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ID Pharm > Beta-Lactam Antibiotics > Flashcards

Beta-Lactam Antibiotics Flashcards

1
Q

Beta-lactam MOA

A

Disrupt the synthesis of bacterial cell wall by interfering with the transpeptidase which catalyzes the cross linking process
Bind to PBPs to inhibit transpeptidation = cell wall destroyed and bacterial cell dies
Time-dependent killer: Time the AUC is above the MIC
Bactericidal to growing bacteria

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2
Q

Beta-lactam Resistance

A

Mutation of genes which control production of PBPs - alter the active site and binding affinity for beta-lactam
Synthesize b-lactamase (pencillinase) which breakdowns b-lactam ring inactivating the Abx

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3
Q

b-Lactam compounds

A 
penicillins
cephalosporins
carbapenems
monobactams
b-lactamase inhibitors - combined with PCNs
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4
Q

Natural PCNs

A

Penicillin G - IM

Penicillin VK - PO

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5
Q

Penicillinase-Resistant PCN

A 
Anti-staphylococcal PCNs
Nafcillin
Dicloxacillin
Oxacillin
Cloxacillin
Methicillin
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6
Q

Antipseudomonal PCNS

A

Extended/Broad Spectrum
Piperacillin
Carbenicillin
Ticarcillin

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7
Q

Aminopenicillins

A

Ampicillin

Amoxicillin

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8
Q

Pen G

A

Gm - cocci: strep, staph
Gm + rods: listeria, actinomyces
Gm - cocci: neisseria
Most anerobes: clostridium

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9
Q

Pen G Dosage

A

IM or IV
Pen G cannot be given oral b/c of the acidic conditions
Pen VK is oral - QID

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10
Q

PCN G benzathine and procaine

A

IM: lasts 10-12 days
used for strep or syphilis
IV: for meningitis and endocarditis

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11
Q

PCN Special Populations

A

Pregnancy Cat B
Lactation Safe
Renal dosing: adjust CrCl < 50
Hepatic Dosing: no adjustment required

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12
Q

PCN Adverse Reactions and CI

A

Local: injection site rxn
Significant: CV, CNS, derm, endocrine, metabolic, GI, Hemat, Onco, hypersensitivity, Immuno, renal
CI: hypersensitivity rxns

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13
Q

PCN warnings/precautions

A

Superinfection: super C.Diff
Seizure disorders: high levels with renal impairment = risk of seizure
Pediatrics: neonate decreased clearance of PCN = require frequent dose adjustments

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14
Q

Pen G/Pen VK DI

A

BCG - diminished BCG effect = X
Mtx - increased mtx conc = C
Probenecid - increase PCN conc = C
Na Picosulfate - lower therapeutic effect of Na Pico - D
Tetracycline derivs. - diminish PCN effect - D
Vitamin K antagonists - enhance anticoag effect - monitor INR
OCPs: PCN will decreased OCP efficacy

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15
Q

Pen VK

A

250-500 TID/QID - DOC for strep pharyngitis
>10% have GI issue
< 1% have acute interstitial nephritis, convulsions, hemolytic anemia, + Coomb’s test

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16
Q

Penicillinase-resistant PCNs - antistaphylococcal

A

semisynthetic - used for b-lactamase producing STAPH and PCN susceptible strains of Strep and Pneumococci
Inactive against enterococci and methicillin resist. strains

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17
Q

Penicillinase-resistant PCNs - antistaphylococcal

A

Dicloxacillin, Oxacillin, Methicillin, Nafcillin, Cloxacillin
Not affected by beta-lactamase enzyme

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18
Q

Penicillinase-resistant PCNs Special Populations

A

Preg. Cat B
Lactation - safety unknown
Renal/Hepatic Dosing: no adjustment required - use discretion

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19
Q

Penicillinase-resistant PCNs - Adverse Effects

A

1-10% GI w/ dicloxacillin

<1% = similar to extreme AE of PCN - look at notes

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20
Q

Penicillinase-resistant PCNs - DI

A

Ariprazole - decreased conc of arip - D
Ca Channel Blockers - naf increases CCB metabolism
Estrogens - naf increases metab of estrogen - D
BCG - Abx diminish bcg effect - X
MTX - increased conc of Mtx - C
Probenecid - increase PCN conc - C
Saxagliptin - 3A4 inducers decrease serum conc of sax - C
Vitamin K antag. - dicloxacillin will diminish anticoag effect - C

