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med chem nucleic acid synthesis inhibitors


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Nucleic acid synthesis inhibitors moa
inhibtion of DDRP (transcription)
What type of enzyme is DDRP
Zn++ metalloenzyme
Term used to describe nucleic acid synthesis inhibitors
ansamacrolides (macrocyclic lactams)
NASI cidal or static
NASI side effects
hepatotoxicity, inducer of CYPs
NASI metabolism
deacetylation, oxidation of hydroquinone to quinone, hydrolysis of imine side chain

excreted via bile, enterohepatic recirculation
NASI use
mycobacterium avium complex (MAC)
Nicotinamide analogs (INH, PZA) mechanism of action
inhibtion of mycolic acid synthesis (INH inactivates enzyme Inh A) and incorporation (oxidation products of agents KatG)
Nicotinamide analog cidal or static
Nicotinamide analog side effects
peripheral neuritis (use pyridoxine)

hepatotoxicity, GI upset
Nicotinamide analog metabolism
acetylation of INH, hydrolysis and oxidation of PZA
PABA antimetabolits- salts or esters of p-aminosalicylic acid cidal or static
PABA antimetabolits- salts or esters of p-aminosalicylic acid pharmacokinetic consideration
competition for acetylation with isoniazid increases the t1/2 of isoniazid
PABA antimetabolits- salts or esters of p-aminosalicylic acid metabolism
glycine conjugate, acetylation, excreted unchanged
PABA antimetabolits- salts or esters of p-aminosalicylic acid side effects
GI upset
Oxazolidinone-Linezolid mechanism of action
inhibits PS by binding to 23S fragment of 50S ribosomal subunit and preventing the formation of the initiation complex
Oxazolidinone uses
bacteremia, nosocomial and CAP, and complicated & uncomplicated skin and skin structure infections caused by:

c)S. agalactiae
d)S. pyogenes
e)S. pneumoniae (pen susc. only)
Linezolid active against:
a)E.faecalis (VSE,VRE)
b)E. faecium (VSE)
c)staph epidermidis
d)staph haemolyticius
e)strep pneumoniea
f)strep viridans
Oxazolidinone metabolism
Non-CYP mediated
-oxidation of morpholine ring positions 2 or 3 w/ subsequent ring opening

-oxidation of resulting aldehyde to carboxylic acid
Oxazolidinone interactions
reversible, non-selective MAOI
b)adrenergic agonists (dopaminergic agents)
-increase pressor response w/ pseudoephedrine and PPA
c)tyramine-containing foods

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