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20 Cards in this Set
- Front
- Back
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Nucleic acid synthesis inhibitors moa
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inhibtion of DDRP (transcription)
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What type of enzyme is DDRP
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Zn++ metalloenzyme
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Term used to describe nucleic acid synthesis inhibitors
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ansamacrolides (macrocyclic lactams)
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NASI cidal or static
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cidal
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NASI side effects
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hepatotoxicity, inducer of CYPs
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NASI metabolism
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deacetylation, oxidation of hydroquinone to quinone, hydrolysis of imine side chain
excreted via bile, enterohepatic recirculation |
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NASI use
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mycobacterium avium complex (MAC)
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Nicotinamide analogs (INH, PZA) mechanism of action
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inhibtion of mycolic acid synthesis (INH inactivates enzyme Inh A) and incorporation (oxidation products of agents KatG)
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Nicotinamide analog cidal or static
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cidal
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Nicotinamide analog side effects
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peripheral neuritis (use pyridoxine)
hepatotoxicity, GI upset |
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Nicotinamide analog metabolism
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acetylation of INH, hydrolysis and oxidation of PZA
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PABA antimetabolits- salts or esters of p-aminosalicylic acid cidal or static
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static
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PABA antimetabolits- salts or esters of p-aminosalicylic acid pharmacokinetic consideration
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competition for acetylation with isoniazid increases the t1/2 of isoniazid
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PABA antimetabolits- salts or esters of p-aminosalicylic acid metabolism
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glycine conjugate, acetylation, excreted unchanged
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PABA antimetabolits- salts or esters of p-aminosalicylic acid side effects
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GI upset
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Oxazolidinone-Linezolid mechanism of action
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inhibits PS by binding to 23S fragment of 50S ribosomal subunit and preventing the formation of the initiation complex
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Oxazolidinone uses
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bacteremia, nosocomial and CAP, and complicated & uncomplicated skin and skin structure infections caused by:
a)VREF b)MSSA, MRSA c)S. agalactiae d)S. pyogenes e)S. pneumoniae (pen susc. only) |
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Linezolid active against:
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a)E.faecalis (VSE,VRE)
b)E. faecium (VSE) c)staph epidermidis d)staph haemolyticius e)strep pneumoniea f)strep viridans g)pasteurella |
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Oxazolidinone metabolism
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Non-CYP mediated
-oxidation of morpholine ring positions 2 or 3 w/ subsequent ring opening -oxidation of resulting aldehyde to carboxylic acid |
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Oxazolidinone interactions
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reversible, non-selective MAOI
a)SSRIs b)adrenergic agonists (dopaminergic agents) -increase pressor response w/ pseudoephedrine and PPA c)tyramine-containing foods |