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21
Q

Aminopenicillins and uses

A

Ampicllin and Amoxicillin - same antimicrobial spectrum as PCN G
Also cover E. coli, Proteus mirabilis, Salmonella, Shigella, H. flu
For otitis, sinusitis, and lower RTI
Amox is better absorbed

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22
Q

Dose in Peds of Aminopenicillins

A

20-40 mg/kg/d divided q8h
Otitis = amox 90mg/kg/day in two doses
3 g/day cut-off in peds

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23
Q

Augmentin

A

amox with clavulanic acid (beta-lactamase inhibitor)

Expands coverage to gram +, gram -, and anerobic organisms

24
Q

Aug. Special Populations

A

Preg Cat B
Lactation = safe
Renal = adust if CrCl < 30
Hepatic = no adjustment nedded

25
Q

Augmentin/Amoxicillin/Ampicillin AE

A

CNS, Derm (SJS), GI (black tongue), Hemat, Hepatic, Renal, anaphylaxis, serum-sickness
Rash in patients with mono

26
Q

Aminopenicillin DI

A

allopurinol = increased allergic or hypersensitivity rxn to amox - C
BCG = dimished BCG effect - X
MTX = increased mtx conc - C
Probenecid = increased conc of PCNs
Na Picosulfate = diminished effect of Na P. - D
Tetracyclines - diminished PCN effect - C
Vitamin K antagonists - enhanced anticoag effect
OCPs - PCN may decrease OCP efficacy

27
Q

Antipseudomonal PCNs Drugs

A

Extended/broad spectrum
Carbenicillin, Piperacillin, Ticarcillin
IV only - standard anti-pseudomonas in hospitals

28
Q

Antipseudomonal PCNs Activity

A

Strep
Enteric Gm - bacilli (E. coli, Klebsiella pneumo, Enterobacter cloacea & aerogenes, Proteus miriabilils)
Pseudomonas
Anaerobes

29
Q

Antipseudomonal PCNs Dosage

A

Ticarcillin IV 3g q4-6h
Peds 150-200 mg/kg/d in 2-3 doses
Adjust for renal disease

30
Q

Timectin

A

Ticarcillin with Clavulunate - broadens spectrum to gram neg aerobes
Actinobacter, Pasteurella, Proteus

31
Q

Piperacillin

Zosyn

A

Pip: more active against Klebsiella, enterococci, and bacteroides = 3-4 g q4-6h - adjust for renal failure
Zosyn = pip with tazobactam = broad spectrum for cellulitis, postpartum endometritis, peritonitis, CA Pneumo, HA pneumo
Dose = 4.5 g q6h - adjust for renal failure

32
Q

Antipseudomonal PCNs SE, AE

A

AE: same as PCNs
Jarisch-Herxheimer Rxn - common in 2nd syphilis
SE: bleeding problems, rash, GI Sx

33
Q

Jarisch-Herxheimer Rxn

A

Common in 2ndary Syphilis
Release of spirochetal lytic products - heat stable proteins and endotoxins
Fever, myalgia, exacerbation of lesions
Occurs w/in 2 hrs of 1st dose
Tx with NSAIDs and corticosteroids
Also in borreliosis, leptospirosis, and brucellosis

34
Q

Beta-Lactamase Inhibitor

A

Clavulanic acid, Sulbactam, Tazobactam

Inhibits bacterial b-lactamases and inhibits aminoglycosides

35
Q

Beta-Lactamase Inhibitor Use

A

in combo with PCN to broaden spectrum of activity
Intra-abdominal/gyn infx
Skin and soft tissue infx
RTI, sinusitis, and lung abscesses

36
Q

Beta-Lactamase Inhibitor Combo’s

A

Augmentin - amox-clavulanic acid
Zosyn - piperacillin-tazobactam
Unasyn - ampicillin-sulbactam
Timectin - ticarcillin-clavulanate

Antipseudomonals - Zosyn and Timectin
Aminoampicillins - Augmentin and Unasyn

37
Q

Interstitial Nephritis

A

AI rxn to PCN-protein complex

38
Q

Cephalosporins

A

6 member ring instead of 5 member ring
2 modifiable side chains = b-lactamase cannot hydrolyze as well
Progression from 1st-3rd gen = increase in gm- coverage and loss in gram + coverage
Well absorbed in GI tract
3-10% cross reactivity with PCNs

