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81 Cards in this Set

  • Front
  • Back

Macrolides:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype= azithromycin
Bacteriacidal/static? Dose, strain dependent
Mode of Action=Reversibly binds 50S ribosomal subunit
Time/Concentration Dependent= time

azithromycin:
Administration?
Absorbtion?
Distribution?
Metabolism/Excretion?

Administration= oral/IV
Absorbtion= good oral absorption
Distribution= Wide, large Vd, low serum levels because drug concentrates in neutrophils, macrophages
Metabolism/Excretion= liver/ bile+urine

azithromycin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Macrolides:
Spectrum= gram +/– aerobes, mycoplasma, legionella, chlamydia
Use=resp infection, use in penicillan allergics
Adverse Effects/Drug Interaction= CYP3A4 inhibitor increases drug concentrations, GI tox

Clindamycin:
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Clindamycin:
Bacteriostatic
Mode of Action= bind inhibits 50S
Time/Concentration Dependent= time

Clindamycin:
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= IV/PO
Absorbtion= good oral absorption
Distribution= most tissues "save" CSF
Metabolism/Excretion= phase 1 liver/ bile +urine

Clindamycin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Clindamycin:
Spectrum= gram + cocci, Gram +/– anaerobes
Use= pulm/abd/ pelvic infections
Adverse Effects/Drug Interaction= GI disturbances, c.diff overgrowth

Nitroimidazole:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Nitroimidazole
Prototype= metronidazole
Bacteriacidal
Mode of Action= damages DNA, cytotoxic
Concentration Dependent

metronidazole:
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= IV/PO
Absorption= complete oral absorption
Distribution= well into most tissue AND CSF
Metabolism/Excretion= liver w/ active metabolites/ urine, feces

metronidazole:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Nitroimidazole:
Spectrum= gram +/– anaerobes (gold standard for gram neg), protazoa
Use= c.diff colitis, other anaerobes
Adverse Effects/Drug Interaction= metallic taste, GI disturb

Quinolones:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Quinolones:
Prototype= levofloxacin
Bacteriacidal (high concentrations)
Mode of Action= topoisomerase inhibitor
concentration dependent

levofloxacin:
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= IV/PO
Absorbtion= good oral.
Distribution= well in most tissues including bone, prostate
Metabolism/Excretion= minimal/ urine

levofloxacin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Spectrum= broad gram –, moderate gram +
Use= resp inf, anthrax exposure, gastroenteritis, osteomyelitis, prostatitis
Adverse Effects/Drug Interaction= GI disturb, CNS, rash, photosensitivity, QT prolongation, tendon rupture, glucose homeostasis

Antifolate:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?

Antifolate
Prototype: trimethaprim/sulfamethoxazole
Bacteriostatic
Mode of Action= inhibit dihydropteroate synthase: dihydrofolate reductase

trimethaprim/sulfamethoxazole:
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= oral
Absorbtion= good oral
Distribution= wide, some into CSF
Metabolism/Excretion= minimal/ urine

trimethaprim/sulfamethoxazole:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Spectrum= gram +/– aerobes, listeria, shigella, pseudomonas
Use= UTIs, stenotrophomonas, pneumocystis jiroveci
Adverse Effects/Drug Interaction= allergies, pancytopenia, photosensitivity

Isonazid
class?
Bacteriacidal/Bacteriostatic?
Mode of Action?

antimycobacterial
Bacteriacidal
Mode of Action= inhibits mycolic acid synthesis

Isonazid
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration=PO
Absorption= good oral absorption
Distribution= widely distributed, includes CSF
Metabolism/Excretion= liver acetylation / renal

Isonazid agents:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Antimycobacterial:
Spectrum= mycobacterium
Use= TB, both phases of treatment
Adverse Effects/Drug Interaction= hepatotoxicity, urticaria, peripheral neuropathy

Rifampin:
class?
Bacteriacidal/Bacteriostatic?
Mode of Action?

Antimycobacterial
Bacteriacidal
Mode of Action= block RNA polymerase

Rifampin
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= PO
Absorption= good oral
Distribution=wide including CSF
Metabolism/Excretion=Liver/ bile

Rifampin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Antimycobacterial agents:
Spectrum=mycobacterium, gram +/–
Use=TB, must be given in combination for gram+
Adverse Effects/Drug Interaction= induces CYP450

Polyenes:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?

polyenes:
Prototype= amphotericin B
Fungicidal
Mode of Action= binds ergosterol causes lysis

amphotericin B:
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= IV
Absorption= poor oral
Distribution= wide
Metabolism/Excretion= bile

amphotericin B:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

polyenes:
Spectrum= yeast and mold
Use= Candida, Cryptococcus, histoplasmosis, blastomycoses, aspergillus, mucormycosis
Adverse Effects/Drug Interaction= nephrotoxicity, infusion reaction, Mg and K wasting

Azoles:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?

