Antibiotic Classes and Drugs Flashcards

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1
Q

Antibiotic Resistance Patterns

A

Staphylococcus - B-lactamases - affects all pcn

MRSA - Alter PBP - affects pcn cephalosporins, some fluoroquinolones

Streptococcus - Alter binding sites - pcn, macrolides

Enterococcus - alterations to target site - vancomycin

Pseudomonas - reduced permeability - pcn, cephalosporins, carbapenems, aminoglycosides, fluoroquinolones

Pseudomonas - B-Lactamase production - pcn

Enterobacteriaceae - b-lactamase production - pcn

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2
Q

Cell Wall Synthesis Inhibitors

A

Includes B-Lactams (pcn, cephalosporins, Carbapenems), Glypcopeptides (Vancomycin), Lipopeptides (Daptomycin)

All function similarly by interfering with or binding to the protein that synthesizes the cell wall.

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3
Q

Penicillins (Cell Wall Synthesis Inhibitors)

A

Natural Penicillins - pcn v (oral), pcn G (IV)

Aminopenicillins - Amoxicillin oral, ampicillin IV

Penicillinase-resistant - Oxacillin, nafcillin

Extended-spectrum/antipsuedomonal - Piperacillin

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4
Q

Natural PCN (Cell Wall Synthesis Inhibitors)

A

PCN VK and G

These cover gm + streptococcus (not pneumoniae) and enterococcus

gm - Neisseria, Treponema pallidum (syphilis)

Only covers mouth flora anaerobes.

Commonly used for pharyngitis, erysipelas, and syphilis (pcnG)

Does not cover Staphylococci due to penicillinase.

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5
Q

Amino-penicillins

A

Ampicillin and Amoxicillin

gm + streptococcus, Enterococcus, Listeria monocytogenes

gm - proteus mirabilis, salmonella, Shigella, some e coli, and some H. influenzae

Only mouth anaerobes.

Commonly used for
URI
H. pylori w/ clarithromycin and PPI
Enterococcal infections
Skin infections
UTIs
CAPs
Lymphadenitis

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6
Q

Penicillinase Resistant Penicillins

A

Dicloxacillin, Nafcillin IV, oxacillin IV

Only cover Gm + Staph (not MRSA), Strep spp

Commonly used against:
B-lactamase producing staph
Cellulitis
Diabetic foot infections
Septic arthritis
Endocarditis

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7
Q

Extended-spectrum PCNs

Good for B. Fragilis

A

Pipercillin/tazobactam

GM+ staph, strep, enterococci (not MRSA)

GM- Enterobacteriaceae (E. Coli, Proteus), PA, H. Influenzae

Good for B. Fragilis (anaerobe)

Commonly used for
Nosocomial Pnuemonia
Intra-abd. infections
gynecological infections
SSTI

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8
Q

Two major forms of PCN resistance

A

Antibiotic destroying enzymes - Penicillinase, B-lactamases, Extended-spectrum B-lactamase (ESBL)

Altered target site - PCN cannot bind to the PBP as seen in MRSA

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9
Q

B-Lactamase Inhibitors

A

Can defeat some beta-lactamase producing organisms

Amoxicillin + clavulanate, Piperacillin + tazobactam, Ampicillin+Sulbactam

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10
Q

ABX Toxic Rxns and immune mediated ADRs

A

Toxic rxns:
disruption of host microbiome may lead to nausea, vomiting, diarrhea
overgrowth of toxic organisms (C. diff)

Antibody mediated:

Type 1 immediate hypersensitivity (IgE-mediated) - leads to hives, angioedema, bronchospasm, CV collapse, anaphylaxis

Type II -hemolytic anemia, thrombocytopenia, leukocytopenia

Type III immune-complex Reaction (4-10 days to develop) - Vasculitis, serum sickness, Arthus Reaction

T-Cell Mediated:
DRESS (2-8wk s/p)
Liver injury, interstitial nephritis
SJS/TEN

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11
Q

PCN allergies

A

10% of Pt report a PNC allergy, but that doesnt preclude the use of the drugs, unless reaction was anaphylaxis.

Can do a skin or oral challenge

prescribe cephalosporins - not if it was an anaphylactic allergy!

