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Comparison of efficacy of Azithromycin vs. Clindamycin and Erythromycin in the treatment of mild to moderate acne vulgaris

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Objective: Acne vulgaris is a prevalent inflammatory skin disorder. Topical solutions of clindamycin and erythromycin are the most common treatment in the patients. This study was conducted to compare the effect of topical solution azithromycin as a new method of treatment against topical solutions of clindamycin and erythromycin. Methodology: A randomized double-blind clinical trial was carried out for 20 weeks at the outpatient clinics of Boo-Ali Sina Hospital in Sari (Iran) on 96 patients with mild to moderate acne vulgaris. They were randomly divided in three groups who were matched together based on Acne Severity Index(ASI) and were treated with 2% alcoholic solution of azithromycin, erythromycin and clindamycin respectively twice daily for 16 weeks. Treatment efficacy was determined by Total acne Lesion Counting (TLC). Results: For each three treatment groups, decreased TLC and ASI were significant at the end of 16 weeks (P<0.05). Azithromycin was more effective than the clindamycin and erythromycin for acne therapy after 16 weeks (P<0.05). Twenty patients (20.8%) of azithromycin group (12.5%) reported to have adverse effects, such as erythema and/or pruritus (P<0.05). Conclusion: Topical solution azithromycin is a more effective treatment for mild to moderate acne vulgaris comparing to clindamycin and erythromycin, but it has more local side effects.
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68 Pak J Med Sci 2011 Vol. 27 No. 1 www.pjms.com.pk
Original Article
Comparison of efficacy of Azithromycin vs. Clindamycin and
Erythromycin in the treatment of mild to moderate acne vulgaris
Zohre Hajheydari1, Mitra Mahmoudi2, Korosh Vahidshahi3, Arezoo Nozari4
ABSTRACT
Objective: Acne vulgaris is a prevalent inflammatory skin disorder. Topical solutions of
clindamycin and erythromycin are the most common treatment in the patients. This study was
conducted to compare the effect of topical solution azithromycin as a new method of
treatment against topical solutions of clindamycin and erythromycin.
Methodology: A randomized double-blind clinical trial was carried out for 20 weeks at the
outpatient clinics of Boo-Ali Sina Hospital in Sari (Iran) on 96 patients with mild to moderate
acne vulgaris. They were randomly divided in three groups who were matched together based
on Acne Severity Index(ASI) and were treated with 2% alcoholic solution of azithromycin,
erythromycin and clindamycin respectively twice daily for 16 weeks. Treatment efficacy was
determined by Total acne Lesion Counting (TLC).
Results: For each three treatment groups, decreased TLC and ASI were significant at the end of
16 weeks (P<0.05). Azithromycin was more effective than the clindamycin and erythromycin
for acne therapy after 16 weeks (P<0.05). Twenty patients (20.8%) of azithromycin group (12.5%)
reported to have adverse effects, such as erythema and/or pruritus (P<0.05).
Conclusion: Topical solution azithromycin is a more effective treatment for mild to moderate
acne vulgaris comparing to clindamycin and erythromycin, but it has more local side effects.
KEY WORDS: Acne vulgaris, Azithromycin, Clindamycin, Erythromycin, Treatment.
Pak J Med Sci January - March 2011 Vol. 27 No. 1 68-72
How to cite this article:
Hajheydari Z, Mahmoudi M, Vahidshahi K, Nozari A. Comparison of efficacy of Azithromycin vs.
Clindamycin and Erythromycin in the treatment of mild to moderate acne vulgaris. Pak J Med
Sci 2011;27(1):68-72
1. Zohre, Hajheydari, MD,
Dept. of Dermatology & Venorology, Boo-Ali Sina Hospital.
2. Mitra, Mahmoudi, PhD,
Department of Pharmacology, School of Medicine.
3. Korosh, Vahidshahi, MD,
School of Medicine.
4. Arezoo, Nozari, MD ,
Boo-Ali Sina Hospital.
1-4: Mazandaran University of Medical Sciences, Sari, Iran.
Correspondence:
Mitra Mahmoudi,
Dept. of Pharmacology, School of Medicine,
Mazandaran University of Medical Sciences,
18th Km of Khazar Road, Sari, Iran.
E-mail: mtmhmit@yahoo.com
* Received for Publication: May 19, 2010
* Accepted: September 25, 2010
INTRODUCTION
Acne, an inflammatory skin disorder, is one of the
most common skin diseases treated by dermatolo-
gists.1,2 Early treatment of acne is necessary to
prevent facial scarring and consequently avoiding
psychological distress.3 Topical antibiotics are com-
monly prescribed to treat mild to moderate acne for
the thirty years. The two most commonly used topi-
cal antibiotics are clindamycin and erythromycin that
reduce the levels of Propionibacterium acnes (P.
acnes) and decrease inflammation.2,4-6 Some antimi-
crobial agents such as Benzoyl peroxide have no anti
inflammatory effect but used to treat mild to moder-
ate acne, specially in combination therapy with eryth-
romycin or Clindamycin to minimize the develop-
ment of resistance. However, because of the emer-
gent of antibiotic-resistant strains, these antibiotics
are becoming less effective.7
Azithromycin is a newer macrolide with widely
tissue distribution and cellular concentration.8
Azithromycin shows activity against gram-positive,
Gram-negative aerobic bacteria and anaerobic
Pak J Med Sci 2011 Vol. 27 No. 1 www.pjms.com.pk 69
Comparison of efficacy of azithromycin
sepsis, including propionibacterium (P. acnes) with
minimal side effects and better compliance.9,10 But
there isn’t any study about topical solution of
azithromycin for treatment of acne.8 So we conducted
this study to compare the efficacy and safety of topi-
cal Alcoholic Solution Azithromycin (ASA) versus
Alcoholic Solution Erythromycin (ASE) and Alco-
holic Solution Clindamycin (ASC) in the treatment
of mild to moderate acne vulgaris.
