Mech of Action therapy/use Toxicity Mech of Rest Other

ANTI-VIRALS
NUCLEIC ACID SYN + UT ANTISEPTICS
hypersensivitiy;
kernicterus
(newborns); alt dihydropteroate synthetase w/ bacteristatic;
blocks form of folate by compet inhibiting gram + & -; nocardiosis, taxoplas + crystalluria in decreased affintity for drug; low rickettisae are
sulfamethoxazole dihydropteroate from PABA UTI; kidneys uptake; increased intracell {PAPA} resistant; p450
increased [ ] in
used in combo w/ septa (bactrim); lower affinity for DHFR; overprod prostrate and vag
Trimethroprim inhibitor of DHFR (micro not mammalian) UTI, PCP, H. flu, stret pneumo same as sulfa DHFR fluids
don't use under age
18 or in preg/nursing
b/c may damage bactericidal; NOT
cartilage and prod of altered DNA gyrase; effective against
Fluoroquinolones (Ciprofloxacin + Ofloxacin) inhibits DNA gyrase gram + & - (often w/ B-lactams) arthropathy decreased uptake Anaerobes

(+): prod of B-lactamase, alt in

essential PBPs, inability to act
inhibits Stage III (note vancomycin & autolysins; (-) overexp of efflux
bacitracin inhibit stage II); affect bact pump, prod of B-lactamase, alt in bactericidal; only work
B-LACTAMS wall syn esst PBPs, alt in porin on actively growing
don't go to CSF, eye +
PCN G: strept pyogenes, strept prostrate (PCNs in
pneum, n mengi (basically +/-); IV general); all excreted
PCN V:alt for Strep A, B, C & G, hypersensivity, by kideny except
PCN G & PCN V strept pneumoniae (oral) anaphylaxis nafcillin--> bile)
Pencillinase prod staphylococci
Oxacillin Pencillnase-rest PCN (NOT MRSA) oral or pareneteral
Pencillinase prod staphylococci Exec in BILE;
Nafcillin Pencillnase-rest PCN (NOT MRSA) parenteral
bact listed for PCNG + group D oral; pencillase
Ampicillin Broad spectrum PCNs strep and more gram (-) (H. flu)_ sensitive
Amoxicillin (+ clavulanic acid = Augmentin "" "" ""
gram (-)s, psuedomonas IV; pencillase
Ticarcillin (+ clavulanic acid = Timentin) "" aeusinosa klebsiellla is usually resistant suspectible
Klebsiella (works 50%), some (-); parenterally;
Piperacillin "" combine w/ aminoglyc if serious pencillase sensitive
does NOT give
allergic rxn like
Aztreonam Newer class + B-lactamase inhibitors very specific for Gram (-) Rods PCN
used for serious only --> broadest
spectrum (does NOT work w/
Imipenum "" MRSA)
" "; inhibitors of B-lactamases; combined
Clavulanic acid + Sulbactam w/ other drugs NOT antibacterial
 resistant to
pencillinases but
maybe inactivated by
other
CEPHALOSPORINS effect bact wall syn like PCN cephalosporinases
gram (+) cocci (not enterococci or
Cephalexin FIRST Generation MRSA); limited gram (-) oral
increased activity ag gram (-); H.
Cefuroxime SECOND generation flu, B fragilis + N gonorrhaeae parenteral
all produce
disulfiram-like rxn w/
enteric gram (-); crosses BBB (tx EtOH EXCEPT Ceftriaxone has longer
Cefotaxamine + Ceftriaxone THIRD generation meningtis), e coli, k pneumonia ceftizoxime) 1/2 life

inhibition of cell wall syn by blocking tx of

the peptidoglycan subunti to the nascent 1st choice for tx of MRSA + PCN Ototoxicity + genes prod new depsipetide; body IV unless tx GI then
Vancomycin cell wall rest strept pneum nephrotoxicity changes to D-ala-D-lac so can't bind oral; bactericidal

