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Antimetabolites, Nucleic acid Synthesis Inhibitors Cheat Sheet by

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SULFON­AMIDES

MOA
Mammalian cells lack dihydr­opt­eroate synthase and require exogenous sources of folate. Inhibiting synthesis of folic acid (folate), a compound required by all cells to make DNA, RNA, and proteins
PK
Absorbed from the stomach and small intest­ines, widely distri­buted to tissues and body fluids (CNS, CSF, placenta, fetus)
Excreted unchanged into the urine.
Eliminated by glomerular filtration and breast milk.
AE
Crysta­lluria, hypers­ens­iti­vity, hemato­poietic distur­bances (hemolytic anemia), kernic­terus
CONTRA
Pregnant women, children <2 mo old

SULFON­AMIDES

ORAL, NONABS­ORB
 
SULFAS­ALAZINE
ORAL, ABSORB­ABLE
SHORT
SULFAC­YTINE
 
SULFIS­OXAZOLE
Indi­cat­ions: UTI
 
FULFAM­ETH­IZOLE
INTERM
SULFAD­IAZINE
Indi­cat­ions: 1st line for acute toxopl­asmosis
 
SULFAM­ETH­OXAZOLE
Indi­cat­ions: UTI
 
SULFAP­YRIDINE
LONG
SULFAD­OXINE
Indi­cat­ion: 2nd line for malaria
TOPI­CAL
 
SODIUM SULFAC­ETAMIDE
 
MAFENIDE ACETATE
 
SILVER SULFAD­IAZINE
Sulf­adi­azine and sulf­ado­xone are used in combo with pyrime­­th­amine

DHFR INHIBITORS

TMP/SMX
Drug of choice for infections such as Pneumo­cystis jiroveci pneumonia, toxopl­asm­osis, nocard­iosis, and occasi­onally other bacterial infections
TRIMET­HOPRIM
UTI
PYRIMETHAMINE
Parasitic
AE: megalo­blastic anemia, leukop­enia, granul­ocy­topenia
 

FLUORO­QUI­NOLONES

MOA
Inhibit one or both of the 2 prokar­yotic type II topois­ome­rases
PK
Well absorbed, widely distri­buted in body fluids and tissues
Excreted really
INDICATIONS
Resistant respir­atory infect­ions, anthrax, gonorrhea, UTI and bacterial diarrhea caused by shigella, salmon­ella, toxigenic E coli, and campyl­obacter
AE
NVD, HA, dizziness, photot­oxic, connective tissue problems
BBW
Tendin­itis, tendon rupture
CONTRA
Avoid in pregos, nursing mothers, and children <18
DDI
THEOPH­YLLINE, WARFARIN, CYCLOS­PORINE
Concen­tra­tio­n-d­epe­ndent killing

FLUORO­QUI­NOLONES

NALIDIXIC ACID
NORFLO­XACIN
OFLOXACIN
CIPROFLOXACIN
No longer recomm­ended for gonococcal in the US
Indi­cat­ions: chlamydial urethr­itis, cervicitis
LEVOFL­OXACIN
No longer recomm­ended for gonococcal in the US
Indi­cat­ions: chlamydial urethr­itis, cervicitis
QD, long t1/2
MOXIFL­OXACIN
Only one not effective in UTI's
QD, long t1/2
Cont­ra: puts predis­posed to arrhyt­hmias or pts that are taking anti arrhythmic meds due to QT prolon­gation

METHEN­AMINE

MOA
Metabo­lized to formal­dehyde and ammonia in acidic pH. The formal­dehyde is lethal to bacteria.
INDICATION
Urinary tract antise­pti­cs/­ant­imi­cro­bials
SIDE EFFECTS
GI distress, may cause albumi­nuria, hematuria, and rashes at higher doses
CONTRA
Pts with renal insuff­iciency
 

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  • Published: 11th September, 2017
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