Antibacterial Agents Flashcards

0
Q

Penicillins pharmacokinetics

A

renal excretion

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1
Q

Penicillins MOA

A

Cell wall synthesis stage 3, bactericidal

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2
Q

Penicillin adverse reactions

A

anaphylaxis (type I, rare), rash (common), convulsions (very high doses)

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3
Q

Penicillin G and V

A
Pen G: IM/IV (poor oral)
Pen V: acid stable, good oral
G+ cocci: All strep, staph, enterococcus
G- cocci: Neisseria, M. Cattarhalsis
Anaerobes: C. perfringens
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4
Q

Penicilinase-resistant: oxacillin, dicloxacillin, methicillin, Nafcillin)

A

good oral (not methicillin or Nafcillin)
G + cocci: All strep, staph, MSSA (narrow spec B lactamase)
good with skin infections (not MRSA)

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5
Q

Extended spectrum (amoxicillin/ampicillin)

A
good oral, less potent than Pen V/G
G+ cocci: All strep, Enteroccocus
G- cocci: E Coli, H. Flu, Proteus
Anaerobes: C. Perfringes
Diarrhea (less with amoxicillin) and Superinfection CDAD
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6
Q

Antipseudomonal (piperacillin, ticarcillin + B Lactamase inhibitor)

A

IV only
G+ cocci: All strep, MSSA, enterococcus
G- cocci: H. Flu, E. Coli, E. Coli (TEM-1), E. Coli (ESBL)
G- bacilli: Klebsiella, pseudomonas
Anaerobes: C. perfringes, bacteriodes fragiles

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7
Q

Name of B-lactamase inhibitors

A

clavulonic acid, tazobactam, piperacillin

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8
Q

Cephalosporins MOA and spectrum/uses

A

Cell wall synthesis inhibition (stage 3) bactericidal

extended spectrum NOT susceptible to penicillinases (NSBL)

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9
Q

Cephalosporins Pharmacokinetics

A

renal excretion (almost all)

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10
Q

cephalosporins adverse reactions

A

allergy (less severe than penicillins)

some cross reactivity in approx 1-5%

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11
Q

1st generation cephalosporins

A

cephalexin, cephradine: good oral
cefazolin: IV/IM only
adverse reactions: diarrhea

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12
Q

2nd generation cephalosporins

A

cefaclor, cefuroxime: good oral
cefoxitin: IV/IM only
adverse reactions: DDI- enhancement of warfarin anticoagulant & superinfections CDAD possible

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13
Q

3rd generation cephalosporins

A

Cefdinir: good oral
cefotaxime, Ceftriaxone: good CNS penetration
Cefepime: 4th generation!
Adverse Reaction: Superinfection CDAD possible

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14
Q

Vancomycin

A

C.W. synthesis inhibition (stage 2) bactericidal
poor oral absorption, renal excretion
Adverse Reactions: infusion related: chills/fever/rash, ototoxicity, renal toxicity, ROUTINE MONITORING OF Cp LEVELS

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15
Q

Carbapenems

A

Imipenem, Meropenem, Eratenem
C.W. synthesis inhib, (stage 3) bactericidal
IV, renal excretion, once daily with Ertapenem
Adverse reactions: nausea/vomiting, diarrhea, seizures possible with high doses

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16
Q

Macrolides MOA

A

Protein synthesis inhibition (50S)

bacteriostatic

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17
Q

Macrolides Pharmacokinetics

A
good oral (also IV)
concentrates in lungs
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18
Q

Macrolides adverse reactions

A
GI disturbances (n/v, diarrhea)
DDI: due to inhibition of P450 metabolism (EXCEPT AZI)
19
Q

Macrolides- Erythromycin

A

QID- liver metabolism

20
Q

Macrolides- Azithromycin

A

QD-Biliary

21
Q

Macrolides- Clarithromycin

A

BID- metabolism to active metabolite

22
Q

Tetracyclines MOA

A

Protein synthesis inhibition (30S)

bacteriostatic

23
Q

Tetracyclines Adverse Reactions

A

Abnormal bone/tooth development

avoid in pregnancy and in less than 8 yo

24
Q

Tetracycline

A

po, renal excretion

n/v/diarrhea, fungal superinfection

25
Q

Doxycycline

A

po, biliary (non-renal excretion)

DD interactions with metal cations (antacids/dairy/iron) in stomach

26
Q

Clindamycin

A
Protein synthesis inhibition (50S), bacteriostatic
good po (also IV), penetrates into bone, hepatobiliary elimination
Adverse reactions: severe diarrhea, pseuomembranous colitis
27
Q

