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Abx * Flashcards

1
Q

Streptomycin

A

Aminoglycoside

  • Binds 30S ribosomal subunit, blocks 3 steps (initiation, translocation, mistranslation)
  • Rapidly bacteriocidal v. G-, post antibiotic effect
  • 2nd-line therapeutic treatment for TB in combo with another agent (INH)
  • Nephrotoxcicity (reversible), Ototoxicity (nonreversible), associated with >5 days of therapy
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2
Q

Tobramycin

A

Aminoglycoside

  • Binds 30S ribosomal subunit, blocks 3 steps (initiation, translocation, mistranslation)
  • Rapidly bacteriocidal v. G-, post antibiotic effect

Treatment of serious systemic G- infections, used in combination with B-lactam (synergism)

  • Nephrotoxcicity (reversible), Ototoxicity (nonreversible), associated with >5 days of therapy
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3
Q

Gentamycin

A

Aminoglycoside

  • Binds 30S ribosomal subunit, blocks 3 steps (initiation, translocation, mistranslation)
  • Rapidly bacteriocidal v. G-, post antibiotic effect

Treatment of serious systemic G- infections, used in combination with B-lactam (synergism)

  • Nephrotoxcicity (reversible), Ototoxicity (nonreversible), associated with >5 days of therapy
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4
Q

Amikacin

A

Aminoglycoside

  • Binds 30S ribosomal subunit, blocks 3 steps (initiation, translocation, mistranslation).
  • Rapidly bacteriocidal v. G-, post antibiotic effect

Treatment in cases of resistance to tobramycin and gentamycin caused by inactivating enzymes

  • Nephrotoxcicity (reversible), Ototoxicity (nonreversible), associated with >5 days of therapy
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5
Q

Neomycin

A

Aminoglycoside

  • Binds 30S ribosomal subunit, blocks 3 steps (initiation, translocation, mistranslation)
  • Rapidly bacteriocidal v. G-, post antibiotic effect

Limited to topical use (skin and eyes)

  • Nephrotoxcicity (reversible), Ototoxicity (nonreversible), associated with >5 days of therapy
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6
Q

Kanamycin

A

Aminoglycoside

  • Binds 30S ribosomal subunit, blocks 3 steps (initiation, translocation, mistranslation)
  • Rapidly bacteriocidal v. G-, post antibiotic effect

Limited to topical use (skin and eyes)

  • Nephrotoxcicity (reversible), Ototoxicity (nonreversible), associated with >5 days of therapy
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7
Q

Tetracycline

A

Tetracyclines

  • Bind 50S ribosomal subunit and interfere with protein synthesis by blocking ribosomal translocation
  • Generally bacteriostatic v. aerobic Gram+ and some Gram-

Indications:

  • Rikettsia (RMSF, typhus, Q)
  • STI’s (Chlamydia, etc)
  • Respiratory infections
  • skin and soft tissue infections (staph, acne)

Contraindications:
GI disturbnces, Teeth and bone issues. Not for children or pregnant women

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8
Q

Oxytetracycline

A

Tetracyclines

  • Bind 50S ribosomal subunit and interfere with protein synthesis by blocking ribosomal translocation
  • Generally bacteriostatic v. aerobic Gram+ and some Gram-

Indications:

  • Rikettsia (RMSF, typhus, Q)
  • STI’s (Chlamydia, etc)
  • Respiratory infections
  • skin and soft tissue infections (staph, acne)

Contraindications:
GI disturbnces, Teeth and bone issues. Not for children or pregnant women

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9
Q

Demeclocycline

A

Tetracyclines

  • Bind 50S ribosomal subunit and interfere with protein synthesis by blocking ribosomal translocation
  • Generally bacteriostatic v. aerobic Gram+ and some Gram-

Indications:

  • Rikettsia (RMSF, typhus, Q)
  • STI’s (Chlamydia, etc)
  • Respiratory infections
  • skin and soft tissue infections (staph, acne)

Contraindications:
GI disturbnces, Teeth and bone issues. Not for children or pregnant women

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10
Q

Minocycline

A

Tetracyclines

  • Bind 50S ribosomal subunit and interfere with protein synthesis by blocking ribosomal translocation
  • Generally bacteriostatic v. aerobic Gram+ and some Gram-

Indications:

  • Rikettsia (RMSF, typhus, Q)
  • STI’s (Chlamydia, etc)
  • Respiratory infections (community-acquired pneumonia)
  • skin and soft tissue infections (staph, acne)

Contraindications:
GI disturbnces, Teeth and bone issues. Not for children or pregnant women

