ANTIBACTERIALS Flashcards
1
Q
BACTERICIDAL vs BACTERIOSTATIC
A
- BACTERICIDAL
o can eradicate an infection in the absence of host defense mechanisms
o kills bacteria
o Generalization: those that inhibit cell wall synthesis and
nucleic acid synthesis - BACTERIOSTATIC
o inhibits microbial growth but requires host defense
mechanisms to eradicate the infection
o does not kill bacteria
o Those that inhibit protein synthesis except
aminoglycosides which are -cidal
2
Q
o as the plasma level is increased above the MIC, an increasing
proportion of bacteria are killed and at a more rapid rate
WHAT MODE OF ANTIBACTERIAL ACTION?
A
CONCENTRATION-DEPENDENT KILLING ACTION
3
Q
o efficacy is directly related to time above MIC
o efficacy independent of concentration once the MIC has been
reached
o EXAMPLES: Penicillins, cephalosporins
WHAT MODE OF ANTIBACTERIAL ACTION?
A
TIME-DEPENDENT KILLING ACTION
4
Q
o seen in aminoglycosides & quinolones
o killing action continues when their plasma levels have
declined below measurable levels
o greater efficacy when administered as single large dose
o toxicity depends on a critical plasma concentration and on
the time such a level is exceeded
▪ shorter with single large dose than multiple small doses
▪ basis for once-daily aminoglycoside dosing protocols
WAHT MODE OF ANTIBIOTIC ACTION?
A
POST-ANTIBIOTIC EFFECT
5
Q
MOA: * binds to penicillin-binding proteins (PBPs) located in the
bacterial cytoplasmic membrane
* inhibits the transpeptidation reaction that cross-links the
linear peptidoglycan chain constituents of the cell wall
A
BETA-LACTAM ANTIBIOTICS: PENNICILIN
6
Q
what are 3 mechanisms of resistance development to penicillin?
A
- Enzymatic hydrolysis of beta-lactam ring by formation of betalactamases
(penicillinases)
o EXAMPLE: Staphylococcus aureus - Structural change in target PBPs
o EXAMPLES: MRSA, Pneumococci, Enterococci - Changes in the porin structures in outer cell wall impeding access of
Penicillins to PBPs
o EXAMPLE: Pseudomonas aeruginosa
7
Q
Examples od Beta Lactamase Inhibitors? (3)
A
(Clavulanic Acid, Sulbactam,
Tazobactam)
8
Q
2 notable SE of penicillin?
A
1) Hypersensitivity, cross allergenicity with other penicillins
* 2) Gastrointestinal Upset
* Think first of these two for the SE of pens
9
Q
DOC for syphilis?
Also for streptococcal, pneumococcal, meningococcal,
G+ bacilli, spirochete infection
A
PENICILLIN G (IV), PENICILLIN V (oral)
10
Q
Long Actin IM preparations of penicillin?
A
Benzathine Penicillin & Procaine Penicillin
11
Q
What drug prolongs the effect of penicillin? because the renal tubular secretion is inhibited
A
Probenecid
12
Q
Penicillins Used for staphylococcal infections
A
Methicillin, nafcillin, oxacillin,
Cloxacillin, dicloxacillin
13
Q
Penicillin that causes
1. Interstitial nephritis????
2. Neutropenia???
A
Interstitial nephritis (methicillin),
Neutropenia (“N”afcillin)
Methicillin – not clinically used – high SE
14
Q
Resistant to inactivation by beta-lactamase
(penicillinase) – IMPORTANT!
A
Methicillin, nafcillin, oxacillin,
Cloxacillin, dicloxacillin
15
Q
Side effect of ampicillin and amoxicillin?
A
Pseudomembranous colitis and Rash (ampicillin)
16
Q
What penicillin?Greater activity against G(-) infections. Infections due to
Pseudomonas, Enterobacter and Klebsiella
A
Piperacillin, Ticarcillin, Carbenicillin
(antipseudomonals)
17
Q
Synergistic with aminoglycosides against Pseudomonas
A
Piperacillin, Ticarcillin, Carbenicillin
18
Q
EXTENDED SPECTRUM PENICILLINS
A
Ampicillin, Amoxicillin
19
Q
Describe the antimicrobial coverage of extended spectrum
Penicillins (HELPSE):
A
“Amoxicillin HELPS kill Enterococci”
Haemophilus influenzae
Escherichia coli
Listeria monocytogenes
Proteus mirabilis
Salmonella sp.
