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91 Cards in this Set

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penicillin G (Bicillin)
original form, orally ineffective. Used against G(+) and G(-)cocci (not rods or anaerobes). *S. pneumoniae (much resistance), Staphs, Neisseria meningitidis, Clostridium, Treponema pallidum
penicillin V (Veetids)
better oral absorption than penicillin G, otherwise very similar (still not good orally for serious infections) (G+ and G(-)cocci. Not rods or anerobes)
oxacillin (Bactocill)
beta-lactamase resistant, used against staph that make penicillinase. USE: mixed staph/strep infections. Enterococci resistant. MRSA drug resistance is growing problem - also resistant to cephalosporins, aminoglycosides, erythromycin, tetracycline and clindamycin.
amoxicillin (Amoxil)
penicillin good for gram(-) bacilli (nonlactamase) (e.coli, H.influenzae, salmonella, shigella). Oral absorption reduced if taken with food. S.effect: rashes. Not penicillin substitute (reduced efficacy against gram(+))
ampicillin (Principen)
penicillin good for gram(-) bacilli (nonlactamase) (e.coli, H.influenzae, salmonella, shigella). Oral absorption reduced if taken with food. S.effect: rashes. Not penicillin substitute (reduced efficacy against gram(+))
piperacillin (Pipracil)
penicillin: anti-pseudomonal (non-penicillinase). Parenterall administration - reserved for serious infections
ticarcillin (Ticar)
penicillin: anti-pseudomonal (non-penicillinase). Parenterall administration - reserved for serious infections
clavulanic acid
beta-lactamase inhibitors (suicide) - structurally like penicillin, won't hydrolyze off enzyme after lactam is cleaved. Synergism when used with amoxicillin (Augmentin)
sulbactam
beta-lactamase inhibitors (suicide) - structurally like penicillin, won't hydrolyze off enzyme after lactam is cleaved. Synergism when used with amoxicillin (Augmentin)
tazobactam
beta-lactamase inhibitors (suicide) - structurally like penicillin, won't hydrolyze off enzyme after lactam is cleaved. Synergism when used with amoxicillin (Augmentin)
cephalosporins
most widely prescribed antibiotic. Inhibit cell wall synthesis. Resistance via cephalosporinase, penicillin resistance mech. Cross-sensitivity with penicillin allergy. S.effects well tolerated: nephrotoxicity more than penicillins, superinfection if G(-) inhibition
cephalexin (Keflex)
1st generation cephalosporin. Oral. G(+) and some commmunity acquired G(-). Surgery prophylaxis. Staph,strep.
cefazolin (Ancef)
1st generation cephalosporin. Parenteral. G(+) and some community acquired G(-). Surgery prophylaxis. Staph,strep
cefaclor
2nd generation cephalosporin. Oral. Extended G(-) spectrum (lessG(+)), some efficacy vs oral and bowel anaerobes.
cefixime (Suprax)
3rd generation cephalosporin. Oral. Expanded G(-) spectrum (lessG(+)), PENETRATE CNS. Use: meningitis from pneumococci, menigococci. Also H.influenza, susceptible E.coli, Dlebsiella, penicillin-resistant N.gonorrhea
cefepime (Maxipime)
4th generation cephalosporin. Parenteral. Extended G(-), but also G(+). PENETRATES CNS. Enhanced resistance to beta-lactamase. USE: enterobactericiae, pseudomonas.
carbapenems
same mechanism of action as penicillin. Parenteral. Renal metabolism and excretion. CNS possible. USE: G(-)rods, G(+), anaerobes. Resistant to many beta-lactamases. Serious nosocomial infections, mixed infections. NOT community acquired, MRSA, VRE.
imipenem (Primaxin)
carbapenem
meropenem (Merrem-IV)
carbapenem. Does not need coadministration of cilastatin
cilastatin
carbapenem
aztreonam (Azactam)
monobactam. Poor oral absorption. IM or IV. Rapid renal elimination. Penetrates inflamed CNS. USE: G(-) rods (similar to aminoglycosides, but less toxic)
polymyxins
cationic peptide detergents (made by soil bacteria) disrupt bacterial cell membranes. Applied topically.
