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163 Cards in this Set
- Front
- Back
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what are the beta lactams?
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Penicillins
Cephalosporins Carbapenams Monobactams |
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What do penicillins target?
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transpeptidases, by binding to it
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SE of the penicillins?
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allergic Hypersensitivity
Immediate response- hives and anaphylatic shock mediated by Ig E Delayed reaction- hepatitis andrash siezures with IV doses |
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What are the penicillinase resistant Ab?
-bc bact develop a B-lactamase (same thing |
Not AFfected by penicillinase-naficillin
oxacillin cloxacillin dicloxicillin methicillin |
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Difference b/t the natural penicillins is
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Pen G-IV
Pen V-oral (acid stable {narrow specrum and met by b-lactamase |
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Broad or extnded spectrum pens include...
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PAMs CAT more GM-
pipe ... "icillin" amp mezlo s carb amoX ticar |
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Penicilllinase inhibitors
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Sulbatam and Clavunic Acid-
they just bind it and it doesnt work combo drugs w/ broad spectrumsin-amox and clav acid) |
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WHat are some combos used if you have a b- lactamase containing bug??
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Augmentin- Clavunic acid+ AMOxicillin
Timentin- Ticaricillin +clavunic acid Unasyn- ampicillin + sulbactam |
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Cefalosporins work how?
SE? |
-same mech as penicillin (inh transpeptidase
SE- when taken with pen u get cross reactivity,, results in a super infectin- C.dificile |
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first gen cephs
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AZOL ALEX
cephalexin cefazolin -parentally |
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second gen cephs include..
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AMYs TIN TAN eUROpean ACL replacement broke, that dumb bitch
cefACLor cefUROxime cefAMYcins -cefoxiTIN -cefoteTAN |
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third gen cefs are the...
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TAZ TRIed the OPERZONE??
ceftazidime ceftriaxone cefoperazone |
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fourth generation cef and its importance?
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EPI
cefepime- it is the latest drug out, AS the cefs get newer as the newer generations come out they are increasing in activit against GM NEG and Increase in entering CNS |
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CARBAPENEMS
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"PENEMS"
IMIpenem - GM +met in kidney by a dihydropeptidase to form toxic product, so always given with cilastin(a peptidase inhibitor MEROpenem - GM - |
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talk about the carbsapenems?
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carbapenems inhibit transpepsidases just lik pens and cephs, broad spectrum, penicillinase resistant
-they causeTROMBOCTYPENIA AND ANEMIA -SEIZURES IN PTS W/ EPILEPSY |
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MONO bactams
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=AZTREONAM
-last b lactam, all of them inh. transpeptidases se-seizures and nausea it is a small molecule and not cross reactive wit Pcn |
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Aztreonam
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monobactam that inh transpeptidase by binding to it
\ SE_ seizures and nausea |
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It is vs aerobic Gm (-) and it is not cross reactive w/ penicillin, it has a b lactam ring
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axtreonam= monobactam
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4tth gen cefs are given ...
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IV
epi |
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alex, azol
acl, uro taz ex tri epi |
the cefs
the pattern of increasing CNS and GM(-) activity with newer gens |
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P
C C M actually inhibit the.... |
Cell wall
pen cef carb mono-az |
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Non containing B-lactam ring
Cell Wall inhibitors are the |
TRACI VANCO CYCLOs FOS
baciTRACIn VANCOmycin CYCLOSrine FOSomycin |
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what inh. CW syn by binding to the DIANALINE residues in the glycoprotein subunit
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VANCOmycin
against GM+ |
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It causes RED NECK syndrome, (Matt VANZANTEN SYNDROME) due to rapid iv infusion crazy rasha nd flushing from histamine realease
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Vancomycin
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Inh Bactoprenol carrier
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bactiTRACIn- very nephrotoxic
non b- lactam cell wall inh topical againnst gm + |
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how is res against vanco mycin created
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bact exchange a lactic acid instead of an analine
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vancomycin txs...
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it treats Superinfections caused by C. dificle ( cef and pens mixed)
can enter cns |
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Fosomycin
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inhibits n-acetyl muramic acid
against gm - and for uncomplicated UTIs |
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analine analog that inhibits incorporation of analine into n-acetyl muramic acid
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CYCLOSERINE
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SE of CYCLOserine
(traci vanco cyclos fos) non b lactam |
headache, tremor, and psychosis (CNS
it is an alanine analog |
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whats a tertiary drug? ex...
