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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
What is the common drug of TMP/SMX?
Co-trimoxazole
26
What is the MOA of sulfamethoxazole?
Structural analogue of PABA Competitively inhibits dihydrofolic acid synthesis
27
What is the MOA of trimethoprim?
Binds to dihydrofolate reductase therefore inhibiting the reduction of dihydrofolic acid to tetrahyrofolic acid
28
What is the resistance of TMP/SMX?
Ability of cell to use preformed folic acid
29
What is the spectrum of SMX and TMP
Wide spectrum of go, gn Chlamydiae Nocardiae Protozoa
30
Spectrum of Activity Co-trimoxazole
Staphylococci - including MRSA Streptococcus pneumonia S. maltophilia Moraxella H. Influenza Enterobacteriaciae Brucellosis Pneumocystis jirovecii
31
Uses for SMX/TMP
UTI Skin and soft tissue infections (MRSA) PJP Many others
32
Adverse Effects of SMX/TMP
Skin rashes - can be severe Hypersensitivity Headache GI (N,V,D) Bone marrow suppression Hyperkalemia & hyponatremia Photosensitivity
33
Drug interaction with TMP/SMX
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
34
Contraindication for TMP/SMX
Cl in first and trimester of pregnancy Caution in renal dysfunction
35
What is the MOA metronidazole?
Unknown but possible inhibition of nucleic acid synthesis and disruption
36
Resistance of Metronidazole
We do not know what because it is hard to test with anaerobic
37
Metronidazole spectrum
Anaerobes including C. Difficile Protozoa - trichomonas, giardia etc. propionibacterium are resistant
38
Dosage form of metronidazole
IV and Po Excellent Bioavailability
39
Metronidazole Adverse effects
GI Metallic taste Headache Dark urine Peripheral neuropathy Disulfiram-like reaction with alcohol Insomnia Stomatitis
40
Drug interaction of Metronidazole
Alcohol - disulfiram reaction Warfarin - increased INR and bleeding
41
What is the MOA of linezolid
Inhibits protein synthesis
42
Spectrum for linezolid
Streptococci Enterococci (VRE) Staphylococci (MRSA) Reserve for multi-drug resistant organisms
43
Dosage form of linezolid
Available IV and oral
44
Type of Antibiotic for Linezolid
Usually bacteriostatic Bactericidal against streptococci
45
Linezolid is the oral alternative for what
Vancomycin
46
Linezolid Adverse Effects
Headache Nausea, vomiting diarrhea Rash Increased LFT’s Myelosuppression Optic/peripheral neuropathy Lactic acidosis Decreased seizure threshold
47
Drug Interactions with Linezolid
Increased serotonin syndrome risk with SSRIs and MAOIs Rifampin decreases linezolid levels
48
MOA Penicillin
bind to PBP resulting in inhibition of peptidoglycan synthesis and activation of autolytic enzymes in cell wall
49
How does resistance develop for Penicillin
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
Give details Penicillin G
highly active against Gram positive bacteria and spirochetes destroyed by beta lactamases acid labile
51
Give details Penicillin V
oral formulation more acid stable but still needs to be taken on an empty stomach
52
Penicillin Uses
for streptococci, pneumococci, meningococci, spirochetes, clostridia, anaerobic gp rods actinomyces Enterococci
53
MOA of Methicillin, cloxacillin, flucloxacillin dicloxacillin
destroyed by beta-lactamases
54
Used for Methicillin, cloxacillin, flucloxacillin dicloxacillin
staphylococcal infections (staph aureus) less gp activity otherwise
55
Aminopenicillins active against
both gp and gn organisms
56
MOA of Aminopenicillins
destroyed by beta-lactamases
57
Ampicillin (pros and cons)
used IV more acid stable than natural penicillins but poor bioavailability
58
Amoxicillin ( pros and cons)
better absorption than ampicillin available combined with clav
59
Aminopenicillins spectrum
Streptococci, enterococci, Neiserria sp., non-beta-lactamase producing H. influenzae, E. coli, P. mirabilis, Salmonella
60
Clavulanic acid MOA
a beta lactamase inhibitor open rings to make them no longer active
61
ESBLs
extended spectrum beta lactamases found in E.coli and klebsiella pneumoniae
62
NDM like
New delhi metallo-beta-lactamase acinetobacter baumannii
63
What type of antibiotics Ureidopenicillins?
piperacillin
64
Ureidopenicllins spectrum
pseudomonas aeruginosa
65
What are the pharmacokinetics factors of penicillins?
oral bioavailability varies wide tissue distribution including CNS most are excreted by the kidneys generally short half life
66
Can you take penicillin when pregnant or breastfeeding?