Enterococci
20
Q
What are the antipseudomonals penicillins?
A
TCP: Takes Care of Pseudomonas
Ticarcillin Carbenicillin Piperacillin
21
Q
What are the diseases associated with Pseudomonas?
A
Pneumonia
Sepsis
Ecthyma gangrenosum,
UTI,
DM,
Otitis externa, Mucopolysaccharidoses –
Cystic Fibrosis, Osteomyelitis,
Nosocomial infection (HAP and VAP)
Skin infection (in burns and hot tub folliculitis)
22
Q
**Bactericidal; mostly IV; all have renal excretion
what drug class?
A
CEPHALOSPORINS
**Bactericidal; mostly IV; all have renal excretion
EXCEPT Cefoperazone and Ceftriaxone **
23
Q
Which microbes are covered by the spectrum of activity of first
generation cephalosporins?
A
PEcK FIRST
Proteus mirabilis
Escherichia coli
Klebsiella pneumoniae
24
Q
How do you remember first generation cephalosporins?
A
FIRST GENERATION CEPHALOSPORINS
FADer, help me FAZ my PHarmacology boards!
CeFADroxil
CeFAZolin
CePHapirin
CePHalexin
CePHalothin
CePHradine
25
Which microbes are covered by the spectrum of activity of
second generation cephalosporins?
HEN PEcKS
Haemophilus influenzae
Enterobacter aerogenes
Neisseria spp.
Proteus mirabilis
Escherichia coli
Klebsiella pneumoniae
Serratia marcescens
26
How do you remember second generation cephalosporins?
SECOND GENERATION CEPHALOSPORINS
In a FAMily gathering, you see your
FOXy cousin wearing a FUR coat and drinking TEA.
CeFAMandole, CeFOXitin,
CeFURoxime, CefoTEtan
FAC! LORA the PROfessional AZhOLE is still on the FONe.
CeFAClor, LORAcarbef, CefPROzil,
CefmetAZOLE, CeFONicid
27
ANTI-PSEUDOMONAL CEPHALOSPORINS?
ANTI-PSEUDOMONAL CEPHALOSPORINS
Ceftazidime Cefepime Cefoperazone
28
General Mnemonics in classifying the generation of the cephalosphorin
1st Generation: Starts with CEPH. Including DRO+ZOL. (CefaDROxil and
CefaZOLin) they start in CEF but are 1st gen
2nd Generation: Starts with CEF. Doesn’t end in -ONE and -IME, plus LORA
ceFU!!!! (dapat with feelings na parang inaaway mo si LORA!
(LORAcarbef and Cefuroxime)
3rd Generation: Starts with CEF. Ends in -ONE and -IME. Plus Moxi Dinir,
Ditoren, Buten.
4th Generation: Cefipime, Cefipirome
29
First Generation Ceph used in surgical prophylaxis?
CEFAZOLIN
30
What generation? Cefazolin, Cefadroxil, Cephalexin,
Cephalothin, Cephapirin, Cephradine
First Generation
31
What generation?
Cefaclor, Cefamandole, Cefmetazole, Cefonicid, Cefuroxime,
Cefprozil, Ceforanide, Cefoxitin, Cefotetan, Loracarbef
Second
32
what second gen ceph causes a disulfiram reaction?
Cefamandole,
Cefotetan
33
2nd Gen Ceph that has Improved action against
pneumococcus and H. influenzae
Cefuroxime
34
Second gen ceph that has Good activity against B. fragilis
(abdominal and pelvic infections) (2)
Cefotetan and cefoxitin
35
What generation?
