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Drugs/Immuno > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

Aminoglycosides (7)

A

-Gentamicin, Tobramycin, Amikacin
MOA: binds 16s rRNA at A site on 30s ribosomal subunit and stops translation, impairs bacterial oxidative phosphorylation
-Parenteral only, eliminated by renal glomerular filtration, bactericidal
-concentration dependent killing by PAE
-nephrotoxicity and ototoxicity, augmented by diuretics
-used against aerobic GNR
-synergistic activity with cell wall active antibiotics for S. aureus/enterococcus
-plasmid exchange of aminoglycoside metabolizing enzymes confer resistance

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2
Q

Tetracyclines (9)

A

-Tetracycline, Doxycycline, Minocycline
MOA: Binds to 16S rRNA/proteins at A site on 30S ribosomal subunit, blocks tRNA access
-bacteristatic, time dependent killing
-chelation of other ions Ca2+, Mg2+, Fe3+, pts must stop
-good orally, distribute to bone and tissue over plasma
-bind to teeth and bones, avoid use in children and pregnant
-GI intolerance N/V/D, photosensitivity
-use for GPC>GNR, aerobes, anaerobes
-resistance caused by TET-A gene which encodes protein to pump tetracyclines out of cell

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3
Q

New Tetracyclines (4)

A

-Glycyclines, Tigecycline
MOA: binds 16s rRNA of the 30s ribosomal subunit and blocks A site
-Parenteral (IV)
-GPC (MRSA,VRSA,VRE), GNR(not Pseudomonas), anaerobes

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4
Q

Macrolides (7)

A

-erythromycin, clarithromycin, telithromycin
-metabolized and inactivate CYP450 excreted in bile
MOA: bind to 23S rRNA of 50s ribosomal subunit and inhibits transpeptidation and translocation
-azithromycin
-unchanged in bile and low amount of drug interactions
-GI complaints, N/V/D, cholestatic jaundice
-use for GPC

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5
Q

Lincosamides (7)

A 
-clindamycin 
MOA: Binds to 23s rRNA in the bacterial 50s ribosomal subunit inhibiting translocation, formation of initiation complex and occupation of the A site 
-time dependent killing
-large volume distribution, except CNS
-Hepatic metabolism by CYP450
-diarrhea and causes C.Diff
-use for GPC, S. Aureus, strep pyogenes, strep viridans, anaerobes, use with other agents in necrotic infections to reduce toxin 
-resistance by rRNA methyltransferases
-use Dtest to ensure susceptibility
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6
Q

Oxazolidinones

A

-Linezolid, Tedizolid
MOA: binds to 23S rRNA at the peptiyl site of the 50s ribosomal subunit, interferes with initiation complex
-bacteristatic/bactericidal depending on organism
-time dependent killing
-good orally, large volume distribution
-use for GPC only, MRSA and VRE
-resistance by mutations in 23s rRNA and rRNA methyltransferase
-myelosuppression, thrombocytopenia, serotonin syndrome

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7
Q

Chloramphenicol

A

MOA: binds 50s subunit and inhibits peptidyl transferase activity

  • oral, IV
  • wide distribution, CNS and bone
  • hepatic Metabolism, glucuronidation, urinary secretion
  • time dependent killing
  • CYP450 inhibitor causing drug interactions
  • mitochondrial toxicity, bone marrow suppression, gray baby syndrome
  • use for GPC, GNR, anaerobes, intracellular bacteria
  • resistance by plasmid mediated CAM acetyltransferase, CFR rRNA methyltransferase confers global resistance
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8
Q

Fluoroquinolones

A

-Ciprofloxacin, levofloxacin, moxifloxicin, delafloxicin
MOA: inhibit DNA topoisomerase II and IV
-bactericidal, concentration dependent killing
-good orally, large distribution
-high amount in bone, kidney, prostate
-BLACK BOX: tendinitis, tendon rupture, peripheral neuropathy, hypoglycemia, teratogenic
-N/V/D , headache, diarrhea, QT prolongation, phototoxicity
-Oral absorption is decreased by sucralfate, antacids, iron, zinc and calcium

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9
Q

Ciprofloxacin

A
  • mostly used against gram negative bacteria

- DO NOT use for URIs, because high rate of resistance in community acquired S. pneumoniae

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10
Q

Delafloxacin

A

-use for MRSA

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11
Q

Levofloxacin

A

-broad spectrum and once daily dosing

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12
Q

Sulfamethoxazole/Trimethoprim

A
  • antifolate drugs - commonly used in combination therapy
  • bactericidal when used in combination
  • use for MRSA, GNR, Nocardia, toxoplasma gondii, Protozoa
  • penetrates CNS, excreted unchanged by kidney
  • avoid in 1st and 3rd trimester of pregnancy
  • may cause Stephen Johnson syndrome, dermatitis, photosensitivity
  • CYP450 inhibition
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13
Q

Metronidazole

A

-bactericidal, concentration dependent killing
MOA: nitro group reduced for activity, forming free radicals to cause DNA breaks
-use for anaerobes, C. Diff, H, pylori, Protozoa, bacterial vag
-penetrates well into body tissue and fluid, including breast milk and CSF
-metallic taste, peripheral neuropathy, disulfiram like rxn with EtOH
-few drug interactions, increase effect of warfarin

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14
Q

Rifamycin

A

MOA: binds to beta sub unity of bacterial DNA dependent RNA polymerase inhibiting RNA synthesis

  • Use for S. Aureus, S. Pneumoniae, legionella, yersinia pestis, coxiella burnetti, neisseria meningtides, mycobacterium
  • bone and joint infections with hardware, TB, and endocarditis
  • rarely used alone, use for bio films
  • turns body secretions red, muscle weakness, pain in limbs
  • CYP450 inducer, many drug interactions
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15
Q

