Azomax (Azithromycin)

Azomax

(Azithromycin)

Antibiotic

Presentation:

Each film coated tablet contains: 

Azithromycin dihydrate U.S.P. equivalentto 500 mg of azithromycin.

Each capsule contains:

Azithromycin dihydrate U.S.P. equivalent to 250 mg of azithromycin.

Each 5ml oral suspension contains:

Azithromycin U.S.P. 200 mg as dihydrate

 

Properties:

Azithromycin is an azalide, derived from the macrolide class of antibiotics.

Azithromycin demonstrates activity in vitro,against a wide range of Gram-positive and Gram-negative bacteria including Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes (Group A) and other Streptococcal species; Haemophilus influenzae and para-influenzae; Moraxella catarrhalis; anaerobes including Bacteroids fragilis;

Escherichia coli; Bordetella pertussis; Bordetella parapertussis; Borrelia burgdorferi; Haemophilus ducreyi; Neisseria gonorrhoeae and Chlamydia trachomatis. Azithromycin also demonstrates in-vitro activity against Legionella pneumophila, Mycoplasma

pneumoniae and hominis, Campylobacter sp, Toxoplasma gondii and Treponema pallidum.

 

Pharmacokinetics:

Following oral administration in humans, azithromycin is widely distributed throughout the body; bioavailability is approximately 37%. The time taken to reach peak plasma levels is 2-3 hours. Plasma terminal elimination half-life closely reflects the tissue depletion half-life of 2to 4 days. Kinetic studies have shown markedly higher azithromycin levels in

tissue than in plasma (upto 50 times the maximum observed concentration in plasma) indicating that the drug is highly tissue bound. Concentrations in target tissue such as lungs, tonsils and prostate exceed the MIC90 for likely pathogens ofter a single dose of 500 mg.

 

Indications:

Azithromycin is indicated for infections caused by susceptible organisms; in lower respiratory tract infections including bronchitis and pneumonia, in upper respiratory tract infections including otitis media, pharyngitis/tonsillitis and sinusitis, skin and soft tissue infections and ačne, mild to moderate typhoid fever caused by multi-drug resistant strains.

In sexually transmitted diseases in men and women,

 

azithromycin is indicated in the treatment of uncomplicated genital infections due to Chlamydia trachomatis. Azithromycin is indicated as second line therapy for typhoid fever caused by s.typhi and s.paratyphi.

 

Dosage and administration:

Azithromycin should be administered as single dose, and as common with many other antibiotics, should be taken at legst 1 hour before or 2 hours after food.

 

Adults:

For  respiratory tract infections and skin and soft tissue infections the total dose is 1.5 a

which should be given as 500 mg as a single dose daily for 3 days. Alternatively an initial dose of 500 mg in the first day be followed by 250 mg daily for further may 4 days.

For sexually transmitted diseases caused by Chlamydia trachomatis the dose is 1g given

as a single dose. For typhoid fever, the dose is 500 mg to 1000 mg once doily for 5-7 days.

Use in children:

There is no information on children under

six months of age. The dose in children is

O mg/kg as a single daily dose for 3

days. For typhoid tever therapy should be

9iven tor 7 days

 

Contra-indications:

Azithromycin is contra-indicated in patients with a known hypersensitivity to azithromycin or any macrolide antibiotics.

Precautions and Warnings:

As with any antibiotic, observation for signs of superinfection with non susceptible

organisms, includingg recommended. As with erythromycin and other macrolides, serious allergic reactions, including angioneurotic oedema and anophylaxis, have been reported. Some of these reactions with azithromycin have resulted in recurrent symptoms and required a long period of observation and treatment.

Use in renal impairment:

No dosage adjustment is needed in patients with mild renal impairment (Creatinine

Clearance >40 ml/min.) but there are no data regarding azithromycin usage in patients with more severe renal impaiment, thus caution should be exercised in using azithromycin in these patients.

Use in hepatic impairment:

As liver is the principal route of excrefion of azithromycin, it should not be usedn patients with hepatic disease.

Use during pregnancy and lactation

Use in  pregnancy:

Animal reproduction studies have demonstrated that azithromycin crosses the placenta, but have revealed no evidence ot harm to the foetus. There are no adequate and wèll controlled studies in pregnant women. Since anima reproduction studies are not always predictive ot human response,  azithromycin should be used during pregnancy only adequate alternatives are not available.

Use in lactation:

No data on secretion of azithromycin in breast milk are available, so azithromycin should only be used in lactating women where adequate alternatives  re not available.

Drug interactions:

Antacids:

In patients receiving azithromycin and antacids, azithromycin should be taken at least 1 hour before or 2 hours after theantacid.

Carbamazepine:

In a pharmacokinetics interaction study in healthy volunteers, no signiticant effect

was observed on the plasma levels of carbamazepine or its active  metabolite.

Cyclosporin:

Some of the related macrolide antibiotics infertere with the metabolism ot cyclosporin. In the absence of pharmacokinetics studies or clinical data  investigating potential inferaction between azithromycin and cyclosporin, caution should be exercised before co-administration of these two drugs. It 

co-administration is necessary, cyclosporin levels should be monitored and the dose adjusted accordingly.

Digoxin:

No interactions have been reported in patients who have received concomitant azithromycin and cardiac glycosides. However, some ot the macrolide antibiotics have been reported to impair the metabolism of digoxin (in the gout) in some patients.

 

 

Theretore, in patients receiving concomitant azithromycin and digoxin the possibility of raised digoxin levels should be borne in mind. 

Ergot derivatives: 

Because of the theoretical possibility of ergotism, azithromycin and ergot derivatives should not be co-administered. 

Warfarin:

In a pharmacokinetics interaction study azithromycin did not alter the anticoagulant effect of a single 15 mg dose of wartarin administered in healthy volunteers. Azithromycin and wartarin may be co-administered, but monitoring of the prothrombin time should be continued as routinely performed.

Side-effects

:Azithromycin is well tolerated with a low incidence of side effects. Most side-effects oDserved were mild to moderate in severity. The majority of side-eftects were of gastrointestinal origin with naUsea, abdominal discomfort (pain/cramps),

vomiting, flatulence, diarrhoea and loose stools being occasionally observed.

Allergic reactions such as rashes have OCCured and there have also been rare reports of serious hypersensitivity reactions.  

Reversible elevations in liver transaminases have been seen with a frequency similar to the comparative macrolides and penicillins used in clinical trials. Transient mild reductions in neutrophil counts have OCcasionally been observed in clinical frials, although a casual relationship to azithromycin has not been  established.

Overdosage:

There are no data on overdosage with nt azithromycin. ofeTypical symptoms of overdosage with n macrolide antibiotics include hearing loss,severe nausea, vomiting and diarrhoea. Gastric lavage and general supportive

measures are indicated.

Storage condition:

Protect trom heat, light and moisture.

Warning:

All drugs should be kept out of the reach of children

Pack size:

Capsules

250 mg, 2x6's capsules in blister pack.

Tablets

500 mg, 2x3's tablets in blister pack.

Suspension

200 mg/5 ml Granules for 15ml oral Uspension.

200 mg/5 ml Granules for 25 ml oral Uspension.

 

For further information please contact: 

Novartis Pharma (Pakistan) Limited,

15, West Wharf, Karachi