Chemistry 6-O-methylerythromycin
Pharmacological
category
Macrolide antibiotic
Pharmacology
Clarithromycin exerts its antibacterial effect by binding to
50s ribosome subunit of susceptible organisms
and inhibiting protein synthesis
Microbiology
It is active invitro against a variety of aerobic and
anaerobic gram positive and gram negative organisms as well as most mycobacterium avium complex organisms
Gram positive aerobes: staphylococcus aureus, streptococcus
pneumonia, streptococcus pyogenes
Gram negative aerobes: haemophilus influenza, Moraxella [Branhamella catarrhalis]
Other aerobes: mycoplasma pneumonia
[Mycobacteriae: mycobacterium avium complex consisting of
:mycobacterium avium and mycobacterium intracellulare]
Pharmacokinetics
Clarithromycin is rapidly absorbed from the gastrointestinal
tract after oral administration. The absolute bioavailability of 250mg
clarithromycin tablet was approximately 50%. Food slightly delays both the
onset of clarithromycin absorption and formation of he antimicrobially active
metabolite, 14-OH-clarithromycin, but does not affect the extent of
bioavailability . therefore clarithromycin tablets may be given without regards
to meals
Indications and uses
Clarithromycin is indicated in the treatment of upper and
lower respiratory tract infections, pharyngitis, tonsillitis due to
streptococcus pyogenes , acute maxillary sinusitis ,cute bacterial exacerbation
of chronic bronchitis , pneumonia, uncomplicated skin and skin structure
infections.
Contraindications
Clarithromycin is contraindicated in patients with known
hypersensitivity to clarithromycin, erythromycin or any of the macrolide
antibiotics
Side effects/adverse
reactions
Diarrheas, nausea, abnormal taste, dyspepsia, abdominal
pain/discomfort, and headache.
Precautions and
warnings
General
In presence of severe
renal impairment, with or without coexisting hepatic impairment, decreased
dosage or prolonged dosing intervals may be appropriate. clarithromycin should
not be used in pregnant women except in clinical circumstances where no
alternative therapy is appropriate. Pseudomembranous
colitis has been reported with nearly all antibacterial agents including
macrolides, and may range in severity from mild to severe.
Pediatric use
Safety and effectiveness of clarithromycin in children under
6 months have not been established
Drug interactions
Clarithromycin use in patients who are receiving theophylline may be associated with an increase in
serum theophylline concentrations. Clarithromycin may increase carbamazepine concentrations. Active metabolite of terfenadine was three times higher when co-administered
with clarithromycin. Concomitant administration of clarithromycin and digoxin has been reported to result in elevated
digoxin levels
Use in pregnancy and lactation
Clarithromycin should be used in pregnancy only if potential
benefits justifies the potential risk to the fetus. The FDA classifies it at pregnancy
category C
It is not known whether clarithromycin is excreted in human
milk. Because many drugs are excreted in human milk, caution should be
exercised when clarithromycin is administered to a nursing woman.
Dosage and
administration
Upper respiratory tract infections 250-500mg q12h for 10-14
days.
Lower respiratory tract infections 250mg q12h for 7- 14 days
uncomplicated skin and skin structure infections 250mg q12h 7-14
days
Overdose symptoms
antidote
Studies on overdose not available
Storage
store below 30°c.
Keep out of reach of children
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