4. Mechanism of resistance: modification of the ribosomal binding site production of esterase that hydrolyze macrolides reduced permeability of cell membrane or active efflux system is involved Cross-resistance is complete between erythromycin and the other macrolides
4. Mechanism of resistance: • modification of the ribosomal binding site • production of esterase that hydrolyze macrolides. • reduced permeability of cell membrane or active efflux system is involved. • Cross-resistance is complete between erythromycin and the other macrolides
General properties of Macrolides 4. ADME 1)Absorption: Stearate and ester of erythromycin are fairly acid-resistant and somewhat batter absorbed Food interferes with absorption
4. ADME 1) Absorption: Stearate and ester of erythromycin are fairly acid-resistant and somewhat batter absorbed. Food interferes with absorption. General properties of Macrolides
General properties of Macrolides 4. ADME 2)Distribution: does not cross BBB. 3 Elimination: it is concentrated in the liver, where some is unactive while some is excreted in active form in the bile
4. ADME 2) Distribution: does not cross BBB. 3) Elimination: it is concentrated in the liver, where some is unactived, while some is excreted in active form in the bile. General properties of Macrolides
General properties of Macrolides 5. Clinical Uses. 1) Mycoplasma(支原体) infections 2) Legionnaire's disease(军因菌病) 3) Chlamydia infections(衣原体感染) 4) Streptococcus(链赇黄) infections 5) Diphtheria(台赛) chincough(百目咳) 6) toxoplasmosis(子形虫病)
5.Clinical Uses: 1) Mycoplasma (支原体) infections. 2) Legionnaire’s disease (军团菌病). 3) Chlamydia infections (衣原体感染). 4) Streptococcus (链球菌) infections. 5) Diphtheria (白喉), chincough(百日咳). 6) toxoplasmosis(弓形虫病). General properties of Macrolides
General properties of Macrolides 6. Adverse response: 1)G Effects: nausea, vomiting, abdominal cramps(痉享)… 2)Liver Toxicity: Cholestatic hepatitis (胆汁淤积性肝炎) 3)Cardiotoxic effects 4)Auditory impairment (ototoxicity) Hypersensitivity reactions Superinfections
6.Adverse response: 1) GI Effects: nausea, vomiting, abdominal cramps(痉挛)… 2) Liver Toxicity: Cholestatic hepatitis (胆汁淤积性肝炎). 3) Cardiotoxic effects 4) Auditory impairment (Ototoxicity) Hypersensitivity reactions Superinfections General properties of Macrolides