PATIENT INFORMATION LEAFLET
INTERNATIONAL NONPROPRIETARY NAME
Powder for oral suspension.
Description: white coloured homogeneous powder with characteristic cherry and banana odour; after dissolution in water - white or almost white coloured homogeneous suspension with characteristic cherry and banana odour.
Active ingredient: 1 bottle 5 ml of suspension azithromycin (as azithromycin dihydrate) 1200 mg 200 mg
Excipients: sucrose, tribasic sodium phosphate anhydrus, sodium benzoate, hydroxypropylcellulose, xanthan gum, cherry flavour, banana flavour.
ATC CODE J01FA10
Systemic antimicrobial preparations. Macrolides and azalides.
PHARMACOLOGICAL PROPERTIES PHARMACODYNAMICS
Azithrosan (azithromycin) is a representative of the subgroup of macrolide antibiotics – azalides - with a wide spectrum of action. Binding to 50S-subunit of the ribosome, azithromycin suppresses peptide translocase at the translation stage and inhibits protein synthesis in the microbial cell.
Azithromycin is active against the following microorganisms:
Gram-positive microorganisms Enterococcus faecalis and the majority of methicillin-resistant strains of Staphylo- coccus, as well as anaerobes Bacteroides fragilis, are resistant to the drug.
Bioavailability after oral administration is 37%; peak plasma concentration (Cmax) is reached within 2-3 hours; volume of distribution is 31.1 l/kg. Plasma protein binding is inversely proportional to the blood concentration and is 12-52%. The substance penetrates through cell membranes (effective in infections induced by intracellular agents). It is transported by phagocytes, polymorphonuclear leukocytes and macrophages to the infection site, where it is released in the presence of bacteria. It easily crosses histohematic barriers and penetrates into tissues. Its concentration in tissues and cells is 50 times higher than that in plasma; its concentration in the focus of infection is 24-34% higher than in healthy tissues.
The drug is slowly eliminated from tissues and has a long half-life of 2-4 days. Therapeutic concentration of azithromycin persists up to 5-7 days after administration of the last dose. Azithromycin is eliminated mainly in the unchanged form: 50% via the intestine, 12% via kidneys. It is demethylated in liver, losing its activity.
Elimination half-life of azithromycin in patients with severe renal failure (creatinine clearance (CC) below 10 ml/min.) increases by 33%.
Infectious and inflammatory diseases induced by susceptible microorganisms:
- infections of the upper respiratory tract and ENT organs (pharyngitis/tonsillitis, sinusitis, otitis media);
- infections of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including pneumonia induced by atypical agents);
- infections of skin and soft tissues (chronic migratory erythema - the initial stage of Lyme disease, erysipelas, impetigo, secondarily infected dermatoses);
- sexually transmitted infections (urethritis, cervicitis);
- gastric and duodenal infections associated with Helicobacter pylori.
DOSAGE AND ADMINISTRATION
Azithrosan suspension is administered orally, once daily, 1 hour before or 2 hours after a meal.
In infections of the upper and the lower respiratory tract, ENT organs, skin and soft tissues: the drug is prescribed in a dose of 10 mg/kg once daily for 3 days; the course dose is 30 mg/kg.
Volume of suspension required for 1 administration
2.5 ml (100 mg of azithromycin)
5.0 ml (200 mg of azithromycin)
7.5 ml (300 mg of azithromycin)
10.0 ml (400 mg of azithromycin)
not less than 45 kg
12.5 ml (500 mg of azithromycin) (corresponds to the dose for adults)
Inchronicmigratoryerythema:the 1st day: 20 mg/kg/day, the 2nd-5th days: 10 mg/kg/day; course dose: 60 mg/kg.
In gastric and duodenal diseases associated with Helicobacter pylori: 20 mg/kg of body weight once daily in combination with an antisecretory agent and other drugs upon the recommendation of the doctor.
In sexually transmitted diseases: uncomplicated urethritis/cervicitis - a single dose of 10 mg/kg of body weight; complicated, persistent urethritis/cervicitis induced by Chlamydia trachomatis - 10 mg/kg of body weight three times with 7 days intervals (1-7-14).
Patients with renal function disorder: no dose adjustment is required in renal function disorder (CC above 40 ml/min.).
Patients with hepatic function disorder: no dose adjustment is required in moderate hepatic function disorder.
Preparation of suspension:
To prepare 30 ml of suspension add 15 ml of water into the bottle containing 1200 mg of azithromycin. Store reconstituted suspension at temperature not exceeding 25°C for not more than 5 days.
Carefully shake the content of the vial before every administration until homogeneous suspension is formed.
Use a measuring syringe, graduated at 5 ml, a measuring spoon, graduated at 1.25 ml, 2.5 ml and 5 ml, and a mea- suring cup, graduated at 15 ml, for dosing of the prepared suspension.
Upon administration of suspension give the child some tea or juice in order to wash off and swallow the suspension remaining in the mouth.
After the use wash the measuring cup and the measuring spoon with running water, dry up and store together with the drug.