Nitrofurantoin

A

-PO only
MOA: reactive forms damage DNA and interfere with RNA synthesis
-GN and GP
-use for UTIs, rapid absorption so not systemic
-avoid in CrCl <30ml/min, or older than 65
-cause neuropathy, hemolytic anemia (if g6pd def), interstitial pulmonary fibrosis in elderly
-probenecid inhibits tubular secretion

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16
Q

Cell wall agents

A
  • all beta lactams, gylcopeptide, lipopeptide, monobactam, polymyxin
  • time dependent
  • use for GAS
  • all cover MSSA except pcn and amp
  • all resistant to MRSA except 5th gen cephalosporin (ceftaroline)
17
Q

Penicillins

List each and what used for

A

-penicillin, ampicillin/amoxicillin, nafcillin
-rash, bone marrow suppression, jaundice
Penicillin: GAS, GBS, S. Viridans,
Amp/Amoxicillin: Enterococcus and resp flora
Nafcillin: MSSA

18
Q

Cephalosporins

List each gen and use

A

-NOT for enterococcus
Cefazolin(cephalexin): GAS, GBS, MSSA, GNR - does not cross BBB
Ceftriaxone: Resp. Flora, beta-lactamase producing organisms - penetrates CNS
Cefepime: ceftriaxone and pseudomonas
Ceftaroline: MRSA, and ceftriaxone

19
Q

Beta lactam/beta lactamase inhibitors

A
  • Ampicillin/Sulbactam: MSSA, GNR, resp flora, anerobes

- Piperacillin/tazobactam: above plus pseudomonas

20
Q

Carbapenems

A

-Ertapenem, imipenem, meropenem

broad spectrum against GPC, GNR, anerobes

21
Q

Glycopeptide

A

Vancomycin
-GPC only and MRSA
-MOA:glycopeptide bind to D-ala end of cell wall block, prevents cross-linking of transglycosylases
Resistance: associated with substitution of another AA at binding site
-eliminated by renal excretion
-IV only because poorly absorbed in gut, use pill for C. Diff
-Nephrotoxicity, histamine release (Red Man syndrome)

22
Q

Lipopeptide

A
  • Daptomycin
  • MOA:binds to bacterial cell membrane and depolarizes, bactericidal
  • GPC only, MRSA and VRE
  • does not reach CNS, surfactant inactivates drugs
  • rhabdomyolysis, eosinophilic pneumonia
23
Q

Polymyxin Antibiotic

A
  • colistin
  • MOA: acts as a detergent to solubilize membranes in GN bacteria
  • concentration dependent
  • GN only, used for salvage therapy of resistant Pseudomonas, Acinetobacter
  • nephrotoxicity and neurotoxicity
24
Q

Monobactam

A
  • Aztreonam
  • GNR only, pseudomonas
  • Not cross reactive with beta lactams so use if allergic to PCN
25
Q

Oseltamivir, Zanamivir

A
  • CDC recommendation for influenza treatment
  • inhibit viral neuraminidase which are useful for release of virus from infected cell
  • O: Oral, used for patients over 1 y/o, may cause nausea and vomiting
  • Z: intranasal route, for pts over 5y/o, not for pts with asthma or COPD, may cause GI effects and respiratory effects like bronchospasm
26
Q

Amantadine, Rimantadine

A
  • binds viral protein M2 and inhibits viral uncoating
  • large volume of distribution, very small therapeutic window
  • amatadine: decrease dose in pts with renal insufficiency, used now for Parkinson’s disease
  • rimantadine: metabolized by the liver
  • cause anticholinergic effects and CNS stimulant effects
  • resistance from influenza has developed to these
27
Q

Vidarabine

A

-Very toxic, used for life threatening HSV and VZV

28
Q

Acyclovir, valcyclovir

A

-inhibit viral DNA synthesis when phosphorylated intracellularly by a viral thymidine kinase
-IV treatment used for HSV encephalitis and in VZV
-guanosine analogs
-resistance: when absence or partial production of TK, common in HSV
-Valaciclovir- oral prodrug that goes rapid first pass to make acyclovir and L-valine
-only works on actively replicating virus, no effect on latent herpes
HSV1>HSV2>VZV>EBV»>CMV

29
Q

Penciclovir, Famciclovir

A
  • acyclic nucleoside analog of guanosine, also activated by TK
  • Famciclovir is the prodrug
  • used for herpes zoster, genital herpes
  • chronic administration may be tumorigenic
30
Q

Ganciclovir

A
  • analog of guanosine, similar to ACV
  • inhibit viral DNA polymerase
  • during CMV, does not depend on viral TK
  • use: suppression of CMV, prevention of CMV in immunocompromised
  • adverse: bone marrow suppression, thrombocytopenia, liver function problems
  • increased toxicity if given with probenecid and imipenem/cilastin
31
Q

Cidofovir

A
  • cytosine analog that has broad antiviral spectrum
  • use: IV in AIDS pts with CMV, HSV, EBV, VZV
  • adverse: nephrotoxicity, ocular hypotony, carcinogenesis
32
Q

Foscarnet

A
  • inorganic pyrophosphate analog that is inhibitory for herpes and HIV
  • inhibits viral nucleic acid synthesis by interacting directly with herpesvirus DNA polymerase or HIV reverse transcriptase
  • does not require phosphorylation
  • use: CMV, ACV resistant HSV
  • IV only
  • adverse: nephrotoxicity, electrolyte disturbance (low K,Ca,P,Mg), anemia, neurotoxic, DI, HTN, genital ulcers

Drugs/Immuno (9 decks)

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