Antimicrobials

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Created by:

m_s_c  on March 24, 2012

Subjects:

usmle, microbiology, pharmacology

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Antimicrobials

Penicillin
Block cell wall synthesis
Gram positives
tox: allergy, hemolytic anemia
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Penicillin Block cell wall synthesis
Gram positives
tox: allergy, hemolytic anemia
Methicillin, nafcillion, oxacillin, dicloxacillin Penicillinase resistant
"Use NAF for STAPH"
Staph MET a NAsty Ox
Only a matter of time - CLOX are oral
S. aureus (not MRSA)
tox: Allergic, Methicillin-interstitial nephritis
Ampicillin, amoxicillin AMPed up Penicillins
amOxicillin Oral
Amp HELPSS kill enterococci
H. influenza, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella
tox: Hyper, Ampicillin rash, Pseudomembranous colitis
Resis: Beta lactamases cleave ring
Ticarcillin, carbenicillin, pipercillin Anti-pseudomonas
Bond brings: Ticks, Car, and Pipe bomb to kill Pseudomonas
TCP: Takes Care of Psedomonas
tox: hsr
Beta lactamase inhibitors the helper CAST
Clavulanic Acid, Sulbactam, Tazobactam
amox+clavulanate
ticar+ clavulanate
ampi+ sulbactam
piper+tazobactam
Cephalosporins Orgs not covered are LAME:
Listeria, Atypicals (chlamydia, mycoplasma), MRSA, Enterococci
Inhibit cell wall synthesis, less susceptible to penicillinases
tox: hsr, vit K def, inc. nephrotoxicity of aminoglycosides, disulfiram-like rxn w/ ethanol, cross-hsr w/ penicillins
Renal excretion
1st Gen Cephalosporins Gram Pos.
PEcK: Proteus mirabilis, E. coli, Klebsiella pneumoniae
PH in name: cephalothin, cephapirin, cephradine, cephalexin, cefazolin, cefadroxil
2nd Gen cephalosporinsGram pos cocci
HEN PEcKS: H. influenzae, Enterobacter aerogens, Neisseria, Proteus mirabilis, E. Coli, Klebsiella pneumo, Serratia marcescens
MMT side chain (cefamandole, cefmetazole, cefotetan) vit K, alcohol
FAMily of FURry FOXes I MET drinks TEa
ceFAMandole, ceFAclor, ceFURoxime, ceFOXitin, cefMETazole, cefoTEtan, cefonicid, loracarbef, cefdinir
3rd gen cephalosporins Ceftriaxone- meningitis and gonorrhea
Ceftazidime- pseudomonas
Serious gram neg infxns
MMT side chain: cefoperazone (vit K & alc)
4th gen cephalosporins Cefepime- PINED for the 4th gen
Inc act against pseudomonas and gram Pos.
Aztreonam Inhibits cell wall synthesis
IV or IM, Renal excrete
Gram neg rods only (penicillin allergies)
*magic bullet for gram negs
tox: occ GI upset
Carbepenams
Imipenam/ Cilastatin, Meropenam
Inhibits cell wall synth
Gram pos cocci, gram neg rods, anaerobes
"I'm a pen crossing out all bacteria"
Limit to life-threatening/ resistant orgs
tox: GI distress, skin rash, CNS toxicity (seizures) - renal excretion
Meropenam: red risk of seizures
Vancomycin Inhibits cell wall mucopeptide formation (D-ala D-ala)
Gram pos- S. aureus, enterococci, C. diff
tox: NOT many probs
Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing "red man" syndrome (use antihistamines)
Resistance: D-ala to D-lac
Protein synthesis inhibitors CLEan TAG
50s: Chloramphenicol, Clindamycin, Linezolid, Erythromycin
30s: Tetracyclines, AminoGlycosides
A
Aminoglycosides Mean GNATS canNOT kill anaerobes
Gentamycin, Neomycin, Amikacin, Tobramycin, Streptomycin
tox: Nephrotoxicity, Ototoxicity, Teratogen
moa: inh initiation complex
use: gram neg rod- synergy w/beta lactam
neomycin- bowel surgery
IV or IM (not oral)
