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INHIBITORS OF
PEPTIDOGLYCAN
CROSS LINKING
Names
-lactams
penicillins,
cephalosporins,
carbapenems
Mechanism
Bind PBPs (transpeptidases),
block cross-linking of
peptidoglycan activation of
autolytic enzymes. Bactericidal
Bugs
Resistance
1.
monobactam aztreonam
2.
3.
4.
-LACTAM:
PENICILLINS
Bacteriocidal
Same
Penicillin G
Streptococci
S pneumo - resistance
Meningococci
Treponema pallidum
Actinomyces
Penicillinase a type of
lactamase
Toxicity
Hypersensitivity with a range of
manifestations urticarial skin rash is
common, but anaphylaxis is possible
IgE mediated rapid onset,
anaphylaxis, angioedema,
laryngospasm
IgM and IgG antibodies fixed to
cells vasculitis, neutropenia,
positive Coombs test
Immune complex formation
vasculitis, serum sickness (fever,
urticaria, proteinuria, arthralgia,
lymphadenopathy 5-10 days after
starting the drug), interstitial nephritis
T cell mediated urticarial and
maculopapular rashes, Sevens
Johnson syndrome
Notes
Most are eliminated
through the kidney
except nafcillin and
oxacillin are eliminated in
bile (N and O say NO to
the kidney!)
Hemolytic anemia
Penicillin V
Streptococci and oral
pathogens
Amino-penicillins =
-lactamase-sensitive
penicillins
Ampicillin
Amoxicillin better
oral bioavailability
Same
HELPSS kill enterococci!
Gram positives
Gram postive cocci not staph
Listeria (ampicillin)
Enterococci
-lactamase-resistant
penicillins
Anti-psuedomonals
lactamase inhibitors
Oxacillin
Nafcillin
Dicloxicillin
Methicillin
Ticarcillin
Piperacillin
Same
Clavulanic acid
Sulbactam
Same
Tazobactam
LACTAM CEPHALOSPORINS
Bacteriocidal
1st generation
Cefazolin
Cephalexin
2nd generation
Cefoxitin
Cefaclor
Cefuroxime
3rd generation
Ceftriaxone
Cefotaxime
Ceftazidime
4 generation
Cefepime
5th generation
Ceftaroline
th
Ceftriaxone meningitis,
gonorrhea, and
community acquired
pneumonia. Largely
elimated in bile.
Ceftazidime
pseudomonas
Doesnt cover
psuedomonas
CARBAPENEMS
Bactericidal
IV ONLY
MONOBACTAMS
Bactericidal
IV ONLY
INHIBITORS OF
PEPTIDOGLYCAN
SYNTHESIS
VANCOMYCIN
Bactericidal
PROTEIN SYNTHESIS
INHIBITORS 30S
SUBUNIT
AMINOGLYCOSIDES
Bactericidal
TETRACYCLINES
Bacteriostatic
Imipenem
Meropenem
Ertapenem
Doripenem
Wide spectrum
Gram positive cocci
Gram negative rods - including
pseudomonas (ertapenem has
pseudomonas coverage)
Risk of seizures limits use to life- Anaerobes
threatening infections
Aztreonam
Vancomycin
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin
Tetracycline
Doxycycline
Minocycline
CLINDAMYCIN
Chloramphenicol
Not 1st line for
anything in
developed countries!
Clindamycin
PROTEIN SYNTHESIS
INHIBITORS 50S
SUBUNIT
CHLORAMPENICOL
Bacteriostatic
No cross-allergenicity with
penicillins or cephalosporins!
Drug inactivation by
acetylation,
phosphorylation, or
adenylation
Nephrotoxicity
Ototoxicity
Hypotension
Thrombophlebitis
Red man syndrome diffuse
flushing. Prevent with antihistamines
and slow infusion rate
Borrelia burdorferi
Mycoplasma pneumonia
Rickettsia and chlamydia
(reaches high intracellular
concentrations)
Acne
Doxycycline prostatitis,
reaches high concentrations
Minocycline meningococcus
carrier states
Renal elimination
Synergistic with
lactams for enterococci
(penicillin G or ampicillin)
and pseudomonas
(extended spectrum)
Neomycin for bowel
surgery
Blocks peptidyltransferase,
Meningitis H influenza, N
meningitidis, S pneumo
Rocky mountain spotted fever
(Rickettsia rickettsi)
Drug inactivation by
acetyltransferase
encoded by plasmids
Bacteriostatic
diaphragm - aspiration
pneumonia, lung abscesses,
and oral infections
(bacteroides, clostridium
perfringens, peptostreptococcus,
fusobacterium, prevotella)
staph with
difficile
erythromycin if
Fever
erythromycin resistant, Diarrhea
will quickly gain
resistance to
clindamycin!
