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Antimicrobials Flashcards

1
Q

Folic Acid Synthesis (DNA Methylation)

PABA–>DHF

A

Sulfonamides: Suflamethoxazole, Sulfisoxazole, Sulfadiazine

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2
Q

Folic Acid Synthesis (DNA Methylation)

DHF -> THF

A

Trimethoprim

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3
Q

DNA Topoisomerase

A

Fluoroquinolones
Ciprofloxacin, Levofloxacin

Quinolone
Nalidixic Acid

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4
Q

Damages DNA

A

Metronidazole

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5
Q

mRNA Synthesis

A

RNA polyermase inhibitor: Rifampin

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6
Q

Protein Synthesis (50S)

A

Chloramphenicol, Macrolides, Linezolid, Clindamycin

+ Streptogramins (quinupristin, dalfopristin)

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7
Q

Protein Synthesis (30S)

A

Aminoglycosides (Gentamicin, Neomycin, Amikacin, Tobramycin, streptomycin)

Tetracyclines (Tetracycline, Doxycycline, Minocycline)

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8
Q

Peptidoglycan Cross Linking

A

Penicillinase-sensitive penicillins:
Pen V&G
Ampicillin
Amoxicillin

Penicillinase-resistant Penicillins:
Oxacillin
Naficillin
Dicloxacillin

Antipseudomonals:
Ticarcillin
Piperacillin

Cephalosporins:
I: Cephazolin
II: Cefoxitin
III: Ceftriaxone
IV: Cefepime
V: Ceftaroline

Carbapenems:
Imipenem, Meropenem, Ertapenem, Doripenem

Monbactams: Aztreonam

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9
Q

Peptidoglycan synthesis

A

Glycopeptides: Vanco and Bacitracin.`

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10
Q

Penicillin G & V

A 
G= IV form
V = Oral

Mech: Bind PBP (transpeptidases), preventing crosslinking. Activate autolytic enzymes

Bactericidal: Used form mostly GP organisms. (S. pneumo, S. pyogenes, Actinomyces). But also N. meningitidis, and T. pallidum.

Cidal to GPC, GPR, , GNC, and spirochetes. but penicillinase sensitive

Toxicity: Hypersensitivity, hemolytic anemia

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11
Q

Aminopenicillins

A

Same as penicillin, but wide spectrum.

amOxicillin = > oral bio
Amp = sulbactam
Amox= clauvonic acid

Combine w/ clauvonic acid to protect from B lactamases

Use: HELPSS kill enterococci
H. influenzae, E. coli, Listeria, Proteus mirabilis, Salmonella, Shigella, enterococci

2ndline for UTIs

Toxicity: Rash (especially w/ EBV), hypersensitivity, and GI like everything

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12
Q

HELPSS

A 
Bacteria killed by aminopenecillins
H. influenza
E. coli
Listeria,
Proteus mirabilis
Salmonella,
Shigella

and Entercocci

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13
Q

Penicillinase resistant bacterias

A

Same as penicillin, narrow spectrum. Bulky R group

S. aureus - MRSA

Toxicity: hypersensitivity reactions, Interstitial nephritis.

Resistants from mecA gene PBP2A

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14
Q

Antipseudomonals (Ticarcillin, piperacillin)

A

Pip w/ Tazobactam
Tic w/ clauvonic acid

Same mech as penicillin, but extended spectrum

Pseudomonas and other GNR

Hypersensitivity reactions

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15
Q

Cephalosporins:

A

B lactams, inhibit synthesis.

Cidal too, but less suceptible to penicillinases

Not covered by Cephalosporins: LAME

Listeria, Atypicals, MRSA, Enterococci.

MRSA (Ceftaroline can cover it)

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16
Q

Not covered by Cephalosprins

A

LAME

Listeria, Atypicals, MRSA, Enterococci

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17
Q

1st Gene Cephalos

A

Cefazolin, Cephalexin –> more gram + cocci and
PEcK and also in surgery to prevent S. wound infections

Gram +ve Cocci (URI) and PEcK (common UTI’s)

These + ampicillin = prohyplaxis against viridan

PEcK = Proteus marabilis, E. coli, Klebsiella

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18
Q

2nd Gene Cephalos

A

Cefoxitin, Cefaclor, Cefprozil, Cefuroxime
Gram + cocci and

HEN PEcKS

H. Influenza, Enterobacter, Neisseria, Proteus Mirabilis, E. Coli, Klebsiella, Serratia

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19
Q

3rd Gene Cephalos

A

Ceftriaxone, Cefotaxime, ceftazidime.
Serious Gram Negative infections resistant to other B lactams

S. pneumoniae, HiB, Gonorrhea, Meningitis, Lyme,

Cefatizidime = Pseudomonas

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20
Q

4th Gen Cephalo

A

Cefepime –> Pseudo and grampositives

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21
Q

5th Gene Cephalo

A

Ceftaroline

Borad, including MRSA,
but not pseudomonas

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22
Q

Cephalo toxicity:

A

Hypersensitivity (5-10% cross reactivity w/ penicillin), Vitamin K deficiency,

Increases nephrotoxicity with aminoglycosides

Disulfuram like reaction

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23
Q

Monobactams

A

Aztreonam

Resistant to B lactamases.