METHODOLOGY
Study design: This was a randomized double–blind
clinical trial of three groups comparison, using alco-
holic solution 2% of erythromycin(ASE),
clindamycin(ASC) and azithromycin(ASA). Ninety-
six patients with mild to moderate acne were selected
among patients referred to clinic of dermatology at
Boo-Ali Sina Hospital in Sari (Iran).This study was
approved by the appropriate regulatory and ethics
committees in Mazandaran University of Medical
Science.
Patients: Male and female patients aged 12-28 years
with mild to moderate acne vulgaris of the face were
eligible. Patients who were using any kind of acne
treatment in the previous month were excluded. Sub-
jects using drugs induced acne and female with poly-
cystic ovarian syndrome were excluded. The patients
were randomized to each treatment in equal num-
bers. The patients applied the medication twice daily.
The patients were assessed at (day 1) and the end of
2, 4, 8, 12, 16 and 20 weeks after the beginning of
study. To maintain blinding, a pharmacist was
responsible for dispensing study medication and for
instructing the patient on the proper method of
application. The scheduled treatment period was 16
weeks and patients were followed at the end of 20
weeks after the beginning of treatment.
Study treatment: Patients in azithromycin group
received alcoholic solution 2% azithromycin (in 60%
ethanol/40% water solution) as the method of Mc
Hugh et al.8 and the other groups received commer-
cial preparation of 2% erythromycin or clindamycin
alcoholic solutions obtained from Pakdarou pharma-
ceutical company in Iran.
Assessment: Treatment efficacy was determined by
total lesion counts of the whole face. In each visit,
the physician assessed global change from baseline
as follow: a reduction of 80% or more was labeled
good, 50-79% moderate, 20-49% mild, and a reduc-
tion less than 20% labeled poor. Adverse events were
recorded throughout the study upon the complain
of patients. All assessors were blinded to the treat-
ment received. To optimize consistency of subjective
evaluations, the same staff saw the same patients at
each of their visits.
Statistical analysis: Data were analyzed by SPSS
software, using ANOVA, Tukey and the other
useful statistical methods with P<0.05.
RESULTS
In total, 96 patients (32 patients in each group) were
randomly selected to treat and were assessed in
March 2006 to December 2007. There were no sig-
nificant differences between the groups in demo-
graphic characteristics and basal non-inflammatory
and inflammatory lesion counts (Tables-I, II).
The results from this study show improvement in
both the non inflammatory and inflammatory lesions
of acne over 16 weeks of treatment period with the
three kinds of topical antibiotics. A significant dif-
ference in total count of non-inflammatory lesion and
total lesion count between three treatment groups is
shown in Figs.1 and 2 and Table-II. In the first four
weeks of treatment the best response was observed
from ASE and from week four onwards the best
therapeutic response was observed from AEA. The
least effect was observed from ASC.
In our study 20.8% of all patients complained of
erythema, pruritus, burning and edema which was
more in azithromycin group (12.5%, P<0.05)
(Table-III).
DISCUSSION
The results from this study show improvement in
both the non inflammatory and inflammatory lesions
of acne over 16 weeks of treatment period with the
three kinds of topical antibiotics. Oral and topical
antibiotics are the most commonly used for acne
lesions. The mechanisms by which antibiotics work
Table-I: Demographic Characteristics.
Azit Eryth clinda P-value
-Sex
Male 4(12.5%) 4(12.5%) 4(12.5%) NS
Female 28(87.5%) 28(87.5%) 28(87.5%)
-Age(years)
Mean± SD 18.9±2.9 19.3±2.9 20.4±4.3 NS
Range 15-26 16-25 12-28
-Family history
Positive 21(65.5%) 17(53.1%) 18(56.3%) NS
Negative 11(34.5%) 15(46.9%) 14(43.7%)
-BMI
Mean±SD 22.3±3.7 23.1±5.4 22.7±4.4 NS
Range 18.6-31.0 16-38 13-30
Azit: Azitromycin Eryth: Erythromycin, Clinda: Clindamycin
BMI: Body Mass Index, NS: Non Significant
70 Pak J Med Sci 2011 Vol. 27 No. 1 www.pjms.com.pk
Zohre, Hajheydari et al.
in acne, varies with the drug. Some medications may
have anti inflammatory or antibacterial properties,
whereas other medications possess both proper-
ties.8,11,12 The useful affect of 2% Alcoholic solution
of the most common antibiotics such as Erythromy-
cin and Clindamycin have showed in various
studies.5,6,8,11
Oral and topical erythromycin and clindamycin
have significant effect in patients with
papulopostular acne that comparable with placebo
and vehicle.13-15
Two randomized double blind clinical trial showed
that the efficacy of erythromycin and clindamycin
are the same for treatment of acne.16,17 Clinical
isolated of P.acnes are known to be highly suscep-
tible to azithromycin.2,18
Our study showed the significant effect of all
topical medications on inflammatory lesion of acne
but the efficacy of erythromycin for the treatment of
comedon in the first few weeks was better but from
week four onwards azithromycin showed more sig-
nificant effect on comedon than the other drugs.
Table-II: Absolute Lesion Count.
