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Pharmacology > Antimicrobials > Flashcards

Antimicrobials Flashcards

1
Q

Infections that cannot switch from parenteral to PO abts

A

Osteomyelitis

Endocarditis

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2
Q

Admin of most PCNs

A

Parenteral as they are unstable in the acidic environment of the stomach

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3
Q

Distribution of PCNs

A

Distributed widely and penetrate CSF in presence of inflammation

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4
Q

Half life of PCN in adults with normal renal function

A

30-90 min

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5
Q

PCN mech of action

A

Inhibition of bacterial cell growth by interference with cell wall synthesis

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6
Q

Agents of choice for gram+ infections

A

PCNs

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7
Q

High dose PCNs in severe renal dysfunction

A

Associated with seizures and encephalopathy

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8
Q

PCN adverse rxn when tx spirochetes (especially syphilis)

A

Jarisch-Herxheimer reaction:

Fever, chills, sweating, flushing

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9
Q

PCN drug interactions

A

Probenecid will increase half life

Parenteral carboxypenecillins have increased Na content (take care with sodium/fluid restrictions)

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10
Q

How does PCN resistance develop

A

Drug is inactivated by bacteria-produced penecillinases or beta-lactamases

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11
Q

Development of beta-lactam inhibitor combos

A

Inhibitor prevents breakdown of beta-lactam by organisms that produce the enzyme

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12
Q

Beta-lactamase producing organisms

A

S. Aureus
Haemophilus influenza
Bacteroides fragilis

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13
Q

Distribution of beta-lactam inhibitor combos

A

Most body tissue except brain and CSF

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14
Q

Beta-lactam inhibitor combos (Drugs)

A 
Amoxicillin-clavulanic acid (Augmentin)
Ampicillin-sulbactam (Unasyn)
Piperacillin-tazobactam (Zosyn)
Ticarcillin-clavulanic acid (co-ticarclav)
Ceftazidime-avibactam
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15
Q

Beta-lactam inhibitor combo half life

A

Approx 1h

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16
Q

Beta-lactam combo mech of action

A

Interfere with bacterial cell wall synthesis by binding to and in activating PBPs

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17
Q

Clinical uses of beta-lactam inhibitor combos

A

Polymicrobial infections
Extensively:
intra-abdominal and gynecologic infections
Skin/soft tissue infections (human/animal bites)
DM foot infections

Also used for aspiration pna, sinusitis, and lung abcess

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18
Q

Adverse events of beta-lactam inhibitor combos

A

Hypersensitivity rxns

GI SEs

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19
Q

Are cephalosporins a beta-lactam group

A

Yes

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20
Q

Beta-lactam groups

A

Cephalosporins
Monobactams
Carbapenems

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21
Q

How are cephalosporins divided

A

Into generations

1st-4th indicated increase in gram- coverage and decrease in gram+

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22
Q

Absorption of cephalosporins

A

Absorbed well through GI tract

2nd-4th penetrate CSF and play a role in tx of bacterial meningitis

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23
Q

Clinical uses for 1st generation cephalosporins

A

Gram+ skin infections, pneumococcal resp infections, UTI, surgical ppx

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24
Q

Clinical use of 2nd generation cephalosporins

A

Community acquired pna, other resp infections, skin infections

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25
Q

Only cephalosporin that covers MRSA

A 
Ceftaroline fossil (Teflaro)
IV
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26
Q

Cephalosporin tx of bacterial meningitis

A

Typically 3rd generation like ceftriaxone or cefotaxime

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27
Q

Cephalosporin tx of nosocomial infections

A

Commonly ceftazidime or cefepime because broad spectrum covers gram- organisms (P. aeruginosa)

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28
Q

Most common SE with cephalosporin

A

GI: N/V, diarrhea

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29
Q

Cephalosporin drug interactions

A

Rare

Probenecid can increase half life

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30
Q

Monobactams

A

Aztreonam (Azactam) is the only one commercially available

Primarily active against gram- organisms

Safer alternative to aminoglycosides

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31
Q

Distribution of monobactams (Aztreonam)