PRescribe a non b-lactam; check allergies

Perform PCN desensitization - very labor intensive and req the ICU to monitor

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12
Q

Cephalosporins (cell wall inhibitors)

A

Different generations have different spectrums of activity and NONE COVER ENTEROCOCCUS

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13
Q

Cephalosporin Generations

A

5 Generations:

1st - cephalexin Oral, Ceazolin IV

2nd -Cefaclor oral, Cefotaxime IV

3rd - Cefpodoxime oral, Ceftriaxone IV

4th - Cefepime IV

5th - Ceftaroline IV

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14
Q

Cephalosporin Properties

A

Similar MOA to PCN -both bind PBP, destroy the cells wall. and are time-dependent killers

Similar Chemical structure - Ampicillin, amoxicillin, cefaclor, cephalexin, cefadroxil; may increase risk for cross-reactivity b/w these agents

Both are considered first-line for the majority of infections - effective and well-tolerated oral/IV, relatively inexpensive.

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15
Q

First Gen Cephalosporins

A

Cefadroxil oral, Cephalexin oral, Cefazolin IV

SPEcK Coverage

GM+ Staph and strep

GM- Proteus, E. coli, Klebsiella pneumoniae

Commonly used for:
UTI
Pharyngitis
Mild SSTI
URI/LRI

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16
Q

2nd Gen Cephalosporins

Cefuroxime - lyme dz
cefoxitin and cefotetan -B. fragilis

A

Cefaclor oral, Cefprozil oral, Cefuroxime oral, Cefotetan IV, Cefoxitin IV

HNMSPEcK coverage

GM+Staph and strep

GM- hemophilus influenzae, N. gonorrhea, Moraxella catarrhalis, Proteus mirabilis, E. Coli, Klebsiella pneumoniae

Commonly used for:
Sinusitis, pharyngitis, otitis media, LRIs

Cefuroxime - lyme dz
cefoxitin and cefotetan -B. fragilis

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17
Q

3rd Gen Cephalosporins

ceftazidime Covers PA

A

Cefidinir oral, cefditoren oral, cefixime oral. cefpodoxime oral, cefotaxime IV, ceftazidime IV, Ceftizoxime IV, Ceftriaxone IV

GM+ Strep. Pneumoniae,

Gram- Enterobacteriaceae, H. influenzae, Moraxella catarhalis

Commonly used for:
CAP, Otitis media, URIs,
Meningitis, febrile neutropenia

ceftazidime Covers PA

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18
Q

Fourth Generation Cephalosporins

A

Cefepime IV

GM+ Strep and Staph

GM- Enterobacteriaceae, H. Influenzae, moraxella, PA

Commonly used for:
Meningitis
febrile neutropenia, pneumonia, nosocomial infections, pyelonephritis.

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19
Q

5th Generation Cephalosporins

A

Ceftazidime+avibactam - for complicated intra-abd infections with metronidazole, complicated UTIs, good against carbapenems resistant Enterobacteriaceae with ESBL

Ceftolozane+tazobactam - Same indications as above, active against MDR PA; less affected by efflux pumps

Ceftaroline - CAP, SSTI, MRSA/VRSA; Coverage similar to ceftriaxone

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19
Q

Cephalosporins cross reactivity

A

2% risk, first generation has the most risk.

Cross sensitivity with penicillin is about 2%

Pt with a positive PCN seem to be at a higher risk.

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20
Q

Monobactams

A

Aztreonam

only one in the USA, Gram - coverage includes PA,

No gram +, atypical, or anaerobic coverage

resistant to many B-lactamases produced by gram - bacteria.

No cross sensitivity with PCN or Cephalosporins; but possible risk with ceftazidime due to similar R1 side Chain

IV or IM Administrations, not available PO

Dose must be adjusted for decreased renal function

Low incidence of adverse effects such as diarrhea.

21
Q

Carbapenems - First line against ESBL!

(E. coli/K. pneumoniae)

A

All IV: Ertapenem, Imipenem/cilistatin, Meropenem, Doripenem

Reserved for srs infections due to ESBLs such as E. coli/K. pneumoniae

Covers Strep, MSSA, Enterococcus, Pseudomonas.

Ertapenem does not cover Pseudomonas or enterococci.

ADRs: GI intolerance, rash, seizures

Special considerations:
Imipenem/cilastatin may decrease seizure threshold.
Carbapenems may increase valproic acid clearance - sup-therapuetic levels.
Doripenem associated with worse survival than imipenem for pneumonia.

