Pefloxacin - Dosage, Uses, Warnings and Side Effects

Overview

Pefloxacin is a member of the fluoroquinolone antibiotic family, which is generally used to treat bacterial infections including gonorrhea (a sexually transmitted illness), pneumonia, typhoid fever, and urinary tract infections. It prevents the activation of bacterial enzymes needed for cell division and DNA (Deoxyribonucleic acid) replication. Pefloxacin is a useful treatment choice for several bacterial illnesses because of its broad spectrum of activity against several distinct types of bacteria. Pefloxacin should only be used to treat bacterial infections under the supervision of a healthcare provider due to the possibility of adverse effects.

How Does Pefloxacin Work?

1. The fluoroquinolone antibiotic Pefloxacin prevents the action of DNA gyrase and topoisomerase IV (intravenous) in bacteria. Pefloxacin inhibits the bacteria from growing and ultimately causes their death by reducing the functioning of these enzymes, which are crucial for bacterial DNA replication and cell division.

2. Pefloxacin binds to the DNA gyrase enzyme and inhibits it from unwinding the DNA molecule during replication, leading to breaks in the DNA strands that stop the bacteria from reproducing. Additionally, topoisomerase IV, which is necessary for dividing cells by separating the duplicated DNA strands, is inhibited by Pefloxacin.

3. Pefloxacin kills various bacteria and efficiently treats several bacterial illnesses by going after these crucial bacterial enzymes. It is crucial to remember that Pefloxacin exclusively combats bacterial illnesses; it has no impact on viral infections.

Dose and Dosing

1. Depending on the illness being treated, an adult dosage of Pefloxacin is 400 to 800 mg (milligrams) taken orally every 12 hours for a maximum of 14 days.

2. A lesser dosage of 400 mg taken orally once a day may be adequate for urinary tract infections.

3. The dosage for older individuals may need to be changed. Pefloxacin dosage for individuals with renal impairment should be modified based on their predicted creatinine clearance.

Directions

1. Follow the doctor's prescription for Pefloxacin precisely. Never take a dose that is higher or lower than what is advised or for longer than is advised.

2. With or without food, take Pefloxacin with a full glass of water. Avoid taking it with dairy items or calcium-rich liquids since they might hinder the medication's absorption.

3. It should be completely swallowed with water; do not break, crush, or chew it.

4. Take the missed dosage as soon as remember. If the next dosage is due, omit the missed one and continue with the normal dosing regimen. Take only one dose at a time to make up for missed ones.

5. Even if one begins to feel better, take Pefloxacin until the end of the recommended term. Early treatment termination increases the chance of the infection recurring.

Drug Warnings:

Healthcare providers should be aware of the following cautions while prescribing Pefloxacin, as with other fluoroquinolone antibiotics:

1. Tendinitis and Tendon Rupture: Fluoroquinolones, including Pefloxacin, have been linked to an increased risk of tendinitis and tendon rupture, especially in people over 60 and in those taking corticosteroid medication concurrently. If a patient feels pain, swelling, or inflammation in a tendon, they should be urged to stop taking their prescription immediately and visit a doctor.

2. Peripheral Neuropathy: Fluoroquinolones, such as Pefloxacin, have been linked to a higher risk of peripheral neuropathy, which can happen immediately after treatment and may be permanent. If patients develop symptoms, including pain, burning, tingling, numbness, or weakness in their arms or legs, they should be encouraged to stop taking the drug immediately and seek medical treatment.

3. Effects on the Central Nervous System (CNS): Fluoroquinolones, such as Pefloxacin, have been linked to an increased risk of CNS side effects, such as seizures, hallucinations, and disorientation, particularly in individuals with a history of CNS problems. If patients have these symptoms, they should be urged to stop taking the drug right away and get help from a doctor.

4. Photosensitivity: When taken with Pefloxacin, individuals exposed to UV (ultraviolet rays) or direct sunlight may get severe sunburn or dermatitis. Patients should be urged to wear sunscreen and protective clothing and avoid exposure to UV or sunlight.

5. Pefloxacin QT Prolongation: Pefloxacin has been linked to a higher risk of QT prolongation, which can result in potentially fatal cardiac arrhythmias. Patients using other drugs that lengthen the QT interval may be at higher risk. Patients should be monitored for symptoms of QT prolongation, and medication should be stopped if it occurs.

