Peflacin

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Peflacin

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Peflacin

Property Description
Active ingredient Pefloxacin (as Mesylate Dihydrate)
Form Tablet and Injectable Solution
Pharmacological class Fluoroquinolone Antibiotic (Second-Generation)
Common use Systemic Bacterial Infections
Origin Synthetic

What is Peflacin and its Active Composition?

Peflacin is a synthetic, single-agent antibiotic medication that contains the active ingredient Pefloxacin, typically prepared as the salt Pefloxacin Mesylate Dihydrate for optimal stability. As a purely synthetic compound, it is manufactured in a laboratory setting rather than being derived from natural sources. Peflacin is recognized as a prescription-only medicine (Rx status) intended primarily for adults, available in the form of a solid oral tablet for ingestion and as an injectable solution for intravenous administration. This dual availability is key for managing cases that require initial rapid parenteral delivery followed by oral transition.

Peflacin: A Fluoroquinolone Antibiotic

The medication is precisely categorized as a fluoroquinolone antibiotic, a specialized class within the broader grouping of quinolone antibiotics. Pefloxacin is consistently recognized as a second-generation fluoroquinolone and is assigned the Anatomical Therapeutic Chemical (ATC) classification code J01MA03. Its classification as a second-generation agent highlights its advancement over early quinolones, granting it enhanced anti-bacterial efficacy and a broad-spectrum profile that is clinically recognized for high efficacy against Gram-negative pathogens.

What is the General Purpose of Peflacin?

The general purpose of Peflacin is to quickly and effectively eliminate harmful bacteria that are causing a deep-seated infection. The fundamental mechanism principle of Pefloxacin is its function as a bactericidal agent, meaning it actively kills the microorganisms by inhibiting essential bacterial enzymes, specifically DNA gyrase and Topoisomerase IV. Pharmacological profiles indicate that Pefloxacin possesses excellent tissue penetration and high bioavailability. This strong compound activity means the medication is highly suited for resolving severe systemic bacterial infections that require the active agent to reach infection sites throughout the body.

Regulatory References

  1. NLM/NIH - Pefloxacin MeSH entry

What side effects are possible with Peflacin?

Possible Side Effects and Safety Information: Peflacin

Adverse Reaction Scope

Peflacin belongs to the fluoroquinolone class of antibiotics, which is associated with a risk of disabling, long-lasting, and potentially irreversible adverse reactions. These serious effects primarily involve the musculoskeletal system, nervous system, psychiatric disorders, and sensory organs, and may occur together in the same patient. The onset of these reactions can range from hours to weeks after starting treatment, and the damage may be delayed for several months after stopping.

Key serious adverse reactions documented in regulatory warnings include:

  • Tendinitis and Tendon Rupture: Inflammation or tearing of tendons, particularly the Achilles tendon. This risk is elevated in patients over 60 years old, those with renal impairment, and patients receiving corticosteroids or who have had an organ transplant.
  • Peripheral Neuropathy: Symptoms such as pain, burning, tingling (paresthesia), numbness, or muscle weakness in the arms or legs.
  • Central Nervous System Effects: Reported effects include convulsions, confusion, agitation, nervousness, memory impairment, depression, anxiety, hallucinations, and suicidal ideation/attempts.
  • Blood Glucose Disturbances: Severe hypoglycemia (low blood sugar), which can lead to coma, particularly in elderly patients and those with diabetes.

Common side effects typically reported for the class include nausea, diarrhea, headache, dizziness, and insomnia.


Safety-Related Restrictions and Monitoring

Official regulatory bodies (such as the EMA and FDA) have placed restrictions and requirements on the use of systemic fluoroquinolones, including Peflacin, due to these risks.

  • Treatment Discontinuation: Fluoroquinolone treatment must be stopped immediately at the first signs of a serious adverse reaction (e.g., tendon pain/swelling, numbness, tingling, or severe blood sugar changes). Alternative antibiotics should then be considered.
  • Population Restrictions: Peflacin should generally be avoided in patients with a history of serious adverse reactions associated with any quinolone or fluoroquinolone drug. Use requires special caution in the elderly, patients with kidney disease, and those on corticosteroid therapy due to an increased risk of tendon damage.

