SOUND MEDICAL SENSE

Dr Shaantanu S Donde
Medical Advisor
TruliMax

PRODUCT AND ITS PROMISE

Chemical Structure

300 times acid stable

Improved tissue
penetration
 Pharmacokinetics

Absorption

Oral - rapid and very consistent

Acid stable

Minimally affected either in children or in old age

Food does not significantly affect the absorption

Serum Concentration

Long terminal half life - 68 hrs

High serum and tissue concentration

 Pharmacokinetics
Plasma Protein Binding: 12%

Distribution
High intracellular concentrations
Tissue concentration higher than available in plasma
Minimal CSF penetration
Metabolism
Primarily metabolized in liver
Less drug-drug interactions
Trulimax not metabolized by CYP 450
Excretion

Primarily biliary
 Safety Profile
Well tolerated regardless of the age of the patient

Low incidence of generally mild-to-moderate reversible side

effects

– Nausea, vomiting, diarrhea, loose stools, abdominal

discomfort (pain/cramps), and flatulence, rash angioedema

No significant drug-interactions

No dosage adjustment for patients with mild to moderate

impairment of renal and hepatic function
The Effect of Dosing Frequency on Patient
Compliance With Antibiotics in RTIs

100 97.6

80
64.9
60

40
ec nail p mo C %

20

0
Once Twice
Daily Dosing

(N = 501; P < 0.00001; odds ratio = 21)

Kardas P. J Applied Res. 2003;3:201-6.
MIC Values of Antimicrobials against
Common Respiratory Pathogens

TRULIMAX
 Tissue:Plasma Concentration in RTIs

TRULIMAX

Wise R : in the symposium - Significance of Antibiotic tissue penetration at the 6

ECCMID at Spain in March 1993.
 C/E Ratios of Different Antibiotics

Trulimax
Highest
C/E Ratio

Bahal N, Nahata MN. Ann Pharmacother 1992; 26:46-55.

 Clinical Uses

Upper Respiratory Tract Infections

• Pharyngitis/ Tonsillitis

• Sinusitis

• Otitis Media

Lower Respiratory Tract Infections

• Bronchitis

• Pneumonia

Skin & Soft Tissue Infections

Uncomplicated genital infections

CLINICAL EVIDENCE
 Clinical Efficacy in Acute Pharyngitis

Meta-analysis of randomized controlled trials comparing 3–5

days of azithromycin with other antibiotics typically given in
longer courses

16 comparisons including 2477 patients

Journal of Antimicrobial Chemotherapy (2001) 48, 677-689

 Azithromycin vs Roxithromycin in
Acute Pharyngo-tonsillitis

Multicenter open label study

No of patients- 139
Outcome-Bacteriological eradicn Muller O. Journal of Antimicrobial Chemotherapy 1996;
 IDSA Guidelines for Treatment of Acute
Streptococcal Pharyngitis

Penicillins - first-choice therapy

Macrolides (erythromycin) and first-generation oral

cephalosporins - suitable alternative therapy

Azithromycin better tolerated and preferred over

erythromycin

Clinical Pediatrics, Vol. 46, No. 4 suppl, 36S-45S (2007

Azithromycin vs Amoxiclav in ABRS

52

AC
Clinical Cure
AZM

82

Ter Arkh.1998;70(5):72-6
American Jour of Managed Care.Nov 2004
Impact of Acute Exacerbation of
Chronic Bronchitis (AECB)
It constitutes 30 per cent of patients seen in chest clinics and accounts
for 1–2.5% of admission in hospitals all over India.

It is both a rural and urban health problem, the prevalence varying from
1% in urban non-smoker to 21% in rural smokers (Indian J Chest Dis
Allied Sci 2001; 43 : -162)

80% of AECB episodes are due to infectious origin, with 40-60% caused
by bacteria such as Streptococcus pneumoniae, H. influenza M.
catarrhalis and atypical pathogens

Up to 30% mortality rate in hospitalized patients

IDSA acknowledge the importance of the atypical pathogens and suggest

treatment regimens which provide coverage aimed at them
IMPORTANCEOF EXACERBATIONS

Connors AF Jr, Dawson NV, Tomas C, et al. Outcomes following acute exacerbations of severe
chronic obstructive lung disease. The SUPPORT investigators (Study to Understanding Prognosis
and Preferences for Outcomes and Risks of Treatment. Am J Respir Crit Care Med
1996;154:959–67.

Sethi S, Murphy TF. Bacterial infection in chronic obstructive pulmonary disease in 2000. A state
of the art review. Clin Microbiol Rev 2001;14:336–63.
 Azithromycin vs Co-Amoxiclav in AECB

Randomized multicenter open label study

No of patients- 139
Outcome-Clinical success rate
Biebuyck XA. J Int Medicine Res 1996; 24: 407-
Efficacy of AZM vs LEVO in AECB
96 96
94
92
92
90 89
88
86 85 AZM
84 LEVOFLOX
82
80
78
clin bact
cure eradn
 Canadian Guidelines- AECB

Basic clinical state First choice Alternatives for treatment

failure
Chronic bronchitis II- generation macrolide, Fluoroquinolone,
without risk factors II/III -generation cephalosporin, β-lactam/β-lactamase
(simple) amoxicillin, doxycycline, inhibitor
trimethoprim/ sulfamethoxazole

Chronic bronchitis Fluoroquinolone, β-lactam/β- May require parenteral

with risk factorsa lactamase inhibitor therapy—consider referral
(complicated) to a specialist or hospital
Chronic suppurative Ambulatory patients: tailor treatment
bronchitis to airway pathogen—P aeruginosa
common (ciprofloxacin)
Hospitalized patients: parenteral
therapy usually required
Community Acquired Pneumonia( CAP)

Common and serious illness

More than 75 % pts treated as outpatients
A pathogen is isolated in approx 50 %
Atypical pathogens constitute upto 25 %
Azithromycin
– active against most lower respiratory pathogens
– unique PK profile
– High and sustained tissue levels
 Better Eradication in CAP

Hopkins S & Williams D. Current Ther Res 1995; 56: 915-925.

 IDSA Guidelines for CAP

azithromycin

Mandell LA, Wunderink RG, Anzueto A, et al.Clin Infect Dis 2007;44(Suppl. 2):S27–S72.
 Safety of Azithromycin

No of patients- 3995
Indications- RTIs and Skin Infectns
Hopkins S.Am J Med. 1991 Sep 12;91(3A):40S-45S
 Broader Spectrum Does Not Improve Efficacy

Rather they increase risk of selecting resistant flora

Respiratory FluroQ

β -lactams

Macrolides
Typical Atypical Resistant Primarily non-respiratory
respiratory pathogens pathogens Gram-negative coverage
pathogens •PRSP
•ERSP
Odenholt I, Lowdin E, Cars O. Antimicrob Agents Chemother. 2001;45:23-29; Lonks JR, et al. Clin Infect Dis. 2002;35:556-564;
Gleason PP. Pharmacotherapy. 2002;22:2s-11s; Neuhauser MM, et al. JAMA. 2003;289:885-888.
 THANK YOU FOR
LISTENING WITH
OPEN MIND