Beta Lactam Flashcards by Sheila Mallari

What are the 4 beta lactam antibiotics

Penicillin
Cephalosporin
Monobactam
Carbapenems

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MOA of bacte. growth inhibition by beta lactam

Interfere with transpeptidation rxn of bacterial cell wall synthesis

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Absorption of all oral penicillins are impaired by food EXCEPT

Amoxicillin

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_ and _ penicillins are formulated to delay absorption resulting to prolonged blood and tissue con’c

Benzathine

Procaine

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Excretion of penicillin (time)

Normal renal: 30mins

Renal failure: 10 hours

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Classification of penicillin

Penicillin G

Penicillin V

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What are the antistaphylococcal penicillins

Oxacillin
Cloxacillin
Dicloxacillin
Nafcillin

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What are the extended spectrum penicillin

Aminopenicillin: amoxicillin, ampicillin

Carboxypenicillin: carbenicillin, ticarcillin

Ureidocillin: pipercillin, mezlocillin, azlocillin

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Antistaph penicillin cleared by biliary excretion

Nafcillin

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Antistaph penicillin cleared by biliary and urinary excretion

Oxacillin
Cloxacillin
Dicloxacillin

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Indicated for strep pharyngitis, syphilis, leptospirosis

Penicillin G

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Penicillin for MILD to MODERATE LOCALIZED staph infxn

(Oral)

Isoxazolyl penicillin: cloxacillin, dicloxacillin

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Penicillin for SERIOUS SYSTEMIC staph infxn

Oxacillin
Nafcillin
(IV)

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Penicillin indicated for shigellosis and listerosis

Ampicillin

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Penicillin with less enterococcal activity

Carboxypenicillin:
Carbepenicillin
Ticarpenicillin

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Extended spectrum penicillin indicated for SERIOUS INFECTIONS

Carboxypenicillin: ticarcillin

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Antipsuedomonal penicillins

Ticarcillin
Piperacillin
Mezlocillin
Azlocillin

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2 drugs given in combi with antipseudomonal penicillin

Aminoglycoside

Fluoroquinolone

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Serious adverse effects of penicillin

Hypersensitivity

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Penicillin: AE is neutropenia

Nafcillin

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Penicillin: AE is hepatitis

Oxacillin

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Penicillin: AE is interstitial nephritis

Methicillin (no longer used)

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Only 1st gen cephalosporin administered IV route?

Cefazolin

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Indicated for UTI, cellulitis, soft tissue abscess

Oral 1st gen cephalosporin

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Advantage of cephalosporin over penicillin

More stable and broader spectrum

Drug of choice for surgical prophylaxis, history of penicillin allergy and serious staph infxns

Cefazoli

2nd gen cephalosporin against anaerobes

Cefoxitin Cefmetazole Cefotetan

What gen of cepha is indicated for sinusitis, otitis, and LRTI

2nd gen

2G cepha for community acquired pneumonia

Cefuroxime

2G cepha for peritonitis, diverticulitis and pelvic inflammatory disease

Cefoxitin Cefmetazole Cefotetan

Dosage of ceftriaxone (3G) for: most serious infections and meningitis

1g per day | 2g every 12 hrs

All 3rd gen cephalosporin can penetrate body fluids and tissues. True or False

False. | Except cefoperazone and oral cephalo

All 3G cephalo need dosage adjustment Px with renal insufficiency. True or False

False. | Not need: cefoperazone & ceftriaxone - billiary excretion

3G cephalo for bacterial meningitis (2)

