ANTIBIOTICS Flashcards
(166 cards)
1
Q
defined ANTIBIOSIS
A
VUILLEMIN
2
Q
ANTIBIOSIS:
Vuillemin’s concept of ____
A
survival of the fittest
3
Q
defined ANTIBIOTIC as a substance produced by MOs which has the capacity of inhibiting the growth or killing other MOs
A
S.A. WALKSMAN
4
Q
- synthetic product produced as a structural analogue of a naturally occuring biosynthetic product
- antagonizes the growth of MOs
A
ANTIBIOTICSC
5
Q
ANTIBIOTICS
effective at ____ concentration
A
low
6
Q
ANTIBIOTICS
a product of ____
A
metabolism
7
Q
ANTIBIOTICS
possess ____ to avoid toxicity
A
selective toxicity
8
Q
ANTIBIOTICS
chemically ____
A
stable
9
Q
ANTIBIOTICS
biotransformation
A
SLOW
10
Q
ANTIBIOTICS
elimination
A
RAPID
11
Q
ANTIBIOTICS
the antibiotic will no longer be able to kill the bacteria that causes the illness
A
ANTIBIOTIC RESISTANCE
12
Q
MECHANISM OF RESISTANCE
- antibiotic destruction/modification
- cleavage by beta-lactamase
A
PENICILLIN
CEPHALOSPORINS
13
Q
PENICILLIN, CEPHALOSPORIN
MECHANISM OF RESISTANCE:
antibiotic ____
A
destruction / modification
14
Q
PENICILLIN, CEPHALOSPORIN
ENZYME ACTIVITY:
cleavage by ____
A
beta-lactamase
15
Q
MECHANISM OF RESISTANCE
- antibiotic efflux
- efflux by TetA
A
TETRACYCLINES
16
Q
MECHANISM OF RESISTANCE
- Alteration/replacement of targets
- rRNA methylation
A
MACROLIDES
17
Q
MACROLIDES
MECHANISM OF RESISTANCE:
____ of targets
A
alteration / replacement
18
Q
MACROLIDES
enzyme activity
A
rRNA methylation
19
Q
- binds to 50s
- inhibits formation of peptide bonds
A
CHLORAMPHENICOL
20
Q
interfere with the attachment of tRNA to mRNA-ribosome complex
A
TETRACYCLINES
21
Q
- changes shape of 30s
- causes code on mRNA to be read incorrectly
A
STREPTOMYCIN
22
Q
drugs that are C/I in pregnancy
A
CATE
Clarithromyxin
Aminoglycosides
Tetracyclines
Erythromycin estolate
23
Q
SITE OF ACTION
CELL WALL
A
Bacitracin
Cephalosporin
Penicillin
Vancomycin
Teicoplanin
24
Q
SITE OF ACTION
CELL MEMBRANE
A
Amphotericin B
Nystatin
Polymyxin
25
# **SITE OF ACTION**
RIBOSOMES
Chloramphenicol
26
# **SITE OF ACTION**
50s
Eryhtromycin
Lincomycin
27
# **SITE OF ACTION**
30s
Aminoglycosides
Tetracyclines
28
# **SITE OF ACTION**
NUCLEIC ACIDS
Actinomycin
Griseofulvin
29
# **SITE OF ACTION**
DNA synthesis
Mitomycin C
30
# **SITE OF ACTION**
mRNA synthesis
Rifampin
31
the only antibiotic that act as an **antiNEOPLASTIC**
Actinomycin
32
* **broad** spectrum
* **EARLIEST** known antibiotic (historical **prototype**)
* **ideal** antibiotic, **low** serum protein binding, widely distributed in body (CNS)
PENICILLIN
33
# **PENICILLIN**
spectrum
broad
34
# **PENICILLIN**
COMMERCIAL source
*Penicillium chrysogenum*
35
# **PENICILLIN**
NATURAL source
*Penicillium notatum*
36
# **PENICILLIN**
TYPES OF PENICILLIN **G**
Pen G **Sodium**
Pen G **Procaine**
Pen G **Potassium**
37
# **PENICILLIN G**
UNITS:
Pen G **Sodium**
1667 units
38
# **PENICILLIN G**
UNITS:
Pen G **Procaine**
1009
39
# **PENICILLIN G**
UNITS:
Pen G **Potassium**
