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208 Cards in this Set

  • Front
  • Back
Aminoglycoside are bacterio___
cidal
Think Gram ___ for aminoglycosides
negative
What's the most toxic aminoglycoside of all?
neomycin B
This aminoglycoside is isolated from Micromonospora sp?
Gentamicin
Why are Aminoglycosides limited to aerobic bacteria?
Bc rely on transporter to get into the bac cell (this transporter is dependent upon O2, electrons, and ATP)

the pump normally brings in sugar (energy) but gets confused and brings in AG's as well bc also very sugary
What two things can inhibit the O2/e- pump for the Aminoglycosides?
divalent cations
acidic environment (spetemia, ketoacidosis, inflammed sites)
What are the 3 reasons why aminoglycosides are cidal drugs and not static?
(1) binding to ribosomal subunits is in an irreverisble manner
(2) the effects of increased permeability of the membrane  leakage and eventually lyses
(3) the ability of the pump has been taken away
Prokaryotes ribosomes have the ___ and ___ units.
23S (50S)

16S (30S)
Eukaryotes ribosomal units are ___ and ___.
28S (60S)

18S (40S)
Which PSI has bad SE's due to it's likely ability to bind with 28S/18S?
chloramphenicol
AUG codon is for ____.
methimine
At what site do aminoglycosides bind on the ribosome?
A site - specifically 16/30S

this is an irreversible bond --> reason why cidal
What 3 ways do aminoglycosides stop/inhibit protein synthesis?
block initiation

block further translation - get premature termination

incorp incorrect AA's --> can't fxn appropriately
Which AA is the difference between the aminoglycoside binding site to prok vs eukaryotes?
Adenine

(humans have guanine at the binding site - thus are not sensitive to AG's)
Which 3 ways do bac become resistant to aminogylcosides?
mutation
loss of permeability
enzymatic alteration (MOST IMPT!!)
Which bug has higher resistance to aminoglycosides due to it's narrower binding area?
Streptomycin
what are the 3 types of aminoglycoside modifying enzymes?
AAC (N-acetyltransfreases)
ANT (O-adneyltransferases)
APH (O-phosphtransferse)

RM these enzymes are made from same soil that AG's were found
____ bulkiness decreases the ability for AG enzymes to modify it and thus create resistance.
Amikacin’s
Which bug species is the most concerned about aminoglycoside inactivating enzymes?
Enterococci sp.

Enterococcus faecalis
Enterococcus faecium
Can you treat an enterococci infection with Vancomycin/Penicillin/AG? Why or why not?
no

synergisim is lost bc of the AG inactivating enzymes the bug possess
What Gram + bug are aminoglycosides good for?
Streptococcus sp.
This class is used for serious sepsis, bone, endocarditis, RTI, and skin/burn infections.
aminoglycosides
T/F

Aminoglycosides treat P. aeruginosa
True

(even tho bug does not have porin channels - but have gated channels)
This aminoglycoside is distinugished by treatment of TB and for binding to a single domain of the 30S A-site.
Streptomycin

(always used in combo of at least 1 other agent when treating TB)
Can treat bacterial endocariditis by Enterococci and Y. pestis.
streptomycin

(RM Enterococci sp must NOT produce inactivating enzymes)

Endocarditis usually treated with PCN for 4-6 wks (w/o AG if in an uncomplicated elder)
Which two bugs especially does Garamycin have excellent activity against?
P. aeruginosa
L. monocytogenes (Gram +)
Gentamicin has a ____ group that will attack the amide on the ____ ring.
amine

B-lactam

(seperate when given to same person - Gent has the greatest potency for this to happen)
Is Nebcin effective as Garamycin in treating Gram + (enterococci) with Pen?
no
This agent is the perferred agent in the initial treatment of nosocomial Gram - bacillary infections
(including DOC for M. avium).
Amikacin (Amikin)
When see oral neomycin think what?
preparation for surgery (kills off bugs in GI lumen)
Vestibular effects is highest with what two AG's?
Streptomycin
Gentamicin
Which 2 AG's have the highest choclear effects?
Amikacin
neomycin
Which AG has equal vestibular and choclear effects?
tobramycin
Which part of the ear is more irreversibly affected with AG's?
CN 8 - vestibular nerve
AG's penetrate the hair cell membranes causes leakage which causes a loss of ____, especially ___.
ions

