Antimicrobials Flashcards

1
Q

time dependent

A

Optimal effect when the antibiotic’s concentration remains above the MIC in any one duration of the dosing interval

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2
Q

concentration dependent

A

Optimal effect when concentrations are appreciably above the MIC for a given organism, up to a specific level

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3
Q

What is AUC?

A

total exposure / time

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4
Q

Bacteriostatic activity

A

refers to the inhibition of bacterial growth

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5
Q

Bactericidal activity

A

refers to killing the bacteria

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6
Q

Gram +

A
  • thicker cell wall (peptidoglycan)

- contains teichoic acid

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7
Q

Gram -

A
  • has periplasmic space
  • thinner cell wall (peptidoglycan)
  • has an outer membrane
  • has endotoxins
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8
Q

Beta-lactam antibiotics

A
  • Inhibit bacterial cell wall synthesis
  • Responsible for antimicrobial action
  • Bactericidal
  • Time-dependent killing
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9
Q

Which medications are in the class Penicillins?

A
  • Penicillin VK
  • Amoxicillin
  • Dicloxacillin
  • Amoxicillin-clavulanate
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10
Q

Penicillin VK

A
  • Veetids®
  • Covers mostly gram-positive organisms: Enterococci and Streptococci
  • Time dependent
  • bactericidal
  • Administer around-the-clock to promote less variation in peak and trough serum levels
  • Take on an empty stomach 1 hour before or 2 hours after meals
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11
Q

Penicillin VK dosages

A
  • Oral (tablet and solution for reconstitution)
  • Children: 25-75 mg/kg/day in divided doses q. 6-8 hours
  • Adults: 125-500 mg PO q. 6-8 hours
  • an IV exists
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12
Q

Penicillin VK uses and indications

A
  • Pharyngitis
  • Otitis media
  • Skin and soft tissue infections
  • Rheumatic fever
  • IV is used for gonorrhea
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13
Q

Penicillin VK adverse effects

A
  • Melanoglossia (blackening of the tongue)
  • Mild GI effects
  • Nausea, vomiting, diarrhea
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14
Q

Amoxicillin

A
  • Amoxil®
  • Gram-positive and some gram-negative coverage
  • Time dependent
  • bactericidal
  • Administer around-the-clock to promote less variation in peak and trough serum levels
  • Suspension: Shake well before use; may be mixed with formula, milk, fruit juice, water, ginger ale, or cold drinks; administer dose immediately after mixing
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15
Q

Amoxicillin dosages

A
  • Oral (capsule and solution for reconstitution)
  • Children: 25-50 mg/kg/day in divided doses q. 8 hours
  • Adults: 250-500 mg PO q. 8-12 hours
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16
Q

Amoxicillin uses and indications

A
  • Pharyngitis
  • Lower respiratory tract infections (and URI’s)
  • Endocarditis prophylaxis
  • ENT/skin and soft tissues infections
  • Animal bite
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17
Q

Amoxicillin adverse effects

A

Nausea, vomiting, and diarrhea

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18
Q

Amoxicillin-clavulanate

A
  • Augmentin®
  • Covers many gram-negative and gram positive organisms; Some anaerobic coverage
  • Dose adjust in renal dysfunction
  • Administer around-the-clock to promote less variation in peak and trough serum levels
  • Administer with food to increase absorption and decrease stomach upset
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19
Q

clavulanate

A

beta lactamase inhibitor

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20
Q

Amoxicillin-clavulanate dosages

A
  • Oral (tablets and solution for reconstitution)
  • Adults: 500 mg q. 8-12 hours or 875 mg q. 12 hours or 2 grams q. 12 hours
  • Children ( < 40 kg): 20-45 mg/kg/day in divided doses two to three times daily
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21
Q

Amoxicillin-clavulanate uses and indications

A
  • Sinusitis
  • Otitis media
  • Lower respiratory tract infections
  • Community acquired pneumonia
  • Urinary tract infection
  • Bite wounds
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22
Q

Amoxicillin-clavulanate adverse effects

A
  • Diarrhea
  • Nausea, vomiting, and abdominal distress
  • Has more GI problems than regular amoxicillin
  • Hepatic dysfunction (rare)
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23
Q

