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| AZITHROMYCIN

04:54 EDT 27th August 2014 | BioPortfolio

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IMAGE Azithromycin Tablets_structure label.jpg
TISSUE OR FLUID TIME AFTER
DOSE (h)
TISSUE OR FLUID
CONCENTRATION
(mcg/g or mcg/mL)
CORRESPONDING
PLASMA OR SERUM LEVEL (mcg/mL)
TISSUE (FLUID)
PLASMA (SERUM) RATIO
SKIN 72-96 0.4 0.012 35
LUNG 72-96 4 0.012 >100
SPUTUM* 2-4 1 0.64 2
SPUTUM** 10-12 2.9 0.1 30
TONSIL*** 9-18 4.5 0.03 >100
TONSIL*** 180 0.9 0.006 >100
CERVIX**** 19 2.8 0.04 70
Pharmacokinetic Parameter
[mean (SD)]
3-Day Regimen
(20 mg/kg x 3 days)
5-Day Regimen
(12 mg/kg x 5 days)
n
11
17
Cmax (mcg/mL)
1.1 (0.4)
0.5 (0.4)
Tmax (hr)
2.7 (1.9)
2.2 (0.8)
Auc0-24 mcg•hr/mL
7.9 (2.9)
3.9 (1.9)
Co-administered Drug Dose of Co-administered Drug

Dose of Azithromycin

n
Ratio (with/without azithromycin)
of Co-administered Drug
Pharmacokinetic Parameters
(90% CI); No Effect = 1




Mean Cmax    Mean AUC
Atorvastatin 10 mg/day x 8 days 500 mg/day PO on days 6-8 12
0.83
(0.63 to 1.08)
1.01
(0.81 to 1.25)
Carbamazepine 200 mg/day x 2 days, then 200 mg
BID x 18 days
500 mg/day PO for days 16-18 7
0.97
(0.88 to 1.06)
0.96
(0.88 to 1.06)
Cetirizine 20 mg/day x 11 days 500 mg PO on day 7, then 250 mg/day on days 8-11 14
1.03
(0.93 to 1.14)
1.02
(0.92 to 1.13)
Didanosine 200 mg PO BID x 21 days 1,200 mg/day PO on days 8-21 6
1.44
(0.85 to 2.43)
1.14
(0.83 to 1.57)
Efavirenz 400 mg/day x 7 days 600 mg PO on day 7 14
1.04* 0.95*
Fluconazole 200 mg PO single dose 1,200 mg PO single dose 18
1.04
(0.98 to 1.11)
1.01
(0.97 to 1.05)
Indinavir 800 mg TID x 5 days 1,200 mg PO on day 5 18
0.96
(0.86 to 1.08)
0.90
(0.81 to 1.00)
Midazolam 15 mg PO on day 3 500 mg/day PO x 3 days 12
1.27
(0.89 to 1.81)
1.26
(1.01 to 1.56)
Nelfinavir 750 mg TID x 11 days 1,200 mg PO on day 9 14
0.90
(0.81 to 1.01)
0.85
(0.78 to 0.93)
Rifabutin 300 mg/day x 10 days 500 mg PO on day 1, then 250 mg/day on days 2-10 6
See footnote
below
NA
Sildenafil
100 mg on days 1 and 4 500 mg/day PO x 3 days 12
1.16
(0.86 to 1.57)
0.92
(0.75 to 1.12)
Theophylline 4 mg/kg IV on days 1, 11, 25 500 mg PO on day 7, 250 mg/day on days 8-11 10
1.19
(1.02 to 1.40)
1.02
(0.86 to 1.22)
Theophylline 300 mg PO BID x 15 days 500 mg PO on day 6, then 250 mg/day on days 7-10 8
1.09
(0.92 to 1.29)
1.08
(0.89 to 1.31)
Triazolam 0.125 mg on day 2 500 mg PO on day 1, then 250 mg/day on day 2 12
1.06* 1.02*
Trimethoprim/ Sulfamethoxazole 160 mg/800mg/day PO x 7 days 1,200 mg PO on day 7 12
0.85
(0.75 to 0.97)/
0.87
(0.80 to 0.95/
0.96
(0.88 to 1.03)
Zidovudine 500 mg/day PO x 21 days 600 mg/day PO x 14 days 5
1.12
(0.42 to 3.02)
0.94
(0.52 to 1.70)
Zidovudine 500 mg/day PO x 21 days 1,200 mg/day PO x 14 days 4
1.31
(0.43 to 3.97)
1.30
(0.69 to 2.43)
Co-administered
Drug
Dose of
Co-administered
Drug
Dose of
Azithromycin
n Ratio (with/without
co-administered drug) of
Azithromycin Pharmacokinetic
Parameters (90% CI);
 No Effect = 1