Mg2+
N-acetyl-L-cysteine has been investigated as a possible prophylactic option for _____.
AG otoxicity
Which AG is the least nephrotoxic and why?
streptomycin

bc it's less concentrating; neomycin concentrates the greatest
How do AG's worsen Myasthenia Gravis (2)? What is a way to fix it.
(1) dec synaptic release of ACh
(2) dec sensitivity of any nicotinic receptor

Give Ca2+ helps by releasing ACh from vesicles to be released
Which agent is rapidly inactivated by metal cations?
TETs

(in food, vitamins, supplements)
What form are TETs water soluble?
as salts - primarily in HCL
At what position is the NH2 in when the TET is active? Inactive?
active = NH2 is going back
inactive = NH2 will go forwards (towards me)
TETs bind to what subunit? and Blocks what site?
16S (30S)

A-site reversible bind - why more STATIC than cidal
Which two TETs are so lipophilic that it is more cidal?
aminocycline
doxycycline

(lipo allows them to stay around longer and penetrate bugs better --> maybe even prokary's)
How do TETs get into the bac cell?
diffuse thru outer membrane (bc lipophilic) - unlike AG's

and thru O2, ATP, electron pump (like AG's)
At high doses what do TETs bind to?
inhibits mammalian 40S subunit
Which class has an antianabolic effect and thus should not be used in prego's.
TETs

(this inc BUN --> renal and hepatic effects)
What 3 ways can TETs create resistance?
(1) dec influx or inc efflux
(2) riobososmal protection proteins
(3) enzymatic inactivation

(why only used for less serious infections like acne and not typical DOC)
TETs indications? (P,L,R,C,C,C)
Add on indications? (2)
Propionibacteria (acne vulgaris)
Lyme Disease (B. burgdorferi)
Ricketts
Chlamydia
Cholera
Clostridium sp

Add on: Y. pestis and B. anthracis
Can TETs treat CA-MSSA, CA-MRSA? Can it treat UTIs?
CA-MSSA/MRSA if there's been a susceptibilty test (some S. aureus are sensitive to TETs)

No - not UTIs
(E. coli, Shigella, Salmonella or other Enterobacteriaceae)
Can TETs treat Shingella or Salmonella?
No, neither
Which class can cause free radical formation from absorption of UV light?
TETs
(the darker the better, but still no way to predict)
This agent is the DOC for N. gonorrhoeae when the pt has a PCN allergy.
Tetracycline (Sumycin)
This agent can be used in combination Bismuth, flagyl and a PPI to treat H. pylori.
Tetracycline (Sumacyin)
Loss of the C ring -OH and -CH3 does what for Minocycline (Minocin)?
increases lipophilicity

(100% oral absorb, stable in acid, and inc in blood levels)
This agent causes membrane leakage AND inhibits the 30S subunit.
Minocycline (Minocin)

also don't take with food or on full stomach
(1 hour before, 2 hours after)
This TET is the most stable, has the longest t1/2 (qd dosing) and is 100% absorbed.
Doxycycline (Vibramycin)
What two bugs does Vibramycin have excellent activity against?
T. pallidum
N. gonorrhoeae
When see Tigecycline what should you think? What are some bugs it covers? (E,K, B, S/S, E, E/R)
think = extended spectrum TET (even tho really new class: glycylcyline)

E. coli
K. pneuomoniae
Bacteroides fragilis
Streptococci/ Staphylococci (MSSA)
Enterococcus sp.
Ehrlichiosis/Rickettsia
DOC for Rocky mountain fever / Ehrlichiosis? Alternate drug?
doxycycline --> trt immediately

chloramphenicol
Where in the body does V. cholerae infect? What's the most common methods of contraction in the US?
small intestines

shellfish and travel
The cholera A toxin binds to what in the cell? What does this cause?
binds to Gs(alpha) when active --> locks it in an active position