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Cycloserine gm+, gm -, and Tb
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telavancin
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a derivative of vancomycin
works on dianaline site and bact. mmbr disruptor |
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Bacterial Protein Synthesis inhibitors
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MATs MLS Lid
Macrolides- "thros" Aminoglycosides Tetracyclines Misc. Prt syn inh- chlorophenicol LINcosamides- "lins" Streptogramins- "pristin OXaLIDinones- LID (or think of protein causing a clot in your arteries and the word "more" in spanish is "mas" so....M.A.S. C.L.O.T." Macrolides Aminoglycosides Streptogramins Chloramphenicol Lincosamides Oxazolidinones Tetracyclines |
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macrolides
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(A.C.E.)-rev binds and inhibits translocation, - p450, inc GI motility(makes u shit)
erithromycin- clarithromycin- azithromycin THRO |
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macrolides mech...
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rev. binds p site on t-RNA inhibiting transloction
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macrolides SE...
resistance.... strange info.... |
GI upset(inc. motility), inh p450, hepatotoxic
res. -bugs just increase its transport out of cell strange info- special coated tab b/c acid unstable includes erythro clarithro and azithromycin |
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Aminoglycosides....2nd "mycins" after macrolides besides vancomycin(non blactam),,, fml
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TOBy, NEO, and KANyA STREPT GENTle AMI down to a NET
tobramycin neomycin kanamycin streptomycin gentamycin amikacin netilmycin |
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aminoglycosides act by
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binding 30s
inh. t-RNA binding all along mRNA irr. mRNA misreading -cidal |
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SE of aminoglycosides
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*A of MATs MLS lid (irr binds30s, inh tRNA, cidal)
ototoxicty nephrotoxicty neuromuscular blockade preg cat D (fetal damage) |
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Aminoglycosides against...
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aerobic bact only, Tb
gm - |
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tetracyclines..
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rev. bind 30s
inh. binding along the "A" site T of MATs MLS lid |
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tetra cyclines include
(a bact prt syn inh... MATs MLS Lid) |
four doctors and mini tigers
tetra doxy mino tige....cycline |
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tetracyclines bind Ca++(alsoFe and Al), fuck up teeth, what else
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-preg cat D
renal and liver tox, gi upset, allergic phtosensitivty Do Not take after expiration?? |
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tetracycline vs
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gm- and gm +
rickettsia, spirochetes, proprioni, bacterium acne |
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chlorophenical inh...
(misc prt inh) |
peptidyl transferase, cidal or static
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chlorophenical gets in the _____ and txs ______
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cns
vs salmonella in pen res. or allergic person |
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lincosamides...
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"lin"
clindamycin not clarithro(macrolide) lincomycin |
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like _______ , lincosamides inhibit the ________
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erythromycin, translocation and binding of tRNA to P site
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SE of lincosamides=
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severe super inf w/ C.dificle
(cef also in cross rxn w. pen causes also) -what cures it??vancomycin Lincosamide "lins" Lof MATs MLS lid |
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lincosamides are popular form of....
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dental prophylaxis
txs anaaerobic gm + and- cLINdamycin and LINcomycin |
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streptogramins=
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"pristin"- bact prt syn inhibtor
quinuPRISTIN dalfoPRISTIN quin and dale ahve pristine gingiva S in MATs MLS lid, used together against gm + Vancomycin Resistant S(staph or strept) joint and muscle pain ar eth SE |
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Quin and Dale are use in combo against...
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gm + vancomycin resistant staph and strep
together they bind the A and P site 50s?? streptgramins |
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oxazoLIDinones=
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linez-o-lid
bact prt syn inh by 50s fmet cant bind to p site |
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linez-o-lid binds...
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50s, inh binding of fmet t RNA to the P site
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oxazoLIDinones(linez-o-lid) txs:
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MRSA
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what are the abs that do not act on cell wall or prt. syn.?
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daptomycin
"acins"- fluroquinolines and other quinolines Antimetabolites (sulfas trimethoprim metronidazole nitrofurantoin |
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how does daptomycin work?
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disrupts cell membrane
loss of k+ and prt syn decreases afterwards txs skin or soft tissue infections not cell wall or prt syn |
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Quinolines inhibit..
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bact topoimoerase
(II and IV specifically) |
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side effect of quinolines include..
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not for pregnancy or kids
cause cartilage damage when its developing, tendinitis and achilles rupture |
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what do sulfa drugs do (anti metabolites )
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inhibits dihydropterate synthetase -- static!!