Mean Cmax Mean AUC
Efavirenz 400 mg/day x 7 days 600 mg PO on day 7 14
1.22
(1.04 to 1.42)
0.92*
Fluconazole 200 mg PO single dose 1,200 mg PO single dose 18
0.82
(0.66 to 1.02)
1.07
(0.94 to1.22)
Nelfinavir 750 mg TID x 11 days 1,200 mg PO on day 9 14
2.36
(1.77 to 3.15)
2.12
(1.80 to 2.50)
Rifabutin 300 mg/day x 10 days 500 mg PO on day 1, then 250 mg/day on days 2-10 6
See footnote
below
NA
Dosage
Regimen

Diarrhea, %
Abdominal
Pain, %
Vomiting, %
Nausea, %
Rash, %
         1-day           4.3%            1.4%                            4.9%               1.0%


      1.0%
         3-day

          2.6%

          1.7%

                          2.3%           0.4%

         0.6%

         5-day          1.8%         1.2%                           1.1%            0.5%         0.4%
Dosage
Regimen
Diarrhea/Loose stools, % Abdominal
Pain, %
Vomiting, % Nausea, % Rash, %






   5-day
          5.8%
           1.9%
           1.9%
           1.9%
          1.6%
Dosage
Regimen
Diarrhea, % Abdominal
Pain, %
Vomiting, % Nausea, % Rash, % Headache%







  5-day
  5.4%
  3.4%
  5.6%
  1.8%
  0.7%   1.1%







Infection* Recommended Dose/Duration of Therapy
Community-acquired pneumonia (mild severity)
Pharyngitis/tonsillitis (second line therapy)
Skin/skin structure (uncomplicated)
500 mg as a single dose on Day 1, followed by 250 mg once daily on Days 2 through 5.
Acute bacterial exacerbations of chronic obstructive pulmonary disease (mild to moderate) 500 mg QD x 3 days
OR
500 mg as a single dose on Day 1, followed by 250 mg once daily on Days 2 through 5.
Acute bacterial sinusitis 500 mg QD x 3 days
Genital ulcer disease (chancroid) One single 1 gram dose
Non-gonoccocal urethritis and cervicitis One single 1 gram dose
Gonococcal urethritis and cervicitis One single 2 gram dose
PEDIATRIC DOSAGE GUIDELINES FOR OTITIS MEDIA,ACUTE BACTERIAL SINUSITIS AND COMMUNITY-ACQUIRED PNEUMONIA (Age 6 months and above, see PRECAUTIONS-Pediatric Use.) Based on Body Weight
OTITIS MEDIA AND COMMUNITY-ACQUIRED PNEUMONIA: (5-Day Regimen)*
Dosing Calculated on 10 mg/kg/day Day 1 and 5 mg/kg/day Days 2 to 5.

    Weight
                   100 mg/5 mL
                                200 mg/5 mL
Total mL     per Treatment Course  Total mg per
 Treatment Course
Kg  Lbs.     Day 1
 Days 2-5
              Day 1   Days 2-5

5
11
2.5 mL (½ tsp)
1.25 mL (¼ tsp)


                7.5 mL
            
        150 mg

10
22
  5 mL  (1 tsp)
2.5 mL (½ tsp)


                15 mL
         300 mg
20
44


          5 mL (1 tsp)   2.5 mL (½ tsp)                 15 mL
          
          600 mg

30
66


    7.5 mL (1½ tsp)  3.75 mL (3/4tsp)               22.5 mL
           900 mg
40
88


       10 mL (2  tsp)
      
    5 mL (1tsp)

                30 mL
         1200 mg
50 and above



12.5 mL (2 ½ tsp)
 6.25 mL (1¼ tsp)              37.5 mL
        1500 mg
OTITIS MEDIA AND ACUTE BACTERIAL SINUSITIS: (3-Day Regimen)*
Dosing Calculated on 10 mg/kg/day Day 1.

