Antimicrobial Review Flashcards

1
Q

Penicillin

MOA

A

Inhibits cell wall synthesis

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2
Q

Penicillin

Mechanisms of Resistance

A
  • B-lactamase production
  • Altered PBP
  • Decreased drug permability
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3
Q

Penicillin

Gram Pos Coverage

List specific bacteria

A

Streptococcus spp
Listeria spp
Clostridium spp

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4
Q

Penicillin

Gram Neg Coverage

List specific bacteria

A

Neisseria spp
Pasteurella

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5
Q

Penicillin

Overall Coverage

A

Gram Positives
Gram Negatives (more limited)
Spirochete (Treponema pallidum)

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6
Q

Penicillin

Side Effects

A
  • IgE-mediated anaphylaxis
  • Integumentary (Maculopapular rash)
  • GI upset- Nausea, vomiting, diarrhea
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7
Q

Antistaphylococcal Penicillins

List the Meds

A

Nafcillin
Oxacillin
Dicloxacillin

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8
Q

Antistaphylococcal Penicillins

Gram Positive Bacterial Coverage

list specific species

A

Gram Positives
* streptococcus spp
* Clostridium spp
* Methicillin-susceptible Staphylococcus Aureus

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9
Q

Antistaphylococcal Penicillins

Side Effects

A

Hematologic/Oncologic: agranulocytosis
GI: cholestasis, n/v/d

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10
Q

Aminopenicillins

Overall Coverage

A

Gram Positives
Gram Negatives
Improved gram neg coverage compared to penicillins

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11
Q

Aminopenicillins

A

Amoxicillin

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12
Q

Aminopenicillins

Gram Positive Coverage

A

Streptococcus spp
Enterococcus spp

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13
Q

Aminopenicillins

Gram Neg Coverage

A

E. Coli
Proteus mirabilis
H. Influenzae
Salmonella spp
Shigella spp
Neisseria meningitidis

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14
Q

Aminopenicillins

Side Effects

A

GI: n/d
Renal: nephrotoxicity

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15
Q

What can aminopenicillins be combined with?

A

beta-lactamase inhibitors

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16
Q

Which is better absorbed, amoxicillin or ampicillin?

A

Oral amoxicillin

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17
Q

Piperacillin/Tazobactam

Side Effects

A

Hypersensitivity (anaphylaxis)
Integumentary: Stevens-Johnson Syndrome, Toxic epidermal necrosis
Renal: nephrotoxicity
GI: n/v/d

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18
Q

Piperacillin/Tazobactam

Overall Bacterial Coverage

A

BROAD SPECTRUM (positives, negatives, anaerobes)

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19
Q

How are piperacillin/tazobactams administered?

A

Infusion (over 4 hrs)

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20
Q

Cephalosporins

MOA

A

binds to penicillin binding proteins to prevent cell wall synthesis

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21
Q

Cephalosporins

Time or concentration dependent?
Bactericidial or bacteriostatic?

A

Time dependent
Bactericidal

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22
Q

Penicillins

Time or concentration dependent?
Bactericidial or bacteriostatic?

A

Time dependent
Bactericidal

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23
Q

Cephalosporins

Class

A

Beta-Lactams

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24
Q

Cephalosporin

Coverage

A

1st Gen: great w/ gram positives, poor gram neg coverage
3rd Gen: equalish gram neg/pos coverage
5th Gen: great gram neg coverage, poor gram pos coverage

