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Pharm - Final exam > Cephalosporins lecture > Flashcards

Cephalosporins lecture Flashcards

1
Q

cephalosporins are closely related to what antibiotic group due to presence of what structure

A

Cephalosporins are similar to the PCN family

Both have beta lactam ring structure

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2
Q

what makes cephalosporins unique and what does this feature do

A

cephalosporins are unique in that they have a 7 methyl group that increases their resistance to Beta-lactamase compared to PCNs

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3
Q

List the features of 1st generation cephalosporins

A

good activity against G+ and moderate against G-
most MSSA G+ cocci susceptible,
good alternative for people with PCN allergy,
some are acid resistant,
increased B-lactamase resistance,
Renal excretion

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4
Q

what is the drug of choice for surgical prophylaxis?

A

Cefazolin (kefzol, ancef) - IV, IM

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5
Q

what are all the 1st generation cephalosporins and their route of administration

A

Cefazolin (kefzol, ancef) - IV, IM
Cephalothin Sodium (Keflin) - IV, IM
Cephalexin (keflex) - ORAL

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6
Q

List the features of the 2nd generation cephalosporins

A
  • they are the same as first generation except have more gram - and less gam + activity
    (e. g. no antipseudomonal activity, increase B-lactamase resistance, some acid resistant, most Renal excretion)
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7
Q

Name the second generation cephalosporins and their route of administration

A

Cefaclor (ceclor) - oral
Cefprozil (cefzil) - oral
Cefuroxime (Zinacef) - IV, IM

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8
Q

Describe the activity of third generation cephalosporins

A
  • less G+ cocci activity
  • more activity against enterobacteriaceae (incl PCNase producing strains)
  • some pseudomonas aeruginosa activity (comb. with aminoglycosides)
  • some are acid resistant
  • increased B-lactamase activity
  • mostly renal excretion (cefoperazone - hepatic secretion)
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9
Q

name the DOC for N. gonorrhoeae and when it should not be used

A

DOC N gonorrheoeae = Ceftriaxone

avoid use in neonates, bilirubin displacement

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10
Q

list all the 3rd gen cephalosporins and their activity

A
  1. Ceftriaxone (Rocephin), CNS penetration, Neisseria
  2. Cefotaxime Sodium (Claforan), CNS penetration
  3. Cefoperazone (Cefobid), CNS penetration, P aeruginosa (metab by liver!!)
  4. Ceftazidime (Fortaz) P. aeruginosa
  5. Cefixime (Suprax) - ORAL
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11
Q

what makes the 3rd generation cephalosporins unique

A

they have CNS penetration and some pseudomonas resistance

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12
Q

List the activity of the 4th generation cephalosporins

A

Similar to 3rd generation, more resistant to some B lactamases, *antipseudomonal, better G+ coverage, renal excretion, broadest coverage**: enterobacteriaceae, MSSA, Pseudomonas, empirical therapy, particularly when resistance to B lactamase are anticipated

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13
Q

how does is the 4th generation of cephalosporins break the pattern of 1st to 3rd generation

A

1st to 3rd have progressing gram- activity and decreasing gram+ activity whereas 4th generation has increased G+ coverage

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14
Q

Name the one 4th generation cephalosporins and what it is used for

A

Cefepime (maxipime) IV is the only fourth generation cephalosporin

It has the broadest coverage (enterobacteriaceae, MSSA, Pseudomonas) so it is used in empirical therapy esp. when resistance to B lactamases are anticipated

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15
Q

Name the characteristics and drug of the “unnamed” generation cephalosporins

A

Unnamed:Ceftaroline fosamil (teflaro) - IV
approved by FDA 2010
no antipseudomonal but DOES cover MRSA and VRSA (this is the only beta lactam active against VRSA)
G+, G- activity, approved for CABG
Renal excretion

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16
Q

Describe the mechanism which the unnamed cephalosporin (Ceftaroline fosamil (teflaro) - IV) acts

