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Pefloxacin mesylate dihydrate is a chemical compound primarily used in the medical field as an antibacterial agent. It belongs to the fluoroquinolone class of antibiotics, which are known for their broad-spectrum activity against both Gram-positive and Gram-negative bacteria. This specific form, the dihydrate, contains two molecules of water of crystallization per molecule of pefloxacin mesylate.
Pefloxacin, the active ingredient, works by inhibiting the bacterial DNA gyrase enzyme, an essential process for bacterial replication. By disrupting this mechanism, pefloxacin effectively halts the growth and multiplication of susceptible bacteria, thereby allowing the immune system to combat the infection or enabling the body to clear the bacteria on its own.
The mesylate salt form of pefloxacin enhances its solubility and stability, making it more suitable for pharmaceutical formulations. As an antibacterial, it is indicated for the treatment of various bacterial infections, including respiratory, urinary tract, skin, and soft tissue infections.
However, like other fluoroquinolones, it should be used with caution due to potential side effects such as gastrointestinal disturbances, headaches, and, in rare cases, more severe adverse reactions like tendonitis and tendon rupture. It's crucial to follow medical advice closely and complete the prescribed course of treatment to avoid the emergence of resistant bacterial strains.
In summary, pefloxacin mesylate dihydrate is a potent antibiotic used to treat a wide range of bacterial infections. Its efficacy and safety profile make it a valuable addition to the arsenal of antimicrobial therapies, albeit with the need for vigilant monitoring of potential side effects.
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Chemical Formula |
C17H20FN3O3 |
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Exact Mass |
333.15 |
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Molecular Weight |
333.36 |
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m/z |
333.15 (100.0%), 334.15 (18.4%), 335.16 (1.6%), 334.15 (1.1%) |
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Elemental Analysis |
C, 61.25; H, 6.05; F, 5.70; N, 12.61; O, 14.40 |
Antibacterial Agent
Mechanism of Action
- Belonging to the fluoroquinolone class of antibiotics.
- It acts by inhibiting DNA gyrase, an enzyme essential for bacterial DNA replication and transcription. By disrupting the function of DNA gyrase, pefloxacin prevents bacterial DNA from being properly replicated and transcribed, leading to bacterial cell death.
Spectrum of Activity
- Pefloxacin demonstrates broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria.
- It is particularly active against organisms such as Staphylococcus aureus, Escherichia coli, other Enterobacteriaceae, and Pseudomonas aeruginosa.
Therapeutic Uses
- Due to its potent antibacterial activity, it is commonly used to treat severe and life-threatening bacterial infections.
- It may be prescribed for infections of the respiratory tract, urinary tract, skin and soft tissues, and other body systems.
Scientific Research & Pharmaceutical Development
Pharmaceutical Intermediates
- Serving as an important intermediate in the synthesis of other pharmaceutical compounds.
- Its unique chemical structure and properties make it a valuable starting material for the development of new antibacterial agents.
Scientific Research
- Researchers utilize it in various scientific studies to investigate its antibacterial mechanisms, spectrum of activity, and potential for the development of new therapeutic strategies.
- It has been featured in scientific literature, contributing to the advancement of knowledge in the field of infectious diseases and antibacterial therapy.
Introduction to Fluoroquinolones Antibiotics
Fluoroquinolones, a class of synthetic antibacterial agents, have revolutionized the field of antimicrobial therapy since their discovery. Here is a detailed account of the discovery history of fluoroquinolones:
- In 1962, the first quinolone drug, nalidixic acid, was introduced into clinical practice. It was discovered as a byproduct during an attempt to synthesize chloroquine by George Y. Lesher at Sterling Winthrop Research Institute in the United States. Nalidixic acid, though primarily used for urinary tract infections due to its high urinary excretion, has been largely phased out due to its low bioavailability.
- Building upon nalidixic acid, the development of fluoroquinolones began. The introduction of fluorine atoms significantly enhanced the antibacterial activity of these compounds.
- In 1974, pipemidic acid, a second-generation quinolone, was synthesized. It exhibited a broader spectrum of antibacterial activity and fewer adverse reactions compared to nalidixic acid.
- The first fluoroquinolone, norfloxacin, was synthesized in 1978. This marked the beginning of the fluoroquinolone era, with subsequent development of numerous fluoroquinolone derivatives.
The third-generation fluoroquinolones, including ciprofloxacin and levofloxacin, emerged in the 1980s and 1990s.
- Ciprofloxacin: Discovered in 1981 and patented by Bayer, ciprofloxacin became available in 1987. It demonstrated strong activity against a wide range of bacteria, making it a mainstay in the treatment of bacterial infections.
- Levofloxacin: Developed jointly by Hoechst (now Sanofi) and Daiichi Sankyo, levofloxacin was introduced in 1985 in Germany and 1993 in Japan. It is a more potent and less reactive form of ofloxacin, with a broader spectrum of antibacterial activity.
The fourth-generation fluoroquinolones, such as moxifloxacin and gatifloxacin, were introduced in the late 1990s and early 2000s.
- Moxifloxacin: Approved for use in various countries, moxifloxacin offers broad-spectrum coverage and good tissue penetration.
- Gatifloxacin: Unfortunately, gatifloxacin was withdrawn from the US and Canadian markets in 2006 due to reports of serious or fatal hypoglycemia or hyperglycemia.
- Despite the success of fluoroquinolones, concerns about adverse effects, such as QT interval prolongation and blood glucose disturbances, led to the exploration of non-fluoroquinolone quinolones.