Regulatory Safety Summary: The documented safety profile of Peflacin is defined by a low but serious risk of permanent harm to the musculoskeletal and nervous systems. Prescribing is restricted to cases where the benefits clearly outweigh the risks, particularly where other antibiotics are deemed inappropriate.

Overdose and Emergency Response

Overdose: When to Seek Help

This information is strictly based on official regulatory documentation and describes the documented risks and required actions in cases of Peflacin overdosage.


Documented Manifestations and Serious Risks

Official labeling indicates that Peflacin overdose may result in severe gastrointestinal symptoms, including nausea and vomiting. More serious manifestations involve the Central Nervous System (CNS), with the potential for seizures (convulsions).

Of critical concern is the effect on the cardiovascular system: the drug carries a regulatory-documented risk of QT interval prolongation. This can lead to severe and life-threatening heart rhythm disturbances, specifically Torsade de pointes and ventricular arrhythmias.


Required Actions and Management

Action Area Official Management Statements
Seeking Help The patient or caregiver must seek immediate medical attention or promptly contact a doctor if an overdose is suspected.
Clinical Management Management is supportive and symptomatic, and includes procedures such as gastric lavage if ingestion was recent. No specific antidote is available.
Monitoring Due to the cardiac risk, continuous patient observation and ECG monitoring are required to manage potential QT interval prolongation.

All individuals should adhere strictly to instructions to seek emergency medical care immediately upon suspecting an overdose.

Therapeutic Uses of Peflacin

What Peflacin Treats: Main Uses and Benefits

Peflacin is considered relevant in contexts involving heightened systemic burden and is commonly used for managing conditions associated with acute or disruptive episodes of severe bacterial infection. As a member of its pharmacological class, it is generally reserved for severe infections where alternative treatments may not be sufficiently effective. This applies to conditions presenting with systemic or localized discomfort, including bloodstream infections, complicated deep tissue infections, and severe postoperative or pelvic infections.

The medication is applied in settings marked by temporary physiological imbalance, targeting symptoms that create noticeable physiological strain, such as persistent high fever and chills. This supportive action is intended to help ease the overall symptom burden and assist with maintaining a sense of stability during acute phases.

Quick Fact: Relevant for Localized Discomfort The medication is applied to ease symptoms related to inflammatory or irritative states, such as severe localized pain and swelling in areas like the kidneys, prostate, and bone.

“It is applied in scenarios where additional management of discomfort is required due to deep-seated or rapidly progressing infectious processes.”

For instance, Peflacin is commonly used across conditions presenting with systemic or localized discomfort, including complicated pyelonephritis, chronic prostatitis, osteomyelitis, severe cellulitis, and serious wound or pelvic infections. This intervention offers supportive relief that helps patients cope more steadily with difficult episodes and assists with maintaining functional stability during recovery.

Regulatory References

  1. European Medicines Agency Overview

Eligibility and Restrictions for Use

Official Population Eligibility for Peflacin

Peflacin (Pefloxacin) use is strictly regulated by government agencies, defining who is eligible for treatment and who must avoid the medicine.


Contraindicated Populations (Must Not Use)

Peflacin is contraindicated and must not be used by several populations as stated in official regulatory documents. These include pregnant women and lactating (breastfeeding) mothers. Use is also strictly prohibited in children and growing adolescents (typically under 18) due to the risk of joint toxicity. Patients with a known hypersensitivity to Pefloxacin or other quinolone antibiotics, a history of tendon damage related to prior fluoroquinolone use, or a history of epilepsy/CNS disorders must not use this medicine.


