Term
|
Definition
AMINOGLYCOSIDE
Mechanism: interfere with bacterial protein syntheis with binding sites on bacterial ribosome, bacteriosidal
Other - 2 more more amino sugars joibed by glycosidic lin, highly polar cation, not well absorbed orally but available prophylactically before abdominal surgery |
|
|
Term
|
Definition
AMINOGLYCOSIDE - GENERIC
USE: gram negative aerobic, increased efficacy against gram positive with beta lactams
Mechanism: interfere with bacterial protein syntheis with binding sites on bacterial ribosome, causes misincorporation of amino acids, BACTERIOCIDAL
Other - 2 more more amino sugars joibed by glycosidic lin, highly polar cation, not well absorbed orally but available prophylactically before abdominal surgery, excreted by kidneys and may be toxic with renal dysfunction
IM or slow IV (30 min)
**most dangerous common antibiotic
Resistance by: uptake mutants (oxygen dependent -anaerobes resistan), (facultative bacteria more resistant in anaerobic conditions), drug modification
Side Effects: ototoxicity (gradual at first, reversible or not, may be after stopping treatment, vestibulat toxicity causes nausea, vertigo, etc), nephrotoxicity (reversible)
- Limited by toxicity, new expended spectrum beta lactams and fluroquinolones are less toxic
- never used in pregnancy |
|
|
Term
|
Definition
AMINOGLYCOSIDE
Mechanism: interfere with bacterial protein syntheis with binding sites on bacterial ribosome, bacteriocidal
Other - 2 more more amino sugars joibed by glycosidic lin, highly polar cation, not well absorbed orally but available prophylactically before abdominal surgery |
|
|
Term
|
Definition
AMINOGLYCOSIDE
Mechanism: interfere with bacterial protein syntheis with binding sites on bacterial ribosome, bacteriocidal
Other - 2 more more amino sugars joibed by glycosidic lin, highly polar cation, not well absorbed orally but available prophylactically before abdominal surgery |
|
|
Term
|
Definition
TETRACYCLINE
uSE: Lyme disease, Rocky Mountain spotted, Q fever, M. pneumoniae, Chlamydia, CA respiratory, broad spectrum, gram -, gram +, amoeba
Mechanism: inhibits bacterial protein synthesis and binds ribodsomes, BACTERIOSTATIC, bind + charged ions such as Ca in some foods, decreased absorption when given with food
Other: made from naphthacenecarboxamide, oRALLY ABSORBED, lots of resistance, absorption by gut is incomplete, co-injgestion with diary products reduces uptake, antacids reduce absorption, widely distributed, crosses BBB and placenta - secreted in breast milk, excretion by kidney, C/I in renal failure, ORAL and IV and topical admin
Adverse: metabolized by CYP and may cause drug intereactions, decreased efficacy of oral contraceptives, resistance involves cross resistance, GI irritation in some, CDAD (pseudomembranous colitis), photosensitivity, incorporate in growing teeth (discoloration), avoid in mid pregnangy and betwen 2mo-8 yrs, superinfection by yeast
Pregnancy cat D |
|
|
Term
|
Definition
TETRACYCLINE
uSE: Lyme disease, Rocky Mountain spotted, Q fever, M. pneumoniae, Chlamydia, CA respiratory, broad spectrum, gram -, gram +, amoeba
Mechanism: inhibits bacterial protein synthesis and binds ribodsomes, BACTERIOSTATIC, bind + charged ions such as Ca in some foods, decreased absorption when given with food
Other: excreted by liver and can be used in renal failure, made by napthacenecarboxamide, ORALLy absorbed, lots of resistance |
|
|
Term
|
Definition
Use: anaerobic infections, bacterial meningitis in pencillin allergies, ricketssial infections (typhus, RMSF) in tetracylcine intolerant, VRE if suscpetible, OTC - limited by toxicity
Mechanism: bacteriostatic, protein synthesis inhibitor binding ribsoome and inhibiting transpeptidation, partially inhibits eukaryotic protein synthesis
Other: widely prescribed, cheap, OTC
Adverse: rare aplastic anermia (hematologic tox), anemia, leukopenia, thrombocytopenia, pancyotpenia, bone marrow suppression (aplastic anemia doese and time independent), GI effects, inhibits cyt P450 enzymes, increases concentration of warfarin and others
