ROLOX 560MG FILM COATED TABLET

Dosage

Children: Refer to specific compound BNF for appropriate dosing guidelines.

Adults: Refer to specific compound BNF for appropriate dosing guidelines.

Mechanism of action

The mechanism of action for dihydrates depends on the specific compound they are associated with. Generally, dihydrates may enhance the solubility and dissolution rate of certain drugs, improving their absorption in the gastrointestinal tract. In some cases, the presence of water molecules can stabilize the drug structure, affecting its release and bioavailability.

Pharmacodynamics

Pharmacodynamics will vary widely based on the specific dihydrate compound being discussed. Generally, dihydrates can improve the pharmacokinetic profiles of drugs by increasing solubility and facilitating better absorption. This can lead to enhanced efficacy and potentially reduced side effects if the drug can be administered at lower doses due to improved bioavailability.

Pharmacokinetics

The pharmacokinetics of a dihydrate compound will depend on its specific properties, including molecular weight, solubility, and stability in physiological conditions. Typically, dihydrate forms of drugs exhibit altered absorption rates and may have different distribution, metabolism, and excretion profiles compared to their anhydrous counterparts. The presence of water molecules can influence the dissolution rates and transport mechanisms across biological membranes.

Indications

• Bacterial infections
• Urinary tract infections
• Respiratory tract infections
• Skin and soft tissue infections
• Bone and joint infections

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing recommendations.

Adults: Refer to the BNF for specific adult dosing guidelines based on the type and severity of the infection being treated.

Mechanism of action

The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria, while topoisomerase IV is the preferential target in gram-positive organisms. This interference leads to strand breakage of the bacterial chromosome, supercoiling, and resealing, ultimately inhibiting DNA replication and transcription.

Pharmacodynamics

Pefloxacin is a fluoroquinolone antibiotic that exhibits excellent activity against gram-negative aerobic bacteria such as E. coli and Neisseria gonorrhoeae, as well as gram-positive bacteria including Streptococcus pneumoniae and Staphylococcus aureus. It is also effective against Shigella, Salmonella, Campylobacter, gonococcal organisms, and multi-drug resistant strains of Pseudomonas and Enterobacter.

Pharmacokinetics

Pefloxacin is well absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. The drug is widely distributed throughout the body, including into tissues and fluids such as urine and lung tissue. It has a half-life of approximately 7 to 12 hours, allowing for once or twice daily dosing. Pefloxacin is primarily excreted unchanged in the urine, making it effective for urinary tract infections.

Contra-indications

• History of hypersensitivity to pefloxacin or other fluoroquinolones
• Tendinopathy or history of tendon rupture related to fluoroquinolone use
• Pregnancy

Adverse effects

• Nausea
• Diarrhea
• Headache
• Dizziness
• Tendon rupture
• Photosensitivity
• QT prolongation

Interactions

• Antacids containing magnesium or aluminum may decrease absorption
• Non-steroidal anti-inflammatory drugs (NSAIDs) may increase risk of CNS stimulation
• Warfarin may have increased anticoagulant effect

Precautions

• Use with caution in patients with a history of seizures or CNS disorders
• Monitor for signs of tendon pain or inflammation
• Avoid in patients with myasthenia gravis

Pregnancy

Pefloxacin should be avoided during pregnancy due to potential harm to the fetus.

Breast-feeding

Pefloxacin is excreted in breast milk, caution is advised when administering to breastfeeding mothers.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Tablets
• Injectable solution

Mechanism of action

The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.

Pharmacodynamics

Pefloxacin is a fluoroquinolone antibiotic. Flouroquinolones such as pefloxacin possess excellent activity against gram-negative aerobic bacteria such as <i>E.coli</i> and <i>Neisseria gonorrhoea</i> as well as gram-positive bacteria including <i>S. pneumoniae</i> and <i>Staphylococcus aureus</i>. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.