6. Clostridium Difficile-Associated Diarrhea: Pefloxacin, like other antibiotics, might disturb the natural gut flora and raise the chance of developing Clostridium difficile-associated diarrhea, which can be extremely serious and even fatal. When prescribing Pefloxacin, medical practitioners should consider this risk and only use it when required and suitable.

7. Antibiotic-Resistant Bacteria: It can arise due to overusing Pefloxacin and other fluoroquinolone antibiotics. Pefloxacin and other antibiotics should be used sparingly by medical experts.

For Patients:

What Is a Bacterial Infection?

Harmful bacteria that infiltrate the body and create illness or disease cause bacterial infections. Bacteria are tiny creatures that may proliferate quickly and harm the body's cells and tissues. Strep throat, urinary tract infections, pneumonia, and TB (tuberculosis) are typical cases of bacterial infections. Bacterial illnesses can be passed from person to person through contaminated food or drink or by touching contaminated surfaces.

Depending on the kind and intensity of the infection, bacterial infections can cause various symptoms, such as fever, chills, lethargy, nausea, vomiting, diarrhea, and swelling or redness at the injection site. Antibiotics, which may eradicate or stop the development of germs, may be used to treat bacterial illnesses.

Learn More About Pefloxacin for Bacterial Infections:

What Is Pefloxacin?

1. The antibiotic drug Pefloxacin is a member of the fluoroquinolone class. It combats bacterial infections by preventing bacterial growth and reproduction. Pefloxacin treats several bacterial illnesses, including gastrointestinal infections, skin infections, respiratory infections, and urinary tract infections.

2. Several gram-positive and gram-negative bacteria, such as E. coli, Salmonella, Shigella, Staphylococcus aureus, and Streptococcus pneumoniae, are resistant to Pefloxacin. Tablets or capsules are the most common forms that are consumed orally.

3. Pefloxacin, like other fluoroquinolones, is often used to treat serious or life-threatening infections and illnesses brought on by germs that are resistant to other antibiotics.

Before Starting Pefloxacin

Before starting Pefloxacin, it is crucial to inform the doctor about any health issues and any prescription drugs or dietary supplements.

This comprises:

1. Allergies, particularly to medicines or fluoroquinolone antibiotics.

2. Other health issues include epilepsy, diabetes, myasthenia gravis (Weakness of skeletal muscles), liver or renal illness, or a history of tendon issues.

3. Any medications, including prescription medications, over-the-counter medicines, and herbal supplements.

4. For those who are nursing a baby or are trying to get pregnant.

5. If one has already had mental health issues like depression or anxiety.

6. If one has ever experienced cardiac issues like an erratic heartbeat or QT prolongation.

7. If one has recently undergone any surgical or medical treatments.

8. If one has ever had low potassium levels in the blood.

When and Why to Use Pefloxacin?

1. A number of bacterial infections, including those of the skin, gastrointestinal system, respiratory tract, urinary tract, bones and joints, and skin, can be treated with Pefloxacin.

2. Even if a person starts to feel better before the prescription is done, it is crucial to take Pefloxacin precisely and complete the whole course of therapy. Antibiotic-resistant bacteria can grow due to incomplete antibiotic use, making it more challenging to treat subsequent illnesses.

3. How and when to take medicine will be explained in detail by the doctor.

4. According to the doctor's instructions, Pefloxacin is normally given orally, with or without meals. To assist in avoiding dehydration, it is crucial to consume enough liquids when taking Pefloxacin. Antacids, multivitamins, and other items containing calcium, magnesium, aluminum, or iron should not be consumed within two hours after taking Pefloxacin since they might hinder absorption.

5. Pefloxacin should only be used for the illness for which it was prescribed; it should not be given to others or used to treat other infections unless the doctor specifically instructs to do so.

How Effective Is Pefloxacin?

1. Pefloxacin was successful against a wide range of bacterial strains at the time it was used, but the type of infection and bacterial strain that caused it impacted how effective it was. Additionally, due to overuse and improper use of medicines, certain bacteria are becoming resistant to Pefloxacin and other fluoroquinolone medications.

2. Pefloxacin is not routinely recommended nowadays and should only be given by a healthcare provider following a careful assessment of the patient's condition and the possible risks and benefits of therapy, even if it may still be useful against some bacterial infections.