Azoles:
Prototype= fluconazole
fungistatic
Mode of Action= inhibits P450, decreasing ergosterol

fluconazole:
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration= IV/PO
Absorbtion= good oral
Distribution= well into tissues and CSF
Metabolism/Excretion= minimal/ eliminated in urine

fluconazole:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Azole: fluconazole
Spectrum=Candida, coccidioides, cryptococcus
Use=Antifungal
Adverse Effects/Drug Interaction=Well tolerated

Echinocandins:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?

Echinocandins:
Prototype= Caspofungin
Fungicidal
Mode of Action=inhibit glucan synthesis

Caspofungin:
Administration?
Absorbtion?
Distribution?
Metabolism/Excretion?

Administration= IV
Absorbtion= poor oral
Distribution= protein bound, wide
Metabolism/Excretion= liver/ renal (active metabolites)

Caspofungin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Echinocandins:
Spectrum= broad candida coverage, aspergillus
Use=invasive candidiasis, 2nd line for invasive aspergillosis
Adverse Effects/Drug Interaction=Well tolerated, hypersensitivity, nausea, nephrotoxicty, inc. ALT/AST

Flucytosine:
Bacteriacidal/Bacteriostatic?
Mode of Action?

fungicidal?
Mode of Action=Becomes fluorouracil, blocks DNA synthesis

Flucytosine
Administration?
Absorption?
Distribution?
Metabolism/Excretion?

Administration=PO
Absorption= good oral
Distribution= good including CSF
Metabolism/Excretion=minimal/urine

Flucytosine:
Spectrum?
Use?
Adverse Effects/Drug Interaction?

Flucytosine:
Spectrum=Candida, cryptococcus
Use=Used in combination as an antifungal
Adverse Effects/Drug Interaction=Toxic in bone marrow, can cause hepatic dysfunction


Natural Penicillins:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype = Penicillin G
Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

Penicillin G:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = Most degraded by gastric acids


Distribution = Well into most tissues + CSF
Metabolism/Excretion = Unchanged into urine

Penicillin G:
Spectrum?
Use?
Adverse Effects/Drug Interaction?"


Spectrum = gram +
Use = Streptococcus/Syphilis/Neissaria Meningitidis
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte

Aminopenicillins:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype = Ampicillin
Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

Ampicillin:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?


Administration = IV
Absorption = Most degraded by gastric acids


Distribution = Tissues, CSF 5–20% unless inflamed meninges = more CSF
Metabolism/Excretion = Unchanged into Urine

ampicillin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?"


Spectrum = narrow gram + and narrow gram –
Use = Same as penicillin, but also enterococcus, listeria, enterobacteriae
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte

Beta–lactamase inhibitor:
Prototype?
Mode of Action?
Administration?
Use?

Prototype = Clavulanic acid
Mode of Action = Inhibits b–lactamases
Administration = with cell wall inhibitor
Use = As an adjunct to b–lactam therapy for resistance strains

1st Gen Cephalosporins:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype = Cefazolin
Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

Cefazolin:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = Most degraded by gastric acids


Distribution = Well into most tissues, CSF 5–20%
Metabolism/Excretion = Unchanged into urine

Cefazolin:


Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = broad gram + and narrow gram –
Use = Streptococcus, MSSA, skin infections, surgical prophylaxis
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte

What are the two prototype 2nd generation cephalosporins?

cefuroxime

cefloxitin

cefuroxime:


class?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

2nd generation cephalosporin


Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

cefuroxime:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV/PO
Absorption = Most degraded by gastric acids


Distribution = Well into most tissues, CSF 5–20%
Metabolism/Excretion = Unchanged into urine

cefuroxime:
Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = narrow gram + and broad gram –
Use = Streptococcus, respiratory infections, pnuemonia
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte

cefloxitin:


class?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?"

2nd generation cephalosporin


Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

cefloxitin:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = Most degraded by gastric acids


Distribution = Well into most tissues, CSF 5–20%
Metabolism/Excretion = Unchanged into urine

cefloxitin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = narrow gram + and broad gram – and anaerobes
Use = Intrabdominal surgical prophylaxis, PID
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte"

3rd gen Cephalosporins:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?

Time/Concentration Dependent?

Prototype = ceftriaxone
Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis

Time Dependent

ceftriaxone:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = Most degraded by gastric acids


Distribution = Well into most tissues, CSF 5–20%
Metabolism/Excretion = Long 1/2 life, biliary excretion

ceftriaxone:
Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = narrow gram + and broad gram –
Use = Pnuemonia, gram negative infections, meningitis
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte

4th gen cephalosporins:
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?

Time/Concentration Dependent?

Prototype = cefepime
Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

cefepime:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?