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11
Q

Doxycycline

A

Tetracyclines

  • Bind 50S ribosomal subunit and interfere with protein synthesis by blocking ribosomal translocation
  • Generally bacteriostatic v. aerobic Gram+ and some Gram-

Indications:
MDR Bacteria - intra-abdominal, skin, soft-tissue infections, community acquired pneumonia

Contraindications:
GI disturbnces, Teeth and bone issues. Not for children or pregnant women

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12
Q

Tigeclycine (glycylcycline)

A

Tetracyclines

  • Bind 50S ribosomal subunit and interfere with protein synthesis by blocking ribosomal translocation
  • Generally bacteriostatic v. aerobic Gram+ and some Gram-

Indications:
Antrhax, malaria, lyme disease

Contraindications:
GI disturbnces, Teeth and bone issues. Not for children or pregnant women

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13
Q

Erythromycin

A

Macrolide

  • Bind 50s ribosomal subunit, interfere with protein synthesis by block ribosomal translocation step
  • Generally bacteriostatic v. aerobic G+ and some G- bacteria

Respiratory infections, Acute otitis media, Streptococcal pharyngitis, Chlamydial infections, Diphtheria, Pertussis

Contraindications: GI disturbances and hepatotoxicity

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14
Q

Clarithromycin

A

Macrolide

  • Bind 50s ribosomal subunit, interfere with protein synthesis by block ribosomal translocation step
  • Generally bacteriostatic v. aerobic G+ and some G- bacteria

Respiratory infections, Acute otitis media, Streptococcal pharyngitis, Chlamydial infections, Diphtheria, Pertussis

Contraindications: GI disturbances and hepatotoxicity

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15
Q

Azithromycin

A

Macrolide

  • Bind 50s ribosomal subunit, interfere with protein synthesis by block ribosomal translocation step
  • Generally bacteriostatic v. aerobic G+ and some G- bacteria

Respiratory infections, Acute otitis media, Streptococcal pharyngitis, Chlamydial infections, Diphtheria, Pertussis

Contraindications: GI disturbances and hepatotoxicity

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16
Q

Telithromycin

A

Macrolide

  • Bind 50s ribosomal subunit, interfere with protein synthesis by block ribosomal translocation step
  • Generally bacteriostatic v. aerobic G+ and some G- bacteria

HEPATOTOXICITY –> ONLY APPROVED FOR COMMUNITY-ACQUIRED PNEUMONIA

Contraindications: GI disturbances and hepatotoxicity

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17
Q

Clindamycin

A

Lincosamide

  • Binds 50S Ribosomal subunit and interferes with protein synthesis by blocking ribosomal translocation step.
  • Bacteriostatic v. aerobic and anaerobic G+

Skin and soft-tissue infections

Contraindications: Diarrhea, pseudomembranous colitis caused by C. diff, skin rashes

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18
Q

Quinupristin/Dalfopristin

A

Streptogramins

  • Bind 50S ribosomal subunit, interfere with protein synth by blocking ribosomal translocation and inhibiting peptide elongation
  • Active v. most G+ bacteria, combination is bacteriocidal v. streptococci, most staph, bacteriostatic vs. enterococci.

Indications:
- treatment of infections caused by VRE, treatment of MSSA

Contraindications: Infusion-related effects of IV only combination, Arthralgias, myalgias

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19
Q

Linezolid

A

Oxazolidinone

  • Binds 50S ribosomal subunit, interferes with protein synthesis by blocking initiation.
  • active against aeorobic and anaerobic G+ bacteria.
  • Bactericidal v. streptococci, bacteriostatic v. staph and enterococci

Indications: treat MDR G+ bacteria MRSA, VRE, penicillin-resistant streptococci.

Side effects: myelosuppression (leukopenia, pancytopenia, thrombocytopenia) with treatment >2 weeks

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20
Q

Sulfisoxazole

A

Anti-folate sulfonamide

  • Competitive antagonist of dihydropteroate synthase
  • bacteriostatic v. many G- and some G+ bacteria

UTI (in combo)

Side Effects: Allergic reactions (fever, rash, photosensitivity, GI), crystalluria, hematuria

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21
Q

Sulfamethoxazole (SMX)

A

Anti-folate sulfonamide

  • Competitive antagonist of dihydropteroate synthase
  • bacteriostatic v. many G- and some G+ bacteria

UTI (in combo)

Side Effects: Allergic reactions (fever, rash, photosensitivity, GI), crystalluria, hematuria