Azit N=32 Eryth N=32 Clinda N=32 One way ANOVA Tukey test
Mean(SD) Mean(SD) Mean(SD) A-E-CP-Value
A vs E A vs C E vs C
P-Value P-Value P-Value
Total number of inflammatory lesions
Week 0 47.9 (56.1) 65.7 (47.1) 54.7 (34.3) NS NS NS NS
Week 2 21.7 (23.7) 23.2 (13.7) 29.1 (24.9) NS NS NS NS
Week 4 15.7 (16.5) 18.2 (12.3) 20.1 (20.2) NS NS NS NS
Week 8 10.3 (9.1) 13.0 (8.5) 16.4 (16.8) NS NS NS NS
Week 12 7.1 (7.8) 9.8 (7.8) 12.1 (13.2) NS NS NS NS
Week 16 5.3 (8.3) 12.0 (12.6) 13.0 (12.2) NS NS NS NS
Follow up 5.5 (9.0) 12.8 (16.7) 12.7 (9.9) NS NS NS NS
20 Weeks
Total number of non-inflammatory lesions
Week 0 148.9 (57.6) 142.7 (50.2) 11.3 (45.9) NS NS NS NS
Week 2 113.3 (45.9) 101.3 (31.3) 117.9 (34.9) NS NS NS 0.044
Week 4 83.6 (43.7) 79.0 (25.9) 98.4 (39.5) 0.011 NS NS 0.009
Week 8 62.3 (30.1) 71.3 (22.0) 84.2 (38.4) 0.005 NS 0.008 0.022
Week 12 47.2 (24.9) 57.1 (21.4) 71.2 (33.9) 0.015 NS 0.012 NS
Week 16 38.2 (24.7) 54.8 (26.3) 70.0 (41.1) 0.014 NS 0.010 NS
Follow up 33.6 (26.7) 52.3 (28.9) 72.6 (38.9) 0.000 NS 0.000 0.005
20 Weeks
Total number of lesions
Week 0 146.8 (96.9) 268.5 (39.4) 215.0 (49.2) NS NS NS NS
Week 2 135.0 (54.1) 124.6 (38.1) 147.0 (55.5) NS NS NS 0.047
Week 4 99.3 (51.6) 97.2 (33.0) 118.6 (51.5) 0.017 NS NS 0.015
Week 8 72.7 (32.1) 84.3 (25.3) 100.6 (40.6) 0.005 NS 0.008 0.023
Week 12 54.3 (27.2) 67.0 (24.3) 83.4 (43.3) 0.013 NS 0.010 NS
Week 16 43.6 (27.3) 66.9 (36.1) 83.0 (50.1) 0.013 NS 0.009 NS
Follow up 39.2 (31.0) 65.2 (43.6) 85.3 (44.4) 0.000 NS 0.000 0.014
20 Weeks
NS: Non Significant Azit: Azithromycin Eryth: Erythromycin Clinda: Clindamycin
Table-III: Side effects detected during treatment.
Drug Azithromycin Erythromycin Clindamycin Total
Side effects N=32 N=32 N=32 N=96
Itch 10(31.3%) 1(3.1%) 2(6.3%) 13(13.5%)
(P=0.002)
Erythema 10(31.3%) 1(3.1%) 4(12.5%) 15(15.6%)
(P=0.007)
Burning 7(21.9%) 2(6.3%) 1(3.1%) 10(10.4%)
(P= 0.031)
Edema 5(15.6%) 0(0%) 0(0%) 5(5.2%)
(P=0.005)
Pak J Med Sci 2011 Vol. 27 No. 1 www.pjms.com.pk 71
Comparison of efficacy of azithromycin
Azithromycin is a newer macrolide that was
developed to overcome the shortcomings of eryth-
romycin, such as gastrointestinal intolerance and
short half life.19 Recently azithromycin was found to
be effective in the treatment of inflammatory
acne.10,15,20 The anti inflammatory action of macrolides
has been shown in various studies. The results of
some studies indicate that macrolides affect several
Fig-1a:
Fig-1b:
Fig-1c:
Fig-1: The median percentage reduction.
In lesion counts from baseline.
1a: Inflammatory lesion count,
1b: Non Inflammatory lesion count,
1c: Total lesion count.
Differences between groups were tested using the
Wilcoxon test.
Fig-2a:
Fig-2b:
Fig-2c:
Fig-2: The percentage of patients with a 30%
improvement or greater from baseline.
2a: Inflammatory lesions,
2b: non-Inflammatory lesions,
2c: Total lesions.
*Statistically significant difference after Bonferroni
correction (Fisher exact test).
inflammatory processes such as migration of
neutrophils, the oxidative burst in phagocytes and
production of pro-inflammatory cytokines.21-23
Azithromycin is a new macrolide which has a unique
and superior pharmacokinetic profile when com-
pared with other macrolides. It penetrates tissues
rapidly, where it remains for prolonged periods and
allow less frequent dosage. Steady-state tissue
levels are substantially increased in relationship to
serum levels. Azithromycine has also no major drug
interactions.8,10,19 Kus et al showed oral azithromycin
decrease the non inflammatory acne lesions as well
72 Pak J Med Sci 2011 Vol. 27 No. 1 www.pjms.com.pk
Zohre, Hajheydari et al.
as the inflammatory lesions which are comparable
to our results, and azithromycin is at least as
effective and safe as doxycycline in acne treatment
and is a good alternative for those patients who
cannot tolerate the side effects of tetracyclines.24,25
In our study 20.8% of all patients complained of
erythema, pruritus, burning and edema which was
more in azithromycin group (12.5%, P<0.05).