22
Q

Newer Carbapenems

A

Tx CRE

Meropenem+vaborbactam - works for UTIs, against KP carbanpenemase

Imipenem.cilistatin+relebactam - UTIS, IAbd; against KP and PA

23
Q

Glycopeptides -Vancomycin

A

Inhibit the cell wall through a slightly different method to PCNs/etc

Commonly used for MRSA, Enterococcus, Streptococcus, C. Diff (enteral or rectal)

Well tolerated, but can be related to nephrotoxicity, ototoxicicty, neutropenia, thrombocytopenia.

Therapeutic drug monitoring required to ensure adequate dosing.

May need higher doses for pneumonia, meningitis, endocarditis.

24
Q

VIR

A

Vancomycin-infusion reaction

Infusion related rxn w/ erythematous or urticarial rxn, flushing, tachycardia, and hypotension.

From the release of histamine and is not an allergic reactions.

Management:
Stop infusion and wait for SE to subside.
Restart are 1gm/hr and adjust rate as tolerated.
May administer diphenhydramine prior to infusion

25
Q

Telavancin -

A

A lipoglycopeptide, similar to vanco, but only has a once daily dosing.

BBW for pregnancy.

Good for complicated SSTI, and nosocomial pneumonia

IV only; adjust for renal dysfuntion

More frequent ADR to Vanco; Nausea and taste changes.

Redman syndrome; infuse overs 60 min, can cause nephrotoxicity, GI upset, metallic taste.

26
Q

Ortavancin and Dalbavancin

A

2nd gen lipoglycopeptides, IV only
Approved for Tx of SSTI

Oritavancin is a one time dose for SSTI

Dalbavancin - ones weekly dosing

27
Q

Daptomycin - the Lipopeptide Antibiotic

A

Works by inserting itself into the Cytoplasmic membrane leading to ION leakage and cell death!

Coverage is similar to vancomycin, but covers VRE as well

Use for SSTI, Bacteremia, endocarditis.

Cannot be used in meningitis as it does not distribute into the CNS
Cannot be used in pneumonia as surfactant destroys it.

Adjust for Renal Dysfunction.

ADR:
Common injection site reaction, fever, chills, D/N/V
Srs rhabdomyolysis. D/C immediately if muscle pain/cramps + elevation of CPK >5 times upper limit of normal.

28
Q

Protein Synthesis inhibitors

A

Includes Tetracyclines, Linezolid, Macrolides, and Aminoglycosides.

29
Q

Tetracyclines (protein synthesis inhibitors) - General stuff

A

Prevents the binding of tRNA to MRNA-ribosome complex, thus inhibiting protein synthesis

Common ADRs include photosensitivity, sunburn, N/V

Can cause
tooth discoloration (enamel agenesis),
Abn bone growth (do not use in pregnancy or in children <8y/o)
Vestibular toxicity with minocycline - dizziness, ataxia, n/v which resolves 24-48 hours after d/c

Must monitor for hepatic toxicity with high doses or long-term use.

30
Q

Tetracyclines (protein synthesis inhibitors) - Usage

A

Tetracycline PO, doxycycline IV/PO, minocycline PO

GM+ S. pneumoniae, S. Pyogenes, CA -MRSA

GM- E. Coli, Klebsiella, H. influenzae

Atypical - Chlaymidia pneumoniae, Mycopalsma pneumoniae, Legionella pneumoniae, chlamydia, trachomatis, Borrelia burgdorferi (lyme)

Commonly used for:
Respiratory infections
CA -MRSA, SSTI, acne

Doxycucline - anthrax, chlamydia, lyme, CA-MRSA

Want to separate from foods containing Al, Mg, Ca, Fe by 1-2 hours

Mino can be taken with or without food
Tertra should be taken on an empty stomach
Doxycycline - must be taken with food due to GI intolerance, but decreases absorption by 20%

31
Q

Tigecycline

A

IV derivative of minocycline

good for MDR GNR (not PA), B fragilis, Strep/Staph (MRSA too!) Enterococcus (some VRE) and Aypicals

Commonly used in SSTI, I-ABd infections, CAPs

ADR n/v anemia

BBW risk of death; only use when all other therapies are unsuitable

32
Q

Omadacycline

A

Approved for CAP, SSTI with no known cases of c diff associated diarrhea in clinical trials