- In the late 1990s, Toyama Chemical Company synthesized a series of 6-H quinolones, challenging the conventional wisdom that fluoroquinolones must contain a 6-fluoro group. Compounds like garenoxacin emerged from this research.
- Another notable non-fluoroquinolone is nemonoxacin, developed by Procter & Gamble and later licensed to TaiGen Biotechnology. Nemonoxacin has shown activity against methicillin-resistant Staphylococcus aureus (MRSA), a significant multidrug-resistant pathogen.
adverse reaction
Pefloxacin Mesylate Dihydrate is a third-generation fluoroquinolone antibacterial drug that exerts broad-spectrum antibacterial effects by inhibiting the activity of bacterial DNA gyrase and topoisomerase IV, blocking bacterial DNA replication. Its antibacterial spectrum covers Gram negative bacteria (such as Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa), Gram positive bacteria (such as Staphylococcus aureus), and some anaerobic bacteria. It is commonly used clinically to treat respiratory infections, urinary system infections, abdominal infections, skin and soft tissue infections, and sepsis.
Common types of adverse reactions and clinical manifestations
Gastrointestinal reactions
Gastrointestinal reactions are the most common adverse reactions of Pefloxacin Mesylate Dihydrate, with an incidence rate of approximately 5% -15%. Clinical manifestations include:
Nausea and vomiting: commonly seen in the early stages of medication, may be related to the direct stimulation of the gastrointestinal mucosa by the drug. A retrospective study involving 200 patients showed that the incidence of nausea was 8.5% and vomiting was 4.2%.
Diarrhea: Some patients may experience watery or watery stools, and in severe cases, it may develop into pseudomembranous colitis (with an incidence rate of about 0.1% -0.5%), characterized by severe abdominal pain, bloody stools, and fever, requiring urgent treatment.
Digestive disorders: including upper abdominal discomfort, bloating, and decreased appetite, which may be related to medication affecting gastrointestinal motility or dysbiosis.
Mechanism of occurrence: Fluoroquinolone drugs may inhibit the growth of beneficial gut microbiota (such as Bifidobacterium and Lactobacillus), leading to the overgrowth of pathogenic bacteria (such as Clostridium difficile) and causing intestinal inflammation.
Central nervous system response
Central nervous system reactions are another common adverse reaction of Pefloxacin Mesylate Dihydrate, with an incidence rate of approximately 3% -8%, mainly including:
Headache and dizziness: mostly mild, can relieve on their own, may be related to the vasodilation effect of drugs on blood vessels or the increase in cerebrospinal fluid concentration.
Insomnia and drowsiness: Some patients may experience sleep disorders, manifested as difficulty falling asleep or daytime sleepiness.
Mental abnormalities: including anxiety, restlessness, confusion, hallucinations, and tremors, and in severe cases, seizures may occur (with an incidence rate of about 0.1% -0.5%). A cohort study on elderly patients showed that the risk of epileptic seizures is closely related to renal dysfunction and excessive drug dosage.
Mechanism of occurrence: Fluoroquinolone drugs can pass through the blood-brain barrier, inhibit the neural transmission of gamma aminobutyric acid (GABA), and thus lower the threshold for epilepsy. In addition, drug metabolites may have direct toxicity to the central nervous system.
Allergic reactions
Allergic reactions are one of the serious adverse reactions of Pefloxacin Mesylate Dihydrate, with an incidence rate of approximately 1% -5% and diverse clinical manifestations
Skin reaction: The most common is rash (with an incidence rate of about 2% -3%), manifested as erythema, papules, or urticaria, often occurring 1-3 days after medication. Severe cases may develop exudative erythema multiforme, Stevens Johnson syndrome (SJS), or toxic epidermal necrolysis (TEN), characterized by extensive skin peeling and mucosal damage, with a mortality rate of up to 10% -30%.
Vascular neuroedema: manifested as facial, lip or throat edema, and in severe cases can lead to airway obstruction, requiring urgent treatment.
Photogenic reaction: Some patients may experience skin redness, swelling, blisters, or burning pain after exposure to sunlight, with an incidence rate of about 0.5% -1%. This is related to the production of phototoxic metabolites after the drug absorbs ultraviolet radiation.
Mechanism of occurrence: Allergic reactions are mainly caused by IgE mediated type I hypersensitivity reactions or T cell-mediated type IV hypersensitivity reactions. The photosensitive reaction is related to the generation of free radicals by drugs after absorbing ultraviolet light, which damages skin cells.
Skeletal muscle system response
The skeletal muscle system response is a specific adverse reaction of Pefloxacin Mesylate Dihydrate, with particular attention paid to its damage to cartilage in juvenile animals
Joint pain: Some patients may experience knee, ankle, or wrist pain, with an incidence rate of about 1% -2%. It is mostly transient and can be relieved after discontinuation of medication.
Tendinitis and tendon rupture: most commonly seen in the Achilles tendon, characterized by pain, swelling, or restricted movement. In severe cases, tendon rupture may occur (with an incidence rate of approximately 0.01% -0.1%). A meta-analysis showed that users of fluoroquinolone drugs have a 2.5 times higher risk of Achilles tendon rupture compared to non users.
Rhabdomyolysis: manifested as muscle pain, muscle weakness, and elevated serum creatine kinase (CK), and in severe cases can lead to acute renal failure (incidence rate of about 0.01%).
Mechanism of occurrence: Fluoroquinolone drugs may interfere with cartilage repair by inhibiting the synthesis of proteoglycans by chondrocytes; Meanwhile, drugs may directly damage tendon cells, leading to collagen fiber rupture.
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