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antimetabolites=
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sulfa drugs
sulfonamides and sulfadiazine side effects: steven johnsons jaundice hemolytic anemia in pts with g6p deficieincy |
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sulfa drugs for
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uti
broad spect |
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trimethoprim inhibits
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dihydrofolate reductase
specifically bacterial |
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megablastic anemia
leukopenia granulocytopenia are |
se of
trimethoprim and prevented by LEUCOVORIN (- dihydrofolate reductase like methotrexate) -Ab that acts on neither CW or prt syn |
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metronidazole is a
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prodrug
converted to a free radical by anaerobic bacteria |
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trimethoprim +sulfamethozole=
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cortimazole
txs UTI |
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metronidazole is used for
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anug or trench mouth (anaerobic bact) and some protozoans
prodrug- free rads by bact |
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nitrofurantoin
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prodrug- same story as metro except for UTIs
converted to a free rad |
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metro causes
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seizures
metronidazole is a prodrug, free rads fuck up anaero bugs txs ANUG and trench mouth affective against protozoans like trichomonas an giardia |
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nitro furantoin causes
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brown colred urine (furan) cough and chest pain,
g6p def-causes hemolytic anemia |
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what are Ab agents used only topically?
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polymixin-binds lps, gm-
gramicidin-gm+ , channels in mmbrs(mixture of 3 abs) neomycin-an aminoglycoside MUpirocin-inh prt syn retapaMUlin-inh prt syn neosporin-(neomycin+polymixin+garmicidn) polysporin-polymixin and baciTRACIn polytrim-trimethoprim+polymixin terak- oxytetracycline and polymixin |
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polymixin
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topical vs LPS-inc cell mmbr permeability
se-nephrotoxic,neuromuscular blockade, neurotoxic |
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gramicidin
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forms holes in cell mmbrs
gm + in neosporin -topical |
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neomycin
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an aminoglycoside
topical in neosporin |
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neosporin=
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gramicidin
polmixin and neomycin poly's new gramma |
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MUpirocin and
retapaMUlin are |
topicals against prt syn
gm+ |
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polysporin =
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polymixin and bacitracin
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polytrim=
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polymixin and trimethoprim
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trichamoniasis would be txed with
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metrinidazole -protozoans also
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chlorophenical inhs.
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peptidyl transferase
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terak=
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topical anti ab
oxytetracycline + polymixn |
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Antimycobacterial agents include...
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I RiPpED one on the myc
isoniazid-prodrug, most imp, cidal in growing cells and vice versa, met by acetylization, inc exc of vit 6-->pellegra rifampin- inh dna dependent rna polymerase,hepatoxicity and red colored body fluids pyrazinamide. (PY In Fat Ass)Inh of Fatty Acid Syn once it gets into macrophages etambutol- (ethanol inh arabs) inh arabinosyl transferase needed for CW, cidal,optic neuritis, red-green vision Dapsone- inh folate syntahse like sulfamides, g6pdh-->hemolytic anemia, txs leprosy |
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An Antimyobacterial agent that causes niacin def.(pellagra) b/c an increased excretion of vit B6, optic neuritis, and hepatoxicity, and slow acetylators have more effects?
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isoniazid
could be taken up to 2 years I RIPpED onthe myc |
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rifampin causes
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red body fluids and hepatotoxicity, its an INDUCER of p450
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pyrazinamide is a ______ andand causes _______
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prodrug
gout and hepatitis |
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ethambutol causes
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optic neuritis
-decrease in red-green vision (inh ARABinonyl transferase |
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dapsone is for
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mycobacterium Leprae-Honson's disease
Leprosy related to the sulfamides(same SE) -Folic acid pathway SE-hemolytic anemia in g6p def pts |
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antimycobacterial agents arent responsive to Cell Wll inh like..
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erythromycins (Macrolide from MATS MLS lid)
and Tetracyclines |
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when do use antibiotic combinations??
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1. mixed bact infections
2. severe inf of unknown origen 3. for synergy-sulfanamides and trimethaprim -b-lactams and aminoglycosides (toby neo and kanya gently strept ami to a net) -for tx of Tb 4. to reduce dose of a drug w/ severe SE |
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Problems with ABs?
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2 agents with same toxicity-
vancomycin and erythromycin cause ototoxicity or px a drug that inh CW and one that needs to pass throough there |
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what is present in fungal cell membranes that is not present in cell membranes of other cells?
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ergosterol
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what are the polyene antibiotics?
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nystatin
amphotericin B natamycin used TOPICALLY to treat fungal skin infections they bind to ergosterol |
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mech. of the polyene antibiotics?