res: transferase enzymes inactivate
TetracyclinesDems stop bloating
Demeclocycline- ADH antagonist (SIADH)
tetracyclin, doxycycline, minocycline
bind 30s, inhibit aminoacyl-tRNA
RICK Cleans his BLEhMp
use: rickettsia, chlamydia, Borrelia & Leptospira, M. pneumoniae, E. histolytica
tox: GI distress, Photoxic Dermatitis, renal (Fanconi) & hepatotox
Teratogen: Ca chelator efx bones and teeth dark
Macrolides erhythromycin, azithromycin, clarithromycin
Inhibit protein synth 50s subunit
clin: Atyp pneumo (Myco, Legion, Chlam), URIs, STDs, gram+ cocci, Neisseria
tox: prolonged QT, GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rash, Inc conc of anticoags & theophyllines
resis: methylation of 23S rRNA binding
Chloramphenicol Blocks 50s. bacterial static
CHLORox turns SHiNs gray
Meningitis "SHiN" (S. pneumo, H. influenza, N. meningitidis)
tox: anemia, aplastic anemia, gray baby (40% fatal)
res: acetyltransferase inact. drug
Clindamycin blocks 50s, bacteriostatic
Anaerobic (bacteroides, C. perfringens) in aspiration pneumonia or lung abscess
"Clean above METRO below"
tox: Pseudomembranous colitis (C. dif), fever, diarrhea
Sulfonamides Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine
moa: PABA, inh Dihydropteroate Synthetase
clin: gram+, gram-, Norcardia, Chlamydia
tox: hsr, Hemolysis if G6PD, Tubulointersitial nephritis, photosens, kernicterus (infants), displace rx albumin
res: Altered enzyme, dec uptake, in PABA
TMP SMX Trimethoprim/Sulfamethoxazole (Bactrim)
TMP Smx
Tree: resp tree: S. pneumo, H. influenzae (otitis media, sinusitis, bronchitis, pnumo)
Mouth: GI tract, gram negs cause diarrhea, Shigella, Salmonella, E. coli
Pee: GU tract, UTIs, prostatitis, urethritis by Enterics, N. gonorrhoeae, Chlamydia
Syndrome: AIDS, prevent PCP w/CD4<200
Trimethoprim Inh bacterial Dihydrofolate Reductase
TMP= Treats Marrow Poorly
tox: megaloblastic anemia, leukopenia, granulocytopenia [treat w/ folinic acid]
FluoroquinolonesCiprofloxacin, norfloxacin, levofloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin
fluoroquinoLONES hurt BONE attachment
Inh DNA Gyrase, not with antacids
Gram-neg rods of GI and GU (inc Pseudomonas), Neisseria, some gram pos
tox: GI sx, skin rash, cartilage, achilles tendonitis, headache, dizzy
res: mutation DNA gyrase
Metronidazole GET GAP on the Metro
Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes (bacteroides, C diff) H. Pylori
moa: free radical toxic metabolites
tox: rxn w/alcohol, headache, metal taste
Antimycobacterial drugs TB treatment RIPE-Rifampin, Isoniazid, Pyrazinamide, Ethambutol
Prophylaxis:
M.Tuberculosis: Isoniazid
M. avium-intercellulare: Azithromycin
Isoniazid (INH) INH- Injures Neurons and Hepatocytes
moa: dec synth mycolic acids
tox: neurotox, hepatotox, lupus
Pyroxidine(B6) can prevent tox
Rifampin 4 Rs: RNA polymerase inh
Revs up microsomal P-450
Red/orange body fluids
Rapid resistance (if used alone)
use: TB, meningococcal prophylaxis H. Influenza type B
tox: minor hepatotox, inc P-450
Pyrazinamide Inh mycolic acid blocking Pyrazanamide
TB
tox: hyperuricemia, hepatotox
Ethambutol Dec carb polymerization of cell wall, blocks arabinosyltransferase
tox: Optic neuropathy (red-green color blindness)
Antimicrobial prophylaxis Meningitis - Ciprofloxacin, rifampin, minocycline
Gonorrhea- Ceftriaxone
Syphilis- benzathine penicillin G
recurrent UTIs: TMP-SMX
Endocarditis w/procedures- penicillins
