Term
What is the MOA of macrolides |
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Definition
Binds to 50s ribosomal subunit
1. Inhibits the translocation of tRNA from A site to P site
2. It inhibits peptidyltransferase from forming peptide bonds between AA |
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Term
Give examples of Macrolides (drug names) |
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Definition
Erythromycin
Azrithromycin
Clathromycon
Lincomycin
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Term
How is resistance developed against macrolides? |
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Definition
1. Efflux pump
2. Methylase enzyme
3. Mutation in 50s ribosomal subunit |
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Term
WHat is the spectrum of action of Macrolides? |
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Definition
1. Gram - ve
2. Some gram +ve
3. ATYPICAL BACTERIA - chlamydia, legionella, Mycobacterium avium complex (MAC), campylobacter |
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Term
What macrolides are used to treat Mycobacterium avium complex? (MAC) |
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Definition
Azithromycin
Clarithromycin |
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Term
What are the ADR's of Macrolides? |
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Definition
1. Diarrhoea - activation of motilin receptors
2. Cholestatic hepatits (erythromycin)
3. Thrombophlebitis (Erythromycin & Azithromycin)
4.CYP450 inhibitors - (erythromycin & clarithromycin) increase toxicity of theophylline, digoxin, phenytoin, carbamezapine, valporic acid, cyclosporin, terfenadine, astemizole, cispride & warfarin |
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Term
What are the ADR's of erythromycin |
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Definition
Thrombophlebitis
Choloestatic hepatitis
CYP450 inhibitor
Diarrhoea (motilin receptor stimulation) |
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Term
What macrolides cause Cholestatic hepatitis? |
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Definition
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Term
What macrolides cause thrombophlebitis? |
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Definition
Erythromycin & Azithromycin |
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Term
WHat macrolides inhibit the CYP40 enzyme..
what drugs and what effect do they have? |
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Definition
Erythromycin & clarithromycin
increase the toxicity of
warfarin, cyclosporin, digoxin, phenytoin, carbamezapine, valporic acid, theophylline, terfenadine, astemizole & cisapride |
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Term
What macrolide is used to treat H.pylori |
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Definition
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