Administration = IV
Absorption = Most degraded by gastric acids


Distribution = Well into most tissues, CSF 5–20%
Metabolism/Excretion = Unchanged into Urine

cefepime:
Spectrum?
Use?
Adverse Effects/Drug Interaction?"


Spectrum = broad gram + and gram –
Use = Hospital acquired infections
Adverse Effects/Drug Interaction = Well tolerated, can see Hypersensitivty, GI, Neurological, Electrolyte

Carbapenems
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype = Imipenem/Cilastatin
Bacteriacidal
Mode of Action = Inhibits transpeptidases, causes cell lysis
Time Dependent

Imipenem/Cilastatin:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = NOT absorbed orally


Distribution = Throughout all tissues
Metabolism/Excretion = Mimally, excreted in urine

Imipenem/Cilastatin:
Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = broad gram + and gram – and anaerobes
Use = Broad spectrum agents for documented resistance
Adverse Effects/Drug Interaction = GI distubances, hypersensitivity, Seizures – Imipenim alone is nephrotoxic

Vancomycin
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?


Bacteriacidal
Mode of Action = Binds to peptidoglycan precursors
Time Dependent

Vancomycin


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV (PO for c. diff)
Absorption = Poorly absorbed


Distribution = Moderate into most tissues, CSF less than 5%
Metabolism/Excretion = minimally, urine excretion unchanged

Vancomycin
Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = Gram + aerobes and anaerobes including MRSA
Use = MRSA, Gram + in beta lactam allergic patients, C. Diff
Adverse Effects/Drug Interaction = Phlebitis, Hypersensitivity, hematologic, nephrotoxic, ototoxic

Aminoglycosides
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype = gentamicin
Bacteriacidal
Mode of Action = Bind to 30S ribosome, causing misreads
Concentration Dependent

gentamicin:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = Poor oral absorbtion


Distribution = Extracellular space, no CSF
Metabolism/Excretion = unchanged in urine

gentamicin:


Spectrum?
Use?
Adverse Effects/Drug Interaction?


Spectrum = broad gram – and narrow gram + and can be used against mycobacteria/protozoa
Use = Gram negative treatment; genitourinary infections
Adverse Effects/Drug Interaction = Nephrotoxicity, Ototoxicity

Tetracyclines
Prototype?
Bacteriacidal/Bacteriostatic?
Mode of Action?
Time/Concentration Dependent?

Prototype = doxycycline
Bacteriostatic
Mode of Action = Reversibly binds to 30S
Time Dependent

doxycycline:


Administration?
Absorption?


Distribution?
Metabolism/Excretion?

Administration = IV
Absorption = Good Oral absorption


Distribution = Especially in bile, liver, kidney, spleen, skin, bone
Metabolism/Excretion = Glucouronidated, urine/bile excretion

doxycycline:
Spectrum?
Use?
Adverse Effects/Drug Interaction?"


Spectrum = broad gram + and gram – and anaerobes and lyme disease
Use = Rickettsiae, Brucellosis, Cholera, Syphilis, Chlamydia, Lyme disease
Adverse Effects/Drug Interaction = Photosensitivity, tooth/bone discoloration, GI disturbances

Define Concentration Dependent. What ratio is used to describe this parameter?

drug works best by achieving a very high peak/Cmax

usually described by Cmax/MIC ratio; ie how many times above the MIC do you need to get your antibiotic to kill bacteria

Define Time Dependent

work best by maintaining concentrations above the MIC for a certain amount of time; moderate sustained levels are more important than hitting a high peak

What ratio is used to describe mixed dependent drugs?

"AUC/MIC"

When administering a concentration dependent drug you should try to maximize ____?

When administering a time dependent drug you should try to maximize _______?

When administering a concentration dependent drug you should try to maximize the single dose concentration.

When administering a time dependent drug you should try to maximize the frequency of administration

What are the main mechanisms of resistance to beta–lactam antibiotics

–Beta–lactamases
–Extended Spectrum Beta–lactamases – render all PCNs and cephalosporins inactive
–Alterations in PBPs

Mechanism of resistance for MRSA and strep pneumoneae?

Alteration in PBP

When do you give penicillins/cephalosporins from these class IV vs PO?

IV is for severe cases

PO is for mild to moderate

Why are Imipenem and cilastatin given together?

Cilastatin prevents breakdown of imipenem by renal dyhydropeptidases which protexts the kidney from toxic byproducts

Aminoglycosides are not used as monotherapy for infections outside _______

the urinary tract

Post antibiotic effect?

Persistent suppression of bacterial growth following exposure to an antimicrobial

you can give a large dose and let it completely clear out of the body because of the PAE. This is thought to reduce toxicity

Which class has a long PAE?

aminoglycosides

What class has notable synergy with Aminoglycosides? Use?

Beta–Lactams

Use: endocarditis, endovascular infections

Most common method of tetracycline resistance?

Drug cannot reach the target site:

Active efflux most common