Cefoperazone, Cefotaxime, Ceftazidime, Ceftizoxime,
Ceftriaxone, Cefixime, Cefpodoxime Proxetil, Cefdinir,
Cefditoren Pivoxil, Ceftibuten, Moxalactam
Third Generation Ceph
36
What generation has this use:
Decreased gram-positive coverage. Increased gramnegative
activity (Pseudomonas, Bacteroides), against
Providencia, Serratia, Neisseria, Haemophilus
Third Gen
37
DOC for Gonorrhea? (2)
Ceftriaxone and Cefixime
38
Third Gen Ceph that causes DISULFIRAM REACTION?
CEFOPERAZONE
39
What Third Gen Ceph?
All have renal excretion except (2)
Cefoperazone and
Ceftriaxone
40
What Third Gen Ceph?
All penetrate BBB except (2)
Cefoperazone and
Cefixime
41
What Third Gen Ceph?
Has very good CNS penetration
Ceftriaxone
42
What 3rd Gen ceph?
Has very good action on pseudomonas
Ceftazidime
43
What 3rd Gen Ceph?
Most active against Penicillin
resistant S. pneumoniae (2)
Ceftriaxone and Cefotaxime
44
Cefepime, Ceftaroline (5th in other references), Cefpirome
What Generation?
4th
45
MOA: Binds to penicillin-binding proteins. Inhibits
transpeptidation in bacterial cell walls.
MONOBACTAM: Aztreonam
46
is the silver bullet. It is design for gram negative
rods. Pseudomonas is a gram-negative rod.
AZTREONAM
47
MOA: Binds to penicillin-binding proteins. Inhibits
transpeptidation in bacterial cell walls.
CARBAPENEMS: IMIPENEM-CILASTATIN, ERTAPENEM, MEROPENEM,
DORIPENEM
48
CARBAPENEMS:
All are active against Pseudomonas and
Acinetobacter EXCEPT ?
ERTAPENEM
49
CARBAPENEMS:
inhibits renal metabolism (Hydrolysis) of
imipenem by Dihydropeptidase (thus given together)
CILASTATIN
50
Most important mechanism of carbapenem resistance?
Production of carbapenemases (carbapenem-hydrolyzing
enzymes) is the most important mechanism of carbapenem
resistance
Other methods of resistance: Porins, efflux pumps, mutations in
penicillin-binding proteins
51
Inhibits inactivation of Penicillins by bacterial betalactamase
(penicillinase)
give 3 drugs?
Clavulanic acid, Sulbactam, Tazobactam
52
Most active against plasmid encoded beta lactamases
(Gonococci, Streptococci, E coli and H. Influenzae)
Not good inhibitor of inducible chromosomal beta
lactamases (Enterobacter, Pseudomonas, Serratia)
Clavulanic acid, Sulbactam, Tazobactam
53
MOA: Inhibits cell wall synthesis by binding to the D-Ala-DAla
terminus of peptidoglycan → inhibit
transglycosylation → prevent elongation and crosslinking
of peptidoglycan chain
Vancomycin, Teicoplanin, Dalbavancin, Telavancin
54
NOTABLE SIDE EFFECT ODF VANCOMYCIN?
Red Man syndrome
55
VANCOMYCIN:
VRSA and VRE are due to
due to D-Ala-D-Lactate formation
Must knows:
● Vancomycin – D-Ala-D-Ala (Dala Dala niya yung Vanco!). Redman
syndrome
● Baci(+)racin – For gram (+), (+)oxic, (+)opical use
56
MOA: Interferes with a late stage in cell wall synthesis in
gram-positive organisms
PEPTIDE ANTIBIOTICS: BACITRACIN
Must knows:
● Vancomycin – D-Ala-D-Ala (Dala Dala niya yung Vanco!). Redman
syndrome
● Baci(+)racin – For gram (+), (+)oxic, (+)opical use
57
MOA: Blocks incorporation of D-Ala into the pentapeptide
side chain of the peptidoglycan
Cycloserine
58
MOA: Binds to cell membrane
causing depolarization
and rapid cell death
DAPTOMYCIN
59
MOA: Cationic detergents.
Attach to and disrupt
bacterial cell membrane,
bind and inactivate
endotoxin. Bactericidal.
