M5 PART 12 Flashcards
1
Q
Drugs have been used for the treatment of infectious diseases since the ____ Century (e.g., quinine and emetine)
A
17th
2
Q
introduced Salvarsan (for syphilis)
(Arsphenamine or Compound 606)
A
PAUL ERLICH
3
Q
Accidental discovery of Penicillin
A
ALEXANDER FLEMMING
4
Q
/
Discovery of the sulfonamides
A
GERHARD DOGMAK
5
Q
Penicillin has been used clinically as an antibiotic
FLOREY & CHAIN
A
1940
6
Q
An ideal antimicrobial agent exhibits ____, which means that the drug is harmful to a pathogen without being harmful to the host.
A
SELECTIVE TOXICITY
7
Q
antibiotics act against a limited group of bacteria
A
NARROW SPECTRUM
8
Q
antibiotics act against a larger group of bacteria
TETRACYCLINE
A
BROAD SPECTRUM
9
Q
Bactericidal drug ____ bacteria
A
KILL
suiCIDAL
10
Q
Bacteriostatic drug ____ of bacteria
A
INHIBITION
11
Q
INHIBITION OF CELL WALL SYNTHESIS
- New peptidoglycan monomers are inserted by transglycosylase (transglycosidase)
- The final rigidity of the cell wall is imparted by cross-linking of the peptide chains by transpeptidase enzyme
- Penicillin-Binding Proteins (PBP) may act as transglycosylase or as transpeptidase
A
BACTERIAL CELL WALL SYNTHESIS
12
Q
INHIBITION OF CELL WALL SYNTHESIS
BACTERIAL CELL WALL SYNTEHSIS:
New peptidoglycan monomers are inserted by ____
A
TRANSGLYCOSYLASE
13
Q
INHIBITION OF CELL WALL SYNTHESIS
BACTERIAL CELL WALL SYNTHESIS:
The final rigidity of the cell wall is imparted by cross-linking of the peptide chains by ____ enzyme
A
TRANSPEPTIDASE
14
Q
INHIBITION OF CELL WALL SYNTHESIS
BACTERIAL CELL WALL SYNTHESIS:
____ may act as transglycosylase or as transpeptidase
A
PENICILLIN-BINDING PROTEIN (PBP)
15
Q
BACTERIAL CELL WALL SYNTHESIS
- All ____ are selective inhibitors of bacterial cell wall synthesis
- block the action of transpeptidase; no cell wall formed
A
β-lactam drugs
16
Q
BACTERIAL CELL WALL SYNTHESIS
Destruction of bacterial ____ (destroys peptidoglycan)
A
AUTOLYSINS
17
Q
only β-lactam drug that has one ring
A
MONOBACTAMS
18
Q
A
19
Q
active in non growing
A
β-lactam antibiotics
20
Q
the only actively used monobactams
A
AZTREONAM
21
Q
The penicillins are derived from molds of the genus
A
penicillium
22
Q
They have the highest activity against Gram-positive organisms, spirochetes, and susceptible to β-lactamases
A
NATURAL PENICILLINS
23
Q
NATURAL PENICILLINS
o Aqueous penicillin G (IV)
o Procaine penicillin G (IM)
o Benzathine penicillin G (IM)
A
PENICILLIN G (BENZYLPENICILLIN)
24
Q
NATURAL PENICILLINS
phenoxymethylpenicillin
A
PENICILLIN V
25
# **NATURAL PENICILLINS**
**anesthetics** combined with Pen G
**Procaine** penicillin G (IM)
**Benzathine** penicillin G (IM)
26
# **NATURAL PENICILLINS**
**stable** in gastric acid, **orally** administered
PENICILLIN V
27
# **NATURAL PENICILLINS**
**gastric acid sensitive** hence administered **parenterally**
PENICILLIN G
28
* **Antistaphylococcal** penicillins
* **Lower activity** against Gram-**positive** organisms and **inactive** against Gram-**negative** organisms.
o Nafcillin
o Methicillin
o Oxacillin
o Dicloxacillin
* Staphylococci resistant to oxacillin and nafcillin have the **mecA gene**
β-lactamase resistant
29
# **β-lactamase resistant**
**Lower activity** against Gram ____ organisms
positive
29
* **Extended**-Spectrum Penicillins
* They have **high activity** against **both** Gram-**positive** and Gram-**negative** organisms but are **destroyed by β-lactamases**
* **Ampicillin**
* **Amoxicillin**
Aminopenicillins
29
# **β-lactamase resistant**
Staphylococci **resistant** to **oxacillin** and **nafcillin** have the ____ gene
mecA
30
# **β-lactamase resistant**
**inactive** against Gram-____ organisms
negative
30
**β-lactamase resistant** drugs
Nafcillin
Methicillin
Oxacillin
Dicloxacillin
31
# **Aminopenicillins**
They have **high activity** against ____ organisms
**both** gram-**negative** & gram-**positive**
31
# **Aminopenicillins**
are **destroyed** by ____
β-lactamases
32
AMINOPENICILLINS
Ampicillin
Amoxicillin
33
# **MAJOR GROUPS OF CEPHALOSPORINS**
Cefo**tax**ime
**Ceft**izoxime
**Ceft**riaxone
Ceftazi**dime**
Cefo**pera**zone
***Moxolactam***
Ce**fix**ime
**Cefp**odoxime proxetil
**Ceft**ibuten
Cef**dinir**
**Cefd**itoren
THIRD GENERATION
33
# **Aminopenicillins + β-Lactamase Inhibitors**
**Ampicillin** is commonly combined with what drug for **β-Lactamase inhibition**
SULBACTAM
34
* Ampicillin + **Sulbactam** (Sultamicillin)
* Amoxicillin + **Clavulanic acid** (Co-Amoxiclav)
Aminopenicillins + β-Lactamase Inhibitors