    Weight
   100 mg/5 mL     200 mg/5 mL Total mL per
 Treatment Course
Total mg per
 Treatment Course
Kg  Lbs.            Day 1-3              Day 1-3

5
11

            2.5 mL (½ tsp)

                7.5 mL
             150 mg
10
22

            5 mL (1 tsp)

                15 mL
             300 mg

20

44

         
               5 mL (1 tsp)
                15 mL
             600 mg

30
66

       
             7.5 mL (1½ tsp)
                22.5 mL
            900 mg
40
88

      
              10 mL (2 tsp)

                30 mL
           1200 mg
50 and above
110 and above

              12.5 mL (2 ½ tsp )
               37.5 mL
          1500 mg
OTITIS MEDIA : (1-Day Regimen)
Dosing Calculated on 30 mg/kg as a single dose
Weight

200 mg/5 mL
Total mL per Treatment course
Total mg per Treatment course
Kg Lbs.
Day1



5
11
3.75 mL (3/4 tsp)
                            3.75  mL
                              150 mg
10
22
7.5 mL (1½ tsp)
                              7.5 mL
                              300 mg
20
44
15 mL (3 tsp)                               15 mL
                              600 mg
30
66
22.5 mL (4 ½ tsp)                               22.5 mL
                              900 mg
40
88
30 mL (6tsp)                               30 mL
                              1200 mg
50 and above
110 and above
37.5 mL (7½ tsp)                               37.5 mL
                              1500 mg
PHARYNGITIS/TONSILITIS: (5-Day Regimen)
Dosing Calculated on 12 mg/kg/day for 5 days
Weight

200mg/5mL
Total mL per Treatment course
Total mg per Treatment course
Kg Lbs.
           Day 1-5



8
18
         2.5 mL (½ tsp)
                            12.5  mL
                              500 mg
17
37
         5 mL (1 tsp)
                              25 mL
                              1000 mg
25
55
        7.5 mL (1 ½ tsp)                               37.5 mL
                             1500 mg
33
73
        10 mL (2  tsp)                               50 mL
                             2000 mg
40
88
        12.5 mL (2 ½ tsp)                               62.5 mL
                             2500 mg

(See INDICATIONS AND USAGE and Pediatric Use.) Pediatric Patients From the perspective of evaluating pediatric clinical trials, Days 11-14 were considered on-therapy evaluations because of the extended half-life of azithromycin. Day 11-14 data are provided for clinical guidance. Day 24-32 evaluations were considered the primary test of cure endpoint. Acute Otitis Media Safety and efficacy using azithromycin 30 mg/kg given over 5 days Protocol 1In a double-blind, controlled clinical study of acute otitis media performed in the United States, azithromycin (10 mg/kg on Day 1 followed by 5 mg/kg on Days 2-5) was compared to amoxicillin/clavulanate potassium (4:1). For the 553 patients who were evaluated for clinical efficacy, the clinical success rate (i.e., cure plus improvement) at the Day 11 visit was 88% for azithromycin and 88% for the control agent. For the 521 patients who were evaluated at the Day 30 visit, the clinical success rate was 73% for azithromycin and 71% for the control agent. In the safety analysis of the above study, the incidence of treatment-related adverse events, primarily gastrointestinal, in all patients treated was 9% with azithromycin and 31% with the control agent. The most common side effects were diarrhea/loose stools (4% azithromycin vs. 20% control), vomiting (2% azithromycin vs. 7% control), and abdominal pain (2% azithromycin vs. 5% control). Protocol 2In a non-comparative clinical and microbiologic trial performed in the United States, where significant rates of beta-lactamase producing organisms (35%) were found, 131 patients were evaluable for clinical efficacy. The combined clinical success rate (i.e., cure and improvement) at the Day 11 visit was 84% for azithromycin. For the 122 patients who were evaluated at the Day 30 visit, the clinical success rate was 70% for azithromycin. Microbiologic determinations were made at the pre-treatment visit. Microbiology was not reassessed at later visits. The following presumptive bacterial/clinical cure outcomes (i.e., clinical success) were obtained from the evaluable group