What Are the Side Effects of Pefloxacin?

Pefloxacin's typical side effects include the following:

1. Nausea and vomiting.

2. Diarrhea.

3. Headache.

4. Dizziness.

5. Insomnia.

6. Itching or rashes.

7. Joint discomfort or swelling.

Pefloxacin can occasionally result in more severe adverse effects, including

1. Tendon rupture or tendinitis.

2. Convulsions or seizures.

3. Irregular rhythms or palpitations in a heartbeat.

4. Symptoms of allergies, such as anaphylaxis.

How to Take Pefloxacin?

The following are some general recommendations for using Pefloxacin:

1. Pefloxacin should always be taken exactly as directed by the doctor. Never take a dose that is higher or lower than what is advised or for longer than is advised.

2. The patient can take Pefloxacin with or without meals. It is advised to take it on an empty stomach to ensure optimal absorption.

3. Along with a full glass of water, swallow the pill whole. Avoid breaking, chewing, or crushing the pill.

Missed Dose: Take the missed dosage as soon as it is recalled. Skip the missed dosage and follow the usual dosing plan if it is almost time for the next dose. To make up for a missed dose, keep the dose the same.

Overdose: Pefloxacin overdoses can result in severe health issues such as seizures, psychosis, and liver damage. Call the local emergency line or go to the closest emergency facility. An overdose may result in tremors, vomiting, stomach discomfort, diarrhea, disorientation, dizziness, seizures, and irregular heartbeats, among other symptoms.

How to Store Pefloxacin?

1. Pefloxacin should be kept at room temperature and out of direct sunlight, heat, and moisture. Keep the medication out of the reach of children and animals and in its original container, with the top securely fastened.

2. Pefloxacin should not be kept in the bathroom or next to the kitchen sink since the humidity and heat might compromise the quality and efficiency of the drug. Additionally, unless specifically advised by the doctor or pharmacist, do not freeze or refrigerate Pefloxacin.

3. Before using a drug, always check the expiration date. Pefloxacin should not be used if it has expired or if the pill seems broken or discolored.

For Doctors

Indications

1. Infections of the Respiratory Tract: Pefloxacin can treat bacterial lung infections such as pneumonia, bronchitis, and sinusitis.

2. Urinary Tract Infections: Pefloxacin can be used to treat urinary tract infections brought on by bacteria that are sensitive to it.

3. Infections of the Skin and Soft Tissues: Pefloxacin can be used to treat infections of the skin and soft tissues, including cellulitis and infected wounds.

4. Gastrointestinal Infections: Pefloxacin can be used to treat infections of the gastrointestinal system, including those brought on by susceptible bacteria like traveler's diarrhea.

5. Sexually Transmitted Infections: Pefloxacin can, in rare circumstances, be used to treat some sexually transmitted diseases, such as gonorrhea.

Pefloxacin should not be used to treat viral infections, such as the common cold or flu; this is an essential distinction.

Dosing

1. Depending on the severity of the illness, the typical adult dose of Pefloxacin is 400 milligrams (mg) taken orally every twelve hours for seven to fourteen days.

2. Depending on the patient's creatinine clearance, the dose of Pefloxacin may need to be changed for those with renal impairment. Pefloxacin is typically administered at 200 mg every twelve hours to individuals with creatinine clearance of thirty to sixty mL/min (milliliter per minute).

3. Pefloxacin dosage must be decreased in individuals with creatinine clearances lower than 30 mL/min to 200 mg per 24 hours.

Dose Considerations

1. Renal Function: Patients with compromised renal function may need dosage changes or a longer treatment interval to avoid toxicity.

2. Age: Due to diminished renal function and poor drug clearance, elderly individuals may need lower dosages of Pefloxacin.

3. Weight: People with low body weight or obesity may require dosage changes.

4. Medication Interactions: Pefloxacin may interact with other drugs, such as antacids and certain antiarrhythmics, necessitating possible dosage modifications.

5. Indication: Depending on the infection's severity and the indication being treated, Pefloxacin's duration and dosage may change.

6. Adverse Effects: Pefloxacin side effects include photosensitivity, QT prolongation, and tendonitis or rupture of the tendon. Patients who suffer these negative effects may need dosage modifications.

