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Azithromycin Mechanism Of Action

azithromycin mechanism of action


Azithromycin is a semi-synthetic macrolide antibiotic of the azalide class. Like other macrolide antibiotics, azithromycin inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit of the bacterial 70S ribosome. Binding inhibits peptidyl transferase activity and interferes with amino acid translocation during the process of translation. Its effects may be bacteriostatic or bactericidal depending of the organism and the drug concentration. Its long half life, which enables once daily dosing and shorter administration durations, is a property distinct from other macrolides.

How should I take azithromycin?

Take azithromycin exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended. The dose and length of treatment may not be the same for every type of infection.

You may take most forms of azithromycin with or without food.

Take Zmax extended release liquid (oral suspension) on an empty stomach, at least 1 hour before or 2 hours after a meal.

To use the oral suspension single dose packet: Open the packet and pour the medicine into 2 ounces of water. Stir this mixture and drink all of it right away. Do not save for later use. To make sure you get the entire dose, add a little more water to the same glass, swirl gently and drink right away.

What should I avoid while taking azithromycin?

Do not take antacids that contain aluminum or magnesium within 2 hours before or after you take azithromycin. This includes Acid Gone, Aldroxicon, Alternagel, Di-Gel, Gaviscon, Gelusil, Genaton, Maalox, Maldroxal, Milk of Magnesia, Mintox, Mylagen, Mylanta, Pepcid Complete, Rolaids, Rulox, and others. These antacids can make azithromycin less effective when taken at the same time.

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or bloody, call your doctor. Do not use anti-diarrhea medicine unless your doctor tells you to.

Avoid exposure to sunlight or tanning beds. Azithromycin can make you sunburn more easily. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.

Mechanism of action

Azithromycin is bacteriostatic and like other macrolides inhibits synthesis of protein by binding reversibly to 50S ribosomal subunits of sensitive microorganisms, at or very close to the site that binds chloramphenicol. It does not inhibit peptide bond formation per se but rather inhibits the translocation step where a recently formed peptidyl tRNA travels from the acceptor site (A) on the ribosome to the peptidyl donor site (P). Alternatively, macrolides may bind and cause a conformational change that terminates protein synthesis by indirectly interfering with transpeptidation and translocation. Thus synthesis of proteins is inhibited.

At high concentrations azithromycin is bactericidal against susceptible strains. Cells are substantially more permeable to the unionized form of azithromycin, which possibly explains the augmented antimicrobial activity at alkaline pH.

Adverse reactions

Gastrointestinal disturbances are the most frequent side effect of azithromycin but are usually mild and less frequent than with erythromycin. Headache, somnolence, and taste disturbances may occur.

Rarely seen side effects are:

GIT: vomiting, gastritis, diarrhoea, decreased appetite, constipation, dyspepsia, flatulence.

CVS: Palpitations, sometime pain in chest.

Genitourinary: vaginitis and nephritis.

CNS: Giddiness, convulsions, headache, vertigo, nervousness and increased sleepiness.

Allergic: Rashes, itching, photosensitivity.

Hematologic – Anemia and decreased WBC count.

General: Fever, fatigue, oedema.

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