1530 units
40
# **PENICILLIN G**
local anesthetic
Pen G Procaine
41
# **PENICILLIN**
**BENZYLPENICILLIN** is active against ____
GRAM POSITIVE
42
# **PENICILLIN**
**CARBAPENEMS** is active against ____
GRAM NEGATIVE
43
GRAM **POSITIVE** BACTERIAS
Corynebacteria
Actinomyces
Nocardia
Bacillus
Listeria
Clostridium
Strap/Strep
| CORny ACTors kNOck BACk LISTERine in the CLOSet
+ looks like t
44
# **PENICILLIN | STRUCTURE**
essential
CIS-STEREOCHEMISTRY
45
# **PENICILLIN | STRUCTURE**
NOT essential
SULFUR/SULPHUR
46
# **PENICILLIN | STRUCTURE**
**5 membered** NITROGEN saturated ring
THIAZOLIDINE RING
47
# **PENICILLIN | STRUCTURE**
* consists of **4 membered ACYCLIC AMIDE** broad, potent, and rapid bactericidal
* **less** frequency of toxic and adverse reactions
B-LACTAM RING
48
# **PENICILLIN | STRUCTURE**
* usually **ionized** and administered as **sodium/potassium salt**
CARBOXYLIC ACID
49
# **PENICILLIN | STRUCTURE**
**CARBOXYLIC ACID** is usually administered as ____
sodium/potassium salt
50
# **PENICILLIN | STRUCTURE**
* **induce** further **strain** on **b-lactam ring**
* **low** acticity when modified with **alcohol/ester**
BICYCLIC SYSTEM
51
# **PENICILLIN | STRUCTURE**
the activity of **BICYCLIC SYSTEM** ***lowers down*** when modified with ____
alcohol / ester
52
# **PENICILLIN | STRUCTURE**
* **LONE pair electron** in nitrogen atom
* MORE **electrophilic**
CARBONYL GROU[P
53
# **PENICILLIN | STRUCTURE**
* **electron withdrawing** group
* render **amide oxygen**
* LESS nucleophilic
* **bulky** group provides **steric hindrance**
ACYL AMINO SIDE CHAINS
54
# **PENICILLIN | STRUCTURE**
ACYL AMINO SIDE CHAIN:
**aminopenicillin**
AMPICILLIN
55
# **PENICILLIN | STRUCTURE**
ACYL AMINO SIDE CHAINS:
**first prototype**
BENZYLPENICILLIN
56
# **PENICILLIN | STRUCTURE**
ACYL AMINO SIDE CHAINS:
**isoxazoyl penicillin**
CLOXACILLIN
57
# **PENICILLIN | STRUCTURE**
ACYL AMINO SIDE CHAIN:
**Pen V** (FIRST **orally** available penicillin)
PHENOXYMETHYLPENICILLIN
| classified under BENZYLPENICILLIN
58
# **PENICILLIN | STRUCTURE**
ACYL AMINO SIDE CHAIN:
**carboxypenicillin**
TICARCILLIN
59
# **PENICILLIN | STRUCTURE**
* also known as **penicillinase**
* responsible for **degradation** of penicillin antibiotics
beta-lactamase
60
# **PENICILLIN | STRUCTURE**
**beta-lactamase** is also known as
penicillinase
61
# **PENICILLIN | STRUCTURE**
* **rigid** cell wall
* with **b-lactamase** and **PBP** (**peptidoglycan** matrix)
GRAM POSITIVE BACTERIA
62
# **PENICILLIN | STRUCTURE**
* **lipopolysaccharide**
* WITHOUT beta-lactamase (**thin** matrix)
GRAM NEGATIVE BACTERIA
63
# **PENICILLIN | STRUCTURE**
involves in the FINAL SYNTHESIS of **peptidoglycan**
PENICILLIN-BINDING PROTEIN
64
# **PENICILLIN BINDING PROTEIN**
**PBP 1-a & 1-b** can lead to ____
SPHEROPLAST
65
# **PENICILLIN BINDING PROTEIN**
**rod** shape, **bacilli**
PBP 2
66
# **PENICILLIN BINDING PROTEIN**
required for **septum formation**
PBP 3
67
# **PENICILLIN BINDING PROTEIN**
* **carboxypeptidases**
