Term
| What are examples of systemically used aminoglycosides? |
|
Definition
gentamicin
tobramycin
amikacin |
|
|
Term
| What are examples of topically used aminoglycosides? |
|
Definition
|
|
Term
| What is the activity of aminoglycosides? |
|
Definition
| bactericidal, concentration dependent |
|
|
Term
| What is the major use of aminoglycosides? |
|
Definition
| major use for over 30 yrs of AG is g-aerobic bacilli |
|
|
Term
| What can aminoglycosides be used synergistically with and what for? |
|
Definition
synergistic bactericidal combination of AG and beta-lactam or vancomycin (inhibition of cell wall synthesis permits increased entry of AG into cell)
used for enterococcal endocarditis (ineffective vs. VRE)
used for pseudomonas (AG plus antipseudomonal penicillin or ceftazidime) |
|
|
Term
| What are AGs ineffective against? |
|
Definition
|
|
Term
| AGs are the DOC for treatment of endocarditis caused by what two bacteria? |
|
Definition
| E. faecalis and non-VRE E. faecium |
|
|
Term
| What is the DOC to treat endocarditis caused by E. faecalis and non-VRE E. faecium |
|
Definition
| penicillin G or ampicillin combined with gentamicin or streptomycin |
|
|
Term
| Gentamicin is the most often used AG for synergism with penicillins vs what three bacteria? |
|
Definition
enterococci
streptococci
staphylococci |
|
|
Term
| What is the major advantage of tobramycin? |
|
Definition
| major advantage is activity (2-4 times as active) against some strains of P. aeruginosa that are resistant to gentamicin |
|
|
Term
| What is the major use of amikacin? |
|
Definition
| empiric therapy of nosocomial aerobic gram- bacillary infections where significant gentamicin resistance exists |
|
|
Term
| Neomycin is used topically for minor soft tissue infections combined with what two drugs? |
|
Definition
|
|
Term
| Why should topical preperations of neomycin be avoided? |
|
Definition
| neomycin may be highly sensitizing and cause dermatological reactions |
|
|
Term
|
Definition
| poor CSF entry even with inflammation; levels attained (20-25% of serum) are inadequate for meningitis |
|
|
Term
|
Definition
excreted entrirely through glomerular filtration
half life of 2-3 hr; greatly increased in renal disease and required dosing adjustment |
|
|
Term
|
Definition
| individualization of dosing regimens is advised due to the low (narrow) therapeutic index |
|
|
Term
| What is the most frequent cause of drug induced contact dermatitis? |
|
Definition
|
|
Term
| What are the characteristics of ototoxicity caused by AGs? |
|
Definition
cochlear
vestibular
may be reversible if toxicity is mild, but extensive damage is usually irreversible |
|
|
Term
| What are predisposing factor for ototoxicity of AGs? |
|
Definition
| concurrent ototoxic drugs |
|
|
Term
| Which AG is more likely to affect vestibular function? |
|
Definition
|
|
Term
| What is usually assocatied with nephrotoxicity of AGs? |
|
Definition
| elevated trough serum levels of AGs |
|
|
Term
| Is renal impairment reversible? |
|
Definition
|
|
Term
| What is a predisposing factor for nephrotoxicity when using AGs? |
|
Definition
| concurrent nephrotoxic drugs |
|
|
Term
| tobramycin solution for inhalation is indicated for... |
|
Definition
| management of cystic fibrosis patients with P. aeruginosa infections |
|
|
Term
| What are the two main sources of tetracyclines? |
|
Definition
|
|
Term
| How are tetracyclines (esp doxycycline) classified? |
|
Definition
| long acting, lipophilic, hepatic elimination, bid dosing |
|
|
Term
| What are tetracyclines spectrum of activity? |
|
Definition
| broad spectrum bacteriostatic |
|
|
Term
| Tetracyclines have good activity against... |
|
Definition
good activity vs. unusual spp.
