Cephalosporins Flashcards

(49 cards)

1
Q

Cephalosporins

A

Beta-lactams structurally related to penicillins, 6-Membered dihydrothiazine ring in place of 5-Membered thiazolidine ring, Modification at 7-position alter antibacterial activity but at 3-alter pharmacokinetics, Bactericidal, Similar to penicillins, Classified by generations

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2
Q

Cefazolin

A

Ancef
First (Narrow Spectrum)
Injection
Streptococci (except penicillin resistant strains), S. aureus (except MRSA)
RECOMMENDED BY AHA for premed prophylaxis in penicillin-allergic patients unable to take oral med
Alt. for methicillin group

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3
Q

Cephalothin

A

Keflin
First (Narrow Spectrum)
Injection
Streptococci (except penicillin resistant strains), S. aureus (except MRSA)

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4
Q

Cephalexin

A

Keflex
First (Narrow Spectrum)
Oral
Streptococci (except penicillin resistant strains), S. aureus (except MRSA)
USED IN DENTISTRY TO PREVENT JOINT INFECTION (Total joint replacement surgery, Dental procedures - Tooth extractions, Gum surgery, Professional cleanings and Orthodontic band)

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5
Q

Cephadroxyl

A

Duricef
First (Narrow Spectrum)
Oral
Streptococci (except penicillin resistant strains), S. aureus (except MRSA)

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6
Q

Cefuroxime

A

Ceftin
Second (Intermediate Spectrum)
Injection
E. Coli, Klebsiella, Proteus, H. Influenzae, M. Catarrhalis, Less active VS Gram + than 1st gen

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7
Q

Cefaclor

A

Ceclor
Second (Intermediate Spectrum)
Oral
E. Coli, Klebsiella, Proteus, H. Influenzae, M. Catarrhalis, Less active VS Gram + than 1st gen

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8
Q

Cefoxitin

A

Mefoxin
Second (Intermediate Spectrum)
Injection
Inferior to Cefuroxime VS S. aureus but increased activity VS Bacteroides fragilis and other Bacteriodes spp.

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9
Q

Cefotetan

A

Cefotan
Second (Intermediate Spectrum)
Injection
Inferior to Cefuroxime VS S. aureus but increased activity VS Bacteroides fragilis and other Bacteriodes spp.
Agents containing Methylthiotetrazole (MTT) side chain (cefotetan) interfere w/ Vit K metabolism and cause clotting problems - Use with caution in patients on warfarin or with underlying clotting problems, Agents also cause disulfiram like rxn with alcohol

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10
Q

Ceftriaxone

A

Rocephin
Third
Injection
Enterobacteriaceae, Pseudomonas aeruginosa, Serratia, Neisseria gonorrhoeae, Activity VS S. aureus, Strep. Pneumoniae and Strep. Pyogenes comparable to 1st gen. Activity VS Bacteroides inferior to cefoxitin and cefotetan
AHA RECOMMENDED as injectable premedication for penicillin allergic patients unable to take oral meds

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11
Q

Cefotaxime

A

Claforin
Third
Injection
Enterobacteriaceae, Pseudomonas aeruginosa, Serratia, Neisseria gonorrhoeae, Activity VS S. aureus, Strep. Pneumoniae and Strep. Pyogenes comparable to 1st gen. Activity VS Bacteroides inferior to cefoxitin and cefotetan

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12
Q

Ceftazidime

A
Fortaz
Third
Injection
Enterobacteriaceae, Pseudomonas aeruginosa, Serratia, Neisseria gonorrhoeae, Activity VS S. aureus, Strep. Pneumoniae and Strep. Pyogenes comparable to 1st gen. Activity VS Bacteroides inferior to cefoxitin and cefotetan
ACTIVE VS. PSEUDOMONAS
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13
Q

Ceftizoxime

A

Cefizox
Third
Injection
Enterobacteriaceae, Pseudomonas aeruginosa, Serratia, Neisseria gonorrhoeae, Activity VS S. aureus, Strep. Pneumoniae and Strep. Pyogenes comparable to 1st gen. Activity VS Bacteroides inferior to cefoxitin and cefotetan