- gut absorption incomplete, widely distributed, crosses BB< croses placenta and secreted in breast milk, enterohepatic cycling of glucuronidated metabolite, dose reduction in hepatic failure, may have resistance |
|
|
Term
|
Definition
MACROLIDE
**SAFEST OF ALL ANTIMICROBIALS
USE: gram - and gram ++ aerobes and some anaerobes like M penumoiae, legionella, b. pertussis, in penicillin allergic patients, not effective v. MRSA, broad spectrum
Mechanism: BACTERIOSTATIC, protein synthesis inhibitor binding to ribosomal subunits, may be antagonized by other antimicrobials
Other: resistance is a problem, ORAL admin, maybe IV for serious infctions, hydrolyzed in stomach do NOT take with food (enteric coated), enters cells and most body sites EXCEPT brain and CSF, concetrated in liver, ecreted in bile with little renal elim
Side effects: rarely serious, GI effects more than arithromycin and clarithromycin, cholestatic jaundice, that is reversible, allergy, decreased elim of theophylline, warfarin, cyclosproine, and others |
|
|
Term
|
Definition
MACROLIDE
USE: gram - and gram ++ aerobes and some anaerobes like M penumoiae, legionella, b. pertussis, in penicillin allergic patients, not effective v. MRSA, broader spectrum than erythromycin, may be used v. STDS
Mechanism: BACTERIOSTATIC, protein synthesis inhibitor binding to ribosomal subunits, may be antagonized by other antimicrobials
Other: resistance is a problem, ORAL admin, maybe IV for serious infctions, hydrolyzed in stomach do NOT take with food (enteric coated), enters cells and most body sites EXCEPT brain and CSF, concetrated in liver, ecreted in bile with little renal elim
Side effects: rarely serious, less common GI effects than erythromycin, cholestatic jaundice, that is reversible, allergy |
|
|
Term
|
Definition
MACROLIDE
USE: gram - and gram ++ aerobes and some anaerobes like M penumoiae, legionella, b. pertussis, in penicillin allergic patients, not effective v. MRSA, broader spectrum than erythromycin
Mechanism: BACTERIOSTATIC, protein synthesis inhibitor binding to ribosomal subunits, may be antagonized by other antimicrobials
Other: resistance is a problem, ORAL admin, maybe IV for serious infctions, hydrolyzed in stomach do NOT take with food (enteric coated), enters cells and most body sites EXCEPT brain and CSF, concetrated in liver, ecreted in bile with little renal elim
Side effects: rarely serious, less common GI effects than erythromycin, cholestatic jaundice, that is reversible, allergy, reduced elim of theophylline, warfarin, cyclosporine, and other drugs |
|
|
Term
|
Definition
MACROLIDE
USE: community acquired respiratory tract infections where resistance to older agents is suspected, s. penumo, influenza, M. catarrhalis, some strains of s. aureus
Mechanism: inhibits protein synthesis and binds ribosomal subunit, shows concentraction-dependent BACTERICIDAL action c. st. penumo strains
Other: new drug class (ketolides), derivative of erythromycin with improved acid stability, increased affinity of bacterial ribosome and reduced induction of bacterial resistance, well absorbed ORALLY, not influenced by food, liver metabolism (50% CYP), eliminated by liver and renal
- does not incude bacterial macrolide resistance path
Side effects: GI, diarrhea, nausea, visual blurriness, difficulty focusing (reversible), exacerbation of disease symtpoms in gravis patiens (BLACK BOX WARNING), adverse drug rxn with cisapride and simvastatin |
|
|
Term
|
Definition
LINCOMYCIN
USE: alternative therapy for B., fragilis (dentists), gram + infection in penicillin allergy, prophylaxis for oral surgery in penicillin reistant patients, in combo therapy with aminoglycoside or cephalosproin in penetrating wounds of gut and pelvic abscesses
Mechanism: BACTERIOSTATIC, binds to ribosome and may result in antagonism with other macrolides, treats drug resistant microbes
Other: well aborbed ORALLY, can be IM or IV as welll, distributes many places but NOT CNS, crosses placenta, biliary excretion with liver metabolism, enterhepatic cyclinc and may lead to AAC
Side Effects: PSEUDOMEMBRANOUS COLITIS (acc), skin rashes, thromophelebitis |
