Term
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Definition
MOA: cyclic lipopeptide that interferes with bacterial membrane functions and pore formation
SOA: gram positives, esp. drug resistant bacteria
MOR: unclear
PK: IV
SE: elevated liver function tests and creatine phosphokinase-if pts have muscle weakness and pain -> discontinue drug |
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Term
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Definition
MOA: disrupts bacterial membranes by charge alteration
SOA: gram negatives
MOR: unclear
PK: topical (with neomycin and bacitracin), IV or IM as well
SE: few if used topically |
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Term
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Definition
MOA: not clear-attacks several pts of bacterial metabolism, mimics radiation damage
SOA: uncomplicated UTIs
MOR: altered levels of reduction enzymes
PK: PO, drug concentrated in urine
SE: turns urine brown, lung problems (pts on prolonged/prophylaxis treatment) |
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Term
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Definition
MOA: produces compounds toxic to DNA; reduced by pyruvate:ferridoxin oxidoreductase system -> promotes formation of intermediate compounds and free radicals that are toxic to the cell
MOR: not clear
SOA: obligate anaerobes and some protozoa (Giardia, Trichomonas)
PK: IV or PO, good tissue penetration (including CNS)
TOX: promote renal retention of lithium and decreased elimination of ergot derivatives, PTS SHOULD NOT DRINK ALCOHOL |
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Term
| Ciprofloxacin, Levofloxacin |
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Definition
fluoroquinolones
-DNA replication inhibitors
MOA: inhibit type II topoisomerases (DNA gyrase, topo IV), bactericidal
SOA: broad spectrum
-ciproflaxin: gram negs, esp. pseudomonas
-levoflaxacin: gram negs and gram pos (strep and staphy), atypical respiratory pathogens (mycoplasma, legionella), also active against myco-not 1st line agent
-used in ear or eye drops-staph, strep, pseduomonas
MOR: target modification in DNA gyrase, topo IV genes; altered uptake or efflux; plasmid-mediated drug modification by quinolone transacetylase
PK: well absorbed from upper GI tract, given orally or IV, tissue distrib good
-not recommended in pregnant pts or those under 18 bc of athropathy
AR: levofloxacin-elongation of QT interval -> arrythmias (not given to pts with heart condition); arthropathy in elderly pts, discontinued in pts who develop joint pain or tendonitis (achilles tendon) |
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Term
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Definition
protein synthesis inhibitor
MOA: inhibit isoleucine tRNA synthetase
SOA: gram positives, esp. drug resistant S. aureus
MOR: target site mutation
PK: topical on skin or mucosal surface, used to treat nasal carriage of S. aureus
AR: unclear |
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Term
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Definition
protein synthesis inhibitor
MOA: binds 50S subunit
SOA: broad, seldom used nowadays
MOR: acetylation, efflux pumping
PK: IV or PO
AR: aplastic anemia, bone marrow suppression, Gray syndrome (circulatory collapse, coma, death), dose adjustment for pt with liver problems |
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Term
| Tetracycline, Doxycycline, Tigecycline |
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Definition
tetracyclines
-protein synthesis inhibitors
MOA: bind 30S ribosomal subunit
SOA: broad, many unusual bacteria and some protozoa
MOR: frequently occuring, often found on plasmids and transposons, efflux pumping, some bact produce protein that binds to ribosome and blocks tetracycline action
-tigecycline not affected by these MOR
PK: IV or PO, good absorption from GI tract and reasonable tissue distribution (including CNS)
-antagonistic to beta-lactams
AR: nausea and photosensitivity common, sun exposure -> rash, not given to children under 8 and pregnant women b/c of teeth discoloration |
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Term
| Streptomycin, Gentamicin, Tobramycin |
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Definition
aminoglycosides
-protein synthesis inhibitors
MOA: bind to 30S subunit, usually bactericidal, initially penetrate by disrupting magnesium bridges b/w LPS moieties -> transported across cytoplasmic membrane in energy-dependent manner (inhibit by divalent cations, inc. osmolarity, acidic pH, anaerobic environ)
SOA: broad, most effect against gram negs, often given along with other antibiot (esp. beta-lactams), inactive vs anaerobes
MOR: common problem-resist genes found on plasmids/transposons; efflux pumping, dec uptake by outer membrane changes, enzymatic inactivation by acetylation, phosphorylation, adenylation
PK: post antibiotic effect (PAE) and conc. dependent killing, synergistic effect with other antibiotics, esp cell wall agents (beta-lactams)
AR: nephrotoxicity-serum levels of drugs and kidney function monitored, ototoxicity; not given to pts with dec. renal function
-admin IV or IM |
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Term
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Definition
Lincosamide
-protein synthesis inhibitor
MOA: binds the 50S ribosomal subunit
SOA: gram positives and some protozoa, but not gram negs (do not get across outer memb)
MOR: ribosome RNA methylation, altered ribosomal proteins, adenylation; both chromosomal and plasmid resistance genes
PK: well absorbed after oral uptake and good tissue penetration-but no CNS, given IV, PO, or topically
AR: some allergic rxns |
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Term
| Erythromycin, Clarithromycin, Azithromycin |
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Definition
macrolides
-protein synthesis inhibitors
MOA: bind 50S ribosomal subunit
SOA: broad, many unusual bacteria and respiratory pathogens, used as alternative for pts with PCN allergy