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25
# Cephalosporins 1st Gen Meds & Admin Route | List med names & PO/IV/IM
Cefazolin (IV) Cephalexin (PO) Cefadroxil (PO)
26
# Cephalosporins 1st Gen Coverage
MSSA Beta-hemolytic *Streptococcus* PEcK
27
# Define PEcK
*Proteus* *E. coli* *Klebsiella*
28
# Cephalosporins 2nd Gen Meds & Admin Route | List med names & PO/IV/IM
Cefaclor (PO) Cefprozil (PO) Cefuroxime (IV/IM/PO) Cefoxitin (IV/IM) Cefotetan (IV/IM)
29
# Cephalosporins 2nd Gen Coverage
MSSA Beta-hemolytic *Streptococcus* HEN PEcKS Oral Anaerobes
30
# Define HEN PEcKS
*H. Influenzae* *Enterobacter aerogenes* *Neisseria* *Proteus* *E. coli* *Klebsiella* *Serratia marcescens*
31
# Cephalosporins 3rd Gen Meds & Admin Route | List med names & PO/IV/IM
Cefotaxime (IV/IM) Ceftazidime (IV/IM/Neb/Intravitreal) Ceftriaxone (IV/IM) Cefixime (PO) Cefpodoxime (PO) Cefdinir (PO)
32
# Cephalosporins 3rd Gen Coverage
MSSA & *Streptococcus* *Neisseria meningitidis & gonnorhea* Oral anaerobes *Pseudomonas* *Moraxella* *H. Influenzae*
33
# Cephalosporins Pearls
* Cross BBB, so can be utilized for meningitis * Ceftazidime has *pseudomona* coverage
34
# Cephalosporins 3rd Gen Contraindications
- Infants < 28 days when also using calcium containing products - Neonates w/ hyperbilirubinemia
35
# Cephalosporins 4th Gen Meds & Admin Route
Cefepime (IV/IM)
36
# Cephalosporins 4th Gen Coverage
MSSA & *Streptococcus* *Neisseria meningitidis & gonnorhea* Oral anaerobes *Pseudomonas*
37
# Cephalosporins Which generations can be used to treat meningitis because they cross the BBB?
- 3rd Gens - 4th Gen
38
# Cephalosporins 4th Gen Contraindications
- use with caution in patients w/ seizures (neurotoxicity)
39
# Cephalosporins 5th Gen Meds & Admin Routes
Ceftaroline (IV) Ceftolozone/Tazobactam (IV)
40
# Cephalosporins Ceftaroline Coverage
MSSA, MRSA, & *Streptococcus* *Neisseria meningitidis & gonnorhea* *Pseudomonas* *Moraxella* *H. Influenzae*
41
# Cephalosporins Ceftolozone/Tazobactam Coverage
*pseudomonas* No MRSA coverage
42
# Cephalosporins Side Effects
n/v, loss of appetite, abd pain, nephrotoxicity, hemolytic anemia, super infection (C. diff)
43
Do cephalosporins have cross reactivity with pencillin allergy?
Yes- greatest in Gen 1 and decreases throughout rest of gens. 3rd Gen and beyond show minimal cross reactivity, but we still avoid in allergy
44
Do cephalosporins cover *Enterococcus* spp?
NO
45
Which cephalosporin does not require renal dose adjustment?
Ceftriaxone
46
Carbapenem Meds
Doripenem ertapenem Imipenem Meropenem
47
# Carbapenems MOA
inhibit cell wall synthesis by binding to PBPs, thus, causing bacterial cell wall defect
48
# Carbapenems Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration Dependent Bactericidal
49
# Carbapenem Bacterial Coverage
Gram neg cocci and bacilli MSSA and *Streptococcus* Anaerobes
50
# Carbapenems Side Effects
n/v, abd pain, seizures, nephrotoxicity, injection site rxn
51
# Carbapenems Does ertapenem cover pseudomonas?
NO
52
Monobactam Med
Aztreonam
53
# Monobactam MOA
inhibits synthesis of bacterial cell wall by blocking peptidoglycan crosslinking
54
# Monobactams Time or concentration dependent? Bactericidial or bacteriostatic?
Time Dependent Bactericidal
55
# Monobactam Coverage
*Citrobacter* spp *Enterobacter* spp *E. coli* *Haemophilus* spp *Klebsiella* spp *Proteus* spp *Serratia* spp
56
# Monobactams Side Effects
n/v/d, pain at injection site, increase in serum transaminases, neutropenia
57
Macrolide Meds
Azithromycin Clarithromycin Erythromycin Fidaxomicin
58
# Macrolides MOA | EXCLUDES FIDAXOMICIN
inhibits RNA-dependent protein synthesis by binds to the 50S ribosomal subunit
59
# Macrolides MOA | Fidaxomicin
Inhibits RNA polymerase by binding to the DNA template RNA polymerase complex
60
# Macrolides Time or concentration dependent? Bactericidial or bacteriostatic?
Time Dependent Bacteriostatic *At high concentrations can be bactericidal*
61
# Macrolides Side Effects
GI: n/v/d, abd pain Hepatic: cholestatic jaundice Cardiac: QT prolongation
62
# Macrolides What is the only bacteria Fidaxomicin is used for? | PPP
*C. diff*
63
# Macrolides Which macrolide has the largest risk of GI disturbance? | PPP
Erythromycin
64
# Macrolides Overall Bacterial Coverage | Excludes fidaxomicin
Gram Positives Atypical Bacteria Spirochete Limited Gram Negatives
65
