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.► FARMACOLOGIA CLÍNICA - JP > Good For > Flashcards

Good For Flashcards

1
Q

Natural Penicillins
Penicillin G, V
Good for

A

Syphilis

  • particularly neurosyphilis
  • penicillin G is drug of choice

Susceptible streptococcal infections

  • pharyngitis
  • endocarditis
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2
Q

Antistaphylococcal Penicillins Good for

A

Infections caused by MSSA

  • endocarditis
  • skin/soft-tissue infections
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3
Q

Aminopenicillins
Amoxicillin, Ampicillin
Good for

A

Ampicillin is drug of choice for susceptible Enterococci:

  • E. faecalis (almost always susceptible)
  • E. faecium (often resistant)

Any beta-lactam has to be combined with an aminoglycoside to achieve bactericidal activity against Enterococci
-should be done in serious infections like endocarditis

Alternative regimen for UTIs in pregnant women because eliminated renally

  • category B
  • resistance to E. coli very high (perform susceptibility testing)
  • always perform follow-up cultures (asymptomatic bacteruria dangerous for pregnant women)

Infections caused by susceptible:

  • GNRs
  • Enterococci
  • Streptococci

Used infrequently in complicated nosocomial infections
-resistance among GNRs is prevalent

Amoxicillin frequently prescribed for infections of upper respiratory tract:

  • Streptococcal pharyngitis (strep throat)
  • Otitis media (ear infection)
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4
Q

Penicillin/BL-inhibitor Combos

Good For

A

Empiric therapy of nosocomial infections
-particularly nosocomial pneumonia (not aminopenicillin combinations)

Have activity against aerobes and anaerobes so good empiric choice for mixed infections

  • intra-abdominal infections
  • diabetic ulcers
  • aspiration pneumonia

Amoxicillin/Clavulanate

  • upper and lower respiratory tract infections (when BL-producing organisms found/suspected)
  • useful for UTIs (when resistance to other drugs seen; should not be given for a short 3 day course as with FQ or SMX/TMP

Sulbactam

  • useful activity against A. baumannii (highly resistant GNR that causes nosocomial infections)
  • high doses of ampicillin/sulbactam can be used
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5
Q

1G Cephalosporins

Good For

A 
Skin and skin structure infections 
Surgical prophylaxis
-most common indication in the hospital 
-no more than 1 dose
Staphylococcal bloodstream infections 
Osteomyelitis 
Endocarditis 
-caused by MSSA

Should not be used in CNS infections

  • may not cross the BBB
  • Antistaphylococcal penicillins do cross BBB
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6
Q

2G Cephalosporins

Good For

A

Upper respiratory tract infections
Community acquired pneumonia
Gonorrhea

Do not cross the BBB

Cephamycins

  • cefmetazole, cefotetan, cefoxitin
  • active against many anaerobes in GI tract
  • often used for surgical prophylaxis in abdominal surgery
  • resistance increasing in B. fragilis group infections (limit duration after surgery; if infection develops, use BL-inhibitor combination or Gram negative agent + Metronidazole)
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7
Q

3G Cephalosporins

Good For

A 
Lower respiratory tract infections
Pyelonephritis 
Nosocomial infections
-ceftazidime 
Lyme disease
-ceftriaxone 
Meningitis 
Gonnorhea 
Skin and skin structure infections 
Febrile neutropenia
-ceftazidime

Useful for treatment of CNS infections

  • ceftriaxone, cefotaxime, ceftazidime cross the BBB
  • ceftazidime poor choice for community acquired meningitis (S. pneumoniae predominates)

Gonorrhea

  • ceftriaxone is drug of choice
  • 250mg IM one time dose
  • should receive azithromycin also (empiric therapy for chlamydia and may reduce emergence of ceftriaxone resistance)

Ceftriaxone

  • effective for UTIs (has dual elimination: renal (does not need to be adjusted for renal dysfunction) and biliary)
  • higher doses for MSSA (2-4 grams per day), particularly invasive infections
  • once daily except for meningitis (2g IV q12H) and vancomycin +/- ampicillin
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8
Q

4G Cephalosporins
Cefepime
Good For

A

Febrile neutropenia
Nosocomial pneumonia
Postneurosurgical meningitis
Other nosocomial infections

Although indicated for UTIs and LRTIs, it is overkill for most community acquired sources of these infections

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9
Q

Ceftaroline

Good for

A

Approved for:

  • complicated skin and soft tissue infections
  • community acquired pneumonia

Successful in case series and retrospective studies for:

  • bloodstream infections
  • endocarditis
  • meningitis
  • osteomyelitis
  • hospital acquired pneumonia
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10
Q

Cephalosporins/BL-inhibitor combinations

Good For

A 
Both:
Multidrug resistant Pseudomonas infections
Mixed aerobic/anaerobic infections
ESBL producing organisms
Intra-abdominal infections

