Description: Azithromycin for Injection is a macrolide antibacterial drug indicated for the treatment of patients with infections caused by susceptible strains of the designated microorganisms in the conditions listed below. Community-Acquired Pneumonia. Due to Chlamydophila pneumoniae,Haemophilus influenzae, Legionella pneumophila, Moraxella catarrhalis,Mycoplasma pneumoniae, Staphylococcus aureus, or Streptococcus pneumoniae in patients who require initial intravenous therapy. Pelvic Inflammatory Disease Due to Chlamydia trachomatis, Neisseria gonorrhoeae, or Mycoplasma hominis in patients who require initial intravenous therapy. If anaerobic microorganisms are suspected of contributing to the infection, an antimicrobial agent with anaerobic activity should be administered in combination with Azithromycin. Azithromycin for Injection should be followed by azithromycin the oral route as required.

Pharmacological effects: Azithromycin is a macrolide antibacterial drug. Mechanism of Action Azithromycin acts by binding to the 50S ribosomal subunit of susceptible microorganisms and, thus, interfering with microbial protein synthesis. Nucleic acid synthesis is not affected. Cross Resistance Azithromycin demonstrates cross-resistance with erythromycin-resistant Gram-positive isolates.Azithromycin has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections as described in. Gram-positive Bacteria Staphylococcus aureus Streptococcus pneumoniae. Gram-negative Bacteria Haemophilus influenzae/Moraxella catarrhalis/ Neisseria gonorrhoeae/Legionella pneumophila.Other Bacteria Chlamydophila pneumoniae/Chlamydia trachomatis/Mycoplasma hominis/Mycoplasma pneumoniae. The following in vitro data are available, but their clinical significance is unknown. Azithromycin exhibits in vitro minimal inhibitory concentrations (MICs) of 2.0 mcg/mL or less against most (≥ 90%) isolates of the following bacteria; however, the safety and effectiveness of azithromycin in treating clinical infections due to these bacteria have not been established in adequate and well-controlled trials. Aerobic Gram-positive Bacteria Streptococci (Groups C, F, G)/Viridans group streptococci. Gram-negative Bacteria Bordetella pertussis. Anaerobic Bacteria Peptostreptococcus species/Prevotella bivia. Other Bacteria Ureaplasma urealyticum
Azithromycin of barriers to bacterial peptide process, thereby inhibiting bacterial protein synthesis. In vitro tests proved right azithromycin many common clinical pathogens effectively, including Gram-positive aerobes: Staphylococcus aureus, Streptococcus pyogenes (group A β - hemolytic streptococcus), pneumonia (chain) cocci, α - hemolytic streptococcus (Streptococcus Green Grass) and other streptococcus, diphtheria (ROD) bacilli. Azithromycin for erythromycin-resistant Gram-positive bacteria, including fecal streptococcus (enterococci), and methicillin-resistant Staphylococcus aureus strains showed a variety of cross-resistance. Gram-negative aerobes: influenza (Haemophilus) bacteria, parainfluenza (Haemophilus) bacteria, cards he (quietly) bacteria, Acinetobacter is, Yersinia species, Legionella pneumophila, pertussis bacteria, vice pertussis bacteria, Shigella species, genus Pasteur, Huo chaos Vibrio vice hemolytic bacteria, like Shigella bacteria topiramate Plesiomonas. Anaerobes: Bacteroides fragilis, Bacteroides is, Clostridium bacteria, Streptococcus digest necrosis fusobacterium, of Propionibacterium acnes.Sexually transmitted disease microorganisms: Chlamydia trachomatis, dense spiral of syphilis, gonorrhea, Duke (Haemophilus) bacilli. Other microorganisms include: Charles borrow spiral of (Lyme pathogens) (Lyme diseaseagent), Mycoplasma pneumoniae, Mycoplasma hominis, Ureaplasma body of the original, Pneumocystis carinii, Mycobacterium is a bird, bending genus, mononucleosis and Lee de bacilli. Following Gram-negative bacteria is usually resistant: Proteus is a Shara genus, Morgan bacteria, green pus (PSEUDOMONAS) bacilli. Animal model studies found that the materials found in phagocytic cells, and when phagocytic cells were activated, after the release of the high concentration of azithromycin. Therefore liver infection sites in a high concentration. 

