Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Cellular Week 3 > Antibacterials II > Flashcards

Antibacterials II Flashcards

(49 cards)

Start Studying
1
Q

inhibitors of nuclei acid synthesis?

A

fluoroquinolones

common:
ciprofloxin (cipro)
levofloxacin (levaquin)
moxifloxacin (avelox)
gemifloxacin (factive)

double bonded O and COOH are important

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

fluoroquinolones:
MoA?
killing?
Mechanisms of resistance?

A

MoA - inhibit DNA gyrase and topoisomerase
- FQ’s form a complex with gyrase and topoisomerase IV, blocking DNA rep, resulting in DNA release, chromosomal disruption and cell death

BACTERICIDAL, CONCETRATION DEPENDENT KILLING!
(bigger doses less frequently)

mechanism of resistance: altered target site, efflux

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

fluroquinolones:
spectrum?
uses?
PK/PD?

A

spectrum - BROAD! (gram +, gram -, atypicals, TB)

Uses - RTI, UTI/prostatitis, GI, osteomyelitis, anthrax, TB

PK/PD - excellent oral absorption, tissue penetration (IV to PO switch)
- Al, Mg, Ca, Fe, Zn impair absorption (di/trivalents)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Fluroquinolones:
adverse SE - regular?
black box? (3)

A

GI: n, loose stools, altered taste
CNS: HA, lightheadedness, dizziness, nervousness, insomnia
Skin: photosensitivity

Black box:

  1. tendonitis/rupture, peripheral neuropathy, dysglycemia (blood glucose), QTc prolongation
  2. generally not recommended in children <18 yr or pregnant women unless benefit is greater than the risk (damage growing cartilage and cause arthropathy - disease of the joints)
  3. FDA (2016) should be reserved for complicated infections
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Inhibitors of 50s ribosomal subunit

A
  • MACROLIDES (erythromycin, clarithromycin, AZITHROMYCIN, fidamicin); Ketolids (telithromycin)
  • OXAZOLIDINONES (LINEZOLID, TEDIZOLID)
  • LINCOSAMIDES (CLINDAMYCIN)
  • CHLORAMPHENICOL
  • streptogramins (quinopristin-dalfopristin)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

inhibitors of the 30s ribosomal subunit

A

-AMINOGLYCOSIDES (GENTAMICIN, TOBRAMYCIN, amikacin, streptomycin, plazomicin)

  • TETRACYLCINES (tetracycline, DOXYCYCLINE, minocycline, omadacycline (2018), sarecycline (2018)
    - glycylcyclines (tigecycline)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

chloramphenicol, macrolides, clindamycin, and streptogramins bind to the 50s subunit and block…

A

peptide bond formation!!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

the tetracyclines and aminoglycosides bind to the 30s subunit and prevent….

A

binding of the incoming charged tRNA unit!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

macrolides/ketolides structure is a ….

important one?

A

macrocyclic lactone ring!

ex. azithromycin (zithromax)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Macrolides inhibit protein synthesis…

killing?

A

usually bacteriostatic, concentration-independent killing; anti-inflammatory

block elongation and exit of peptides from 50s ribosomal subunit tunnel; produces a defective intermediate, unable to fold correctly

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

macrolides resistance…
low level?
high level?

A

low level - efflux pump

high level - target site modification

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

macrolides spectrum?

A

BROAD
gram +, neisseria, treponema
drug of choice for atypicals!!!! (mycoplasma, legionella, chlamydia)

**good for intracellular bad

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

macrolides pharmacology?

A

erhythromycin - many formulations; erratic absorption, acid labile, excreted in bile; take EMs with food to decrease GI upset

clarithryomycin, azithromycin - better absorbed, higher tissue levels and longer half life!!!!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

clinical use of macrolides?

A

ALTERNATIVES IN PREGNANCY AND PEN ALLERGY!!!

STI - CHLYAMYDIA (azithromycin), gonorrhea!!!!
RTI - phyrungitis, otitis, CAP (azithromycin)!!!!
Treating gastroparesis - stimulates motilin receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Macrolide adverse effects?

A

GI - higher than most classes!!

  • erythromycin - 50% have bloating, cramping, n, d
  • somewhat less with clark-, lowest with azithromycin

MAY INCREASE QTc INTERVAL! - torsades, block cardiac K+ channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

erthyromycin drug interactions?