Tetracyclines are the first-line antiacne
antibiotics.9,26 However tetracyclines may be associ-
ated with a fairly large number of adverse effects.
Comparative clinical trials have shown that
azithromycin’s tolerability profile is superior to con-
ventional antiacne treatment such as erythromycin
and doxycycline.10,15,24 But the concern in use of oral
antibiotics is the potential transfer of antibiotic
resistance to other organisms.7
In order to diminish the risk of resistance emerg-
ing, oral antibiotics should not be used in mild acne
where topical agents may sufficient.27 Topical
azithromycin is a promising agent in the treatment
of acne and has durable effect, but upon our study’s
results, topical azithromycin has local side effects and
further controlled studies comparing the effective-
ness and tolerability of topical azithromycin with
conventional antibiotics are suggested.
ACKNOWLEDGMENTS
This research was supported by a grant from the
vice chancellor for research, Mazandaran University
of Medical Sciences, Sari, Iran.
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Rosacea is a common chronic, and sometimes progressive, dermatosis. It is characterized, alone or in combination, by central facial erythema,symmetric flushing, stinging sensation, inflammatory lesions (papules and pustules), telangiectasias, and phymatous changes (tissue hyperplasia and nodules). Rosacea can occur in adults of any ethnicity,and adversely affects patients' quality of life. The condition can be effectively controlled with therapy tailored to the specific subtype of rosacea that is affecting the patient. Topical metronidazole, sulfacetamide/sulfur, and azelaic acid are generally effective for patients with mild rosacea. For moderate papulopustular rosacea, combination therapy with oral tetracyclines and topical agents is the first-line choice. Treatment with a topical agent, such as metronidazole, may help maintain remission. Patients with ocular involvement may benefit from long-term oral antibiotics and metronidazole gel. Referral to a subspecialist is necessary for patients who have ocular rosacea with ophthalmic complications, severe or recalcitrant rosacea, or phymatous changes.
Article
Synopsis Azithromycin is an acid stable orally administered macrolide antimicrobial drug, structurally related to erythromycin, with a similar spectrum of antimicrobial activity. Azithromycin is marginally less active than erythromycin in vitro against Gram-positive organisms, although this is of doubtful clinical significance as susceptibility concentrations fall within the range of achievable tissue azithromycin concentrations. In contrast, azithromycin appears to be more active than erythromycin against many Gram-negative pathogens and several other pathogens, notably Haemophilus influenzae, H. parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Ureaplasma urealyticum and Borrelia burgdorferi. Like erythromycin and other macrolides, the activity of azithromycin is unaffected by the production of β-lactamase. However, erythromycin-resistant organisms are also resistant to azithromycin. Following oral administration, serum concentrations of azithromycin are lower than those of erythromycin, but this reflects the rapid and extensive movement of the drug from the circulation into intracellular compartments resulting in tissue concentrations exceeding those commonly seen with erythromycin. Azithromycin is subsequently slowly released, reflecting its long terminal phase elimination half-life relative to that of erythromycin. These factors allow for a single dose or single daily dose regimen in most infections, with the potential for increased compliance among outpatients where a more frequent antimicrobial regimen might traditionally be indicated. The potential disadvantage of low azithromycin serum concentrations, however, is that breakthrough bacteraemia may occur in patients who are severely ill; nevertheless, animal studies suggest that tissue concentrations of azithromycin are more important than those in serum when treating respiratory and other infections. The clinical efficacy of azithromycin has been confirmed in the treatment of infections of the lower and upper respiratory tracts (the latter including paediatric patients), skin and soft tissues (again including paediatric patients), in uncomplicated urethritis/cervicitis associated with N. gonorrhoeae, Chlamydia trachomatis or U. urealyticum and in the treatment of early Lyme disease. Azithromycin was as effective as erythromycin and other commonly used drugs including clarithromycin, β-lactams (penicillins and cephalosporins), and quinolone and tetracycline antibiotics in some of the above infections. Some patients with acute exacerbations of chronic bronchitis due to H. influenzae may be refractory to therapy with azithromycin (as is the case with erythromycin) indicating the need for physician vigilance, although it should be noted that azithromycin is of equivalent efficacy to amoxicillin in the treatment of such patients. In the therapy of urethritis/cervicitis associated with C. trachomatis, N. gonorrhoea or U. urealyticum, a single dose azithromycin regimen offers a distinct advantage over currently available pharmacological options, while providing effective therapy. Furthermore, it is likely that azithromycin may supersede erythromycin in the treatment of early Lyme disease and become an alternative to therapy with penicillin or tetracycline antibiotics in this condition. Similarly, if the finding of clinical efficacy of azithromycin in a preliminary study of chancroid is sustained in further clinical trials, then the use of azithromycin might supplant the traditional use of a more frequent erythromycin regimen in this condition. Small initial trials have shown azithromycin to be effective at least in the amelioration of Mycobacterium avium infection in AIDS patients. Comparative clinical trials have shown azithromycin to be better tolerated than erythromycin, principally through fewer gastrointestinal disturbances. Such studies have also shown the tolerability profile of azithromycin to be superior to that of cefaclor, doxycycline or amoxicillin plus probenecid. In conclusion, with its broad spectrum of antimicrobial activity, proven efficacy in a wide range of community-acquired infections, improved tissue pharmacokinetic and tolerability