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bind to ergosterol
used topically for fungal skin infections |
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what is used to treat ringworm
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tolnaftate
ciclopirox terbinafine (also miconazole and other azoles are used for candida and ringworm) |
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what is used to treat both ringworm and candida
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miconazole and other azoles
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which drugs are used TOPICALLY to treat fungal skin infections
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the polyene antibiotics: nystatin, amph B, natamycin
the ones for ringworm: tolnaftate, ciclopirox, terbinafine the ones for candida and ringworm: miconazole and other azoles |
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when would you give a SYSTEMIC drug for a fungal skin infection
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for toe and fingernail infections since it would be hard to apply a topical antibiotic to it since the nail is covering it
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what drugs are used systemically to treat fungal skin infections
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griseofulvin
terbinafine |
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griseofulvin and terbinafine are given _____ to treat fungal skin infections
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systemically
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mech of action of griseofulvin
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taken up by growing skin cells and concentrated in keratin
binds to fungal microtubules and inhibits mitosis used systemically to treat fungal skin infections |
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side effects of griseofulvin
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(a systemic drug for fungal skin infections)
rash if you are allergic to penicillin induces p450 headach |
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mech of action of terbinafine
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(a systemic drug used for fungal skin infections)
inhibits synthesis of ergosterol by inhibiting the enzyme squalene epoxidase |
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side effects of terbinafine
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inhibits p450
liver damage |
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what is the drug of choice for severe systemic fungal infections
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amphotericin B
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what is the mech of action of amphoteracin b
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causes membrane leakage by binding to ergosterol in fungal cell membrane
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side effects for amphotericin b
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impaired renal function in >80% of patients!!!!!!!!!
thrombophlebitis (irritation at site of injection) fever nausea headache convulsions anemia |
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is amphotericin b soluble or insoluble in water?
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insoluble
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what drugs can be used to treat systemic mycoses?
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ampho. B
imidazoles ("azoles") triazoles ("azoles") flucytosine terbinafine echinocandins ("fungin") |
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what are the imidazoles
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ketoconazole
clotrimazole |
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what are the triazoles
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fluconazole
itraconazole posaconazole voriconazole |
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side effects of ketoconazole (imidaolze drug used to treat systemic mycoses)
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decrease adrenal and gonadal steroids
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side effects of itraconazole
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(a triazole drug used to treat systemic mycoses)
strong p450 inhibitor causes heart problems |
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side effects of voriconazole
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(a triazole drug used to treat systemic mycoses)
visual disturbances fetal damage |
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which triazole causes fetal damage
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voriconazole
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which triazole causes heart problems
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itraconazole (corazon is heart in spanish and this drug is spelled similar to that)
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how does flucytosine work?
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it is used to treat systemic mycoses
a pyrimidine analog that inhibits thymidine synthesis and is converted to 5-FU in the fungus |
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how does terbinafine work
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it inhibits squalene epoxidase and is used to treat systemic mycoses
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side effect of terbinafine
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liver damage
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what drug is used in combination with amphoteracin b so that you can lower the does of ampho B which decreases side effects?
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flucytosine can be used in combo. with ampho b
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what are the echinocandins?
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"fungin's"
caspofungin micafungin anidulafungin |
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what are the side effects of the echinocandins ("fungins")
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fetal damage
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mech of action of echinocandins
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inhibit synthesis of a fungal cell wall component
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what drugs are used to treat herpes infections
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"cyclovir/ciclovir + f.f.c."
acyclovir valacyclovir famciclovir ganciclovir valganciclovir cidofovir foscarnet fomivirsen |
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which are the only herpes drugs that are NOT prodrugs?