A

VERY POTENT CYP 3A4 INHIBITOR!
(theopylline, warfarin, triazolam, carbamazepine, cyclosporine, simvastatin, lovastatin, sildenafil, many others)

  • erthyromycin > clarithromycin > azithromycin
  • few or no drug interactions with azithromycin!!!
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

oxazolidinones (linezolid [zyvox, IV/PO]; tedizolid [sivextro, IV/PO])

relevant chemistry?
MOA?
Killing?
spectrum?
therapeutic use?
A

Relevant chemistry - totally synthetic; originally developed as a MAOI

MoA - inhibits early protein synthesis at initiation complex
- primarily BACTERIOSTATIC, TIME DEPENDENT KILLING

spectrum - narrow (gram +)

use - alt to vanco for MRSA; also used for VRE (vanco resistant enterococci)!!!!!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

linezolid and tedizolid (oxazolidinones) Adverse side effects?

A

GI (most common)!!!
SKIN RASHES - dose related

hematologic (cytopenias; weekly CBC)
neuropathy, optic neuritis
SEROTONIN SYNDROME: a few cases in pts on SSRIs ANTIDEPRESSANTS due to inhibition of MAO by linezolid (FDA WARNING!)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Lincosamides ex.?

A

clindamycin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q 
lincosamides: clindamycin
MoA?
killing?
MoR?
Spectrum?
Study These Flashcards
A

MoA - binds to 50s, inhibits protein synthesis

BACTERIOSTATIC, TIME-DEPENDENT!

MoR - altered target, decreased binding, efflux

spectrum - BROAD. ; gram positive anaerobes

21
Q

common uses of lincosamides (clindamycin)

Study These Flashcards
A

SKIN, SOFT TISSUE, BONE (HIGH BONE LEVELS), INHIBITS TOXIN PRODUCTION
alternative in PEN-ALLERGY!
toxoplasmosis, pneumocytosis
topical for acne, rosacea

22
Q

adverse effects of lincosamides (clindamycin)

Study These Flashcards
A

diarrhea, C.diff colitis

hypersensitivity, rash

23
Q 
chloramphenicol
Moa?
killing?
spectrum?
therapeutic uses?
PK?
Study These Flashcards
A

Moa: reversibly binds to 50s ribosomal subunit preventing aa from being transferred to growing peptide chain

bacteriostatic for most

BROAD SPECTRUM! many trap +, - aerobes, anaerobes

use - alt in drug allergy!!! (meningitis, brain abscess)

PK - metabolism - extensive hepatic glucoronidation!! drug interactions too

serum monitoring - therapeutic - 15-20 ug/ml

24
Q

chloramphenicol adverse effects? (3)