A

Well into most tissues
Penetration into CSF with inflamed meninges
Not extensively bound to proteins

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32
Q

Half life of Aztreonam

A

2 hours

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33
Q

Aztreonam mech of action

A

Interferes with cell wall synthesis by binding to/inactivation PBPs

Almost no action against gram+

Not active against anaerobic organisms

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34
Q

Clinical uses of aztreonam

A

Complicated and uncomplicated UTIs and resp tract infections (one, bronchitis) when needing aerobic gram-coverage

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35
Q

Cross allergy PCN, cephalosporin, Aztreonam

A

If all to PCN and cephalosporin should be able to take Aztreonam

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36
Q

Carbapenems

A

Bicyclal beta-lactams with a common carbapenem nucleus

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37
Q

Most broad spectrum agents available

A

Carbapenems

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38
Q

Administration of carbapenems

A

IV, not absorbed PO

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39
Q

Half life of carbapenems

A

Approx 1h

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40
Q

Distribution of carbapenems

A

Widely distributed

CSF penetration depends on degree of meningeal inflammation

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41
Q

Carbapenem mech of action

A

Interferes with cell wall synthesis by binding to PBPs

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42
Q

Drugs with the broadest spectrum of activity of all beta-lactam compounds

A

Imipenem, meropenem, doripenem

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43
Q

Carbapenem with no aignificant activity against P. aeruginosa

A

Ertapenem

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44
Q

Why use meropenum over imipenem in tx of CNS infections

A

Lower risk of causing seizures

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45
Q

Carbapenems adverse events

A

GI
Neurotoxicity (seizures)
Risk factors: impaired renal function
Improper dosing
Age
Previous CNS disorder
Meds that decrease seizure.
threshold

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46
Q

Carbapenemen drug interactions

A

Probenecid causes decreased clearance and increased half life

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47
Q

Most commonly prescribed FQs

A

Ciprofloxacin
Levofloxacin
Moxifloxacin

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48
Q

Pharmacodynamics of FQs

A 
Bacetericidal
Excellent bioavailability (easy transition from IV to PO)
Distributes well into most tissues except CNS
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49
Q

Half life of FQs

A

4-12h

Longest half lives: levofloxacin, gemifloxacin, moxifloxacin

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50
Q

FQ mech of action

A

Strong inhibitors of components of bacterial DNA, without which it cannot replicate

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51
Q

Only oral agents available to tx P. aeruginosa

A

Ciprofloxacin

Levofloxacin

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52
Q

Preferred agents for nosomial pna and other hospital acquired infections

A

Cipro or Levaquin

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53
Q

Recommended for meningococcal ppx

A

Cipro

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54
Q

Rare but serious SE of FQs

A

QT prolongation
Tendon rupture
Tendonitis
Peripheral neuropathy

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55
Q

FQs may increase effects of…

A

Theophylline
Warfarin
Tizanidine
Propranolol

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56
Q

What can decrease absorption of FQs

A 
Antacids
Sulcrafate
Magnesium
Calcium
Iron salts
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57
Q

FQs with corticosteroids

A

Increased risk of tendonitis and tendon rupture

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58
Q

Only agent known as a ketolide

A

Telithromycin

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59
Q

Macrolides

A

Azithromycin
Clarithromycin
Erythromycin

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60
Q

Distributions of macrolides

A

Good tissue penetration
Achieve high intracellular concentrations
Exhibits minimal protein binding

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61
Q

Half life of erythromycin

A

2h

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62
Q

Half life of clarithromycin (Biaxin)

A

4-5h

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63
Q

Half life of azythromycin

A

50-60h

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64
Q

Clarithromycin and erythromycin with renal failure

A

Dosage adjustments are needed

65
Q

Half life of telithromycin

A

Approx 10h

66
Q

Macrolide mech of action

A

Inhibition of bacterial protein synthesis by binding to the 50s subunit of ribosome

