Antibiotics Flashcards

1
Q

Beta-Lactams

A

Inhibits cell wall CROSSLINKING (synthesis): Penicillins, Cephalosporins, Monobactams, Carbapenems

DOES THIS BY IRREVERSIBLY BINDING TRANSPEPIDASES (Penicillin Binding Proteins) PREVENTING CROSSLINKING

Restance occurs via beta-lactamases (degrades lactams) and by mutating Penicllin binding proteins so drugs no longer have affinity to PCPs

Vanco (glycopeptide) actually binds the D-ALA D-ALA parts of the cell.

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2
Q

Penicillin, Methicillin, Oxacillin

When do you use Naficillin?

A

D-ala-D-ala peptidoglycan side chain, inhibiting transpeptidase from forming crosslinks

Resistance develops vai lactamase expression. Counter with lactamase inhibitor

“Use Naf for staph” aures (not MRSA tho)

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3
Q

Ampicillin kills?

A

“HELPSS” kill enterococci

H Flu, E coli, Listeria monocytogenes, Proteus, Salmonella, Shigella

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4
Q

Piperacillin

A

Combo with Tazobactam (b-lactamase)

Used specifically for Psuedomonas A.

Efficacy against G+, G-, and Anaerobes (psuedo is an aerobe than can also be a faculative anaerobe–grows very well in low/no O2)

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5
Q

Clavulanic Acid

A

Beta Lactmase Inhibitor. Given with Beta lactams to increase their half lives as well to be used in bacteria expressing beta-lactamases.

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6
Q

Monobactams

A

Beta-lactams that only have one ring. Less likely to act as haptens thus they are good to use in G- infections in ppl w/ Pencillin allergies.

Aztreonam

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7
Q

Cephalosporins

Cef’s cover?

Cef’s don’t cover?

A

Beta Lactams: Prefix: Cefs;

Increased resistance to beta-lactamases

Cover (2nd gen): HEN PEcKS (H flu, Enterobacter, Neisseria, Proteus, E coli, Kleb, Serratia)

Don’t Cover: “LAME” Listeria, Atypicals (chlamy, Mycoplasma), MRSA, Enterococci

Worsen Nephrotoxicity of Aminoglycocides

4th Generation best for Psuedomonas (Cefepime)

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8
Q

Carbapenems (Imipenem)

A

Beta-lactam, Big Gun used in ICUs

ALWAYS ADMINISTERED WITH Cilastatin**** (decreases renal tubular inactivation by inhibiting renal dehydropeptidase I)

Binds PBP’s like cillins.

Last Resort used for highly resistant organisms (klebseilla, serratia (red ring on toilet), enterobacter) because of GI/Seizure SEs

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9
Q

Vancomycin

A

Glycopeptides, G+: Inhibits elongation via D-ala D-ala binding.

Enterococci have resistance by switching to D-ala-D-lactose, which can be horizontally transfered to Staph Aur via VRE plasmid

“Glyco_P_eptide works like _P_enicillin”

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10
Q

Bacitracin

A

Glycopeptide, G+, inhibits NAG-NAM tranpsort to outer wall

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11
Q

Protein Synthesis Inhbitors

A
  • Aminoglycosides–Targets 30s portion of Ribosome
  • Tetracycline/Doxycycline–
  • Chloramphenicol
  • Macrolides
  • Lincosamides
  • Mupriocin
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12
Q

Aminoglycosides

A

Strepomycin, Gentamycin, Tobramycin, Amikacin, Neomycin (GANTS)

Anti-30s subunit of Ribo; post-antibiotic effect (activity persists beyond detectable amounts)

“Aminoglycosides=small protein sugars used to inhibit the smaller part of the ribo”

ACUTE RENAL FAILURE** (made worse by Cephalosporins)

“GANTS caNNOT kill anaerobes”

N-ephrotox, N-euromuscular blockade, O-totox, T-eratogen

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13
Q

Tetracycline/Doxycycline

A

Competes with tRNA for A site on 30s (“with tetracyclines the ribosome never has a chance to start cycling”–prevents initiation)

Active against G+/- and protozoa

Not for children dt deposition in teeth (grey) or bone (deformation)

“Vacum the bedroom” Vibrio, Acne, chlamydia, Ureaplasma, Mycoplasma, Tuleramia, H Pylori, Borrellia, Rickettsia”

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14
Q

Chloramphenicol

A

Binds 50s inhibiting translocation of ribosome

Protein synth inhibitor

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15
Q

Macrolides

A

Erythromycin, Azithromycin (Z-pak)

Binds 50s subunit inhibiting translocation “macrolides stop the ribo slide”

Risk of Prolonged QT**** (“z prolongs the qt”)

Erythro: also has GI/Liver (p450) issues

“MACRO”: Motility (GI) issues, Arrthymias (Qt), Cholestatic hepatitis, Rash, eOsinophillia

“Atypical PUS: Atyipical Pneumonia (myco and legionella), URI, STDs”

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16
Q

Clindamycin

A

Protien synth inhibitor; binds to 23s portion of the 50s ribo subunit, causing premature tRNA dissociation

Lincosamide class: Used for skin and soft tissue infections: SE–>pseudomembranous colitis

“Clinda causes premature ejac” of the ribosome

ANAEROBIC INFECTIONS (aspiration pneumonia, lung abscesses, MRSA)

