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Med Pharm 7/3 Other ICWS and Sulfonamides
Sulfonamides and Other Inhibitors of Cell Wall Synthesis
11
Pharmacology
Professional
03/13/2014

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Term
Vancomycin (Vancocin®)
Definition

Inhibitor of Cell Wall Synthesis

Use: gram+ infections in penecillin allergic pts; PRSA and MRSA; Staph aureus and C dif superinfections

Mechanism: Bactericidal, binds the D-Ala-D-Ala ending of the side peptide of the precursor units of the bacterial cell wall, this inhibits elongation of peptidoglycan chain as well as the transpeptidation of the peptidoglycan chains

Synergistic effect with aminoglycosides, also synergistic tox!

Spectrum: penicilllin-RSA and MRSA

Resistance: Gram - organisms are not sensitive (porin structure may not let large vanco molecules through); Mutation in terminal D-Ala-D-Ala to D-Ala-D-Lactate;

Adverse effects: ototoxicity, nephrotoxic (dropped GFR), "red man" syndrome 

Term
Daptomycin (Cubicin®)
Definition

Inhibitor of Cell Wall Synthesis; lipopeptid Abx

Mechanism: bind to bacterial membranes and cause a rapid depolarization of membrane potential (CW more permeable); Bactericidal against gram+ bacteria

IV administration

excreted unchanged by kidneys

THIS IS ALL YOU NEED TO KNOW FOR THIS DRUG

Term
Fosfomycin (Monurol®)
Definition

Cell wall synth inhibitor

Mechanism: inhibits cell wall synth at one of the first steps in the synthesis of peptidoglycan

Spectrum: active against both gram + and gram - bacteria

Term
Bacitracin
Definition

Abx

Mechanism: interferes with dephosphorylations step in phospholipid carrier cycle (impeded mucopeptide transfer to growing cell wall)

Spectrum: gram +

Tox: rarely used due to serious nephrotoxicity

Term
Cycloserine (Seromycin®)
Definition

Abx

Use: 2nd line in active TB and UTI

Mechanism: inhibits incorporation of D-alanine into bacterial cell walls

Adverse: CNS effects including anxiety, confusion, disorientation c memory loss, depression, dizziness, drowsiness, somnolence, dysarthria, nervousness, headache, hyperrefexia, lethargy, paresthesias, paresis, major and minor clonic seizures, convulsions, tremor, vertigo.

Term
Sulfadiazine
Definition

Sulfonamide

Use: combo with pyrimethamine for tx of toxoplasmosis; UTIs, nocardiosis, toxoplasmosis, trachoma, Pneumocystis jiroveci (carinii)

Mechanism: bacteriostatic; bactericidal concentration for UTIs can be reached; competes with PABA for dihydropteroate synthase (converts to dihydrofolic acid) thereby inhibiting folic acid synthesis; doesn't effect mammallian cells

Bacteria Spectrum: Group A strep, Pneumococci, E. coli, Nocardia, Actinomyces, Chlamydia, pneumocystis jiroveciimalaria

Term
Sulfasalazine (Azulfidine®; SAS 500®)
Definition

Sulfonamide combo

Use: Ulcerative colitis

Metabolized primarily in liver

Term
Silver Sulfadiazine (Silvadene®)
Definition

Topical Sulfonamide

Use: 2nd and 3rd degree burns, 

Bacteria Spectrum: Group A strep, Pneumococci, E. coli, Nocardia, Actinomyces, Chlamydia, pneumocystis jiroveciimalaria

Metabolized primarily in liver

Term
Sulfamethoxazole + Trimethoprim, TMP-SMX
Definition

Sulfonamide combo

Board: Pneumocystis Jirovecii

Use: UTIs, travelers diarrhea Moraxella catarrhalis, P. jiroveci pneumonia, shigellosis, systemic salmonella infections, UTI, prostatitis, nontuberculous mycobacterial infection.

Trimethoprim=inhibits dihydrofolate reductase, can lead to megaloblastic anemia

Bacteria Spectrum: Pneumococcus, Haemophilus species, Moraxella catarrhalis, klebsiella pneumoniae (NOT Mycoplasma pneumoniae)

Metabolized primarily in liver

Term
Co-trimoxazole (Bactrim®, Septra®)
Definition

Sulfonamide combo

Use: UTIs, nocardiosis, toxoplasmosis, trachoma, Pneumocystis jiroveci (carinii)

Bacteria Spectrum: Group A strep, Pneumococci, E. coli, Nocardia, Actinomyces, Chlamydia, pneumocystis jiroveciimalaria

Metabolized primarily in liver

Term
Sulfadoxine + Pyrimethamine (Fansidar®)
Definition

Sulfonamide combo

Use: Presumptive tx of malaria

Mechanism: antagonizes parasitic PABA/inhibits parasitic dihydrofolate reductase respectively

No longer recommended due to possibly fata toxic epidermal necrolysis (TEN)

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