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Foundations 5 > Antibiotics > Flashcards

Antibiotics Flashcards

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1
Q

Beta lactam structure

A

Analogs of D-alanyl-D-alanine

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2
Q

Beta lactam cidal and or static

A

Cidal - inhibits cell wall synthesis and more susceptible to lysis

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3
Q

Mechanism of Beta Lactams

A

Inhibit Transpeptidases (PBPs) that remove one alanine from a peptidoglycan polymer and cross link other alanine to antoher adjacent polymer

Form covalent bonds

Can’t form rigid 3D sturcutre

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4
Q

Regular, ES, anti staph, Anti psueod penicillins and routes

A

Penicillin G (I)
Amoxicillin (O)
Nafcillin (I)
Peperacillin (I)

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5
Q

Resistance to Beta lactam and example of each

A

beta lactamases cleave lactam ring (Staph aureus)

Mutated PBPs have decreased binding affinities (MRSA)

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6
Q

Each lactamase

A

Hydrolyzes a different set of beta-lactams

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7
Q

Penicillin spectrum

A

Braod

+,-, anaerobes, spirochetes

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8
Q

Regular pen coverage

A

Good for anaerobes and spirochetes but not gram -

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9
Q

ES penicillins coverage

A

Improved gram - coverage

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10
Q

Anti staph penicillins coverage

A

Best for Non-MRSA staph

Only strand resistant to some beta-lac

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11
Q

Anti pseudo pen coverage

A

Improved of P aeruginosa and other gram - bacilli

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12
Q

How to ES and anti pseudo penicillins get into gram negative bacteria

A

Have side chains that can go through porins…these are + charged chains

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13
Q

Pen absorption

A

Oral bioavailability is poor

Amoxicillin is good for oral

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14
Q

Pen distribtuion

A

Do not enter bone or CNS

G used for neurosyphilis

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15
Q

Pen elimination

A

Rapid renal elimination so short duration

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16
Q

Pen dosing

A

Most in milligrams
G in IUs
V in either mg or IUs

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17
Q

Adverse effects of penicillins

A

Rare

Superinfections (more likely with broader)
Serizures (at very high levels, caution with epileptics)
Skin rashes (ES can cause non-allergic rash with mono)

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18
Q

What is common is penicillins

A

Hypersensitivity reactions…most serious being anaphylaxis and least being skin rashes

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19
Q

All penicillins cross react

A

With each other and at a lower frequency with other beta lactams

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20
Q

Cephalosporins we need to know and generation

A

1 - cefazolin (I)
3 - Ceftiaxone (I)
4 - Cefepime (I)

