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Miscellaneous Antibiotics

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Bactrim, Septra (Trimethoprim+Sulfamethoxazole)   SMX – structural analogue of PABA; blocks production of folic acid TMP – DHFR inhibitor that blocks the conversion of DHF to THF. Together this combination produces a synergistic effect  
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Bactrim, Septra (T+S) PK   Distributes to most tissue/fluid including the CSF & prostate Needs renal adjustment b/c cleared by kidney  
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Bactrim dosing   5:1 ration of SMX to TMP. Dosing based on TMP 80TMP:400SMX is reg. strength tab 160TMP:800SMX is dbl strength tab 16TMP:80SMX/ml IV. Every 10ml IV is like a dbl-strength tab. KNOW HOW TO CONVERT FR ml IV to mg PO! Oral dose is BID. IV is Q6h  
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Bactrim (Septra) SoA   G+: S. pneumo, not for DRSP; MSSA, Listeria, CA-MRSA on SKIN ONLY (NOT IV HA-MRSA pneumo) G-: E. Coli, UTIs, COPD (H. influ, M. catarrhalis, Kleb) Septra is #1 for: S. maltophila, B. cepacia, Toxoplasmosis, Prostatitis, Shigellosis, CA-MRSA, Nocardi  
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Bactrim dosing (cont'd)   Usual dose: 1 DS BID PCP prophylaxis is 1 DS TIW  
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Bactrim ADRs   NV Insoluble, crystallization sun sensitivity -> rash/allergy hypo/hyperglycemia hyperK with IV Pancreatits, Hepatitis Blood dyscrasias teratogenic  
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Bactrim DDIs   Warfarin: check INR (increases) - more bleeds MTX (methotrexate) is displaced Increases hypoglycemic effect of sulfonylureas  
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Clindamycin (Cleocin) PK & MoA   Static, 50s ribosomal protein synthesis inhibitor Penetrates most tissue well except CSF Accumulates in Segs/Macs and in abscessed tissue Above diaphragm anaerobic agent Main antibiotic implicated in C. dif colitis  
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Clindamycin SoA   Oral anaerobes, abscess Abdominal C. diff, C. perfringens, and B. Fragilis Used topically for acne If PCN allergy, good for Staph, MSSA, Strep G. vaginalis (G- rod, facultative anaerobe, vaginitis) dental prophy NOT for enterococcus  
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Clindamycin ADRs   AAD (C. diff) Metabolizes to benzyl alcohol. If used in kids, monitor conc to avoid seizures. Bitter taste Prolongs NMJB (neuromuscular junction blockers) - reverse w/ pancuronium Dizziness & HA  
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Metronidazole (Flagyl) PK & MoA   Mainly used for anaerobes BELOW diaphragm (but active above as well. Cidal mostly No activity against aerobes (req anoxic pore to enter organism) Penetrates all tissues and fluids  
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Metronidazole (Flagyl) SoA   Best for anaerobic C. diff, B. frag IA infections Trichomonas, Giardia, Entamoeba, Gardnerella, H. pylori  
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Metronidazole (Flagyl)   Contraindicated in pregnancy and nursing moms nasty metallic taste (take with snack) Dizziness, HA, rarely -seizures, neuropathy, tingling, numbness Pancreatitis dark urine  
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Metronidazole (Flagyl) interactions   Warfarin (increased conc. more bleeding risk) Alcohol (disulfiram rxn like Antabus) *Avoid in alcholics! Light - degrades Flagyl and makes it browner  
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Nitrofurantoin (MacroBID, Macrodantin) uses & SoA   UTI Tx or prophylaxis E. coli, S. sap, E. faecalis, Group B Strep (prenatal)  
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Nitrofurantoin (MacroBID, Macrodantin) MoA & PK   Binds to ribosomal protein, damages DNA May antagonize quinolone activity when Tx G- absorbed in small intestine Excretion decreases in proportion w/ ClCr decreases Macrocrystal helps w/ absorption. Causes dark brown feces Not given to kids  
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Nitrofurantoin (MacroBID, Macrodantin) ADRs   Pulmonary rxns (asthma-like, SOB, fibrosis) Diarrhea Elevated LFTs G6PD deficiency -> anemia peripheral neuropathy discolors urine orange/brown  
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Colistin (Colistimethate sodium, Coly-Mycin) MoA & PK   Cidal Cationic polypeptide polymixin - detergent-like mechanism which interferes with cytoplasmic membrane of G- organisms Removed by GFR almost completely unchanged Concentration dependent  
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Colistin SoA   G-: mostly used for MDR (multidrug resistant) Pseudomonas, Kleb, Acinetobacter, Enterbacteria, E. Coli Proteus, Providencia, Serratia, Burkholderia, Stenotropheomonas Only drug that works for NMD1 beta-lactamases!! NOT for anaerobes  
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Colistin ADRs   nephrotoxicity neurotoxicity respiratory arrest, apnea (breathing cessation) w/ IM due to NMJ blockade SEs worse w/ renal dysfxn  
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Metronidazole dose for Trichomoniasis   2g x single dose  
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