Each sachet of 1.5 g granules for oral suspension contains Azithromycin 250 mg (as azithromycin dihydrate).
Excipients/Inactive Ingredients: Saccharose, kyron T-112 B, aspartame, strawberry aroma.
Pharmacotherapeutic group: Antibacterial for systemic use; Macrolides. ATC code: J01FA10.
Pharmacology: Pharmacodynamics: Azithromycin is a macrolide antibiotic belonging to the azalide group. The mechanism of action of azithromycin is based upon the suppression of bacterial protein synthesis by means of binding to the ribosomal 50S subunit and inhibition of peptide translocation.
Azithromycin susceptibility breakpoints for typical bacterial pathogens are: Aerobic Gram-positive microorganisms: Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes.
Aerobic Gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida.
Anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp.
Other microorganisms: Chlamydia trachomatis.
Pharmacokinetics: Azithromycin given orally is about 40% bioavailable. Peak plasma concentrations are achieved 2 to 3 hours after a dose, but azithromycin is extensively distributed to the tissues, and tissue concentrations subsequently remain much higher than those in the blood; in contrast to most other antibacterials, plasma concentrations are therefore of little value as a guide to efficacy. High concentrations are taken up into white blood cells. There is little diffusion into the CSF when the meninges are not inflamed.
Small amounts of azithromycin are demethylated in the liver, and it is excreted in bile as unchanged drug and metabolites. About 6% of an oral dose is excreted in the urine. The terminal elimination half-life is about 68 hours.
Azithromycin is indicated for the treatment of infections: Upper respiratory tract infections: Ear, nose and throat infections like sinusitis, tonsillitis, otitis media, etc.
Lower respiratory tract infections: Pneumonias, acute bronchitis.
Skin and soft tissue infections: Furunculosis, pyoderma, impetigo due to Staphylococcus aureus.
Sexually transmitted diseases: Urethritis and cervicitis, non-gonococcal urinary tract infections and pelvises.
Adults: Upper and lower respiratory tract infections, skin and soft-tissue infections: Initial dosage is 500 mg as a single dose on the first day and followed by 250 mg once daily for 4 days.
Sexually Transmitted Diseases: 1 g as a single dose.
Children: One single dose of 10 mg/kg/day for 3 days.
Administration: Azicine 250 mg is administered orally. Dissolved in warm water.
Administer at least 1 hour before or 2 hours after a meal.
Symptoms: The typical symptoms of an overdose with macrolide antibiotics include reversible loss of hearing, severe nausea, vomiting and diarrhoea.
Treatment: The administration of medicinal charcoal and general symptomatic treatment and supportive measures are indicated as required.
Azithromycin is contraindicated in patients with known hypersensitivity to azithromycin, erythromycin, or any macrolide antibiotic.
The use of the drug is not recommended in children under 6 months.
Serious hypersensitivity reactions, including angioedema, anaphylaxis, and dermatologic reactions, have occurred rarely in patients receiving azithromycin.
Because azithromycin is eliminated principally via the liver, the drug should be used with caution in patients with impaired hepatic function.
Because of limited data regarding use of azithromycin in patients with renal impairment, the drug should be used with caution in patients with glomerular filtration rates less than 10 mL/minute.
Prolonged cardiac repolarization and QT interval with risk of cardiac arrhythmia and torsades de pointes has been reported rarely with macrolides. The possibility of such effects with azithromycin cannot be completely ruled out in patients at increased risk for prolonged cardiac repolarization.
To reduce development of drug-resistant bacteria and maintain effectiveness of azithromycin and other antibacterials, the drug should be used only for the treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.
Azicine 250 mg contains sucrose (saccharose). Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
Azicine 250 mg contains aspartame. Aspartame is a source of phenylalanine. It may be harmful if the patient has phenylketonuria (PKU), a rare genetic disorder in which phenylalanine builds up because the body cannot remove it properly.
Pregnancy: There are no adequate and controlled studies to date using azithromycin in pregnant women, and the drug should be used during pregnancy only when clearly needed.
Lactation: Azithromycin has been detected in human milk. The drug should be used with caution in nursing women.
As for erythromycin, azithromycin is well tolerated with a low incidence of side effects (approximately 13% of all treated patients). The most frequent adverse reactions of azithromycin are gastrointestinal disturbances (10%) in origin with nausea, abdominal discomfort (pain/cramps), vomiting, flatulence, diarrhea, and loose stools being occasionally observed, but they are usually mild and less frequent than with erythromycin. Transient elevations of liver enzyme values have been reported. Rashes, headache, and dizziness may occur. Transient alterations in neutrophil counts have been seen in patients receiving azithromycin.
In investigational studies where higher doses were used for prolonged periods of time, reversible hearing impairment was seen in some patients.
Gastrointestinal: Nausea, diarrhea, pain, vomiting.
General: Fatigue, headache, vertigo, somnolence.
Gastrointestinal: Flatulence, dyspepsia, appetite loss.
Skin: Skin eruptions, itch.
Others: Vaginosis, colpitis, etc.
General: Anaphylactic reaction.
Liver: Elevated transaminase.
Blood: Slight transient decrease of neutrophils.
Aluminium/magnesium hydroxide antacids: May reduce the peak levels of azithromycin, and administration should be separated.
Anticoagulants: A marked increase in the effects of warfarin and bleeding has been seen in a small number of patients given azithromycin, but most patients are unlikely to develop a clinically important interaction.
Digitalis glycosides: Some patients unpredictably show a rapid and marked two to fourfold increase in serum digoxin levels when given azithromycin. The same interaction has been seen with digitoxin and azithromycin. Digitalis toxicity can occur.
Ergotamine or dihydroergotamine: Acute ergot toxicity characterized by severe peripheral vasospasm and dysesthesia.
Triazolam: Decreases the clearance of triazolam and thus may increase the pharmacologic effect of triazolam.
Drugs metabolized by the cytochrome P-450 system: Elevations of serum carbamazepine, cyclosporine, hexobarbital, and phenytoin levels.
Store in a well-closed container, in a dry place. Do not store above 30°C.
Shelf-Life: 24 months from the date of manufacturing.
J01FA10 - azithromycin ; Belongs to the class of macrolides. Used in the systemic treatment of infections.
Granules for oral susp (sachet) 250 mg (white, sweet tasting and with strawberry aroma) x 1.5 g x 6's.