# Macrolides Gram Positive Coverage | Excludes Fidaxomicin
Group A Streptococci *Corynebacterium diphtheriae* *Cutibacterium acnes*
66
# Macrolides Atypical Bacterial Coverage | Excludes Fidaxomicin
*Mycoplasma pneumoniae* *Chlamydia trachomatis* *Chlamydophila pneumoniae* *Legionella* spp
67
# Macrolides Spirochete Coverage | Excludes Fidaxomicin
*Treponema pallidum* *Borrelia burgdorferi*
68
# Macrolides Gram Negative Coverage | Excludes Fidaxomicin
*Campy*
69
# Lincosamide MOA
inhibits protein synthesis by binding to the 50S ribosomal subunit
70
Lincosamide Med
Clindamycin
71
# Lincosamide Time or concentration dependent? Bactericidial or bacteriostatic?
Time Dependent Bacteriostatic *at high concentrations it can be bactericidal*
72
# Lincosamides Side Effects
GI: n/v/d, *C. diff* infection Integum: Stevens-Johnson Syndrome Cardiac: QT prolongation
73
# Lincosamides Overall Coverage
Gram Positives Anaerobes
74
Can Clindamycin be used for community acquired MRSA?
Yes
75
Tetracycline Meds
Doxycycline Minocycline Tetracycline
76
# Tetracyclines MOA
Binds to the 30S ribosomal unit, inhibiting protein synthesis
77
# Tetracyclines Time or concentration dependent? Bactericidial or bacteriostatic?
Combination of concentration and time dependent Bacteriostatic
78
# Tetracyclines Risk of what injury if patient doesn't take with water & remain upright? | PPP
Esophageal injury
79
# Tetracyclines Contraindications | PPP
Avoid in children < 8 and pregnant women due to concern of dental discoloration & bone development delay
80
# Tetracyclines Overall Coverage
Broad Spectrum AF
81
# Tetracyclines Gram Positive Coverage
MRSA *Streptococcus* (watch for increasing resistance) *Bacillus anthracis*
82
# Tetracyclines Gram Negative Coverage
*Rickettsiae* *H. Influenzae* *Helicobacter pylori* *Vibrio cholerae*
83
# Tetracyclines Anaerobe/Spirochete/Atypical Bacteria Coverage
Anaerobe: *bacteriodes fragilis* Spirochetes: *treponema pallidum, berelia burgodrferi* Atypicals: *mycoplasma pneumoniae, chlamydia trachomatis, chlamydophila pneumoniae, Legionella* spp
84
# Tetracyclines Side Effects
- Teeth & Bone Effects - Integum: photosensitivity - GI: n/d/v, *C. diff* infection
85
# Aminoglycosides MOA
interferes with bacterial protein synthesis by irreversibly binding to the 30S ribosomal subunit
86
Aminoglycoside Meds
Gentamicin Tobramycin Amikacin
87
# Aminoglycosides Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration Dependent Bactericidal
88
# Aminoglycosides Gram Negative Coverage
PEcK *Pseudomonas* *Enterobacter* *Shigella*
89
# Aminoglycosides Side Effects
Renal Toxicity Vestibular/Auditory Toxicity Neuromuscular Blockades
90
Are aminoglycosides uses as a mono treatment? | PPP
NO- paired with broad spectrum beta-lactams
91
Sulfonamide Meds
Sulfamethoxazole Trimethoprim
92
# Sulfonamides Time or concentration dependent? Bactericidial or bacteriostatic?
Time Dependent Bacteriostatic
93
# Sulfonamides Sulfamethoxazole MOA
Inhibits bacterial folic acid synthesis via competing with para-aminobenzoic acid inhibiting formation of dihydrofolic acid formation
94
# Sulfonamides Bacteria Coverage
Broad Spectrum Gram Positives (including MRSA) Gram Negatives Protozoa (cyclo) Fungi
95
# Sulfonamides Trimethoprim MOA
competitively inhibits folic acid production by inhibiting dihydrofolic acid reduction to tetrahydrofolate, leading to inhibition of the enzymes in folic acid production
96
# Sulfonamides Side Effects
GI: n/v/d Heme: thrombocytopenia, hemolytic anemia, severe hyperkalemia Integum: photosensitivity
97
# Sulfonamides Contraindications | PPP
- hypersensitivity to sulfa - hx of drug induced thrombocytopenia - infants < 2 mo - pregnancy
98
# Fluoroquinolones MOA
Inhibiting the activity of DNA gyrase and topoisomerase which are enzymes essential for bacterial DNA replication
99
Fluoroquinolones Meds
Ciprofloxacin Levofloxcain Moxifloxacin Ofloxacin Gemifloxacin Delafloxacin
100
# Fluoroquinolones Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration Dependent Bactericidal
101
# Fluoroquinolones Gram Pos Coverage
*Staphylococcus* spp *Streptococcus* spp (minus cipro) *Enterococcus faecalis* *Listeria monocytogenes*
102
# Fluoroquinolones Gram Neg Coverage
PEcK *H. influenzae* *pseudomonas* (only cipro)
103
# Fluoroquinolones Which meds have coverage against addition atypical bacteria? ## Footnote 2
levo moxi
104
# Fluoroquinolones Side Effects
GI: n/v Cardio: QT prolongation Neuro: CNS adverse effects (insomnia, hallucinations, seizures) Integum: photosensitivity Musculo: TENDON RUPTURE
