterobacter spp.
   • Serratia spp.
   • Acinetobacter spp.

1. High concentration in tissues: After taking pefloxacin, a high concentration in the body tissues is achieved, which ensures effective penetration of the antibiotic into the focus of infection.
2. No effect on cytochrome P450: Pefloxacin has no clinically significant effects on the cytochrome P450 system, making it less likely to cause interactions with other drugs.

Pharmacokinetics

1. Absorption: After oral administration of pefloxacin, it is well absorbed from the gastrointestinal tract, and reaches maximum blood concentrations in about 1-2 hours.
2. Distribution: After absorption, pefloxacin is rapidly distributed to the tissues and organs of the body, including lungs, kidneys, skin, soft tissues and other organs. It also penetrates the mucous membranes, which allows it to be effective in treating infections.
3. Metabolism: Pefloxacin is largely metabolized in the liver. The main metabolite is desethylpefloxacin.
4. Excretion: Mainly pefloxacin is excreted with urine as unchanged drug and metabolites. Excretion may be delayed in patients with impaired renal function.
5. Semi-disposition: The elimination half-life of pefloxacin from the body is about 8 hours, which allows it to be taken usually 2 times a day.
6. Nutritional effects: Food may slow down the rate and completeness of absorption of pefloxacin from the gastrointestinal tract, but usually this does not affect its clinical efficacy.

Dosing and administration

The following are general recommendations for the use of pefloxacin, but it is important to follow your doctor's instructions and the directions for use that come with the drug.

Oral tablets:

• For adults: The usual starting dose is 400 mg twice daily. The dosage may be adjusted depending on the severity of the infection and the body's response to treatment. The course of treatment usually lasts from 7 to 14 days, but may be extended depending on clinical response.
• Tablets should be taken whole, drinking enough water. It is best to take the medicine 1-2 hours before or after a meal, as food can affect the absorption of the antibiotic.

Solution for intravenous injection:

• For adults: The dosage and duration of intravenous administration will be determined by a physician based on the severity of the infection and the patient's condition. Intravenous administration is usually started at the same dose as for oral administration and may be adjusted as needed.

Eye drops:

• Dosage and method of administration of eye drops: will vary depending on the specific product and should follow the manufacturer's instructions or ophthalmologist's recommendations.

Important Notes:

• During treatment with pefloxacin, you should drink enough fluids.
• Prolonged sun exposure or use of a tanning bed should be avoided during treatment with pefloxacin because of the increased risk of photosensitivity.
• At the first sign of an allergic reaction, severe irritation, or in case of side effects such as tendon pain, you should immediately stop taking pefloxacin and contact your doctor.

Use Pefloxacin during pregnancy

During pregnancy, pefloxacin is generally not recommended because of the potential risk to fetal development. Fluoroquinolones, including pefloxacin, may cross the placenta and have toxic effects on the fetus, especially in early pregnancy. Use of fluoroquinolones during pregnancy may be associated with a risk of joint and cartilage disorders in the child.

Contraindications

1. Hypersensitivity to pefloxacin or other quinolone antibiotics: Patients with known allergy or hypersensitivity to pefloxacin or other quinolone antibiotics should not use the drug.
2. Pediatric age: The use of pefloxacin in children and adolescents may be limited as the efficacy and safety of this drug in this age group may not be adequately studied.
3. Pregnancy and lactation: Pefloxacin may have adverse effects on fetal development, therefore its use is not recommended in pregnancy and during lactation unless the benefits outweigh the potential risks to the fetus or child.
4. Problems with the daily rhythm of the heart (QT-interval): Patients with heart rhythm abnormalities such as QT interval prolongation or arrhythmias should avoid using pefloxacin because it may worsen these abnormalities.
5. Problems with the daily rhythm of the heart (QT-interval): Patients with heart rhythm abnormalities such as QT interval prolongation or arrhythmias should avoid using pefloxacin because it may worsen these abnormalities.
6. Tendinitis and risk of tendon rupture: The use of pefloxacin may increase the risk of tendinitis (tendon inflammation) and tendon rupture, especially in elderly patients and those already predisposed to these conditions.
7. Epilepsy and central nervous system disorders: The drug should be used with caution in patients with epilepsy and other central nervous system disorders, as it may increase the risk of seizures.

Side effects Pefloxacin

1. Gastrointestinal Disorders: Including diarrhea, nausea, vomiting, abdominal pain, dyspepsia (digestive disorders), appetite disorders and dysbacteriosis.
2. Nervous system: Dizziness, headache, drowsiness, insomnia, anxiety, nervousness, mental disorders (including depression and anxiety), peripheral neuropathy (similar to numbness and tingling), increased symptoms of neuralgia, and rare cases of convulsions and psychosis.
3. Cardiovascular system: Increase or decrease in blood pressure, changes in heart rate, arrhythmias including tachycardia and atrial fibrillation.
4. Hematopoietic system: Anemia, leukocytosis, leukopenia, thrombocytopenia.
5. Skin reactions: Dyspnea, skin rash, pruritus, urticaria, allergic reactions, photodermatitis, photosensitization, and rare cases of toxic epidermal necrolysis (severe skin complication).
6. Senses: Deterioration of hearing, including tinnitus (ringing in the ears), changes in taste, redness of the eyes and irritation of the conjunctiva.
7. Musculo-articular symptoms: Muscle pain, arthralgias (joint pain), tendonitis (inflammation of tendons).
8. Other side effects: It is possible to develop infections caused by resistant microorganisms, as well as influence on liver and kidney function.

Overdose

1. Symptomatic treatment: Since there is no specific antidote for pefloxacin overdose, treatment will focus on symptomatic relief of overdose symptoms. Your doctor may prescribe symptom relievers such as analgesics or antihistamines.
2. Gastric cleansing: In case of fresh oral administration of pefloxacin, gastric lavage may be performed to remove unabsorbed drug.
3. Maintenanceof organ and system functions: In severe overdose, measures may be required to maintain the functions of important organs and systems such as cardiovascular, respiratory and renal.
4. Medical Surveillance: Patients who have overdosed on pefloxacin may require close medical monitoring to assess the condition and detect possible complications in a timely manner.

Interactions with other drugs

1. Preparations containing aluminum, iron, zinc, magnesium: These metals may reduce the absorption of pefloxacin. Therefore, the administration of the antibiotic should be separated by time from the administration of drugs containing these metals.
2. Antacids: The use of antacids concomitantly with pefloxacin may reduce its bioavailability, so they should also be taken at intervals from the antibiotic.
3. Drugs that reduce the acidity of gastric juice (e.g. Proton pump inhibitors): They may reduce the absorption of pefloxacin, therefore it is also recommended to separate their administration in time.
4. Drugs that increase the risk of heart rhythm disturbances (QT-interval): Pefloxacin may increase the risk of heart rhythm abnormalities when used concomitantly with other drugs that also affect the QT-interval (e.g., antifungal agents, some antiarrhythmic drugs).
5. Drugs causing phototoxicity: Pefloxacin may increase the risk of phototoxic reactions when used concomitantly with certain drugs (e.g. Tetracyclines, sulfonamides).
6. Drugs causing neurotoxicity: Concomitant use of pefloxacin with drugs that increase neurotoxicity (e.g. Some antiepileptic drugs) may increase the risk of neurological side effects.
7. Blood glucose-lowering drugs: Pefloxacin may increase the hypoglycemic effect of blood glucose-lowering drugs.