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14
Q

Cefpodoxime proxetil

A

Vantin
Third
Oral
Enterobacteriaceae, Pseudomonas aeruginosa, Serratia, Neisseria gonorrhoeae, Activity VS S. aureus, Strep. Pneumoniae and Strep. Pyogenes comparable to 1st gen. Activity VS Bacteroides inferior to cefoxitin and cefotetan

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15
Q

Cefeprime

A

Maxipime
Fourth
Injection
Comparable to third-gem but more resistant to some Beta-lactamases
Zwitterion - Enhanced ability to penetrate porin in outer membrane of Gram - bacteria

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16
Q

First Generation Cephalosporins

A

Greatest activity VS Gram + (Few Gram - P. mirabilis, E. coli, K. pneumoniae), Good bone penetration and greater activity VS Staph., Excellent for joint prosthesis prophylaxis, More stable to bacterial beta-lactamase (Cefazolin for Methicillin group) but not good activity VS Anaerobes (Bacteroides), Excretion by glomerular filtration and tubular secretion, Probenacid will increase serum levels (Blocks tubular secretion), Adjust dose in renal impairment

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17
Q

Second Generation Cephalosporins

A

Expanded activity against Gram - including cephalothin resistant E.coli, Klebsiella and P. mirabilis, Increased spectrum of action due to greater affinity for PBP, Greater penetration of Gram - envelope and Greater resistance to Beta-lactamase hydrolysis, Cephamycins (Cefoxitin) are active against Bacteroides fragilis and Serratia marcescens - Useful to treat mixed anaerobic infections

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18
Q

Third Generation Cephalosporins

A

Good activity VS many Gram - organisms (Enterobacteriaceae, H. influenzae and N. gonorrhoea), Increased Gram - activity due to addition of aminothiazole moiety to beta lactam ring, Good CSF level for treating bacterial meningitis, Ceftazidime and Cefoperazone active VS Pseudomonas, Sensitive to some beta-lactamases from Enterobacter

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19
Q

Fourth Generation Cephalosporins

A

Similar to third but active VS Pseudomonas aeruginosa and organisms resistant to third gen agents, Greater resistance to beta-lactamase than third, Chemical modification at position 7 renders agents more stable against beta-lactamase

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20
Q

Fifth Generation Cephalosporins

A

Ceftaroline (Teflaro) and Ceftobiprole (Future - Not available in US), Active VS Multidrug resistant S. aureus including MRSA, VISA, VRSA, Increased binding to PBP2a responsible for MRSA, Administered IV,
Ceftaroline - Community acquired pneumonia and skin infections

21
Q

Cephalosporin Mechanism of Action

A

Similar to Penicillin, Inhibit cell wall synthesis

22
Q

Cephalosporin Pharmacokinetics

A

Cephalosporins of third gen useful for meningitis by Gram - organisms, First and Second gen do not enter CSF in adequate concentrations, Most excreted by active transport in liver

23
Q

Cephalosporins Adverse Effects

A

Intrathecal admin may cause convulsions, Agents containing Methylthiotetrazole (MTT) side chain (cefotetan) interfere w/ Vit K metabolism and cause clotting problems - Use with caution in patients on warfarin or with underlying clotting problems, Agents also cause disulfiram like rxn with alcohol; Allergic rxns, cross allergenicity to penicillins