Pharmacology

Mechanism of Action

Pefloxacin interferes with the function of the bacterial enzymes DNA gyrase and topoisomerase IV, which are essential for the transcription and replication of bacterial DNA. This interferes with the bacterial enzymes' ability to kill bacteria. The main target of quinolones for gram-negative bacteria seems to be DNA gyrase. In gram-positive species, topoisomerase IV is the preferred target. The strand breaks, supercoiling, and resealing of the bacterial chromosome are caused by interference with these two topoisomerases. DNA replication and transcription are subsequently hindered.

Absorption

Well absorbed when taken orally.

Metabolism

The liver is the site of Pefloxacin's substantial metabolism, where it is predominantly changed into the inactive metabolite N-acetyl Pefloxacin. Then, this metabolite is eliminated through the urine.

The liver enzyme CYP1A2 (cytochrome P1A2) is principally responsible for Pefloxacin's metabolism and converting the medication to its inactive state. Pefloxacin's metabolism can be impacted by a number of variables, including genetic variation and the concurrent use of drugs that stimulate or inhibit CYP1A2 activity.

Route of Elimination

The kidneys are the main organs of Pefloxacin removal from the body. Pefloxacin and its metabolites are eliminated in the urine after being broken down in the liver to their inactive metabolite, N-acetyl Pefloxacin. Pefloxacin is mostly eliminated from the body through the kidneys' glomerular filtration system and active tubular secretion. Approximately 70 to 90 percent of the dosage is removed after 48 hours of ingestion and is excreted unaltered in the urine.

Half-Life

In individuals with normal renal function, the elimination half-life of Pefloxacin is around 8.6 hours.

Toxicities

Clinical Toxicity

1. As previously noted, Pefloxacin can raise the risk of tendinitis and tendon rupture, especially in individuals over 60 and those taking concomitant corticosteroid treatment.

2. Pefloxacin may result in peripheral neuropathy, which may become permanent.

3. Seizures, hallucinations, and disorientation are just a few of the CNS effects that Pefloxacin may have.

4. Pefloxacin's ability to lengthen the QT interval can result in potentially fatal cardiac arrhythmias.

5. Due to its photosensitivity, Pefloxacin can give people exposed to UV or direct sunlight severe sunburn or dermatitis.

Nonclinical Toxicity:

1. Pefloxacin and other fluoroquinolone overused may cause the emergence of microorganisms that are resistant to antibiotics.

2. Pefloxacin and its metabolites can be excreted in urine and pollute wastewater and the environment, which could result in the emergence of bacteria that are resistant to antibiotics.

Contraindications

1. Patients with hypersensitivity to Pefloxacin or other fluoroquinolone antibiotics should not use Pefloxacin.

2. Pefloxacin is not recommended for people with a history of tendinitis or tendon rupture linked to fluoroquinolone usage.

3. Pefloxacin is not recommended during pregnancy or lactation owing to the possibility of damage to the developing fetus or nursing newborn.

4. Pefloxacin is typically not advised for use in children due to the possibility of harm to the musculoskeletal system.

5. Due to the possibility of lowering the seizure threshold, Pefloxacin is not recommended for use in individuals with a history of seizures or other CNS problems.

6. Pefloxacin is not recommended for use by those with a history of myasthenia gravis since it might worsen their symptoms.

Drug Interactions:

1. Drug-Drug Interaction: This Pefloxacin may interact with blood thinners (Aspirin, Warfarin), asthma medications (Theophylline), and anti-diabetic drugs (Chlorpropamide, Glimepiride, Glipizide, Glyburide, Metformin, Tolazamide, and Tolbutamide).

2. Drug-Food Interactions: Avoid dairy items like milk and yogurt while taking Pefloxacin since they may reduce efficacy.

3. Drug-Disease Interactions: Pefloxacin may interact with diabetes, renal, liver, and cardiac issues, as well as tendonitis (tendon inflammation).

Other Specifications

Alcohol

When a person is drunk while taking Pefloxacin for a condition, unpleasant and significant side effects may result. Alcohol should thus be avoided when using Pefloxacin.

Pregnancy

Pefloxacin should not be taken while pregnant unless a doctor has recommended it. Before using this medication, please talk to the doctor. The doctor will only recommend medication if the advantages outweigh the hazards.

Breastfeeding

Pefloxacin is not advised to be used during nursing unless a doctor has prescribed it. Before using this medication, talk to the doctor if nursing.