67
Q

FQ suffix

A

-Oxacin

68
Q

Macrolides and atypical organisms

A 
Chlamydia
Mycoplasma
Legionella
Rickettsia
Mycobacteria
Spirochetes
69
Q

Rare but serious SE of macrolides

A

Hepatotoxicity

70
Q

Adverse rxn associated with telithromycin

A

Acute hepatic failure

Severe liver injury

71
Q

Drug interactions of macrolides and ketolides

A

Inhibits CYP34A and interacts with an extensive list of meds including warfarin

Take care when Admin with meds that prolong QT interval

72
Q

Major drawback of aminoglycosides

A

Potential for nephrotoxicity and cytotoxicity

Length of therapy is restricted

73
Q

Absorption and distribution of aminoglycosides

A

Poorly absorbed through GI tract. Parenteral admin necessary for systemic infections

Distributes into ECF

74
Q

Absorption and distribution of aminoglycosides

A

Poorly absorbed through GI. Parenteral Admin needed for systemic infections

Distributs into ECF (may be sig affected in ICU patients and in malnutrition, obesity, ascites)

75
Q

Half life of aminoglycosides

A

Approx 1-3h

Increased with renal impairment

76
Q

What is used to monitor therapy with aminoglycosides

A

Renal function and serum levels

Narrow range between therapeutic and toxicity

77
Q

Macrolides (drugs)

A

Azithromycin
Clarithromycin
Erythromycin
Telithromycin (ketolide)

78
Q

Aminoglycosides (drugs)

A

Gentamicin
Tobramicin
Streptomycin
Amikacin

79
Q

Aminoglycoside mech of action

A

Binds to 30s ribosomal unit of bacteria inhibiting bacterial protein synthesis

80
Q

Activity of aminoglycosides

A

Aerobic gram- bacilli

Gram+ cocci (with cell wall active agent like ampicillin, ampicillin, vancomycin)

81
Q

Clinical uses of aminoglycosides

A

Empiric tx of neutrogenic fever and nosocomial infections

Routinely used in combo with other agents

Monotherapy not recommended except with UTIs

82
Q

How does nephrotoxicity occur with aminoglycosides

A

Accumulation of drug in proximal tubule cells of the kidney

83
Q

Labs monitored with aminoglycosides

A

BUN/creat and serum levels

84
Q

Forms of aminoglycoside ototoxicity

A

Auditory (healing loss, tinnitus)
Vestibular (N/V, vertigo)

Increases when admin with high dose loop diuretics, macrolides, or vancomycin

85
Q

Aminoglycoside drug interactions

A

Increased risk of neuromuscular blockade when Admin with neuromuscular blockers, general anesthetic, calcium channel blockers

Admin of calcium glucometer often reverses blockade

86
Q

Tetracycline suffix

A

-cycline

87
Q

Activity of tetracyclines

A

Gram+, gram-, atypical organisms

88
Q

Adsorption of tetracyclines

A

GI tract
Empty stomach increases absorption except with long acting (doxycycline, minocycline)

Eliminated by glomerular filtration except for doxycycline

89
Q

Tetracycline mech of action

A

Binds to 30s ribosomal unit to inhibit protein synthesis

90
Q

Clinical uses for tetracyclines

A

When beta-lactams aren’t an option

Doxy for early Lyme disease and community acquired pna

91
Q

Tx of SIADH

A

Demeclocycline (Declomycin)

92
Q

Adverse events of tetracyclines

A

Anorexia, N/V, epigastric distress, gray-green discoloration of teeth (not for kids under 8)

Sensitivity to the sun

93
Q

Drug interactions with tetracyclines

A

Absorption decreased by iron, cholestyramine, sulcrafate, antacids, dairy

Potentiate the effects of warfarin by impairing vitamin k synthesis by intestinal flora