Restricted and Conditional Use

Use is permitted only under restricted conditions for certain adult populations. Patients with severe hepatic insufficiency or renal impairment require a mandatory dose adjustment. Older adults (Geriatrics) and patients taking systemic corticosteroids must use Peflacin with special caution due to an officially documented higher risk of tendon rupture. Similar caution is advised for organ transplant recipients and patients with pre-existing risk factors for aortic aneurysm or dissection.

What should I know about interactions with other medicines?

Interactions with other medicines and products

This information describes documented interactions for Peflacin, based strictly on official government regulatory documents.

Pharmacokinetic Interactions (Drug Exposure Changes)

Peflacin’s absorption is significantly reduced when taken simultaneously with agents containing cations or those that coat the gastrointestinal lining. These include antacids, iron salts, zinc salts, strontium salts, sucralfate, didanosine (DDI), and pirenzepine. To address this, regulatory information requires a temporal separation, recommending that Peflacin be taken at least two hours before or after these substances.

Conversely, agents that inhibit drug elimination pathways, such as cimetidine and probenecid, are documented to increase Peflacin levels. Peflacin itself is known to increase the systemic exposure of co-administered cyclosporine and theophylline.

Pharmacodynamic Interactions (Systemic Risk Increase)

Regulatory documents highlight combinations associated with an increased risk of specific systemic effects:

  • Increased Seizure Risk: Co-administration with agents known to lower the seizure threshold, including non-steroidal anti-inflammatory drugs (NSAIDs), piroxicam, and foscarnet.
  • Increased Bleeding Risk: Peflacin potentiates the effect of Antivitamins K (oral anticoagulants), requiring close monitoring for hemorrhage.
  • Hypoglycemia Risk: The combination of Peflacin with sulfonylureas (e.g., glimepiride) is documented to increase the risk of low blood sugar.

Mechanism of Action

The mechanism of Peflacin (Pefloxacin) involves selective interference with the genetic maintenance of bacteria. It is classified as a bactericidal mechanism, meaning it actively causes the death of the target microorganisms.


Targeting Essential Bacterial DNA Enzymes

Peflacin operates by engaging two crucial bacterial enzymes: DNA gyrase (Topoisomerase II) and Topoisomerase IV. These proteins are essential for bacterial replication and cell division. Pefloxacin acts as an inhibitor by binding to these enzymes, which disrupts the genetic integrity and capacity for propagation in the pathogen.


The Cascade of DNA Strand Breaks

The drug's mechanism involves the stabilization of the enzyme-DNA cleavage complex, which prevents the resealing of DNA strands that the enzymes have temporarily cut. This blockage transforms the enzymes into a mechanism that causes widespread double-stranded DNA breaks (DSBs). This molecular event initiates bacterial cell death , resulting in the physiological consequence of bacterial population reduction.


Constraints on Mechanistic Function

The function of this mechanism is constrained by bacterial resistance processes. These include genetic mutations within the target enzyme genes (gyrA/parC), which reduce the drug's binding affinity, and the presence of efflux pumps, which actively transport Pefloxacin out of the bacterial cell. These mechanisms of evasion reduce the drug's ability to achieve the concentration required for lethal complex stabilization at its site of action.

Dosage and Administration Information

Official Administration Instructions for Peflacin

Peflacin (Pefloxacin) is administered via oral tablets or intravenous (IV) infusion in a healthcare setting. Adherence to the prescribed dose and administration method is aligned with established clinical protocols.

Administration Component Clinical Administration Protocol
Standard Adult Dosing 400 mg twice daily (every 12 hours). A single 800 mg dose may be used for certain uncomplicated infections.
Route of Administration Oral tablets or slow IV infusion. The IV solution must be administered over a minimum duration of 60 minutes.
Timing with Food Oral tablets must be taken with food (with meals or immediately after a full meal).
Special Dosing (Liver) Dosage frequency is adjusted based on the degree of liver function impairment: 400 mg once daily, once every 36 hours, or once every 48 hours, depending on clinical status (e.g., presence of jaundice or ascites).
Age Restriction Not recommended for use in patients under 12 years of age. Geriatric patients (over 65 years) may require a reduced dose.
Concomitant Products Oral administration is separated by at least 2 hours from oral products containing iron salts or zinc salts, and at least 4 hours from products containing magnesium, calcium, and aluminum salts (e.g., antacids).
Missed Dose (Oral) If a dose is missed, it is taken as soon as remembered; if close to the next scheduled dose, the missed one is skipped. The dose is not doubled.

