ID: Quinolones, Urinary Antiseptics, and Anti-mycobacterial agents Flashcards

1
Q

*Ending for fluoroquinolines

A

-floxacin or -oxacin

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

*first gen quinolone? And its spectrum

A
  • nalidixic acid

- narrow spectrum for gram-

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

*what was the quinolone class modified to? Spectrum? Resistance? Kinetics?

A
  • fluoroquinolones
  • larger spectrum vs quinolones
  • more effective against resistance vs quinolones
  • improved kinetics vs quinolones
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

*Pros to Floroquinolones (4)

A
  • highly effective
  • broad spectrum
  • high PO bioavailability
  • large volume of distribution
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

*cons to floroquinolones (3)

A
  • widespread use had lead to resistance
  • serious adv eff can occu
  • multiple drug-drug interactions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

*generally when do we use fluoroquinolones?

A

-when benefits outweight the risk

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q
  • list the second gen Fluoros + routes

* spectrum

A
  • Ciprofloxacin—PO, IV, ophthalmic, otic
  • Ofloxacin—PO, ophthalmic, otic

Spectrum:

  • increased acitivty
  • aerobic gram- bacteria **
  • *cipro has weak coverage aganst strep pneumoniae

Ofloxacin: enhanced coverage of staph and strep

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q
  • List the third gen fluoros + routes

- spectrums

A

-levofloxacin—PO, IV

Spectrum:
-same as second gen
+
better gram+ coverage and atypical organisms

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

*list the fourth gen Fluoros + routes

A
  • Gatifloxacin—ophthalmic
  • Delafloxacin—PO, IV
  • Moxifloxacin—PO, IV, ophthalmic
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

*two enzymes that fluoros target?

A
  • DNA gyrase: found in gram-

- Topoisomerase IV inhibition: in gram+

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

*action of fluoros on bacteria— bacteriostatic or cidal

A

-cidal bcause it causes cell death

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

*MOA fluoros

A

-targets two enzymes: DNA Gyrase and Topoisomerase IV inhibition
DNA gyrase—removes excess positive supercoiling in the DNA helix (gram-)
T. IV Inhib—affects separation of interlinked daughter DNA molecules (gram+)

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

*Spectrum for fluoros:

A
  • aeriobic gram +
  • aerobic gram-
  • atypical: chlamydia, Legionelle, Mycoplasma
  • anaerobes
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

*should fluoros be used for tx of uncomplicated infecetions? Why?

A
  • NO
  • due to adverse effects—also when alternative agents with lower toxicity profiles are available
  • in 2016 FDA recommended this
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

*ex of uncomplicated infections that should not be tx with fluoros

A
  • acute rhinositis
  • uncomplicated cystitis
  • acute bronchitis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

which is the best fluoro for aerobic, gram-, pseudomonas

  • UTI
  • Pyelonephritis
  • gastroenteritis
  • otitis
  • eye infections
A

Ciprofloxacin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Spectrum for Ciprofloxacin

A

aerobic gram-
Pseudomonas
*not much gram+ coverage

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

indications for Cirpofloxacin

A
UTI 
Pyelonephritis 
gastroenteritis 
Otitis--drops 
eye infections 

***much better for gram- vs gram+

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

which has better gram + coverage:

-Ciprofloxacin or Levo/Moxifloxacin

A

Levo and moxi

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

spectrum and indications for Levofloxacin

A

spectrum:
* *more gram + coverage vs cipro
* gram-
* gram+
* anaerobes
* mycobacterium
* respiratory infections: strep, hamepholius, and moraxella

  • 2nd DOC for mycobacterium TB
  • UTI
  • Pyelonephritis
  • pneumoina
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

which fluroquinoloine is best for anaerobes, esp gram+

A

Moxifloxacin

22
Q

Kinetics for Fluoros

  • abs?
  • wht reduces absoprtion
  • where are [ ] high
  • dose adjustments?
  • drug-drug interactions
A

Absorption: good after PO— bioavail of <90%

  • zinc *iron *sucralfate *Ca can reduce absoprtion
  • [ ] are high in bone, CNS, urine, prostate tissue, lungs, kidney
  • most excreted renally–needs dose adjustment EXCEPT FOR MOXIFLOXACIN