Binds to PBP3.

Synergistic w/ Aminoglycosides

ONLY FOR GNRs.

Nothing against anaerobes or gram positives.

For penicillin allergies who can’t tolerate aminoglycosides (Renal insufficiency)

Usually non toxic

Aminoglycoside pretender

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24
Q

Ceftriaxone

A

Longest 1/2 life. 1 q Day

IV/IM

3rd gen

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25
Q

Cefotaxime

A

3rd Gen

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26
Q

Ceftazidime

A

3rd Gen

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27
Q

Cefazolin

A

1st Gen

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28
Q

Cephalexin

A

1st Gen

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29
Q

Cefoxitin

A

2nd Gen

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30
Q

Cefaclor

A

2nd Gen

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31
Q

Cefuroxime

A

2nd Gen

32
Q

Cefepime

A

4th Gen

33
Q

Ceftaroline

A

5th Gen

34
Q

Carbapenems

A

Imipenem (always with cilastatin, Renal dehydropeptidase kills it otherwise),
Meropenem (reduced seizure risk)
Ertapenem, Doripenem

Broad spectrum, B lactamse resistant carbapenem

Newer ones (ertapenem and dorpenem) have limited pseudo coverage

GPC, GNR, and anaerobes. Huge spectrum

Save for life threatening infections.

Toxicity: Gi distress, skin rash, CNS toxicity (Seizures, less w/ mero).

35
Q

Vancomycin

A

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

Cidal

Gram positive only. for Serious MDR organisms. MRSA, enterococci, C. diff (oral)

Well tolerated usually

NOT trouble free.
Nephrotoicity, ototoxicity, thrombophlebitis

Red man syndrome, no allergy, just give anti histamines and slow infusion rate.

Resistance via D ala dala to dala dlac

36
Q

Aminoglycosides

A

Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin GNATS and NNOT

Bacteriocidal (vs tetracyclines)

30s
Inhibits formation of initiation complex.
“A initiates Alphabet”

Leads to misreading of mRNA and Blocks translocation

MUST have O2

Can’t use on anaerobes

Use: Synergistic w/ B lactams, specifically Azteronam

Neomycin for bowel

NNOT
Nephrotoxicity (especially w/ cephalosporins), NMJ block, Ototoxicity (especially w/ loops), Teratogen

Mech of resistance: Bacterial transferase enzyme inactivates drug by acetylation, phosphorylation, adenylation

37
Q

Tetracyclines:

A

Static (vs aminoglycosides)
Doxyc, Tetra, minocycline

Binds to 30s,

  • Prevents attachment of aminoacyl-tRNA*
  • Binds to “A” site*

Limited CNS penetration

Doxycylcine is fecally eliminated*
Good in renal failure patients

Milk, antacids, and Iron (divalent cations) block absorption in the gut

Use: Borrelia, M. pneuoniae,
Acuumulates intracellularly –> good for rickettsi and chlamydia
Also in bartonella w/ macrolides, Brucella w/ rifampin. And Acne

Toxicity: GI distress, discoloration of teeth and inhibition in bone growth of children.
Photosensitivity and contradindicated in pregnancy

Mechanism of resistance: Decrease uptake or increase efflux out of bacterial cells
Plasmid encoded transport pumps

38
Q

Macrolides

A

Azithro, Clarithro, Erythro

Inhibits 50S by blocking Translocation (macroSLIDES). Binds to *23S rRNA but doesn’t directly affect peptidyl transferase.

Static

Use: Atypical pneumoniaes (Mycoplasma, Chlamydia, Legionella), STDs (chlamydia), GPC (Strept, specially if allergic to penicillin)

Toxicity is MACRO
gi Motility, Arrythmia (prolonged QT w/ Zpack), acute Cholestatic hepatitis, Rash, eOsinophilia

Increase serum concentrations of theophyllines and oral anticoagulants

Mechanism of resistance: Methylation of 23S rRNA binding sight.

39
Q

Chloramphenical

A

Blocks Peptidyltransferase (23S of 50S)

Static

Not used much.

Meningitis (HiB, S. pneumo, N. mening), RMSF

Limited from toxicities

Toxic: Anemia (dose dependent), Aplastic anemia (Dose independent*).