In the safety analysis of this study, the incidence of treatment-related adverse events, primarily gastrointestinal, in all patients treated was 9%. The most common side effect was diarrhea (4%). Protocol 3In another controlled comparative clinical and microbiologic study of otitis media performed in the United States, azithromycin was compared to amoxicillin/clavulanate potassium (4:1). This study utilized two of the same investigators as Protocol 2 (above), and these two investigators enrolled 90% of the patients in Protocol 3. For this reason, Protocol 3 was not considered to be an independent study. Significant rates of beta-lactamase producing organisms (20%) were found. Ninety-two (92) patients were evaluable for clinical and microbiologic efficacy. The combined clinical success rate (i.e., cure and improvement) of those patients with a baseline pathogen at the Day 11 visit was 88% for azithromycin vs. 100% for control; at the Day 30 visit, the clinical success rate was 82% for azithromycin vs. 80% for control.Microbiologic determinations were made at the pre-treatment visit. Microbiology was not reassessed at later visits. At the Day 11 and Day 30 visits, the following presumptive bacterial/clinical cure outcomes (i.e., clinical success) were obtained from the evaluable group

In the safety analysis of the above study, the incidence of treatment-related adverse events, primarily gastrointestinal, in all patients treated was 4% with azithromycin and 31% with the control agent. The most common side effect was diarrhea/loose stools (2% azithromycin vs. 29% control). Safety and efficacy using azithromycin 30 mg/kg given over 3 days Protocol 4In a double-blind, controlled, randomized clinical study of acute otitis media in pediatric patients from 6 months to 12 years of age, azithromycin (10 mg/kg per day for 3 days) was compared to amoxicillin/clavulanate potassium (7:1) in divided doses q12h for 10 days. Each patient received active drug and placebo matched for the comparator.For the 366 patients who were evaluated for clinical efficacy at the Day 12 visit, the clinical success rate (i.e., cure plus improvement) was 83% for azithromycin and 88% for the control agent. For the 362 patients who were evaluated at the Day 24-28 visit, the clinical success rate was 74% for azithromycin and 69% for the control agent.In the safety analysis of the above study, the incidence of treatment-related adverse events, primarily gastrointestinal, in all patients treated was 10.6% with azithromycin and 20% with the control agent. The most common side effects were diarrhea/loose stools (5.9% azithromycin vs. 14.6% control), vomiting (2.1% azithromycin vs. 1.1% control), and rash (0% azithromycin vs. 4.3% control). Safety and efficacy using azithromycin 30 mg/kg given as a single dose Protocol 5A double blind, controlled, randomized trial was performed at nine clinical centers. Pediatric patients from 6 months to 12 years of age were randomized 1:1 to treatment with either azithromycin (given at 30 mg/kg as a single dose on Day 1) or amoxicillin/clavulanate potassium (7:1), divided q12h for 10 days. Each child received active drug, and placebo matched for the comparator.Clinical response (Cure, Improvement, Failure) was evaluated at End of Therapy (Day 12-16) and Test of Cure (Day 28-32). Safety was evaluated throughout the trial for all treated subjects. For the 321 subjects who were evaluated at End of Treatment, the clinical success rate (cure plus improvement) was 87% for azithromycin, and 88% for the comparator. For the 305 subjects who were evaluated at Test of Cure, the clinical success rate was 75% for both azithromycin and the comparator. In the safety analysis, the incidence of treatment-related adverse events, primarily gastrointestinal, was 16.8% with azithromycin, and 22.5% with the comparator. The most common side effects were diarrhea (6.4% with azithromycin vs. 12.7% with the comparator), vomiting (4% with each agent), rash (1.7% with azithromycin vs. 5.2% with the comparator) and nausea (1.7% with azithromycin vs. 1.2% with the comparator). Protocol 6In a non-comparative clinical and microbiological trial, 248 patients from 6 months to 12 years of age with documented acute otitis media were dosed with a single oral dose of azithromycin (30 mg/kg on Day 1).For the 240 patients who were evaluable for clinical modified Intent-to-Treat (MITT) analysis, the clinical success rate (i.e., cure plus improvement) at Day 10 was 89% and for the 242 patients evaluable at Day 24-28, the clinical success rate (cure) was 85%