* needed in hydrolysis of **D-Ala**
PBP 4-6
68
# **PENICILLINS**
NATURAL penicillins
Ampicillin
Amoxicillin
Benzylpenicillin
Phenoxymethylpenicillin
| AMP! AMO ni BEN si PHEN
69
# **PENICILLINS**
ANTI-**STAPHYLOCOCCALS**
Methicillin
Nafcillin
Isoxazoyl penicillin (Cloxacillin)
| STAPH taking a NAF after METH, ISOX! (aysus)
70
# **PENICILLINS**
ANTI-**PSEUDOMONALS**
Carboxypenicillins
Ureidopenicillins (Piperacillin)
| pseudO
carbO
ureidO
71
# **PENICILLINS**
NATURAL / **BIOSYNTHETIC**
Pen G
Pen G Procaine, Benzathine
Phenoxymethoxypenicillin
72
# **PENICILLINS**
NATURAL / BIOSYNTHETIC:
**repository** form (**depot**)
| depot - long acting injectable (used in anesthesia)
Pen G **Procaine**
73
# **PENICILLINS**
NATURAL / BIOSYNTHETIC:
**depot** form
Pen G **Benzathine**
74
# **PENICILLINS**
NATURAL / BIOSYNTHETIC:
**FIRST** SYNTHETIC penicillin
PHENOXYMETHOXYPENICILLIN
75
# **PENICILLINS**
PENICILLINASE-**SENSITIVE**
Pen G
Pen V
Ampicillin
Amoxicillin
Carbenicillin
Mezlocillin
Ticarcillin
Piperacillin
| Good Vibes lang AMP! CAR tiCAR ni MEZ AMO kinuha ni PIPER
76
# **PENICILLINS**
PENICILLINASE-**RESISTANT**
Methicillin
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin
| NAF after METH OXA, CLOXA, DICLOXA
77
# **PENICILLINS**
PENICILLINASE-RESISTANT:
* **SECOND** SYNTHETIC penicillin
* causes **interstitial nephrities**
METHICILLIN
78
# **PENICILLINS**
PENICILLINASE-**RESISTANT** spectrum
NARROW
79
# **PENICILLINS**
PENICILLINASE-**RESISTANT** is active against ____
GRAM + COCCI
80
# **PENICILLINS**
**Oxacillin**, **Cloxacillin**, **Dicloxacillin** are classified under ____
ISOXAZOLYL
81
# **PENICILLINS**
ACID-**SENSITIVE**
Pen G
Methicillin
Carbenicillin
Ticarcillin
Piperacillin
| PIPER, tara G! METH tayo sa CAR
82
# **PENICILLINS**
ACID-**RESISTANT**
Pen V
Ampicillin
Amoxicillin
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin
83
# **PENICILLINS**
has greater potency against ***P. aeuroginosa*** & ***Bacteriocides***
EXTENDED SPECTRUM
ANTI-PSEUDOMONAL
84
# **PENICILLINS | ANTI-PSEUDOMONAL**
CARBOXYPENICILLINS
Carbenicillin
Ticarcillin
| CAR
85
# **PENICILLINS | ANTI-PSEUDOMONAL**
CARBOXYPENICILLINS:
for **UTI**
Carbenicillin
86
# **PENICILLINS | ANTI-PSEUDOMONAL**
CARBOXYPENICILLINS:
**isostere of carbenicillin**
Ticarcillin
87
# **PENICILLINS**
which class should **NOT** be administered **orally?**
ACID-SENSITIVE
| best route: IM, IV
88
# **PENICILLINS | ANTI-PSEUDOMONAL**
ACYLUREIDOPENICILLINS
Mezlocillin
Piperacillin
| si AC ay nameMEZ si PIPER
89
# **PENICILLINS | ANTI-PSEUDOMONAL**
DOC for ***Strep. pyogenes*** sepsis
(from sore throat to **fasciitis**)
BENZYLPENICILLIN
90
# **PENICILLINS | ANTI-PSEUDOMONAL**
* **narrow** spectrum: ***Staph. aureus*** (MRSA)
* STABLE to **TEM1 beta-lactamase**, similar with **methicillin**, **nafcillin**
* similar SAFETY PROFILE with **benzylpenicillin**
CLOXACILLIN
91
# **PENICILLINS | ANTI-PSEUDOMONAL**
* very important **INTERMEDIATES** for synthetic antibiotics