Dicloxacillin

A
  • Only covers staphylococcus epidermis & aureus (MSSE and MSSA)
  • Administer 1 hour before or 2 hours after meals with at least 120 mL of water (to protect the kidneys)
  • Administer around-the-clock to promote less variation in peak and trough serum levels.
  • Should not be administered in the supine position or immediately before going to bed
  • Drug-drug interaction with warfarin (lower effects of warfarin -> lower INR)
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24
Q

Dicloxacillin dosages

A
  • Oral capsule

- 125-500 mg q. 6 hours

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25
Q

Dicloxacillin uses and indications

A
  • Skin and soft tissue infections
  • Bite wounds
  • Impetigo
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26
Q

Dicloxacillin adverse effects

A
  • Abdominal pain
  • Diarrhea
  • Nausea
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27
Q

What do the Penicillins have in common?

A
  • time dependent killing
  • bactericidal
  • GI effects: nausea, vomiting, diarrhea
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28
Q

Which drugs are in the Cephalosporins class?

A
  • Cephalexin
  • Cefaclor
  • Ceftriaxone
  • Cefepime
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29
Q

Cephalosporins

A
  • Classified by generations: 1st - 4th
  • Some cross-sensitivity in patients with penicillin allergy
  • NONE OF THEM COVER ENTEROCOCCI (which is a gram +) but more broad spectrum
  • also beta lactams
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30
Q

Cephalexin

A
  • Keflex®
  • 1st generation cephalosporin
  • Covers streptococci and staphylococcus aureus; some gram negative
  • Dose adjust with renal impairment
  • can take with food if GI distress
  • Give around-the-clock to promote less variation in peak and trough serum levels
  • Associated with elevated INR
  • drug interaction w/ metformin (increases met. levels)
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31
Q

Cephalexin dosages

A
  • Oral (capsule and suspension for reconstitution)
  • Adult: 250 -1,000 mg q. 6 hours or 500 mg q. 12 hours (max: 4 g/ day)
  • Children: 25-100 mg/kg/day in divided doses q. 6-8 hours (max: 4 g/day)
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32
Q

Cephalexin uses and indications

A
  • Impetigo
  • Skin and soft tissue infections
  • Pharyngitis
  • Urinary tract infection
  • Otitis media
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33
Q

Cephalexin adverse effects

A
  • Abdominal pain
  • Diarrhea
  • Dyspepsia
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34
Q

Cefaclor

A
  • Ceclor®
  • 2nd generation cephalosporin
  • Covers streptococci and staphylococcus aureus
  • Expanded gram negative coverage and Anaerobic coverage
  • Dose adjust in renal impairment
  • Administer around-the-clock to promote less variation in peak and trough serum levels.
  • Administer without regard to meals; shake oral suspension well before using
  • Extended release tablets: Do not chew, crush, or split; administer with or within 1 hour of food
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35
Q

Cefaclor dosages

A
  • Oral (capsule, tablet, and suspension for reconstitution)
  • Adult: 250-500 mg q. 8 hours (500 mg q. 12 hours for ER)
  • Children: 20-40 mg/kg/day divided q. 8-12 hours
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36
Q

Cefaclor uses and indications

A
  • Bronchitis

- Otitis media

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37
Q

Cefaclor adverse effects

A
  • Diarrhea; Use with caution in patients with history of GI diseases
  • Increase in transaminases; monitor LFT’s
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38
Q

Ceftriaxone

A
  • Rocephin®
  • 3rd generation cephalosporin
  • Covers gram-positive and gram-negative organisms
  • Contraindicated in hyperbilirubinemic neonates (< 28d old) b/c drug displaces bilirubin off of albumin
  • contraindicated in use of this w/ IV Ca++ (which is highly bound to albumin)
39
Q

Ceftriaxone dosages

A
  • Given IV or IM
  • Adults: 1 -2 g q. 12-24 hours
  • Children: 50-100 mg/kg/day in 1-2 divided doses q. 12-24 hours
40
Q