Ceftazidime/avibactam:
Carbapenem resistant Enterobacteriaceae infections

Avibactam has novel MOA
-works against many beta lactamases produced by K. pneumoniae and P. aeruginosa

Ceftolozane is 3G cephalosporin
-evades many resistance mechanisms of P. aeruginosa

Only ceftazidime/avibactam active against carbapenem resistant Klebsiella and other enteric GNRs

Substantial resistance to these agents among gut anaerobes (unlike penicillin based BL combinations)
-add metronidazole

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11
Q

Carbapenems
All
Good For

A

Mixed aerobic/anaerobic infections
ESBL producing organisms
Intra-abdominal infections

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12
Q

Carbapenems
Imipenem, Doripenem, Meropenem
Good For

A

Nosocomial pneumonia
Febrile neutropenia
Other nosocomial infections

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13
Q

Monobactams
Aztreonam
Good for

A

Gram- infections
-including Pseudomonas

Useful in patients with history of beta lactam allergy

  • except patients who have specific allergy to ceftazidime
  • ceftolozane also shares this side chain

Shares virtually same spectrum as ceftazidime

Can be administered via inhalation to prevent exacerbations of cystic fibrosis

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14
Q

Glycopeptides
and Short Acting Lipoglycopeptides
Vancomycin
Good for

A

Drug of choice for MRSA
-also empiric use when MRSA is concern (ex: nosocomial pneumonia)

Other Gram+ infections when patient has severe beta lactam allergy

Oral form

  • absorbed very poorly
  • only for C. difficile associated disease
  • IV form does not reach high enough intracolonic concentrations to kill C. difficile

Does not kill MSSA as quickly as beta lactams
-use cefazolin or nafcillin instead

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15
Q

Glycopeptides
and Short Acting Lipoglycopeptides
Telavancin
Good for

A

Indicated for:
Skin and skin structure infections
Hospital acquired pneumonia

More rapidly bactericidal than vancomycin
-clinical evidence showing this as a benefit is currently lacking

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16
Q

Long Acting Glycopeptides
Dalbavancin, Oritavancin
Good For

A

Skin and skin structure infections
-Gram+ organism either known or highly suspected

Dosing:

Dalbavancin
-1000mg on day 1 then 500mg a week later
or
-1500mg once

17
Q

Fluoroquinolones

Usage

A 
Antipseudomonal doses
Ciprofloxacin:
-400mg IV q8h
or
-750mg PO q12h

Levofloxacin:
750mg IV/PO daily

Most FQ cleared renally and require dose reduction in renal dysfunction

  • moxifloxacin not excreted into urine (not approved for UTIs)
  • gemifloxacin has dual elimination (UTI usage not established; does require dose adjustment in renal failure)

Risks outweigh benefits for most cases of sinusitis, bronchitis, and uncomplicated UTIs unless other options not available due to rare but serious side effects

18
Q

Fluoroquinolones
Ciprofloxacin
Indications

A 
CAP, sinusitis, AECB: -
UTI: +
Intra-abdominal infection: +
Systemic Gram- infections: +
Skin/soft tissue infection: -
Pseudomonas (+/- beta lactam): +
Treatment/prophylaxis in bioterrorism scenario (active vs anthrax, plague, tularemia): +
19
Q

Fluoroquinolones
Levofloxacin
Indications

A 
CAP, sinusitis, AECB: +
UTI: +
Intra-abdominal infection: +
Systemic Gram- infections: +
Skin/soft tissue infection: +
Pseudomonas (+/- beta lactam): +
Treatment/prophylaxis in bioterrorism scenario (active vs anthrax, plague, tularemia): +
20
Q

Fluoroquinolones
Moxifloxacin
Indications

A 
CAP, sinusitis, AECB: +
UTI: -
Intra-abdominal infection: +
Systemic Gram- infections: +
Skin/soft tissue infection: +
Pseudomonas (+/- beta lactam): -
Treatment/prophylaxis in bioterrorism scenario (active vs anthrax, plague, tularemia): ?
21
Q

Fluoroquinolones
Gemifloxacin
Indications

A 
CAP, sinusitis, AECB: +
UTI: ?
Intra-abdominal infection: ?
Systemic Gram- infections: ?
Skin/soft tissue infection: +
Pseudomonas (+/- beta lactam): -
Treatment/prophylaxis in bioterrorism scenario (active vs anthrax, plague, tularemia): ?
22
Q

Aminoglycosides

Usage

A

Relatively poor distribution to many tissues (including lungs and CNS)
-less than optimal as monotherapy for many severe infections

Base dose on ideal or adjusted body weight rather than total body weight

Differences in activity:

For Pseudomonas:
amikacin > tobramycin > gentamicin

For Klebsiella:
amikacin = gentamicin > tobramycin

Streptomycin has limited uses:
Enterococcus
Tuberculosis
Plague

23
Q

Aminoglycosides

Good for

A 
In combination with a beta lactam:
Serious infections with documented or suspected Gram- pathogens
-febrile neutropenia 
-sepsis 
-exacerbations of cystic fibrosis
-ventilator associated pneumonia

Primarily gentamicin also used in combination with a beta lactam or glycopeptide for serious Gram+ infections

  • endocarditis
  • osteomyelitis
  • sepsis

Streptomycin and Amikacin
-in combination with other antimycobacterial sided for drug resistant infections with Mycobacterium tuberculosis or other mycobacteria

24
Q

Tetracyclines
Doxy/Mino/Tetracycline
Good for

A

Uncomplicated respiratory tract infections

  • useful but not highly studied alternatives
  • acute exacerbations of chronic bronchitis
  • sinusitis
  • community acquired pneumonia

Drugs of choice for many tick-borne diseases

Alternative for:

  • skin or soft tissue infections
  • syphilis
  • pelvic inflammatory disease (with cefoxitin)

Alternative to ciprofloxacin in bioterrorism scenarios

  • anthrax
  • plague
  • tularemia

Malaria
-prophylaxis and treatment

Doxycycline preferred in most situations over minocycline or tetracycline

Tetracycline eliminated renally
-should not be used in cases of renal insufficiency (can worsen renal dysfunction)
Doxycycline does not need to be adjusted in renal or hepatic dysfunction

25
Q

Glycylcyclines
Tigecycline
Good for

A

May have a role in treatment of complicated polymicrobial infections

  • intra-abdominal infections
  • complicated skin and skin structure infections

Very large volume of distribution

  • distributes highly into many tissues
  • leads to low bloodstream concentrations (not ideal for treating primary bloodstream infections

Should not be used for UTIs

  • eliminated hepatically
  • achieves low urinary concentrations
26
Q

Macrolides and Ketolides

Good for

A 
Upper and lower respiratory tract infections
Chlamydia 
Atypical mycobacterial infections 
Traveler's diarrhea
-azithromycin

Macrolides are bacteriostatic drugs (should not be used when cidal activity is usually required

  • meningitis
  • endocarditis
  • etc.

H. pylori induced GI ulcer disease
-Prevpac contains clarithromycin, lansoprazole, and amoxicillin

Their spectrum makes them ideal choice for community acquired pneumonia
-high resistance rate to S. pneumoniae makes them risky choices as monotherapy for infection worse than mild (treat with something else or add beta lactam active against S. pneumoniae)

Erythromycin used as prokinetic agent for impaired GI motility (GI stimulant)

27
Q

Oxazolidinones
Linezolid, Tedizolid
Good for

A

Resistant Gram+ organisms

  • MRSA
  • VRE

Linezolid:

  • pneumonia
  • skin and skin structure infections
  • UTIs
  • other uses

Tedizolid:

  • only indicated for skin and skin structure infections (studied as a 6 day therapy; comparable to 10 days of linezolid)
  • may be useful for other types

Linezolid has dual hepatic and renal elimination
-do not need to adjust dose for renal or hepatic dysfunction

Tedizolid eliminated primarily by liver
-may not sufficiently concentrate in urine to treat UTIs

28
Q

Nitroimidazoles
Metronidazole
Good for

A

Documented or suspected abdominal anaerobic bacteria
-add second drug for aerobic coverage if necessary

Vaginal trichomoniasis

GI infection caused by susceptible protozoa

  • amebiasis
  • giardiasis
  • etc.

Is a component of therapy for H. pylori GI ulcer disease in combination

C. difficile
-mild to moderate disease

Metronidazole has ~100% bioavailability
-switch from IV to PO when possible

Tinidazole

  • spectrum similar to metronidazole
  • approved only for parasitic infections
29
Q

Nitrofurans (nitrofurantoin)
and Fosfomycin
Good for

A

Uncomplicated cystitis

  • only for infections of lower urinary tract
  • in patients who have significant renal dysfunction (CrCL < 50mL/min), there may be insufficient accumulation of the drug in the urine for activity

Prophylaxis against recurrent uncomplicated lower UTI
-nitrofurantoin

Nitrofurantoin
-can be used for 5 days instead of traditional 7 day regimen
Fosfomycin
-single dose

Ineffective for infections outside of lower urinary tract

  • only reach high concentrations in the urine due to PK limitations
  • should not be used for more severe UTIs like pyelonephritis and urosepsis

Retain excellent activity against E. coli
>90% in most studies
-have adequate coverage of other common community acquired urinary tract pathogens