AC is continually stimualte so cCAMP is continually activated and now all electrolytes and water are steadily effluxed out --> diarrhea
This class is made of sugars, but lipophilic, has a pKa of ~8, and is bacteriostatic.
macrolides
What subunit and site do macrolides bind?
23S (50S) at the P-site

RM: TETs and AG's bind to 16S/30S
What 3 ways do bugs become resistant to mac's?
Efflux of drug by active pump mech (MAIN ONE IN US --> low level resistance)
Ribosomal protection via methylation
Mutation at teh 23S subunit
When see macrolides think Gram ____?
positive

(Gram - bugs intrinsic resistant due to a lack of penetration of drug)
European bugs more resistant to which class?
Macrolides

(they req much more drug to kill)
Which 2 drug especially inc the half-life of macrolides and may cause toxicity?
astemizole
terfenidine

(3A4 inhibitors)
Name 4 drugs that should not be given with macrolides?

(E, T, Br, M)
ergotamine
theophylline
bromocryptine
methylprednisolone
Which mac causes pro-propulsition thru gastrin stimulation?
erthromycin
Name 5 drugs that should not be coadmin with macrolides?

(Cy, Be, O, S, C)
cyclosporin
benzo's
OC's
statins
CCBs
Usually go to drug for PCN allergies
macrolides
DOC for H. pylori?
macorlides
Clarithromycin is best!!!
This agent is deactivated in acid (ketals), is dec to nothing when given with food, rarely DOC except maybe L. pneumonphila, and requires heavy, spordic dosing.
Erythromycin (E-Mycin)
Purpose of ethylsuccinate?
mask bitter taste of drug

(RM - prodrug bc has ester --> dosed less often)
What does Biaxin's change to -OCH3 do for the drug?
increases lipophilicity
dec ketal formation --> less cramps

Adds extraordinary potency against H. influenza
This bug releases VacA (vacuolating cytotoxin) which causes vacuolation of lumincal cells.
H. pylori

(RM: dec somatostatin and inc gastrin release at the gene level)
This agent is a loading agent, syngergisitic with Cephs to treat gonorrhea, and has dec 3A4 inhibition.
Azithromycin
This agent has a mac backbone but replaced sugar with ketone, is only indicated for MDRI S. penumoniae, and has a black box warning bc bad SE's.
Telithromycin (Ketek)

SE's: severe liver damage (esp when given with 3A4 drugs [statins]), spontaneous fainting, visual disturbance including visual loss
This agent is not really a MAC, inhibits mRNA, good for C. diff (>18 yo), and is poorly absorbed so min systemic SE's.
Fidaxomicin (Dificid)

(oral = effective as oral vanc with 1 less risk of occurrence)
This agent is quite lipophilic, binds to the 50S subunit, broad spectrum, and treats P. acnes.
Cleocin
Which MISC protein synthesis inhib has similar resistance to macrolides?
Cleocin
This agent inhibits the binding of tRNA to the 70S ribosome, thus preventing the formation of the ternary complex.
Linezolid (Zyvox)
When see Linezolid which 4 bugs should you think of? When should use?
MRSA
VRSA
VISA
VRE

when nothing else has worked on them
At which site specifically does Zyvox bind?
the P-site

(70S - combined structure)
Which agent causes serotonin syndrome?
LineZOlid (Zyvox)
This agent binds to the 23S RNA of the 50S subunit, prevents tRNA binding to the A-site, and is highly toxic due to mammalian cell death (protein syn stops)
Chloramphenicol (Chlomycetin)
Which agent should not be given in anemic patients? Why?
Chloramphenicol (Chlomycetin)

it causes aplastic anemia --> leads to hemorrhaging, bruising, and leukopenia
Which agent is a last resort for bacterial menigitis? Is does it have a broad or small spectrum?
Chloramphenicaol (Chlomycetin)

think BROAD
This agent is resevered for treatment of serious infections caused by multiple drug resistant E. faecium.
Synercid
(Q&D pritsin)
T/F

