Erythromycin

Introduction
• Belonge to maacrolide
• Obtained from streptomyces erytherus in
1952
• Bacteriostatic
• Used instead of pencilline in patients who
have alllergy
 Explanation
• Intermediate spectrum macrolide antibiotic
• Trade names ( A-
mycin,Eromycin,etrocin,Erythrocin eryc )
• Active against G+ bacteria
• Plasma half life 2 hours
• Metabolism via liver
• Its main elimination route is in the bile with
little renal excretion, 2%-15% unchanged drug.
 Explanation

• Dosage..250 mg and 500 mg tablets

• In children 30 to 50mg/kg/day
• Protien binding 65%-90%
• Ditribution.. Diffused well in tissue of
organisms
• Slightly diffuse in CSF
• Liphophilic
• Unstable in acidic enviornment
 Metabolism
• In liver
• By enzyme of cytochrome P450 system
• CY3AP4
• Liphophilic in nature cant excreted by kidney..
Reabsorbed in Kidney tubules
 CytochromeP45O
• CYtochrome P450 enzymes are essential for
the metabolism of many medications.
• Although this class has more than 50
enzymes, six of them metabolize 90 percent of
drugs, with the two most significant enzymes
being CYP3A4 and CYP2D6.
• Primarily found in liver and GIT
 Interaction with other drugs

• Known to inhibit the oxidation of a number of

drugs through their interaction with
cytochrome PP450
 Route of administration

• Oral(both tablets and capsules)

• Parentral(IV and IM)
• Topical(ointment)
 MECHANISM OF ACTION
• Target 50s ribosomal subunit
• Inhibition of translocation of mRNA
 Indication of erythromycine
• Alternative to pencillin in hypersensitive patients
• Bacterial infections
• Bronchitis
• Eye infections
• GI infections
• Lower respiratory tract infection
• Pharyngitis
• Pneumonia
• Acne vulgaris(esotek)
• Otitis media
• Bone and joint infection
 Prophylaxis

• Bacterial endocarditis
• Sexually transmitted infections
• Skin infections
 Side effects
• Hepatitis
• Pancreatitis
• Psychosis
• Thrombophlebitis(intravenous administration)
• Hearing loss
• Diarrhea
• Rashes
• Abdominal pain
• Anorexia
 Contraindication

• Hepatic dysfunction
• Hypersensitivity
• Pregnany… can cross the placental
barrier...epilepsy
• This contain sucrose so patients with sucrase
isomaltase insufficiency should not take this
medicine
 Resistance
• Methylation of ribosomes(erm..erythromycin
ribosomal methylation gene)

• Efflux pump

• Examples..E.coli,hemophillus
influenza,clostridium perfringens
Methylation of ribosome
Efflux pump
 Telithromycine
• Semi-synthetic erythromycine derivative
• 10 times higher affinity than erythromycin to
bind with 50s ribosomal subunit
• Acid stable