94
Q

Glycylcycline

A

Tigecycline

Available IV only

95
Q

Tigecycline dosage adjustments

A

Not for renal insufficiency but for severe underlying liver disease

96
Q

Tigecycline mech of action

A

Binds to 30s subunit to inhibit bacterial protein synthesis

Activity against MRSA and VRE

97
Q

Clinical uses for Tigecycline

A

Complicated skin infections, intra-abdominal infections, community acquired pna

98
Q

Adverse events Tigecycline

A

N/V, asymptomatic hyperbilirubinemia

99
Q

Sulfonamides (drugs)

A

Sulfadiazine
Sulfisoxazole
Trimethoprim
Trimethoprim-sulfamethoxazole (bactrim)

100
Q

Absorption/distribution of sulfonamides

A

Readily absorbed through GI

Distributed through all body tissues including CSF, plural fluid, synovial fluid

101
Q

Half life of sulfonamides

A

Varies from hours to days

102
Q

Sulfonamide mech of action

A

Inhibits the incorporation of para-aminbenzoic acid required for folic acid synthesis necessary for bacterial cell growth

103
Q

Sulfonamide used to treat ulcerative colitis

A

Sulfasalazine

Lacks sig microbial activity

104
Q

Why are sulfonamides typically used with other agents

A

Limited spectrum of activity and increasing resistance

105
Q

Adverse events of sulfonamides

A

Rash (occurs within 1-2 wks), fever, GI

Hemolytic anemia with G6PD deficiency

106
Q

Sulfonamide drug interactions

A

Potentiates effect of warfarin, phenytoin, hypoglycemic agents, methotrexate

107
Q

Glycopeptides (drugs)

A

Vancomycin
Dalbavancin
Oritavancin
Telavancin

108
Q

Monitoring glycopeptides

A

Monitor renal function

Serum monitoring with unpredictable kidney function, severe infection, when therapy exceeds 3-5 days

109
Q

Clinical uses for vancomycin

A

Serious gram+ when allergic or unable to tolerate beta-lactams

Drug of choice for MRSA and other resistant organisms

110
Q

Adverse events of glycopeptides

A

Fever, chills, “red man” syndrome (associated with rate of infusion of vanc)

111
Q

Red man syndrome

A

Pruritus, flushing of head, neck, and face, hypotension

112
Q

Glycopeptide contraindicated during pregnancy

A

Telavancin

113
Q

Drug interactions of glycopeptides

A

Unlikely as it does not undergo sig hepatic metabolism

114
Q

Oxazolidinones available

A

Linezolid (Zyvox)

Tedizolid (Sivextro)

115
Q

Absorption and administration of oxazolidinones

A

GI tract absorption
Bioavailability greater than 90%
Admin without regard to food
Eliminated nonrenally

116
Q

Oxazolidinone mech of action

A

Binds to 50s ribosomal subunit to disrupt bacterial protein synthesis

Particularly good action against resistant organisms

117
Q

Oxazolidinones drug interactions

A

Sympathomemtic agents like pseudoepinephrine, SSRI antidepressants, herbal products, and foods rich in tyramine

118
Q

Lipopeptide available

A

Daptomycin

119
Q

Daptomycin txs what

A

MDR Gram+ pathogens

120
Q

Daptomycin dosing

A

6mg/kg x 7 days

121
Q

Half life of daptomycin

A

Approx 8h

122
Q

Daptomycin mech of action

A

Bonds to bacterial membranes and causes a rapid depolarization of membrane potential. Low membrane potential leads to cell death

123
Q

Daptomycin activity

A

MRSA, VRE

124
Q

Clinical uses of daptomycin

A

Complicated skin infections
S. Aureus bacteremia
R sided endocarditis caused by methicillin susceptible and methicillin resistive isolates