CAUSES C. DIFF INFECTION

17
Q

Mupirocin

A

Protein Synth Inhibitor

Blocking protein synth via Inhibits isoleucyl tRNA synthase

Used for S. Aureus skin infections

18
Q

Purine Synthesis Inhibitors

A
  • DHF reductase inhibitors
  • Suflonamides
19
Q

Trimethoprim

A

DHF Reductase Inhibitors (methotrexate also hits DHFR)

Synergizes: TMP-SMZ

“TMP” Treats Marrow Poorly (megaloblastic anemia, leukopenia, granulocytopenia)

20
Q

Sulfonamides

A

Analog of PABA blocking PABA–>Dihydropteroate synthase inhibitors (bacteria need to make folate since they cannot absorb it)

Synergizes: TMP-SMZ (Bactrim)

Hypersensitivity reactions, Hemolysis (G6PD def), nephrotox, photosensitivity, Kernicertus (thus dont use in Preggers), Stevens Johnson Syndrome

21
Q

Flouoroquinolones

A

-floxacins (cipro, gemi, levo)

inhbitis DNA topoisomerase II (DNA GYRASE) “cipro-circular-gyrase”

UTIs from pseudomonas; prophylaxis for anthrax

Associated with ruptured tendons (damages cartilage), tendonitis (particularly achilles tendon) “Fluoroquinolones hurt attachments to your bones”

22
Q

Metronidazole

A

Nitro group is released by bacterial metabolism and reacts with DNA

Flagyl, used for anaerobic bacteria nd protozoa

GET GAP on the Metro: Giardia, Entamoeba, Trichomona, Gardnerella, Anaerobic bacteria, h Pylori

DISULFIRAM LIKE REACTION W/ ETOH

23
Q

Inhibitors of Cyp P450’s

A

“PICK EGS”

Protease Inhibitors, Isoniazid, Cimetidine/Cipro, Ketonacozle, Erythromycin, Grape Fruit Juice, Sulfonamides

Acute ETOH is inhibitor (Chronic is inducer)

24
Q

Inducers of Cyp P450’s

A

BCG PQRS

Barbiturates, Carbamazepine, Grisesofluvin, Phenytoin, Quinidine, Rifampin, St. Johns Wort

Chronic ETOH=Inudcer (acute is inhibitor)

25
Q

Daptomycin

A

Lipopeptide Antiobiotic. Disrupts bacterial cell membrane leading to loss of membrane potential. Also inhibits macromolecule synthesis

Good to use for very drug resistant bacteria.

Causes myopathy.

26
Q

Linezolid

A

Inhibits the 23s portion of the 50s ribosomal subunit.

“draws a line btwn the 50s and 30s subunits”

Can be used in MRSA VRE resistant infections

SEs: Optic Neuritis, and Thrombocytopenia; Weak MAO increasing risk for Serotonin syndrome

27
Q

Isoniazid

A

Decreases synth of mycolic acids.

Bacterial catalase-peroxidase needed to activate INH.

Competes with Pyridoxine (B6) causing:

1) Neurotoxicity (decreased NT/GABA synth)
2) Hepatotoxicity (needed for transaminase Rxns)

“INH=Injures Neurons and Hepatocytes”

“B6 is RIPES” for TB

28
Q

Rifampin

A

Inhibits DNA-dependent RNA polymerase (“crab claw”)

Used for Tb and for menignococcal and H. Influ type B** prophylaxis

Minor Hepatotox and drug interactions (“AMPs P450”—Rifabutin does not), orange body fluids.

4R’s of Rifampin: 1) RNA poly inhibtior 2) Ramps up P450, 3) Red/Orange body fluids, 4) Rapid resistance if used alone.

29
Q

Pyrazinamide

SEs?

A

Hyperuricemia, hepatotoxicity

WORKS BEST AT LOW pH*** P-yrazinamide at low p-H (works intracellularly)

Increases Acidity of Macrophage phagolysosome increasing their killing.

“PyraziMIDE causes Tb to DIE INSIDE the macros”

30
Q

Ethambutol

A

Inhibits Arabinosyltransferase decreasing carb polymerization of Mycobacterium. (resistance via increased arabinosyltransferase translation)

SEs: Optic neuropathy (red-green blindness) requiring periodic testing.

Etham hurts Eyes***

31
Q

Vancomycin

A

Inhibits Cell wall peptidoglycan formation by binding D-ala D-ala.

SEs: “NOT” trouble free: N-ephrotoxicity, O-totoxicity, T-hrombophlebitits.

RED MAN SYNDROME: release of antihistiamines causing rapid flushing when administered (treat by slowling infusion and giving antihistamine)

Restance: D-ala D-ala to D-ala D-lac

Given as IV cuz of poor absorption unless you want to target C diff (then give orally)

32
Q

Amphotericin B

A

Binds Ergosterol forming pores.
“Amphotericin tears holes in fungi, RBCs, heart, and kidneys”

Need to supplement AND MONITOR K and Na because of altered renal tubule permeability. Risk for arrthymia (again Na/K issue). Anemia

33
Q

Tx for Anaerobic bacteria?

A

Metronidazole and Clindamycin

Aminoglycosides cannot kill anaerobes

34
Q

As you increase in Cephalosporins what you do you do to the spectrum?

First gens good for which bacteria?

A

As you increase generation of cephalo’s you INCREASE G- coverage and DECREASE G+ coverage.

PEcK: Proteus, Ecoli, Kleb