105
Nitroimidazole Meds
Metronidazole
106
# Nitroimidazoles MOA
diffuses into the organism and inhibits protein synthesis by interacting with DNA which leads to the loss of DNA helical structure and strand breakage
107
# Nitroimidazoles Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration Dependent Bactericidal
108
# Nitroimidazoles Bacterial Coverage
Anaerobic bacteria Protozoan parasites
109
# Nitroimidazoles Side Effects
GI: n/v/d Neuro: seizures, peripheral neuropathy
110
# Nitroimidazoles Describe restrictions on alcohol use | PPP
Avoid alcohol during therapy and 3 days after completion of series. Disulfiram-like reaction occurs which will induce severe nausea and vomiting if alcohol is used with this med.
111
Glycopeptide/Lipoglycopeptide Meds
Vancomycin Dalbavancin Telavancin Oitavancin
112
# Glycopeptides/Lipoglycopeptides MOA
inhibits transpeptidation by binding to the D-alanyl-D-alanine residues of the bacterial cell wall.
113
# Glycopeptide Time or concentration dependent? Bactericidial or bacteriostatic? | Vancomycin
Time Dependent Bactericidal
114
# Lipoglycopeptides Time or concentration dependent? Bactericidial or bacteriostatic? | Dalbavancin, telavancin, oritavancin
Concentration Dependent Bactericidal
115
# Glycopeptide Bacterial Coverage | Vancomycin
- most gram positive cocci & bacilli (good for resistant strains) - *Enterococcus* - *C. diff* (PO ONLY)
116
# Lipoglycopeptides Bacterial Coverage | Dalba/Tela/Orita
*Streptococcus* *Enterococcus* spp- including VRE *Staphylococcus aureus*- Orita active against VRSA
117
# Glycopeptides/Lipoglycopeptides Side Effects
GI: n/v, taste disturbance GU: nephrotoxicity (vanco, tela), foamy urine
118
Vancomycin infusion related rxn | PPP
Red Man Syndrome - flushing, redness, hypotension, chest pain - Directly related to infusion rate, should not be administered faster than 1 gram/hr
119
Polypeptides Meds
Colistin Bacitracin Polymyxin B
120
# Bacitracin MOA
Polypeptide antibiotic that inhibits cell wall synthesis
121
# Colstin & Polymyxin B MOA
Binds to the anionic outer membrane and thereby neutralizes the bacteria's toxicity and causes cell death
122
# Colstin & Polymyxin B Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration Dependent Bactericidal
123
# Polypeptide Bacterial Coverage | for Colistin & Polymyxin B
*E. coli* *Enterobacter* spp *Klebsiella* spp *Citrobacter* spp *Salmonella* spp *Shigella* spp
124
# Polypeptides Bacterial Coverage | Bacitracin
most superficial skin infections caused by *Staph aureus*
125
# Polypeptides Side Effects
Nephrotoxicity, paresthesia, vertigo, slurred speech, muscle weakness
126
What type of infections is Bacitracin used for? | PPP
topical infections
127
Streptogramins
Quinupristin Dalfopristin
128
# Streptogramin Quinupristin MOA
inhibits the early phase of protein synthesis
129
# Streptogramin Quinupristin MOA
inhibits the late phase of protein synthesis
130
# Streptogramin Bacterial Coverage
- *Streptococcus* - *Staphylococcus* - *C. perf* - *Peptostreptococcus* spp - *Enterococcus faecium* including VRE - some gram negative anaerobic bacilli - Atypical respiratory pathogens
131
# Streptogramin Side Effects
muscle/joint pain, n/v/d, rash, headache
132
How should streptogramins be administered? | PPP
via central line due to phlebitis when given peipherally
133
When do we adjust the dose of streptogramins? | PPP
in hepatic insufficiency
134
Oxazolidanones Meds
Linezolid Tidezolid
135
# Oxazolidanones MOA
binds 50S subunit and blocks bacteria's ability to assemble transfer RNA-ribosomal complex which ultimately inhibits protein synthesis
136
# Oxazolidanones Time or concentration dependent? Bactericidial or bacteriostatic?
Time Dependent Bacteriostatic: *Enterococcus* and *Staphylococcus* Bactericidal: *Streptococcus*
137
# Oxazolidanones Bacterial Coverage
*Streptococcus* *Enterococcus* includes VRE *Staphylococcus* includes MRSA *Mycobacteria* spp Anaerobes
138
# Oxazolidanones Side Effects
Reversible myelosuppression, irreversible peripheral neuropathy, reversible optic neuropathy, serotonin syndrome
139
What drug use is contraindicated with oxazolidanones? | PPP ## Footnote Hint: think of the side effects
MAOIs Do not use oxazolidanones within 2 wks of MAOI use
140
# Nitrofurantoin MOA
inhibits bacterial enzymes responsible for cell wall synthesis
141