Ceftriaxone uses and indications

A
  • Endocarditis
  • Gonorrhea
  • GI infections
  • Meningitis
41
Q

Ceftriaxone adverse effects

A
  • Diarrhea
  • Skin tightness & warm sensation at injection site (IM)
  • Pancreatitis (rare)
42
Q

Cefepime

A
  • Maxipime®
  • 4th generation cephalosporin
  • Covers gram-positive and gram-negative organisms; Expanded coverage of organisms with multiple-drug resistance patterns
  • Dose adjust in renal impairment
43
Q

Cefepime dosages

A
  • Usually given IV
  • Adults: 1-2 g q. 8-12 hours
  • Children: 50 mg/kg/dose q. 8-12 hours
44
Q

Cefepime uses and indications

A
  • Intra-abdominal infections
  • Pneumonia
  • Urinary tract infection
  • Meningitis
45
Q

Cefepime adverse effects

A
  • Positive direct Coombs test (false positive)
  • Transaminitis (increase in LFT’s)
  • Hypophosphatemia
  • Neurotoxicity (rare)
46
Q

What are the classes of Protein Synthesis Inhibitors?

A
  • Aminoglycosides
  • Tetracyclines
  • Macrolides
  • Clindamycin
47
Q

Aminoglycosides

A
  • Binds to the 30S ribosomal subunit
  • Bactericidal
  • Concentration dependent
  • poor bioavailability
48
Q

Which drugs are Aminoglycosides ?

A
  • Gentamycin
  • Tobramycin
  • Neomycin
49
Q

Gentamicin

A
  • Covers mostly gram-negative organisms
  • TDM is required
  • Avoid in pregnant women
  • Dose adjust in renal impairment
50
Q

Gentamicin dosages

A
  • IV or IM dosing

- 2-5 mg/kg/day in divided doses q. 8 hours

51
Q

Gentamicin uses and indications

A
  • Endocarditis
  • Meningitis
  • Intra-abdominal infections
  • Sepsis/septic shock
  • Synergy
52
Q

Gentamicin adverse effects

A
  • Nephrotoxicity
  • Neurotoxicity
  • Ototoxicity
  • Neuromuscular toxicity
53
Q

Tetracyclines

A
  • Bind to 30S ribosome subunit
  • Bacteriostatic
  • Time-dependent
54
Q

Which drugs are in the Tetracycline class?

A
  • Doxycycline (Vibramycin®, Adoxa®)
  • Minocycline (Minocin®)
  • Demeclocycline
55
Q

Doxycycline

A
  • Vibramycin®, Adoxa®
  • Some gram-positive and gram negative organisms; some anaerobes; atypical organisms
  • Chronic ethanol use may reduce the serum concentrations of doxycycline.
  • Serum levels may be slightly decreased if taken with high-fat meal or milk.
  • Administration with iron or calcium may decrease doxycycline absorption.
  • May cause tissue hyperpigmentation, tooth enamel hypoplasia, or permanent tooth discoloration when used during tooth development in last half of pregnancy, infancy, and childhood ≤8 years of age
56
Q

Doxycycline dosages

A
  • Oral (immediate-release and extended-release formulations)
  • 100-200 mg/day in one-to-two divided doses
57
Q

Doxycycline uses and indications

A
  • Pneumonia
  • Rock Mountain spotted fever
  • Chlamydia
  • Lyme Disease
58
Q

Doxycycline adverse effects

A
  • GI inflammation/ulceration (esp if taken without water or lying down)
  • Intracranial hypertension
  • Photosensitivity
  • Tissue hyperpigmentation
  • Hepatotoxicity (rare)
59
Q

Macrolides

A
  • Bind to 50S ribosome subunit
  • Time-dependent or concentration-dependent
  • Bacteriostatic
60
Q

Which drug classes are in the Macrolide class?