bacitracin
interferes with cell wall biosynthesis. Nephrotoxicity limits use to topical application. Oral for gut infection.
daptomycin (Cubicin)
cyclic lipopeptide. Mechanism: depolarizes G(+) bacteria, rapidly bactericidal. IV admin, renal elim (adjust dose w/renal insufficiency). Resistance observed, cross resistance not expected. S.effects: mm pain/weakness. USE: skin and soft tissue infections from G(+). S.aureus (MRSA), strep, and vanc-sensitive enterococcus faecalis. MRSA bacteremia.
fosfomycin (Monurol)
inhibits cell wall biosynthesis (blocks peptidoglycan syn.). Well absorbed, distributed. Low CNS levels unless inflamed. Excreted unchanged in urine. Resistance if multiple doses in monotherapy. S.effects: diarrhea, vaginitis. USE: single dose oral tx of uncomplicated UTIs in women caused by susceptible E.faecalis and E.coli
vancomycin (Vancocin)
inhibits synthesis of cell wall by blocking precursor formation. Poor oral absorption. No IM. Distributes throughout body, including CNS. Excreted via kidney, dose adjustments if renal fx (high dose oto and renal toxicities). Plasmid encoded resistance leads to latered cell wall subunits. USE: G(+), MRSA, penicillin-resistant s.pneumonia. combo with aminoglycoside is synergistic
the beta lactams
penicillins, penicillinase inhibitors, carbapenems, monobactams, cephalosporins. 2 membered ring, smaller ring is lactam
amikacin (Amikin)
aminoglycoside. Binds 30s subunit (bactericidal). Also causes misincorporation of a.acids. Poor oral; IM or slow IV. Excreted by kidneys. Ototoxicity, nephrotoxicity. USE: aerobic G(-) w/ beta lactam for G(+). Significant toxicity limits use
gentamicin
aminoglycoside. Binds 30s subunit (bactericidal). Also causes misincorporation of a.acids. Poor oral; IM or slow IV. Excreted by kidneys. Ototoxicity, nephrotoxicity. USE: aerobic G(-) w/ beta lactam for G(+). Significant toxicity limits use
neomycin
aminoglycoside. Binds 30s subunit (bactericidal). Also causes misincorporation of a.acids. Poor oral; IM or slow IV. Excreted by kidneys. Ototoxicity, nephrotoxicity. USE: aerobic G(-) w/ beta lactam for G(+). Significant toxicity limits use
tobramycin
aminoglycoside. Binds 30s subunit (bactericidal). Also causes misincorporation of a.acids. Poor oral; IM or slow IV. Excreted by kidneys. Ototoxicity, nephrotoxicity. USE: aerobic G(-) w/ beta lactam for G(+). Significant toxicity limits use
tetracycline (Sumycin)
binds 30s subunit (bacteriostatic). Binding Ca in gut reduced uptake. CNS, placenta, breast milk distribution. Oral, parenteral, topical (eye). Excreted by kidneys. Metabolized by CYP, BCP efficacy reduced with tetracycline. S.effects: GI, AAC, photosensitivity, discolored growing teeth. USE: lyme, RMSF, Qfever, m.pneumonia, chlamydiae, community acquired resp infections, broad spectrum G(-), G(+), amoeba.
doxycycline
tetracycline. binds 30s subunit (bacteriostatic). Binding Ca in gut reduced uptake. CNS, placenta, breast milk distribution. Oral, parenteral, topical (eye). Excreted by liver, use with renal failure is ok. Metabolized by CYP, BCP efficacy reduced with tetracycline. S.effects: GI, AAC, photosensitivity, discolored growing teeth. USE: lyme, RMSF, Qfever, m.pneumonia, chlamydiae, community acquired resp infections, broad spectrum G(-), G(+), amoeba.
