Azimex 500 mg

Description

Indications
Azimex is prescribed for infections caused by susceptible microorganisms. It is effective in treating lower respiratory tract infections, including bronchitis and pneumonia, as well as upper respiratory tract infections such as sinusitis and pharyngitis/tonsillitis. Additionally, it is used to manage otitis media, skin and soft tissue infections. In the treatment of sexually transmitted diseases, Azimex is recommended for non-gonococcal urethritis and cervicitis caused by Chlamydia trachomatis.

Pharmacology
Azithromycin is stable in acidic conditions, allowing it to be taken orally without the need for protection from gastric acids. It is efficiently absorbed, with higher absorption levels observed when taken on an empty stomach. Peak plasma concentrations are typically achieved within 2.1 to 3.2 hours post-administration. Due to its high concentration in phagocytes, the drug is transported directly to the site of infection, where it is released during active phagocytosis. Tissue concentrations of azithromycin can be significantly higher than plasma levels, attributed to its lipid solubility and ion trapping.

The prolonged half-life of azithromycin allows for a single-dose regimen while maintaining effective bacteriostatic concentrations in infected tissues for several days. Following a single 500 mg dose, plasma levels decline in a polyphasic manner, with an average plasma clearance of 630 mL/min and a terminal elimination half-life of approximately 68 hours. The primary route of excretion is via the biliary system, with a small fraction (around 6%) excreted unchanged in urine.

Mechanism of Action & Microbiology
Azithromycin exerts its antibacterial effect by binding to the 50S ribosomal subunit of susceptible bacteria, inhibiting protein synthesis without affecting nucleic acid synthesis. It has demonstrated efficacy against a range of pathogens, including:

• Gram-positive bacteria: Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes
• Gram-negative bacteria: Haemophilus ducreyi, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae
• Other organisms: Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma pneumoniae
• Anaerobic bacteria: Peptostreptococcus species, Prevotella bivia

Dosage & Administration
Oral Dosage:

• Adults: 500 mg once daily for three days, or 500 mg on the first day followed by 250 mg daily for the next four days. For sexually transmitted infections due to Chlamydia trachomatis, a single 1 g dose or an alternative regimen of 500 mg on day 1 followed by 250 mg daily for the next two days may be used.
• Children: 10 mg/kg once daily for three days (for children over six months old). Specific doses based on weight:
  • 15-25 kg: 200 mg daily for three days
  • 26-35 kg: 300 mg daily for three days
  • 36-45 kg: 400 mg daily for three days
  • Typhoid fever: 500 mg once daily for 7-10 days

Intravenous (IV) Infusion:

• Community-acquired pneumonia (adults): 500 mg IV daily for at least two days, followed by 500 mg orally daily (as two 250 mg tablets) to complete a 7-10 day treatment course.
• Pelvic inflammatory disease (adults): 500 mg IV daily for one or two days, followed by 250 mg orally daily to complete a 7-day course.
• Pediatric Use: Not established for children under 16 years for IV administration.

Suspension Reconstitution Instructions

1. Shake the bottle to loosen the powder.
2. Add boiled and cooled water up to the indicated mark.
3. Shake well until fully mixed.
4. Administer at least one hour before or two hours after meals.

Drug Interactions

• Antacids: Should be taken at least 1 hour before or 2 hours after azithromycin.
• Cyclosporin & Digoxin: Possible interaction; monitor blood levels if co-administered.
• Ergot Derivatives: Contraindicated due to risk of ergot toxicity.
• Warfarin: Co-administration requires monitoring of prothrombin time.
• Terfenadine: No significant QT prolongation observed but should be used with caution.

Contraindications
Azimex should not be used in individuals with hypersensitivity to azithromycin or other macrolide antibiotics. It is also contraindicated in patients with hepatic disease or those taking ergot derivatives.

Side Effects
Common side effects include mild gastrointestinal discomfort, nausea, vomiting, diarrhea, and flatulence. Rare allergic reactions such as skin rash and photosensitivity may occur. Serious but infrequent adverse effects include hepatic dysfunction and reversible hearing impairment in high-dose treatments.

Pregnancy & Lactation
Classified as Pregnancy Category B, azithromycin has shown no fetal harm in animal studies, but adequate studies in pregnant women are lacking. It should only be used when no safer alternatives are available. Excretion in breast milk is uncertain; caution is advised when administering to nursing mothers.

Precautions & Warnings

• Rare cases of severe allergic reactions, including angioedema and anaphylaxis, have been reported.
• Use with caution in patients with severe renal impairment (creatinine clearance <40 mL/min).
• As azithromycin is primarily eliminated by the liver, it should not be used in patients with hepatic impairment.
• No significant effect on driving ability or machinery operation has been observed.

Overdose & Management
Symptoms of overdose include nausea, vomiting, diarrhea, and potential hearing loss. Treatment involves gastric lavage and symptomatic management.

Storage Conditions
Store in a dry place, away from light and heat. Keep out of the reach of children.

Frequently Asked Questions (FAQs)

• What is Azimex 500 mg Tablet used for?
  It is used for treating infections such as respiratory tract infections, pharyngitis, tonsillitis, skin infections, and sexually transmitted diseases.
• Can Azimex 500 mg Tablet cause diarrhea?
  Yes, diarrhea may occur due to the disruption of gut bacteria. If severe, consult a doctor.
• Is Azimex 500 mg Tablet safe?
  It is safe when taken as prescribed by a healthcare provider.
• What if symptoms persist after taking Azimex?
  If no improvement is observed within three days, consult your doctor.

Quick Tips

• Complete the full course of treatment even if symptoms improve early.
• Take one hour before or two hours after meals.
• Avoid antacids within two hours of taking the medication.
• Seek medical attention if allergic reactions occur.