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ID PHARM 152 > Antibiotics > Flashcards

Antibiotics Flashcards

1
Q

What is the MOA of Aminoglycosides?

A

Inhibit protein synthesis by inhibiting 30DS subunit of bacterial ribosome

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2
Q

What is common resistance pathways of Aminoglycosides?

A

Mutation or methylation of 16S rRNA-binding site
Enzymatic destruction of the drug
Lack of permeability to the drug molecule
Active effleurage
Lack of active transport

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3
Q

What organisms does Aminoglycosides work against?

A

Aerobic gnb

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4
Q

What organism can be covered with Aminoglycosides and penicillins (synergistic)?

A

Enterococci and streptococci

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5
Q

What is the dosage form for Aminoglycosides?

A

IV/IM

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6
Q

What are some pharmacokinetics of Aminoglycosides?

A

Penetrate tissues relatively poorly (not CNS)
Renal eliminations
Requires dose adjustment with renal dysfunction

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7
Q

Side Effects of Aminoglycosides

A

Nephrotoxicity
Ototoxicity
Neuromuscular blockade
Allergies rare

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8
Q

Drug Interactions with Aminoglycosides

A

Other nephrotoxic drugs
Other ototoxic drugs
Neuromuscular blocking agents

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9
Q

What are examples of fluroquinolones?

A

Ciprofloxacin
Levofloxacin
Moxifloxacin

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10
Q

MOA of Fluoroquinolones

A

Inhibit DNA gyrase or to poison erase II & IV

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11
Q

What are some examples of resistance of fluoroquinolones?

A

Alteration of the A and B subunit of DNA gyrase
Mutation in ParC or ParE of to poison erase IV
Change in outer membrane permeability
Effluent pumps

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12
Q

What is the spectrum of fluoroquinolones?

A

Highly active against gnb
haemophilus sp
Neisseriae
Chlamydiae

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13
Q

What is the spectrum of ciprofloxacin?

A

Most active against P aeruginosa

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14
Q

What is the spectrum of levofloxacin?

A

Activity against S. pneumoniae

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15
Q

What is spectrum of moxifloxacin?

A

Activity against anaerobes

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16
Q

Uses for fluoroquinolones

A

UTI
STIs
Lower resp tract infections
Enteritis/travellers diarrhea
Drug resistant mycobacteria’s infections

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17
Q

What are pharmacokinetics of fluoroquinolones?

A

Bacteriocidal
Excellent oral bioavailability

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18
Q

What is the dosage form of fluoroquinolones?

A

Normal PO
But available in IV

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19
Q

Pharmacokinetic facts about ciprofloxacin and levofloxacin

A

Renal elimination

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20
Q

Pharmacokinetics facts about moxifloxacin

A

Elimination from biliary pathway

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21
Q

Adverse Effects of Fluoroquinolones

A

Nausea, vomiting diarrhea
Insomnia, headache and dizziness
Seizures
Skin rashes
Impaired liver function
Tendinitis/tendon rupture
Prolongation of QTc interval
Hypo/hyperglycaemia
C. Difficult
peripheral neuropathy

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22
Q

Drug interaction of fluoroquinolone

A

Bind di and tri-valent cations
QTc prolongation
CYP 1A2 inhibition can result in increased levels of many drugs ( e.g. clozapine, duloxetine, methotrexate, quinapril, rasagiline, ropinirole, varenicline,etc)
Increased INR with warfarin

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23
Q

What is red flag patients for fluoroquinolones?

A

Renal Patients
Diabetes
<18 years old

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24
Q

What does sulfonamides work with?

A

Trimethoprim

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25
Q

What is the common drug of TMP/SMX?

A

Co-trimoxazole

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26
Q

What is the MOA of sulfamethoxazole?

A

Structural analogue of PABA
Competitively inhibits dihydrofolic acid synthesis

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27
Q

What is the MOA of trimethoprim?

A

Binds to dihydrofolate reductase therefore inhibiting the reduction of dihydrofolic acid to tetrahyrofolic acid

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28
Q

What is the resistance of TMP/SMX?