# Nitrofurantoin Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration dependent Bactericidal
142
# Nitrofurantoin Bacterial Coverage
*E. coli* *Citrobacter* spp *S. saprophyticus* *E. faecalis*
143
# Nitrofurantoin Side Effects
GI disturbance, headache, dizziness, confusion, pancreatitis
144
Which *E. coli* does nitrofurantoin specifically cover due to resistance? | PPP
ESBL *E. coli*
145
# Rifampin MOA
binds to and inhibits DNA dependent RNA polymerase
146
# Rifampin Time or concentration dependent? Bactericidial or bacteriostatic?
Concentration Dependent Bactericidal
147
# Rifampin Bacterial Coverage
*Staphylococcus* spp *Streptococcus* spp *Legionella* spp *B. fragilis* *Y. pestis* *C. burnetti* *Neisseria meningitides*
148
# Rifampin Side Effects
hepatotoxicity, thrombocytopenia, AKI, flu-like syndrome
149
What is Rifampin a strong inducer of? | PPP
CYP enzymes, many drug-drug interactions
150
Acyclic Analogues of 2' deoxyguanosine
Acyclovir Valacyclovir Penciclovir Famciclovir
151
Nucleoside Analogues of Guanosine
Ganciclovir Valganciclovir
152
Neuraminidase Inhibitors
Oseltamivir Zanamivir
153
Acyclic Phosphonate Nucleotide Analog
Cidofovir Brincidofovir
154
# Acyclovir & Valacyclovir MOA
competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates the viral DNA polymerase
155
# Acyclovir & Valacyclovir Coverage
Herpes virus
156
# Acyclovir & Valacyclovir Side Effects
n/v, abd pain, dizziness nephrotoxicity (more w/ acyclovir)
157
# Acyclovir & Valacyclovir ____ is a prodrug of ____ | PPP
1. Valacyclovir 2. Acyclovir
158
What do you give the pt to prevent nephrotoxicity with IV formulations? | PPP
hydrate with 1mL/kg/hr
159
# Penciclovir & Famciclovir MOA
selectively inhibits viral DNA polymerase by competing with deoxyguanosine triphosphate
160
# Penciclovir & Famciclovir Coverage
Herpes virus & hepatits B virus
161
# Penciclovir & Famciclovir Side Effects
Mild erythema, headache, fatigue, GI disturbances
162
# Penciclovir & Famciclovir ____ is a prodrug of ___
1. Famciclovir 2. Penciclovir
163
Penciclovir is formulated as: Famciclovir is available as:
1. cream only 2. tablet
164
# Ganciclovir & Valganciclovir MOA
competitively inhibits incorporation of deoxyguanosine triphosphate into elongating DNA resulting in short subgenomic CMV DNA fragments that are not considered infectious
165
# Ganciclovir & Valganciclovir Coverage | primary & secondary coverages
herpes virus some coverage for vaccina virus, HPV, and influenza A
166
# Ganciclovir & Valganciclovir ____ is a prodrug of ____ | PPP
1. valganciclovir 2. ganciclovir
167
What is ganciclovir's main use? | PPP
treatment or prevention of CMV infection in immunocompromised pts
168
# Oseltamivir & Zanamivir MOA
reversible inhibitor of influenza neuraminidase which inhibits the release and spread of the infectious form of the virus
169
# Oseltamivir & Zanamivir Coverage
Influenza A some Influenza B activity
170
# Oseltamivir & Zanamivir Side Effects
n/v/d, headache, rash Bronchospasm (zanamivir)
171
When must oseltamivir & zanamivir therapy begin following sx onset?
48 hrs
172
How is zanamivir formulated?
powder for inhalation
173
CMV
cytomegalovirus
174
# Cidofovir & Brincidofovir MOA for CMV
competitive inhibitor and an alternate substrate for CMV DNA poly. Incorporates into the CMV DNA strand and blocks further viral DNA synthesis leading to non-productive infection.
175
# Cidofovir & Brincidofovir MOA for HPV
infected cells are trapper in the S phase which stops DNA synthesis. Also causes induction of DNA fragment and caspase-3-protease activity leading to apoptosis
176
# Cidofovir & Brincidofovir Coverage
Herpes virus, adenoviruses, papillomavirus
177
# Cidofovir & Brincidofovir Side Effects
nephrotoxicity, neutropenia, alopecia, application site rxn
178
____ is a prodrug of ____ | Cidofovir & Brincidofovir
1. brincidofovir 2. cidofovir
179
# Foscarnet MOA
binds reversibly near the pyrophosphate-binding site of DNA polymerase and then blocks the cleavage of the pyrophosphate moeity from deoxynucleotide triphophate which halts DNA chain elongation
180
# Foscarnet Coverage
Herpes virus Hep B HIV
181
# Foscarnet Side Effects
GI Disturbances, injection site rxn, vision changes
182
What is foscarnet almost exclusively used for? | PPP
CMV- esp if ganciclovir cannot be used Acyclovir resistant HSV and VZV
183
# Docosanol MOA
inhibits the fusion between human cell plasma membrane and HSV envelope preventing viral entry into the cell and subsequent viral replication