azithromycin (Zithromax)
macrolide. Binds 50s subunit (bacteriostatic). Oral or IV (IM painful). Hydrolyzed in stomach. No CNS. Lots in liver, active form excreted in bile. Maybe safest antibiotic. S.effects:GI, cholestatic jaundice, fewer drug interactions than eryth. USE: G(-)G(+) aerobes, m.penumoniae, legionella, b.pertussis (anaerobes). often used for penicillin allergic pts. USE: STDs
clarithromycin (Biaxin)
macrolide. Binds 50s subunit (bacteriostatic). Oral or IV (IM painful). Hydrolyzed in stomach. No CNS. Lots in liver, active form excreted in bile. Maybe safest antibiotic. S.effects:GI, cholestatic jaundice, likely inhibits P450. USE: G(-)G(+) aerobes, m.penumoniae, legionella, b.pertussis (anaerobes). often used for penicillin allergic pts
erythromycin (E-mycin)
macrolide. Binds 50s subunit (bacteriostatic). Oral or IV (IM painful). Hydrolyzed in stomach. No CNS. Lots in liver, active form excreted in bile. Maybe safest antibiotic. S.effects:GI, cholestatic jaundice, likely inhibits P450. USE: G(-)G(+) aerobes, m.penumoniae, legionella, b.pertussis (anaerobes). often used for penicillin allergic pts
telithromycin (Ketek)
ketolide. Binds 50s subunit. (-cidal vs s.pennumoniae. derivative of macrolide (erythromycin). Improved acid stability, increased affinity for bact ribosome, reduced resistance. Oral, can take with food. Eliminated by both liver and renal. S.effects:GI, visual. not good with m.gravis, cisapride, simvastatin. USE: community resp infections (s.penumoniae, h.influenzae, moraxella catarrhalis, some s.aureus
clindamycin (Cleocin)
lincomycin. Binds 50s subunit. Oral, IM, IV. No CNS. Yes placenta. Enterohepatic cycling. Similar resistance as erythromycin. S. effects: p.colitis, skin rashes, thrombophlebitis. USE: dental (B.fragilis), G(+) if pen allergic, in combo with aminoglycoside or cephalosporin for anaerobe (penetrating wound, pelvic abscess)
quinuprisitin
streptogramin. *Synercid with dalfopristin. Bind 50s subunit. No oral, give parenteral. Liver metabolized, bile and renal excretion. No oto or nephro toxicity, inhibits met of cyclosporine, Ca channel blockers, HIV meds, and others. USE: VRE
dalfopristin
streptogramin. *Synercid with quinupristin. Bind 50s subunit. No oral, give parenteral. Liver metabolized, bile and renal excretion. No oto or nephro toxicity, inhibits met of cyclosporine, Ca channel blockers, HIV meds, and others. USE: VRE
chloramphenicol (Chloromycetin)
binds 50s subunit (bacteriostatic) by blocking transpeptidation reaction. Partially inhibits eukaryotes too. CNS, placenta, breast milk distribution. Enterohepatic cycling of glucuronidated metabolite. Inhibits P450. tematologic toxicitytoxicity greatly limits use. USE: severe anaerobic infections where others won't work.
linezolid (Zyvox)
new ribosomal binding site - no cross resistance. Orally available. Liver met, renal excret. S.effects: diarrhea, HA, vomiting, mild thrombocytopenia. USE: vanc. Resistant enterococcus faecium, multiple drug resistant organisms
mupirocin (Bactroban)
reversible inhibition of bact isoleucyl tRNA synthetase (bactericidal). USE: topical - impetigo(s.aureus, s.pyogenes) Systemic admin quickly metabolized to inactive form. Resistance rarely observed, happens if modified tRNA made.