profiles, and suitability for once daily dosing, azithromycin provides a useful alternative to erythromycin and other macrolides with similar activity. In patients with uncomplicated urethritis or cervicitis associated with C. trachomatis, N. gonorrhoeae or U. urealyticum, azithromycin as a single dose regimen offers distinct advantages over current pharmacological options and should therefore be considered as a first-line therapy. Antimicrobial Activity Azithromycin has a spectrum of in vitro activity similar to that of erythromycin, although differences in activity have been recorded for particular organisms. Azithromycin was active against isolates of Staphylococcus aureus, including β-lactamase producing strains, although less so than clarithromycin and roxithromycin. Azithromycin was also active against some S. epidermidis isolates and other coagulase-negative staphylococci; however, staphylococcal resistance to macrolides was often encountered, and azithromycin was also inactive in these instances. Azithromycin was active against streptococci Groups A,B,C,F,G, other oral streptococci and Streptococcus bovis included among other strains tested together. However, Group A streptococci that were resistant to erythromycin were also resistant to azithromycin. Azithromycin was inactive against Enterococci (group D streptococci). Although S. viridans was resistant overall to azithromycin in the analysis, both susceptibility and resistance were reported in the individual studies analysed. S. pneumoniae strains susceptible to erythromycin and those not selected for antimicrobial sensitivity or resistance were susceptible to azithromycin although more so to the other macrolides tested. S. pneumoniae erythromycin-resistant strains were also resistant to azithromycin. Isolates of Listeria monocytogenes were moderately susceptible to azithromycin but were more susceptible to erythromycin, clarithromycin or roxithromycin. Corynebacterium species were generally resistant to azithromycin. Azithromycin was active against Bordetella pertussis (particularly) and B. parapertussis and was marginally more active than other macrolides tested against the latter organism. Clinical isolates of Campylobacter jejuni were more susceptible to azithromycin than to erythromycin, roxithromycin or clarithromycin. Helicobacter pylori isolates were also susceptible to azithromycin and similarly susceptible to erythromycin and roxithromycin although more so to clarithromycin. Azithromycin was more active against this organism than rifampin, metronidazole and a selection of quinolone antimicrobials. Azithromycin showed greater activity than other macrolides against isolates of Haemophilus influenzae and H. parainfluenzae, including β-lactamase producing strains, although the microbiologically active 14-hydroxy metabolite of clarithromycin showed similar activity to azithromycin against H. influenzae. Azithromycin was particularly active against H. ducreyi; the susceptibility of this organism to azithromycin was not affected by β-lactamase production or tetracycline resistance. Moraxella catarrhalis strains, including those producing β-lactamase, were susceptible to azithromycin and most other macrolides, although less so to erythromycin, roxithromycin or clindamycin. Azithromycin was also more active than benzyl penicillin against M. catarrhalis, even when isolates producing β-lactamase were excluded from the analysis. Azithromycin was active against Neisseria gonorrhoeae (including β-lactamase producing strains) and N. meningitidis and was more active than erythromycin against these pathogens. Legionella species were susceptible to azithromycin, although these organisms were more susceptible to erythromycin and other macrolides. Azithromycin was particularly active against Gardnerella vaginalis and Mobiluncus species and was also active against Actinobacillus actinomycetemcomitans and Bruceila melitensis. Pooled results of in vitro tests against Bacteroides species showed overall resistance to azithromycin; however, when species were tested individually, either susceptibility or resistance were recorded. Clostridium species were moderately susceptible to azithromycin overall, although in the majority of individual studies these isolates were susceptible. Azithromycin was active against C. perfringens and active or moderately active against C. difficile. Azithromycin was highly active against Propionibacterium acnes, although only moderate activity was recorded against anaerobic Gram-positive cocci (including Peptococcus and Peptostreptococcus species). Azithromycin was active against the commonly isolated urogenital pathogens C. trachomatis and U. urealyticum, and was also active against the atypical respiratory pathogens C. pneumoniae and Mycoplasma pneumoniae. M. hominis isolates were either moderately susceptible or resistant to azithromycin, although consistently resistant to erythromycin. Mycobacterium avium complex isolates were resistant to azithromycin, but the replication rate of this organism was slowed by azithromycin in cultured macrophages. Isolates of Borrelia burgdorferi were notably more susceptible to azithromycin than to either benzyl penicillin or tetracycline. Treponema pallidum protein synthesis was inhibited by azithromycin, however, the effective concentration range exceeded clinically relevant concentrations. Like metronidazole, azithromycin inhibited the growth of Entamoeba histolytica, although unlike metronidazole, azithromycin showed considerable variation in activity against Giardia duodenalis. Azithromycin had only a minimal effect on the growth of G. lamblia. Azithromycin appears to be parasitostatic against Toxoplasma gondii. In general, bacterial strains resistant to erythromycin are also resistant to azithromycin, although bacterial strains resistant to penicillins are susceptible to azithromycin where macrolide resistance is absent. Therefore, the resistance mechanism involving the production of β-lactamase alone does not appear to influence susceptibility to azithromycin. Azithromycin is bactericidal against a variety of organisms including S. aureus, S. epidermidis, S. pneumoniae, H. influenzae, Klebsiella pneumoniae, Bordetella species, L. pneumophila, M. catarrhalis, C. trachomatis, C. pneumoniae, M. avium complex and B. burgdorferi. A postantibiotic effect of 1.7 to 3.9 hours was recorded