No known CYP450 drug interactions

IV and PO

33
Q

Eravacycline

A

Approved for complicated I-Abd infections

less incidence of n/v than tigecycline

Worse than levofloxacin for UTIs

IV only

34
Q

Macrolide - protein synthesis inhibitor - general stuff

A

Important to be aware of QTc prolongation CYP450 drug interactions

inhibits translocation of step of protein synthesis

CYP450 interactions: inhibits cyp3A4: erythromycin> clarithromycin>azithromycin

Some GI intolerance w/ n/v/d abd pain (25% with erythromycin)

CV: QT prolongation risk (same order as above)

Food interactions:

Clarithromycin with or w/o food

Azithromycin ER suspension and erythromycin: 1 hour before or 2 hours after a meal

Fidaxomicin: with or w/o food

34
Q

Macrolide - protein synthesis inhibitor - general stuff

A

Important to be aware of QTc prolongation CYP450 drug interactions

inhibits translocation of step of protein synthesis

CYP450 interactions: inhibits cyp3A4: erythromycin> clarithromycin>azithromycin

Some GI intolerance w/ n/v/d abd pain (25% with erythromycin)

CV: QT prolongation risk (same order as above)

Food interactions:

Clarithromycin with or w/o food

Azithromycin ER suspension and erythromycin: 1 hour before or 2 hours after a meal

Fidaxomicin: with or w/o food

35
Q

Macrolides - protein synthesis inhibitors - Uses

A

erythromycin IV/PO, Clarithromycin PO, Azithromycin IV/PO

Gm+ Strep

Gm_ H. influenzae, N. gonorrhea

Atypical - Chlaymidia pneumoniae, Mycopalsma pneumoniae, Legionella pneumoniae, chlamydia, trachomatis

Common uses:
Alternative for PCN allergic Pts
CAPs
Pharyngitis
SSTI
Otitis media

Azithromycin - urethritis, MAC, COPD exacerbation prevention (anti inflammatory)

Erythromycin Tx post op ileus and improves GI Motility.

Fidaxomicin PO is for C. Diff

36
Q

Clindamycin - Protein Synthesis Inhibitor - general stuff

A

Lincosamide - associated with C. Diff colitis

ADRs:
N/D, dyspepsia
less commonly -hepatotoxicity, skin rashes
Higher incidence of C. Diff associated D vs other ABX

Food Considerations:
Take with food due to GI Upset.
Full glass of water to decrease Esophageal ulceration.

37
Q

Clindamycin - Protein Synthesis Inhibitor - Usages

A

Clindamycin IV/PO

Gm+ SA (MSSA/CA-MRASA) Strep, Peptostreptococcus.

Anaerobes Clostridium (not diff), bacteroides, Prevotella, Fusobacterium.

Common uses:
SSTI (CA-MRSA), Strept, Anaerobic infections, aspiration pneumonia.

Alternative Pcn allergic Patients with otitis media, dental prophylaxis

Can be used for CA-MRSA, but resistances can develop rapidly.

38
Q

Oxazolidinediones Protein Synthesis Inhibitor - General Stuff

A

Linezolid and tedizolid; good for MRSA IV or PO

ADRs with prolonged Tx >2 weeks:
myelosuppression –> thrombocytopenia
peripheral or optic neuropathy (which can be partially reversible)
less risk with tedizolid v linezolid

Increased risk of serotonin syndrome:
hyper-reflexia, hallucinations, myoclonus, tachycardia, shivering
use with caution with Pts on SSRIs, TCAs, or MAOIs
avoid tyramine-rich foods such as wine, cheese, processed meat
less risk with tedizolid v linezolid

Increased risk of hypertension

Oral formulation shows 100% bioavailability

39
Q

Oxazolidinediones Protein Synthesis Inhibitor - Linezolid

A

IV or PO

Gm +: SA (all) Strep, enterococcus faecium

Used for resistant infections such as MRSA or Vancomycin resistant E. Faecium

Used for SSTI, Bone and joint infections, bacteremia, Pneumonia

BID dosing.

40
Q

Oxazolidinediones Protein Synthesis Inhibitor - Tedizolid

A

Approved For Acute bacterial skin and skin structure infections only. Once daily dosing.

IV or PO

Gm +: SA (all) Strep, enterococcus faecium

Used for resistant infections such as MRSA or Vancomycin resistant E. Faecium

41
Q

Aminoglycosides Protein Synthesis Inhibitor - General stuff

A

Use high-dose extended interval dosing if the Pt has good renal function.