The used side effects frequency parameters presented below are classified in the following way: very common (≥ 1/10), common (from ≥ 1/100 to < 1/10), uncommon (from ≥ 1/1000 to < 1/100), rarely (from ≥ 1/10000 to
< 1/1000), very rarely (< 1/10000), unknown frequency - frequency parameters can not be estimated from the available data.
Most of the observed adverse reactions are reversible and disappear after the end of the treatment course or after withdrawal of the drug.
GIT disorders: very common - nausea, abdominal pain, diarrhea, flatulence; common - vomiting; uncommon - constipation; rarely - cholestatic jaundice, loss of appetite, gastritis; very rarely - candidamycosis of the oral mucosa. Allergic reactions: common - rash, skin itching; uncommon - urticaria; rarely - angioneurotic edema and anaphy- lactic shock.
Laboratory abnormalities: common - increase eosinophil count; uncommon - reversible increase in liver transa- minases activity, bilirubin activity; these indices return to normal rates within 2-3 weeks after the end of treatment. In very rarely cases a transitory decrease of neutrophil count is possible in the setting of azithromycin therapy, but no causal relationship has been determined.
Cardiovasculardisorders:uncommon - palpitations, chest pain.
Nervous system disorders: common - dizziness, headache, paresthesias; uncommon - somnolence; rarely - vertigo; unknown frequency - agitation; in children: common - headache (in otitis media therapy); uncommon - neurosis, sleep disturbances; rarely - hyperkinesia; unknown frequency - irritability, anxiety.
Urogenital system disorders: uncommon - vaginal candidiasis; unknown frequency - nephritis.
Other disorders: uncommon - conjunctivitis, photosensitivity, increased fatigue.
If you missed one dose of the drug, take the next dose as soon as possible, and the subsequent ones with 24 hours intervals.
Use Azithrosan with caution in moderate hepatic failure, moderate renal failure (CC > 40 ml/min.), in arrhythmias or predisposition to arrhythmias and to QT interval prolongation.
Using the drug in patients with diabetes mellitus and those on a low-calorie diet, take into consideration that the suspension contains saccharose (908.3547 mg/g of powder for suspension).
INFLUENCE ON ABILITY TO DRIVE AND OPERATE MECHANISMS
In case of development of CNS and vision adverse effects, exercise caution while driving and performing other potentially dangerous activities requiring increased mental alertness and speed of psychomotor reactions.
PREGNANCY AND LACTATION
Administration of Azithrosan during pregnancy is possible only when the benefit for the mother outweighs potential risk of complications for the fetus.
If administration of the drug during lactation is necessary, discontinue breast feeding.
Azithrosan suspension is administeredin children over 6 months. In children under 6 months the drug is prescribed in the form of powder for oral suspensionin concentrationof 100 mg/5 ml.
Antacids do not affect bioavailability of azithromycin, but decrease its Cmax by 25%, thus the drug should be used at least 1 hour before or 2 hours after administration of antacids.
Concomitant administration of fluconazole reduces Cmaxof azithromycin by 18%.
If concomitant administration of cyclosporine is required, control of blood cyclosporine concentration must be estab- lished due to a significant increase of area under the concentration-time curve.
In case of simultaneous administration of digoxin and azithromycin blood digoxin control must be established, as many macrolides increase intestinal digoxin absorption, thus increasing its Cmax.
Azithromycin is not used concomitantly with ergotamine and dihydroergotamine derivatives due to possible deve-
lopment of ergotism.
Ergotamine and dihydroergotamine may exercise toxic action in concomitant administration with macrolides.
If simultaneous administration with indirect-action anticoagulants (coumarin-type anticoagulants, including warfarin) is required, strict control of prothrombin time must be established.
It has been found that concomitant administration of terfenadine or cisapride with macrolide antibiotics induces arrhythmia and prolongation of the QT interval.
In simultaneous administration of azithromycin and rifabutin development of neutropenia is possible in rare cases. Mechanism of development and causal relationship are not known.
In concomitant administration of azithromycin with zidovudine the former does not influence plasma pharmaco- kinetic parameters of the latter or renal elimination of zidovudine or of its metabolite glucuronide. However, con- centration of the active metabolite - phosphorylated zidovudine - in monocytes increases.
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea, abdominal pain, hepatic function disorder.
Treatment: gastric lavage, symptomatic therapy (administration of activated charcoal), control of vital functions.
Powder for oral suspension 200 mg/5 ml in a 60 ml polyethylene bottle with a polypropylene cap with a white colored induction foil.
1 bottle with a measuringsyringe, a measuringspoon, 15 ml water together with the enclosed leaflet in a carton box.
Store at temperature not exceeding 25°С. Keep out of reach of children!
Store reconstituted suspension not longer than 5 days.
3 years from the manufacturing date. Do not use after expiry date.
Sold under prescription.
AZITHROSAN is a product and a trade mark of "Sanolife", Great Britain.
“WORLD MEDICINE İLAÇ SAN. VE TİC. А.Ş.”, TURKEY