POLYMYXIN B,
Polymyxin E
60
MOST NOTBALE SIDE EFFECT OF DAPTOMYCIN?
Myopathy
Monitor Creatine
Phosphoki nase weekly
61
What drug?
* More rapidly
bactericidal than
Vancomycin
* Inactivated by
pulmonary surfactants
so cannot be used
against pneumonia
DAPTOMYCIN
62
* Proteus and Neisseria
are resistant
* For Topical use only (to
limit toxicity)
* *Both are Preg Cat C
what drug?
POLYMIXIN B AND E
63
MOA: MOA: Inactivates the enzyme UDP-Nacetylglucosamine-
3-enolpyruvyltransferase
which is important in peptidoglycan synthesis
(very early stage of bacterial cell wall synthesis)
USE: Uncomplicated UTI; safe for pregnant
patients; renal excretion; resistance emerges
rapidly
FOSFOMYCIN
64
Which antibiotics are considered drugs of last resort?
I" AM your Last Shot at Victory"
Imipenem
Amikacin
Meropenem
Linezolid
Streptogramins
Vancomycin
65
What are the protein synthesis inhibitors?
“AT CELLS”
Aminoglycosides
Tetracyclines
Chloramphenicol (HNBS)*
Erythromycin (Macrolides)
Lincosamides (Clindamycin)
Linezolid
Streptogramins
66
All bacterial protein synthesis inhibitors are bacteriostatic except ???, ???, ???
to the
following bugs: Hemophilus, Neisseria, Bacteroides and Streptococcus
pneumoniae.
Aminoglycosides, Streptogramins, and Chloramphenicol
67
(+)/(-) Mycoplasma pneumoniae,Chlamydia, Rickettsia
and Vibrio, and other atypical organisms
WAHT DRUG?
Tetracycline, Doxycycline, Minocycline,
Tigecycline, Demeclocycline, Lymecycline
(All are Preg Cat D)
68
WHat tetracycline is used in SIADH?
Demeclocycline
69
What tetracycline is used in CAP and Bronchitis; Lyme disease
Doxycycline
70
Most notable SE of Tetracycline
GI disturbance, Teratogen (tooth enamel dysplasia/
discoloration),
MNEMONICS:
T = TeTracyclines
Block aTTachment of T-RNA to acceptor site
Teeth-racycline = tooth enamel dysplasia / discoloration
71
Mechanism of resistance to tetracycline?
Resistance:
* 1) Development of efflux pumps for active extrusion
of tetracyclines
* 2) Formation of ribosomal protection proteins that
interfere with tetracycline binding
72
* Derivative of: MINOCYCLINE
* Broadest spectrum + longest t½ (30-
36hrs)
* Given IV only and is unaffected by
common tetracycline resistance
mechanisms.
what drug?
TIGECYCLINE
73
Inhibits transpeptidation (catalyzed by
peptidyl transferase)
What drug?
Chlorampenicol
74
Most notable SE of chlorampenicol?
Aplastic anemia
(idiosyncratic), Gray baby syndrome,
75
Mechanism of resistance to chlorampenicol?
Resistance is due to the formation of
acetyltransferase that inactivates drug
76
is a bacteriostatic antibiotic but is
bactericidal to the ff: Hemophilus influenza, Neisseria,
Bacteroides and Streptococcus pneumoniae.
Chlorampenicol
77
is the way to metabolize chloramphenicol
Glucoronidation
premature neonates are deficient in hepatic
glucuronosyltransferase
78
characterized by decreased red
blood cells, cyanosis and
cardiovascular collapse
* Characteristic ashen gray skin
Gray baby syndrome
79
Drug class?
ERYTHROMYCIN, AZITHROMYCIN, CLARITHROMYCIN,
TELITHROMYCIN, ROXITHROMYCIN
Macrolides
80
Most notable SE of MACROLIDES?
Gastrointestinal upset, QT prolongation,
Cholestatic hepatitis,
81
All macrolides inhibit CYP450 EXCEPT
Azithromycin
82
What macrolide has Biliary excretion?
Erythromycin
83
What macrolide has hepatic and urinary excretion?