A

ceftaroline fosamil (teflaro)-IV can bind PBP2A with very high affinity; PBP2A is the mutated PBP other beta lactamases cannot bind to

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17
Q

DOC Moraxella catarrhalis infection

A

second or third generation cephalosporin

2nd: Cefaclor, Cefprozil, Cefuroxime
3rd: Ceftriaxone, Cefotaxime, Cefoperazone, Ceftazidime, Cefixime

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18
Q

DOC Neisseria gonorrhoeae

A

Ceftriaxone (Rocephin)
Cefixime (Suprax) -oral

*both are third generation cephalosporins

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19
Q

DOC e. coli, Klebsiella, Proteus (these are Gram -)

A

first or second generation cephalosporin

1st: Cefazolin, Cephalothin Sodium, Cephalexin
2nd: Cefaclor, Cefprozil, Cefuroxime

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20
Q

DOC salmonella

A

third generation cephalosporins

3rd: ceftriaxone, cefotaxime, cefoperazone, ceftazidime, cefixime

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21
Q

DOC PCN resistant S. pneumonoiae

A

ceftriaxone (rocephin)

*this is a third generation cephalosporin

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22
Q

DOC B. burgdorferi

A

Ceftriaxone (rocephin)
(late disease)
*this is third gen cephalosporin

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23
Q

Describe the toxicity of cephalosporins

A

~fairly safe, 10% cross sensitivity with PCN (rash, hives, fever, eosinophilia)
~superinfection (enterococci, G-bacilli, Pseudomembranous colitis or candida)
~direct and indirect positive Coomb’s tests
~GI - anorexia, N/V, diarrhea
~dose dep renal tubular necrosis *works syngergistically with aminoglycosides –> nephrotoxicity

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24
Q

what is the therapeutic advantage of Cefazolin (Kefzol, ancef) - IV, IM and what generation does this cephalosporin belong to

A

Cefazolin (kefzol, ancef) is a first generation ceph
advantage: good bone penetration; parenteral med has long duration of action and similar spectrum of action compared to the other first gen cephalosporins (Cephalothin sodium (Keflin) - IV,IM; Cephalexin (Keflex) -oral

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25
Q

What is the therapeutic advantage of Cephalexin (Keflex)- oral and what gen does this ceph belong to?

A

Cephalexin (Keflex)-oral belongs to 1st gen ceph

advantage: prototype of 1st gen oral cephalosporins, PO 2x/day effective against pharyngitis

26
Q

What is the therapeutic disadvantage of Cefaclor (Ceclor) - oral

A

Cefaclor (ceclor) -oral is a second generation cephalosporin associated with serum sickness

27
Q

What is the generation and therapeutic advantage of Cefuroxime (Zinacef) -IV,IM

A

Cefuroxime (zinacef) IV, IM is a second generation cephalosporin
advantage: prototype Parenteral 2nd gen cephalosporin w/ longer t1/2 life than similar agents, can cross BBB and can be used for community acquired bronchitis or pneumonia in elderly and for immunocompromised

28
Q

What is the Therapeutic advantage and generation of Cefixime (Suprax) - oral

A

Cefixime (Suprax) - oral is a 3rd gen cephalosporin

advantage: PO 1x/day

29
Q

What is the therapeutic advantage and generation of cefotaxime (claforan) - IV, IM

A 
Cefotaxime Sodium (Claforan) - IV, IM is a 3rd generation cephalosporin
Advantage: good CSF penetration
30
Q

What is the therapeutic advantage and generation of Ceftazidime (fortaz, tazidime) IM, IV?

A

Ceftazidime (tazidime) IV, IM is a 3rd gen ceph

Advantage: active against P aeruginosa

31
Q

What is the therapeutic advantage and generation of Ceftriaxone (rocephin) IM, IV

A

Ceftriaxone (Rocephin) IM, IV is a 3rd gen ceph
Advantage: longest half life of ceph (6-8 hr) allows once a day dosing. High levels can be achieved in blood and CSF. Effective against genital, anal and pharyngeal PCN-resistant N gonorrhoeae. May use in pt with renal insufficiency bc excreted in bile. Good bone penetration

32
Q

Name the one monobactam

A

Aztreonam (Azactam)

33
Q

What is the activity of the monobactam class and what drug comprises this class?