184
# Docosanol Coverage
herpes labialis
185
# Docosanol Side Effects
application site rxn (redness, burning, dryness, swelling)
186
When is the best time to use Docosanol? At what point is efficacy reduced? | PPP
1. Best time is at the first sign of a cold sore 2. Efficacy is reduced if blisters have already formed.
187
Polyene Meds
Amphotericin B Nystatin
188
-azole derivatives
Clotrimazole Ketoconazole Fluconazole Itraconazole Voriconazole Posaconazole
189
Echinocandins
Anidulafungin Caspofungin Micafungin
190
# Nystatin MOA
binds to ergosterol
191
# Nystatin Time or concentration dependent? Fungicidal or Fungiostatic?
Concentration Dependent Fungicidal
192
# Nystatin Fungal Coverage
Aspergillus fumigatus Candida albicans Coccidoides immitis Cryptococcus neoformans Histoplasma capsulatum
193
# Nystatin Side Effects
Mouth irritation, n/v/d
194
How is Nystatin most commonly used? | PPP
Mouth rinse for thrush
195
# Amphotericin B MOA
binds to ergosterol in the fungal cell membrane, which leads to the formation of pores, ion leakage, and ultimately fungal cell death
196
# Amphotericin B Time or concentration dependent? Fungicidal or Fungiostatic?
Concentration Dependent Fungicidal
197
# Amphotericin B Overall Fungal Coverage
Broad Spectrum
198
# Amphotericin B What does it not cover fungally?
Candida lusitaniee, Aspergillus terreus, Scedosporium spp, Trichosporon spp
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# Amphotericin B Side Effets
- infusion rxn (chills, fever, anorexia, headache, hypotension, n/v) - Nephrotoxicity - Electrolyte abnormalities
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What must Amphotericin B standard formulation be given with? Why? | PPP
1. 5% dextrose in water 2. Precipitation
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Why is the lipid formulation of Amphotericin B preferred? | PPP
Less nephrotoxicity, fewer infusion related rxns
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# -azole derivatives MOA
inhibits the C14-alpha demethylation of lanosterol in fungi, which intereferes with the synthesis of ergosterol in the fungal cell membrane
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# -azole derivitaves Time or concentration dependent? Fungicidal or Fungistatic?
Time Dependent Fungistatic
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# -azole derivatives Clotrimazole Coverage
*Candida* spp *Malassezia furfur* Dermatophytes
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# -azole derivatives Ketoconazole Coverage
*Candida* spp *Malassezia furfur* Dermatophytes some dimorphic fungi
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# -azole derivatives Fluconazole Coverage
*Candida* spp (not glabrata or krusei) *Malassezia furfur* Dermatophytes *Cryptococcus neoformans* *Blastomyces dermatitidis* *Coccidioides immitis* *Histoplasma capsulatum* *Prototheca* spp Demitiaceous molds
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# -azole derivatives Itraconazole Coverage
Fluconazole coverage + *Aspergillus* spp *Sporothrix schenckii*
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# -azole derivatives Voriconazole Coverage
*Candida* spp (resistant strands) *Aspergillus* spp (Ampho B resistant *A. terreus*) *Fusarium* spp *Scedosporium apiospermum* *Trichosporon* spp molds
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# -azole derivatives Posaconazole
Fluconzole Coverage plus Zygomycetes
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# -azole derivatives Shared Side Effects
GI discomfort
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# -azole derivatives Clotrimazole Side Effects
skin irritation, elevated LFTs
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# -azole derivatives Ketonconazole Side Effects
acne, cracked/dry skin BB: hepatotoxicity
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# -azole derivatives Fluconazole Side Effects
rash
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# -azole derivatives Itraconazole Side Effects
Hypertension, hypokalemia BB: heart failure
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# -azole derivatives Voriconazole Side Effects
hepatotoxicity, visual disturbances, QT interval prolongation
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# -azole derivatives Posaconazole Side Effects
QT interval prolongation, hepatitis