Metronidazole for
anaerobes below the
diaphragm
MACROLIDES
Bacteriostatic
Azithromycin
Clarithromycin
Erythromycin
Same as clindamycin
(macroslides). Bind to the 23S
rRNA of the 50s subunit
Atypical pneumonias
mycoplasma (including avium),
chlamydia, legionella
STDs chlamydia
Gram positive cocci
streptococcal infections in
patients allergic to penicillin
Methylation of target
site on 23S rRNA
prevents drug binding
MACRO:
Motility issues
Arrhythmia by QT
Acute cholestatic hepatitis
Rash
eOsinophilia
serum concentration of
theophyllines, oral anticoagulants
Can cause serotonin syndrome
Clarithromycin
combine with
metronidazole and PPI in
triple therapy for H pylori
Azithromycin
prophylaxis in AIDS for
Mycobacterium avium
(CD4 < 50)
LINEZOLID
Bacteriostatic (usually)
Linezolid
Very rare
STREPTOGRAMINS
Bacteriostatic alone,
Bacteriocidal together
Quinupristin
Dalfopristin
Inactivating enzymes,
efflux
Sulfamethoxazole
Sulfisoxazole
Sulfadiazine
Sulfasalazine
Gram positives
Gram negatives
Nocardia
Chlamydia
Triple sulfas or Bactrim for UTI
Altered enzyme,
uptake, or PABA
synthesis
Hypersensitivity
Hemolysis if G6PD deficient
Nephrotoxicity tubulointerstitial
nephritis
Photosensitivity
Displace bilirubin and other drugs
from albumin e.g., warfarin;
kernicterus in infants and
pregnancy
Stevens Johnson syndrome
Sulfasalazine ulcerative
colitis
Altered dihydrofolate
reducatase
TRIMETHOPRIM
Bacteriostatic
Trimethoprim
Usually combined w/
trimethoprim to avoid resistance
Bactrim:
UTIs
Shigella and salmonella
Pneumocystis jirovecii disc
shaped yeast, causes interstitial
pneumonia in AIDS
Pneumonia treatment and
prophylaxis
Toxoplasmosis prophylaxis
DNA TOPOISOMERASES
FLOUROQUINOLONES
Bactericidal
Ciprofloxacin
Norfloxacin
Levofloxacin
Oflofloxacin
Sparfloxacin
Moxifloxacin
Gemifloxacin
Enoxacin
Mutation in DNA
gyrase (topoisomerase
II) encoded by
chromosome.
More common
GI upset
Superinfections
Skin rashes
Headache, dizziness
Rare
Tendonitis, tendon rupture (esp >
60 yrs, taking prednisone), leg
cramps, myalgias
QT
Contraindicated in pregnant women,
nursing moms, and kids under 18 yrs
due to possible damage to cartilage
QUINOLONE
Nalidixic acid
DAMAGES DNA
METRONIDAZOLE
Bacteriocidal
Antiprotozoal
Metronidazole
Isoniazid
RIFAMYCINS
Rifampin
Rifabutin
PYRAZINAMIDE
Pyrazinamide
Acidifies intracellular
environment by conversion to
pyrazinoic acid effective in
acidic pH of phagolysosome,
where TB engulfed by
ANTIMYCOBACTERIAL
DRUGS
ISONIAZID
TB
Leprosy delays resistance to
dapsone
Can use for prophylaxis with
Neisseria meningitidis or
exposure to kids with H
influenza. But ciprofloxacin is
the drug of choice for
menginococcal prophylaxis)
TB
Enzyme alteration
Hyperuricemia
Hepatotoxicity
4 Rs of Rifampin
1. RNA polymerase inhibitor
2. Ramps up microsomal
P450
3. Red/orange body fluids
4. Rapid resistance if used
alone
ETHAMBUTOL
Ethambutol
macrophages is found
carbohydrate polymerization
of mycobacterium cell wall by
blocking arabinosyltransferase
TB
Antifungal Drugs
Drug Class
POLYENES
Names
Amphotericin
B
Mechanism
Binds ergosterol and forms membrane
pores leakage of electrolytes.
