| 1 |
dpavlin |
1.1 |
<p><b>Sumamed Information for Physicians and Pharmacists</b></p> |
| 2 |
|
|
<p><b>Absorption<br> |
| 3 |
|
|
</b>Sumamed is rapidly absorbed and distributed throughout body tissues and |
| 4 |
|
|
fluids, reaching high and sustained concentrations, that extend the anti-microbial |
| 5 |
|
|
activity of Sumamed well beyond the completion of dosing. Azithromycin's superior |
| 6 |
|
|
absorption, in comparison to erythromycin, is due to its good stability in the |
| 7 |
|
|
acid environment of the stomach. After a single oral dose of 500 mg, peak serum |
| 8 |
|
|
concentration is reached after two to three hours. Sumamed should be taken one |
| 9 |
|
|
hour before or two hours after a meal because food reduces the absorption of |
| 10 |
|
|
azithromycin by approximately 50%.</p> |
| 11 |
|
|
<p><b>Distribution</b><br> |
| 12 |
|
|
As a weak base, it easily penetrates the cell membrane and accumulates within |
| 13 |
|
|
the cell, mainly in lysosomes. High concentrations of azithromycin are found |
| 14 |
|
|
in infected tissues since phagocytes, polymorphonuclear leukocytes and macrophages |
| 15 |
|
|
deliver azithromycin to the infection site and release it there in the presence |
| 16 |
|
|
of bacteria. Following a single 500 mg dose, azithromycin achieves relatively |
| 17 |
|
|
low serum concentrations. As an exceptional advantage in relation to other antibiotics, |
| 18 |
|
|
azithromycin has significantly higher concentrations in tissues than in serum. |
| 19 |
|
|
Tissue concentrations of azithromycin remain high for five to seven days after |
| 20 |
|
|
the completion of dosing, resulting in sustained anti-microbial activity despite |
| 21 |
|
|
the short dosing regimen.</p> |
| 22 |
|
|
<p><b>Metabolism<br> |
| 23 |
|
|
</b>The bio-transformation of azithromycin occurs mainly in the liver. Until |
| 24 |
|
|
now, 10 azithromycin metabolites with no anti-microbial activity have been isolated, |
| 25 |
|
|
50% of biliary excreted azithromycin is in the form of the unchanged compound. |
| 26 |
|
|
</p> |
| 27 |
|
|
<p><b>Elimination<br> |
| 28 |
|
|
</b>Biliary excretion of azithromycin is a major route of elimination. Only |
| 29 |
|
|
6% of the drug is excreted via urine.</p> |
| 30 |
|
|
<p><b>Terminal half-life</b> is approximately 68 hours.</p> |
| 31 |
|
|
<p><b>Microbiological properties</b><br> |
| 32 |
|
|
Mechanism of <b>action:</b><br> |
| 33 |
|
|
Azithromycin acts by interfering with bacterial DNA synthesis (by binding to |
| 34 |
|
|
the 50S ribosomal subunit). Although this mechanism is considered bacteriostatic |
| 35 |
|
|
concentrations several times higher than minimum inhibitory concentrations (MIC) |
| 36 |
|
|
contribute to the bactericidal activity of azithromycin.<br> |
| 37 |
|
|
Mechanism of<b> resistance:<br> |
| 38 |
|
|
</b>The most common mechanism of resistance to azithromycin is genetically determined |
| 39 |
|
|
biochemical interference with the binding of azithromycin to the 50S ribosomal |
| 40 |
|
|
subunit. Some bacteria, resistant to erythromycin, show cross-resistance to |
| 41 |
|
|
other macrolides. </p> |
| 42 |
|
|
<p><b>Anti-microbial spectrum</b> <br> |
| 43 |
|
|
Sumamed is active against the most common pathogens that cause infections of |
| 44 |
|
|
the respiratory tract, skin and soft tissue, and sexually transmitted diseases. |
| 45 |
|
|
It is also effective in the treatment of gastric and duodenal infections caused |
| 46 |
|
|
by <i>Helicobacter pylori</i>. One advantage is its activity against Gram-negative |
| 47 |
|
|
organisms, particularly <i>Haemophilus influenzae</i>. Sumamed also demonstrates |
| 48 |
|