Aminoglycoside MOA

A

Protein synthesis inhibition (30S)

bactericidal

28
Q

Aminglycoside pharmacokinetics

A

poor oral absorption (IV/IM)
distributed in extracellular fluid
accumulates in kidney/inner ear
renal excretion

29
Q

Aminoglycoside Adverse Reactions

A

vestibular and auditory toxicity
nephrotoxicity
ROUTINE MONITORING OF Cp LEVELS

30
Q

Aminoglycoside AB names

A

tobramycin
gentamicin
neomycin
streptomycin

31
Q

Chloramphenicol MOA, Pharmaco, and Adverse Reactions

A

MOA: protein synthesis inhibitor (50S), bacteriostatic
Pharm: good po (also IV), distrubtes to CNS/CSF, metabolized by gluconuridation
Adv. Reac.: bone marrow toxicity, gray baby syndrome, GI upset, toxicity limits use in US

32
Q

Oxazolidinones MOA, Pharm, Adv Reac

A

Linezolid
MOA: protein synthesis inhibition (50S), bacteriostatic (-cidal for strep)
Pharm: excellent po, also used IV, eliminated by non-enzymatic oxidation (50%) plus renal (30%)
Adv Reac: well tolerated (minor: GI, HA, rash), thrombocytopenia (2.4%), inhibit MAO –> serotonin syndrome

33
Q

Streptogamins MOA, Pharm, Adv Reac

A

Dalfopristin, Quinupristin
MOA: protein synth inhibition (50S), synergistic action results in -cidal action against many bacteria
Pharm: IV only, primarily biliary excretion (80%)
Adv Reac: infusion-related (pain, phlebitis), INHIBITS CYP3A4, significant DDI possible

34
Q

Fluoroquinolones MOA

A

inhibition of DNA gyrase

bactericidal

35
Q

Fluorquinolones Pharmacokinetics

A

good oral (also IV)

36
Q

Fluoroquinolones Adv Reactions

A

well tolerated, some GI upset
superinfections possible (CDAD)
DDI with theophylline (decreased metabolism) and antacids (decrease FQ absorption)
Rare: CNS disorders, increased QT interval
NOT 1st choice in children (potential arthralgias)

37
Q

Ciprofloxacin

A

type of fluoroquinolone
2nd generation
primarily renal excretion

38
Q

Levofloxacin

A

type of fluoroquinolone
3rd generation
respiratory FQ
primarily renal excretion

39
Q

Minofloxacin

A

type of fluoroquinolone
4th generation
respiratory FQ
primarily hepatic excretion (20% renal)

40
Q

Nitrofurantoin MOA, Pharm, Adverse Reactions

A

MOA: reduced in cell to intermediates that damage bacteria DNA
bacterical
Pharm: rapid, complete GI absorption but rapid excretion via kidneys, thus acts as urinary antiseptic
Adv Reactions: GI side effects, macrocrystalline forms better tolerated

41
Q

Metronidazole MOA, Pharm, Adv Reactions

A

MOA: reduced intracellularly to active form, intereference with DNA function
bactericidal
Pharm: good oral bioavailability, hepatic metabolism
Adv Reac: nausea, headache, GI distress
ANTABUSE- like rxn, occasional candidal superinfections

42
Q

sulfonamides AB names

A

sulfamethoxazole

trimethoprim (not sulfa)

43
Q

sulfonamides MOA

A

inhibition of folate metabolism
interference with DNA synthesis
bacteriostatic if either used alone, bactericidal if combo (SMX/TMP)

44
Q

sulfonamides Pharmacokinetics

A
good po (also IV)
hepatic/renal elimination
45
Q

sulfonamides adverse reactions

A

hypersensitivity skin reactions
kernicterus in neonates
renal crystalluria (rarely) via decreased water solubility of metabolites

46
Q

Non-renally elminated drugs

A

Doxycycline
Quinolones: cipro renally but non-substrate inhib of P450 (caffeine-theophylline)
Clindamycine
Rifampin: inducer of p450, potential for hepatotoxicity
Isoniazid: genetic polymorphism of N-acetyl transferase metab, potential for hepatotoxicity
Metronidazole: DDI iwth alcohol due to inhib of aldehyde metab
Erythromycine-like: DDI due to inhib of P450 (Clar-Ery, NOT Azi)
Sulfonamides: N-acetylated to a more lipid-soluble metabolite–> concern for renal crystalluria