Synercid can be used for E. faecalis.
False

for E. faecium!!!
This agent is approved for MDR or Vanco resistant E. faecium and skin/skin structure infections from MSSA or S. pyogenes.
Synercid

(Q&D pristin) --> RM only by IV
Quin binds to ____ while Dalf binds to ____.
Q = P-site

D = A-site

(enzymatic inactivation - only way for resistance)
This agent has SE's that are infused, is a potent inhibitor of 3A4s, and can cause toxicity and HTN when given with other 3A4 substrates.
Synercid

(Q & D prisitin)
Amoebiasis are diseases of the ___ intestines caused by _____ ____.
LARGE

Entamoeba histolyctica
This parasite has 2 forms: motile trophozoite (formed in the SI) and a dormant cyst.
Amoebiasis

(RM: chlorinated water does not kill)
What's the main cause of traveler's diarrhea? Where is the infection in the body?
Giardiasis (water-borne --> US)

Small intestines
Which parasite has a infectious cyst: Amoebiasis or Giardiasis?
Giardiasis
This parasite causes ocular disease to unborn babies 15-20 years later.
Toxoplasmosis
How is Toxoplasmosis linked to Schizophrena/paranoia?
(1) Acute Toxo infections can cause psychosis (2) some antiphy drugs actually inhibit toxo growth – like haloperidol (3) higher AB’s against this organism in schizo pts vs. not schizo patients (4) organism can damage astrocytes in brain similarily to those we see in schizo pt
AIDS plus toxoplasmosis = ??
Toxoplasmic-encephalitis (major cause of death)
What's also good for Toxoplasma gondii, besides Flagyl?
sulfa/trimeth (Bactrim)
This agent can treat ALL anaerobic cocci and bacilli (Bacteroides sp.)
Flagyl

(distinguishing feature)
How is Flagyl similar to Nitrofurantoin?
metabolized by sensitive species
This agent offers protection from Parkinson, creates N or O reactive species, and is CI during 1st trimester of prego.
Flagyl
This agent is used for resistant species of ameobiasis and is only available thru the CDC.
Diloxanide FURoate (FURomide)
This drug is limited to Giardiasis only - so reserved for special use only.
Nitazoxanide (Alinia)
Tindamax is similar to ____. What 3 parasites is it approved for?
Flagyl

Trich (and bac) vaginalis
Giardiasis (> 3)
Ameobiasis (> 3)
This parasite primiarily occurs in AIDs patients (w/ 50% occurance), immunosuppressed pts post transplant, and premature/malnourished infants.
Pneumocystis

P. jirovecii (formally P. carinii)
This parasite is an opportunistic microbe and infects lung lining & alveolae.
pneumocystis
What 4 agents can be used for Pneumocystis Pneumonia?
(S, C, TF, A)
Sulf/Trim (trt and pvt)
Clindamycin
Trimetrexate + Folinic acid
Atovaguone
MOA of Trimetrexate + Folinic acid?
Neutrexin inhibits DHRF

Leucovorin replenishes mammaliam folate
Malaria is caused by the genus ___ and in humans mostly by the ____ species.
Plasmodium

falciparum
This has a classical feature of cyclical fevers, 2 stages (liver and RBC), and feeds more on prego's.
Malaria in humans
This has merozoires involved in it's growth process? What is one prevention of getting?
P. falciparum

Sickle cell hetero's of A and S
When are Quinine (8S, 9R) and Quinidine (8R, 9S) used?
when other anti-malarials have not worked

this is bc they are quite toxic
DOC's for malaria? MOA?
Chloroquine (Aralen)
Hydroxychoroquine (Plaquenil)

basic drugs --> get into lysosome bac --> now malaria can't use it to breakdown the hemoglobin they usu do
Aralen and Plaquenil are excellent against what species? Does it work against E. histolytica?
Plasmodium

suppress P. vivax and P. ovale
prevents P. falciparum

Yes, also E. hist
If a pt has a chloroquine-resistant Plasmodium sp. what should be used?
Mefloquine (Lariam)

good for suppression and prevention

(higher SE's!)
Pyrimethamine (Daraprim) reduces THF synthesis is Plasmodium - thus get a def in what 3 things?
thymidine
purines
methimine

good for trt and prevention of chloroquine-resistant malaria
This agent is given to prevent P. falciparium and to treat acute, uncomplicated P. falciparum.
Malarone (Atovaquone and Proquanil)
What is the make up of Malarone? (specifics)
Atovaquone - selective inhib of parastic mitochondrial e- transport

