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AZITHROMYCIN

Wockhardt USA LLC.

Azithromycin Tablets 600 mg


FULL PRESCRIBING INFORMATION: CONTENTS*




FULL PRESCRIBING INFORMATION

Rx only

AZITHROMYCIN DESCRIPTION

2R,3S,4R, 5R,8R,10R,11R,12S,13S,14RCOL-riboxylo3872212
AZITHROMYCIN3872212


Pharmacokinetics




MEAN (CV%) PK PARAMETER
DOSE/DOSAGE FORM (serum, except as indicated) Subjects Day No. Cmax (mcg/mL) Tmax (hr) C24 (mcg/mL) AUC (mcg•hr/mL) T½ (hr) Urinary Excretion (% of dose)
500 mg/250 mg capsule 12 Day 1 0.41 2.5 0.05 2.6a -- 4.5
and 250 mg on Days 2-5 12 Day 5 0.24 3.2 0.05 2.1a -- 6.5
1200 mg/600 mg tablets 12 Day 1 0.66 2.5 0.074 6.8b 40 --
%CV (62%) (79%) (49%) (64%) (33%)
600 mg tablet/day 7 1 0.33 2 0.039 2.4a
%CV (25%) (50%) (36%) (19%)
7 22 0.55 2.1 0.14 5.8a 84.5 --
%CV (18%) (52%) (26%) (25%) --
600 mg tablet/day (leukocytes) 7 22 252 10.9 146 4763a 82.8 --
%CV (49%) (28%) (33%) (42%) -- --
a0-24
b

minmaxmin




max

max

max

max





AZITHROMYCIN CONCENTRATIONS FOLLOWING TWO 250 mg (500 mg) CAPSULES IN ADULTS
TISSUE OR FLUID TIME AFTER DOSE (h) TISSUE OR FLUID CONCENTRATION (mcg/g or mcg/mL)1 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
1
*
**
***
****





max

max

Renal Insufficiency

max0-120max0-120DOSAGE AND ADMINISTRATION

Hepatic Insufficiency




Mechanism of Action



in vitro In vivo

Microbiology

in vitro

Aerobic Gram-Positive Microorganisms
    Staphylococcus aureus
    Streptococcus agalactiae
    Streptococcus pneumoniae
    Streptococcus pyogenes

Enterococcus faecalis

Aerobic Gram-Negative Microorganisms
    Haemophilus influenzae
    Moraxella catarrhalis

“Other” Microorganisms
    Chlamydia trachomatis

in vitro

Mycobacteria
    Mycobacterium avium
    Mycobacterium avium
    Mycobacterium intracellulare.
in vitrobut their clinical significance is unknown.

in vitro

Aerobic Gram-Positive Microorganisms



Aerobic Gram-Negative Microorganisms
    Bordetella pertussis
    Campylobacter jejuni
    Haemophilus ducreyi
    Legionella pneumophila

Anaerobic Microorganisms
    Bacteroides bivius
    Clostridium perfringens
    Peptostreptococcus species

“Other” Microorganisms
    Borrelia burgdorferi
    Mycoplasma pneumoniae
    Treponema pallidum
    Ureaplasma urealyticum

Susceptibility Testing of Bacteria Excluding Mycobacteria

in vitro2in vitro2

in vitro

Dilution Techniques :
1
MIC (mcg/mL) Interpretation
≤ 2 Susceptible (S)
4 Intermediate (I)
≥ 8 Resistant (R)





Microorganism MIC (mcg/mL)
Escherichia coli ATCC 25922 2.0-8.0
Enterococcus faecalis ATCC 29212 1.0-4.0
Staphylococcus aureus ATCC 29213 0.25-1.0
Diffusion Techniques :
2


Zone Diameter (mm) Interpretation
≥ 18 (S) Susceptible
14-17 (I) Intermediate
≤ 13 (R) Resistant



Microorganism Zone Diameter (mm)
Staphylococcus aureus ATCC 25923 21-26
In Vitro Activity of Azithromycin Against Mycobacteria.
in vitroMycobacterium aviumM. aviumM. intracellulare,M. aviumM. avium

in vitroMycobacterium avium

Drug Resistance

Mycobacterium aviumEscherichia coli 3,4Mycobacterium aviumM. avium

Susceptibility testing for Mycobacterium avium complex (MAC):
In vitroMycobacterium aviumM. aviumM. intracellulare
in vitroMycobacteriumtuberculosis

AZITHROMYCIN INDICATIONS AND USAGE



Mycobacterial Infections
Prophylaxis of Disseminated M ycobacterium avium complex (MAC) Disease
Mycobacterium avium

Treatment of Disseminated Mycobacterium avium complex (MAC) Disease

AZITHROMYCIN CONTRAINDICATIONS


WARNINGS

CONTRAINDICATIONSrecurred soon thereafter in some patients without further azithromycin exposure



Clostridium difficileC. difficile.

