unit 10.3: beta-lactam - cephalosporins

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Cephalosporin

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41 Terms

1

Cephalosporin

  • Derivatives of 7-aminocephalosporanic acid

  • With 2 sites of attachment for various R1 and R2 groups

  • More stable to many bacterial β–lactamases, has broader spectrum of activity

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Giuseppe Brotzu

  • Isolated Cephalosporin C compound in from the fungus Acremonium, previously known as "Cephalosporium” in 1945.

    • Found in the sea near a sewage outfall in Su Siccu, by Cagliari harbour in Sardinia, Italy

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R group at 7-position

alters antibacterial activity

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R group at 3-position

modifies pharmacokinetic profile

  • whether they can traverse the blood-brain barrier or not

  • hydrophobic or hydrophilic

  • biliary or urinary

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  • Cephalexin

  • Cefazolin

  • Cefadroxil

  • Cephalotin

  • Cephradine

  • Cephapirin

First generation

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  • Cefuroxime

  • Cefoxitin

  • Cefotetan

  • Cefamandole

Second generation

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  • Ceftriaxone

  • Cefotaxime

  • Cefoperazone

  • Ceftazidime

  • Cefixime

Third generation

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Cefepime

Fourth generation

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  • Ceftaroline

  • Ceftolozane

Fifth generation

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Bind to PBPs

Mechanism of Action

inhibit cell wall synthesis, similar to penicillins

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Structural differences

Mechanism of Action

___ render them less susceptible to penicillinases produced by staphylococci

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MRSA

Mechanism of Action

resistant to cephalosporins

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Most are parenteral

Pharmacokinetics

administered or occurring elsewhere in the body than the mouth and alimentary canal.

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renal excretion

Pharmacokinetics

Major elimination

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hepatic metabolism

Pharmacokinetics

some with side chains

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Cefoperazone and ceftriaxone

Pharmacokinetics

excreted in the bile

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1st- and 2nd-generation

Pharmacokinetics

Do not enter the CSF when the meninges are inflamed1st- and 2nd-generation

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1st Gen: Cefazolin and cephalexin

Clinical Use

  • against G+ cocci, E coli, K pneumoniae

  • Surgical prophylaxis

  • Minimal activity (Gram (-) cocci, Enterococci. MRSA, Most gram (-) rods)

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Second Generation

Clinical Use

  • Less activity against gram (+)

  • Extended coverage for gram (-)

  • Marked differences in activity occur among the drug

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Cefotetan, Cefoxitin

Clinical Use: 2nd Gen

  • Anaerobic coverage

  • B. fragilis

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Cefamandole, cefuroxime, cefaclor

Clinical Use: 2nd Gen

H influenzae, M catarrhalis

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Ceftazidime, cefoperazone, cefotaxime

  • penetrates BBB except cefoperazone, cefotaxime

Clinical Use: 3rd Gen

  • Increased activity against gram (-) organisms resistant to other beta-lactam drugs

  • Ability to penetrate the blood-brain barrier

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Ceftriaxone

Clinical Use: 3rd Gen

  • gonococcal urethritis - purulent discharge

  • Single injection for acute otitis media

  • As effective as 10 days of amoxicillin

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Ceftriaxone (IV) and cefixime

Clinical Use: 3rd Gen

Drug of choice for gonorrhea

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Cefepime

Clinical Use: 4th Gen

  • more resistant to beta lactamases

  • combines gram positive activity / coverage of 1st gen with wider gram neg

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Ceftaroline

Clinical Use: 4th Gen

  • active against MRSA that is resistant to Cephalosporins

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rashes to anaphylactic shock

Toxicity

  • Allergy

  • Complete cross reactivity should be assumed

  • less frequently than penicillins

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5-10%

Toxicity: Allergy

  • Partial cross reactivity between penicillin and cephalosporin

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  • Pain at IM injection site

  • Phlebitis after IV injection

  • Increase nephrotoxicity of aminoglycosides

Toxicity:

Other adverse effects

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Cefamandole, cefoperazone, cefotetan

Toxicity: Other adverse effects

  • Drugs containing a methylthiotetrazole group

  • May cause hypoprothrombinemia

  • Disulfiram-like reactions with ethanol

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  • Listeria

  • Atypicals

  • Methicillin-resistant staphylococcus aureus (MRSA)- except Ceftaroline

  • Enterococcus

Cephalosporins are “LAME” because they are inactive against

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Cephalexin

First Generation:

  • effective against pharyngitis (above umbilicus infections) which (back then) were mostly gram-positive

  • cell wall will be thicker for gram-positive

  • gram-negative are resistant with beta lactams

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Cefazolin

First Generation:

  • parenteral route (IV)

  • longer duration of action, but similar spectrum

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Cefuroxime

Second Generation:

  • given parenterally

  • longer half life

  • it can cross blood brain barrier

  • used for community-acquired bronchitis & pneumonia

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Cefuroxime axetil

Second Generation:

  • twice daily

  • quite resistant even against to beta-lactamase-producing organism

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Ceftriaxone

Third Generation:

  • effective against genital, anal and pharyngeal penicillin-resistant neisseria gonorrhoeae

  • excreted through the bile

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Ceftazidine

Third Generation:

  • anti-pseudomonal coverage

    • Pseudomonas are hospital-acquired germ with numerous resistance

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Cefotaxime

Third Generation:

  • good choice for infections (bacterial encephalitis & bacterial meningitis)

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Cefepime

Fourth Generation:

  • anti-pseudomonal property

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interstitial nephritis and tubular necrosis

  • if combined with aminoglycoside (protein synthesis inhibitor

  • cephalosporin don’t go along well w/ aminoglycoside

Adverse Reactions of Cephalosporins

Renal

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Hypoprothrombinemia and bleeding disorders

Adverse Reactions of Cephalosporins

Hematologic

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