* produced from **penicillin** and **cephalosporin** (partial cross-allergy: maxx **10%**)
6-AMINOPENICILLANIC ACID
(6-APA)
92
# **PENICILLINS | ANTI-PSEUDOMONAL**
**6-APA** is produced from
penicillin & cephalosporin
93
# **PENICILLINS**
ADVERSE EFFECTS
Rashes, Urticaria
Hypersensitivity, Anaphylaxis
Hepatotoxic
Hemorrhage
94
# **PENICILLINS**
ADVERSE EFFECTS:
**most severe reaction**
Hyprsensitivity
95
# **PENICILLINS | DRUG INTERACTIONS**
inhibit **renal excretion** of penicillin (**potentiation**)
PROBENECID
96
# **PENICILLINS | DRUG INTERACTIONS**
penicillin **inreases entry** (***synergism***) form an **inactive complex** if mixed in infusion fluid
AMINOGLYCOSIDE
97
# **PENICILLINS | SUB FOR PENICILLIN ALLERGY**
mainly for **gram POSITIVE**
MACROLIDES
98
B-LACTAM INHIBITORS
Clavulanic acid
Sulbactam
Tazobactam
99
# **BETA-LACTAMASE INHIBITORS**
principle behind beta-lactamase inhibitors
SUICIDE SUBSTRATE
100
# **BETA-LACTAMASE INHIBITORS**
have **heteroatom** leaving group at position **one**
CLASS I inhibitors
101
# **BETA-LACTAMASE INHIBITORS**
CLASS I INHIBITORS:
from ***Strep. Clavugeris***
Clavulanic acid + Amoxicillin
102
# **BETA-LACTAMASE INHIBITORS**
CLASS I INHIBITORS:
**Sultamicillin**
Sulbactam + Ampicillin
103
# **BETA-LACTAMASE INHIBITORS**
CLASS I INHIBITORS:
**Tazobactam** + ____
Piperacillin
104
# **BETA-LACTAMASE INHIBITORS**
CLASS II INHIBITORS:
from ***Streptomyces cattleya***
THIENAMYCIN
105
# **PENICILLIN**
PENICILLINASE-RESISTANT:
**Methicillin** causes ____
interstitial nephritis
106
# **BETA-LACTAMASE INHIBITORS**
CLASS I INHIBITORS:
**Clavulanic acid** is from
Strep. Clavugeris
107
# **BETA-LACTAMASE INHIBITORS**
CLASS II INHIBITORS:
**Thienamycin** is from
Streptomyces cattleya
108
# **BETA-LACTAMASE INHIBITORS**
CLASS II INHIBITORS:
**inhibitor** of **hydropeptidases**
IMIPENEM
| Cilastatin (BN)
109
# **BETA-LACTAMASE INHIBITORS**
CLASS II INHIBITORS:
**2nd gen CARBAPENEMS**
Meropenem
Biapenem
110
# **BETA-LACTAMASE INHIBITORS**
CLASS II INHIBITORS:
against **gram negative** infections due to extended-spectrum b-lactamase (ESBL) producing organisms
Imipenem
Cilastatin
Meropenem
Biapenem
111
# **BETA-LACTAMASE INHIBITORS**
CLASS II INHIBITORS:
**NEW** member of the group but **NOT** active agains ***Pseudomonas***
ERTAPENEM
112
# **BETA-LACTAMASE INHIBITORS**
* beta-lactam antibiotic that is **sensitive** to **dehydropeptidase I**
* use for tx of **enterobacter** infections
* active against **highly** penicillin-**resistant**
CARBAPENEMS
113
# **BETA-LACTAMASE INHIBITORS**
* NO cross-sensitivity and HIGHLY **resistant** to b-lactamase
* **LARGEST** spectrum of activity
* Septicemia
* can cause **renal tubular cells** metabolized by **renal dipeptidases**
IMIPENEM
114
# **BETA-LACTAMASE INHIBITORS**
**IMIPINEM** can cause ____
renal tubular cells
115
# **BETA-LACTAMASE INHIBITORS**
IMIPINEM can cause renal tubular cells **metabolized** by ____
renal dipeptidases