INHIBITORS of PROTEIN SYN CLE - 50s;TAg - 30s;

aerobic gram (-) bacilli
blocker of Initiation; inhibit only gentamicin, tobramycin,
AUROBES b/c diffuse via O2 dept amilcacin: used for systemic; alt binding site on 30s; decrease
Aminoglycosides process streptomycin: TB Ototoxicity + nephro uptake, prod enzy that mod drug binds 30s; parenteral
alt tx for N. gonorrhaoe that is rest
to PCN + tetracyline; or for preg
Spectinomycin blocker of Translocation women binds 30s; IM
Aplastic anemia; 50s of 70s; inact by
gray baby glucuronyl transferase
syndrome; rev bone --> mod dose in liver
Chloramphenicol blocker of Elongation serious infections marrow tox prod CAT that inactivates drug disease

photosens; Fanconi
Syn; don't give
under age 18 or
preg --> deposits in 30s; imparied by milk
Tetracycline blocker of Elongation mycoplasma penumoniae, RMSF teeth in bones + antacids

50s of 70s; inact by

glucuronyl
hepatotox + transferase --> mod
Erythromycin blocker of Translocation legionnares, mycoplasma, etc esinophilia methylase -mod binding site dose in liver disease
mod to severe Anaerobes; also
Clindamycin blocker of Elongation PCP + taxo in AIDS hepatotox, rashes methylase -mod binding site
vanomycin rest e. faecium (NOT e.
faecalis), MRSA, PCN rest
Streptogramins pneumonia 50s of 70s
also Reverisble MAO inhibitor - do
NOT give w/ MAOIs, tricy dep, avoid
Oxazolidinones (Linezolid) foods high in tyramine "" 50s
 Disulfiram rxn w/
ETOH; do NOT use
Metrondazole (Flagyl) disrupts DNA -->cell death ANaerobic only in preg

ANTI-VIRALS
Tx for Influenza:
accumulation can
occur b/c therapeutic
blocks uncoating of Inf A by bind to the dose is 1/2 of toxic
Amantadine M2 ion channel prevention; inf A only dose
zanamivir: throat _
inf A & B; best for prevention but nasal discomfort +
can decrease symptoms & bronchospasms in
Zanamivir (Relenza) + Oseltamivir (Tamiflu) neuraminadase inhibitors duration asthmatics
Tx for Herpes Simplex
phosph by thrymidine kinase (but not by
cellular) --> inhibits herpes DNA herpes genitalis, labialis, keratitis, carcinogenic +
Acyclovir polymerase--> DNA chain terminator enceph + zoster teratogenic
Tx for AIDS
Azidothymidine (AZT) RT inhibitor
lipodystrophy +
Ritonavir protease inhibitor hyperlipidemia
fusion inhibitor; blocks HIV affinitiy to high incidence of
CD4+ cells by interfering w/ viral pg41 pneumonia + skin twice/day subcut
Enfuvirtide mediated fusion --> blocks HIV entry rxns injections; $20,000/yr
drug combo of protease inhibitor + 1 or 2
HAART RT inhibitors

ANTI-FUNGALS
10X selectivity for
forms complex w/ ergosterol + forms erosterol over chol liposomal form:
transmemb pore --> ions leak out -> but still low therp increased therp levels
Amphotericin B osmotic instability -> death crypto meg, candidia, cocid meng index; Nephrotoxin rare + lower toxicity; IV

at high levels: bone

marrow suppression,
blocks DNA syn: forms complex w/ hair loss, GI distress, mutation in cytosine permease or
5-Fluorocytosine thymidylate synthase hapatotox cytosine deaminase rarely used alone
Gi, lower liver fxn;
Azoles: Ketoconazole, Fluconazole, blocks ergosterol syn by inhibiting C- blastomycosis, histoplasmosis, drug interactions b/c only Fluconazole pent
Intraconazole 14alpha demethylase (p450 dept enzy) candidiasis p450 CNS