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foscarnet
fomivirsen both of these are used to treat cytomegalovirus (a type of herpesvirus) |
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mech of action of all the agents used to treat herpes (and cytomegalovirus) and hepatitis b... EXCEPT FOMIVIRSEN
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inhibit DNA polymerase
fomivirsen is an antisense molecule that binds to cytomegalovirus mRNA |
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what drugs are used to treat Hep B and how do they work
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"EAL"
they inhibit DNA polymerase entecavir...liver problems, lactic acidosis adefovir...renal, liver problems lamivudine...inhibits DNA pol and reverse transcriptase |
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which herpes med is orally available? GAiN VALs CIDer
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valacyclovir...it has first pass metabolism which is good since it is a prodrug so the liver breaks it down to acyclovir
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side effects of acyclovir
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with IV doses:
renal damage delerium (enters CNS) |
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side effects of ganciclovir
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neutropenia
thrombocytopenia fetal defects |
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side effects of cidofovir
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kidney damage
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side effects of foscarnet
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kidney damage
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what drug is injected directly into the eye for CMV retinitis
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fomivirsen (an antisense molecule that binds to CMV mRNA)
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which agent is used to treat hep b and works by inhibiting both DNA polymerase and reverse transcriptase
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lamivudine
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side effects of adefovir
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kidney and liver problems
(used to treat hep b) |
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s.e. of entecavir
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liver problems
lactic acidosis (used to treat hep b) |
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what drugs are used to treat RSV
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ribavirin
palivizumab |
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mech of action of ribavirin (used to treat rsv)
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a guanosine analog
it is phosphorylated in the cell and inhibits rna dependent rna polymerase |
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side effects of ribavirin (used for rsv)
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fetal damage
hemolytic anemia lung damage heart damage |
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mech of action of palivizumab (used for rsv)
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humanized monoclonal antibody directed against the binding site on rsv to prevent it from fusing to the target cell
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influenza A drugs
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amantadine...renal failure, teratogen, enters cns
rimantadine...fewer SE's both block the uncoating of the virus |
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Częściowo ( what is this ?? )
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Partially
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which drug can also be used to treat parkinson's
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amantadine (it increases release of dopamine)
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what are the drugs used to treat influenza A and B
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zanamivir (relenza)
oseltamivir (tamiflu) both block the release of newly formed viruses from the cell by INHIBITING NEURAMINIDASE! |
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which drug is administered as a dry powder
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zanamir (relenza) to treat influenza A and B
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what can be used to treat hepatitis virus and how does it work
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recombinant interferon alpha...treats Hep B and C
enhances normal immune cell functions can inhibit viral mRNA replication |
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what are the different classes of HIV drugs
|
nucleoside analog reverse transcriptase inhibitors (DAZLEST)
non-nucleoside reverse transcriptase inhibitors (NEED) protease inhibitors ("navir") fusion inhibitors (ME) integrase inhibitor (reltegravir) |
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what are the nucleoside analog reverse transcriptase inhibitors used to treat HIV
|
DAZLEST
didanosine abacavir zidovudine lamivudine emtricitibine stavudine telbivudine |
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what are the non-nucleoside analog reverse transcriptase inhibitors used to treat HIV
|
NEED
nevirapine efavirenz etravirine delaviridine |
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what are the protease inhibitors used to treat HIV
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"navir"
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what are the fusion inhibitors used to treat HIV
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ME
maraviroc-blocks on host cell enfuvirtide-inh hiv from binding cd4 |
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what is the inTEGrase inhibitor used to treat HIV
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relTEGavir
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which HIV drugs can cause steven's johnson's snydrome and liver damage
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nevirapine
etravirine delaviridine (non-nucleoside reverse transcriptase inhibitors) |
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common s.e. of ALL the nucleoside analog reverse transcriptase inhibitors used to tread HIV
|
(DAZLEST)
ALL can cause: anemias neutropenias muscle pain and damage didanosine...pancreatitis abacavir...hypersens. rxn lamivudine...fewer se's |
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side effects of the protease inhibitors used to treat HIV
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"navir"
nausea inhibit p450 altered fat distribution (less fat in face and limbs, more fat in gut, chest, back) increase triglycerides increase hyperglycemia increase in diabetes |
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what is the most potent known p450 inhibitor
|
ritonavir ("right on avir")...a protease inhibitor used to treat HIV
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how does the FUsion inhibitor for HIV enfuvirtide work
|
enFUvirtide
inhibits binding of HIV to the CD4 target cell by binding to a specific site ON THE VIRUS (maraviroc binds to a site on the host cell) |
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s.e. of enfuvirtide
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FUsion inhibitor used for HIV
irritation at injection site possible insomnia |
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how is enfuvirtide given (HIV fusion inhibitor)
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injection
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side effects of maraviroc (HIV fusion inhibitor)
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hepatotox.
allergic rxn |
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what is the integrase inhibitor used for HIV and how does it work
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reltegravir
prevents viral replication in the cell |
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which HIV drug can cause arrhythmias
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atazanavir (protease inhibitor)
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which HIV drugs can cause allergic rxn b/c they contain sulfur
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fosamprenavir
tipranavir |
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chlorophenical..
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inhibits peptidyl transferase
causes gray aby syndrome aplastic anemia and megablastic anemia in g6pdh def pts. |
