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Pharmacology > From Jen: Antimicrobials > Flashcards

From Jen: Antimicrobials Flashcards

1
Q

Bacteriostatic Drugs

A 
Erythromycin
Clindamycin
Sulfamethoxazole
Trimethoprim
Tetracyclines
Chloramphenicol

ECSTaTIC about bacteriostatics

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2
Q

Bactericidal Drugs

A 
Vancomycin
Fluoroquinolones
PCN
Aminoglycosides
Cephalosporins
Metronidazole

Very Finely Proficient At Cell Murder

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3
Q

PCN

A

PCN G (IV), PCN V (oral)

Protoype beta-lactam abx

MOA: bind PCN-binding proteins (transpeptidases); block transpeptidase linking of cell wall; activate autolytic enzymes

Use: bactericidal for Gram + cocci/rods, Gram - cocci, and spirochetes

Toxicity: hypersensitivity, hemolytic anemia

Resistance: PCNase

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4
Q

Nafcillin, oxacillin, dicloxacillin

A

PCNase-resistant penicillins

Same MOA as PCN (bind PCN-binding protein, inhibit cell wall cross-linking, activate autolytic enzymes)

**Narrower spectrum: PCNase resistant b/c bulkier R group

Use: S.aureus, except MRSA, which has altered PCN binding protein target site (Naf for Staph)

Toxicity: Hypersensitivity

Methicillin: interstitial nephritis

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5
Q

Ampicillin, amoxicillin

A

Amniopenicillins

MOA: same as PCN.
**wider spectrum

PCN-ase sensitive: combine with clavulanic acid (PCNase inhibitor) to enhanve specturm

Use: Extended spectrum for PCN; H. influenza, E. coli, listeria monocytogenes, Proteus miribilis, Salmonella, enterococci
(HELPS kill Enterococci)

Toxicity: hypersensitivity, rash, pseudomembranous colitis

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6
Q

Ticarcillin
Carbenicillin
Piperacillin

A

Antipseudomonals

MOA: same as PCN (bind PCN-binding protein, inhibit cell wall cross-linking, activate autolytic enzymes)

Use: pseudomonas species and Gram - rods

**Susceptible to PCNase, use with clavulanic acid (beta-lactamase inhibitor)

Toxicity: hypersensitivity reactions

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7
Q

cephalosporins

1st generation

A

MOA: beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to PCNase. BacteriCIDAL.

Cefazolin, cephalexin

Use: Gram+ cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae (PEcK)

Adverse: hypersentisitivity, cross hypersensitivity with PCN (5-10%)
nephrotoxicity of aminoglycosides
cefamandole: disulfram-like reaction with ethanol (methylthiotetrazole group)

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8
Q

cephalosporins

2nd generation

A

MOA: beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to PCNase. BacteriCIDAL

Cefoxitin, cefaclor, cefuroxime

Use: Gram+ cocci, H. influenza, Enterobacter aeogenes, Neisseria spp, Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marcenscens
HEN PEcKS

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9
Q

cephalosporins

3rd generation

A

MOA: beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to PCNase. BaceriCIDAL.

Ceftriaxone, cefotaxxime, ceftazidime

Use: Serious Gram- infections resistant to other beta-lactams; meningitis

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10
Q

cephalosporins

4th generation

A

MOA: beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to PCNase. BacteriCIDAL.

Cefepime

Use: increased activity against pseudomonas and Gram+ organisms

Toxicity: Cross hypersensitivity with PCN

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11
Q

Aztreonam

A

Monobactam resistant to beta-lactamases

MOA: inhibits cell wall synthesis (binds to PBP3)

Synergistic with aminoglycosides
**No cross allergenicity with PCN

Use: Gram- rods (Klebsiella, Pseudomonas, Serratia)
No activity against Gram+ or anaerobes
**Best for PCN-allergic patients who cannot tolerate aminoglycosides (renal insufficiency)

Toxicity: usually nontoxic, occasional GI upset

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12
Q

Imipenem/cilastatin,

meropenem

A

MOA: Imipenem is a broad spectrum, beta-lactamase resistant carbapenem. Always administered with cilastatin to decrease inactivation in renal tubules

Use: Gram+ cocci, Gram- rods, anaerobes
Drug of choice for Enterobacter

Toxicity: Significant side effects limit use- GI, skin rash, CNS toxicity

Meropenem: lower risk of seizures, stable to renal tubules (does not require cilastatin)

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13
Q

Vancomycin

A

Inhibits cell wall mucopetpide formation by binding D-ala D-ala precursors. BacteriCIDAL. Resistance occurs with change to D-ala D-lac

Use: Serious, Gram+ multi-drug resistant organisms (S. aureus, C. difficile)

