Zimax®

Azithromycin
Macrolide

COMPOSITION
Zimax® 500 Tablet : Each film coated tablet contains Azithromycin USP
500 mg as Azithromycin Dihydrate USP.
Zimax® Capsule : Each capsule contains Azithromycin USP 250 mg as
Azithromycin Dihydrate USP.
Zimax® Dry Powder for Suspension: When reconstituted, each 5 ml
suspension contains Azithromycin USP 200 mg as
Azithromycin Dihydrate USP.
PHARMACOLOGY
Zimax® (Azithromycin) is an azalide antibiotic, subclass of the macrolide
class of antibiotics.
Zimax® (Azithromycin) acts by binding to the 50S ribosomal subunit of
susceptible organisms and thus interferes with microbial protein synthesis.
Following oral administration in humans, Zimax® (Azithromycin) is rapidly
absorbed and widely distributed throughout the body ; bioavailability is
approximately 37%. The time taken to peak plasma levels is 2-3 hours.
However, kinetic studies have shown markedly higher Zimax®
(Azithromycin) levels in tissue than in plasma or serum indicating that the
drug is higher tissue bound, resulting in rapid distribution into tissues and
high concentration within cells. Concentrations in target tissues such as
lung, tonsil and prostate exceed the MIC90 for likely pathogens after a single
dose of 500 mg.
A large fraction of the absorbed dose of Zimax® (Azithromycin) remains
unmetabolised. There is some metabolism in the liver mainly by N-
demethylation, the metabolite being excreted in the bile.
The terminal elimination phase of Zimax® (Azithromycin) from the serum is
due to hepatic metabolism, biliary excretion and transintestinal passage. The
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half-life of this phase is approximately 40-60 hours. The major route of

elimination is biliary excretion of the unchanged compound. Transintestinal
excretion of the unchanged drug is also an important route of elimination.
Only a small amount of the dose is excreted unchanged in the urine.
Zimax® (Azithromycin) demonstrated activity in vitro, against a wide range
of Gram-positive and Gram-negative bacteria including: Staphylococcus
aureus, Streptococcus pneumoniae, Streptococcus pyogenes (Group A) and
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other Streptococcal species ; Haemophilus influenzae and parainfluenzae ;

Moraxella catarrhalis ; anaerobes including Bacteroides fragilis, Escherichia
coli, Bordetella pertussis, Bordetella parapertussis, Borrelia burgdorferi,
Haemophilus ducreyi, Neisseria gonorrhoeae and Chlamydia trachomatis.
Zimax® (Azithromycin) also demonstrates activity in vitro against Legionella
pneumophila, Mycoplasma pneumoniae and hominis; Campylobacter spp.,
Toxoplasma gondii and Treponema pallidum.
INDICATION
Zimax® (Azithromycin) is indicated for infections (caused by susceptible
organisms) in lower respiratory tract infections including bronchitis and
pneumonia, in upper respiratory tract infections including sinusitis and
pharyngitis/tonsillitis, in otitis media, and in skin and soft tissue infections.
In sexually transmitted diseases in men and women, Zimax® (Azithromycin)
is indicated in the treatment of non-gonococcal urethritis and cervicitis due
to Chlamydia trachomatis.
DOSAGE AND ADMINISTRATION
Zimax® capsule and suspension should be taken at least 1 hour before or 2
hour after meal. However, Zimax® 500 tablet can be taken with or without
food. To reconstitute Zimax® suspension, add 10 ml or 2 spoonfuls of just
boiled and cooled water to the content of the bottle and shake well to mix
uniformly.
Adults: For lower respiratory tract infections including bronchitis and
pneumonia, upper respiratory tract infections including sinusitis and
pharyngitis/tonsillitis, otitis media and skin and soft tissue infections, the
total dose of Zimax® is 1.5 gm given as 500 mg once daily for 3 days. An
alternative to this dosage schedule is that 500 mg once daily on day 1,
followed by 250 mg once daily for next 4 days.
For sexually transmitted diseases caused by Chlamydia trachomatis, the
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dose of Zimax® is 1 gm given as a single dose. Alternatively, 500 mg once

