Active Pharmaceutical Ingredients

Molecular Formula: C41H76N2O15

Molecular Weight: 837.047

CAS No.: 80214-83-1

Roxithromycin is the most commonly used broad-spectrum and highly effective anti-inflammatory drug. It is commonly used for pharyngitis and tonsillitis caused by Streptococcus pyogenes, and various inflammations caused by sensitive bacteria.

Description

It is a white or almost white, crystalline powder. It is very slightly soluble in water, freely soluble in acetone, in alcohol and in methylene chloride, slightly soluble in dilute hydrochloric acid.

Application

It is the most commonly used broad-spectrum and highly effective anti-inflammatory drug. It is commonly used for pharyngitis and tonsillitis caused by Streptococcus pyogenes, and various inflammations caused by sensitive bacteria.

Roxithromycin is a semi-synthetic macrolide antibiotic. Its mechanism of action is similar to that of erythromycin. Its antibacterial effect in the body is 1-4 times stronger than that of erythromycin. It is more effective against gram-positive bacteria than erythromycin. Slightly worse, the effect on Legionella pneumophila is stronger than that of erythromycin, and its antimicrobial effect on Chlamydia pneumoniae, Mycoplasma pneumoniae and Ureaplasma urealyticum is similar to or slightly stronger than that of erythromycin.

Packing

25Kg per drum

Storage：

Preserve in tight containers in a dry place.

Shelf Life :

24 months from date of production when stored in good condition.

Minimum Order

One package.

Roxithromycin Introduction

Item	Details
Generic Name	Roxithromycin
Trade Names	Rulide, etc.
Classification	Macrolide antibiotic
Chemical Structure	It has a 14 – membered macrolactone ring structure, with a desosamine sugar attached. The molecular formula is C₄₃H₇₅NO₁₅, and the molecular weight is 837.06. This unique structure enables it to interact with the bacterial ribosome.
Pharmacological Action	Roxithromycin binds to the 50S subunit of the bacterial ribosome. This binding inhibits the translocation step during protein synthesis, preventing the elongation of the polypeptide chain. As a result, bacteria are unable to produce essential proteins for their survival and growth, leading to their death or inhibition. It has a broad – spectrum antibacterial activity, mainly effective against Gram – positive bacteria such as Streptococcus pneumoniae, Staphylococcus aureus, and also has activity against some Gram – negative bacteria like Haemophilus influenzae, as well as atypical pathogens such as Mycoplasma pneumoniae and Chlamydia trachomatis.
Clinical Applications	1. Respiratory Tract Infections: – Used for the treatment of community – acquired pneumonia, often caused by Streptococcus pneumoniae, Mycoplasma pneumoniae. – Acute exacerbations of chronic bronchitis, where it can target Haemophilus influenzae and other pathogens. – Pharyngitis and tonsillitis, especially when caused by Streptococcus pyogenes. 2. Genitourinary Tract Infections: – Treats non – gonococcal urethritis and cervicitis caused by Chlamydia trachomatis. 3. Skin and Soft Tissue Infections: – Effective against skin infections such as impetigo and cellulitis caused by Staphylococcus aureus and Streptococcus pyogenes.
Dosage and Administration	Adults: – For most infections, the usual oral dose is 150 mg twice daily. – In some cases, for more severe infections, the dose can be increased to 300 mg twice daily. Children: – The dose is calculated based on body weight. Generally, it is 2.5 – 5 mg/kg body weight twice daily. Roxithromycin is usually taken orally, and it is recommended to take it on an empty stomach (1 hour before or 2 hours after a meal) for better absorption. However, if gastrointestinal discomfort occurs, it can be taken with food.
Adverse Reactions	1. Gastrointestinal Effects: Nausea, vomiting, diarrhea, abdominal pain, and loss of appetite are common side effects. These symptoms are usually mild to moderate and may be more likely to occur when the drug is taken on an empty stomach. 2. Allergic Reactions: Although rare, rashes, itching, and in severe cases, anaphylactic shock can occur. 3. Hepatotoxicity: In some cases, it may cause mild and transient elevations in liver enzymes, such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST). 4. Cardiovascular Effects: Rarely, it may be associated with QT – interval prolongation, which can potentially lead to serious cardiac arrhythmias, especially in patients with pre – existing cardiac conditions or those taking other drugs that also affect the QT interval.
Drug Interactions	1. With CYP3A4 – related Drugs: Roxithromycin is metabolized by the cytochrome P450 3A4 enzyme system. Drugs that inhibit CYP3A4. such as ketoconazole, can increase the levels of roxithromycin, leading to an increased risk of side effects. On the other hand, drugs that induce CYP3A4. like rifampicin, can decrease the levels of roxithromycin, potentially reducing its efficacy. 2. With Theophylline: Co – administration with theophylline can increase the blood levels of theophylline, increasing the risk of theophylline toxicity, such as seizures and cardiac arrhythmias. Close monitoring of theophylline levels is required when used together. 3. With Warfarin: Roxithromycin may enhance the anticoagulant effect of warfarin, increasing the risk of bleeding. Regular monitoring of prothrombin time or international normalized ratio (INR) is necessary when these two drugs are used concomitantly.
Special Population Considerations	1. Pregnant Women: Use during pregnancy is generally not recommended, as there is limited data on its safety. However, in some cases where the benefits outweigh the potential risks, it may be used under strict medical supervision. 2. Breastfeeding Women: It is excreted in breast milk in small amounts. Caution should be exercised when using it during breastfeeding, and in some cases, breastfeeding may need to be temporarily discontinued. 3. Patients with Liver Impairment: The drug should be used with caution in patients with significant liver impairment, as its metabolism may be affected, leading to increased drug levels and a higher risk of side effects. Dosage adjustment may be required. 4. Elderly Patients: Elderly patients may be more sensitive to the drug’s side effects, especially gastrointestinal and cardiovascular effects. Close monitoring is needed when prescribing roxithromycin to the elderly.
History and Development	Roxithromycin was developed as an improvement over earlier macrolide antibiotics. It was designed to have better pharmacokinetic properties, such as improved oral bioavailability and longer half – life compared to some of its predecessors. This allows for less frequent dosing and potentially better patient compliance. It has been widely used in clinical practice since its introduction for the treatment of various infections caused by susceptible organisms.

 

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