They are safe for pregnancy but it distributed to breast milk
67
What are the counselling points of penicillins?
taken on an empty stomach except for amoxicillin
68
Adverse effects of penicillin
allergic reactions anaphylactic shock serum sickness skin rashes fever, nephritis, eosinophilia seizures, encephalography, delirium electrolyte imbalances neutropenia, thrombocytopenia diarrhea, gi upset
69
Cephalosporins MOA
same as penicillins destroys beta lactams
70
Cephalosporins resistance
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
First Generation cephalosporins
cephalexin and cefadroxil
72
What is the spectrum for first gen cephalosporins?
active against gpc NOT enterococci or MRSA and some gnb e. coli, proteus and klebisella
73
Second gen cephalosporins
cefuroxime cefprozil
74
Spectrum of second gen cephalosporins
active against organisms covered by first gen greater coverage of gnb, but not pseudomonase aeruginosa
75
Third gen cephalosporin
cefotaxime ceftriaxone ceftazidime cefixime
76
What is the spectrum of 3 gen cephalosporin?
decreased activity against gpc except strep pneumoniae enhanced activity against gnb ability to penetrate the CNS
77
When is ceftazidime reserved for?
ps. aeruginosa
78
Fourth gen Cephalosporins
cefepime ceftaroline and ceftobioprole
79
Spectrum of cefepime
enhanced activity against enterobacter and citrobacter active against ps. aeruginosa
80
Spectrum of ceftaroline and ceftobiprole
activity against MRSA, ampicillin sensitive E. faecalis and penicillin resistance S. pneumoniae
81
Adverse Effects for Cephalosporins
hypersensitivity diarrhea skin rash other - fever granulocytopenia hemolytic anemia
82
What side effect specific to ceftriaxone?
biliary pseudolithiasis
83
Carbapenems (two types)
imipenem ertapenem
84
Examples of imipenem
cilastatin meropenem
85
What is the spectrum imipenem?
gram positive, gram negative, including Pseudomonas, and anaerobic organisms
86
What is the spectrum ertapenem?
long half-life (once daily); poor activity against Enterococcus sp and P. aeruginosa
87
MOA of imipenem
inactivated by renal dihydropeptidases
88
MOA of cilastatin
peptidase inhibitor
89
MOA of monobactams
monocyclic beta lactam ring resistant to beta lactamases
90
What is monobactams's spectrum?
Active against gnb including Ps. Aeruginosa not active against ESBL or AmpC producers
91
Macrolides
erythromycin clarithromycin azithromycin
92
MOA of macrolides
attach to the 23S rRNA on the 50S subunit of bacterial ribosome resulting in inhibition of protein synthesis
93
What is macrolides resistance?
methylation of the rRNA receptor Inactivating enzymes Active efflux
94
Spectrum of activity for macrolides
Gram positive – pneumococci, streptococci and corynebacteria (reserved for penicillin allergic patients) M pneumoniae Chlamydia trachomatis C. pneumophilia Bordatella pertussis Campylobacter jejuni Helicobacter pylori
95
What is the adverse effects of erythromycin?
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
Clarithromycin and azithromycin spectrum
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
Azithromycin and its half life (what gets affected)
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
Uses for macrolides
upper respiratory tract infections STI acne
99
DI with macrolides
erythro and clarith are both inhibitors of CYP3A4
100
Clindamycin MOA
attach to the 23S rRNA on the 50S subunit of bacterial ribosome resulting in inhibition of protein synthesis
101
Clindamycin spectrum
anerobes S. aureus including some MRSA as well as streptococci
102
Uses for Clindamycin
used in pt with pen allergies or resistant organisms
103
Clindamycin adverse effects
Nausea, vomiting, diarrhea Rash Elevated LFTs Esophageal irritation Associated with C. difficile diarrhea
104
Tetracyclines
tetracycline, minocycline, doxycycline
105
Tetracyclines MOA
inhibit binding of aminoacyl-tRNA to the 30S unit of ribosome thereby inhibiting protein syntehsis
106
Tetracyclines mechanism of resistance
active against many gram positive and negative but high rates of resistance
107
Tetracyclines drugs of choice for
rickettsiae bartonella chlamydiae m. pneumoniae nocardia p. acnes
108
Tetracyclines adverse effects
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
What are adverse effects specific for minocycline?
vestibular toxicity (dizziness, vertigo, ataxia) more hypersentivity reactions
110
DI with tetracyclines
some anticonvulsants may reduce tetracyclines divalent and trivalent reduce absorption increased INR and bleeding with warfarin
111
Glycylcines
vancomycin
112
Glycylcines MOA
inhibits cell wall peptidoglycan
113
Glycyclines spectrum
gpc in particular enterococci, PRSP and MRSA; active against clostridia, Clostrioides and some bacilli
114
Glycylcines resistance
VRE, S. aureus (VISA)
115
Glycyclines elimination factors
eliminated through biliary tract and feces
116
Vancomycin PO is used for
c. difficile
117
Vancomycin Adverse Effects
nephrotoxicity ototoxicity red-man syndrome granulocytopenia
118
Similar drugs to vancomycin
teicoplanin daptomycin
119
Details about teicoplanin
structurally similar to vancomycin
120
details about Daptomycin
lipopeptide; parenteral; once daily; major adverse effect is myopathy

ID PHARM 152 (11 decks)

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