daily on day 1, followed by 250 mg once daily for next 2 days may also be
given.
Use in the elderly: Normal adult dosage is recommended. Children: The dose
of Zimax® in children over 6 months of age is 10 mg/kg body weight once
daily for 3 days. Alternatively, 10 mg/kg on day 1, followed by 5 mg/kg for
next 4 days is also recommended. There is no information on use of
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Azithromycin on children under 6 months of age. For children with body

weight 15-25 kg (3-7 years), the dose is 200 mg once daily for 3 days; for
body weight 26-35 kg (8-11 years), the dose is 300 mg once daily for 3 days;
for body weight 36-45 kg (12-14 years), the dose is 400 mg once daily for 3
days. For body weights over 45 kg, normal adult dosage is recommended.
CONTRAINDICATION AND PRECAUTION
Azithromycin is contra-indicated in patients with a known hypersensitivity to
azithromycin or any of the macrolide antibiotics. Because of the theoretical
possibility of ergotism, azithromycin and ergot derivatives should not be co-
administered. As the liver is the principal route of excretion of azithromycin
it should not be used in patients with hepatic disease.
Avoid concomitant administration with terfenadine or astemizole.
Precaution should be taken in patients with more severe renal impairment.
SIDE EFFECT
Zimax® (Azithromycin) is well tolerated with a low incidence of side-effects.
The side-effects include nausea, vomiting, abdominal discomfort
(pain/cramps), flatulence, diarrhoea, headache, dizziness, and skin rashes
and are reversible upon discontinuation of therapy.
Reversible elevations in liver transaminases have been observed
occasionally. Transient mild reductions in neutrophil counts have
occasionally been observed in clinical trials, although causal relationship to
azithromycin has not been established.
DRUG INTERACTION
Antacids: Peak serum levels but not the total extent of absorption are
reduced by aluminium - and magnesium - containing antacids in the
stomach. Azithromycin should therefore be taken at least 1 hour before or 2
hours after taking these antacids.
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Ergot Derivatives: Because of the theoretical possibility of ergotism,

concomitant administration of ergot derivatives and azithromycin should be
avoided.
Digoxin & Cyclosporin: Macrolides have been known to increase the plasma
concentration of Digoxin & Cyclosporin and so caution should be exercised
while co-administration is necessary.
Anti-Histamines: A potentially life threatening interaction between
erythromycin and terfenadine or astemizole have been reported. Although
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such an interaction with azithromycin is not established yet and undergoing

clinical study, so it is wise to avoid concomitant use of azithromycin and
terfenadine or astemizole.
There have been no pharmacokinetic drug interactions between
azithromycin and warfarin, theophylline, carbamazepine,
methylprednisolone and cimetidine.
In clinical trials, around 45% patients receiving azithromycin also received
other drugs concomitantly, e.g. bronchodilators, analgesics, corticosteroids,
diuretics, anxiolytics and antiarthritic drugs. No drug interaction problems
were encountered.
USE IN PREGNANCY AND LACTATION
Recent clinical studies have recommended that azithromycin should be
considered for the initial treatment of chlamydial cervicitis in pregnancy. In
other infections, azithromycin should be used only when clearly needed.
It is not known whether azithromycin is excreted in breast milk. Exercise
caution when administering to a nursing women.
OVERDOSAGE
There are no data on overdosage with azithromycin. Typical symptoms of
overdosage with macrolide antibiotics include hearing loss, severe nausea,
vomiting and diarrhoea. Gastric lavage and general supportive measures are
indicated.
STORAGE CONDITION
Zimax® capsules and dry powder for suspension should be stored at room
temperature (below 30˚C). Any unused portion of reconstituted Zimax®
suspension should be discarded after 5 days.
HOW SUPPLIED
Zimax® 500 tablet : Box containing 1 x 3 Zimax® film
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coated tablet in Alu-Alu blister pack.

Zimax® capsule : Box containing 1 x 6 Zimax® capsule
in Alu-Alu blister pack.
Zimax® Dry Powder for Suspension : Sealed cap bottle containing Zimax®
dry powder for reconstituting 15 ml
Zimax® Suspension.