A
  • Azithromycin (Zithromax®)
  • Erythromycin (E.E.S. 400®, Ery-Tab®)
  • Clarithromycin (Biaxin®)
  • Fidaxomicin (Dificid®)
61
Q

Azithromycin

A
  • concentration dependent
  • Bacteriostatic
  • Coverage: Some gram-positive and gram-negative; Atypical organisms
  • Inhibitor of P-gp -> drug interactions
  • Avoid in combination with amiodarone
62
Q

Azithromycin dosages

A
  • Oral formulations
  • 1-2 g as a single dose (Chlamydia)
  • 500 mg daily
  • 500 mg on day 1, followed by 250 mg daily on days 2-5
63
Q

Azithromycin uses and indications

A
  • Pneumonia
  • Sinusitis
  • Chlamydia
  • H. pylori infection
  • Pharyngitis
  • Pelvic inflammatory disease
64
Q

Azithromycin adverse effects

A
  • GI: loose stools (common), vomiting, nausea, diarrhea (not as common)
  • QT prolongation
65
Q

Clindamycin

A
  • Cleocin®
  • Lincosamide
  • Bind to 50S ribosome subunit
  • Bacteriostatic
  • Time-dependent
  • Coverage: expanded gram-positive and anaerobic organisms
  • Use with caution in patients with GI disease
  • Caution in patients with moderate to severe hepatic impairment
66
Q

Clindamycin dosages

A
  • Oral and IV
  • Adults: 150 – 450 mg PO q. 6 hours; 600-2700 mg/day in 2-4 divided doses
  • Children: 8-40 mg/kg/day PO in 3-4 divided doses; 20-40 mg/kg/day in 3-4 divided doses
67
Q

Clindamycin uses and indications

A
  • Pneumonia
  • Otitis media
  • Bone and joint infections
  • Intra-abdominal infections
  • Lower respiratory tract infections
  • Skin and soft tissue infections
68
Q

Clindamycin adverse effects

A
  • Diarrhea
  • Metallic taste: IV formulation
  • Black-box warning: Colitis
69
Q

Metronidazole

A
  • Flagyl®
  • Nitroimidazole pro-drug
  • Reduced by organism to active form
  • Bactericidal
  • Concentration-dependent
  • Effects organism’s DNA: Disrupts structure, Inhibits replication
  • Coverage: Anaerobic organisms, Parasites
  • IV formulation contains sodium
  • Taking alcohol with this can lead to: abd cramps, nausea, vomiting, headaches, and flushing
  • avoid alcoholic beverages or products containing propylene glycol during oral or injectable therapy and for at least 3 days after therapy
  • Dose adjust with severe hepatic impairment
  • Contraindicated in first trimester of pregnant patients
  • Drug-drug interactions: Warfarin, Lopinavir
70
Q

Metronidazole dosages

A
  • Oral and IV formulations

- 250-750 mg q. 8 hours

71
Q

Metronidazole uses and indications

A
  • Amebiasis
  • Bacterial vaginosis
  • Intra-abdominal infections
  • Trichomoniasis
  • Giardiasis
  • Clostridium difficile-associated diarrhea (important)
72
Q

Metronidazole adverse effects

A
  • Headache (not as common, can take with food if IR)
  • Nausea (not as common, can take with food if IR)
  • Metallic taste
  • CNS-related effects
  • Black Box Warning: Metronidazole has been shown to be carcinogenic in mice and rats
73
Q

Sulfamethoxazole & Trimethoprim components

A
  • Sulfamethoxazole
    • Sulfonamide with structural similarity to PABA
    • Inhibits the conversion of PABA to dihydropteroic acid by inhibiting the enzyme dihydropteroate synthase
  • Trimethoprim
    • Prevents reduction of dihydrofolic acid to tetrahydrofolic acid by inhibition of dihydrofolate reductase
74
Q

Sulfamethoxazole & Trimethoprim

A
  • bactericidal
  • Concentration-dependent
  • Coverage: Staphylococci, Gram-negative organisms
  • many drug interactions; can cause increased INR
  • Avoid in first trimester of pregnancy
  • Dose adjust in renal impairment
  • Avoid in patients with G6PD deficiency -> could cause hemolysis
  • Avoid in sulfa hypersensitivity
75
Q

Sulfamethoxazole & Trimethoprim dosages

A
  • Dosing (PO and IV)
  • Bactrim DS® (PO) 160 mg TMP/800 mg SMX tablets -> 1 tablet PO q. 12 hours
  • Bactrim SS® (PO) 80 mg TMP/400 mg SMX tablets -> 2 tablets PO q. 12 hours
  • IV: 80 mg TMP/400 mg SMX
76
Q