Proquanil (bc's cycloquaril) - selective DHFR inhib in parasites
What 3 drugs dec plasma concentrations of malarone?
TETs
Metoclopramide
Rifamfin/Rifabutin
This agent is good to treat acute attacks due to chloroquine-resistant P. falciparum.
TETs

(RM - sulfonamides are also active against)
What are the 2 causes of Tapeworms?
Taenia saginate (Beef)
Taenia solium (pork --> BAD)
Which worm is capable of penetrating the foot?
Larvae of the hookworm
This worm is most widely spread, lives in GI lumen, causes itching around anus/vagina.
Pinworms
This worm can cause blindness, heart attacks, convulsions and psychotic disorders.
Tapeworm
Mebendazole (Vermox) and Albendazole (Zental) can treat which 2 helminths?
Nematodes (Hook, pin, & round)
Cestodes (Tapeworms)
What 3 functions do microtubules do? Which drugs affect them?
1. forming the worm's cytoskeleton
2. spindle formation
3. vesicular trafficking

Meb and Albend
What is the secondary mechanism of Meb and Albend?
blocking ATP (essentially)
How is resistance conferred in Benzimidazoles (Alben and Meb)?
1. switching the B-tubulin for 1 to 2
2. mutations in B-tululine genes (simple hydroxy change)
Mectizan and Stromectol is excellent against which worm types?
Pinworm
Roundworm
What is the DOC for onchocerciasis (river blindness)?
Mectizan, Stromectol
Ivermectin MOA?
causes paralysis of organism
binds to glutamate gated Cl- channels

(dec feeding behavior in nematodes)
This agent has a MOA of Ca2+ influx (paralysis), inhibits phosphoinositide (contractions), and drug induced damage to tegument (AB attack on worm's antigen).
Praziquantel (Biltricide)
Does Praziquantel (Biltricide) treat Nematodes?
No

(just cestode and trematodes)
Pin-X is used for what worms only? Why is it safe to be OTC?
pinworms, roundworms, hookworms

bc confined to GI tract and not systemically absorbed
Pin-X moa?
NMBA (paralysis)
Activates nicotinic receptors
1% g-benzene hexachloride is ____?
Lindane (Kwell)
Why does Lindane cause dizziness, clumsiness and confusion? What weight does it bc 2nd line for scabies and lice?
bc it binds to GABA-R --> allows constant stimulation

<110 lbs
Pyrethryins are contracted from ____ and are less toxic so kids can use. What some examples? (2)
mums

A-200 and RID
Permithrin is synthetic derivative from Py's...what are some examples? (3)
Nix-1
Elimite
Acticin

(RM they have increased stability so do not need a synergist like Py's)
MOA of Pyrethryins and Permithrin?
blocks the arm of the Na+ channel --> so leaves it open

works very quickly
Why are Pyrethryins and Permithrins not toxic to humans?
bc humans very quickly metabolize them to various harmless products in the body

bugs take much longer to do so
What is added to Pyrethryins in a 10:1 ratio? What do they do?
Piperonyl butoxide (PBX)

inhibit the CYP450 enzyme that breaks down the pyrethryin
This agent is approved for head lice ( > 4 yo), contains benzyl alcohol, and causes 100% paralysis in insects.
Spinosad (Natroba)
What is the 3 step process of tetrahydrofolic acid synthesis?
Dihydropteroate Synthase (Dihy + PABA)
Conjugation (Dihy acid + glutatmate)
Dihydrofolate Reductase (DHFR) --> tetrafol
What enzyme in the tetrafolate synthesis do we not have compared to bugs? What type of inhibition is it with sulfonamides?
we dont have dihydro synthase (1st step)