A

Only monobactam = Aztreonam (Azactam)
*has monocyclic beta lactam ring
*relatively B lactamase resistant
*acitve ONLY against AEROBIC G- rods (pseudomonas, serratia, klebsielle, proteus)
no G+ or anaerobe activity
parenteral admin
few side effects (phlebitis, rash, abn liver func)
*no cross sensitivity with other B lactams thus good if pt has PCN allergy

34
Q

List the carbapenems

A
  1. Imipenem; Cilastatin (primaxin)
  2. Meropenem (merrem)
  3. Ertapenem (invanz)
35
Q

What must imipenem (primaxin) be given with and why? What overall group does imipenem belong to?

A

Imipenem (Primaxin) is a Carbapenem. Must be given with cilastatin, a dihydropeptidase inhibitor bc it is rapidly inactivated by renal tubule dihydropeptidases

36
Q

Imipenem (primaxin), a carbapenem, is inactivated by renal tubule dihydropeptidase and must be admin with cilastatin. What is another carbapenem (not ertapenem) and does it need any special protection

A

The other carbapenem besides Imipenem (primaxin) and ertapenem (invanz) = Meropenem (merrem).

Meropenem is not inactivated by dihydropeptidases

37
Q

What is the activity of Imipenem (primaxin), Meropenem (merrem) and what class do they fall under

A

Imipenem (primaxin) and Meropenum (Merren) are Carbapenems (IV admin)

  • broad spectrum activity - anaerobes, G+/- (good for mixed infections)
  • B lactamase resistant
  • Good idea to combo with an aminoglycoside bc Pseudomonas can dev resistance
38
Q

What is a risk of taking the carbapenem, Imipenem (Primaxin) at high levels?

A

Seizures; use cautiously if renal failure, brain lesion, head trauma, or hx of CNS disorders

39
Q

which is more likely to cause a seizure… Meropenum (Merrem) or Imipenem (Primaxin)

A

Imipenem (primaxin) has the seizure risk

*caution if renal failure, brain lesion, head trauma, hx CNS disorders ie seizure

40
Q

What is the DOC for B lactamase producing enterobacter infections

A

Imipenem (Primaxin) and Meropenem (Merrem)

*these are carbapenems

41
Q

Detail the route and activity/qualities of Ertapenem (Invanz)

A

Ertapenem (invanz) -IV, IM is a carbapenem

  • highly stable against B lactamase
  • wide variety of G+/- and anerobic (Enterobacteriaceae)
  • less active against Pseudomonas (don’t use)

IV,IM 95% protein binding, renal elim

42
Q

What class of drugs is generally the class that is susceptible to B lactamase producing bacteria?

A

PCNs

43
Q

What is the mechanism of action of Vancomycin (vancocin)

A

Vancomycin (vancocin) is an ICWS but is NOT a B-lactam

*it DOES prevent transpeptidation of peptidoglycan chain by binding to the terminal D-ala-D-ala

44
Q

Why is vancomycin (vancocin) useful

A

Vancomycin (vancocin) is good against PCN and MRSA infections!!, & for G+ infections in PCN allergic pt (IV)… ONLY G+

45
Q

Oral vancomycin (vancocin) is used for…

A

treating superinfections caused by staphylococcus and C diff

*note that first choice for C diff is METRONIDAZOL

46
Q

Why should vancomycin (vancocin) be drug of last resort

A

bc of emerging VRE (vancomycin resistant enterococci) and need for alt. MRSA tx

47
Q

What are some of the adverse side effects of Vancomycin (Vancocin)

A

risk of thrombophlebitis (if IV injection)
Ototoxic*
Nephrotoxic*
“red man” syndrome (from histamine release)

48
Q

Fosfomycin (Monurol) - mechanism?