for azithromycin against S. pyogenes, S. pneumoniae, H. influenzae, M. catarrhalis, K. oxytoca, and K. pneumoniae. Azithromycin produces its antibacterial effect by inhibition of protein synthesis. Azithromycin has demonstrated antimicrobial activity in experimental models of infection induced by a variety of Gram-positive and Gram-negative organisms (including Staphylococci, Streptococci, H. influenzae, L. pneumophila) and other organisms including T. gondii, T. pallidum, B. burgdorferi, C. trachomatis and M. avium complex. Pharmacokinetic Properties Azithromycin is considerably more stable than erythromycin at low pH. Following oral administration to healthy volunteers, the bioavailability of azithromycin was estimated as 37%. The pharmacokinetic profile of azithromycin appears to be characterised by rapid and extensive uptake from the circulation into intracellular compartments followed by slow release. This may explain the low peak plasma concentration (Cmax) of about 0.4 mg/L attained within approximately 2.5 hours of a 500mg oral dose, relative to those achieved following administration of other commercially available macrolide drugs at therapeutic doses. Similarly, area under the plasma concentration-time curve (AUC) was 2- to 39-fold lower for azithromycin than for other macrolides. In multiple dose studies, azithromycin 500mg twice daily on day 1 followed by 500 mg/ day for a further 4 days resulted in mean AUC values rising from 1.77 mg/L · h on day 1 to 3.18 mg/L· h on day 5, and mean Cmax increased from 0.41 to 0.62 mg/L over the same period. A similar trend was seen with administration of azithromycin 250mg twice daily on day 1 followed by 250 mg/day for a further 8 days. Azithromycin appears to be widely distributed throughout the body, generally achieving higher concentrations in tissues, organs, tissue fluids and a variety of cell types including phagocytes, than in blood. Indeed, the reported values for volume of distribution have been large — 23 to 31 L/kg. Binding of azithromycin to human plasma proteins was 50% at a concentration of 0.02 to 0.05 mg/L, reducing to 7% at 1 mg/L. The degree of binding of azithromycin is much lower than that of erythromycin (72% at 0.4 mg/L) or roxithromycin (96% at 2.5 mg/L), suggesting the capacity for higher concentrations of free azithromycin to be available for distribution to infection sites. Available pharmacokinetic data suggest that azithromycin is mainly excreted unchanged, principally in the faeces and to a lesser extent in the urine. Transintestinal excretion may be the primary elimination mechanism for the unchanged compound. The elimination of azithromycin from serum follows a polyphasic pattern, with values for terminal phase elimination half-life ranging from 10 to 57 hours depending on the dose regimen and sampling interval. The pharmacokinetic profile of azithromycin is not altered significantly in elderly patients with mild renal impairment, nor in patients with mild to moderate hepatic impairment. Pharmacokinetic data are not available for paediatric patients, or for patients with more severe renal or hepatic dysfunction. Therapeutic Efficacy Azithromycin is effective in the treatment of several types of infection when administered as a 1.5g total dose over 3 or 5 days to adults and as a 30 mg/kg total dose over 3 or 5 days to children. In the treatment of urogenital and sexually transmitted infections, a single 1g dose appears to be as effective as a 3-day regimen (500mg on day 1 then 250 mg/day for an additional 2 days), while AIDS patients with M. avium complex infection have benefited from an azithromycin regimen of 500 mg/day for 10 to 30 days. In comparative (mostly nonblind) studies of patients with lower respiratory tract infections, treatment with azithromycin was associated with clinical cure rates of 36 to 80%, clinical success (cure plus improvement) rates of 92 to 100% and bacteriological eradication rates of 52 to 93%. In these investigations, the clinical efficacy of azithromycin was judged to be equivalent to that of erythromycin, josamycin, amoxicillin (with or without clavulanic acid) or cefaclor. In 2 non-comparative studies of patients with lower respiratory tract infections clinical cure and/or bacteriological eradication rates were high; 95 and 91%, respectively. However, in the treatment of patients with acute purulent exacerbations of chronic bronchitis the cure rate declined from 55% at the end of treatment to 33% 1 month after initiation of therapy, reflecting the incidence of reinfection. Furthermore, the development of H. influenzae resistance to azithromycin appeared to be a major factor in the failure of this antibiotic. Azithromycin, however, was at least as effective as amoxicillin in the treatment of patients with (mainly severe) acute exacerbations of chronic bronchitis when assessed 12 days after initiation of therapy (clinical cure and success rates; 64 and 96% vs 52 and 80%, and bacteriological eradication rates; 52 vs 40%, respectively). Furthermore, in this study, eradication rates for Haemophilus spp. were similar for the 2 antimicrobials. Upper respiratory tract infections (including those of the middle ear) also responded to therapy with azithromycin. In comparative (mostly nonblind) studies that recruited adults, azithromycin therapy resulted in clinical cure and success rates of 66 to 81% and 93 to 100% in patients with acute maxillary sinusitis, 76 to 87% and 96 to 99% of patients with acute streptococcal pharyngitis and/or tonsillitis, and 79 and 97% of patients with acute otitis media. In paediatric patients with acute otitis media azithromycin was clinically curative for 78 to 95% and clinically successful for 93 to 99% of children. Azithromycin was also effective in the treatment of paediatric pharyngitis and/or tonsillitis with clinical cure rates of 86 to 93% and clinical success rates of 95 to 98%. Bacteriological eradication rates in adults ranged from 87 to 100%, while in children with bacterial pharyngitis, eradication rates ranged from 91 to 95%. Therapy with azithromycin in adults and/or children was considered equivalent to a standard regimen of amoxicillin or clarithromycin in patients with acute sinusitis, phenoxymethyl penicillin, erythromycin or clarithromycin in patients with bacterial pharyngitis and/or tonsillitis, erythromycin in patients with acute sinusitis