Clarithromycin
84
MEchanism of resistance of MACROLIDES
Resistance is due to development of efflux pumps and
production of methylase enzyme
85
What drug?
has a good pharmacokinetic profile.
has a tremendous 4-day half-life and has
a high volume of distribution. It is greater in tissue
macrophage than the plasma level.
Azithromycin
86
WHAT MACROLIDE?
Highest Vd and slowest elimination???
Used for macrolide-resistance???
Azithromycin
Telithromycin
87
What drug class?
Clindamycin, Lincomycin
LINCOSAMIDES
88
Most notable SE of LINCOSAMIDES?
Can cause Pseudomembranous colitis (C. difficile
overgrowth
(CLINDAMYCIN AND LINCOMYCIN)
89
Mechanism of resistance of LINCOSAMIDES?
Resistance is due to methylation of binding sites and
enzymatic inactivation
90
??? for anaerobic infections ABOVE the diaphragm.
??? for anaerobic infections BELOW the diaphragm.
CLINDAMYCIN for anaerobic infections ABOVE the diaphragm.
* METRONIDAZOLE for anaerobic infections BELOW the diaphragm.
91
WHAT DRUG?
Binds to the 23S ribosomal RNA of 50S subunit
OXAZOLIDINONE: LINEZOLID, TEDIZOLID
92
What drug is used?
Drug-resistant gram-positive cocci such as Staphylococci
and Enterococcus (MRSA, VRSA, VRE), Listeria,
Corynebacteria
OXAZOLIDINONE: Linezolid, Tedizolid
From the parent compound name, meron sila lahat ZOLID
93
Binds 50S subunit. Bactericidal.
what drug?
STREPTOGRAMIN: Quinupristin-Dalfopristin
94
What drug class?
Gentamicin, Tobramycin
AMINOGLYCOSIDES
95
Most notable SE of Streptogramins: Quinupristin-Dalfopristin
severe Arthralgia-myalgia
syndrome
96
Multi Drug-Resistant Tuberculosis (2nd line drug)
AMIKACIN
97
WAHT AMINOGLYCOSIDES?
Synergistic with: Beta-lactams
* LEAST RESISTANCE but
* NARROWEST therapeutic window
AMIKACIN
98
Uses: Tuberculosis, Tularemia, Bubonic plague, Brucellosis,
Enterococcal endocarditis
SE Additional: Teratogen (congenital deafness), Injection
site reactions
what drug?
Streptomycin
99
Most ototoxic Aminoglycoside
KANAMYCIN
100
What aminoglycoside?
Uses: Drug-resistant gonorrhea, Gonorrhea in penicillinallergic
patients
SE Additional: Anemia
Spectinomycin
101
has the narrowest therapeutic window among
aminoglycosides
Amikacin
102
What drug class?
bind to the 30S ribosomal subunit and interfere with protein synthesis:
o block formation of the initiation complex
o cause misreading of the code on the mRNA template
o inhibit translocation
Aminoglycosides
103
MEchanism of resistance of aminoglycosides
* plasmid-mediated formation of inactivating enzymes (group
transferases)
104
Resistance to streptomycin mechanism?
resistance to STREPTOMYCIN develops due to changes in the
ribosomal binding site
105
What are the aminoglycosides?
AminOglycosides require O2 for transport.
They won’t work under anaerobic conditions.
"Mean GNATS canNOT kill anaerobes."
Gentamicin
Neomycin
Amikacin
Tobramycin
Streptomycin
Nephrotoxicity
Ototoxicity
Teratogen
106
AMINOGLYCOSIDES:
o MOST OTOTOXIC: ?? and ??
o MOST VESTIBULOTOXIC: ??? and ???
o MOST OTOTOXIC: kanamycin, amikacin
o MOST VESTIBULOTOXIC: tobramycin, gentamicin
o cumulative ototoxicity when used with loop diuretics
107
Most nephrotoxic aminoglycoside? (2)
tobramycin, gentamicin
108
Aminoglycosides associated with skin reactions?
Neomycin and Streptomycin
109
MOA: Inhibits translocation process during protein
synthesis; an antibiotic isolated from the
fermentation broth of Fusidium coccineum;
used as topical antimicrobial against most
common skin pathogens including S. aureus
waht drug?