Toxicity: Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing (red man syndrome)

Well tolerated in general

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14
Q

Protein synthesis inhibitors

30S

A

Aminoglycosides

Tetracyclines

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15
Q

Protein synthesis inhibitors

50S

A

Chloramphenicol
Clindamycin
Erythromycin
Linezolid

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16
Q

Aminoglycosides

A

Gentamycin, Neomycin, Amikacin, Toramycin, Streptomycin

MOA: Inhibit formation of initiation complex, causing misreading of mRNA
**Requires O2 for uptake, thus no use against anaerobes

Use: Severe Gram - rod infections
***Synergistic with beta-lactam abx
Neomycin: bowel surgery

Toxicity: Nephrotoxicity (esp with cephalosporins)
Ototoxicity (esp with loop diuretics, TERATOGEN

17
Q

Tetracyclines

MOA

A

Tetracycline, Doxycycline, demeclocycline, minocycline

MOA: Bacteriostatic; bind 30S and prevent attachment of aminoacyl-tRNA

  • *limited CNS penetration
  • *Do not take with milk, antacids, or iron containing preparations

Doxycycline: fecal elimination (good for pts with renal failure)

Demeclocycline: ADH antagonist; acts as diuretic in SIADH

18
Q

Tetracyclines

Use/Toxicity

A

Use: Vibrio cholera, acne, chlamydia, ureaplasma, urealyticum, mycoplasma pneumoniae, tularemia, H. pylori, Borrelia burgdorferi, Rickettsia

(VACUUM THe BedRoom)

Toxicity: GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity
**Contraindicated <8 years

19
Q

Macrolides

A

Erythromycin, Azithromycin, Clarithromycin

MOA: Inhibit protein synthesis by irreversibly blocking translocation; bind the 23S rRNA of the 50S subunit

USE: URI, PNA, STDs (Gram + cocci)

Strep infection in pts allergic to PCN
Mycoplasma, Legionella, Chlamydia, Neisseria

Toxicity: GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes
CYP inhibitor

20
Q

Chloramphenicol

A

Inhibits 50S peptidyltransferase activity (inhibits creation of peptide bonds)

Use: Meningitis (H. influenzae, Neisseria meningitidis, Strep pneumoniae)

Toxicity: conservative use due to toxicity
Anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome (preemies b/c they lack liver UDP glucuronyl transferase)

21
Q

Clindamycin

A

Blocks peptide bond formation at 50S ribosomal subunit.
Bacteriostatic

Use: anaerobic infections (clostridium perfringerns, bacteriodes fragilis)

Toxicity: pseudomembranous colitis, fever, diarrhea

22
Q

Sulfanomides

A

Sulfamethoxazole, sulfisoxazole, sulfadiazine

MOA: PABA antimetabolites that inhibit dihydropteroate synthetase (a step in creating folic acid, required for thymidine and purine synthesis)

Use: Gram +/-, Nocardia, Chlamydia, UTI

Toxicity: Hypersensitivity rxn, hemolysis if G6PD deficient, nephrotoxic (tubulointerstitial nephritis), photosensitivity, kernicterus in infants

**displace other drugs form albumin (warfarin, etc.)

23
Q

Trimethoprim

A

Inhibits bacterial dihydrofolate reductase

Use: In combination with sulfonamides; synergistic block of folate synthesis

Recurrent UTI, Shigella, Salmonella, Pneumocystis jiroveci pneumonia

Toxicity: Megaloblastic anemia, leukopenia, granulocytopenia

24
Q

Sulfa drugs causing hypersensitivity

A 
Sulfonamides (antimicrobials) 
sulfasalazine
sulfonylureas
thiazide diuretics
furosemide
acetazolamide
25
Q

Fluoroquinolones

A

Ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin

MOA: Inhibit DNA gyrase (prokaryotic topoisomerase II)
**Do not take with antacids

Use: Gram - rods of urinary and GI tracts (including pseudomonas), Neisseria, some Gram +

Toxicity: GI upset, superinfections, headache, skin rash, contraindicated in pregnancy and children.
Tendon rupture in adults; leg cramps/myalgias in children

26
Q

Metronidazole

A

MOA: forms toxic metabolites that damage DNA.
BacteriCIDAL, antiprotozoal

Use: Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes
Used with bismuth and amoxicillin for triple therapy against H.pylori.

Toxicity: Disulfram-like RSN with ethanol, headache metallic taste

27
Q

Polymyxins

A

Polymyxin B, E

MOA: Bind to bacterial cell membrane and disrupt their osmotic properties. Polymyxins are cationic, basic proteins that act like detergents.

Use Resistant Gram - infections

Toxicity: Neurotoxicity, acute renal tubular necrosis

Pharmacology (18 decks)

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