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22
Q

Sulfasalazine

A

Anti-folate sulfonamide

  • Competitive antagonist of dihydropteroate synthase
  • bacteriostatic v. many G- and some G+ bacteria

Ulcerative colitis and enteritis

Side Effects: Allergic reactions (fever, rash, photosensitivity, GI), crystalluria, hematuria

23
Q

Trimethoprim/Sulfamethoxazole (TMP-SMX)

A

Anti-folate TMP-SMX Combo

  • TMP is a competitive antagonist of dihydrofolate reductase.
  • TMP is bacteriostatic v. many G- and some G+
  • SMX Competitive antagonist of dihydropteroate synthase
  • SMX bacteriostatic v. many G- and some G+ bacteria

TMP-SMX is bacteriocidal

Indications: UTI, PCP, Shigellosis, Salmonella, prostatitis, acute exacerbations of chronic bronchitis.

Contraindications: 5 days of treatment, megaloblastic anemia, leukopenia

24
Q

Ciprofloxacin

A

Fluoroquinolones

  • Inhibit TOPO II (DNA gyrase) in G- and inhibit TOPO IV in G+
  • Bactericidal v. G-, G+

Indications:

  • UTI
  • Diarrhea from shigella, salmonella, E. coli
  • soft tissue bone and joint infections
  • intra-abominal infections
  • *anthrax treatment and prevention