FUSIDIC ACID or
Na FUSIDATE
(Group: Fusidane)
110
* weakly acidic compounds that have a common chemical nucleus
resembling p-aminobenzoic acid (PABA)
what drug class?
SULDONAMIDES
111
Short Acting Sulfonamides? (3)
Sulfacytine
Sulfisoxazole
Sulfamethizole
112
Intermediate Acting Sulfonamides? (4)
Sulfadiazine
Sulfamethoxazole
Sulfapyridine
* Trimethoprim
113
Long Acting Sulfonamides?
Sulfadoxine
* Pyrimethamine
114
* structurally similar to folic acid
* weak base that is trapped in acidic environments
* reaches high concentrations in prostatic and vaginal fluids
What sulfonamides?
TRIMETHOPRIM
115
MOA of ANTIFOLATES:
o bacteriostatic inhibitors of folic acid synthesis
o competitive inhibitors of dihydropteroate synthase
waht drug?
Sulfonamides
S for S = Synthase for Sulfonamide;
Don’t forget: when used alone they are bacteriostatic. What used together
they act bactericidal
116
MOA: o selective inhibitor of bacterial dihydrofolate reductase
TRIMETHOPRIM
117
Mechanism of resistance to Anti FOlates?
● plasmid-mediated and results from:
o decreased intracellular accumulation of the drugs
o increased production of PABA by bacteria
● decrease in the sensitivity of dihydropteroate synthase to
118
Commonly used in UTI as well as P. jiroveci pneumonia?
Co-Trimoxazole
119
Used in burn infections, displaces protein binding of other drugs/bilirubin
Silver Sulfadiazine, Mafenide Acetate
120
OTHER SULFONAMIDES AND ANTIFOLATE DRUGS:
only for lower UTI
SULFISOXAZOLE
121
DOC for Toxoplasmosis
SULFADIAZINE-PYRIMETHAMINE
122
2nd line agent for malaria
SULFADOXINE-PYRIMETHAMINE
123
used for lower UTI, may be safely given to
patients with sulfonamide allergy
TRIMETHOPRIM
124
co-administered with Leucovorin to limit
bone marrow toxicity
PYRIMETHAMINE
125
* caused by increased levels of unconjugated bilirubin
* due to immaturity of fetal blood brain barrier
* histopathology
o bilirubin deposits in subcortical nuclei and basal ganglia
* clinical presentation
o hypo/hypertonia, lethargy, high-pitched cry, opisthotonos
Kernickterus
126
MOA: * interfere with bacterial DNA synthesis by inhibiting:
o Topoisomerase II (DNA Gyrase) in gram-negative organisms
* prevents relaxation of supercoiled DNA
o Topoisomerase IV in gram-positive organisms
▪ interferes with the separation of replicated
chromosomal DNA during cell division
QUINOLONES
127
What generation of Quinolones?
o Nalidixic acid, Cinoxacin, Rosoxacin, Oxolinic acid
o Urinary tract infections
First
128
What generation of Quinolones?
o Ciprofloxacin, Ofloxacin, Norfloxacin, Lomefloxacin, Enoxacin
o gram negatives, gonococci, gram positive cocci and Mycoplasma
Second
129
What gen of quinolones?
o Levofloxacin, Gemifloxacin, Moxifloxacin, Sparfloxacin, Grepafloxacin,
Gatifloxacin, Pazufloxacin, Tosufloxacin, Balofloxacin
o less gram negative and more gram positive activity,
streptococci and enterococci
Third
130
What generation of quinolones?
o Trovafloxacin, Alatrofloxacin, Prulifloxacin, Clinafloxacin
o broad spectrum, including anaerobes
4TH GENERATION
*WITH INCREASING GENERATION, INCREASING GRAM POSITIVE
ACTIVITY (unlike cephalosporins where increasing generation leads to
increasing gram negative activity)
131
General properties of quinolones: good oral bioavailability, high
Vd, t½ 3-8hrs, absorption is impeded by antacids, elimination is
via kidneys by tubular secretion (may compete with probenecid
for excretion) EXCEPT for
Moxifloxacin
132
What generation of Quinolones cause QTc prolongation?