24
Q

Azetreonam Chemistry

A

Monocyclic lactam w/unique spectrum of action

25
Azetreonam Spectrum of Action
Active VS Most Gram - bacteria including P. aeruginosa, No activity VS Gram +, Resistant to some Gram - Beta-lactamase, Effective VS P. aeruginosa, Enterobacteriaceae, H. influenzae and Gonococci
26
Azetreonam Uses
Useful in patients with serious penicillin allergy who have infections caused by resistant Gram - organisms
27
Azetreonam Mechanism of Action
Possess a sulfonic acid group attached to N at 1-Position in structure that causes it to bind preferentially to PBP-3 of Gram - bacteria
28
Azetreonam Pharmacokinetics
Poorly absorbed from gut as it is converted to an inactive ring form by intestinal flora, Must be administered IM or IV, Well distributed including CNS, Largely excreted unchanged and eliminated by filtration and tubular secretion, Short t1/2 so frequent dosing necessary, also causes IV site phlebitis
29
Azetreonam Adverse Effects
Similar to other beta-lactams, Pain at site of injection, rash, GI discomfort in form of nausea, vomiting, diarrhea, Alternative to patients allergic to penicillins
30
Daptomycin Mechanism of Action
Unclear, but seems like daptomycin integrates into cell membrane and oligomerize to form pores, resulting in K+ efflux, membrane depolarization and cell death, Given IV, Active VS Gram + organisms, Used to treat complicated skin infections, bacteremia or endocarditis from S. Aureus, Active VS MRSA
31
Daptomycin Adverse Effects
Myopathy, Eosinophilic pneumonia, AAC (C. difficile diarrhea), Do not administer Daptomycin with statin drugs due to common adverse effect of myopathy
32
Bacitracin Spectrum of Action
Topical polypeptide antibiotic, Bactericidal VS Gram + cocci and bacilli, Group A Streptococci are very sensitive
33
Bacitracin Mechanism of Action
Inhibit cell wall synthesis by inhibiting lipid carrier involved in murein monomer synthesis, Zn2+ or Mg2+ required
34
Bacitracin Uses
Used topically for skin, eye and mucus membrane infections caused mainly by group A Streptococci and Staphylococci
35
Bacitracin Pharmacokinetics
Not absorbed orally so remain in gut lumen and occasionally used to treat C. difficile colitis or eradicate vancomycin-resistant enterococci in GI tract
36
Bacitracin Adverse Effect
Significant kidney, bone marrow and neurological effects so not generally used systemically
37
Mupirocin
Bactroban 2% Unique action, Irreversible binding to bacterial isoleucyl t-RNA synthetase blocking protein and RNA synthesis, Topical use for S. aureus skin infections and intra-nasal to treat health worker carriers of MRSA, Bacteriocidal only at high conc., Rare anapylactoid reactions and AAC
38
Fosfomycin Spectrum of Action
Active VS many Gram + and - Bacteria, Used as single dose for uncomplicated lower urinary tract infection in women
39
Fosfomycin Mechanism of Action
Inhibits first step in synthesis of peptidoglycan
40
Fosfomycin Pharmacokinetics and Adverse Effects
Administered orally, Excreted in urine, Safe in pregnancy, Minimal side effects
41
Cycloserine Spectrum of Action
Used to treat TB that is resistant to first line agents, Active VS Gram + and - organisms
42
Cycloserine Mechanism of Action
Structural analogue of D-Ala that inhibit cell wall synthesis by irreversible inhibiting both the alanine racemase that converts L-Ala to D-Ala, and D-Ala-D-Ala ligase that joins together 2 D-Ala. This prevents incorporation of D-Ala into peptidoglycan pentapeptide
43
Cycloserine Pharmacokinetics
Widely distributed in tissue, Excreted in urine as active drug
44
Cycloserine Adverse Effects
Causes serious dose related CNS toxicity w/ headaches, seizures, peripheral neuropathy, tremors and psychosis, Toxicity potentiated by alcohol, isoniazid and ethionamide, Cyclosporine inhibit metabolism of phenytoin
45
Penicillin VK Dose
Child: 25-50mg/kg body weight q6h or q8h for 7days; Max dose - 3g/day Adult: 500mg q6h for 7 days
46
Clindamycin Dose
Child: 8-25mg/kg in 3-4 doses Adult: 150-450mg q6h for 7 days, Max dose - 1.8g/day
47
Amoxicillin Dose
Child: 20-40mg/kg/day q8h if <40kg; 250-500mg q8h or 875mg q12h for 7 days; Max dose - 2g/day Adult: 250-500mg q8h or 875mg q12h for 7 days; Max dose - 2g/day
48
Cephalexin Dose
Child: 25-50mg/kg/day in q6h; Severe infection - 50-100mg/kg/day in q6h; Max dose - 3g/24h Adult: 250-1000mg q6h; Max dose - 4g/day
49
Augmentin - Amoxicillin/Clavulanic Acid
Child: 20-40mg/kg/day in q8h if <40kg; 250-500 mg/kg/day in q8h or 875mg q12h for 7 days; Max dose - 2g/day Adult: 250-500mg q8h or 875mg q12h for 7 days; Max dose - 2g/day