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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
Cefotaxime
3rd Gen
26
Ceftazidime
3rd Gen
27
Cefazolin
1st Gen
28
Cephalexin
1st Gen
29
Cefoxitin
2nd Gen
30
Cefaclor
2nd Gen
31
Cefuroxime
2nd Gen
32
Cefepime
4th Gen
33
Ceftaroline
5th Gen
34
Carbapenems
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
Vancomycin
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
Aminoglycosides
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
Tetracyclines:
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
Macrolides
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
Chloramphenical
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
Clindamycin
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
Sulfonamides
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
Trimethoprim
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
Fluoroquinolones
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
Metronidazol
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
Antimycobacterials
TB: Prophylaxis = INH TX: RIPE MAC: P = Azithromycin
46
INH (Isonazid)
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
Rifamycins
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
Pyrazinamide
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
Ethambutol
Decrease carbohydrate polymerization of cell wall. *Blocks arabinosyltransferase* M TB Causes Optic neuroapthy, Red-Green color blindess. Reversible though
50
Prophylaxis: Endocarditis w/ surgery/dental procedures
Penicillins, amox, 1*cephalos
51
Prophylaxis: Gonorrhea (rape)
Ceftriaxone
52
Prophylaxis: Recurrent UTI's
Bactrim, Amox, Nitro?
53
Prophylaxis: Meningococcal
Cipro (Drug of choice), but Rifampin for children
54
Prophylaxis: Pregant w/ GBS
Intrapartum amp
55
Prophylaxis: Prevention of gonococcal or chlamydial conjunctivitis in newborns
Erythromycin ointment
56
Prophylaxis: Post surgical infection from Staph
Cefazolin
57
Prophylaxis: Strept pharyngitis w/ prior rheumatic fever
Pen V
58
Prophylaxis: Syphillis
Benzathine Pen G
59
Prophylaxis:
Bactrim: PCP
60
Prophylaxis:
Prophylaxis: PCP and Toxo
61
Prophylaxis:
Azithromycin MAC
62
Lanosterol Synthesis
Squalene --> Squalene epoxide *Squalene epoxidase* Terbafine
63
Ergosterol Synthesis
Lanosterol --> Ergosterol 14 a demethylase Azoles Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole
64
Nucleic acid synthesis (Fungal)
5- flucytosine
65
Membrane pores (fungal)
Polyenes: Amphotercin B and Nystatin
66
Cell Wall synthesis (fungal)
Echinocandins: | Caspofungin, micafungin, anidulafungin
67
Amphotercin B
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
Nystatin
Same as amphotericin b, but topical form Oral candidiasis, diaper rash, vaginal candidias
69
Azoles
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
Flucytosine
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
Echinocandins
Caspofungin, micafungin, anidulafungin Inhibits cell wall synthesis. Inhibits *B-glucan* synthesis Invasive aspergillosis and Candida Causes GI upset, flushing via histamine release
72
Terbafine
Inhibits fungal squalene epoxidase Dermatophytoses, especially onychomycosis. Causes GI upset, headaches, hepatotoxicity, taste disturbances
73
Griseolfulvin
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
Antiprotozoan
Pyrimethamine (toxoplasmosis), Suramin and melasoprol (trypansoma brucei), nifurtimox (t. cruzi), Sodium stibogluconate (leishmaniasis) + ampho for visceral
75
Chloroquine
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
Antihelminthic
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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