(Third and Fourth Gen)
133
Most active agent against Gram
Negative organisms esp.
Pseudomonas
CIPROFLOXACIN
134
WHAT QUINOLONES:
Does not achieve adequate plasma
levels for use in systemic infections
Norfloxacin
135
QUINOLONE:
Drug vs C. trachomatis
Ofloxacin
136
Quinolones:
Newest members of this family and are
considered to have the broadest
spectrum of activity with increased
activity against anaerobes ang
atypical agents.
Moxifloxacin
Gemifloxacin
137
Quinolones
used for CAP caused by Chlamydia, Mycoplasma
and Legionella “THE ATYPICALS”
superior activity against G(+) bacteria
including S. pneumoniae ;
Levofloxacin
138
Used as alternatives to Ceftriaxone and Cefixime in
gonorrhea
Third Gen Quinolones
Levofloxacin
Moxifloxacin
139
Third Gen QUinolones: FQ elimination is via kidneys by tubular secretion (may
compete with probenecid for excretion)
Moxifloxacin
140
Notable SE of Trovafloxacin?
Hepatotoxicity
141
Mechanism of resistance to fluproquinolones?
* decreased intracellular accumulation of the drug via the
production of efflux pumps
* changes in porin structure
* changes in the sensitivity of the target enzymes via point
mutations in the antibiotic binding regions
142
MOA: Reactive reduction by ferredoxin forming free radicals
that disrupt electron transport chain. Bactericidal
Nitroimidazole (Antiprotozoal)
Metronidazole, Tinidazole, Secnidazole
143
DOC for amoebiasis, giardiasis &
Pseudomembranous colitis
METRONIDAZOLE
144
MOA: Forms multiple reactive intermediates when acted upon
by bacterial nitrofuran reductase →
disrupt protein, RNA and DNA synthesis. Bactericidal
NITROFURANTOIN
145
USed in Uncomplicated Urinary tract infections (EXCEPT
Proteus and Pseudomonas)
Nitrofurantoin
146
Inhibits Staphylococcal isoleucyl tRNA synthetase.
Bactericidal.
Uses Gram positive cocci including methicillin-susceptible
and MRSA, for minor skin infections such as Impetigo
Mupirocin
147
Which anti-TB drugs are hepatotoxic?
ISO a Red PYRe! (I saw a red fire!)
Isoniazid < Rifampin < Pyrazinamide
148
All can be used for ACTIVE TB. ??? and ??? can
be used for LATENT TB.
ISONIAZID AND RIFAMPICIN
149
MOA Inhibits mycolic acid synthesis. Bactericidal.
ISONIAZID
150
SE of Isoniazid?
Hepatitis, Neurotoxicity
151
IN Isoniazid, we can prevent neurotoxcity by co-administering waht?
Pyridoxine (vitamin B6)
152
M OA: Inhibits DNA-dependent RNA polymerase → inhibits
RNA production. Bactericidal.
Rifampicin (Rifampin), Rifabutin, Rifapentine, Rifaximin
153
Side effect: Red-orange Body Fluids, Light chain proteinuria,
Skin rash, Thrombocytopenia, Nephritis, Hepatotoxicity,
Flulike Syndrome, Anemia, Cholestasis
Rifampicin
154
The 4 Rs of Rifampicin?
The Rs of Rifampicin
RNA polymerase inhibitor
Red-orange body fluids
Rapid development of resistance
Revs up cytochrome P450 (inducer)
155
is a Rifampin derivative that is not
absorbed in the GIT, and so is used for the prevention
of hepatic encephalopathy, for treatment of traveler’s
diarrhea, (off-label use: for IBS and
Pseudomembranous colitis)
RIFAXIMIN
156
is equally effective as anti-mycobacterial
agent with less drug interaction and it is the preferred
anti-TB for AIDS patients
RIFABUTIN
157
MOA: Unknown. Converted to active pyrazinoic acid under
acidic conditions of macrophage lysosomes.