A

Ability of cell to use preformed folic acid

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29
Q

What is the spectrum of SMX and TMP

A

Wide spectrum of go, gn
Chlamydiae
Nocardiae
Protozoa

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30
Q

Spectrum of Activity Co-trimoxazole

A

Staphylococci - including MRSA
Streptococcus pneumonia
S. maltophilia
Moraxella
H. Influenza
Enterobacteriaciae
Brucellosis
Pneumocystis jirovecii

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31
Q

Uses for SMX/TMP

A

UTI
Skin and soft tissue infections (MRSA)
PJP
Many others

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32
Q

Adverse Effects of SMX/TMP

A

Skin rashes - can be severe
Hypersensitivity
Headache
GI (N,V,D)
Bone marrow suppression
Hyperkalemia & hyponatremia
Photosensitivity

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33
Q

Drug interaction with TMP/SMX

A

2C9 inhibitor; 3A4 substrate – increased levels of carvedilol, digoxin, phenytoin
Increased INR and bleeding with warfarin
Hypoglycemic agents – increased risk of hypoglycemia
Drugs which increase potassium levels

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34
Q

Contraindication for TMP/SMX

A

Cl in first and trimester of pregnancy
Caution in renal dysfunction

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35
Q

What is the MOA metronidazole?

A

Unknown but possible inhibition of nucleic acid synthesis and disruption

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36
Q

Resistance of Metronidazole

A

We do not know what because it is hard to test with anaerobic

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37
Q

Metronidazole spectrum

A

Anaerobes including C. Difficile
Protozoa - trichomonas, giardia etc.
propionibacterium are resistant

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38
Q

Dosage form of metronidazole

A

IV and Po
Excellent Bioavailability

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39
Q

Metronidazole Adverse effects

A

GI
Metallic taste
Headache
Dark urine
Peripheral neuropathy
Disulfiram-like reaction with alcohol
Insomnia
Stomatitis

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40
Q

Drug interaction of Metronidazole

A

Alcohol - disulfiram reaction
Warfarin - increased INR and bleeding

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41
Q

What is the MOA of linezolid

A

Inhibits protein synthesis

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42
Q

Spectrum for linezolid

A

Streptococci
Enterococci (VRE)
Staphylococci (MRSA)

Reserve for multi-drug resistant organisms

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43
Q

Dosage form of linezolid

A

Available IV and oral

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44
Q

Type of Antibiotic for Linezolid

A

Usually bacteriostatic
Bactericidal against streptococci

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45
Q

Linezolid is the oral alternative for what

A

Vancomycin

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46
Q

Linezolid Adverse Effects

A

Headache
Nausea, vomiting diarrhea
Rash
Increased LFT’s
Myelosuppression
Optic/peripheral neuropathy
Lactic acidosis
Decreased seizure threshold

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47
Q

Drug Interactions with Linezolid

A

Increased serotonin syndrome risk with SSRIs and MAOIs
Rifampin decreases linezolid levels

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48
Q

MOA Penicillin

A

bind to PBP resulting in inhibition of peptidoglycan synthesis and activation of autolytic enzymes in cell wall

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49
Q

How does resistance develop for Penicillin

A

production of beta-lactamases
lack of PBPs or altered PBPs
efflux of drug out of cell
failure to synthesize peptidoglycans such as mycoplasmas or metabolically inactive bacteria

50
Q

Give details Penicillin G

A

highly active against Gram positive bacteria and spirochetes
destroyed by beta lactamases
acid labile

51
Q

Give details Penicillin V

A

oral formulation
more acid stable but still needs to be taken on an empty stomach

52
Q

Penicillin Uses

A

for streptococci,
pneumococci,
meningococci,
spirochetes,
clostridia,
anaerobic gp rods
actinomyces
Enterococci

53
Q

MOA of
Methicillin, cloxacillin, flucloxacillin dicloxacillin

A

destroyed by beta-lactamases

54
Q

Used for
Methicillin, cloxacillin, flucloxacillin dicloxacillin

A

staphylococcal infections (staph aureus)
less gp activity otherwise

55
Q

Aminopenicillins active against

A

both gp and gn organisms

56
Q

MOA of Aminopenicillins

A

destroyed by beta-lactamases

57
Q

Ampicillin (pros and cons)

