Antibiotic Classes and Drugs Flashcards

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

B-Lactamase Inhibitors

A

Can defeat some beta-lactamase producing organisms

Amoxicillin + clavulanate, Piperacillin + tazobactam, Ampicillin+Sulbactam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Cephalosporins (cell wall inhibitors)

A

Different generations have different spectrums of activity and NONE COVER ENTEROCOCCUS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
VIR
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
Telavancin -
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
Ortavancin and Dalbavancin
2nd gen lipoglycopeptides, IV only Approved for Tx of SSTI Oritavancin is a one time dose for SSTI Dalbavancin - ones weekly dosing
27
Daptomycin - the Lipopeptide Antibiotic
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
Protein Synthesis inhibitors
Includes Tetracyclines, Linezolid, Macrolides, and Aminoglycosides.
29
Tetracyclines (protein synthesis inhibitors) - General stuff
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
Tetracyclines (protein synthesis inhibitors) - Usage
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
Tigecycline
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
Omadacycline
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
Eravacycline
Approved for complicated I-Abd infections less incidence of n/v than tigecycline Worse than levofloxacin for UTIs IV only
34
Macrolide - protein synthesis inhibitor - general stuff
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
Macrolide - protein synthesis inhibitor - general stuff
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
Macrolides - protein synthesis inhibitors - Uses
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
Clindamycin - Protein Synthesis Inhibitor - general stuff
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
Clindamycin - Protein Synthesis Inhibitor - Usages
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
Oxazolidinediones Protein Synthesis Inhibitor - General Stuff
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
Oxazolidinediones Protein Synthesis Inhibitor - Linezolid
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
Oxazolidinediones Protein Synthesis Inhibitor - Tedizolid
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
Aminoglycosides Protein Synthesis Inhibitor - General stuff
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
Aminoglycosides Protein Synthesis Inhibitor - Uses
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
NA synthesis Inhibitors
Include Sulfonamides, Fluoroquinolones, Metronidazole
44
Sulfonamides -NA synthesis Inhibitors - General Stuff
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
Sulfonamides -NA synthesis Inhibitors - Uses
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
Fluoroquinolones - DNA synthesis inhibitors - general
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
Fluoroquinolones - DNA synthesis inhibitors - Cirprofloxacin, ofloxacin, norfloxacin
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
Fluoroquinolones - DNA synthesis inhibitors - Levo, Moxi, Gatifloxacin
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
Fluoroquinolones - DNA synthesis inhibitors - Delafloxacin
Delafloxacin - 5th gen Similar to levo but also covers MRSA SSTI infections only
50
Metronidazole - the basics
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