Sulfa mimicing PABA --> competitive
How can bugs bc intrinsically resistant to sulfonamides?
by getting their folate (dihydrofolate acid) from the environment (like we do) and making tetrafol from that

ie: not making folate acid de novo
What are 2 ways of sulfonamide resistance?
1. low affinity of the sulfo for the dihydro synthase
(happens thru mutations, plasmids)

2. increased PABA synthesis
Which sulfanilamide form is active? Which form can penetrate into the bug?
ionized form is active

but unionized form is only way to get into bug (bc is lipid soluble)
Sulfanilamide is a(n) _____ drug despite its ___ pKa.
acidic drugs (suflone is what's e- withdrawing)

high pKa (~10.5)

so they need a more basic environment to bc active (ionized)
In the urine sulfanilamide is more ionized or unionized? what' the result?
unionized (bc it's a like-like situation)

this causes concentration --> crystals
What does the phenyl ring do for sulfadiazine?
dec it's pKa --> less acidic --> more ionizable form in body --> more water soluble in urine
What are 2 reasons why Sulfadiazine is 142X better than Sulfanilamide?
greater lipophilicity (inc t1/2)

AND

low pKa

(RM lipo is not only reason bc the -amide can get in bug too, just can't get activated once inside)
When see sulfonamides think ____ spectrum.
BROAD

(cover everything)
Triple Sulfa is used for ____ and is often dosed with ______ to increase clearance.
UTI
(from anything)

Na-Bicarbonate
What is Silvadene is used for? What action does it provide?
for: non-life threatening burns

provides synergism with sulfadiazine and Ag+
This sulfo covers Gram + and Gram - organisms very well. And inhibits growth of nearly all bac and fungi in vitro.
Silvadene
This sufla has good activity for UTIs and otitis media. Is rapidly absorbed and eliminated.
Sulfisoxazole (Gastrisin)
What make Phenazopyridine good with sulfisoxazole?
adds local analgesic properties to urinary tract

RM Azo-Gantrisin is good for UTIs but will stain clothes, urine, contact lenses, etc
The nitro proton with the acetyl group in Sulfisoxazole Acetyl does what? What does it have good activity against?
grants tastelessness

good for otitis media
This sulfa is slower absorbed and eliminated, has a pKa of 6 and has a very WIDE spectrum.
Sulfamethoxazole (Gantanol)

GRAND-DADDY of the Sulfa's
Does Gantanol cover MRSA?
not on it's on

(does cover T. gondii tho)
This sufla is distinguishably by the fact it is excellently water soluble - thus used extensively in ophthalmic infections.
Sulfacetamide (Isoptocetamisde, Na-sulamyd)
What is connected to the sulfonamide that cause allergic rxns?
arylamine

(RM not enough Glutathione is the problem)
Why doesn't trimethoprim recognize mammalian DHFR?
bc of a single difference in the enzyme

(RM trimethroprim works at the end of tetrafolate formation - works very well with sulfon's)
Can Bactrim treat MRSA?
yes, some (??)

very wide spectrum
What happens if a pt is on Trimethoprim + an ACE, ARB or sprionolactone?
hyperkalemia

(RM this is bc Trimethoprin dec K+ excretion)
Which sulfonamide has the lowest (best) MIC? Highest?
lowest = sulfamethoxazole

highest = sulfanilamide
____ is the most potent antibacterial thus far. Why?
Quinolones

bc not real resistance as of yet

(RM florou group is added at the 6th position)
DNA gyrase cutting and gluing back together is called:
decatenation (cutting)

catenation
For humans what enzyme is similar to DNA gyrase?
Topoisomerase II
This enzyme is absolutely required for decatanation ahead of the replication fork of DNA.
Topoisomerase IV

(works with DNA-gyarse; it didnt have Top IV rep would NOT occur; didn't have DNA-gyrase --> slows rep down to the point cell cannot live long)
MOA for Quinolones?
inhibit DNA synthesis by binding and inhibting DNA gyrase (stops supercoiling & tension relxation) and TOPO IV (stops decetanation & causes SCISSION)
In Gram + bugs quinolone's primary target is...?
TOPO IV
In Gram - bugs quinolone's primary target is...?
DNA Gyrase
High doses of quinolones can cause what?
dec in selectivity of the TOPO's --> so TOPO II maybe inhibited rather than IV
Where do quinolones bind on the DNA gyrase? On the TOPO IV?
DNA gyrase --> gyrA or gyrB

