roxithromycin

Action and Spectrum

Actions and spectrum: 

roxithromycin is an antibiotic medication belonging to the macrolide class. It works by inhibiting bacterial protein synthesis, preventing the growth and multiplication of susceptible bacteria.

It is effective against a wide spectrum of gram-positive bacteria, including Streptococcus species (such as Streptococcus pyogenes and Streptococcus pneumoniae), Staphylococcus aureus, and some anaerobic bacteria. roxithromycin is also active against certain gram-negative bacteria, such as Haemophilus influenzae and Moraxella catarrhalis. 

Drug Interaction

Adverse Reaction

Frequency defined 

Gastrointestinal Nausea 

epigastric pain 

anorexia 

pseudomembranous colitis 

vomiting 

diarrhea (rarely contains blood) 

flatulence 

Black Box Warning

Black Box Warning: 

roxithromycin does not have any black box warnings. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with a known hypersensitivity or allergy to roxithromycin or any other macrolide antibiotics should not take this medication. 
• History of Jaundice or Liver Dysfunction: roxithromycin can cause liver problems in some cases. It should be avoided in patients with a history of jaundice or liver dysfunction. 
• Concomitant Use with Ergot Alkaloids: Concurrent use of roxithromycin and ergot alkaloids (used for migraine treatment) can increase the risk of serious side effects. 
• Concomitant Use with Terfenadine or Astemizole: roxithromycin can prolong the QT interval in the heart’s electrical activity and using it together with terfenadine or astemizole can lead to life-threatening arrhythmias. 
• Pregnancy and Breastfeeding: roxithromycin may have adverse effects on the developing fetus and should be used with caution during pregnancy and lactation.

Caution: 

• Liver Function: roxithromycin can occasionally cause liver problems, such as hepatitis or jaundice. It is essential to monitor liver function in patients with pre-existing liver disease or a history of liver dysfunction. 
• QT Prolongation: roxithromycin can prolong the QT interval in the heart’s electrical activity, leading to potential heart rhythm disturbances. Caution is advised in patients with a history of heart rhythm disorders or taking other medications that can also prolong the QT interval. 
• Gastrointestinal Issues: roxithromycin may cause gastrointestinal side effects, such as nausea, vomiting, or diarrhoea. Patients with a history of gastrointestinal disorders should be monitored closely during treatment. 
• Allergic Reactions: Like all antibiotics, roxithromycin can cause allergic reactions in some individuals. If any signs of an allergic reaction, such as rash, itching, or difficulty breathing, occur, medical attention should be sought immediately. 

Comorbidities: 

• Cardiovascular Disorders: roxithromycin can prolong the QT interval in the heart’s electrical activity, leading to potential heart rhythm disturbances. Caution is advised in patients with a history of heart rhythm disorders or other cardiovascular conditions. 
• Gastrointestinal Disorders: roxithromycin may cause gastrointestinal side effects, such as nausea, vomiting, or diarrhoea, which can be problematic in patients with pre-existing gastrointestinal disorders. 
• Myasthenia Gravis: roxithromycin may worsen symptoms in patients with myasthenia gravis, a neuromuscular disorder characterized by muscle weakness. 
• Allergies: Patients with known allergies to roxithromycin or other macrolide antibiotics should avoid its use. 
• Kidney Disease: While roxithromycin is excreted via the liver, patients with severe kidney impairment may require adjusted dosing or close monitoring. 
• Immune Disorders: Patients with compromised immune systems may require careful consideration when using roxithromycin, as it can affect the body’s ability to fight infections. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast milk: yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

roxithromycin is a semi-synthetic macrolide antibiotic belonging to the class of drugs known as macrolides. It exerts its antibacterial effects by inhibiting bacterial protein synthesis, primarily by binding to the 50S ribosomal subunit of the bacterial ribosome. This binding prevents the translocation step in protein synthesis, thus inhibiting the growth and replication of susceptible bacteria. 

roxithromycin has a broad spectrum of activity against both Gram-positive and some Gram-negative bacteria. It is effective against various respiratory tract infections, skin and soft tissue infections, and certain sexually transmitted diseases caused by susceptible bacteria.  