Sulfamethoxazole & Trimethoprim uses and indications

A
  • Urinary tract infections
  • Pneuomcystis carinii jirovecii (PJP)
  • Nosocomial infections
  • Otitis media
77
Q

Sulfamethoxazole & Trimethoprim adverse effects

A
  • GI: nausea, vomiting (take with food to decrease)
  • Rise in serum creatinine (has nothing to do with renal function; this is due to renal tubular secretion)
  • Hyponatremia
  • Crystaluria (drink plenty of fluid to avoid this)
  • Hyperkalemia (Trimethoprim component, it looks like amiloride)
78
Q

Nitrofurantoin

A
  • Activated by enzymatic reduction
  • Damage bacterial DNA
  • Bactericidal
  • Concentration-dependent
  • Coverage: Gram-positive and Gram-negative organisms
  • Take with food
  • Avoid in patients with a history G6PD deficiency
  • Contraindications: Pregnant patients at term (38-42 wks), CrCl < 60 mL/min, History of cholestatic jaundice or hepatic dysfunction
  • interacts with magnesium; lowers the effect of the drug
79
Q

Nitrofurantoin dosages

A
  • Oral dosing
  • Macrodantin®: 50-100 mg q. 6 hours
  • Macrobid®: 100 mg PO BID
80
Q

Nitrofurantoin uses and indications

A

Urinary tract infection

81
Q

Nitrofurantoin adverse effects

A
  • Colors urine brown
  • Optic neuritis & peripheral neuropathy (rare); associated with long term use
  • Pulmonary toxicity
  • Hepatic reactions (rare)
82
Q

Fluoroquinolones

A
  • Inhibition of DNA gyrase and topoisomerase IV
  • Bactericidal
  • Concentration-dependent
  • Coverage: broad spectrum; minimal gram + but many gram -
  • Atypical organisms
  • Varying anaerobic organisms coverage
  • Avoid concomitant administration of antacids, certain iron salts, and certain zinc salts
  • Black box warning: due to high ADE’s, this should be reserved for pts that have no alternative treatment options for the following indications: acute exacerbation of chronic bronchitis, acute sinusitis, and acute uncomplicated cystitis (UTI)
83
Q

Which drugs are in the Fluoroquinolone class?

A
  • Ciprofloxacin (Cipro®)
  • Levofloxacin (Levaquin®)
  • Moxifloxacin (Avelox®)
84
Q

Compare and contract Fluoroquinolone agents with respect to coverage

A
  • Levofloxacin and moxifloxacin are better respiratory-covering agents
  • Moxifloxacin has expanded coverage
85
Q

Fluoroquinolone uses and indications

A
  • UTI
  • Endocarditis
  • Prostatitis
  • Pneumonia
  • STIs
  • GI and abdominal infections
  • Respiratory tract infections
  • Bone, joint, and soft tissue infections
86
Q

Fluoroquinolones adverse effects

A
  • GI upset
  • CNS effects
  • QT prolongation
  • Hepatotoxicity
  • Tendon rupture
  • Hypoglycemia
  • Crystaluria
  • Photosensitivity
87
Q

Ciprofloxacin

A
  • PO: 500-750 mg q. 12 hours
  • IV: 400 mg q. 12 hours
  • Dose adjust in renal impairment
  • Drug-drug interactions
88
Q

Levofloxacin

A
  • PO or IV: 250-750 mg q. 24 hours
  • Dose adjust in renal impairment
  • Minimal hepatic metabolism
89
Q

Moxifloxacin

A
  • PO or IV: 400 mg q. 24 hours
  • PO or IV: 400 mg q. 24 hours
  • Not metabolized via CYP450 isoenzymes
  • Highest risk of QT prologation
  • not to be used for UTIs
90
Q

Minocycline brand name

A

Minocin®

91
Q

Erythromycin brand name

A
  • E.E.S. 400®

- Ery-Tab®

92
Q

Clarithromycin brand name

A

Biaxin®

93
Q

Fidaxomicin brand name

A

Dificid®

94
Q

Moxifloxacin brand name

A

Avelox®