TOPo IV --> parC

(if mutate these areas = resistance; 1 = low level resistance, both = high)
What bug is unsual in that it has higher resistant rates with Quinolones?
N. gonerrhea
Levaquin 500 vs Levaquin 750?
500 led to low level resistance
750 now used bc kills all bugs by binding to both gyrA and parC
This QL is extensively used in Gram - UTI and is P. aeurginosa resistant.
Nalidixic Acid (Negram)
This gen FQ has poor serum/tissue conc, not available for systemic infcections, and limited to UT disinfectants?
1st gen FQ
Which FQ gen lacks P. aeruginosa, Gram + organisms, and intracellular organisms?
1st gen FQ's
What does the floro group add to quinolones?
lipophilicity

now can penetrate bac membranes better (and some human cell membranes too!)
This FQ is more Gram - than Gram +, is very potent with low MIC, covers P. aeruginosa, and antagonizes the GABA-A receptor.
Norfloxacin (Noroxin)
2nd gen

RM: convulsions can occur bc of the GABA-A binding
This FQ gen is excellent for systemic infections, has no activity for anaerobes, good Gram - and weak Gram +, and covers P. aeruginosa?
2nd gen
Cipro is what FQ gen? Does it cross CSF?
2nd gen

yes - some family members will be treated prohlayaxis with this drug
DOC for anthrax?
Cipro

(2nd gen)
Is Levofloxin better at Gram + bugs than cipro? What isomer is more potent?
yes better at Gram +

S- is more potent
(Ofloxacin rarely used anymore - mixture)
URI are more Gram ____ so see which FQ used more?
positive

levofloxacin
LRI and UTIs are more Gram ___, so see which FQ used more?
negative

cipro
Which FQ can target MSR pneumoniae?
Levofloxacin
This FQ class has once daily dosing, active against S. pneuomoniae, and is better penetrating.
3rd gen
Are 3rd gen FQ's good given systemically?
No (cause QT prolongation and liver tox)

Zagam (sparfloxacin) and Tequin (gatifloxacin) BOTH removed from the market
This FQ is less active against UTI (due to elimination), better at intracellular bac, and is excellent against S. pneumonia.
Moxifloxacin
Is Avelox used for anaerobes like Bacteroides fragilis?
yes

(RM better tho at Gram + than Gram - since a 4th gen)
What gen is Factive? What should you think of when see this gen (2)?
4th gen

Gram + and QT prolongation
What does the urine have to be for FQ's to cause crystalurina?
basic

(rare tho)
What chem structure causes convulsions in FQ's? Which drug class enhance convulsions with the FQ's?
the piperazine ring (less in newer agents)

NSAIDs
What is the age restriction on FQ's? Why?
18 years or older

causes arhtropathy
Do FQ's cause chelation? Photosenstivity?
yes and yes!
Quinolone drug interactions is with CYP____. Which 4 drugs should be avoided when given together?
1A2

Warfarin, Theophylline (esp w/ Cipro), Caffeine, Antacids
Hiprex generates ____ and ____. Why are Proteus sp resistant to it while almost all other bac are sensitive to it?
ammonia and formaldehyde (why an antispetic)

bc they make urine more basic (need acid to get A and F) --> never used alone to treat UTI
This agent inhibits DNA and RNA functions, is used for E. coli and Enterococci sp. only, and comes in 3 forms?
Nitrofurantoin
This Nitrofurantoin is a powder is most associated with creating N/V. It changes urine color to brown.
Furadantin
This Nitrofurantoin is in a crystal form, it decreases the initial absorption of drug so less n/v.
Macrodantin
This Nitrofurantoin has crystals and a gelatenous polymer mixture. It slows absorb very much and last longer so only need BID.
Macrobid