and other upper respiratory tract infections and clarithromycin in patients with acute otitis media. Azithromycin has also shown clinical efficacy in the treatment of urogenital and other sexually transmitted infections. In comparative studies, the clinical cure and rates for azithromycin in patients with urethritis and/or cervicitis associated with C. trachomatis, N. gonorrhoeae or U. urealyticum ranged from 56 to 100% when assessed within 28 days of initiating therapy, although in most studies clinical cure was noted for more than 90% of patients. Bacteriological eradication rates were either comparable with, or exceeded, clinical cure rates, and almost invariably surpassed 90%. In these comparative studies, azithromycin 1g was equally effective whether administered in a single or dose or as a 3-day regimen. Furthermore, azithromycin was at least as effective as doxycycline and tended to show superior efficacy to ciprofloxacin when these drugs were given in standard 7-day regimens. In the treatment of adults with skin and soft tissue infections, therapy with azithromycin was associated with clinical cure rates of 53 to 83%, clinical success rates of 86 to 99%, and bacteriological eradication rates of 60 to 99%. Treatment with azithromycin was considered to be as effective as a standard regimen of cloxacillin, cephalexin or erythromycin. In the treatment of early Lyme disease azithromycin was considered to be at least as effective as phenoxymethyl penicillin, doxycycline or amoxicillin plus probenecid. A preliminary study of AIDS patients with M. avium infection has revealed azithromycin 500mg to be effective in reducing mycobacteraemia and the clinical symptoms of this infection when administered over a 10- to 30-day period. Tolerability In comparative studies involving a total of 3995 patients who were treated with azithromycin 1.5g in divided doses over 5 days, the overall adverse effect rate was 12%; this decreased to 9.3% in patients aged ⩾ 65 years and 5.4% in patients aged ⩽ 14 years. The overall incidence of adverse effects was comparable to, or lower than, that reported for other antibacterial agents studied. The most common adverse effects were gastrointestinal (9.6%), followed by central and peripheral nervous system effects (1.3%). Most adverse effects were mild or moderate, with only 6% rated as severe (predominantly gastrointestinal disturbances, dizziness, headache, fatigue and cutaneous events). Treatment was discontinued in 0.7% of patients because of adverse events; this compares with 1.3 to 15.2% for most of the comparator drugs studied. Fewer discontinuations were noted during the first 5 days of therapy in azithromycin recipients compared with the majority of other antibacterial drugs. Dosage and Administration The recommended adult oral dosage regimen for azithromycin in the treatment of infections, excluding those transmitted sexually, is 500mg once daily for 3 days or 500mg as a single dose on day 1 followed by 250mg once daily for a further 4 days. Both dosage regimens have been shown to provide target tissue concentrations of azithromycin above the MIC values for key pathogens during and for 5 to 10 days following therapy. Chlamydial urethritis or cervicitis may be treated with a single oral dose of 1g; this dose also appears effective in the treatment of chancroid and uncomplicated gonorrhoea. In paediatric patients, an oral dosage regimen of 10 mg/kg on the first day and 5 mg/kg for a further 4 days is recommended. However, children weighing more than 45kg should receive the adult dosage. In the treatment of Lyme disease, a standard 5-day azithromycin regimen or azithromycin 250mg twice daily for 2 days followed by 250mg daily for 8 days has proven effective. Preliminary studies indicate that azithromycin 500mg daily for 10 to 30 days has a beneficial effect in the treatment of M. avium complex infection in patients with AIDS. Studies have indicated that dosage adjustment is not necessary in elderly patients with mild renal impairment or in patients with mild to moderate hepatic dysfunction; however, the manufacturer recommends that azithromycin be used with caution in patients with creatinine clearance rates <2.4 L/h, and patients with hepatic disease should not be administered the drug. Azithromycin is contraindicated in patients with known macrolide hypersensitivity and in those receiving ergot alkaloids; serum concentrations of cyclosporin or digoxin should be monitored when coadministered with azithromycin. Azithromycin should be given at least 1 hour before or 2 hours after food or antacids.
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Background: Acne affects a large number of young adults, including women, who often present with facial as well as truncal involvement. Systemic antimicrobial agents currently used for the reduction of inflammatory papules and cysts require frequent administration and are sometimes associated with uncomfortable side-effects contributing to a decrease in compliance. Methods: Ninety-nine episodes of inflammatory acne in 79 patients treated with oral antimicrobial agents were studied retrospectively over a period of 46 weeks. Patients were treated with tetracycline, erythromycin, minocycline, and doxycycline, the most commonly prescribed oral antimicrobials used to treat acne. Individuals that were unable to tolerate this therapy or had failed conventional therapy were treated with the azalide antibiotic azithromycin, given in a single oral 250-mg dose three times a week. The other agents were administered daily in divided doses as is current practice. Patients were also on topical care. Results: The efficacy and reported side-effects were examined for all agents. Significant improvement was noted in 4 weeks. All agents were effective in reducing inflammatory lesions and improving acne. Azithromycin produced a slightly higher percentage of patients with a greater than 80% reduction in their inflammatory acne lesions (85.7%) vs. an average of 77.1% for all other agents. All differences observed were not statistically significant. Conclusions: The results show that azithromycin is a safe and effective alternative in the treatment of inflammatory acne with few side-effects and good compliance, and suggest the need for further investigation with a clinical trial that will compare the long-term efficacy and tolerability.