Unfortunately also binds cholesterol to a
lesser degree toxicity
Poor penetration into CNS combine w/
flucytosine for cryptococal meningitis
Nystatin
TRIAZOLES
Fluconazole
Ketoconazole
Clotrimazole
Miconazole
Itraconazole
Voriconazole
PYRIMIDINES
Flucytosine
ECHINOCANDIN
S
Caspofungin
Micafungin
Anidulafungin
Terbinafine
TERBINAFINE
Dermatophytes
GRISEOFULVIN
Dermatophytes
Griseofulvin
Use
Serious, systemic mycoses
Cryptococcus neoformans,
candida +/- flucytosine for
meningitis
Mucor
Aspergillis
Blastomyces, coccidiodes
histoplasma
Resistance
Toxicity
Low ergosterol
Caused by cholesterol binding:
content in cell Fever & chills
membranes
Hypotension
Nephrotoxicity because GFR - w/
hydration
Hypomagnesemia, hypokalemia in most
pts altered permeability of renal tubules
Arrhythmias
Anemia - renal EPO
IV phlebitis
Resistance is
fast if used solo
Notes
Give intrathecally for fungal
meningitis
Give w/ K+ and Mg2+
Drug Class
Inhibit
release of
viral progeny
Name
Zanamivir
Oseltamivir
Mechanism
Inhibit influenza neuraminidase to release of progeny
virus
Use
Influenza A and B
(orthomyxyviruses)
Inhibit nucleic
acid
synthesis
Ribavarin
RSV
Chronic Hep C
Acyclovir
Famcyclovir
Valacyclovir
Gancicyclovi
r
Foscarnet
Cidofovir
Inhibit viral
protein
synthesis
Interferon
Resistance
Toxicity
Hemolytic anemia
Severe teratogen makes sense
b/c human cells use IMP
dehydrogenase to make GMP
Must be adequately hydrated!
Risk of obstructive crystalline
nephropathy and acute renal
failure!
Notes
Amantidine and rimantidine
used to inhibit influenza
uncoating no longer used
b/c of resistance
Renal toxicity
More toxic to host enzymes than
acyclovir:
Leukopenia
Neutropenia
Thrombocytopenia
Nephrotoxicity
Nephrotoxicity coadminister with
probenicid and IV saline to
Neutropenia
Myopathy
Valgancyclovir is a prodrug
with better
Drug class
Nucleoside
Reverse
Transcriptase
Inhibitors
Drug Names
Nucleosides:
Lamivudine
Stavudine
Zidovudine
Emtricitabine
Didanosine
Abacavir
Mechanism
Competitive inhibition of nucleotide binding to reverse
transcriptase terminates DNA chain (lacks 3 OH group)
The nucleosides need to be phosphorylated for activity, tenofovir
doesnt.
Use
Toxicity
CHOOSE 2 for part 1 Bone marrow suppression reverse
of triple therapy
with G-CSF and EPO!
Peripheral neuropathy
Nucleosides lactic acidosis
Nucleotides rash
Zidovudine anemia
Didanosine - pancreatitis
Notes
Choose 2, then use with 2 out of 3:
NNRT, protease inhibitor, integrase
inhibitor
Nucleotide:
Tenofovir
Non-nucleoside
Reverse Transcriptase
Inhibitors
Efavirenz
Nevivirapine
Delavirdine
Protease
Inhibitors
-navir
Atazanavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Ritonavir
Saquinavir
Integrase
Inhibitor
Raltegravir
Fusion
Inhibitor
Enfuvirtide
Maraviroc
Nephropathy
Hematuria - idinavir
Rash
Hepatotoxicity
Efavirenz CNS symptoms and rash,
avoid in pregnancy
Delavirdine avoid in pregnancy
Hyperglycemia
GI intolerance nausea, diarrhea
Lipodystrophy
Hypercholesterolemia
Psuedomonas
Bug
Treatment
Ticarcillin, pipercillin, cefepime 4th generation, ceftazidime 3rd
generation, aminoglycosides, others?
MRSA
VRE
Notes
PROTOZOA
Toxoplasmosis
Trypanosoma brucei
Trypanosoma cruzi
Nifurtimox
Leishmaniasis
Sodium stibogluconate
PLASMODIA
Plasmodium vivax, ovale, malariae
Chloroquine.
If life threatening quinidine in the US, quinine elsewhere, or artesunate
Plasmodium falciparum
Artemether/lumefantrine or atovaquone/proguanil
If life threatening quinidine in the US, quinine elsewhere, or artesunate
HELMINTHS
Nematodes (round worms): Enterobius vermicularis (pinworm), ascaris
lumbricoides (giant roundworm), ancylostoma duodenale
Praziquantel
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