Have risk of ototoxicity and nephrotoxicity -
usually when >5 day durations.
More common in the elderly or in patients with impaired renal function.
Vestibular and auditory toxicity is irreversible

Traditional Dosing:
Gentamicin/Tobramycin (2mg/kg q8): Goal is to peak at 6-10mg/dl, trough <2mg/dl
Amikacin(5mg/kg q8): goal is to peak at 25-30mg/dl, trough undetectable

High Dosing, extended interval (5-7mg/kg q24)
Considered more effective and less likely to induce resistance and has a lower risk of nephrotoxicity.
-

42
Q

Aminoglycosides Protein Synthesis Inhibitor - Uses

A

Genamicin IV, Tobramycin IV, Amikacin IV

Gm+ synergy against SA, Strep, Enterococcus.

Gm- Enteric GNR, Pseudomonas

Rarely used alon, even for Gram (-) infections

Synergy with cell-wall active agents against gram + organisms as in endocarditis.

UTI, Pneumonia, Meningitis

43
Q

NA synthesis Inhibitors

A

Include Sulfonamides, Fluoroquinolones, Metronidazole

44
Q

Sulfonamides -NA synthesis Inhibitors - General Stuff

A

Bactrim has retained excellent activity against most pathogens, including CA-MRSA

Considered bacteriostatic; analogues of PABA

Sulfa allergy to non-sulfonamide drugs has minimal cross reactivity

Increases serum creatine when initiating; thus nephrotoxicity can occur

Dosed on trimethoprim component, and adjusted for renal function

N/V/D, photosensitivity, rash

SJS/TENS
Blood dyscrasias, aplastic Anemia, Granulocytopenia, thrombocytopenia, hemolytic anemia (in Pt with g6pd deficiency)

45
Q

Sulfonamides -NA synthesis Inhibitors - Uses

A

Bacrtim IV/PO, Sulfisoxazole, Sulfadiazine, Sulfasalazine

Gm+ Staph, S. pneumoniae, Anthrax, Clostridium tetani

Gm- E. colio, Proteus, H. influenzae

Atypicals - Chlamydia trachomatis

Common uses:
UTI
toxoplasmosis (combo with pyrimethamine.

Considered 1st line for CA-MRSA, PJP Tx and prophylaxis, and URI

46
Q

Fluoroquinolones - DNA synthesis inhibitors - general

A

Increased use of these has been associated with MRSA

Inhibit DNA gyrase and topoisomerase, preventing the uncoiling and De-catenation of copied DNA from its parent

Absortion is reduced when administered concomitantly with divalent or trivalent cations (Mg, Ca, Al, Fe, Zinc)

Avoid use with medications that prolong QT interval (cipro is least likely to cause issues, moxifloaxacin is the most likely)

GI intolerance, h/a, rash, photosensitivity, hypo/hyperglycemia

BBW = tendonitis or tendon rupture

47
Q

Fluoroquinolones - DNA synthesis inhibitors - Cirprofloxacin, ofloxacin, norfloxacin

A

Cirprofloxacin, ofloxacin, norfloxacin - 2nd gen

Gm- Enterobacteriaceae, H. influenzae, M. catarrhalis, Neisseria, Pseudomonas (cipro only)

Cipro and ofloxacin cover atypicals

Common Uses:
Norfloxacin is for uncomplicated UTIs

Cipro and ofloxacin - Complicated and uncomplicated UTIs, Gastroenteritis, prostatitis, STDs, skin infections

Cirpo - anthrax

Overall Gm- activity Cipro> levo=gati=moxi>sparfloxacin

48
Q

Fluoroquinolones - DNA synthesis inhibitors - Levo, Moxi, Gatifloxacin

A

Levo, Moxi, Gatifloxacin(ophthalmic only) - 3rd and 4th gen

Gm+ S. pnuemoniae

Gm- Enterobacteriaceae, H. influenzae, M. catarrhalis, Neisseria, Pseudomonas (levo)

Atypicals

Similar indications to 2nd gen plus CAP and URIs

49
Q

Fluoroquinolones - DNA synthesis inhibitors - Delafloxacin

A

Delafloxacin - 5th gen

Similar to levo but also covers MRSA

SSTI infections only

50
Q

Metronidazole - the basics

A

Anaerobic workhorse - Steals Ions to become a toxic free radical that destroys DNA

ADR - Peripheral neuropathy, GI intolerance, Dry mouth, metallic taste.

DO NOT drink alcohol during and 48 hrs s/p d/c - gives hangover reactions, with flushing, tachycardia, n/v, sob