Pharmacokinetics: In patients hospitalized with community-acquired pneumonia receiving single daily one-hour intravenous infusions for 2 to 5 days of 500-mg azithromycin at a concentration of 2 mg/mL, the mean Cmax ± S.D. achieved was 3.63 ± 1.60 mcg/mL, while the 24-hour trough level was 0.20 ± 0.15 mcg/mL, and the AUC24 was 9.60 ± 4.80 mcg·h/mL. The mean Cmax, 24-hour trough and AUC24 values were 1.14 ± 0.14 mcg/mL, 0.18 ± 0.02 mcg/mL, and 8.03 ±0.86 mcg· h/mL, respectively, in normal volunteers receiving a 3-hour intravenous infusion of 500 mg azithromycin at a concentration of 1 mg/mL. Similar pharmacokinetic values were obtained in patients hospitalized with community-acquired pneumonia who received the same 3-hour dosage regimen for 2-5 days.
a   500 mg (2 mg/mL) for 2-5 days in community-acquired pneumonia patients.
b   500 mg (1 mg/mL) for 5 days in healthy subjects.
Infusion Concentration, Duration Time after starting the infusion (hr)      
 
0.5  
1 2 3 4 6  
8  
12  
24
2 mg/mL, 1 hr 2.98 ±1.12 3.63 ±1.73 0.60 ±0.31 0.40 ±0.23 0.33 ±.16 0.26 ±0.14 0.27 ±0.15 0.20 ±0.12 0.20 ±0.15
1 mg/mL, 3 hr 0.91 ±0.13 1.02 ±0.11 1.14 ±0.13 1.13 ±0.16 0.32 ±0.05 0.28 ±0.04 0.27 ±0.03 0.22 ±0.02 0.18 ±0.02
Comparison of the plasma pharmacokinetic parameters following the 1st and 5th daily doses of 500 mg intravenous azithromycin showed only an 8% increase in Cmax but a 61% increase in AUC24 reflecting a threefold rise in C24 trough levels. Following single-oral doses of 500 mg azithromycin (two 250 mg capsules) to 12 healthy volunteers, Cmax, trough level, and AUC24 were reported to be 0.41 mcg/mL, 0.05 mcg/mL, and 2.6 mcg·h/mL, respectively. These oral values are approximately 38%, 83%, and 52% of the values observed following a single 500-mg I.V. 3-hour infusion (Cmax: 1.08 mcg/mL, trough: 0.06 mcg/mL, and AUC24: 5.0 mcg·h/mL). Thus, plasma concentrations are higher following the intravenous regimen throughout the 24-hour interval.

Indications: This applies to sensitive goods caused by the bacteria of the following infections: Otitis media, sinusitis, pharyngitis and tonsillitis, upper respiratory infection; Bronchitis, pneumonia and other lower respiratory tract infections . Skin and soft tissue infections. Genital Chlamydia trachomatis infections caused by simple. 

Adverse reaction: In clinical trials of intravenous azithromycin for community- acquired pneumonia, in which 2 to 5 IV doses were given, the reported adverse reactions were mild to moderate in severity and were reversible upon discontinuation of the drug. The majority of patients in these trials had one or more co-morbid diseases and were receiving concomitant medications. Approximately 1.2% of the patients discontinued intravenous Azithromycin for Injection, USP therapy, and a total of 2.4% discontinued azithromycin therapy by either the intravenous or oral route because of clinical or laboratory side effects. In clinical trials conducted in patients with pelvic inflammatory disease, in which 1 to 2 IV doses were given, 2% of women who received monotherapy with azithromycin and 4% who received azithromycin plus metronidazole discontinued therapy due to clinical side effects. Clinical adverse reactions leading to discontinuations from these studies were gastrointestinal (abdominal pain, nausea, vomiting, diarrhea), and rashes; laboratory side effects leading to discontinuation were increases in transaminase levels and/or alkaline phosphatase levels. Overall, the most common adverse reactions associated with treatment in adult patients who received IV/Oral Azithromycin in studies of community-acquired pneumonia were related to the gastrointestinal system with diarrhea/loose stools (4.3%), nausea (3.9%), abdominal pain (2.7%), and vomiting (1.4%) being the most frequently reported. Approximately 12% of patients experienced a side effect related to the intravenous infusion; most common were pain at the injection site (6.5%) and local inflammation (3.1%). The most common adverse reactions associated with treatment in adult women who received IV/Oral Azithromycin in trials of pelvic inflammatory disease were related to the gastrointestinal system. Diarrhea (8.5%) and nausea (6.6%) were most commonly reported, followed by vaginitis (2.8%), abdominal pain (1.9%), anorexia (1.9%), rash and pruritus (1.9%). When azithromycin was co-administered with metronidazole in these trials, a higher proportion of women experienced adverse reactions of nausea (10.3%), abdominal pain (3.7%), vomiting (2.8%), infusion site reaction,stomatitis, dizziness, or dyspnea (all at 1.9%)