C. difficileC. difficile

C. difficileC. difficile

PRECAUTIONS


General

CLINICAL PHARMACOLOGY - Renal Insufficiency

torsades de pointes



Information for Patients









Drug Interactions







max



0-8max

0-∞max

thmax

max



max





maxmaxmaxmax

max










450


Laboratory Test Interactions:

Carcinogenesis, Mutagenesis, Impairment of Fertility:

Pregnancy: 2
2

2



Nursing Mothers:

Pediatric Use:

Safety in HIV-Infected Pediatric Patients:


Geriatric Use:





Geriatric Patients with Opportunistic Infections, Including Mycobacterium avium complex (MAC) Disease:

AZITHROMYCIN ADVERSE REACTIONS


Clinical

Multiple-dose regimen:



Cardiovascular:

Gastrointestinal:

Genitourinary:

Nervous System:

General:

Allergic:

Chronic therapy with 1200 mg weekly regimen:Mycobacterium avium

Chronic therapy with 600 mg daily regimen combined with ethambutol:

Single 1-gram dose regimen:

Post-Marketing Experience



Allergic:

Cardiovascular: torsades de pointes.

Gastrointestinal:

General:

Genitourinary:

Hematopoietic:

Liver/Biliary:

Nervous System:

Psychiatric:

Skin/Appendages:

Special Senses:

Laboratory Abnormalities
















DOSAGE AND ADMINISTRATION (See INDICATIONS AND USAGE.)


Pediatric Use





Prevention of Disseminated MAC Infections
Mycobacterium avium

Treatment of Disseminated MAC Infections

in vitro
0-120CLINICAL PHARMACOLOGY-Renal Insufficiency.


CLINICAL PHARMACOLOGY-Hepatic Impairment.

HOW SUPPLIED





CLINICAL STUDIES IN PATIENTS WITH ADVANCED HIV INFECTION FOR THE PREVENTION AND TREATMENT OF DISEASE DUE TO DISSEMINATED COMPLEX (MAC) (See INDICATIONS AND USAGE)


Prevention of Disseminated MAC Disease



MAC bacteremia


Cumulative Incidence Rate, %: Placebo (n = 89)
Month MAC Free and Alive MAC Adverse Experience Lost to Follow-up
6 69.7 13.5 6.7 10.1
12 47.2 19.1 15.7 18
18 37.1 22.5 18 22.5
Cumulative Incidence Rate, %: Azithromycin (n = 85)
Month MAC Free and Alive MAC Adverse Experience Lost to Follow-up
6 84.7 3.5 9.4 2.4
12 63.5 8.2 16.5 11.8
18 44.7 11.8 25.9 17.6



Cumulative Incidence Rate, %: Rifabutin (n = 223)
Month MAC Free and Alive MAC Adverse Experience Lost to Follow-up
6 83.4 7.2 8.1 1.3
12 60.1 15.2 16.1 8.5
18 40.8 21.5 24.2 13.5
Cumulative Incidence Rate, %: Azithromycin (n = 223)
Month MAC Free and Alive MAC Adverse Experience Lost to Follow-up
6 85.2 3.6 5.8 5.4
12 65.5 7.6 16.1 10.8
18 45.3 12.1 23.8 18.8
Cumulative Incidence Rate, %: Azithromycin/Rifabutin Combination (n = 218)
Month MAC Free and Alive MAC Adverse Experience Lost to Follow-up
6 89.4 1.8 5.5 3.2
12 71.6 2.8 15.1 10.6
18 49.1 6.4 29.4 15.1


5

Clinically Significant Disseminated MAC Disease


Discontinuations From Therapy For Drug-Related Side Effects


Safety

INCIDENCE OF ONE OR MORE TREATMENT RELATED* ADVERSE EVENTS ** IN HIV INFECTED PATIENTS RECEIVING PROPHYLAXIS FOR DISSEMINATED MAC OVER APPROXIMATELY 1 YEAR
Study 155 Study 174
Placebo Azithromycin 1200 mg weekly Azithromycin 1200 mg weekly Rifabutin 300 mg daily Azithromycin + Rifabutin
(N = 91) (N = 89) (N = 233) (N = 236) (N = 224)
Mean Duration of Therapy (days) 303.8 402.9 315 296.1 344.4
Discontinuation of Therapy 2.3 8.2 13.5 15.9 22.7
Autonomic Nervous System
Mouth Dry 0 0 0 3 2.7
Central Nervous System
Dizziness 0 1.1 3.9 1.7 0.4
Headache 0 0 3 5.5 4.5
Gastrointestinal
Diarrhea 15.4 52.8 50.2 19.1 50.9
Loose Stools 6.6 19.1 12.9 3 9.4
Abdominal Pain 6.6 27 32.2 12.3 31.7
Dyspepsia 1.1 9 4.7 1.7 1.8
Flatulence 4.4 9 10.7 5.1 5.8
Nausea 11 32.6 27 16.5 28.1
Vomiting 1.1 6.7 9 3.8 5.8
General
Fever 1.1 0 2.1 4.2 4.9
Fatigue 0 2.2 3.9 2.1 3.1
Malaise 0 1.1 0.4 0 2.2
Musculoskeletal
Arthralgia 0 0 3 4.2 7.1
Psychiatric
Anorexia 1.1 0 2.1 2.1 3.1
Skin & Appendages
Pruritus 3.3 0 3.9 3.4 7.6
Rash 3.2 3.4 8.1 9.4 11.1
Skin discoloration 0 0 0 2.1 2.2
Special Senses
Tinnitus 4.4 3.4 0.9 1.3 0.9
Hearing Decreased 2.2 1.1 0.9 0.4 0
Uveitis 0 0 0.4 1.3 1.8
Taste Perversion 0 0 1.3 2.5 1.3