Pharmacodynamics: 

• Bacteriostatic Activity: roxithromycin exhibits bacteriostatic activity, which means it inhibits bacterial growth and replication rather than directly killing the bacteria. It achieves this by interfering with the synthesis of essential bacterial proteins, which are necessary for bacterial survival and reproduction. 
• Antibacterial Effects: By inhibiting bacterial protein synthesis, roxithromycin prevents the formation of new bacterial proteins, including enzymes and structural components. This disruption in protein synthesis impairs the bacteria’s ability to survive, grow, and spread, leading to bacterial cell death or reduction in bacterial population. 
• Time-Dependent Killing: roxithromycin’s bacteriostatic action is time-dependent, which means the drug needs to be present in the body for a sufficient duration to achieve optimal bacterial inhibition. Regular dosing ensures sustained therapeutic levels of the drug, enhancing its efficacy in treating bacterial infections. 
• Post-Antibiotic Effect: After roxithromycin exposure, there may be a post-antibiotic effect, where bacterial growth remains suppressed even after the drug is no longer present. This effect allows for dosing intervals that provide continuous protection against bacterial proliferation.

Pharmacokinetics: 

Absorption 

roxithromycin is well-absorbed from the gastrointestinal tract after oral administration. Food can delay its absorption, but it does not significantly affect its overall bioavailability. The peak plasma concentration is reached within 2 to 4 hours after oral intake. 

Distribution 

roxithromycin is widely distributed throughout the body tissues, including the respiratory tract, skin, and soft tissues. It can penetrate the respiratory secretions, allowing it to target respiratory infections effectively. 

Metabolism 

roxithromycin undergoes hepatic metabolism in the liver, primarily through the cytochrome P450 enzyme system. It is metabolized into several inactive metabolites. 

Elimination and excretion 

The elimination of roxithromycin and its metabolites occurs primarily through the bile and feces. Only a small portion is excreted through the urine. 

Adminstartion

Administration: 

• Dosage Form: roxithromycin is commonly available in tablet or capsule form. The tablets or capsules should be swallowed whole with a glass of water, with or without food, as directed by the healthcare provider. 
• Oral Suspension: If roxithromycin is prescribed as an oral suspension, it should be measured using a dosing syringe, dropper, or measuring cup provided with the medication. The suspension should be shaken well before each use to ensure even distribution of the drug. 
• Dosage and Frequency: The dosage and frequency of roxithromycin administration will depend on the specific condition being treated, the severity of the infection, and the patient’s age and weight. It is crucial to adhere to the prescribed dosage and dosing schedule to ensure optimal therapeutic outcomes. 
• Duration of Treatment: The duration of roxithromycin treatment may vary based on the infection being treated. It is essential to complete the full course of treatment as prescribed by the healthcare professional, even if symptoms improve before the course is finished. Stopping the medication prematurely may lead to treatment failure or the development of drug-resistant bacteria. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: roxithromycin 

Pronounced: (roks-ih-throw-MY-sin)  

Why do we use roxithromycin? 

• Respiratory Tract Infections: roxithromycin is prescribed to treat respiratory tract infections, including acute bronchitis, chronic bronchitis, and community-acquired pneumonia. 
• Soft and skin tissue infections: It is used to treat soft and skin tissue infections like cellulitis, impetigo, and erysipelas. 
• Ear and Throat Infections: roxithromycin is effective in treating ear infections (otitis media) and throat infections (pharyngitis and tonsillitis) caused by susceptible bacteria. 
• Sinusitis: roxithromycin can be used to treat sinusitis, which is an inflammation of the sinuses. 
• Sexually Transmitted Infections: In some cases, roxithromycin is used to treat sexually transmitted infections like non-gonococcal urethritis. 
• Respiratory Tract Infections in COPD Patients: It may also be prescribed to patients with chronic obstructive pulmonary disease (COPD) who develop respiratory tract infections.