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Antibiotics Flashcards

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1
Q

What are the desired properties of antibiotics?

A

broad range
can get into body tissues
high therapeutic index

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2
Q

What are some synergistic drug interactions

A

Sulfamethoxazole-Trimethoprim (SxT) (blok sequential steps)

Loperamide-Tetracycline (facilitate drug entry)

Augmentin (amoxicillin-clavulanate) one drug inhibits detox enzymes

Synercid (quinupristin-dalfopristin) individually they are bacteriostatic protein synthesis inhibitors, together they are bacteriocidal

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3
Q

When would you use multiple antibiotics

A

systemic or multiple infections
to delay resistance in long-term use
synergisms

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4
Q

When would you use prophylaxis

A

before contact with known agent
before surgery (>3% risk of infections complication)
predisposition to infection

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5
Q

Mode of action of beta-lactams?

A

cell wall inhibitors: inhibit transpeptidation and activate autolysins in cell wall

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6
Q

Resistances to beta-lactams?

A

beta-lactamase enzyme
lack of penicillin binding proteins (PBPs)
autolysin mutations

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7
Q

What drugs are beta-lactamase inhibitors?

A 
clavulanic acid (+amoxicillin= Augmentin)
sulbactam (+ampicillin)
tazobactam (+piperacillin= Zosyn or Tazomed)
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8
Q

What are natural penicillins best against?

A

G+

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9
Q

Name the beta-lactamase resistant penicillins

A

nafcillin
oxacillin
cloxacillin

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10
Q

Name the expanded spectrum penicillins (G+ and G-)

A

ampicillin
piperacillin
mezlocillin
ticarcillin (vs. pseudomonas)

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11
Q

What penicillins are acid resistant?

A

amoxycillin, Pen V, oxacillin

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12
Q

What drug group do cephalosporins belong to and what differentiates them from other drug families in that group?

A

belong to beta-lactams (so mode of action is a cell wall inhibitor)

less sensitive to beta-lactamases than penicillins

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13
Q

What are the 1st gen cephalosporins, what bugs do they target, when are they used?

A

cephalexin, cephalothin, cefazolin

G+ action

only used for prophylaxis

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14
Q

What are the 2nd gen cephalosporins, what bugs do they target, when are they used?

A

cefaclor, cefuroxime, cefoxitin

G+ and G- action

can target Bacteroids, but not Pseudomonas

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15
Q

What are the 3rd gen cephalosporins, what bugs do they target, when are they used?

A

ceftazidime, cephotaxime, cephtriaxone, cefdinir

G+ and G- action (including Pseudomonas)

used mostly for G-, can penetrate CNS for meningitis

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16
Q

What are the 4th gen cephalosporins, what makes them special?

A

cefepime

broadest spectrum of all cephalosporins

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17
Q

What are the 5th gen cephalosporins, when are they used?

A

ceftaroline

activity vs. MRSA and drug-resistant S. pneumoniae (but not Pseudomonas)

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18
Q

What group do monobactams belong to, and what makes them special?

A

beta-lactams

monocyclic beta-lactam ring gives resistance to beta-lactamases

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19
Q

What are monobactams effective against, and name the members

A

ONLY effective vs. G- (not G+ or anaerobes)

aztreonam

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20
Q

What group do carbapenes belong to,what bugs do they target, and what is their drawback?

A

beta-lactams

broad spectrum against G- and G+

may be toxic (causes seizures)

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21
Q

What drugs belong to the carbapenems

Study These Flashcards
A

imipenem, ertapenem, meropenem

22
Q

What are the possible side effects of beta-lactams?

Study These Flashcards
A

allergy (pen > ceph > mono)

toxicity [carba (seizures) > ceph (thrombophlebitis) > pen > mono]

23
Q

Mode of action, uses, and side effects of Bacitracin?

Study These Flashcards
A

blocks dephosphorylation of bactoprenol (cell wall inhibitor)

Used topically against G+ (often in conjunction with others)

poorly absorbed, renal toxicity

24
Q

On a scale of 1 to fucking huge, how big is bacitracin?