Contraindications: generally well tolerated, minor GI disturbances

25
Lomefloxacin
Fluoroquinolones - Inhibit TOPO II (DNA gyrase) in G- and inhibit TOPO IV in G+ - Bactericidal v. G-, G+ Indications: - UTI - Diarrhea from shigella, salmonella, E. coli - soft tissue bone and joint infections - intra-abominal infections Contraindications: generally well tolerated, minor GI disturbances
26
Levoflaxin
Fluoroquinolones - Inhibit TOPO II (DNA gyrase) in G- and inhibit TOPO IV in G+ - Bactericidal v. G-, G+ Indications: - UTI - Diarrhea from shigella, salmonella, E. coli - soft tissue bone and joint infections - intra-abominal infections - **Respiratory tract infections Contraindications: generally well tolerated, minor GI disturbances
27
Ofloxacin
Fluoroquinolones - Inhibit TOPO II (DNA gyrase) in G- and inhibit TOPO IV in G+ - Bactericidal v. G-, G+ Indications: - UTI - Diarrhea from shigella, salmonella, E. coli - soft tissue bone and joint infections - intra-abominal infections Contraindications: generally well tolerated, minor GI disturbances
28
Gemifloxacin
Fluoroquinolones - Inhibit TOPO II (DNA gyrase) in G- and inhibit TOPO IV in G+ - Bactericidal v. G-, G+ Indications: - UTI - Diarrhea from shigella, salmonella, E. coli - soft tissue bone and joint infections - intra-abominal infections - ** Resipiratory tract infections Contraindications: generally well tolerated, minor GI disturbances
29
Moxifloxacin
Fluoroquinolones - Inhibit TOPO II (DNA gyrase) in G- and inhibit TOPO IV in G+ - Bactericidal v. G-, G+ Indications: - UTI - Diarrhea from shigella, salmonella, E. coli - soft tissue bone and joint infections - intra-abominal infections - ** Resipiratory tract infections Contraindications: generally well tolerated, minor GI disturbances
30
Penicillins
penicillin G, cloxacillin, amoxicillin mimic D-ala-D-ala, blocking peptidoglycan x-link, no more petidoglycan additions to cell wall. - acid labile, B-lactamase susceptible. - vs. g+, g- cocci, non-B-lactamase-producing anaerobes
31
Clavulinic acid
beta-lactamase inhibitor, must be Rx with a beta lactam like penicillan. (sulfbactam and tazobactam are other beta-lactamase inhibitors)
32
cefazolin
1st generation cephalosporin - Broad spectrum, best v. G+ - Used for surgical prophylaxis, does not penetrate CNS
33
cefamandole
2nd generation cephalosporin - G+, G- - no allergic cross-reactivity with penicillin
34
ceftazidime
3rd generation cephalosporin - more G-, less G+ - some cross to CNS - vs. inducible B-lactamase production but not constitutive B-lactimase producing strains
35
cefeprime
4th generation cephalosporin - True broad spectrum drugs - penetrate CNS - more reisistant to chromosomal B-lactamases - Good against pseudomonas, enterobacteriacae, staph, haemophilus, tessera, most penicillin resistant strep.
36
ceftaroline
latest generation cephalosporin - approved against MRSA - high affinity toward MRSA transpepsidase - administered IV - works on G+, G-
37
aztreonam
monobactam - no activity toward G+ ( does not bind transpeptidase) - vs. G- rods, resistant to B-actamases
38
carbapenem
imipenem - broad spectrum against g- rods g+ and anaerobes (mixed infections) - Inactivated by dehydropeptidases in renal tubules so use CILASTATIN to increase t1/2
39
polymyxins
lipopetides (membrane disruptors) - large, used topically in neosporin - perforates G- bacteria by binding lipoplysacc. on membrane - resistance = lipopolysaccharide structural changes
40
Inhibitors of peptidoglycan precursors
fosfomycin, bacitracin, D-cycloserine
41
Oxacillin, cloxacillan, and dicloxacillin
Anti-staphylococcal penicillans - acid stable, B-lactamase resistant - vs. B-lactamase-producing staph, penicillan-susceptible strep and pneumonococci. - NOT for enterococci, anaerobic bacteria, G- occci and rods.
42
amoxicillan
extended-spectrum penicillans - acid stable vs. G- because they penetrate outer membrane - B-lactamase susceptible. - Use in UTIs, otitis, LRT infections
43
meropenam
carbapenam, resistant to modification by renal dehydropeptidase
44
Vancomycin
Non-beta-lactam cell wall synthesis inhibitor - glycopeptide - large complicated structure binds D-ala-D-ala in cell wall - vs. G- - VRE = D-Ala-D-Lac, reduce binding affinity of Vanco - Vanco-resistant Staph creates thickened peptidoglycan layer
45
Daptomycin
lipopeptide pore former - makes membrane pores__> K+ exists without cell rupture. Bacteria cannot grow. - v. G+ skin and soft tissue infections involving MRSA
46
Peptidoglycan precursors assembly steps
1. Nag converted to Nam-UDP (Fosfomycin) 2. Peptide chains added to Nam-UDP (ala, glu, lys) 3. More peptide chains added to Nam-UDP (D-ala, D-ala) 3. 1 Lipid phosphotase dephosphorylates a lipid carrier on cell membrane (Bacitracin) 4. Nam-UDP added to lipid on lipid membrane with NAG 5. Flipped to outside
47
Fosfomycin
Cell membrane synthesis inhibitor Inhibits first committed step in cell wall-synthesis; Nag conversion to Nam by MurA - TB naturally resistant
48
Bacitracin
Cell membrane synthesis inhibitor Inhibits lipid phosphotase that dephosphorylates the lipid carrier of Nam and Nag. - use topically, nephrotoxic - vs. G+, used with other Abx
49
D-cycloserine
Cell membrane synthesis inhibitor - competitively inhibits alanine racemes and D-ala ligase when d-ALA to be addd to Nam. Looks like D-alanine. - serious toxicity (Dose related CNS: tremors, convulsions, psychosis) - 2nd line for TB
50
Isoniazid (INH)
- bactericidal against extracellular and intramacrophage mycobacteria - target mycolic acid synthesis in mycobacterial membrane - Use with other drugs - TB - activated by bacterial KatG, compound with NAD - targets FAS-II multiple enzyme system which makes long chain on mycolic acid - hepatitis, peripheral neuropathy (looks like B6) - metabolism depends on fast or slow acetylators (determined by genetics)
51
Ethambutol (EMB)
- Bacteriostatic mycobacterial drug - Targets arabinogalactan in mycobacterial membrane - blocks EmbA and EmbB arabinosyl transferases, weaken cell wall, make TB susceptible to damage - works bets against fast growing extracellular Mtb - can cause red-green color blindness, optic neuritis
52
Pyrazinamide (PZA)
TB/mycobacterial drug that inhibits protein synthesis by targeting ribosomal protein S1 in latent bacteria. - a stalled ribosome presents danger to cell (incomplete polypeptide) and cell uses RpsA/tmRNA mechanism to recycle the ribosome. PZA interacts with RpsA, to block the ribosome from interacting with tmRNA. Trans-translation is blocked. Stalled ribosome => depletion of available ribosomes, accumulation of deleterious proteins.
53
Rifampin (RIF)
First line TB drug - RNA synthesis inhibitor, inhibits transcription elongation (bacterial nascent RNA gets stuck, cannot depart from gene promotors) - bacteriacidal to G-, G+, mycobacteria, chlamydia - complex, semi-synthetic - induces P450 CYP3A (increased elimination of other drugs)
54
Rifabutin and Rifapentine
Act like Rifampin but they are more potent, longer t1/2, better membrane permeability, and less CYP3A induction

MICROBIO DRUGS (6 decks)

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