HIV prophylaxis CD4<200: TMP-SMX *PCP
CD4<100: TMP-SMX *PCP, toxoplasmosis
CD4<50: Azithromycin *mycobacterium avium
Treat resistant bacteria MRSA- vancomycin
VRE- linezolid, streptogamins (quinupristin/dalfopristin)
Empiric therapy community-acquired pneumonia outpatient: Macrolides
inpatient: Fluoroquinolones
ICU setting: Beta-lactam + (fluoroquinolones OR azithromycin)
Amphotericin B "tears" holes in the fungal membrane
moa: binds Ergosterol, pores
clin: Serious Systemic mycoses
cryptococcus, blastomyces, coccidioides, aspergillus, histoplasma, candida, mucor
tox: 1. Nephrotoxic 2. Acute febrile rxn 3. Anemia 4. Phlebitis at IV site
Nystatin "tears" holes in the fungal membrane
moa: binds Ergosterol, pores
Only topical- too toxic for systemic
clin: "swish and swallow" oral candida
Topical diaper rash or vaginal
AzolesFluconazole, Ketoconazole, Clotrimazole, Miconazole, Itraconazole, Voriconazole
moa: inh p450 to convert lanosterol to ergosterol
use: Systemic mycoses.
Fluconazole: Cryptococcal meningitis in AIDS, Candidal infxns
Ketoconazole: blasto, coccidioides, histo, candida, hypercortisolism
Clotrimazole & Miconazole: topical fungal
tox: N&V, anorexia, Hepatotoxic,
Inh P450 causes: gynecomastia, impotence, dec sex drive & sperm
Flucytosine Inh DNA synth- cytosine deaminase
clin: systemic fungal w/ Amp B
tox: N&V, diarrhea, bone marrow supp.
Caspofungin Inh cell wall synth- Inh beta glucan
clin: Invasive aspergillosis, Candida
tox: GI upset, flushing
Terbinafine Inh enzyme squalene epoxidase
clin: Dermatophytoses esp onychomycosis (nails)
tox: abnormal LFTs, visual probs
Griseofulvin Inh microtubule func, disrupts mitosis
clin: oral for superficial infxns, inhibits dermtophytes (tinea, ringworms)
tox: Teratogen, carcinogen, confusion, headaches, inc p450 and warfarin metab
Chloroquine Blocks plasmodium heme polymerase
clin: Plasmodium species
Mefloquine, Quinine (resistant) w/ Pyrimethamine/Sulfonamide
tox: Retinopathy, G6PD hemolysis
Antiprotozoan drugs Pyrimethamine: Toxoplasmosis or P. falciparum
Suramin/Metarsoprol: Trypanosoma brucei
Nifurtimox: T. cruzi
Sodium stibogluconate: Leishmaniasis
Protease inhibitors NAVIR (never) TEASE a proTEASE
Protease cleaves HIV mRNA into func parts
Ritonavir: Inh P450, inc other drugs
tox: hyperglycemia, GI probs, lipodystrophy
NRTIs Inh nucleotide binding to reverse transcriptase and terminate DNA. Need thymidine kinase to activate.
ZDV prophylaxis and during pregnancy
tox: bone marrow supp, peripheral neuropathy, lactic acidosis, rash, megaloblastic anemia (ZDV)
nNRTIs Inhibit reverse transcriptase
tox: bone marrow supp, peripheral neuropathy, lactic acidosis, rash, megaloblastic anemia (ZDV)
Integrase inhibitors Raltegravir
moa: Inh HIV integration into host chromosome- reversibly inh integrase
tox: hypercholesterolemia
Antibiotics to avoid in pregnancyCountless SAFe Moms Take Really Good Care
Clarithromycin- embryotoxic
Sulfonamides- kernicterus
Aminoglycosides- ototoxicity
Fluoroquinolones- cartilage, damage
Metronidazole- mutagenesis
Tetracyclines: color teeth, inh bone growth
Ribavirin- teratogenic
Griseofulvin- teratogenic
Chloramphenicol- "gray baby"
Cephalosporins w/ MMT side chains I MET a PER of MAN with MOXi for TEa with a hangover
cefMETazole, cefoPERazone, cefaMANadole, lataMOXef, cefMenOXime, MOXalactam, and cefoTEtan,

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