intracellular organisms (highly active vs. spirochetes, mycoplasma, chlamydia, and rickettsia) |
|
|
Term
| What interaction can tetracyclines have that decreases their absorbance? |
|
Definition
| Chelate with divalent and trivalent cations to form insoluble complexes which are not absorbed (dairy products, mineral and vitamin supplements, antacids, cathartics) |
|
|
Term
| Food greatly reduces the availability execpt for what two drugs? |
|
Definition
|
|
Term
| Describe tetracycline distribution into the CSF and placental barrier? |
|
Definition
Poor entry into CSF even in inflammation; not indicated for meningitis
Crosses placental barrier and undergoes permanent sequestration in newly forming bone and teeth |
|
|
Term
| How is doxycycline eliminated? |
|
Definition
| Active biliary excretion and enterohepatic circulation (reabsorption); doxycycline half life unchanged in renal disease |
|
|
Term
| What tetracycline is used for acne vulgaris? |
|
Definition
oral tetracyclines, low-dose, long-term
used in chronic, severe cases of acne vulgaris
no serious toxicity since doses are low |
|
|
Term
| What tetracycline is used in Lyme Disease (Borrelia burgdoferi)? |
|
Definition
doxycycline
DOC for tx of early stage of Lyme Disease |
|
|
Term
| What is the DOC for relapsing fever (Borrelia recurrentis)? |
|
Definition
| tetracycline or doxycycline |
|
|
Term
| What is the DOC for urogenital infections caused by C. trachomatis? |
|
Definition
| doxycycline is the DOC for STDs (like non-gonococcal urethritis) |
|
|
Term
| For PID (salpingitis) what must you provide coverage for and with what drugs? |
|
Definition
Gonococcus (cephalosporin)
C. trachomatis (doxycycline) |
|
|
Term
| What respiratory infection is doxycycline the DOC for? |
|
Definition
| atypical pneumonias (Mycoplasma, Chlamydia); however in vitro activity of doxycyclines is less than that of the macrolides |
|
|
Term
| What rickettsial infections is doxycycline the DOC for? |
|
Definition
Rocky mountain spotted fever
typhus |
|
|
Term
| What tetracycline is the DOC for Vibrio infections and what are two example of vibrio infections? |
|
Definition
doxycycline
cholera, gastroenteritis |
|
|
Term
| Tetracyclines are the DOC for anthrax (B. anthracis) - how are they used? |
|
Definition
treatment of inhalational anthrax
treatment of cutaneous anthrax
prophylaxis
|
|
|
Term
| Demeclocycline is used for... |
|
Definition
| management of syndrome of inappropriate antidiuretic hormone relases (SIADH) |
|
|
Term
| Explain how tetracyclines are incorporated into bone and teeth and what this causes? |
|
Definition
| Dose-dependent incorporation into growing teeth, producing a yellow brown discoloratoin of enamel and possible faulty enamel formation |
|
|
Term
| Explain how tetracyclines can cause deposits in crown of anterior teeth? |
|
Definition
| Crown formation complete by 6-7 years, high risk of permanent teeth discoloration when used in children less than 8 years (least likely to occur with doxycycline but should avoid all tetracyclines in children less than 8 years and in pregancy) |
|
|
Term
| Tetracyclines can cause temporary cessation of bone growth or bone deformity so what does this mean? |
|
Definition
| contraindicated in pregnant or nursing women or in children < 9 years |
|
|
Term
| What tetracycline must be taken on an empty stomach? |
|
Definition
|
|
Term
| What two tetracyclines must be taken with meals? |
|
Definition
| doxycycline and minocycline |
|
|
Term
| Doxycycline may necessitate administration with meals because... |
|
Definition
|
|
Term
| What should not be given for at least 2 hrs after dosing? |
|
Definition
| no antacids, bismuth subsalicylate, vitamins, or mineral supplemants |
|
|
Term
| Should tetracyclines be taken with a full glass of water and be given at bedtime? |
|
Definition
| take with a full glass of water, do not give at bedtime |
|
|
Term
|
Definition
| no affected by the two major tetracycline resistance mechanisms (ribosomal binding site alteration, active efflux); considered bacteriostatic |
|
|
Term
| What is tigecycline approved to treat? |
|
Definition
| complicated skin/skin structure infections (MRSA), complicated intraadbdominal infections (anerobes), CAP |
|
|
Term
| What are two common macrolides? |
|
Definition
azithromycin
erythromycin |
|
|
Term
| Is erythromycin bacteriostatic or bactericidal? |
|
Definition
|
|
Term
| What is erythromycin used to treat? |
|
Definition
| gram + cocci: used as an alternative for penicillin allergic patients |
|
|
Term