|
|
Term
|
Definition
STREPTOGRAMINS - natural cyclic peptides
USE: vancomycin resistant Enteroccoccus faecium VREF
Mechanism: binds to ribosome to interfere with protein synthesis (not like daptomycin)
Other: not absorbed orally, delivered IV, extensive liver metabolism, biliary and renal excretion (more biliary), WORKS WITH DALFOPRISTIN
Side effects: inflammation, pain, edema, infusion site reaction, thrombophelbitis, nausea, vomit, diarhea, no ototoxicity or nephrotoxicity, inhibits metabolism of cyclosporine, calcium channel blockers, HIV NNRTI and protease inhibitors and others
- resistance by bacterial modification of both peptides |
|
|
Term
|
Definition
STREPTOGRAMINS - natural cyclic peptides
USE: vancomycin resistant Enteroccoccus faecium VREF
Mechanism: binds to ribosome to interfere with protein synthesis (not like daptomycin)
Other: not absorbed orally, delivered IV, extensive liver metabolism, biliary and renal excretion (more biliary), WORKS WITH QUINUPRISTIN
Side effects: inflammation, pain, edema, infusion site reaction, thrombophelbitis, nausea, vomit, diarhea, no ototoxicity or nephrotoxicity, inhibits metabolism of cyclosporine, calcium channel blockers, HIV NNRTI and protease inhibitors and others
- resistance by bacterial modification of both peptides |
|
|
Term
|
Definition
OXAZOLIDINONE - SYNTHETIC ANTIMICROBIAL
Use: vancomycin-resistant enteroccus faecium (VREF) and to treat multiple drug resistant organisms (MRSA)
Mechanism: protein synthesis inhibitor, novel ribosomoal binding site
Other: no cross resistance with other anti-microbials, high ORAL F, hepatic metabolism, renal excretion
Side effects: diarrhea, headache, vomiting, mild thromobyctopenia, resistance in some in vitro |
|
|
Term
|
Definition
Use: topical treatment of impetifo due to s. aureus and s. pyogenes, against MRSA but not systemically
Mechanism: reversibly inhibits bacterial isoleucly tRNA synthetase - novel mechanism
Other: TOPICAl admin, rapidly metabolized to inactive form upon systemic admin
Adverse effects: only in sensistive individuals, resistance rare but from production of modified tRNA |
|
|
Term
|
Definition
SULFONAMIDES - ANTIFOLATE ANTIBIOTIC
USE: BROAD spectrum, many gram + and -, plasmodium and toxoplasma gondii, not typically used alone for bacterial infections, malaria
Mechanism: block bacterial folic acid synthesis, inhibit DNA< RNA< and protein synthesis (decrease thymidine, purine and methionine production)
- blocks the fisrt step blocking the covalent link of ptiridine to PABA and fail to make purines - COMPETITIVE inhibition of PABA binding to DHPS enzyme
Other: SYNERGISTIC WITH trimethorprim to be bactericidal - otherwise bacteriostatic; high PABA levels inhibits sulfa acctivity, oral OR iv OR tOPICAL admin, distributed all over including CNS and CSF, excreted by kidney, metabolized by liver, decrease dose in renal failure
Toxicity: DHPS enzyme is not in humans and bacteria must make folic acid to live, we get it from our diet like spinach, etc., Gi distress and rash are common, bone marrow and liver tox, hemolytic anemia with G6PD deficiency, kernicterus in infants, Stevens-johnson sysndome - hypersensitivity iwth mucosal sloughing, skin eruptionns
Resistance - widespread in staph, strep and enterobacteriacea, cross resistance to all sulfas are common, resistance by overproduction of PABA, encode mutatnt DHPS enzyme, upregulate efflux pumps |
|
|
Term
|
Definition
DHFR INHIBITORS
USE: BROAD spectrum, many grma + and -, NOT pseudomonas, anaerobes or atrypical bacteria like legionella and chlamydia (not good for gut organisms)
Mechanism: stops DHFR from converting dihydrofolic acid to tetrahydrofolic acid, BACTERIOSTATIC if used alone, synergistically with sulfa drugs for BACTERIOCIDAL
Side effects: good selective toxicity, does not target our cells, bone marrow suppression with neutropenia, stevens johnsons syndrome, anit-folate effect (carefult use in alcoholics and prengnacy), same toxicities as sulfas
Other: admine is ORAL, wide and good absorption even to CNS and prostrate, excreted in urine