Tx for Asthma
not used prophy or
Short acting B2 selective agonists; maint --> potential for
Albuterol, Levalbuterol, Metaproternol bronchodilator prompt rev of bronchospasm desen (controversial)
only partial agonist -
Long acting B2 selective agonists decreased risk of
(more lipophilic); inhibits release from exercise induced asthma + desent; often
mast ells, decreases edema, increases nocternal ashtma; May also be combined w/ inhaled
Salmeterol, formoterol mucociliary clearance used in COPD steroids --> Advair
 cAMP physphodiesterase inhibitor -->
bronchodilation; antagonizes adenosine maintance + prophy --> decreases
by blocking receptor --> decreases severity; may also improve
Theophylline inflammation; airlfow in COPD low therp index
Anti-inflammatory: decreases # of
inflam cells & vascular leakage & muc
Inhaled Glucocorticoids prod while increases # of B2 receptors
Anti-inflammatory: non steroidal, maintance: 2-4wks before optimal
Cromolyn Sodium inhibitor of mast cell degran effects
Leukotriene receptor anatagonists:
bronchodil, decrease much secretion,
Zafirlukast decrease # of esino + basoph
oral but not proven to
low toxicitiy but do be as preditable as
Zileuton 5-lipxygenase inhibitor interfere w/ p450 ICS
monoclonal Antibody against IgE that
decrease IgE binding to mast cells + expensive,
Omalizumab decrases inflammation effectiveness TBA

does NOT cross BBB

Tx for COPD b/c quat

Muscarnic Receptor Antagonist:

bronchodil by decreasing parasym tone; more prom + therap use in COPD
Ipratropium (Atrovent) may also lessen prod of muc gland sec than astham
M1 & M3 selective anatagonist; since
no block of M2 it does not enhance
Tiotropium neurotran release
long acting B2 recep agonists are also good (salmeterol)
theophylline may also improve airflow

6mo: isoniazid, rifampin +

pyrizinamide for 2mo,; INH + rifampin
for next 4 mo; can add ethambutol if
Tx for TB INH rest

hepatox; peripheral overprod of InhA gene prod gives bactericidal for active
also used 6-12mo prophy after + CNS neuropathy; low rest; mut or deletion of TB; met by acetylation
Isoniazid penetrates intracell exposure uses p450 katGgene (catalase) gives high rest (rapid in Asians)
hepatox, uses p450,
can decrease effect
Rifampin inhibits DNA dept RNA poly of contraceptives
optic neuritis
(red/green discrim)
recovers after drug dont use by itself b/c
Ethambutol (also used for MAC) removed of resistance
hepatox;
hyperuricemia don't use by itself b/c
Pyrazinamide (gout) of resistance
 Ethambutol + azithromycin or
clarithromycin; tx is for LIFE; rifabutin
Tx for Mycobacterium Avium Complex used for prophy

Tx for Pulmonary Arterial HTN

prostacyclin therapy: vasodil, ant-prolif, improves exercise intolerance,
Epoprostenol decreases thrombosis hemodyn + long term survival short 1/2 life: 3min; IV

antagonist of ETA & ETB endothelin

receptor: decreases vasoconst, prolif of improves pul hemodyn, exercise
Bosentan smooth m, fibrois, and proinflamm med capacity, and 2yr survival liver toxicity
works through Nitric Oxide pathway; one study showed it
elevates cGMP in pulm arterial cells --> was as effective as
Sildenafil vasodil used mainly for old men to get it up bosentan

Tx for Nicotine Addiction

only one FDA
"atypical" catecholamine/serotonin begin 1 wk AFTER cessation; approved; doubles
Buproprion reuptake inhibitor continue 7-12wks quit rates
NOT FDA approved;
Rimponabent B1 receptor anatagonist increases cessation