MOR: methylation of ribosomes, efflux pumping
PK: reasonable oral bioavail, given IV or PO, good tissue distrib
-azithromycin has longer half-life, taken less often; given to children and pregnant women
-extended release version of clarithromycin available
AR: erythromycin -> more nausea than others and greater risk of QT elongation (seldom used) |
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Term
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Definition
oxazolidinones
-protein synthesis inhibitor
MOA: bind to 50S subunit
SOA: gram positives, but not gram negs, usually used with multiply resistant staph and and enterococci
MOR: mutation of 23s rRNA
PK: IV or PO, good absorption
AR: thrombocytopenia-pts on long term therapy monitor platelets, CBC, creatinine, LFT; not give to pts on SSRIs |
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Term
| Quinupristin/dalfopristin combo (synercid) |
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Definition
streptogramins
-protein synthesis inhibitors
MOA: bind to 50S ribosomal subunit
SOA: gram positives, esp. drug resistant enterococci
MOR: target alteration by ribosome methylation, efflux pumping but resistance readily occurs if only one of two given
PK: IV
AR: athralgias and myalgias, dose needs adjustment of pt has liver problems |
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Term
| Sulfamethoxazole, Sulfadiazine, Dapsone, Trimethoprim (structure and MOA) |
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Definition
-all sulfa drugs are derivatives of para-aminobenzene sulfonamide
Trimethoprim: analog of dihydrofolic acid-binds bacterial dihydrofolic acid reductase blocking formation of folic acid, used in conjunction with sulfa drug (TMP-SMX, Bactrim)
Dapsone: analog of PABA, useful against mycobacteria (esp. leprosy), pnemocystis jirovecii/carinii (fungus) |
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Term
| Sulfamethoxazole, Sulfadiazine, Dapsone, Trimethoprim (SOA, MOR, PK, AR) |
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Definition
folate metabolism inhibitor
-cell wall synthesis inhibitor
-broad spectrum drugs active against gram positives and negatives, pneumocystis jirovecii/carinii (fungus), toxoplasma (protozoa)
MOR: major problem-mutated genes for target enzymes, high levels of expression of enzymes, newly transferred genes w/ resistant enzymes, altered uptake and efflux, resistance found on both chromosome and plasmids
PK: good bioavail, IV or PO, sulfa given with silver ions -> topical cream
AR: HIV pts -> neutropenia and exfoliative dermatitis; allergic rxns that can be severe (anaphylaxis), not given to those who have glucose 6-phosphate deficiency or are pregnant
-sulfa and trimethoprim -> synergistic |
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Term
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Definition
cell wall synthesis inhibitor (polypeptide)
MOA: inhibits dephosphorylation of the lipid carrier (blocks transfer of cell wall components)
SOA: gram positives mostly
MOR: unclear
PK: topical, often used with neomycin or polymixin B
AR: very few, rarely allergic rx -> anaphylaxis |
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Term
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Definition
-cell wall synthesis inhibitor (glycopeptide)
-binds to D-alanine and prevents cross-linking by steric hindrance
SOA: gram positives mostly, often used against gram positive infections in which organisms are resistant to other antibiotics (beta-lactams)
MOR: set of genes on transposon that encode enzymes that make cell wall with D-serine or D lactate
PK: usually IV, can be given orally, good tissue avail, not CNS w/o inflamm, conc of vanco monitored to determine time above MIC
AR: rapid IV admin -> red man syndrome (histamine mediated rxn-flushing and redness of upper body), nephrotoxicity (esp. w/aminoglycosides), linear IgA bullous dermatosis |
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Term
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Definition
monobactam
-cell wall synthesis inhibitor
-admin IV
-same target as penicillin |
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Term
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Definition
carbapenem
-cell wall synthesis inhibitor
-administered IV
-same target as penicillin
-cilistatin has no antibacterial action but prolongs half-life of Imipenem, prevents nephrotoxic effects |
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Term
| Cephalexin, Ceftazidime, Cefotaxime, Ceftriaxone |
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Definition
cephalosporins
Cephalexin: 1st gen (PO)
Ceftazidime, Cefotaxime, Ceftriaxone: 3rd gen (IV)
-same target as penicillin
-cell wall synthesis inhibitor
-each generation has broader SOA and more resistant to beta-lactamases
-PCN allergic pts have 5-10% incidence of cross-hypersensitivity rxns to cephalosporins |
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Term
| Amoxycillin/Clavulanate, Ampicillin/Sulbactam, Piperacillin/Tazobactum |
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Definition
penicillin/beta-lactamase inhibitor combos
-amoxicillin/clavulanate given PO and often used when IV admin not cared for
-piperacilllin/tazobactum only given IV |
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Term
| Penicillin, Nafcillin, Dicloxacillin, Ampicillin, Amoxicillin |
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Definition
cell wall synthesis inhibitor
MOA: bind transpeptidases and prevent crosslinking
SOA: very broad, drug of choice when organism is sensitive, increasing resistance -> combos given now
MOR: mutations in genes encoding transpeptidases, penicillin binding proteins; beta-lactamases that hydrolyze beta-lactam ring; altered uptake
PK: good bioavail, cross BBB when inflamm, short half-lives, some IV, others PO, some both
AR: allergies, desensitization |
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