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Pharm > cephalosporins 67 > Flashcards

cephalosporins 67 Flashcards

1
Q

Cefazolin (generic, Ancef) - parenteral

A

First Generation (Older) Cephalosporin

  • drug of choice for surgical prophylaxis*
  • activity against staph and some G- enterics
  • SE: disulfiram-like rxn, anticoagulation (kill off vitamin K- methlythiotetrazole group in the R2 position)
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2
Q

Cephalexin (Keflex), cephalexin HCl monohydrate (Keftab) - oral

A

First Generation (Older) Cephalosporin

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3
Q

Cefaclor (Ceclor) -oral

A

Second Generation Cephalosporin

  • good for sinusitis and OM (S. pneumoniae, H. influenzae, M. Catarrhalis, S. Pyogenes)
  • more commonly implicated in causing serum-sickness like reactions: erythema multiforme or maculopapular pruritic rash or urticaria accompanied by arthritis, arthalgia and fever.
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4
Q

Cefoxitin (Mefoxin) - parenteral

A

Second Generation Cephalosporin

activity against B. fragilis (anaerobe)

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5
Q

Cefuroxime Axetil (Ceftin) –oral; Cefuroxime (Zinacef) - parenteral

A

Second Generation Cephalosporin

  • good for sinusitis and OM (S. pneumoniae, H. influenzae, M. Catarrhalis, S. Pyogenes)
  • coverage against S. pneumo, B-lactamase producing H. flu and Kleb – Making it useful for CAP
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6
Q

Cefprozil (Cefzil) – oral

A

Second Generation Cephalosporin

-good for sinusitis and OM (S. pneumoniae, H. influenzae, M. Catarrhalis, S. Pyogenes)

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7
Q

Ceftriaxone (Rocephin) - parenteral

A

Third Generation Cephalosporin

  • longest half life (8 hrs)
  • enter the CNS, can be used for meningitis
  • eliminated via bile, not need to adjust for renal failure
  • 1st line for tx Gonorrhea
  • neurologic complications of lyme disease
  • gonorrhea*
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8
Q

Cefixime (Suprax) - oral

A

Third Generation Cephalosporin

gonorrhea

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9
Q

Cefotaxime (Claforan) - parenteral

A

Third Generation Cephalosporin

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10
Q

Ceftazidime (Fortaz, Tazidime) – parenteral

A

Third Generation Cephalosporin

activity against Pseudomonas, use combo with amino glycoside to tx pseudomonal meningitis

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11
Q

Cefepime (Maxipime) - parenteral

A

Fourth Generation Cephalosporin

useful for enterobacter infections (UTI)

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12
Q

Ceftaroline fosamil (Teflaro) – parenteral

A

Fifth Generation Cephalosporin

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13
Q

Ceph structure

A

similar in structure to penicillins and have a beta-lactam ring structure
derivative of 7.amino cephalosporonic acid (7-ACA)
(Chemical modifications at the 7 position of the beta-lactam ring (R1) are associated with changes in antibacterial activity, changes in the 3 position (R2) of the dihydrothiazine ring are associated with changes in metab/pharmko props

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14
Q

Ceph MOA

A

interfere with bacterial cell wall synthesis and are bactericidal
-split in the B-lactam ring structure destroys the activity

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15
Q

1st gen all have PH in their name

A

To know the first generation
cephalosporins you must have a PH.D. in Pharmacology:
cephalexin

exceptions – cefazolin and cefadroxil are first generation drugs without a Ph in their name but don’t let
that Faze you its just a fad.
(others: cephalothin, cephapirin, cephradine)

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16
Q

2nd gen mnemonic

A 
have a fam, fa, fur, fox, tea in their names. After you get your Ph.D. your family will want to celebrate – The FAMily is gathered, some wearing FUR coats, and your FOXy cousin is drinking TE(A) and taking PROzac while driving her CAR.
It's NICe to have METlife insurance
cefamandole
*cefaclor
*cefuroxime 
*cefoxitin 
cefote(a)tan 
*cefprozil 
loracarbef
cefmetazole
cefonicid
17
Q

3rd gen mnemonic

A

Most of the third generation drugs have a T in their name and T is for TRI and
after you drive your car you might have to FIX it.
exceptions – cefoperazone, cefpodoxime, Cefdinir

  • ceftriaxone
  • ceftazidime
  • cefotaxime
  • cefixime

Note – cefote(a)tan has a t but it is a second generation drug because your foxy cousin is drinking tea and cefmetazole is a second generation (cause you need METlife insurance)

18
Q

Ceph 1/2 life

absorption can be decreased by ??

A

most have half-lives in range of 1-3 hrs
*Ceftriaxone has longest 1/2 life of 8 hours : 1-2x day possible

-antacids (cefaclor), H2 antagonists (cefdoxime, cefuroxime)

19
Q

Ceph tissue distr.