25
Mode of action and resistance to Glycopeptides?
bind to end of A.A. side chain and block transglycosylation and transpeptidation (cell wall inhibitors) resistance when -ala-lactate is used rather than -ala-ala (chromosomal (vanB) and plasmid (vanA) genes
26
Name the glycopeptide drugs and what they're used against
vancomycin, telavancin used against Staphylococci and Enterococci (not G-)
27
What is the mode of action of cycloserine, when would you use it, and what are the side effects?
D-ala analog that inhibits alanine racemase (cell wall inhibitor) Sometimes used for UTI, 2nd line TB drug neurotoxic
28
What are the Mycobacterium specific drugs, and what are their mode of actions?
isoniazid- inhibits pyridoxine step in mycolic acid synthesis (first line TB drug) ethionamide- same as isoniazid ethambutol- inhibits arabinogalactan synthesis pyrazinamide- activated by Mycobacterium enzyme; inhibits translation which is necessary to restart stalled ribosomes during stress response (and rifampin) (isoniazid, pyrazinamide, ethambutol, rifampin is treatment for TB)
29
What are the mode of action and uses of Polymyxins (colistin)
dissolves phosphatidylethanolamine (cell membrane disruptor) used topically (because toxic), often with bacitracin and neomycin, given as last resort for resistant bugs
30
Mode of action and uses of Daptomycin (cubicin)
cyclic lipopeptide that dissolves in membrane and disrupts membrane potential- ion shuttle (cell membrane disruptor) Used against G+ cocci (MRSA!!), must be given I.V., synergy with B-lactams
31
Mode of action, resistance, and uses of Sulfonamides (Sulfone and Trimethoprim)
inhibit steps in pyrimidine scavenge pathway Resistance: overproduction of PABA, altered enzymes used against Nocardia; synergistic with SxT for UTI, salmonella, shigella
32
Name some Fluoroquinolones and their mode of action
ciprofloxacin, moxifloxacin inhibit DNA gyrase (nucleic acid inhibitors)
33
What are the resistances, uses, and side effects of fluoroquinolones?
resistance: altered DNA gyrase, drug exclusion uses: UTI, G- and G+ infections; 2nd line mycobacterium, pseudomonas side effects: prolonged QT interval
34
Mode of action and uses of Fidaxomycin (Dificid)
targets switch region of RNAp and prevents interaction of RNAp with DNA (nucleic acid inhibitor) used for C. diff colitis (as alternative for vanco and for vanco resistant C. diff)
35
Name some Rifamycin derivatives and their mode of action
rifampin, rifabutin, rifaximin blocks RNA polymerase elongation subunit (nucleic acid inhibitors)
36
Uses, resistance, and side effects of rifamycin
uses: with isoniazid to delay resistance in Mycobacteria; crosses CNS so used for meningitis; blocks assembly of poxvirus side effects: orange sweat and urine
37
Mode of action and uses of Metronidazole
forms a partially reduced complex with ferredoxin and interacts with DNA and breaks DNA strands (nucleic acid inhibitor) uses: antiprotozoal (Giardia); against anaerobic bacteria (Bacteriodes, Clostridium)
38
Name some aminoglycosides and their mode of action
streptomycin, neomycin, gentamycin, tobramycin, amikacin binds to 30S rib and blocks attachment of t-RNA (protein synthesis inhibitor)
39
What are the uses and resistance of aminoglycosides
G- enterics; synergistic with cephalos or pens which facilitate entry of aminoglycosides resistance: altered P12 ribosomal protein, aminoglycosidases, altered permeability
40
Name some tetracyclines and their mode of action
doxycycline, tigecycline inhibit binding of aa-tRNA to A-site of 30S ribosome
41
What are the uses, resistance, and side effects of tetracycline?
rickettsia, chlamydia, mycoplasmas efflux pumps toxicity, dizziness, tinnitus, NEVER USE IN PREGNANCY
42
Name some macrolides and their mode of action
erythromycin, clarithromycin, azithromycin binds rRNA and inhibits translocation (protein synthesis inhibitor)
43
What are the uses, resistance, and side effects of macrolides
G+ and some G- methylation of rRNA prolonged QT interval and increased risk of cardiovascular death
44
Mode of action and uses of lincosamides (clindamycin)
binds to rRNA and inhibits translocation (protein synthesis inhibitor) (same action as macrolides) used against anaerobes (Bacteroides) and anti-malarial (doesn't penetrate CNS; major disruptor of native flora)
45
Mode of action and uses of nitrofurantonin
inhibits 30S (protein synthesis inhibitor) used vs. UTI because it concentrates in urine
46
Mode of action and uses of Mupirosin
inhibits ile-tRNA synthase used topically vs. G+
47
Mode of action and uses of Streptogramins. What common synergy is used?
inhibits 50S (protein synthesis inhibitor) used for VRE and VRSA Synercid = quinupristin + dalfopristin
48
Mode of action and uses of oxazolidinones (linezolid)
inhibits 50S (protein synthesis inhibitor) used for VRE and MRSA
49
Mode of action and uses of methenamine
releases formaldehyde in acidified urine used for UTI
50
What is the mode of action of C10 and BF8
"wake up" persister cells and make then sensitive to antibiotics

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