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21
Q

Ceph spectrum and how different than penicillins

A

+, - , anaerobes, spirochetes

better at gram - than pen
More stable against lactamases

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22
Q

Cefazolin use

A

Highest against gram + and anaerobes

Wound infections and surgicial prophylaxis

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23
Q

Ceftriaxone use

A

More serious gram - bacilli

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24
Q

Cefepime use

A

Similar to ceftriaxone but more psuedomonas activity

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25
Ceph resistance
Lactamases (decreased with later generations)
26
ESBLs
On some strains of gram - bacilli...resistant to 3rd gen cephalosporins
27
Ceph absorption
Oral are there for 1-3 gen
28
Ceph elimination
Most are short and secreted by kidney | Ceftriaxone undergoes biliary elimination and longer T1/2
29
Ceph deistribtuoon
Moves to restricted better than pen
30
Ceph toxicity
Hypersensitivity (can use with pts who have a delayed penicillin reaction) Superinfections (with broader spect) Nephrotoxicity (rare)
31
Carbapanems we need to know
Meropenem
32
Carbapenems are improvement because
Very broad spectrum and insentivie to lactamases that destroy cephs and pens
33
Most important use for carbapenems
Difficult to treat gram negative bacteria (entero, klebsiella)
34
Carbapenems spectrum
+, -, anaerobes
35
Carb resistance
Typically due to non-lactamase mechanism | Recent spread of metallo beta lactamases in Klebsiella pneumoniae
36
Cilastatin
Used with imipenem to decreased effect of renal dehydropeptidase
37
Absorptions Carb
Only injection
38
Distributon Carb
Go to bone, CNS, restricted compartments well
39
Adverse effects of Carb
Seizures...decrease valproate levels, whcih is important anti-epileptic drug
40
Beta lactamase inhibitors
Clavulanic acid | Bind to catalytic site and extend spectrum of beta lactams
41
Augmentin
Amox and clavulanic acid
42
Augmentin example useful in
Beta-lactamase producing strands of gram-negative bacteria
43
Glycopeptide example and route
Vancomycin (I,O)
44
Vancomycin strucutre
Large and hydropihlic
45
Vancomycin mechanism
Inhibits transglycosylase that attaches new monomers to polymer...earlier step than beta-lactams
46
Vanco spectrum
+ and anaerobes...totally insensitive to lactamases and PBPs
47
Vancomycin used for
MRSA...pen still preferred for other S aureus strains | Severe C dif induced diarrhea
48
Resistance to vancomycin
High level - D-lactate replaces bidning sites D-alanine Low level - Vancomycin creep due to increased production of peptidoglycan
49
Vancomycin absorption
Oral form not absorbed but used for GI infections
50
Vanco elimination
Renal
51
Distribution of Vanco
Penetrates BBB when inflamed
52
Vanco adverse effect
Nephrotoxicity
53
Red Man Syndrome
Histmaine release during infusion of Vancomycin...prevent by slow infusion and pre-admin of antihistamines Hypotension and vasodilation
54
Protein suppression is normally
Bacteriostatic...can survive by going dormant
55
Which bind to 30S and 50S subunits
30 - aminoglycosides | 50 - lincosamides and oxazolidinones
56
Linezolid inhibits
Assembly of 70S complex
57
Aminoglycosides inhibit
Early elongation of new amino acid binding to the A site
58
Lincosamides inhibit
Late elongation - bond formed between existing peptide at P site and new amino acid at A site
59
Aminoglycoside example and form
Gentamicin (I,T)...bactericidal
60
Aminoglycoside structure
Polycations...sugars with glycosydic links
61
Aminoglycoside mechanism
Binds to and changes conformation of the 30S subunit and causes miscoding...miscoded protein disrupt membrane
62
aminoglycoside type of killing
Concentration dependent killing with a long post-antibiotic effect
63
Resistance to aminoglycoside
Acetylase inactivates
64
Aminoglycoside scope
Some positive, more negative No anaerobes because transport dependent on membrane potential
65
Aminoglycoside absorp
Not absorbed orally
66
Aminoglycoside distribution
Dont enter restricted well
67
Aminoglycoside elimination
Renal so short T1/2
68
Main use of aminoglycosides
Hospital setting for serious Often combined with beta lactams
69
Aminoglycoside adverse effects
Nephrotoxicity (reversible) Ototoxicity (partially reversible) Vestibular toxicity (partially reversible at best)
70
How can you elimate nephrotoxicity of aminoglycoside
Keep trough concentrations low and avoid other nephrotoxic drugs
71
Dosing of aminoglycosides
Once daily allows peaking of the concentration so more killing and saturation of renal uptake 3 times daily is other way
72
Lincosamide example and route
Clindamycin (I, O, T, vaginal)
73
Clindamycin routes and why
Oral and injection dosage for systemic Topical for acne vulgaris Vaginal for bacterial vaginosis
74
Clindamycin spectrum
Gram positive and anaerobes...especially anaerobes
75
Clindamycin absorp
Very good oral
76
Clindamycin distribution
Very good except CNS...good for bone
77
Clindamycin elimination
Hepatic oxidation...in feces for long time
78
Clindamycin adverse effects
Diarrhea, thrombocytopenia...most likely to cause C dif
79
Clindamycin most useful as
Beta lactam alternative for treating anaerobic infections...also for some S aureus infection
80
Oxazolidinone example and route
Linezolid (I,O) - cidal or static depnding
81
Resistance to Linezolid
Binding site mutation or methylation
82
Linezolid spectrum
Gram positive only...good for multi drug resistant gram + cocci
83
Linezolid side effects
Mild to moderate thrombocytopenia Peipheral neurotixicity sometimes Serotonin syndrome
84
Linezolid absorption
Excellent oral
85
Distribution of linezolid
Well distributed including CNS
86
Linezolid elimination
Mostly through non-enzymatic hepatic oxidation
87
Sulfonamides example, route, and what they mimic
Sulfamethoxazole (I,O)...mimics PABA | Trimethoprim (I, O, T) - acts on DHFRs...mimics Folate
88
Human vs bacteria - folate
Bacteria only have dihydropteroate synthase that sulfonamides inhibit Both have DHFR that trimethoprim acts on
89
Folates needed for
Synthesis of nucleosides and nucleic acids
90
Why use SMX-TMP
Similar kinetics and less reistance Cidal when given together
91
SMX-TMP spectrum
+, -, intracellular
92
Uses of SMX-TMP
Urinary tract and community acquired MRSA
93
Resistance to SMX-TMP
Mutated sulfonamide binding site
94
Sulf absorp
Good oral
95
Sulf elimination
Both hepatic and renal...get concentrations in urine
96
Sulf distribution
Good into restircted compartments like CNS | Some bind to albumin
97
Sulfonamides and pregnancy
Neonates have large amounts of bilirubin...sulfonamides compete with binding to albumin freeing bilirubin...leads to encephalopathy
98
Sulfonamides toehr side effects
Crystal in urine...prevent with fluids Hemolytic anemia Hypersensitivity
99
Don't use trimethoprim if
Patient has folate definiciency induced anemia
100
Stevens-Johnson syndrome
Most serious reacton to SMX-TMP

Foundations 5 (13 decks)

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