A

used IV
more acid stable than natural penicillins but poor bioavailability

58
Q

Amoxicillin ( pros and cons)

A

better absorption than ampicillin
available combined with clav

59
Q

Aminopenicillins spectrum

A

Streptococci, enterococci, Neiserria sp., non-beta-lactamase producing H. influenzae, E. coli, P. mirabilis, Salmonella

60
Q

Clavulanic acid MOA

A

a beta lactamase inhibitor
open rings to make them no longer active

61
Q

ESBLs

A

extended spectrum beta lactamases found in E.coli and klebsiella pneumoniae

62
Q

NDM like

A

New delhi metallo-beta-lactamase
acinetobacter baumannii

63
Q

What type of antibiotics Ureidopenicillins?

A

piperacillin

64
Q

Ureidopenicllins spectrum

A

pseudomonas aeruginosa

65
Q

What are the pharmacokinetics factors of penicillins?

A

oral bioavailability varies
wide tissue distribution including CNS
most are excreted by the kidneys
generally short half life

66
Q

Can you take penicillin when pregnant or breastfeeding?

A

They are safe for pregnancy but it distributed to breast milk

67
Q

What are the counselling points of penicillins?

A

taken on an empty stomach except for amoxicillin

68
Q

Adverse effects of penicillin

A

allergic reactions
anaphylactic shock
serum sickness
skin rashes
fever, nephritis, eosinophilia
seizures, encephalography, delirium
electrolyte imbalances
neutropenia, thrombocytopenia
diarrhea, gi upset

69
Q

Cephalosporins MOA

A

same as penicillins
destroys beta lactams

70
Q

Cephalosporins resistance

A

Lack of PBP or altered PBP with reduced affinity
Beta-lactamase production*
*Resistant to beta-lactamases produced by Staph aureus and common gnb
Efflux
Inability of drug to penetrate

71
Q

First Generation cephalosporins

A

cephalexin and cefadroxil

72
Q

What is the spectrum for first gen cephalosporins?

A

active against gpc NOT enterococci or MRSA and some gnb
e. coli, proteus and klebisella

73
Q

Second gen cephalosporins

A

cefuroxime
cefprozil

74
Q

Spectrum of second gen cephalosporins

A

active against organisms covered by first gen
greater coverage of gnb, but not pseudomonase aeruginosa

75
Q

Third gen cephalosporin

A

cefotaxime
ceftriaxone
ceftazidime
cefixime

76
Q

What is the spectrum of 3 gen cephalosporin?

A

decreased activity against gpc except strep pneumoniae
enhanced activity against gnb
ability to penetrate the CNS

77
Q

When is ceftazidime reserved for?

A

ps. aeruginosa

78
Q

Fourth gen Cephalosporins

A

cefepime
ceftaroline and ceftobioprole

79
Q

Spectrum of cefepime

A

enhanced activity against enterobacter and citrobacter
active against ps. aeruginosa

80
Q

Spectrum of ceftaroline and ceftobiprole

A

activity against MRSA, ampicillin sensitive E. faecalis and penicillin resistance S. pneumoniae

81
Q

Adverse Effects for Cephalosporins

A

hypersensitivity
diarrhea
skin rash
other - fever
granulocytopenia
hemolytic
anemia

82
Q

What side effect specific to ceftriaxone?

A

biliary pseudolithiasis

83
Q

Carbapenems (two types)

A

imipenem
ertapenem

84
Q

Examples of imipenem

A

cilastatin
meropenem

85
Q

What is the spectrum imipenem?

A

gram positive, gram negative, including Pseudomonas, and anaerobic organisms

86
Q

What is the spectrum ertapenem?

A

long half-life (once daily); poor activity against Enterococcus sp and P. aeruginosa

87
Q

MOA of imipenem

A

inactivated by renal dihydropeptidases

88
Q

MOA of cilastatin

A

peptidase inhibitor

89
Q

MOA of monobactams

A

monocyclic beta lactam ring
resistant to beta lactamases

90
Q

What is monobactams’s spectrum?