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The important role played by macrolides in the chemotherapy of infectious diseases is well established, but there is still much speculation about their anti-inflammatory potential. A review of in-vitro and ex-vivo studies reported in the literature shows that macrolides have potentially relevant immunomodulatory effects. In-vitro data suggest that erythromycin A derivatives have a direct effect on neutrophil function and the production of cytokines involved in the inflammation cascade. The ex-vivo results indicate that short-term administration of macrolides may enhance the immune response while long-term administration results in immunosuppression. Further research is required to improve our understanding of the therapeutic activity of macrolides.
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Although topical therapies alone can be very effective for milder acne, there are often cases for which oral antibiotics are needed to control disease. Through both antibacterial and antiinflammatory effects, oral antibiotics in combination with other drugs such as retinoids and benzoyl peroxide can be highly effective in the treatment of more severe disease. Patients and their parents often have many questions regarding the safety and efficacy of long-term antibiotic use. It is important for the physician to have a thorough understanding of the antibiotics at their disposal as well as their side effects. Through careful discussion, antibiotic compliance can be optimized and side effects minimized ultimately resulting in treatment success.
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With its broad spectrum of antimicrobial activity, proven efficacy in a wide range of community-acquired infections, improved tissue pharmacokinetic and tolerability profiles, and suitability for once daily dosing, azithromycin provides a useful alternative to erythromycin and other macrolides with similar activity. In patients with uncomplicated urethritis or cervicitis associated with C. trachomatis, N. gonorrhoeae or U. urealyticum, azithromycin as a single dose regimen offers distinct advantages over current pharmacological options and should therefore be considered as a first-line therapy.
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Azithromycin contains an aza-methyl substitution in the 15-membered aglycone ring and as such it is the prototype antibiotic of the azalide class, similar in mechanism of activity to the macrolides. It demonstrates a broad spectrum of activity against many aerobic and anaerobic Gram-positive species, and also inhibits a number of important aerobic and anaerobic Gram-negative bacteria. Significantly, azithromycin shows good activity against Haemophilus influenzae, an organism against which older macrolide antibiotics have proved disappointing. It is highly effective in inhibiting clinically significant intracellular pathogens such as Chlamydia trachomatis and Legionella. Bactericidal activity is seen for certain streptococci and for H. influenzae. Closely linked with azithromycin's microbiologic activity are its novel pharmacokinetics. Azithromycin moves rapidly from blood to tissue compartments where it remains for prolonged periods. Although serum concentrations remain low, the levels attained in the tissues (often greater than 2 mg/kg) are higher than the minimum inhibitory concentration for many common pathogens, and delivery of drug to infection sites by phagocytic cells contributes to these concentrations. This penetration into eukaryotic and prokaryotic cells may be responsible for azithromycin's expanded spectrum of activity, particularly against intracellular organisms. The use of antibiotic blood levels as breakpoints for susceptibility would appear to be inappropriate in the case of azalides. Rather, levels of drug at the tissue site of infection should be considered as guides to predicting efficacy. The in vitro activity of azithromycin, together with its unique tissue pharmacodynamics, define an agent that should demonstrate utility in infections of the respiratory tract, skin and skin structures, and certain sexually transmitted diseases.
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Azithromycin achieves high concentrations in phagocytic cells and in fibroblasts. The newer macrolides also have this property but the intracellular penetration of azithromycin in relation to extracellular concentration is particularly notable. As a weak base, azithromycin is thought to concentrate in lysosomes of phagocytes and fibroblasts but many in vitro factors such as pH and temperature also affect the uptake process. Uptake of azithromycin by polymorphonuclear leucocytes results in an intracellular/extracellular concentration ratio of approximately 40 after one hour of incubation. Intraphagocytic antimicrobial activity has been demonstrated but is rather less than might be anticipated from the intracellular concentrations that are reached. Importantly, the high antibiotic levels found intracellularly do not appear to disrupt normal phagocyte function. Although azithromycin levels in the blood are low soon after administration, tissue concentrations are high and sustained. It appears that fibroblasts serve as a reservoir of drug in tissue, allowing activity against organisms and possibly transferring antibiotic to phagocytic cells for activity against intracellular pathogens and delivery to infection sites.
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Sixty-nine informed subjects participated in a split-face, double-blind trial of topical erythromycin base 2% in Vehicle/N versus Vehicle/N alone. All subjects had grades II or III acne as described by Pillsbury. Study solutions were assigned to a randomly selected side of the subject's face. Solutions were applied twice daily. Inflammatory lesion counts were performed by the same investigator during the eight weeks of study at biweekly intervals. The difference in inflammatory lesion counts from beginning to end of study for each side of the face was compared utilizing Student's paired t-test. There was not a statistically significant difference in mean inflammatory lesions at the end of eight weeks (D = 1.46, t = 1.36, df 68). There was, however, a significant difference at two and six weeks (D = 2.59, t = 3.72, df 68; D = 1.41, t = 2.03, df 68). Observed differences in lesion counts were not considered to be clinically significant.
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A stable solution of erythromycin was developed using a vehicle of ethanol, propylene glycol, and citric acid buffer. In a controlled, randomized, double-blind comparison, a 2% solution of erythromycin applied to moderately severe facial acne was found to be superior to the blank vehicle in reducing the number of inflamed papules. During a period of 12 weeks, such papules were reduced by 56% in the erythromycin group, compared with 33% in the blank vehicle group. In the erythromycin group, 62% of the subjects had a good or excellent response, compared with 27% of those in the blank vehicle group. Adverse effects were similar in type in both groups and included redness, scaling, dryness, oiliness, burning, itching, and irritation of the eyes. No allergic reactions or skin infections were encountered.