125
Q

Daptomycin drug interactions

A

CPK levels weekly for concomitant use of stations and/or renal insufficiency

126
Q

Streptogramins

A

Only available is quinupristin/dalfopristin (Synercid)

127
Q

Administration of Synercid

A

IV, not absorbed through GI tract

128
Q

Synercid mech of action/activity

A

Binds to 50s ribosomal subunit inhibiting bacterial protein synthesis

Active against gram+ aerobic organisms

129
Q

Clinical uses of Synercid

A

Skin infections, VRE

130
Q

Administration of Synercid

A

Through a central line

131
Q

Clindamycin

A

Anti anaerobic agent

Gram+ anaerobic bacterial infections

132
Q

Distribution of clindamycin

A

Reaches most tissues and bone but distribution into CSF is limited

133
Q

Clindamycin dosage adjustments

A

With liver impairment

134
Q

Clindamycin mech of action

A

Binds to 50s subunit inhibiting protein synthesis

135
Q

Clinical uses for clindamycin

A

Gram-/+ infections, toxoplasmosis, toxic shock

136
Q

SE of clindamycin

A

Diarrhea assoc with c. Diff

137
Q

Drug interactions with clindamycin

A

Skeletal muscle relaxants can potentiate neuromuscular blockade

138
Q

Meteonidazole (flagyl) absorption and penetration

A

Completely absorbed through GI

Penetrates most tissues

139
Q

Half life of flagyl

A

6-9h

140
Q

Clinical uses for flagyl

A

Bacterial vaginosis
Trichomoniasis
C. Diff

141
Q

Adverse events with flagyl

A

GI SE and metallic taste
Seizures with high doses
Peripheral neuropathy with prolonged therapy

142
Q

Flagyl drug interactions

A

Enhances effect of warfarin

With alcohol disulfiram-like rxn (flushing, palpitations, nausea, vomiting)

143
Q

What increases metabolism of flagyl leading to tx failure

A

Phenobarbital, phenytoin, and rifampin

144
Q

Chloramphenicol

A

Wide spectrum of activity against gram+/-, and anaerobic organisms

145
Q

Chloramphenicol limitation

A

Limited due to toxicity profile which includes gray baby syndrome, optic neuritis, and fatal aplastic anemia

146
Q

Availability and penetrance of chloramphenicol

A

IV
Penetrates into most tissues and body fluids including CSF
Crosses the placenta

147
Q

Chloramphenicol mech of action

A

Binds to 50s ribosomal subunit inhibiting protein synthesis

148
Q

Half life of chloramphenicol

A

3-4h

149
Q

Clinical usage of chloramphenicol

A

Alternative to tx meningitis when life threatening PCN allergy
Rocky mountain spotted fever and typhoid fever in patients allergic to tetracyclines or in pregnant women

150
Q

Adverse events of chloramphenicol

A

Gray baby syndrome
Blood dyscrasias
Aplastic anemia,
Optic neuritis (assoc with long term use)

151
Q

Chloramphenicol drug interactions

A

Prolongs half life of warfarin, phenytoin, and cyclosporine

152
Q

Clinical usage of rifampin

A

1st line tx for TB

Post exposure ppx for n. Meningitidis and h. Influenza type b

153
Q

Rifampin mech of action

A

Suppresses initiation of chain formation for RNA synthesis in susceptible bacteria by inhibiting DNA-dependent RNA polymerase

154
Q

Absorption and distribution of rifampin

A

Completely absorbs

Distributes into most tissues and fluids including CSF

155
Q

Half life of rifampin

A

Approx 3h

156
Q

Adverse events of rifampin

A

Changes body fluids red-orange

Hepatotoxicity

157
Q

Rifampin drug interactions

A

Increases clearance of antiarrhythmics, azole antifungals, clarithromycin, estrogens, most statins, warfarin, and many HIV meds

158
Q

Macrobid

A

Only for uncomplicated UTIs

159
Q

Half life of macrobid

A

Less than 30 min

Pharmacology (11 decks)

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