Ceftriaxone | Cefotaxime

3G cephalo bacte coverage: B fragilis

Ceftizoxime | Moxalactam

3G cephalo active against pseudomonas

Ceftazidime | Cefoperazone

3G cephalo indicated for febrile neutropenia

Ceftazidime

Excretion of 1G cephalo

Glomerular filtration | Tubular secretion

Excretion of 1G cephalo is blocked by what drug

Probenecid

3G cephalo is avoided in treatment of which organisms which can cause drug resistance

``` ESCHAPPM Enterobacter Serratia Citrobacter Hafnia Aeromonas Proteus Providencia Morganella ```

Which gen of cephalo penetrates well the csf and cleared by the kidney

4G Cefepime

1st beta lactam against MRSA

Ceftaroline (5G)

What increases the risk of cross reactivity rxn among cephalosporin

R1 side chains

Cephalosporin that contains METHYLTHIOTETRAZOLE GROUP

CefaMANDOLE (2G) CefMETAZOLE (2G) CefoTETAN (2G) CefoPERAZONE (3G)

AE of methylthiotetrazole group

Hypoprotothrombinemia and bleeding disorders

Tx for AE of methylthiotetrazole group containing cephalosporin

Vit K1 (10mg twice weekly)

Monobactam: Aztreonam is structurally similar to which drug?

CeftaziDIME

Gram (-) spectrum of Aztreonam is similar to which gen of cephalosporin?

3rd

Aztreonam bacterial coverage is limited to?

Aerobic gram (-) rods including P. aeruginosa

AE include skin rashes and elevation of serum aminotransferase during its administration

Aztreonam

Available only in combi with specific penicillin.

B-lactamase inhibitor

B-LI are potent inhibitors of all B-lactamase. True or False

False. Not good against CLASS C B-lactamase

Which class is B-LI most active against?

Class A beta lactamase

3 pairs of penicillin-beta lactamase inhibitor

Amoxicillin-Clavulinic acid Ampicillin-Sulbactam Pipercillin-Tazobactam

Indicated for empirical therapy, mixed aerobic and anaerobic infxn such as intra abdominal infxn

Beta lactamase inhibitors

Carabapenem with longest half life

Ertapenem (4 hours) 1g IV or IM once a day

MOA of Carbapenems

Inhibit cell wall synthesis

Which carbapenem do NOT inhibit pseudomonas, enterococcus, and actinobacter

Ertapenem

Carbapenem with AE as seizure

Imipinem-cilastatin

AE of most carbapenem

Low platelets, fever

Carba used for meningitis

Meropenem

Carba used for intra abdominal

Ertapenem

Carbe used for nocardia

Imipenem

It inactivates imipinem in renal tubules resulting to low urinary conventrations

Dehydropeptidase

An inhibitor of renal dehydropeptidase which is administerd together with imipenem

Cilastatin

``` Indicated for: Mixed aerobic and anaerobic infections Enterobacter infxns ESBL gram (-) Febrile neutropenia ```

Carbapenem

Carbapenems are indicated for febrile neutropenia EXCEPT

Ertapenem

Carbapenem LESS ACTIVE against P. aeruginosa and actinobacter

Ertapenem

Carbapenem with GREATER activity against gram (-) aerobes and LESS activity against garm (+)

Doripenem | Meropenem

Excessive amount of this carbapenem can cause seizure

Imipenem

Inhibits cell wall synthesis by binding firmly to d-Ala-d-Ala terminus of nascent peptidoglycan pentapeptide

Vancomycin

Inhibits the transglycosylase preventing further elongation of peptidoglycan and cross-linking

Vancomycin

Resistance to vancomycin in enterococci is due to replacement of terminal d-Ala by

D-lactate

90% of vancomycin is excreted by

Glomerular filtration

Vancomycin con’c for cellulitis

10-15mcg/ml (mild to moderate infection)

Vancomycin con’c for endocarditis, meningitis, necrotizing pneumonia

15-20 mcg/ml (serious infections)

First line of treatment for severe cases of C. difficile infection or cases that fail to respond to metimazole

Vancomycin

Indicated for bloodstream infxn and endocarditis caused by MRSA

Vancomycin

Vancomycin is used in combination with what drug for Tx of enterococcal ndocarditis with serious penicillin allergy

Gentamycin

Can cause phlebitis at site of injection

Vancomycin

When used with vancomycin, it can increase the risk of oto- and nephrotoxicity

Aminoglycosides

AE of vancomycin: infusion related flushing due to release of histamine

Red man syndrome

Red man syndrome can be prevented by?

1. Prolonging the infusion period to 1-2 hours | 2. Pretreatment with antihistamine (diphenhydramine)

Glycopeptode very similar to vancomycin

Teicoplanin (once daily IV or IM)

Semisynthetic lipoglycopeptide derived from vancomycin

Telavancin

Tx for complicated skin and soft tissue infections and hosp-acquired pneumonia

Telavancin

Monitoring of serum telavancin is required. True or False.

False

Derived from Teicoplanin

Dalbavancin (once weekly IV)

Improved activity agains gram (+) bacte and MRSA and VISA

Dalbavancin

Novel cyclic lipopetide

Daptomycin

Bacterial coverage: Vanco-resistant enterococci and S. aureus

Daptomycin

MOA: bind to cell membrane via calcium dependent insertion of its lipid tail

Daptomycin

Tx for skin and soft tissue infxns, bacteremia, and endocarditis

Daptomycin

What antagonized by pulmonary surfactant and therefor not be used in treating pneumonia

Daptomycin

AE include myopathy and allergic pneumonitis

Daptomycin | Phosphokinase levels should be monitored weekly

Inhibits the addition of phosphoenolpyruvate to UDP-N-acetylglucosamine

Fosfomycin

Tx of uncomplicated lower urinary tract infections in women

Fosfomycin (single 3g dose)

Used topically

Bacitracin

Causes suppression of mixed bacterial flora in surface lesions of skin or mucous membranes

Bacitracin

Inhibits alanine racemase

Cycloserine

Tx for tuberculosis caused by Mycobacterium tuberculosis resistant to 1st line agents

Cycloserine