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132 Cards in this Set

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"We're ECSTaTiC about bacteriostatics."
Erythromycin
Clindamycin
Sulfamethoxazole
TMP
Tetracyclines
Chloramphenicol
Bactericidal antibiotics
"Very Finely Proficient At Cell Murder"
Vancomycin
Fluoroquinolones
Penicillin
Aminoglycosides
Cephalosporins
Metronidazole
PCN G is given by this route
IV
PCN V is given by this route
oral
Give 3 mechs of PCN
1. blocks PBP
2. blocks crosslinking of cell wall
3. activates autolytic enzymes
Spectrum of 1st gen PCNs? (x2)
G+ organisms and syphilis
Toxicity of PCNs?
-hypersensitivity reaction
-hemolytic anemia
Name the PCN-ase resistant PCNs (x3)
methicillin
nafthacillin
dicloxacillin
Spectrum of pcnase resistant pcns?
Naf for staph --> use for Staph aureus, except MRSA
methicillin has this unusual toxicity
interstitial nephritis
Name the 2x aminopcns
-ampicillin
-amoxicillin
Which of the aminopcns has greater oral bioavailability?
amOxicillin for ORAL
Aminopcns are given with this drug to enhance spectrum
clavulanic acid (B-lactamase inhibitor)
Coverage of aminopcns?
-HELPS kill enterococci:

Haemophilus influenzae
E coli
Listeria monocytogenes
Proteus mirabilis
Salmonella
enterococci
Name the 3x antipseudomonals
ticaricillin, carbenicillin, piperacillin

"James Bond uses pipe bomb, car, and explosive tick to kill Pseudomonas"
Coverage of ticaricillin/carbenicillin/piperacillin? (x2)
Pseudomonas spp. and G- rods
Must give this drug with antipseudomonal pcns
clavulanic acid (B-lactamase inhibitor)
Name 3x B-lactamase inhibitors ("CAST")
Clavulanic Acid
Sulbactam
Tazobactam
Give the spectrum of 1st gen cephalosporins ("PEcK" + ___)
PEcK =

Proteus mirabilis
E. coli
Klebsiella pneumoniae

G+ cocci
("HENS PEcK")
Haemophilus influenzae
Enterobacter
Neisseria
Serratia marcescens

Proteus mirabilis
E coli
Klebsiella
Give the spectrum of 3rd gen cephalosporins
serious G- infections resistant to other B-lactam abx
Give the spectrum of 4th gen cephalosporins
Pseudomonas, G+ organisms, G- organisms
Which antibiotic is associated with VitK deficiency?
cephalosporins
Which antibiotic is associated with a disulfuram-like reaction when used with alcohol?
cephalosporins
Monobactam that is resistant to B-lactamases and inhibits cell wall synthesis?
Aztreonam
Spectrum of Aztreonam
G-RODS only

Used in (1) pcn-allergic patients and (2) pts with renal insufficiency who can't tolerate AG's
Name the 2x carbapenem drugs
-imipenem/cilastatin
-meropenem
why must imipenem be given with cilastatin?
Cilastatin = inhibitor of renal dihydropeptidase I

renal DHP I inactivates the drug, so want to block this enzyme
Coverage of carbapenems? (x3)
G+ cocci
G- rods
Anaerobes

(however, many sfx, so limited to life-threatening infxns)
3x side effects of carbapenems?
-GI distress
-skin rash
-CNS (seizures)
Protein synthesis inhibitors specifically target this bacterial structure
ribosome (70S; eukaryote ribosome is 80S)
Explain the acronym "Buy AT 30, CCELL at 50"
Acronym to remember protein synthesis inhibitors

30S inhibitors:
A - AG
T - tetracyclines

50S inhibitors
C-chloramphenocil
C-clindamycin
E-erythromycin
L-lincomycin
L-linezolid
AG's:

Mean GNATS canNOT kill anaerobes

Explain
GNATS = drugs

Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin

-----

NOT = toxicities
-N: nephrotoxic
-O: ototoxic
-T: teratogenic
Coverage of AG's?
Severe gram negative rod infections
AG's are synergistic with this class of abx
B-lactams
mechanism of AG's
inhibits formation of initiation complex, causes misreading of mRNA
mech of tetracyclines?
bind to 30s subunit and prevent attachment of aminoacyl trna
how can you tell that a drug is a tetracycline?
all end in -cycline
why can doxycycline in particular be used in pts with renal failure?
fecally eliminated
why must patients taking tetracyclines avoid milk, antacids, or iron-containing products during drug administration?
divalent cations bind drug in the gut --> inactivates
why are tetracyclines so effective against Rickettsia and Chlamydia?
These are both obligate intracellular parasites, and tetracyclines accumulate intracellularly
3x toxicities of tetracyclines?
-GI discomfort

-discoloration of teeth and inhibition of bone growth in kids

-gray baby syndrome
resistance to tetracyclines x2?
-decreased uptake
-increased efflux

2ry to plasmid-encoded transport pumps
macrolides bind to this aspect of the ribosome
23S rRNA of the 50S subunit
mechanism of macrolides?
inhibit protein synthesis by blocking translocation
spectrum of macrolides?