Study These Flashcards
A
  1. reversible bone marrow suppression (anemia, leukopenia, thrombocytopenia) - concentrations >25 ug/ml
  2. aplastic anemia
    idosncratic - NOT CONCENTRATION RELATED!
    may occur weeks to months after completing therapy - CBC twice weekly!
  3. Gray Baby syndrome!!!
    - circulatory collapse, cyanosis, acidosis, myocardial depression, coma, death
    - newborns lack effect glucoronic acid conjugation mechanisms to metabolize; associated with serum lvls >50ug/ml
25
aminoglycosides ex.?
``` gentamicin tobramycin amikacin streptomycin plazomicin ```
26
aminoglycosides chemistry? bacteriocidal!
hexose ring with various amino sugars attached by glycosidic bonds water soluble, polar active in alkaline pH (put pus is acidic)
27
``` aminoglycosides MoA? killing? MoR? spectrum? ```
MoA - irreversibly binds to 30s ribosome RAPIDLY CIDAL, CONCENTRATION DEPENDENT KILLING WITH LONG PAE - post antibiotic effect? MoR - enzyme modification, altered 30s efflux spectrum - primarily gram neg; SYNERGISTIC ACTIVITY with cell wall agents for GRAM POS!
28
``` aminoglycosides... kinetics? dosing (normal renal)? monitoring? uses? ```
kinetics: poor absorption, limited tissue, distribution, not metabolized, 100% renal elimination dosing (normal renal): high dose, extended interval REQUIRES SERUM CONCENTRATION MONITORING uses: mainly in combination with other agents: severe gram neg infections, synergy with gram pos infections, TB!
29
aminoglycoside toxicity (3)
1. nephrotoxicity!! - ACCUMULATION IN THE PROXIMAL TUBULE (SATURABLE) - USUALLY GRADUAL, MILD, REVERSIBLE - INCREASE IN SCR OR TROUGH ACCUMULATION AFTER 5-7 DAYS - requires dosage modification or d/c - increased risk with other nephrotoxins 2. ototoxicity - 8th nerve damage, destruction of type II hair cells - VESTIBULAR (vertigo, ataxia) and HEARING (high frequency initially) - irreversible 3. NEUROMUSCULAR BLOCKADE! - associated with rapid, bolus infusion in post surgical pts, neonates (calcium salts can reverse)
30
tetracyclines and glycylcyclines primary agents? new in 2018?
primary agents: tetracycline, DOXYCLCINE, minocycline, TIGECYCLINE New in 2018: eravacycline, omadacycline, sarecycline
31
tetracyclines and glycylcyclines ``` MoA? killling? spectrum? active against what? uses? ```
MoA: - bind to 30s ribosome, blocking formation of the initiation complex (same as amino glycosides) - tigecycline has 5 fold > binding to overcome resistance, not a substrate for efflux pump! bacteriostatic, time dependent!! BROAD SPECTRUM! Tigecycline and new 2018 ervacycline and omadacycline active against many MDR isolates!! uses: MANY TICK BORNE INFECTIONS!, travelers diarrhea, RTI, STI
32
tetracyclines and glycylcyclines AE?
GI: n/d, epigastric distress PHOTOSENSITIVITY CONTRAINDICATED IN CHILDREN <8YR, PREGNANCY, BREAST FEEDING - gray-brown to yellow discoloration of teeth and enamel hypoplasia in children; retards bone growth!!!! TIGECYCLINE BOXED WARNING (2013) - INCREASED RISK OF DEATH!!!
33
tetracycline and glycylcyclines: drug interactions
Ca, Mg, Al, Fe, NaHCo3, dairy products impair absorption!! (separate doses by > 2h) MAY DECREASE THE EFFECTS OF ORAL CONTRACEPTIVES! may potentiate effects of oral anticoagulants
34
Sulfonamides and trimethoprim (a pyrimidine) are inhibitors of what? killing??? blocks what?
folate inhibitors synergisitc, bacteriacidal combination (NEVER USED ALONE! STATIC AND GREATER RESISTANCE) BLOCKS PURINE PRODUCTION AND NUCLIC ACID SYNTHESIS!
35
sulfonamides and trimethoprim... spectrum? use?
broad spectrum: many gram pos, neg, pneumocystis, atypical mycobacteria, plasmodium, toxoplasma common use - UTI!
36
trimethoprim/ sulfamethoxazole... PK?
``` excellent absorption widely distributed hepatic metabolized (acetylation, glucuronidation) long half-life ```
37
trimethoprim/ sulfamethoxazole... ADR? Warning? drug interactions?
ADR: - GI, SKIN (rash, urticaria, photosensitivity) - hypersensitivity (stevens-johnson, TEN) - hematologic (bone marrow suppression) - renal (hyperK+, AKI - acute kidney injury) WARNING: - should NOT be used in 3rd trimester or newborns (KERNICTERUS) - bilirubin displacement from plasma proteins leading to brain damage drug interactions: CYP 2C8/9 INHIBITOR! -may increase effects of sulfonylureas, warfarin, anticonvulsants, cyclosporine, methotrexate
38
nitrofurantoin MOA? resistance? spectrum? indications?
moa - inhibits several enzyme systems, including acetyl coA, inhibiting metabolism resistance - low spectrum - PRIMARILY GRAM NEG!! (E.COLI) indications - UTI (CYSTITIS)
39
nitrofurantoin | PK?
WELL ABSORBED! (macrodantin) - MACROCRYSTALS ABSORBED SLOWER, ALLOWING FEWER GI EFFECTS! - renal dose adjustment - do not use CrCl <40ml/min - Mg-containing antacids decrease absorption!!
40
nitrofurantoin ADR?
- GI - RASH - PULMONARY (<1/100,000) acute pulm: REVERSIBLE HYPERSENSITIVITY phenomenon gradual onset of nonproductive cough, dyspnea, interstitial infiltrates on CXR; possible eosinophilia rapid improvement after drug D/C ``` chronic pulm: S/Sx similar to acute occurs after 1-6 mos of therapy usually improvement after drug D/C IRREVERSIBLE FIBROSIS, FATALITIES HAVE OCCURRED (VERY RARE) ```
41
fluoroquinolones common SE?
GI CNS stim photosensitivity warning - cartilage malformation, tendon rupture, neuropathy, prolonged QT, drug interactions
42
macrolides common SE?
GI warning - prolonged QT drug interactions
43
lincosamides (clindamycin) common SE?
GI
44
chloramphenicol common SE?
anemia (conc-related and idiosyncratic aplastic anemia) bone marrow suppression gray baby syndrome
45
oxazolidinones (linezolid) common SE?
GI CNS myelosuppression
46
aminoglycosides common SE?
nephrotoxicity, ototoxicity
47
tetracylces/glycylcyclines common SE?
``` GI rash/allergy photosensitivity superinfection warning! not in children - athropathy (disease of joints), teeth discoloration, drug interactions ```
48
sulfonamides common SE
``` GI rash/allergy photosensitivity myelosuppression warning!! do not use in third trimester or newborns, drug interactions ```
49
nitrofurantoin common SE?
GI rash pulmonary

Cellular Week 3 (21 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions