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Flashcards in Cephalosporins Deck (17)
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1
Q

What is the general structure of cephalosprins?

A

Beta-Lactam ring

Dihydrothiazine ring - metabolism and pharmacokinetic properties

acyl side chain - antibacterial spectrum activity

2
Q

Oral cephalosporins are available in what form and how are they metabolized?

A

Prodrug esters

Hydrolyzed in the intestine to the active drug

3
Q

What is the MoA of cephalosporins?

A

Binds to PBPs, inhibiting crosslinking of peptidoglycan strains

Efficacy is related to affinity to PBPs

4
Q

Why are cephalosporins good for meningitis?

A

They penetrate the CSF, especially if the meninges are inflamed

5
Q

How are cephalosporins excreted? What are the exceptions?

A

Renal excretion

Ceftiaxone, Cefoperazone - Hepatic elimination

6
Q

What are the adverse effects of cephalosporins?

A

Hypersensitivity reactions - rash,drug fever

Hematology - bleeding

Alcohol, disulfiram-like intolerannce

GI-Diarrhea, Pseudomembranous colitis

Renal - interstitial nephritis

Immunologic - serum sickness (Cefaclor)

7
Q

What are the drug interactions associated with cephalorpsorins?

A

Warfarin - potentiation

Alcohol - only agents with NMTT side chain

Probenecid - prolongs excretion in CSs that have tubular secretion

8
Q

What do cephalosporins generally not cover?

A

Enterococcus and MRSA - except ceftaroline

Chlamydia, Mycoplasma, Legionella

Listeria monocytogenes

9
Q

What is Zerbaxa?

A

Ceftolozane/tazobactam

Cephalosporin with beta lactamase inhibitor

Approved for complicataed UTIs/pyelonephritis

10
Q

What is Ayvcaz?

A

Ceftazidime/avibactam

3rd gen cephalosporin with BL inhibitor

11
Q

What are the uses for cephalosporins?

A

Community acquired pneumonia

Nosocomial pneumonia

Meningitis - ceftriaxone

Skin soft tissue

Surgical prophylaxis - cefazolin

Febrile neutropenia

Endocarditis

STD (Neisseria resistant to PCNs)

12
Q

What is Vabomere?

A

Meropenem-vaborbactam

complicated UTIs including pyelonephritis

13
Q

How do carbapenems work?

A

Binds to PBP resulting in cidal effect

14
Q

What carbapenem has the longest half life?

A

Ertapenem (Invanz)

Allows once daily administration

15
Q

How is imipenem (Primaxin) metabolized?

A

Extensive renal metabolism

Cilastatin added to prevent renal metabolism

16
Q

What are the adverse effects of carbapenems?

A

Seizures
Cross allergenicity w/ PCN

Anemia, Leukopenia, Thrombocytopenia

17
Q

What is aztreonam used for?

A

Serious gram negative infections or penicillin allergic patients