| What bacteria is erythromycin active against and what is it inactive against? |
|
Definition
active vs group A and B streptococci, S. viridans, and penicillin-sensitive S. pneumoniae
ineffective vs. enterococci
active vs C. diptheriae and Bordatella pertussis (whooping cough) |
|
|
Term
| What intracellular organisms is erythromycin active against? |
|
Definition
| Legionella pneumonphila, mycoplasmas (M. pneumoniae, U. urealyticum), chlamydiae (C. pneumoniae) |
|
|
Term
| Azithromycin has superior activity versus what? |
|
Definition
| Mycoplasma, Chlamydia, H. influenzae |
|
|
Term
| Either azithromycin (A) or erythromycin (E) is the DOC for... |
|
Definition
-pneumonia caused by Chlamydia, Mycoplasma, or Legionella (A)
-whooping cough (Bordatella pertussis, E)
-diptheriae (C. diptheriae; E + antitoxin)
-PID due to C. trachomatis (A); cephalosporin or flouroquinolone for gonoccocal coverage |
|
|
Term
| What is used to treat pneumonia caused by Chlamydia, Mycoplasma, or Legionella? |
|
Definition
|
|
Term
| What is used to treat Bordatella pertussis (whooping cough)? |
|
Definition
|
|
Term
| What is used to treat diptheriae (C. diptheriae) |
|
Definition
|
|
Term
| What is used to treat PID due to C. trachomatis? |
|
Definition
| azithromycin - cephalosporin or flouroquinolone for gonococcal coverage |
|
|
Term
| What is used for prophylaxis for gonoccocal and chlamydial ophthalmia neonatorum |
|
Definition
| erythromycin topical 5% ointment |
|
|
Term
| What is erythromycin's active form (base) inactivated by? |
|
Definition
| inactivated by acid, so use delayed release (enteric coated) tablets |
|
|
Term
| Chemical modification of base (erythromycin)? |
|
Definition
ethylsuccinate ester
estolate |
|
|
Term
| Best availability of erythromycin is when? |
|
Definition
| when taken in fasting state, except for stearate which should be taken with meals |
|
|
Term
|
Definition
|
|
Term
|
Definition
new tablets may be taken without regard to meals
once daily dosing |
|
|
Term
|
Definition
|
|
Term
| Describe some erythromycin GI side effects and why they exist: |
|
Definition
| nausea, diarrhea, cramps; dose related effects attributed to agonist effects at motilin receptors |
|
|
Term
| Describe the toxicity associated with estolate? |
|
Definition
| cholestatic hepatitis (probably safe in children, estolate offers no therapeutic advantage and should be avoided in adults) |
|
|
Term
| Macrolides and cardiac side effects? |
|
Definition
-may prolong the QT interval
-erythromycin has been associated with rare cases of torsades |
|
|
Term
| Erythromycin and drug interactions? |
|
Definition
| drug interactions due to inhibition of P450 system |
|
|
Term
| Which macrolide has the least amount of P450 inhibition? |
|
Definition
|
|
Term
| What is telithromycin used for? |
|
Definition
| developed specifically for treatment of community-acquired respiratory tract infections caused by both common and atypical pathogens, including resistant strains |
|
|
Term
| Telithromycin and resistance? |
|
Definition
| Telithromycin is unaffected by resistance mechanisms used against macrolides |
|
|
Term
|
Definition
-strongly inhibits CYP3A4
-may prolong the QTc interval
-case reports of patients with jaundice, abnormal hepatic function, acute hepatic failure, and fulminant hepatitis leading to transplant or fatality |
|
|
Term
| What type of bacteria does clindamycin treat? |
|
Definition
| anaerobes (due to the association with pseudomembranous colitis, use of clindamycin is largely restricted to anaerobic infections) |
|
|
Term
| What is clindamycin also used to treat? |
|
Definition
| also used for mixed intraabdominal and female genital tract infections in combination with an AG |
|
|
Term
| How is clindamycin prepared for use in acne? |
|
Definition
|
|
Term
| Clindamycin and CSF distribution? |
|
Definition
| poor entry into CSF (about 10% of serum levels); not indicated for meningitis |
|
|
Term
| How is clindamycin used to treat anaerobic infections? |
|
Definition
| alternate DOC for infections due to B. fragilis; alternative to penicillin G for other anaerobes |
|
|
Term
| Clindamycin can also be used for anaerobic coverage for... |
|
Definition
| mixed aerobic-anaerobic infections |
|
|
Term
| Clindamycin can be used to treat two other things... |
|
Definition
bone and joint infections (staphylococcal or anaerobic osteomyelitis)
acne vulgaris (topical preperations) |
|
|
Term
| Describe clindamycin antibiotic associated psedomembranous colitis (AAPMC) |
|
Definition