A
  • 1st and 2nd gen Cephs tend not to have good penetration into the CNS even if inflamed meninges, not used for meningitis
  • EXCEPT Cefuroxime (2nd) does penetrate CNS, but less active against bac that cause meningitis compared to 3rd gen cephs, NOT typically used
20
Q

ceph 3rd gen advantages

A

penetrate CNS and can be used for meningitis: Ceftriaxone, Cefotaxime, Ceftazidime

4th gen: Cefepime: enters CNS and can be used for meningitis
5th gen: Ceftaroline: experimentally can be used for meningitis

21
Q

ceph elimination

A

most via renal excretion by glom. filt. and tubular secretion (organic acid. sec. mech)

adjust w. renal failure
probenicid slows sec. of most ceps
excretion of 3rd ten : Ceftriazone is mainly via bile, not nec. to adjust for renal failure

22
Q

ceph toxic effects

A

90% of pts allergic to PCNs may be able to take cephs
5-10% cross-allergenicity

  • if pt has sev. immediate rxn (anaphylaxis) to PCN: should NOT get ceph
  • if mild rxn to PCN, can cautiously take ceph
  • no skin test to predict allergic rxns
  • T1 hypersensitivity: urticaria, pruritis, angioedema, bronchospasm, maculopapular rash, fever, eosinophilia, rarely severe anaphylaxis and death
23
Q

ceph SEs

A

intolerance of etOH, disulfiram-like rxn via inhibition of aldehyde dehydrogenase–> accumulation of acetaldehyde

  • flushing ha, N/V, hypotension
  • avoid ingestion of etOH while taking and 24-72 hrs after drug
  • Cefazolin more effect: methylthiotetrazole group in R2
24
Q

ceph adverse: bleeding disorders

A

PT deficiency, thrombocytopenia, dec. in platelets, platelet dysfunc.

  • kills off vit. K producing bac in GIT
  • vit. K confers biol. activity upon PT and factors 7,9, 10
  • Cefazolin*
  • administer vit K (10mg 2x/wk)
25
Q

other ceph adverse

A
  • Nephrotoxicity: renal tubular necrosis, synergistic nephrotoxic effect w. co-admin of loop diuretic/aminoglycoside (esp. oldies and renal disease pts)
  • seizures in pts w. renal impairment (if dose not lowered)
  • oral admin: N/V/D
  • Superinfection with opportunistic microorganisms (e.g. pseudomembranous colitis caused by clostridium difficult)
  • pregnancy category B: safety not established, appear to be safe
26
Q

resistance to cephs

A

The most important resistance mechanism to cephalosporins is destruction of the beta-lactam ring.
1st gens are inactivated by B-lactamase.
in general, subsequent gens. are more resistant to breakdown by B-lactamases
*Cefaclor is a susceptible 2nd gen drug
-The best way to minimize resistance to the cephalosporins is to limit or restrict the usage of the drug.

27
Q

Cephalosporins are classified into Generations (1-4) based on Antimicrobial activity

A

First gen ceph have good activity against G+ and S. pneumo, and modest activity against G-
2nd gen: less S. pneumo,
3rd gen: less G+ coverage

4th and 5th?
5th: coverage against MRSA and Enterococcus

28
Q

1st gen

A

G+ EXCEPT Enterococci, MRSA, MRSE (S. epidermidis)

  • activity against oral cavity anaerobes: peptostrp, (B. fragilis is resistant)
  • some G- enterics: Proteus mirabilis, E. coli, Kleb (PEK)
29
Q

1st gen uses

A
  • NOT for serious systemic infections
  • staph and strep infections in pts w. mild allergic rxns to PCNs
  • oral agents for UTIs, minor staph infections, minor polymicrobial infections (cellulitis, ST abscess)
30
Q

2nd gen activity

A

G+ : less activity than 1st gen
G-: MORE activity than 1st gen (H. flu, M. cat)
-use for *RTIs (1st gens are NOT)
anaerobes, i.e. Cefoxitin activity against B. fragilis
-NOT active against pseudomonas
-do have activity against enterobacter, but not used here clinically (due to B-lactamase induction)

31
Q

2nd gen uses

A

oral: sinusitis, OM, CAP
- activity against Strep, H. flu, M. cat, Kleb
- mixed anaerobic infections (peritonitis, diverticulitis)
- skin/ST, UTIs
* not for meningitis

32
Q

3rd gen drugs

A

-much more active against G- than 2nd, useful against G- bacilli resistant to other ceps, PCNs, aminoglycosides
-Broader spectrum because they are resistant to B-lactamases
-less active than 1st gen against G+
-in vitro activity against enterobacter species but should not be used clinically since mutants that express a chromosomal β-lactamase emerge rapidly during
treatment

33
Q

3rd gen uses

A
  • serious inf. resistant to other drugs
  • 1st line for tx Gonorrhea (N. ton) (*Ceftriaxone IM, Cefixime)
  • penetrate CNS, used to tx meningitis (S. pneumo, H. flu, enteric G- rods)
  • what if Listeria? Amp
  • what if highly PCN resistant? vanco
  • empiric sepsis tx
  • sepsis, RTIs, UTIs, skin/ST, bone/jt
34
Q

4th gen

A
  • extended spectrum compated to 3rd gen
  • more resistant to breakdown by plasmid and chromosomal B-lactamases
  • against G- resistant to 3rd gen (pseudomenas, enterobacteriaceae)
  • PCN resistant Strep
  • uses similar to 3rd gen (UTIs, skin/ST, pneumonia, complicated intro-abd. inf.)
  • used for meningitis, penetrates CSF
35
Q

5th gen

A

-increased binding to PBP, responsible for methicillin-resistance so: ACTIVITY AGAINST MRSA
-some activity against Enterococci
used for:
-CAP: Strep pneumo, Staph (needs to be MSSA if respiratory), H. flu, Kleb, E. coli
skin infections: MRSA, strep pyogenes, strep agalactiae, E. coli, Kleb

Pharm (45 decks)

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