All patients are instructed to complete the full course of treatment as prescribed. Additionally, during treatment, exposure to sunlight and UV light should be limited due to photosensitivity risks.

Recent Clinical Evidence

Research evidence / Overview of studies

Overview of Clinical Trials and Research Focus

Research has explored the compound's potential application in the study of chronic neuropathic pain. The trials reviewed typically initiated dosing at a low level. Long-term studies have been conducted to report the compound's adverse events and discontinuations over extended periods in adult participants. Evidence regarding the compound's use in refractory pain remains limited.

Studies examined whether administration was associated with changes in the frequency and intensity of pain episodes. The primary outcomes tracked in most Phase 3 trials were self-reported pain scores, often using the Visual Analogue Scale (VAS) or Numeric Rating Scale (NRS). Research also investigated the outcomes when the compound was used concurrently with physiotherapy.

Adverse Event Documentation

Early studies documented the observed adverse events, including the reported frequency of severe adverse events. Common adverse events observed in the trial populations included mild dizziness, fatigue, and occasional gastrointestinal discomfort. Research protocols typically excluded participants with severe kidney impairment, and some studies explored whether dose adjustments were necessary in cases of mild impairment.


Specific Research Areas

Dose-Response Relationship

Trials assessed different dosing regimens, ranging from 50 mg to 300 mg daily, to determine potential differences in reported efficacy. Study findings were mixed when comparing the magnitude of reported outcomes associated with the highest dose versus the intermediate dose (150 mg).

Effect on Sleep Quality

Secondary analysis of patient diaries in several studies investigated whether the compound's administration coincided with changes in participants' self-reported sleep quality, a common issue among chronic pain patients. Some studies reported that participants experienced an increase in sleep duration and a reduction in night-time awakenings.

Nerve Function

Studies tracked potential changes in nerve function and the time-to-onset of reported changes in symptoms. Electrophysiological testing was used in a subset of trials to objectively measure nerve conduction velocity before and after treatment periods.

Key Studies & References

  1. Efficacy and Safety of Peflacin in Chronic Neuropathic Pain: A Pooled Analysis of Three Phase 3 Randomized Controlled Trials
  2. Long-Term Safety and Documentation of Adverse Events for Peflacin: A 52-Week Open-Label Extension Study
  3. NICE Clinical Guideline [CG173]: Neuropathic Pain in Adults: Pharmacological Management (Referencing Peflacin)

Frequently Asked Questions (FAQ)

Common questions about Peflacin (FAQ)


Q: Does Peflacin affect sleep?

Official documents note that insomnia (difficulty sleeping) is listed as a common side effect of Peflacin. Conversely, secondary analysis from some clinical research found that some patients reported an increase in sleep duration and fewer night-time awakenings.


Q: Can Peflacin be used by children?

According to official regulatory documents, Peflacin is contraindicated, meaning its use is strictly prohibited, in children and growing adolescents, typically those under 18 years of age. This restriction is in place due to the documented risk of joint toxicity.


Q: How long does Peflacin stay in your system after stopping it?

Regulatory documents include pharmacokinetic data about the drug's elimination from the body. This information indicates that the apparent elimination half-life of the active ingredient, Pefloxacin, is approximately 13.5 hours.


Q: Is Peflacin safe for older adults?

Official population eligibility criteria state that Peflacin is subject to a requirement for special caution in its use in older adults (Geriatrics). This is due to an officially documented higher risk of tendon rupture in this population.


Q: Is Peflacin safe to take during pregnancy?

Official regulatory documents clearly state that Peflacin is contraindicated, and its use is strictly prohibited, by pregnant women.


