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Pharmacology Review - Antimicrobials

1st gen cephalosporin: G+ cocci, PEcK (Proteus

mirabilis, E. coli, Klebsiella pneumoniae)

1.

2nd gen cephalosporin: G+ cocci, HEN PEcKS

(Haemophilus influenze, Enterobacter aerogenes,

Neisseria species, Proteus mirabilis, E. coli, Klebsiella

pneumoniae, Serratia marcescens

2.

30S protein synthesis inhibitors: Aminoglycosides and

tetracyclines

3.

3rd Generation cephalosporin: serious G- infections

resistant to other Beta lactams; meningitis (most

penetrate BBB)

4.

4th gen cephalosporin: increased activity against

pseudomonas G+ organisms

5.

50S protein synthesis inhibitors: CELL /

Chloramphenicol, Erythromycin, Lincomycin,

cLindamycin // all are bacteriostatic

6.

Aminoglycosides: (streptomycin, gentamicin, tobramycin,

amikacin) / bactericidal

7.

Aminoglygosides: Mechanism of Action: Block protein

synthesis at 30s ribosomal subunit

8.

Amphotericin B: Mechanism of Action: disrupt fungal cell

membranes

9.

Ampicillin: Mechanism of Action: Blocks cell wall

synthesis by inhibition of petidoglycan cross-linking

10.

Ampicillin, Amoxicillin: Same mechanism of action as

penicillin. Wider spectrum; penicillinase sensitive

11.

Ampicillin, amoxicillin (clinical use): ampicillin /

amoxicillin HELPS kill enterococci (Haemophilus

influenzae, Escherichia coli, Listeria monocytogenes,

Proteus mirabilis, Salmonella, enterococci)

12.

Ampicillin, amoxicillin (toxicity): Hypersensitivity

reactions; ampicillin rash; pseudomembranous colitis

13.

Aztreonam: A monobactam resistant to Beta lactamases.

Inhibits cell wall synthesis - synergistic w/

aminoglycosides / no cross-alergenicity w/ penicillins

14.

Aztreonam: Mechanism of Action: Blocks cell wall

synthesis by inhibition of peptidoglycan cross-linking

15.

Aztreonam (clinical use): G- rods (klebsiella species,

Pseudomonas species, Serratia species) // no activity

against anaerobes. // used for penicillin-allergic

patients and those w/ renal insufficiency who can't

tolerate aminoglycosides / usually nontoxic - can cause

GI upset

16.

Bacitracin: Mechanism of Action: Block peptidoglycan

synthesis

17.

Carbenicillin, Piperacillin, ticarcillin: Same mechanism

of action as penicillin; extended spectrum -

pseudomonas species and G- rods; susceptible to

penicillinase; use w/ clavulanic acid; can cause

hypersensitivity reaction

18.

Cephalosporin toxicity: hypersensitivity, increased

nephrotoxicity of aminoglycosides, disulfiram-like

reactions w/ ethanol

19.

Cephalosporins: Mechanism of Action: Blocks cell wall

synthesis by inhibition of peptidoglycan cross-linking

20.

Cephalosporins (mechanism of action): beta lactam

drugs that inhibit cell wall synthesis but are less

susceptible to penicillinases; bactericidal

21.

Chloramphenicol: Mechanism of Action: Block Protein

synthesis at 50s ribosomal subunit

22.

Clindamycin: Mechanism of Action: Block Protein

synthesis at 50s ribosomal subunit

23.

DOC for enterobacter: imipenem / cilastatin24.

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Erythromycin/Macrolides: Mechanism of Action: Block

Protein synthesis at 50s ribosomal subunit

25.

fluconazole (azoles): Mechanism of Action: disrupt fungal

cell membranes

26.

Gonorrhea: Ceftriaxone (3rd Gen ceph)27.

Imipenem: Mechanism of Action: Blocks cell wall

synthesis by inhibition of peptidoglycan cross-linking

28.

Imipenem / cilastatin: Broad-spectrum, beta

lactamase-resistant / always given w/ cilastatin (inhibits

renal dihydropeptidase 1 --> decrease imipenem

inactivation in renal tubules)

29.

Imipenem / Cilastatin (clinical use): G+ cocci, G- rods,

and anaerobes

30.

Imipenem / cilastatin (toxicity: GI distress, skin rash, and

CNS toxicity (seizures) at high plasma levels

31.

Lincomycin: Mechanism of Action: Block Protein

synthesis at 50s ribosomal subunit

32.

methicilin, nafcillin, dicloxacillin (toxicity):

hypersensitivity reactions

33.

Methicillin (toxicity): interstitial nephritis34.

Methicillin, nafcillin, dicloxacillin: same mechanism of

action as penicillin. Narrow spectrum; Penicillinase

resistant due to bulkier R group

35.

Methicillin, nafcillin, dicloxacillin: clinical use --> treat

staph aureus

36.

Nystatin: Mechanism of Action: disrupt fungal cell

membranes

37.

Penicillin: 2 forms G (IV form) // Penicillin V (oral)38.

Penicillin: Mechanism of Action: Blocks cell wall synthesis

by inhibition of peptidoglycan cross-linking

39.

Penicillin (clinical use): bactericidal for G+ cocci, G+

rods, G- cooci, and spirochetes. Not penicillinase

resistant

40.

Penicillin (mechanism of action): 1. Binds

penicillin-binding proteins 2. Blocks transpeptidase

cross-linking of cell wall 3. Activates autolytic enzymes

41.

Penicillin (toxicity: hypersensitivity reactions, hemolytic

anemia

42.

Pentamidine: Mechanism of Action: unknown mechanism

of action

43.

Piperacillin: Mechanism of Action: Blocks cell wall

synthesis by inhibition of peptidoglycan cross-linking

44.

Polymyxins: Mechanism of Action: Disrupt

bacterial/fungal cell membranes

45.

Pseudomonas: ceftazidime (3rd gen ceph)46.

Quinolones: Mechanism of Action: Block DNA

topoisomerases

47.

remember: amOxicillin has greater Oral bioavailability

than ampicillin

48.

Rifampin: Mechanism of Action: Block mRNA synthesis49.

Streptogramins (quinupristin,dalfopristin): Mechanism

of Action: Block Protein synthesis at 50s ribosomal

subunit

50.

Tetracyclines: bacteriostatic51.

Tetracyclines: Mechanism of Action: Block protein

synthesis at 30s ribosomal subunit

52.

Ticarcillin: Mechanism of Action: Blocks cell wall

synthesis by inhibition of peptidoglycan cross-linking

53.

Vancomycin: Mechanism of Action: Block peptidoglycan

synthesis

54.

Vancomycin (clinical use): used for serious, G+

multidrug-resistant organisms. including staph aureus

and Clostridium difficile (pseudomembranous colitits)

55.

Vancomycin (mechanism of action): inhibits cell wall

mucopeptide formation by binding D-ala D-ala portion

of cell wall precursors / Bactericidal / resistance occurs

w/ amino acid change of D-ala D-ala to D-ala D-lac

56.

Vancomycin tocicity: NOT - Nephrotoxicity, Ototoxicity,

and Thrombophlebitis, diffuse flushing -->"red man

syndrome" (can prevent w/ pretreatment w/

antihistamines and slow infusion rate)

57.

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What can you combine w/ ampicillin or amoxicillin to

enhance spectrum: clavulanic acid (penicillinase

inhibitor)

58.