(one big one)
-ATYPICAL PNEUMONIAS (mycoplasma, chlamydia, legionella)

-URI, STD, G+ cocci, Neisseria
resistance to macrolides
methylation of 23S rRNA binding site
mechanism of chloramphenicol?
inhibits 50S peptidyltransferase activity
how to tell that a drug is a macrolide?
-thromycin is the suffix
spectrum of chloramphenicol?

(one big disease)
MENINGITIS (H flu, N meningitidis, Strep pneumo)
Why does chloramphenicol cause gray baby syndrome?
Toxicity:

infants lack UDP-glucuronyl transferase, required to eliminate the drug
mechanism of clinda?
-binds 50S subunit
-blocks peptide bond formation
spectrum of clindamycin?
ANAEROBIC INFECTIONS in aspiration pneumonia or lung abscesses
drug used to treat anaerobes ABOVE the diaphragm
clindamycin
drug used to treat anaerobes BELOW the diaphragm
metronidazole
sulfonamides inhibit this enzyme
dihydropteroate synthetase

(competitive inhibitor)
TMP inhibits this enzyme
dihydrofolate reductase
in what way are TMP and SMX synergistic?
inhibition of different steps in the bacterial folate synthesis pathway

thus blocks bacterial DNA synthesis
3x mechs for resistance to sulfonamides?
- altered dihydropteroate synthetase
-dec. uptake
-inc PABA synthesis (overcomes competitive inhibition)
toxicity of TMP?
TMP = treats marrow poorly

megaloblastic anemia
leukopenia
granulocytopenia

Occurs because inhibition of DHFR --> decreased nucleotides for DNA synthesis
a. What compound can be used to treat TMP toxicity?

b. what is this treatment called?
a. folinic acid (bypasses step catalyzed by DHFR)

b. leukovorin rescue
quinolone mechanism?
inhibits DNA gyrase (TOPO II)
spectrum of quinolones?
G- rods of urinary and GI tracts
what unique toxicity is seen with quinolones?
FluoroquinoLONES hurt attachments to your BONES

-Tendonitis and tendon rupture
resistance to fluoroquinolones?
mutated topo II (DNA gyrase)
mechanism of metronidazole?
forms free radical toxic metabolites in bacterial cells that damage DNA
mechanism of polymyxins?
Detergent - MYXIN up the membrane

binds to bacterial cell membranes and disrupts osmotic properties
use of polymixins?
resistant G- infections
four drugs used in M. tuberculosis therapy
RIPE for tx:

Rifampin
Isoniazid
Pyrazinamide
Ethambutol
TB prophylaxis?
INH
How is pyrazinamide useful in tx of TB?
works well in acidic pH of phagolysosome where TB engulfed by macrophage is found
ethambutol mechanism?
decreased carbohydrate polymerization of mycobacterial cell wall
important ethambutol sfx?
optic neuropathy --> red/green color blindness
most important sfx (x1) of most drugs for TB other than ethambutol?

hint: can't drink and take TB drugs
hepatotoxicity
mech of INH?
inhibits synth of mycolic acids
toxicity of INH x2?
INH = injures neurons and hepatocytes

neurotoxicity
hepatotoxicity
lupus
how can INH toxicity be prevented?
give with vit B6 (pyridoxine)
4 R's of Rifampin:
RNA pol inhibitor
Revs up P450 system (inducer)
Red/orange body fluids (nonhazardous)
Rapid resistance with monotherapy
Give the best abx to use for:

Meningococcus
rifampin
Give the best abx to use for:

Gonorrhea
ceftriaxone
Give the best abx to use for:

syphilis
PCN G
Give the best abx to use for:

recurrent UTI
TMP-SMX
Give the best abx to use for:

Pneumocystis jirovecii pneumonia (AIDS)
TMP-SMX
Give the best abx to use for:

endocarditis with surgical or dental procedure
PCNs
Give the best abx to use for:

Mycobacterium avium intracellulare
azithromycin
Give the best abx to use for:

MRSA
Vancomycin
Give the best abx to use for:

VRE
linezolid + streptogramins
What fatty compound is unique to the membrane of fungi?
ergosterol
give the synthesis pathway for ergosterol (two steps)
squalene --> lanosterol --> ergosterol
mechanism of amphoteracin B?
binds ergosterol --> pore in membrane allows leakage of electrolytes
uses of amphoteracin B?
-SERIOUS, SYSTEMIC mycoses