39
Q

Cephalosporin Generation Trends

A

1st: Gram + = cephalexin and cefazolin
2nd: decreasing Gram + and increasing gram - = ceftin for otitis, sinusitis, and RTI
3rd: gram - with some Gm +
4th: Gram + and Gm -

40
Q

3rd and 4th generation cephalosporins

A

DOC for Gm - meningitis
Good alternative to aminoglycosides
Watch for resistance - combo therapy best w/ pseudomonas
Ceftriaxone DOC for gonorrhea
Ceftazidime effective in pseudomonas meningitis

41
Q

1st Gen. Cephalosporins

A

cephalexin (Keflex), cefazolin (Ancef), cefadroxil
Good Gm + coverage - strep and staph
Some Gm -
Good for anaerobic cocci - peptococcus, peptostreptococcus

42
Q

1st Gen Cephs Dosage, Use, SE

A

Cephalexin: 250-500 mg QID - uncomp. cellulitis
Cefazolin: 1-2 gm IV - complicated cellulitits or surgical prophylaxis
SE: GI, allergy, C. diff

43
Q

2nd Gen Cephalosporins

A

cefaclor (Ceclor) PO 250-500 mg 2-4/day
cefuroxime (Ceftin) PO 250-500 mg bid; IV 1-1.5 g q8h
cefoxitin (Mefoxin) IV 1-2 g q6-8h
cefotetan (Cefotan) IV 1-2 g q12h

44
Q

2nd Gen Ceph Activity

A

Gm + cocci
Gm - for Klebsiella, H. influenzae
No pseudomonas coverage
Cefaclor susceptible to b-lactamase hydrolysis

45
Q

2nd Gen Ceph uses

A

Cefuroxime - sinusitis, otitis, RTI, CA pneumo because H. flu, Klebsiella, and penicillin-resistant pneumo coverage
Cefoxitin - anaerobic activity, GI surgery prophylaxis, peritonitis and diverticulitis b/c Gm - rods and bacteroides coverage

46
Q

3rd Gen Cephalosporins

A

Cefotaxime: IV 1-2g q6-12h
Ceftaidime: IV 1-2g q8-12h
Ceftriaxone: 1-2g q 24h - IV or IM

47
Q

3rd Gen Cephalosporins Activity

A

Gm - against meningococcus, citrobacter, b-lactamase resistant H. flu and Neisseria
Ceftazidime good for pseudomonas aeruginosa
Cefotaxime and ceftriaxone cross BBB

48
Q

3rd Gen Cephalosporins Use and SE

A

ceftriaxone and cefotaxime treat meningitis
Empirical therapy b/c cover PCN-resistant pneumococci
Ceftriaxone: treats gonorrhea and Lyme
SE: rash, NV, elevated LFTs, eosinophilia, HA

49
Q

4th Gen Cephalosporins and Activity

A

Cefepime (Maxipime) - IV 0.5-2g q12h
Peds: 75-120mg/kg/d divided in 2-3 days
Gm + and Gm -
Pseudomans, Staph aureus, Strep pneumo, H. flu, Neisseria

50
Q

4th Gen Cephalosporins Use and SE

A

Crosses BBB - can treat meningitis, sepsis etc.
Combo with aminoglycoside when treating pseudomonas
SE: NVD, HA, rash

51
Q

Carbapenems - General

A

Treat MDR bacteria
Hospitalized patients
More resistant to resistance than other b-lactams
Some klebsiella and enterobacteria resistance

52
Q

Carbapenems Drugs

A

Imipenem/cilastatin - IV 250-500 mg q6-8h, better coverage than meropenem
Meropenem - IV 1-2 q8h

53
Q

Carbapenems Activity

A

Very resistant to b-lactamase cleavage
Gm+ coverage - enterococcus faecalis & listeria
G - coverage - H. flu, N. gonorrhea, enterobacter, pseudomonas
Anaerobes (bacteroides)

54
Q

Carbapenems Uses and SE

A

meningitis, intra-abdominal infx, resistant UTIs
Pseudomonas w/ or w/o aminoglycoside for neutropenic patient
SE: NVD, rash, infusion site rxn
Imipenem: renal failure + seizures

55
Q

Monobactams

A 
b-lactam ring is alone, not fused
Gm - only (Neisseria, Pseudomonas) 
aztreonam (Azactam)
AE: rash, abnormal LFTs
No cross reactivity
Can trigger seizures at high doses

ID Pharm (6 decks)

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