Presumed Bacteriologic Eradication




Day 11
Azithromycin
Day 30
Azithromycin
S. pneumoniae
61/74 (82%)
40/56 (71%)
H. influenzae 43/54 (80%)
30/47 (64%)
M. catarrhalis
28/35 (80%)
19/26 (73%)
S. pyogenes
11/11 (100%)
7/7
Overall
177/217 (82%)
97/137 (73%)

Manufacturer

Rebel Distributors Corp.

Active Ingredients

Source

Clinical Trials [214 Associated Clinical Trials listed on BioPortfolio]

Local Pharmacokinetics of Azithromycin Eye Drops in Healthy Volunteers

To compare the pharmacokinetic behavior of azithromycin eye drops in the tear with the original azithromycin eye drops, and evaluate the release behavior of both in the eye.

A Study of Azithromycin in HIV-Infected Patients

To assess the dose proportionality of azithromycin concentrations and toleration when delivered in tablet formulation to HIV-infected patients. The need exists to further assess the antib...

The Study Of Azithromycin Switch Therapy For Treatment Of Community Acquired Pneumonia (CAP)

Azithromycin has high rates of clinical response and eradication, wide spectrum of activity, so we suppose the development of the azithromycin injectable formulation in Japan would deliver...

Trial II of Lung Protection With Azithromycin in the Preterm Infant

The hypothesis of this study is that administration of azithromycin to ventilated premature infants will decrease the incidence and severity of BPD. The purpose of this study is to determ...

A Study to Evaluate the Effects of Azithromycin on MAC Disease Prevention in HIV-Positive Patients

This study is designed to find out whether HIV-positive patients whose immune systems have improved after receiving anti-HIV treatment should take azithromycin to prevent Mycobacterium avi...

PubMed Articles [85 Associated PubMed Articles listed on BioPortfolio]

Neisseria gonorrhoeae 23S rRNA A2059G mutation is the only determinant necessary for high-level azithromycin resistance and improves in vivo biological fitness.

The global emergence of Neisseria gonorrhoeae isolates displaying high-level azithromycin resistance is a major concern for the currently recommended azithromycin/ceftriaxone dual therapy. N. gonorrho...

Synthesis and evaluation of biological activity of benzoxaborole derivatives of azithromycin.

Novel benzoxaborole derivatives of azithromycin in which benzoxaborole residue is attached to the 4″-hydroxy-group of azithromycin have been synthesized. Antibacterial activity of synthesized deriva...

Safety of azithromycin in infants under six months of age in Niger: A community randomized trial.

Mass azithromycin distribution reduces under-5 child mortality. Trachoma control programs currently treat infants aged 6 months and older. Here, we report findings from an infant adverse event survey ...

Oral Fluoroquinolones and Risk of Fibromyalgia.

The Food and Drug Administration (FDA) has recently included a black box warning on fibromyalgia like symptoms with fluoroquinolones (FQs) but no large epidemiologic study is to date available. We und...

Antimicrobial resistance following mass azithromycin distribution for trachoma: a systematic review.

Mass azithromycin distribution is a core component of trachoma control programmes and could reduce mortality in children younger than 5 years in some settings. In this systematic review we synthesise ...

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Presumed Bacteriologic Eradication
Day 11
Day 30

Azithromycin
Control 
Azithromycin
Control

S. pneumoniae
25/29 (86%)
26/26 (100%)
22/28 (79%)
18/22 (82%)