Resistance: by overexpression of DHFR, expression of mutatnt DHFR, location dependent |
|
|
Term
|
Definition
TRIMETHOPRIM-SULFAMETHOXAZOLE COMBO
USE: UTI, pneumocystis pneumonia in AIDS/transplant, sinusitis, otitis media, CA MRSA |
|
|
Term
|
Definition
FLUOROQUINOLONES
USE: complicated UTI, serious acute bacterial prostatit, penumonia, STD, majority inappropriate, better gram + coverage including streptocoocci, poor anearobic activity, good for gram negative including pseudomonas (better than levo or moxi), good for nosocomial, atypical bacteria, DO NOT achieve syndergy when used with other antimicrobials
Resistance - from decreased permeability, increased efflux pump, mutation of enzymes, generally spontaneous mutation in gyrA and parC, 2 mutations lead to high resistance, not used in MRSA, gonorrhea, slamonella, campylobacter
Mechanism: BACTERICIDAL, rapid inhibitor of bacterial DNA synthesis, inhibit bacterial DNA gyrase and topoisomerase, blocks DNA unwinding, induces irreversible DA damage/degredation, concentration dependent killing
Other: keep AUC/MIC to 25 in immunocompromised and AUC/MIC to 100 in non-immunocompromised
- admind ORAL and IV, good GI absorption, wide distribution with high F, low in CSF, form chelates with cations to reduce absorption (do not take with Ca), eliminated by liver and kidney (decrease dosing with failure)
Side effects: well tolerated, G, arthropathy (not for use in kids), achilles tendon rupture, hepatotoxiciuty, MRSA and C. dificile |
|
|
Term
|
Definition
FLUOROQUINOLONES
USE: complicated UTI, serious acute bacterial prostatit, penumonia, STD, majority inappropriate,better gram + coverage including streptocoocci (better than cipro), poor anearobic activity, good for gram negative including pseudomonas (better than moxi), good for nosocomial, atypical bacteria, DO NOT achieve syndergy when used with other antimicrobials
Resistance - from decreased permeability, increased efflux pump, mutation of enzymes, generally spontaneous mutation in gyrA and parC, 2 mutations lead to high resistance, not used in MRSA, gonorrhea, slamonella, campylobacter
Mechanism: BACTERICIDAL, rapid inhibitor of bacterial DNA synthesis, inhibit bacterial DNA gyrase and topoisomerase, blocks DNA unwinding, induces irreversible DA damage/degredation, concentration dependent killing
Other: keep AUC/MIC to 25 in immunocompromised and AUC/MIC to 100 in non-immunocompromised
- admind ORAL and IV, good GI absorption, wide distribution with high F, low in CSF, form chelates with cations to reduce absorption (do not take with Ca), eliminated by liver and kidney (decrease dosing with failure)
Side effects: well tolerated, G, arthropathy (not for use in kids), achilles tendon rupture, hepatotoxiciuty, MRSA and C. dificile |
|
|
Term
|
Definition
FLUOROQUINOLONES
USE: complicated UTI, serious acute bacterial prostatit, penumonia, STD, majority inappropriate, better gram + coverage including streptocoocci (better than levo and cipro), poor anearobic activity, good for gram negative including pseudomonas (worse than levo or cipro), good for nosocomial, atypical bacteria, DO NOT achieve syndergy when used with other antimicrobials
Resistance - from decreased permeability, increased efflux pump, mutation of enzymes, generally spontaneous mutation in gyrA and parC, 2 mutations lead to high resistance, not used in MRSA, gonorrhea, slamonella, campylobacter
Mechanism: BACTERICIDAL, rapid inhibitor of bacterial DNA synthesis, inhibit bacterial DNA gyrase and topoisomerase, blocks DNA unwinding, induces irreversible DA damage/degredation, concentration dependent killing
Other: keep AUC/MIC to 25 in immunocompromised and AUC/MIC to 100 in non-immunocompromised
- admind ORAL and IV, good GI absorption, wide distribution with high F, low in CSF, form chelates with cations to reduce absorption (do not take with Ca), eliminated by liver and kidney (decrease dosing with failure)
Side effects: well tolerated, G, arthropathy (not for use in kids), achilles tendon rupture, hepatotoxiciuty, MRSA and C. dificile |
|
|