50s antagonism drugs
clindamycin, chloramphenicol, erythromycin - waste of time to use together, they compete for the same binding site
sulfamethoxazole
sulfonamide. Competitively blocks binding of PABA and dihydropteroate synthase (DHPS), used to make folic acid. Oral, IV. CNS. Liver met, renal excret (reduce dose in renal failure). G(+)G(-), malaria, t.gondii (CNS), UTIs. Cross resistance to all sulfas typical - mutant DHPS on plasmid, more PABA, efflux pumps. s.effects: GI, rash. bone marrow, liver toxicity. hemolytic anemia with G6PD deficiency, Kernicterus(competes for albumin binding) STEVENS-JOHNSON SYNDROME.
trimethoprim (Trimpex)
DHFR inhibitor - folic acid synthesis (selective for bact).
tmp-sulfa (Bactrim, Septra)
DHFR inhibitor+sulfonamide - synergistic bactericidal. Alone, both are bacteristatic. Oral. CNS, prostate. Renal excretion. G(+)G(-), not pseudomonas, anaerobes, atypical bacteria (legionella, chlamydia). Resistance: DHFR overexpression, mutant DHFR from plasmid. bone marrow suppression. anti-folate effects. USE: UTI, pneumocystis pneumonia, sinusitis, otitis media, community acquired MRSA
ciprofloxacin (Cipro)
fluoroquinolone (2nd gen). Bactericidal. Inhibit DNA gyrase and topoisomerase; irreversible DNA damage. Oral, IV (chelates with cations). Poor anaerobic activity. spectrum: nosocomial infections (pseudomonas, complicated G(-)), atypical bacteria (Legionella, mycoplasma, chlamydia). additive, not synergistic with other agents. NOT for kids. s.effects: GI, achilles tendon rupture, hepatotoxicity, superinfections. USE: complicated UTIs, bacterial prostatitis, pneumonia, STDs. 2nd line TB drug
levofloxacin (Levaquin)
fluoroquinolone. Bactericidal. Inhibit DNA gyrase and topoisomerase; irreversible DNA damage. Oral, IV (chelates with cations). Poor anaerobic activity. spectrum: nosocomial infections (pseudomonas, complicated G(-)), atypical bacteria (Legionella, mycoplasma, chlamydia). additive, not synergistic with other agents. NOT for kids. s.effects: GI, achilles tendon rupture, hepatotoxicity, superinfections. USE: complicated UTIs, bacterial prostatitis, pneumonia, STDs
moxifloxacin (Avelox)
fluoroquinolone. Bactericidal. Inhibit DNA gyrase and topoisomerase; irreversible DNA damage. Oral, IV (chelates with cations). Poor anaerobic activity. spectrum: nosocomial infections (pseudomonas, complicated G(-)), atypical bacteria (Legionella, mycoplasma, chlamydia). additive, not synergistic with other agents. NOT for kids. s.effects: GI, achilles tendon rupture, hepatotoxicity, superinfections. USE: complicated UTIs, bacterial prostatitis, pneumonia, STDs
deferasirox (Esjade)
oral iron. S.effect: headache, renal toxicity (peritubular damage)
desferoxamine (Desferal)
parenteral iron. S.effect: ototoxicity, ocular toxicity
ethambutol (Myambutol)
unknown mechanism. Mycolic acid incorporation into cell wall is inhibited, effective against dividing mycobacteria only. Oral, excreted unchanged in urine. S.effects: vision (optic neuritis, can't tell red from green), rash, fever, itching, joint pain, GI, HA, dizziness.
isoniazid (Nydrazid)
hydrazide of isonicotinic acid. Inhibits mycolic acid biosynthesis. Oral or parenteral, good distribution (CNS). Excreted in urine. S.effects:rash, fever, jaundice, periph neuritis
pyrazinamide (Rifater)
pyrazine analog of nicotinamide. Bactericidal. Oral, good distribution. Metabolized and excreted by kidney. S.effects: liver toxicity, GI.