| incidence estimated at 1.9 per 1000 courses of clindamycin (1.5 for cephalosporins, 2.1 for ampicillins); incidence of significant lincosamide-induced colitis ranges from 0.1-10% |
|
|
Term
| What are the sxs of AAPMC? |
|
Definition
| profuse, watery diarrhea (10-20 stools/d); blood and mucous may be present in the stool (5-10%), intestinal lesions produced are covered by a pseudomembrane |
|
|
Term
|
Definition
| superinfection of bowel by C. dificile, and production of two extracellular toxins (enterotoxin and cytotoxin) which causes the colitis |
|
|
Term
| What is the DOC for AAPMC? |
|
Definition
|
|
Term
| What is the alternative agent for eradicating C. dificile? |
|
Definition
| po vancomycin (reserve for cases not responsive to two courses of metronidazole or in life threatening colitis) |
|
|
Term
| What drugs are contraindicated in the treatment of AAPMC? |
|
Definition
| intestinal antimotility drugs |
|
|
Term
| What bacteria are chloramphenicol used to treat? |
|
Definition
| virtually all obligate anaerobes are suseptible (good activity vs Rickettsia spp.) |
|
|
Term
| CSF penetration of chloramphenicol? |
|
Definition
CSF levels about 20-50% of plasma levels in the presence of uninflamed meninges, and about 45-90% of plasma levels in the presence of inflamed meninges; formerly used for empiric therapy of meningitis in combination with ampicillin
brain tissue levels about 9 times that of plasma - treat brain abcesses |
|
|
Term
| Does chloramphenicol have a low or high TI? |
|
Definition
| low TI; reserved only for serious infections for which less toxic agents are ineffective or contraindicated |
|
|
Term
| Chloramphenicol is alternative DOC for: |
|
Definition
| rickettsial infections in pregnancy or tetracycline allergy; for non-pregnant individuals > 8 yrs in the absence of allergy, doxycycline is the DOC for Rocky Mountain Spotted Fever |
|
|
Term
| What drug is useful in the treatment of epiglottitis, septic arthritis, or osteomyelitis due to H. infuenzae in penicillin allergic patients? |
|
Definition
|
|
Term
| What is the ADR of chloramphenicol? |
|
Definition
|
|
Term
| The narrow TI can causes? |
|
Definition
-reversible bone marrow depression
-aplastic anemia
-"gray" syndrome in full-term neonates and premature infants |
|
|
Term
| Describe the aplastic anemia associated with chloramphenicol... |
|
Definition
-pancytopenia with aplastic marrow
-idiosyncratic, neither dose nor duration related
-poor prognosis, high % fatalities; only tx is bone marrow transplant |
|
|
Term
| Describe "gray" syndrome associated with chloramphenicol use... |
|
Definition
unaltered drug accumulates to toxic levels (deficient glucuronidation, low GFR), causing inhibition of mitochondrial oxidative phosphorylation
usually reversible is drug d/c at onset of sxs |
|
|
Term
| What is the main affect of mupirocin? |
|
Definition
| inhibits bacterial proteins synthesis |
|
|
Term
| What are the dosage forms and uses of mupirocin? |
|
Definition
2% ointment for dermatologic use (not for ophthalmic use): indicated for topical tx of impetigo due to S. aureus, beta-hemolytic strep, and S. pyogenes
2% ointment for intranasal use: indicated for eradication of nasal colonization with methicillin-resistant S. aureus in adult patients and healthcare workers |
|
|
Term
| What does Quinopristin/dalfopristin affect? |
|
Definition
| combination is synergistic, affecting both the early (dalfopristin) and late (quinupristin) stages of proteins synthesis |
|
|
Term
| What is Quinupristin/dalfopristin used to treat? |
|
Definition
| serious or life threatening infections associated with vancomycin-resistant E. faecium bacteremia (VREF; bacteriostatic) |
|
|
Term
| ADR of quinupristin/dalfopristin? |
|
Definition
| administered by IV infusion; most frequent ADR is at the infusion site |
|
|
Term
| DI of quinupristin/dalfopristin |
|
Definition
| potent inhibitor of CYP3A4 |
|
|
Term
| Linezolid approved indications? |
|
Definition
-VRE E. faecium including concurrent bacteremia
complicated skin/skin structure infections, including -diabetic foot infections, without concominant osteomyelitis
-CAP: PSSP, MSSA, DRSP
-preferred DOC for VISA and VRSA
-preferred DOC for PRSP pneumonia |
|
|
Term
|
Definition
thrombocytopenia
myelosuppression |
|
|
Term
|
Definition
-weak, reversible, nonselective MAOI
-potential DI with adrenergic and serotonergic agents
-interaction with tyramine containing foods may cause hypertension
-reports of serotonin syndrome with concurrent use of serotonergic agents |
|
|