Ciprofloxacin is a CYP450 INHIBITOR

23
Q

SE fluoros (8)

A
  • generally well tolerated*
    but. .. when cmpared to other ABX:
  • GI upset more common
  • CNS: HA, dizziness, sleep issues are more common
  • Incidence of C. Diff is more common
  • small risk of photoxicity
  • hypersensitivity
  • dysglycemia: hyper or hypo
  • periph neuropathy

BBW: Tendinopathy*****

24
Q

Contra for fluoros (4)

A

hx of Aortic aneurysm
pregnancy/BF
<18
avoid in Myasthenia gravis

25
Q

which fluoroquinolone is CYP450 inhibitor

A

Ciprofloxacin
*if given with those other drugs, will increase their serium [ ]
EX: warfarin, theophylline, caffiene,

26
Q

Sulfonamines

  • new/old drug?
  • moa
  • spectrum
  • how does resistance occur
  • contras (3)
A

old drug

MOA: folate antagonists

  • compete with PABA to prevent production of dihydrofolic acid
  • *bacteriostatic

spectrum:
+ and -

resistance:
- when bacteria are able to obtain folate from the environment, plasmid transfer or random mutations

contra:
* pregnant PT bc of kernicterus
* newborns <2 MO
* pt on methenamine

27
Q

Kinetics for Sulfas

  • abs
  • penetrates?
  • excretion
A

*well absopred EXCEPT FOR SULFASALAZINE

  • penetrates CNS, and placenta
  • excretion: urine, breastmilk, have to renally dose
28
Q

ADV rxn to sulfas (5)

A
  1. hypersensitivity
  2. Crystalluria
  3. Hemolytic anemia
  4. Kernicterus
  5. Inhibition of CYP P2C9
29
Q

Trimethoprim

  • MOA
  • spectrum
  • potency
  • indications
  • se (2)
A

MOA:

  • alone or combo with Sulfamethoxazole (MC used in combo)
  • potent inhibitor of dihydrofolate reductase–blocks folic acid production–abnoral cell function in bacteria

Spectrum:
*same as sulfonamide BUT 20-50X more potent

INd:

  • UTI
  • prostatitis

SE:

  • hyperK
  • FOlic acid deficiency
30
Q

pharmkinetics of Trimethoprim

A

-rapidly absorbed after oral admin

  • good penetration in acidic fluids– like vagina and prostate
  • good CNS penetration
31
Q

Cotrimoxazole

  • route
  • dosing
  • adv rxn
A

IV, PO

spectrum: better antimicrobial activity together versus alonE AKA synergistic****
* renal dosing needed

Adv Rxn:

  • n/v
  • skin rash
  • hematologic toxicity
  • hyperK
32
Q

Silver Sulfadiazine (Silvadene)

  • spectrum
  • indications
A

INDS: topical

  • superficial skin infections
  • burns

***silver natural superficial abx

Gram +/- bacteria

33
Q

Sulfacetamide

-indications (2)

A
topical 
-bactericidal 
-gram+/- 
Indications: 
-blepharitis 
-ocular infections
34
Q

Methenamine

  • MOA
  • only effective when?
  • indications
  • contra 2
  • adv rxn
A

MOA

  • hydrolyzed to ammonia + formaldehyde–>denatures protein and nucleic acid–>cell death
  • **bacteriocidal
  • *only effective if urinary ph is acidic

INDS:
*chronic suppression of frequent UTIs

adv rxn: gi upset

contra

  • sulfonamide tx
  • hepatic dysfunction
35
Q

Nitrofurantoin

  • moa
  • indications
  • adv rxn (3)
  • contras (3)
A

MOA: inhibits DNA and RNA synthesis
*bactericidal

Indications: UTI caused by:

  • e. coli
  • enterococcus
  • Klebsseila
  • staph

adv rxn:

  • N/v/d
  • rare: drug induced liver injury, periph. neuropathy

contra:
- renal dz
- last 30 days of pregnancy
- elderly

36
Q

Mycobacteria

  • explain cell wall
  • creates?
A

highly lipid cell wall—- so does not retain the normal gram stain…
**acid fast staining necessary