rifampin (Rifadin)
inhibits bacterial DNA dependent RNA polymerase. Oral (food decreases uptake). Enterhepatic cycling. Induces hepatic metabolism (drug interactions). Good distribution (CNS). S.effects: rash, fever, nausea, vomiting, jaundice USE: TB, leprosy, N.meningitidis carriers
streptomycin
aminoglycoside. Ototoxicity, nephrotoxicity. 2nd line choice for TB because of toxicities (other aminoglycosides can also be used for TB - kanamycin, amikacin)
rifabutin (Mycobutin)
treatment for mycobacterium avium complex infection
dapsone (Avlosulfon)
sulfone - structurally and mechanistically related to sulfanilamide (competitively blocks DHPS and PABA). Used to treat M.leprae.
amphotericin B (Fungizone)
polyene. Target cell membrane. Systemic infections. Binds ergosterol, disrupts fungal plasma membrane (forms pore), administered as complex with deoxycholate. Poor oral absorption. IV, binds plasma proteins. No CNS. Relatively rare resistance. S.effects: chills, fever, aches, nausea (pretreat with NSAIDS) lipid forms less toxic.
nystatin (Nilstat, Mycostatin)
polyene. Binds ergosterol, disrupts plasma membrane (pore). Superficial infections. Topical only. Spectrum: Candida infections of skin, mucous, bowel.
clotimazole (Lotrimin)
imidazole. Inhibits ergosterol synthesis. Superficial infections. Topical only. USE: oral, vaginal, cutaneous candidiasis
ketoconazole (Nizoral)
imidazole. Inhibits ergosterol synthesis. Systemic infections. Oral with food (but not antacids or cimetidine) no CNS, CYP metabolism. Gynecomastia/menstrual irregularities (sex sterol synthesis). Long term Tx necessary but undesireable - replaced with triazoles (fluconazole and itraconazole) spectrum: chronic mucocutaneous candidiasis and paracoccidiodomycosis, non life threatening conditions - replacing amphoB, not usually a first choice
miconazole (Monistat, Micatin)
imidazole. Inhibits ergosterol syntehsis. Superficial infections. Topical only. USE: oral, vaginal, cutanous candidiasis
fluconazole (Diflucan)
triazole. Inhibits ergosterol biosynthesis. Systemic infections. Oral. Excreted unchanged in urine. CNS. Competes with drugs for metabolism by P450, increasing their levels. Spectrum: oropharyngeal and esophageal candidiasis.
voriconazole (Vfend, Voritrol)
triazole - newer. Inhibits ergosterol biosynthesis. Systemic infections. Oral. Excreted unchanged in urine. CNS. Competes with drugs for metabolism by P450, increasing their levels. Spectrum: oropharyngeal and esophageal candidiasis.
terbinafine (Lamisil)
allylamine. Inhibits squalene epoxidase (ergosterol biosynthesis). Superficial infections. Oral, topical. Liver metabolism (P450), renal excretion. Accumulates in hair and nails, secreted in sebum. Spectrum: oral - onychomycosis of toe/fingernail due to dermatophytes. topical - skin infections with trichophyton, candida
caspofungin (Cancidas)
echinocandin. Blocks fungal cell wall synthesis (beta (1,3)-D-glucan synthase). Systemic infections. IV only, renal and liver elimination (dose adj for liver only). USE: aspergillus and Candida. (Candidemia and abscesses, peritonitis, pleural infections, esophageal)
flucytosine (Ancobon)
DNA synthesis antimetabolite. Prodrug selectively activated in target cell to 5-FU which blocks thymidylate synthetase. Can be incorporated into RNA. Oral, CNS, excreted unchanged by kidneys. Often used with amphotericin B or a triazole. USE: Candidia, Cryptococcal
griseofulvin (Fulvicin, Gris-PEG)
target mitotic spindle (microtubule). Superficial infections. Natural product from Penicillium griseofulvin (cross allergicity with beta lactams). Oral (aided by fatty food). High affinity for skin - binds keratin. Need long admin. Not good topically. liver inactivates via demethylation (P450), excreted in urine. been around a long time - inexpensive - replaced by triazoles and terbinafine. Spectrum: epidermophyton, microsporum, trichophyton
tolnaftate (Tinactin)
antifungal for superficial infections
amantadine (Symmetrel)
antiviral - penetration inhibitor. Influenza A only. Blocks acidification of endocytic vescicle. Excreted unaltered by kidneys. S.effects: insomnia, CNS symptoms.