-intrathecal for fungal meningitis
review toxicity of ampho B?
everything - "amphoterrible"

fever/chills, hypoTN, nephrotoxicity, arrythmias, anemia, IV phlebitis

-hydration reduces nephrotox
-liposomal ampho B (form of the drug) reduces other toxicity
nystatin mech?
binds ergosterol to create pores in fungal cell membrane
why is nystatin use always topical?
too toxic for systemic use
"Swish and swallow" nystatin for this infection
oral/esophageal candidiasis
Topical nystatin for these 2x conditions
-diaper rash
-vaginal candidiasis
mechanism of azoles?
squalene --> lanosterol --||--> ergosterol

azoles block P450 system that converts lanosterol to ergosterol
Indications for azoles (x2)?
1. cryptococcal meningitis in AIDS (crosses BBB)

2. candidial infections
this drug is used in tx of invasive aspergillosis
capsofungin
this drug is used to treat onchyomycosis
terbafine

mech: inhibits ergosterol synthesis:

[squalene -||-> lanosterol --> ergosterol]
this drug is used to inhibit the growth of dermatophytes (all the tineas)
griseofulvin
what is the mechanism of amantidine?
blocks viral penetration/uncoating

influenza A must acidify its core via an ion channel (M2 protein) to uncoat the viral core and liberate the genome. amantidine blocks this channel.
amantidine is useful for the treatment of this neurological disease
Parkinson's disease

causes release of DA from intact nerve terminals

--> can cause cerebellar problems in normal individuals due to inc DA
amantidine can be used to treat this virus
influenza A only

Note that 90% of influenza is resistant to amantadine, so not used anymore
Name the drug class:

zanamavir, oseltamavir
neuraminidase inhibitors
What is the mechanism of the drug(s) below?

zanamavir, oseltamavir
Neuraminidase inhibitors - prevent virus from cleaving sialic acid residues and thus prevents virions from being released from an infected cell
mechanism of ribavarin?
inhibits synthesis of guanine nucleotides
uses of ribavarin x2?
-RSV
-chronic hepatitis C
toxicity of ribavarin
-hemolytic anemia
-SEVERE teratogen
viral nucleic acid synthesis can be blocked by these two drug classes
-purine/pyrimidine analogs
-reverse transcriptase inhibitors
acyclovir mechanism?
guanosine analog

-inhibits viral DNA pol
-phosphorylated by VIRAL thymidine kinase only, so no effect on host cells
ganciclovir mechanism?
guanosine analog

-inhibits viral DNA pol
-phosphorylated by VIRAL thymidine kinase only, so no effect on host cells
acyclovir coverage?
-HSV
-VZV
-EBV

HHV 1-4
ganciclovir coverage?
CMV (HHV5)
acyclovir resistance (x1)
lack of viral thymidine kinase
ganciclovir resistance? (x2)
-mutated CMV DNA pol
-lack of viral TK
foscarnet mechanism?
FOScarnet = pyroFOSphate analog

inhibits viral DNA pol
two *very specific* uses of foscarnet?
-CMV retinitis in immunocompromised pts when ganciclovir fails

-acyclovir resistant HSV
foscarnet resistance x1?
mutated DNA pol
HAART therapy requires at least (#) drugs to prevent development of resistance
3 drugs:

2 NTRI's + 1 protease inhibitor
2 NTRI's + 1 NNRTI
How can a reader tell that a drug is an HIV protease inhibitor?
ends with -navir

NAVIR tease a protease
mechanism of HIV protease inhibitors?
inhibits HIV protease, whose function is to cleave HIV polypeptide into functional proteins
a. NRTI's and NNRTI's have similar mechanisms - describe it

b. what is different about their mechanism?
a. both competitively inhibit nucleotide binding to RT and terminate the DNA chain

b. NRTI's must be PHOSPHORYLATED before they are active; NNRTI's do not require this step
identify the class of the drugs below:

-nevirapine
-efavirenz
-declaviridine
NNRTI

= non-nucleoside reverse transcriptase inhibitors
identify the class of the drugs below:

-zidovudine
-didanosine
-zalcitabine
-stavudine
NRTI

nucleoside reverse transcriptase inhibitor
identify the class of the drug below:

-enfuvirtide
enFUvirtide = fusion inhibitor
what is the mechanism of enFUvirtide, a fusion inhibitor?
binds viral gp41 --> inhibits conformational change required for fusion with CD4 cells, blocking entry and replication
what is the mechanism of IFNs as related to viral therapy?
in virally infected cells, induce formation of glycoproteins that block replication of both RNA and DNA viruses
IFN-B is used to treat this condition
MS
IFN-y is used to treat this condition
NADPH oxidase deficiency
Review abx to avoid in pregnancy
SAFE Moms Take Really Good Care:

Sulfonamides
Aminoglycosides
Fluoroquinolones
Erythromycin
Metronidazole
Tetracyclines
Ribavarin
Griseofulvin
Chloramphenicol

FA 198
antimicrobial chemotherapy for toxoplasma gondii?

(2x agents used together)
-sulfadiazine
-pyrimethamine