Macrolide
Macrolide
Macrolide
Macrolides are antibiotics having macro cyclic lactone rings with one or two amino-sugars.Clarithromycin and
azithromycin are semi synthetic derivatives of erythromycin
MOA
Spectrum Activity
Erythromycins are active against many gram-positive organisms, including streptococci (e.g., Streptococcus pneumoniae), and
Corynebacterium and Neisseria species as well as some strains of Mycoplasma, Legionella, Treponema, and Bordetella. Some
Staphylococcus aureus strains that resist penicillin G are susceptible to erythromycins.
Clarithromycin is more active than erythromycin against staphylococci and streptococci. In addition to activity against other
organisms covered by erythromycin, it is also active in vitro against MAI, Toxoplasma gondii, and Cryptosporidium spp. (b) Th
erapeutic uses. Th is agent is indicated for the prevention of Mycobacterium
Azithromycin is less active than erythromycin against grampositive cocci but more active against H. infl uenzae and other gram-
negative organisms. Azithromycin concentrates within cells, and tissue levels are higher than serum levels
Uses
a. Erythromycins are the preferred drugs for the treatment of Mycoplasma pneumoniae and Campylobacter infections,
Legionnaires disease, chlamydial infections, diphtheria, and pertussis.
b. In patients with penicillin allergy, erythromycins are important alternatives in the treatment of pneumococcal pneumonia, S.
aureus infections, syphilis, and gonorrhea.
c. Erythromycins may be given prophylactically before dental procedures to prevent bacterial endocarditis.
Clarithromycin is indicated for the prevention of Mycobacterium avium complex (MAC) infection and is useful in otitis media,
sinusitis, mycoplasmal pneumonia, and pharyngitis. Clarithromycin is also used with proton pump inhibitors (PPIs) for
Helicobacter pylori eradication.
Azithromycin is useful in nongonococcal urethritis caused by chlamydia, lower respiratory tract infections, Mycobacterium
avium-intracellulare (MAC or MAI) infection and prophylaxis, pharyngitis, pelvic infl ammatory disease, and Legionnaires
disease. Azithromycin is also indicated for pediatric use.
Side Effect of Erythromycin
a. Gastrointestinal (GI) distress (e.g., nausea, vomiting, diarrhea, epigastric discomfort) may occur with all erythromycin forms
and are the most common adverse effects.
b. Allergic reactions (rare) may present as skin eruptions, fever, and eosinophilia.
c. Cholestatic hepatitis may arise in patients treated for 1 week or longer with erythromycin estolate; symptoms usually
disappear within a few days after drug therapy ends. There have been infrequent reports of hepatotoxicity with other salts of
erythromycin.
d. IM injections of more than 100 mg produce severe pain persisting for hours.
e. Transient hearing impairment may develop with high-dose erythromycin therapy
Drug interactions
a. Erythromycin inhibits the hepatic metabolism of theophylline, resulting in toxic accumulation.
b. Erythromycin interferes with the metabolism of digoxin, corticosteroids, carbamazepine, cyclosporin, and lovastatin, possibly
potentiating the eff ect and toxicity of these drugs.
c. Clarithromycin (Biaxin) may potentiate oral anticoagulants (monitor prothrombin time), increase cyclosporine levels with
increased toxicity, and increase digoxin and theophylline levels.
d. Coadministration of clarithromycin and cisapride may increase risk of serious cardiac arrhythmias; coadministration is
contraindicated.
e. Sudden deaths have been reported when clarithromycin was added to ongoing pimozide therapy; coadministration is
contraindicated.