Bacteriostatic but can be bactericidal on actively
dividing mycobacteria.
PYRAZINAMIDE
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Also known as “sterilizing agent” used during the first
2 months of therapy
* Most hepatotoxic anti-TB drug
PYRAZINAMIDE
159
MOA: Inhibits arabinosyl transferases involved in the
synthesis of arabinogalactan in mycobacterial cell wall.
Bacteriostatic.
Ethambutol
160
SE: Visual disturbances (decreased visual acuity, red-green
color blindness, retrobulbar neuritis, retinal damage),
Headache, Confusion, Hyperuricemia, Peripheral
neuritis
Ethambutol
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perform what examination before starting antimycobacterial therapy?
Perform baseline ophthalmologic examination before
starting antimycobacterial therapy
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MOA Inhibit protein synthesis by binding to S12 ribosomal
subunit. Bactericidal.
STREPTOMYCIN
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MOA Inhibition of folic acid synthesis. Bacteriostatic.
Uses: Leprosy, PCP pneumonia (backup)
DAPSONE, ACEDAPSONE (Sulfones)
164
Most active drug against M. leprae
DAPSONE
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is a repository form of dapsone which has
drug action that can last for several months
ACEDAPSONE
166
Binds to guanine bases in bacterial DNA. Bactericidal
CLOFAZIMINE
167
Interferes with microtubule function. Inhibits
synthesis and polymerization of nucleic acids.
Fungistatic.
GRISEOFULVIN
168
Interfere with ergosterol synthesis by inhibiting fungal
squalene oxidase. Fungicidal.
Terbinafine, Butenafine, Naftifine
169
MOA Binds to ergosterol in fungal cell membranes, forming
artificial pores. Fungicidal.
Uses: Candidiasis (Oropharyngeal, Esophageal, Vaginal)
POLYENE:
Nystatin, Natamycin
170
MOA Inhibit fungal P450-dependent enzymes blocking
ergosterol synthesis. Fungistatic.
Uses:Mucocutaneous candidiasis, Dermatophytosis,
Seborrheic dermatitis, Pityriasis versicolor
Clotrimazole, Miconazole, Ketoconazole, Butoconazole, Econazole,
Sulconazole, Oxiconazole, Terconazole, Tioconazole
171
MOA Binds to ergosterol in fungal cell membranes, forming
artificial pores. Fungicidal.
Uses: Systemic fungal infections (Aspergillus, Blastomyces,
Candida albicans, Cryptococcus, Histoplasma, Mucor)
Amphotericin B
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Has the WIDEST antifungal spectrum
AMPHOTERICIN B
173
MOA: Accumulated in fungal cells by the action of permease and
converted by cytosine deaminase to 5-FU, which inhibits
thimidylate synthase. Fungistatic.
Uses Cryptococcosis, Systemic candidal infections,
Chromoblastomycosis
Flucytosine
174
MOA: Inhibit fungal P450-dependent enzymes blocking
ergosterol synthesis. Fungistatic.
* SE: Gastrointestinal disturbances (vomiting, diarrhea), Rash and
Hepatotoxicity
AZOLES
175
narrow spectrum azole that is Used Chronic mucocutaneous candidiasis, Dermatophytosis
KETOCONAZOLE
176
AZOLE
Uses: Cryptococcal meningitis (treatment and prophylaxis)
Candidiasis (esophageal, oropharyngeal, vulvovaginitis),
Coccidioidomycosis
Fluconazole [D],
177
Alternative to Amphotericin B in the treatment of
C. neoformans
* As effective as Amphotericin B in candidemia
FLUCONAZOLE
178
Alternative to Amphotericin B in the treatment of
C. neoformans
* As effective as Amphotericin B in candidemia
POSACONAZOLE
179
Broad spectrum azole, Poor CNS Penetration
ITRACONAZOLE
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MOA Inhibits â-glucan synthase decreasing fungal cell wall
synthesis
Uses: Disseminated and mucocutaneous candidiasis, Salvage
therapy for invasive aspergillosis
ECHINOCANDIN:
Caspofungin, Anidulafungin, Micafungin
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