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Which -azole derivative has the fewest drug-drug interactions via CYP enzymes? | PPP
Fluconazole
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In what environment should itraconazole/ketoconazole capsules be taken for optimal absorption? | PPP
I: Acidic- empty stomach K: acidic- with an acidic beverage
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What increases the bioavailability of posaconazole? | PPP
high fat meal- increases by 400%
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# Echinocandins MOA
inhibits beta-1,3,-D-glucan synthase which is an ezyme neccesary for the synthesis of an essential component of the fungal cell wall
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# Echinocandins Time or concentration dependent? Fungicidal or Fungistatic?
Concentration Dependent Fungicidal (Candida) Fungistatic (Aspergillus)
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# Echinocandins Fungal Coverage
*Candida* spp *Aspergillus* spp
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# Echinocandins Side Effects
All: infusion site rxn C/M: GI disturbances, electrolyte disturbances
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Why do echocandins have fewer drug-drug interactions than -azole derivatives? | PPP
Echocandins are not hepatically metabolized
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# Flucytosine MOA
penetrates the fungal cell wall which is converted to 5-fluorouracil which competes with uracil, this interfering with fungal RNA
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# Flucytosine Time or concentration dependent? Fungicidal or Fungistatic?
Concentration Dependent Fungistatic
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# Flucytosine Fungal Coverage
*Candida* spp Crypto spp
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# Flucytosine Side Effects
Bone marrow suppression, hepatotoxicity, enterocolitis, GI disturbances
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Why can Flucytosine not be used as a mono treatment?
Rapid development of resistance if used as mono treatment
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3 types of parasites
1. single cell organisms 2. multicellular helminths 3. ectoparasites
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Which areas are most impacted by parasitic infetions?
Tropical areas with poor sanitation
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Antimalarial Meds
Pyrimethamine Chloroquine/Hydroxycholorquine Artemether Artesunate Malarone Mefloquine Primaquine Tafenoquine
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# Pyrimethamine MOA
inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines
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# Pyrimethamine Parasitic Coverage
*Plasmodia* *Toxoplasma*
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# Pyrimethamine Side Effects
n/v, insomnia, anorexia
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# (Hydroxy)Cholorquine MOA
inhibits the formation of hemozoin (Hz) from the heme released by the digestion of hemoglobin (Hb). The free heme lyses membranes leading to parasitic death.
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# (Hydroxy)Chloroquine Parasitic Coverage
asexual erythrocytic stages of: * *Plasmodium falciparum* (not active against mature gametocytes) * *Plasmoidum vivax* * *Plasmodium malariae* * *Plasmodium ovale*
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# (Hydroxy)Chloroquine Side Effects
n/v, tremors, convulsions, coma
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# Artesunate and Artemether MOA
reacts with heme, generating free radicals which inhibit protein and nucleic acid synthesis of the Plasmodium parasites during all erythrocytic stages
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# Artesunate and Artemether Parasitic Coverage
All human malarial parasites including multi-drug resistant *Plasmodium falciparum* strains
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# Artesunate and Artemether Side Effects
QT prolongation, bradycardia, n/v/d
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What 2 drugs constitute Malarone?
atovaquone + proguanil
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# Malarone MOA of atovaquone
causes collapse of the parasitic mitochondrial membrane potential