Acid-fast bacilli

creates granulomatous dz and serious infections (TB)

37
Q

Mycobacterium avium and intracellulare

  • cause?
  • which population
A

mainly affects the immunocomp–HIV

Pulmonary dzs

38
Q

Mycobacterium Tuberculosis

  • growth rate
  • treatment length?
  • tx? Acute
A

slow growing… so long duration of treatment

RIPE or RIPS
x2MO: all four drugs
x4 more MO: rifampin and Isoniazid
x6MO total drug tx

Rifampin
Isoniazid
Pyrazinamide
Ethambutol (or streptomycin)

39
Q

Rifamycins

  • list the drugs
  • MOA
  • why is it not given alone?
A

Rifampin
Rifabutin
Rifapentine

MOA:
*blocks RNA transcription–bacteriCIDAL

*not given alone bc of resistance

Indications:

  • TB
  • mycobacterium avian complex
  • Mycobacterium Leprae (leprosy)
40
Q

Pharmkinetics of Rifampin

  • abs
  • distribution
  • metabolism
  • interactions
  • adv rxn
A
  • adequately absorbed
  • well distributed in all body fluids and organs–poorly in CNS
  • enterophepatic recycling
  • CYP 450 Inducer–decreases [ ] of other drugs

Adv Rxn:

  • metabolites can turn urine, tears, sweat organge/red
  • flu like s/s

contra:
- caution with heptatic dz PT
- concomitant hepatotoxins

41
Q

Rifabutin

-indications

A

better to give to PT’s for tx of TB who are also undergoing HIV treatment

**because it is a less potent inducer of CYP 450

42
Q

Rifapentine

  • indications
  • T 1/2?
A

Latent TB

VERY long half life

43
Q

Isoniazid

  • MOA
  • abs
  • penetrates?
  • indication
  • SE
A
  • prodrug
  • when activated MOA: inhibs mycolic acid–>disrupts cell wall
  • **only works specifically for M. tuberculosis

IND:
*TB only

abs: readily via PO on empty stomach

penetration:

  • good tissue pen
  • good CNS

SE:

  • potentially fatal hepatitis
  • periphereal neuropathy/parethesia caused by peroxidase deficiency—— to prevent this give B6**
  • Seizures=common
44
Q

cannot have fattys meals when administering wht medication?

A

Isoniazid

45
Q

Pyrazinamide

  • MOA
  • inds
  • SE 3
A

MOA: unclear

Distribution:

  • CNS
  • tissues

INDS:
-acute TB… only for the first two MO.. then discontinued

SE:

  • hepatitis and Hyperuricemia (avoid in PT with gout)
  • photosensitive dermatologic rash
  • arthralgias
46
Q

Ethambutol

  • MOA
  • spectrum
  • distribution
A

Cell wall inhibitor of Mycobacteria
**bacteriostatic

Narrow spectrum

CNS penetration is variable
but generally good distribution

SE:
-optic neuritis–esp in PT with renal dz

-caution in gout bc it can elevate uric acid

47
Q

what to do before putting patient on ethambutol tx?

A

test visual acuity and color

48
Q

Dapsone

  • structure
  • uses
  • SE
  • abs
A

structurally sim to sulfonamides
-MOA inhibits folate synthesis, has anti-inflamm., anti-protozoal, antimicrboial effects

*bacteriostatic

abs:
* good levels in skin
* well abs

INDS:

  • mycobacterium leprae
  • Pneumocyctis Jirovecci Pneumonia (PCP)
  • dermatitis herpetiformis
  • malaria

SE:

  • severe hemolytic anemia *esp in pt with G6PD
  • peripheral neuropathy
49
Q

Clofazimine

  • moa
  • penetration
A

MOA:

  • binds to DNA
  • Bactericidal against: M. leprae, Mycobacterium TB, and non TB mycobacterium

penetrates tissues but NOT CNS

SE:

  • photoxicity
  • brownish/black skin discoloration during tx
  • QT»»
  • GI upset
50
Q

what is the triple tx for leprosy and how long

A

Dapsone
Clofazimine
Rifampine
for 12 MOnths