Gray baby syndrome (premies), Lack UDP glucuronyl transferase). Can’t conjugate to bile, increase in serum

Mechanism of resistance: Plasmid encoded acetyltransferase inactiavtes (like aminoglycosides)

40
Q

Clindamycin

A

Blocks Translocation via 50S. like macrolide

Static

USed in anaerobes

Clinda (anaerobes above diaphragm) vs (metro anaerobes below the diaphragm)

Aspiration pneuonnia, lung abscesses, oral infections. GAS, MRSA.

Can lead to C. diff, fever and diarrhea

41
Q

Sulfonamides

A

Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine

INhibits folate synthesis (PABA –> DHF) Dihydropteroate synthase

Gram positives, Gram negatives, Nocardia, Chlamydia, Proteus. Simple UTI

Prophylaxis for Toxo and PCP

Toxicity: Hypersensitivity reactions, G6PD, nephro (tubulointerstitial nephritis), photosensitivity, kernicterus in infants.

Displaces other drugs from albumin

Mechanism of resistance: Altered enzyme, decrease uptake, or increase PABA synthesis

42
Q

Trimethoprim

A

Inhibits DHF reductase.

Static

Often as bactrim

UTI, Shigella, Salmonella, PCP treatment and prophylaxis, and toxo prophylaxis

Pyrimethamine works similar (toxo)

TMP Treat Marrow Poorly
Megaloblastic anemia, leukopenia, granulocytopenia

43
Q

Fluoroquinolones

A

Cirpofloxacin, norflo, levofloxacin, oflo, sparfloxacin, moxi, nalidixic (quinolone)

Inhibits DNA Gyrase (topoisomerase II) and Topoisomerase IV.

Cidal (like penicillins, and aminoglycosides)

Can’t take w/ antacids (like tetras)

GNR of UTI and GI. Pseudo, neisseria, some Gram positives.
Legionella, Antrax, Salmonella typhi

Toxicity: Gi upset, superinfections, skin rashes, headaches, dizziness

Tendonitis, rupture, leg cramps, myalgia

Contraindicated in pregnant, nursing, or children under 18 –> Cartilage damage.

Prolonged QT.

worse rupture if prednisone

Mechanism of resistance: Chromosome incoded mutation of DNA gyrase,

Plasmid mediated,

Efflux pumps

44
Q

Metronidazol

A

Forms free radical toxic metabolites in bacterium, damage DNA.

Cidal and antiprotozoal

GET GAP: Gardanella, Entamoeba, Trichomonas, Giardia, Anaerobes, Pylori

Anaerobes below diaphragm

Disulfiram like reaction (severe flushing, tachycardia, hypotension)

Headache, metalic taste

45
Q

Antimycobacterials

A

TB: Prophylaxis = INH TX: RIPE

MAC: P = Azithromycin

46
Q

INH (Isonazid)

A

Decrease synthesis of mycolic acids.

Bacterial catalacse peroxidase is required (KatG gene) for INH to become active

TX Tb, or solo prophylaxis.

1/2 life depends on acetylation speed

Toxicity: neuro, hepato, B6 can help..

HIPP lupus

INH Injures neurons and hepatocytes

47
Q

Rifamycins

A

Rifampin and Rifabutin

Inhibits DNA dependent RNA polymerase

TB:
delays resistance to dapsone in leprosy

Meningococcal prophylaxis, and HiB prophylaxis.

Brucella too.

Minor hepatotoxicity, drug interactions (increases p-450)

Orange fluids. Rifabutin > rifampin w/ HIV, less p450 effects

4 Rs: RNA polymerase, Ramps c P450, red secretions, Rapid resistance alone

48
Q

Pyrazinamide

A

Mechanism uncertain. converted to pyrazinoic acid. effective in acid pH of phagolyososmes, where TB is found

Only used in TB

Leads to hyperuricemia and hepatotoxicty

49
Q

Ethambutol

A

Decrease carbohydrate polymerization of cell wall. Blocks arabinosyltransferase

M TB

Causes Optic neuroapthy, Red-Green color blindess. Reversible though

50
Q

Prophylaxis: Endocarditis w/ surgery/dental procedures

A

Penicillins, amox, 1*cephalos

51
Q

Prophylaxis: Gonorrhea (rape)

A

Ceftriaxone

52
Q

Prophylaxis: Recurrent UTI’s

A

Bactrim, Amox, Nitro?