rimantadine (Flumadine)
antiviral - penetration inhibitor. Influenza A only. Blocks acidification of endocytic vescicle.
enfurtidine (Fuseon)
antiviral - penetration inhibitor
maraviroc (Selzentry)
antiviral - inhibitor of penentration - reversible block between gp120 and CCR5. HIV-1 only. Hepatotoxicity. Higher serum concentration with protease inhibitors, lower serum concentration with non-nuceloside RT inhibitor efavirenz. S.effects: hepatotoxicity preceeded by rash. also cough, URTI, rash, musculoskeletal symp.
ribavirin (Virazole)
antiviral - inhibitor of nucleic acid synthesis
foscarnet (Foscavir)
antiviral - polymerase/RT inhibitor. IV only. (-) DNA polymerase of HSV, CMV, and others. Gets into CNS. Seffects: renal, nausea, vomiting.
oseltamivir (Tamiflu)
antiviral neuraminidase inhibitor (inhibits release). Influenza A AND B. acute therapy if less than 2 days of symptoms. Pill or liquid esterified pro-drug well absorbed. Eliminated by kidneys. RARE steven's Johnson syndrome or anaphylaxis.
zanamivir (Relenza)
antiviral neuraminidase inhibitor (inhibits release). Influenza A AND B. acute therapy if less than 2 days of symptoms. Pill or liquid esterified pro-drug well absorbed. Eliminated by kidneys. RARE steven's Johnson syndrome or anaphylaxis.
acyclovir (Zovirax)
antiviral - nuceoside analog. Activated by viral thymidine kinase and inhibits DNA pol. Tx: 1ary and 2ndary HSV infections (encephalitis even), varicella zoster (immunocomp), prophylaxis in transplants
ganciclovir (Cytovene, Vitrasert)
antiviral - nuceoside analog. Prodrug phosphorylated by CMV, inhibits DNA pol. For immunocomp. Mngmnt of CMV retinitis, pneumonia, and GI lesions. Toxicity limits dosage: low WBC, platelets, renal impairment.
famciclovir (Famvir)
antiviral - nuceoside analog. Tx: acute herpes zoster and recurrent genital herpes in nrml pts.
idoxuridine
antiviral - nuceoside analog. Thymidine analog. Used topically to treat herpetic keratitis (cornea)
vidarabine (Vira-A)
antiviral - nuceoside analog. Adenine analog. Used IV to treat disseminated herpes in immunocomp (2ndry to acyclovir)
zidovudine (AZT) (Retrovir)
antiviral - RT inhibitor, nucleoside analog. Not selectively activated, but once activated, specific for HIV RT. Oral ok. Hard to tolerate side effects.
efavirenz (Sustiva)
antiviral - RT inhibitor, NOT nucelosidee analog (binds at diff site, combo good). Metabolized by P450. s.effects: skin reactions, hepatotoxicity
nevirapine (Viramune)
antiviral - RT inhibitor, NOT nucelosidee analog (binds at diff site, combo good)
indinavir (Crixivan)
antiviral - protease inhibitor. HIV polyprotien can't mature. Used in combo Tx. Major side effects: hyperglycemia, fat redistribution and many others..
ritonavir (Norvir)
antiviral - protease inhibitor. HIV polyprotien can't mature. Used in combo Tx. Major side effects: hyperglycemia, fat redistribution and many others..
enfuvirtide (Fuzeon)
antiviral - HIV fusion inhibitor. Binds gp41 of HIV-1. SQ admin 2x daily (like insulin). S.effects: injection site rxns, pneumonia, hypersensitivity rxns.
raltegravir (Isentress)
antiviral - HIV integrase inhibitor. HIV-1 only. Oral. For Tx experienced pts. Rifampin (TB drug) coadministration decreases serum concentration. Causes myopathy and rhabdomyolysis.