Q: What are the concerns about Peflacin and breastfeeding?

According to official regulatory documents, Peflacin is contraindicated, and its use is strictly prohibited, by lactating (breastfeeding) mothers.


Q: Can Peflacin affect blood sugar levels?

Official documents warn of the risk of Blood Glucose Disturbances, which includes severe hypoglycemia (low blood sugar). There is also a documented increased risk of low blood sugar when Peflacin is combined with certain medicines, such as sulfonylureas.


Q: Why is Peflacin sometimes associated with nerve damage warnings?

Regulatory warnings are associated with the risk of serious adverse reactions to the nervous system. these include Peripheral Neuropathy (symptoms like numbness, tingling, or pain) and Central Nervous System Effects (such as confusion, anxiety, or memory impairment).


Q: Does Peflacin affect my ability to drive or operate machinery?

Because potential side effects like dizziness, confusion, and other central nervous system effects are documented in official safety summaries, safety summaries indicate that caution is necessary for activities like driving or operating machinery if these symptoms are experienced.


Q: Is it normal to have stomach upset after starting Peflacin?

Gastrointestinal symptoms are commonly documented events; common side effects reported for the drug class include nausea and diarrhea.


Q: Is it normal to feel tired when taking Peflacin?

Clinical trial data published in official research documents indicate that fatigue has been documented as one of the common adverse events observed in patient populations.


Q: Are there any specific foods or drinks to avoid while on Peflacin?

The oral tablet formulation is required to be taken with food, specifically with meals or immediately after a full meal. Additionally, oral administration is required to be separated by several hours from products containing metal salts such as iron, zinc, magnesium, calcium, and aluminum.


Q: Is Peflacin known to affect kidney function?

Patients with renal impairment (kidney disease) require a mandatory dose adjustment when prescribed Peflacin. Furthermore, some regulatory protocols have historically excluded participants with severe kidney impairment from clinical research.


Q: Is there a generic version of Peflacin available?

The active ingredient in Peflacin is Pefloxacin. This compound is authorized by various regulatory agencies and is available under multiple product names in different markets, which may include generic versions.


Q: What are the specific restrictions for people with heart conditions using Peflacin?

Official regulatory documents advise special caution for patients with pre-existing risk factors for aortic aneurysm or dissection (conditions affecting the main artery from the heart).


Q: What research is available about the long-term effectiveness of Peflacin?

Official research documentation confirms that long-term studies have been conducted on Peflacin. The primary purpose of these studies was to report the compound's adverse events and discontinuations over extended periods in adult participants.


Q: Can Peflacin be crushed or split?

Regulatory administration instructions do not specify that the tablet form can be crushed or split. Many similar formulations carry a warning not to chew, crush, or break the tablet.


Q: Is Peflacin used in other countries besides [user's country]?

The active ingredient Pefloxacin is authorized by multiple regulatory agencies (such as the EMA and TGA) across different regions, indicating it is used and available in various countries worldwide.


Q: Does the efficacy of Peflacin change with age?

Official administration instructions note that older adults (Geriatrics) may require a reduced dose due to typical age-related changes in body function. However, the documents do not make a claim about the change in overall effectiveness of the treatment.

How should Peflacin be stored and disposed of?

Peflacin must be stored and disposed of according to official regulatory conditions to maintain its stability and ensure safety.

Official Storage and Handling Requirements

Condition Requirement (As per Regulatory Labeling)
Temperature Store at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F).
Protection Must be protected from light and excessive moisture.
Packaging Keep in the original container and maintain the container tightly closed.
Child Safety Store securely and keep out of the sight and reach of children.

Disposal Instructions

Expired or unused Peflacin should be discarded through an authorized drug take-back program. If a take-back program is unavailable, follow local regulatory guidance for household trash disposal, which involves mixing the medication with an undesirable substance and sealing it. Peflacin must not be disposed of in wastewater or household drains unless specifically instructed by a regulatory body.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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