A

Fosfomycin (monurol) is an ICWS at early step in peptidoglycan synthesis by acting as analog of PEP to prevent NAG ==> NAM reduction. *Structurally unrelated to other drugs

49
Q

Activity of Fosfomycin (Monurol).. admin, excretion, use?

A

G+/G-
admin Orally, excreted by kidney
Use: uncomplicated low UTI
*combo with B-lactam, aminoglycoside, or fluoroquinolone for synergistic effect

50
Q

Bacitracin (AK-tracin) Inhibits CWS how?

A

interferes with final dephos step in PL carrier cycle –> can’t transport NAG-NAM across inner membrane thus can’t assemble cell wall

51
Q

What is/are the route(s) for Bacitracin (AK-tracin) and what is it’s activity?

A

Bacitracin (AK-tracin) is admin parenterally rarely (bc nephrotoxicity risk), usu topical polypeptide antibiotic (NEOSPORIN) to prevent superficial skin/eye infections

G+
G- when combo w/ neomycin and polymyxin

52
Q

What is the MOA of cycloserine (seromycin)

A

Cycloserine (seromycin) ICWS by preventing D-ala from being incorportated into Peptidoglycan pentapeptide

53
Q

What is cycloserine (seromycin) used for

A

cycloserine (seromycin) is used as 2nd line, broad spectrum antibiotic to treat activit pulmonary and extrapulmonary TB and UTI’s

*can be bactericidal or bacteriostatis)

54
Q

what are the adverse effects of cyclserine (seromycin) therapy

A

CNS side effects (HA, depression, psychosis) are the adverse side effects assoc with cycloserine (seromycin) tx

55
Q

MOA: vancomycin, B-lactams, Bacitracin, Cycloserine, Fosfomycin
*all ICWS

A

Vancomycin: Prevents elongation of Peptidoglycan and cross lining of peptide chains by binding to D-ala-D-ala and inhibits transpeptidation

B lactams: interfere with PBP, prevents structurally strong cell wall

Bacitracin: Maintains lipid carrier in phosphorylated state so can’t transport NAG-NAM across membrane to assemble cell wall

Cycloserine: prevents D-ala from being incorportated into peptidoglycan pentapeptide (don’t make proper peptide chain)

Fosfomycin: acts as PEP analog in the early phase of peptidoglycan synthesis preventing NAG –> NAM reduction

56
Q

What is DOC for M. Catarrhalis (G- cocci aerobe)

A

2nd/3rd gen cephalosporin

2nd: Cefaclor (Ceclor) -ORAL, Cefprozil (Cefzil) -ORAL, Cefuroxime (Zinacef) -IV,IM
3rd: Ceftriaxone (Rocephin), Cefotaxime sodium (claforan), Cefoperazone (Cefobid), Ceftazidime (Tazidime) **ALL 3rd gen = IV/IM except Cefixime (suprax) - ORAL

57
Q

DOC N gonorrhoeae (G- bacilli aerobe)

A

Cefriaxone (Rocephin) - 2nd gen

Cefpodoxime

58
Q

DOC Enterobacter, Citrobacter, Serratia (G- bacilli aerobe)

A

Carbapenem: Imipenem (Primaxin), Meropenem (Merrem)

  • Ertapenem (invanz)?? not sure if this carbapenem is included as DOC
59
Q

DOC MRSA (G+cocci)

A

vancomycin (vancocin)

60
Q

DOC Bacillus species (non anthracis)? (G+ bacilli aerobe)

A

vancomycin (vancocin)

61
Q

DOC salmonella (G- bacilli, aerobe)

A

Cephalosporin 3rd gen

  1. Ceftriaxone (rocephin),
  2. Cefotaxime sodium (clarforan),
  3. Cefoperazone (cefobid),
  4. Ceftazidime (tazidime)
    * all above are IV, IM
  5. Cefixime (suprax) - ORAL
62
Q

DOC B. burgdorferi (spirochetes) - Lyme disease

A

late stages: Ceftriaxone

Pharm - Final exam (3 decks)

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