116
# **BETA-LACTAMASE INHIBITORS**
* RELATIVELY resistant to b-lactamase and active against gram **negative rods**
* NO activity on **gram +** and **anaerobes**
* NO cross sensitivity
* SYNERGISTIC with **aminoglycosides**
MONOBACTAMS
117
# **BETA-LACTAMASE INHIBITORS**
MONOBACTAMS:
**poor oral** bioavailability, NON toxic
AZTREONAM
118
# **BETA-LACTAMASE INHIBITORS**
MONOBACTAMS:
**orally active**
TIGEMONAM
119
# **B-LACTAM ANTIBIOTICS | MOA**
LETHALITY of pathogen is due to **selective** inhibition of **cell wall** specifically ____
PENICILLIN-BINDING PROTEINS
120
# **B-LACTAM ANTIBIOTICS | MOA**
Penicillin and Cephalosporins **acylate** the ____ making MO **inactive** to from **cross-linking** of the peptidoglycan
PBP
121
SYNONYMS of **peptidoglycan**
murein
mucopeptide
122
# **PENICILLINS**
VERY HIGH doses can cause ____
neurotoxicity
123
# **PENICILLINS**
NEVER give penicillin ____
intrathecally
124
* contain beta-lactam **dihydrothiazine ring** and **PYROGENIC**
* derivative of **7-aminocephalosporanic acid**
* ELIMINATION via **renal (kidneys)** except ***Ceftriaxone***, ***Cefoperazone*** (in LIVER)
* SAR: treat infection caused by **AEROBIC**, gram-**negative**, and some **positive**
* MAIN USE: against ***Klebsiella penumoniae***, ***streptococcal***, ***pneumococcal*** (esp. in px allergic to penicillin)
CEPHALOSPORINS
125
# **CEPHALOSPORINS**
derivative of ____
7-aminocephalosporanic acid
126
# **CEPHALOSPORINS**
ELIMINATION via
renal (kidneys)
127
# **CEPHALOSPORINS**
those that are eliminated via the **LIVER**
Ceftriaxone
Cefoperazone
128
# **CEPHALOSPORINS**
those that has **DISULFIRAM-like** effect
Cefamandole
Cefotetan
Cefoperazone
129
# **CEPHALOSPORINS**
ADVERSE EFFECTS:
**cross sensitivity** with ____
penicillins
130
# **CEPHALOSPORINS**
discovered cephalosporins in **1945**
Guiseppe Brotzu
131
# **CEPHALOSPORINS**
are derived from ____
*Cephalosporium spp*
132
# **CEPHALOSPORINS**
discovered:
* Ceph P1
* Ceph N
* Ceph C
ABRAHAM & NEWTON
133
# **CEPHALOSPORINS**
ABRAHAM & NEWTON:
**steroidal** type
Ceph P1
134
# **CEPHALOSPORINS**
ABRAHAM & NEWTON:
**Penicillin N** (gram **negative** >>> gram positive)
Ceph N
135
# **CEPHALOSPORINS**
ABRAHAM & NEWTON:
**dihydrothiazine ring**
Ceph C
136
# **CEPHALOSPORINS**
**6-membered** ring structure
DIHYDROTHIAZINE RING
137
# **CEPHALOSPORINS**
most are prepared ____
parenterally
138
# **CEPHALOSPORINS**
trend with **generation** and **activity**
as the generation increases, the activity also increases
139
# **CEPHALOSPORINS**
when **Ceftriaxone** and **Cefoperazone** are prescribed, they are need to be monitored with what **test**
liver function test
140
# **CEPHALOSPORINS | SAR**
* **semi-synthetic** incorporation
* influence the **antibacterial activity**
* affects **binding** of **b-lactamase**
7-position substituent
141
# **CEPHALOSPORINS | SAR**
if **S** is exchanged with:
**O**
oxacepham
142
# **CEPHALOSPORINS | SAR**
if **S** is exchanged with:
**C**
carbacepham
143
what should be prescribed if **sensitive** to PENICILLIN or CEPHALOSPORIN
MACROLIDES
| Azithromycin - usually prescribed
144
# **CEPHALOSPORINS | SAR**
* useful during **formulation**
* **prodrug development**
CARBOXYLIC ACID
145
# **CEPHALOSPORINS | SAR**
* chemical / metabolic **instability**
* effect on antibacterial activity
3-position substituent
146
# **CEPHALOSPORINS**
NOT covered by cephalosporins
LAME
Listeria
Atypical pathogen (chlamydia)
MRSA
enterococci
147
# **CEPHALOSPORINS**
* HIGHEST activity with **G+**
* LOWEST activity with **G-**
1st gen
148
# **CEPHALOSPORINS**
* LOW activity with **G+**
* LOWER activity with **G-**
2nd gen
149
# **CEPHALOSPORINS**
* LOWER activity with **G+**
* HIGHER activity with **G-**
3rd genm
150
# **CEPHALOSPORINS**
* LOWEST activity with **G+**
* HIGHEST activity with **G-**
4th gen
151
# **CEPHALOSPORINS**
GENERATION:
**Cefuroxime**
can be 2nd or 3rd
152
# **CEPHALOSPORINS**
Cephalexin
Cephalotin
Cephapirin
Cephradine
**Cefadroxil**
**Cefazolin**
1st gen
**"Ceph"**
153
# **CEPHALOSPORINS**
Cefaclor
Cefamandole
Ceforanide
Cefonicid
Cefotetan
Cefoxitin
**Cefmetazole**
**Cefprozil**
**Loracarbef**
**Cefpodoxime**
2nd gen
**"Cef + vowel"**
(does not end with **-one**, **-ime**)
154
# **CEPHALOSPORINS**
Ceftazi**dime**
Ceftizoxime
Ceftriaxone
Ce**fix**ime
Cefo**pera**zone
Cefo**tax**ime
Ceftibuten
Moxalactam
3rd gen
**"Cef + consonant"**
ends with **-one**, **-ime**
connected with MONEY
155
# **CEPHALOSPORINS**
Cepefime
Cefpirome
Cefoselis
Cefcidin
4th gen
156
# **CEPHALOSPORINS**
Ceftobiprole
Ceftaroline
5th gen
157
# **CEPHALOSPORINS**
* gram **POSITIVE**
* **PEcKS**
* do **NOT** cross BBB
* NON toxic
| P. mirabilis, E. coli, Klebsiella pneumoniae, Staph
1ST GEN
158
# **CEPHALOSPORINS**
* active against **inhibited** by **1st gen**
* extended coverage for gram-**negative**
* do **NOT** cross BBB
* **HENPEcK**
| Hemophilus, Neisseria, P. mirabilis, E. coli, K., pneumoniae, Staph
2nd gen
159
# **CEPHALOSPORINS**
**2nd gen** ceph are not active in
| (2)
enterococci
P. aeruginosa
160
# **CEPHALOSPORINS**
* extended gram-**negative**
* **CAN** pass BBB
* active against **Citrobacter** & **Providencia** (targets the **brain**)
* **HENPEcKSSS**
3rd gen
161
# **CEPHALOSPORINS**
* MORE resistant to **hydrolysis** by **chromosomal b-lactamase**
4th gen
162
# **CEPHALOSPORINS**
**ESKAPE**
* Enterococcus faecium
* Staphylococcus aureus
* Klebsiella pneumoniae
* Acinetobacter baumanii
* Pseudomonas aeruginosa
* Enterobacter spp
5th gen
163
# **CEPHALOSPORINS**
ORAL cephalosporins
Cepha**lexi**n
Cefa**clor**
Cefu**roxi**me
Ce**fixi**me
| nag ORAL si Lexi, Clor, Roxi at Fixi
164
# **CEPHALOSPORINS**
PARENTERAL cephalosporins
Cephradine
Cefazolin
Cefoxitin
Cefuroxime
Cefotaxime
Ceftriaxone
Ceftazidime
Cefepime
Cefpirome
165
# **CEPHALOSPORINS**
MAIN USES:
for **extreme/complicated** ____
UTI
166
# **CEPHALOSPORINS**
MAIN USES:
what can treat **bacterial meningitis**
3rd gen