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# Malarone MOA of proguanil
inhibits dihydrofolate reductase after CYP catalyzed cyclization
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# Malarone Parasitic Coverage of Atovaquone
asexual stages of many parasites
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# Malarone Parasitic Coverage of Proguanil
only used for the prevention of falciparum malaria
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# Malarone Side Effects
n/v, anorexia, insomnia, weakness
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# Mefloquine MOA
inhibit merozoite invasion and interact with proteins involved with lipid trafficking and nutrient uptake
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# Mefloquine Coverage
sexual forms of *Plasmodium* spp some activity against sexual forms of *P. vivax, malariae* and *ovale*
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# Mefloquine Side Effects
dizziness, anxiety, insomnia, vivid dreams, visual disturbances, depression, psychosis
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# Primaquine & Tafenoquine MOA
not well understood possibly generates reactive O2 species or interferes with ETC
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# Primaquine & Tafenoquine Parasitic Coverage
all stages of the plasmodium development in humans & *Pneumocystis jiroveci*
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# Primaquine & Tafenoquine What is radicle cure?
anti-relapse therapy
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# Primaquine & Tafenoquine Against what parasites do Primaquine & Tafenoquine induce radical cure? | PPP
*P. vivax* *P ovale*
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# Primaquine & Tafenoquine Side Effects
n/v/, tarry stools, dizziness, anorexia, hemolytic anemia
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Antihelmentics
Albenazole Mebendazole Ivermectin Praziquantel Pyrantel pamoate
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# Albendazole & Mebendazole MOA
Selectively bind to nematode beta-tubulin, inhibiting polymerization, thus preventing the formation of microtubules and so stopping cell division
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# Albendazole & Mebendazole Coverage
helminths and protozoa
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# Albendazole & Mebendazole Side Effects
prolonged courses can cause liver function abnormalities, bone marrow toxicity
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# Ivermectin MOA
influx of chloride ions through the cell membrane of invertebrates by activation of specifc ivermectin-sensitive ion channels. The hyperpolarization leads to muscle paralysis
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# Ivermectin Coverage
most nematode parasites, ectoparasites infeestations, helminth parasites
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# Ivermectin Side Effects
fever, myalgia, malaise, lightheadedness
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# Praziquantel MOA
causes a rapid calcium influx leading to severe spasms and paralysis of the worm
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# Praziquantel Coverage
trematodes except *Fasciola* spp
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# Praziquantel Side Effects
headache, dizziness, abd pain, nausea, ithcing
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Parasiticides
Permethrin Spinosad
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# Permethrin MOA
acts on the nerve cell membrane to disrupt the sodium channel current by which the polarization of the membrane is regulared leading to paralysis of the scabies/lice
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# Permethrin Coverage
lice, ticks, fleas, mites, other arthropods
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# Permetrin Side Effects
irritation, burning, itching
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# Spinosad MOA
alters the function of nicotinic and GABA-gated ion channels leading to rapid excitation of the parasites nervous system. Leads to involuntary muscle contractions, tremors, paralysis, and death.
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# Spinosad Coverage
lice, scabies
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# Spinosad Side Effects
application site rxns (redness, swelling, itching, burning)