|
excellent activity against intracellular and other organisms (<i>Mycoplasma |
| 49 |
|
|
pneumoniae, Chlamydia pneumoniae, Chlamydia trachomatis</i> and <i>Legionella |
| 50 |
|
|
pneumophila</i>).</p> |
| 51 |
|
|
<p>Sumamed is active against following:</p> |
| 52 |
|
|
<ul> |
| 53 |
|
|
<li><b>upper respiratory tract infections</b> (<i>Streptococcus pneumoniae, |
| 54 |
|
|
Streptococcus pyogenes, Haemophilus influenzae, Moraxella catarrhalis</i>),</li> |
| 55 |
|
|
<li><b>lower respiratory tract infections</b> (<i>Mycoplasma pneumoniae, Streptococcus |
| 56 |
|
|
pneumoniae, Haemophilus influenzae, Chlamydia pneumoniae, Moraxella catarrhalis</i>),</li> |
| 57 |
|
|
<li><b>sexually transmitted diseases</b> (<i>Chlamydia trachomatis, Neisseria |
| 58 |
|
|
gonorrhoeae, Ureaplasma urealyticum</i>),</li> |
| 59 |
|
|
<li><b>skin and soft tissue infections</b> (<i>Staphylococcus aureus, Streptococcus |
| 60 |
|
|
pyogenes</i>)</li> |
| 61 |
|
|
<li>Sumamed is active against <i>Helicobacter pylori</i>.</li> |
| 62 |
|
|
</ul> |
| 63 |
|
|
<p>These facts make Sumamed a reasonable choice for empirical therapy.</p> |
| 64 |
|
|
<p><b>Clinical efficacy<br> |
| 65 |
|
|
</b>Numerous clinical trials have confirmed Sumamed's efficacy in the treatment |
| 66 |
|
|
of:</p> |
| 67 |
|
|
<ol> |
| 68 |
|
|
<li><b>upper respiratory tract infections</b>: |
| 69 |
|
|
<ul> |
| 70 |
|
|
<li>bacterial pharyngitis/tonsillitis,</li> |
| 71 |
|
|
<li>bacterial sinusitis,</li> |
| 72 |
|
|
<li>bacterial otitis media.</li> |
| 73 |
|
|
</ul> |
| 74 |
|
|
</li> |
| 75 |
|
|
<li><b>lower respiratory tract infections</b>: |
| 76 |
|
|
<ul> |
| 77 |
|
|
<li>bacterial bronchitis,</li> |
| 78 |
|
|
<li>acute exacerbation of chronic bronchitis,</li> |
| 79 |
|
|
<li>interstitial pneumoniae,</li> |
| 80 |
|
|
<li>alveolar pneumoniae.</li> |
| 81 |
|
|
</ul> |
| 82 |
|
|
</li> |
| 83 |
|
|
<li><b>sexually transmitted diseases</b>: |
| 84 |
|
|
<ul> |
| 85 |
|
|
<li>uncomplicated urethritis,</li> |
| 86 |
|
|
<li>uncomplicated cervicitis.</li> |
| 87 |
|
|
</ul> |
| 88 |
|
|
</li> |
| 89 |
|
|
<li><b>gastric and duodenal infections</b> caused by <i>Helicobacter pylori</i>.</li> |
| 90 |
|
|
<li><b>skin and soft tissue infections</b>: |
| 91 |
|
|
<ul> |
| 92 |
|
|
<li>erysipelas,</li> |
| 93 |
|
|
<li>impetigo secondary pyoderma,</li> |
| 94 |
|
|
<li>erythema migrans.</li> |
| 95 |
|
|
</ul> |
| 96 |
|
|
</li> |
| 97 |
|
|
</ol> |
| 98 |
|
|
<p><b>Drug interactions</b><br> |
| 99 |
|
|
Azithromycin, unlike majority of macrolides, does not bind to cytochrom P-450 |
| 100 |
|
|
in the liver, resulting in low potential for drug to drug interaction.</p> |
| 101 |
|
|
<p><b>Safety</b><br> |
| 102 |
|
|
Azithromycin is either better or equally well tolerated, compared to other antibiotics. |
| 103 |
|
|
The toleration and safety profile of azithromycin have been assessed in 4,727 |
| 104 |
|
|
patients enrolled in clinical trials carried out in Croatia, the Czech Republic, |
| 105 |
|
|
Hungary, Macedonia, Poland, the Slovak Republic, Slovenia, Russia and the former |
| 106 |
|
|
Yugoslavia.</p> |
| 107 |
|
|
<p><b>Side effects</b> were recorded in 5.65% of the adult patients treated with |
| 108 |
|
|
azithromycin. A statistically higher incidence of side effects (13.89%) was |
| 109 |
|
|
noticed in adult patients treated with comparative antibiotics. In children |
| 110 |
|
|
treated with azithromycin, side effects were recorded in 6.52% of the patients. |
| 111 |
|
|
The incidence of side effects (17.65%) was statistically higher in children |
| 112 |
|
|
treated with other antibiotics. </p> |
Parent Directory
| 
Revision Log