30
Q

Streptogramins
Quinupristin/Dalfopristin
Good for

A

MRSA or E. faecium
-in patients not responding to or intolerant of other medications

E. faecalis is more common in most hospitals

  • less likely to be VRE
  • only use if species is known (linezolid and daptomycin do not have this issue)

No longer considered 1st line for VRE
-the indication was removed from labeling due to lack of follow up data after the initial approval

Must be mixed with D5W
-becomes insoluble and can crystallize when given with NS

31
Q

Cyclic Lipopeptides
Daptomycin
Good for

A 
Skin and skin structure infections
-caused by resistant Gram+ organisms
Staphylococcal bacteremia 
-including right sided endocarditis (few antibiotics have this indication)
Enterococcal bacteremia 
-not indicated or as well studied

Cannot be used for pneumonia

  • binds to human pulmonary surfactant (renders drug inactive)
  • however it does penetrate lung tissue well

FDA approved dosing is 4-6mg/kg/day

  • studies show higher doses may be more effective without causing substantially more toxicity
  • may see up to 12mg/kg/day for difficult to treat infections
32
Q

Folate Antagonists
Trimethoprim/Sulfamethoxazole
Good for

A 
Uncomplicated lower UTIs
-empirically only in areas with low resistance 
Prophylaxis against recurrent UTIs
Listeria meningitis 
P. jirovecii pneumonia
-treatment and prophylaxis 
Toxoplasma encephalitis 
Alternative for:
Bacterial prostatitis 
Typhoid fever
MRSA
-predominant outpatient strain likes to cause skin infections with often large abscesses (must drain abscess)

Used to be first line for acute uncomplicated cystitis in women
-in areas with E. coli resistance greater than 15-20%, use alternative (nitrofurantoin); in these cases at least don’t use as empiric therapy for complicated UTI (pyelonephritis or urosepsis)

TMP/SMX has excellent oral bioavailability
Fairly insoluble in IV solutions; relatively large volumes of diluent needed for it to go into solution

Other drugs in class used against parasitic/fungal infections:
Dapsone
Pyrimethamine 
Sulfafoxine 
Sulfadiazine
-toxoplasmosis
33
Q

Lincosamides
Clindamycin
Good for

A 
Skin and soft tissue infections
Infections of oral cavity
Anaerobic intraabdominal infections 
Acne
-applied topically 
P. jirovecii pneumonia 
-used second line 
-in combination with primaquine
Malaria
-in combination with other drugs 
Bacterial vaginosis 
Bacterial endocarditis 
-prophylaxis

Consider it a mix of vancomycin + metronidazole

  • an alternative for Gram+ infections (such as beta lactam allergy)
  • more variable activity against MRSA (more community acquired strains are susceptible to TMP/SMX than to clindamycin) and S. pyogenes
  • higher level of resistance among Gram- anaerobes (B. fragilis)
  • best used empirically for nonsevere infections of skin and oral cavity; or definitive therapy when susceptibilities known

Reasonable alternative for staphylococcal infections
-organisms that are clindamycin susceptible but erythromycin resistant harbor a gene that may lead to high level clindamycin resistance during therapy (these strains should be screened with a D-test: if positive, inducible clindamycin resistance is present)

Useful in necrotizing fasciitis and other toxin mediated diseases

  • due to inhibition of protein synthesis and activity against organisms in stationary phase growth
  • consider adding it onto beta lactam based therapy for these infections

Nearly 100% bioavailable
-oral doses usually lower than IV to improve GI tolerance

34
Q

Polymixins
Colistin (colistimethate sodium); polymixin B
Good for

A

Multidrug resistant Gram- infections (poorly studied; other drugs should be used if pathogens susceptible)

  • pneumonia
  • bacteremia
  • sepsis
  • complicated UTIs

Give both drugs with loading dose

Polymixin B given in active form

  • has more predictable PK
  • not eliminated renally; should not be dose adjusted in renal dysfunction (unlikely successful in treating UTIs)
  • 1mg = 10,000 units

Colistin given as renally eliminated prodrug

  • colistimethate sodium converted to active colistin in the body
  • 400mg colistimethate = 150mg colistin base activity
  • European countries dose in international units (1mg CBA = 33,333 units rounded to 30,000); (1,000,000 IU = 80mg colistimethate = 30mg CBA); (1mg CBA = 2.7mg colistimethate = 30,000 units)

Oral form of colistin only for bowel decontamination
-such as before GI surgery

Aerosolized forms used to decrease colonization with Gram- bacteria (mainly Pseudomonas) in some patients

  • especially in cystic fibrosis
  • prepare just before administration
  • some experts have used for pneumonia (not very strong evidence)
35
Q

Fidaxomicin

Good for

A

A

.► FARMACOLOGIA CLÍNICA - JP (50 decks)

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