Changes in Laboratory Values


Prophylaxis Against Disseminated MAC Abnormal Laboratory Values*
Placebo Azithromycin 1200 mg weekly Rifabutin 300 mg daily Azithromycin & Rifabutin
Hemoglobin < 8 g/dl 1/51 2% 4/170 2% 4/114 4% 8/107 8%
Platelet Count < 50 x 103 /mm3 1/71 1% 4/260 2% 2/182 1% 6/181 3%
WBC Count < 1 x 103 /mm3 0/8 0% 2/70 3% 2/47 4% 0/43 0%
Neutrophils < 500/mm3 0/26 0% 4/106 4% 3/82 4% 2/78 3%
SGOT > 5 x ULNa 1/41 2% 8/158 5% 3/121 3% 6/114 5%
SGPT > 5 x ULN 0/49 0% 8/166 5% 3/130 2% 5/117 4%
Alk Phos > 5 x ULN 1/80 1% 4/247 2% 2/172 1% 3/164 2%
a

Treatment of Disseminated MAC Disease






Response to therapy of patients taking ethambutol and either azithromycin 600 mg qd or clarithromycin 500 mg bid
Azithromycin 600 mg qd Clarithromycin 500 mg bid **95.1% CI on difference
Patients with positive culture at baseline 68 57
Week 24
Two consecutive negative blood cultures* 31/68 (46%) 32/57 (56%) [-28, 7]
Mortality 16/68 (24%) 15/57 (26%) [-18, 13]





Sterilization by Baseline Colony Count

Azithromycin 600 mg (N = 68) Clarithromycin 500 mg bid (N = 57)
Groups Stratified by MAC Colony Counts at Baseline No. (%) Subjects in Stratified Group Sterile at Week 24 No. (%) Subjects in Stratified Group Sterile at Week 24
≤ 10 cfu/mL 10/15 (66.7%) 12/17 (70.6%)
11-100 cfu/mL 13/28 (46.4%) 13/19 (68.4%)
101-1,000 cfu/mL 7/19 (36.8%) 5/13 (38.5%)
1,001-10,000 cfu/mL 1/5 (20.0%) 1/5 (20%)
> 10,000 cfu/mL 0/1 (0.0%) 1/3 (33.3%)

Susceptibility Pattern of MAC Isolates



ANIMAL TOXICOLOGY



REFERENCES:
  • National Committee for Clinical Laboratory Standards. Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically-Third Edition. Approved Standard NCCLS Document M7-A3, Vol. 13, No. 25, NCCLS, Villanova, PA, December 1993.
  • National Committee for Clinical Laboratory Standards. Performance Standards for Antimicrobial Disk Susceptibility Tests-Fifth Edition. Approved Standard NCCLS Document M2-A5, Vol. 13, No. 24, NCCLS, Villanova, PA, December 1993.
  • Dunne MW, Foulds G, Retsema JA. Rationale for the use of azithromycin as Mycobacterium avium chemoprophylaxis. American J Medicine 1997; 102(5C):37-49.
  • Meier A, Kirshner P, Springer B, et al. Identification of mutations in 23S rRNA gene of clarithromycin-resistant Mycobacterium intracellulare. Antimicrob Agents Chemother. 1994;38:381-384.
  • Methodology per Inderlied CB, et al. Determination of In Vitro Susceptibility of Mycobacterium avium Complex Isolates to Antimicrobial Agents by Various Methods. Antimicrob Agents Chemother 1987; 31:1697-1702.

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AZITHROMYCIN

AZITHROMYCIN

AZITHROMYCIN TABLET, FILM COATED

Product Information

Product Type Human prescription drug label Item Code (Source) NDC:64679-962
Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety

Ingredient Name Basis of Strength Strength
AZITHROMYCIN ANHYDROUS AZITHROMYCIN ANHYDROUS 600 mg

Inactive Ingredients

Ingredient Name Strength
cellulose, microcrystalline
STARCH, CORN
CROSCARMELLOSE SODIUM
MAGNESIUM TRISILICATE
MAGNESIUM STEARATE
COLLOIDAL SILICON DIOXIDE
hydroxypropyl cellulose
SODIUM LAURYL SULFATE
HYPROMELLOSES
titanium dioxide
polyethylene glycol

Product Characteristics

Color Size Imprint Code Shape
white (white film-coated) 17 mm W962 OVAL

Packaging

# Item Code Package Description Marketing Start Date Marketing End Date
1 NDC:64679-962-01 30 in 1 BOTTLE

Marketing Information

Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA065302 2008-02-11


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