A

Active against gnb including Ps. Aeruginosa
not active against ESBL or AmpC producers

91
Q

Macrolides

A

erythromycin
clarithromycin
azithromycin

92
Q

MOA of macrolides

A

attach to the 23S rRNA on the 50S subunit of bacterial ribosome resulting in inhibition of protein synthesis

93
Q

What is macrolides resistance?

A

methylation of the rRNA receptor
Inactivating enzymes
Active efflux

94
Q

Spectrum of activity for macrolides

A

Gram positive – pneumococci, streptococci and corynebacteria (reserved for penicillin allergic patients)
M pneumoniae
Chlamydia trachomatis
C. pneumophilia
Bordatella pertussis
Campylobacter jejuni
Helicobacter pylori

95
Q

What is the adverse effects of erythromycin?

A

Gi
Increased liver function tests (LFTs)
Cholestatic hepatitis – increased with estolate and pregnancy
QT prolongation/cardiac arrhythmias particularly when combined with CYP 3A inhibitors

96
Q

Clarithromycin and azithromycin spectrum

A

Enhanced activity against a variety of organisms such as L. pneumophilia, Chlamydia trachomatis, Chlaydiophila pneumoniae, Moraxella catarrhalis, H. influenzae (azithro), Mycobacterium avium complex and other mycobacteria

some MRSA cases

97
Q

Azithromycin and its half life (what gets affected)

A

long half life leads to long intracellular concentrations
5 days of azith = 10 days of therapy
long periods of sub inhibitory concentrations may lead to more resistance

98
Q

Uses for macrolides

A

upper respiratory tract infections
STI
acne

99
Q

DI with macrolides

A

erythro and clarith are both inhibitors of CYP3A4

100
Q

Clindamycin MOA

A

attach to the 23S rRNA on the 50S subunit of bacterial ribosome resulting in inhibition of protein synthesis

101
Q

Clindamycin spectrum

A

anerobes
S. aureus including some MRSA as well as streptococci

102
Q

Uses for Clindamycin

A

used in pt with pen allergies or resistant organisms

103
Q

Clindamycin adverse effects

A

Nausea, vomiting, diarrhea
Rash
Elevated LFTs
Esophageal irritation
Associated with C. difficile diarrhea

104
Q

Tetracyclines

A

tetracycline, minocycline, doxycycline

105
Q

Tetracyclines MOA

A

inhibit binding of aminoacyl-tRNA to the 30S unit of ribosome thereby inhibiting protein syntehsis

106
Q

Tetracyclines mechanism of resistance

A

active against many gram positive and negative but high rates of resistance

107
Q

Tetracyclines drugs of choice for

A

rickettsiae
bartonella
chlamydiae
m. pneumoniae
nocardia
p. acnes

108
Q

Tetracyclines adverse effects

A

Gi upset (N, V, D)
Skin rashes
Photosensitivity
Yeast overgrowth
Deposited in bones and teeth; do not use in children < 8 years old
Hepatitis

109
Q

What are adverse effects specific for minocycline?

A

vestibular toxicity (dizziness, vertigo, ataxia)
more hypersentivity reactions

110
Q

DI with tetracyclines

A

some anticonvulsants may reduce tetracyclines
divalent and trivalent reduce absorption
increased INR and bleeding with warfarin

111
Q

Glycylcines

A

vancomycin

112
Q

Glycylcines MOA

A

inhibits cell wall peptidoglycan

113
Q

Glycyclines spectrum

A

gpc in particular enterococci, PRSP and MRSA; active against clostridia, Clostrioides and some bacilli

114
Q

Glycylcines resistance

A

VRE, S. aureus (VISA)

115
Q

Glycyclines elimination factors

A

eliminated through biliary tract and feces

116
Q

Vancomycin PO is used for

A

c. difficile

117
Q

Vancomycin Adverse Effects

A

nephrotoxicity
ototoxicity
red-man syndrome
granulocytopenia

118
Q

Similar drugs to vancomycin

A

teicoplanin
daptomycin

119
Q

Details about teicoplanin

A

structurally similar to vancomycin

120
Q

details about Daptomycin

A

lipopeptide; parenteral; once daily; major adverse effect is myopathy

ID PHARM 152 (11 decks)

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