53
Q

Prophylaxis: Meningococcal

A

Cipro (Drug of choice), but Rifampin for children

54
Q

Prophylaxis: Pregant w/ GBS

A

Intrapartum amp

55
Q

Prophylaxis: Prevention of gonococcal or chlamydial conjunctivitis in newborns

A

Erythromycin ointment

56
Q

Prophylaxis: Post surgical infection from Staph

A

Cefazolin

57
Q

Prophylaxis: Strept pharyngitis w/ prior rheumatic fever

A

Pen V

58
Q

Prophylaxis: Syphillis

A

Benzathine Pen G

59
Q

Prophylaxis:

A

Bactrim: PCP

60
Q

Prophylaxis:

A

Prophylaxis: PCP and Toxo

61
Q

Prophylaxis:

A

Azithromycin MAC

62
Q

Lanosterol Synthesis

A

Squalene –> Squalene epoxide
Squalene epoxidase

Terbafine

63
Q

Ergosterol Synthesis

A

Lanosterol –> Ergosterol
14 a demethylase

Azoles
Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole

64
Q

Nucleic acid synthesis (Fungal)

A

5- flucytosine

65
Q

Membrane pores (fungal)

A

Polyenes: Amphotercin B and Nystatin

66
Q

Cell Wall synthesis (fungal)

A

Echinocandins:

Caspofungin, micafungin, anidulafungin

67
Q

Amphotercin B

A

Binds Ergosterol, forms membrane pores –> leakage of electrolytes

Used in serious, systemic mycoses. Cryptococus (w/wo flucytosine), Balstomyces, coccidioides, histo, candida, mucor,

Intrathecal for fungal meningitis
Supplement K and Mg –> alters renal permeability

Fever/Chills (shake and bake)
hypotension, nephrotoxicity, arrythmias, anemia, IV phlebitis.

Hydration helps with nephro and liposomal helps with toxicity

68
Q

Nystatin

A

Same as amphotericin b, but topical form

Oral candidiasis, diaper rash, vaginal candidias

69
Q

Azoles

A

Inhibits fungal sterol synthesis (14 a demethylase, a c p450 enzyme that converts lanosterol to ergosterol)

Local and less serious systemic mycoses. Fluconazole for chronic suppresion of Cryptococcal meningitis in AIDS, candida of all types.

Itraconazole for Blasto, Histo and Coccidioid, aspergillus, sporothorix,

Clotrimazole and miconazole for topical

Toxicity: INhibits cortisol and testosterone synthesis (gynecomastia keto), liver dysfucntion (ihnibits cy p450)

70
Q

Flucytosine

A

Inhibits DNA and RNA biosynthesisi by conversion to 5-FU by cytosine deaminase (thymidilate synthase inhibitor)

Systemic fungal infections (meningitis fro crypto) + amphotercin B

Toxicity: bone marrow suppression and GI

71
Q

Echinocandins

A

Caspofungin, micafungin, anidulafungin

Inhibits cell wall synthesis.

Inhibits B-glucan synthesis

Invasive aspergillosis and Candida

Causes GI upset, flushing via histamine release

72
Q

Terbafine

A

Inhibits fungal squalene epoxidase

Dermatophytoses, especially onychomycosis.

Causes GI upset, headaches, hepatotoxicity, taste disturbances

73
Q

Griseolfulvin

A

Unique: Oral for hair + nail

Interferes with microtubule function. disrupting mitosis.

Deposits in keratin containing tissues

Oral treatment of rsuperficial infections

Teratogenic, GI, Carcinogenic, confusion, headaches, increase p 450, and warfarin metabolism (Seizure meds, OTC)

74
Q

Antiprotozoan

A

Pyrimethamine (toxoplasmosis),
Suramin and melasoprol (trypansoma brucei),
nifurtimox (t. cruzi),
Sodium stibogluconate (leishmaniasis) + ampho for visceral

75
Q

Chloroquine

A

Blocks detoxification of heme into hemozoin. toxic to plasmodia

Treats all but P. falciparum. Resistance from pump.

P. falciparum = artemether/lumefantrine or atovaquone/proguanil

IV quinidine if life threatening

Primaquine if Vivax/ovale

Can cause retinopathy, pruritis

76
Q

Antihelminthic

A

Mebendazole, pyrantel pamoate, ivermectin, diethylcarbamazine, praziquantel (imobilize helminths)

Round worms (nematodes)
Enterobius: Bendazole or Pyrantel pamoate

Ascariasis: Bendazole or Pyrantel pamoate

Strongyloides: Ivermectin or bendazole

Ancylostoma/Necator: Bendazole or Pyrantel pamoate

Onchocerca: Ivermectin

Loa Loa: Diethylcarbamazine

Wuchereria bancrofti: Diethylcarbamazine

Toxocara: Bendazole

Cestodes (tapeworms)
Taenia solium: Praziquantol (+bendazole if neuro)

Diphyllobothrium: Praziquantal

Echnioccous: Bendazole

Flukes:
Schistoma: Praziquantal
Clonorchis: Praziquantal

Microbio (11 decks)

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