34
# **Aminopenicillins + β-Lactamase Inhibitors**
**Amoxicillin** is commonly combined with what drug for **β-Lactamase inhibition**
CLAVULANIC ACID
34
**Piperacillin** is commonly combined with what drug for **β-Lactamase inhibition**
TAZOBACTAM
34
anti-pseudomonal
* **Carbenicillin**
* **Ticarcillin**
Carboxypenicillins
34
# **MAJOR GROUPS OF CEPHALOSPORINS**
MRSA active
Ceftaroline
Ceftobiprole
34
* **Piperacillin** (anti-pseudomonal)
* **Mezlocillin**
Ureidopenicillins
35
# **Cephalosporins**
Cephalosporins tend to be **resistant** to the
β-lactamases
35
* The mechanism of action is **analogous** to that of **penicillins**
* tend to be **resistant** to the** β-lactamases**
* have been arranged into major groups, or “**generations**”
Cephalosporins
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
**FIRST** GENERATION
**Ceph**alothin
**Ceph**apirin
***Cef**azolin*
**Ceph**alexin
**Ceph**radine
***Cef**adroxil*
## Footnote
first yr students - positive (gram +)
**CEPH**
35
# **Cephalosporins**
Cephalosporins have been **arranged** into major groups, or
GENERATIONS
35
Ureidopenicillins
**Piperacillin** (anti-pseudomonal)
**Mezlocillin**
35
# **Cephalosporins**
The mechanism of action is **analogous** to that of
PENICILLINS
35
Carboxypenicillins
* Carbenicillin
* Ticarcillin
35
**Ticarcillin** is commonly combined with what drug for **β-Lactamase inhibition**
CLAVULANIC ACID
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
**SECOND** GENERATION
**Cef**amandole
**Cef**uroxime
**Cef**onic acid
**Cef**aclor
**Cef**oxitin
**Cef**otetan
**Cef**prozil
**Cef**uroxime axetil
***Cefmetazole***
***Lorocarbef***
## Footnote
**CEF + VOWEL**
equal activity = not positive, not negative
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
**Cef**amandole
**Cef**uroxime
**Cef**onic acid
**Cef**aclor
**Cef**oxitin
**Cef**otetan
**Cef**prozil
**Cef**uroxime axetil
***Cefmetazole***
***Lorocarbef***
SECOND GENERATION
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
**Ceph**alothin
**Ceph**apirin
***Cef**azolin*
**Ceph**alexin
**Ceph**radine
***Cef**adroxil*
FIRST GENERATION
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
only **1st gen** drug administered **intravenously**
CEFAZOLIN
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
the **very first first generation** drug
Cephalexin
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
**very first second generation** drug
Cefuroxime
35
# **MAJOR GROUPS OF CEPHALOSPORINS**
THIRD GENERATION
Cefo**tax**ime
**Ceft**izoxime
**Ceft**riaxone
Ceftazi**dime**
Cefo**pera**zone
***Moxolactam***
Ce**fix**ime
**Cefp**odoxime proxetil
**Ceft**ibuten
Cef**dinir**
**Cefd**itoren
## Footnote
**CEF + CONSONANT**
numbers/money
gram negative
36
# **MAJOR GROUPS OF CEPHALOSPORINS**
FOURTH GENERATION
Cefepime
Cefpirome
36
# **Summary of Activity of Cephalospirins**
Gram **(+)** cocci and **PEcK** (P.
mirabilis, E. coli, K. pneumoniae)
1st gen
36
# **Summary of Activity of Cephalospirins**
Gram **(+)** cocci and **HENPEcK** (H. influenzae, E. aerogenes, N. gonorrhae, P. mirabilis, E. coli, K. pneumoniae)
2nd gen
37
# **Summary of Activity of Cephalospirins**
Gram **(+)** cocci and **HENPPEcK** (H. influenzae, E. aerogenes, N. gonorrhae, P. aeruginosa, P. mirabilis, E. coli, K. pneumoniae)
3rd gen
38
# **Summary of Activity of Cephalospirins**
Gram **(+)** cocci [**MRSA**] and E. coli, K. pneumoniae, P. mirabilis, and P. aeruginosa
4th gen
39
**deactivates** **imipinem**
**inhibits** **cilastatin**
RENAL DEHYDROPEPTIDASE
40
# **RENAL DEHYDROPEPTIDASE**
deactives ____
imipenem
41
# **RENAL DEHYDROPEPTIDASE**
inhibits ____
cilastatin
42
has **good activity** against many Gram-**negative rods**, Gram-**positive** organisms, and **anaerobes**.
Imipenem + Cilastatin
43
Imipenem + Cilastatin
Meropenem
Ertapenem
CARBANEPAMS
44
* **Aztreonam**
* It has antimicrobial activity **directed primarily against** the **Enterobacteriaceae** (Pseudomonas), including **P. aeruginosa**.
* **No activity** against Gram-**positive** organisms and **anaerobes**
MONOBACTAMS
45
# **ADVERSE EFFECTS**
**Hypersensitivity**, Diarrhea, Nephritis, Neurotoxicity, Hematologic toxicities, Cation toxicity
PENICILLIN
46
# **ADVERSE EFFECTS**
**Allergic** manifestations
CEPHALOSPORINS
47
# **ADVERSE EFFECTS**
Imipenem/Cilastatin - **N&V** & **diarrhea**
**Imipinem** - may provoke **seizures**
CARBAPENEMS
48
# **ADVERSE EFFECTS**
**Aztreonam** may cause **phlebitis**, **skin rash**, and occasionally **abnormal liver function** tests
MONOBACTAM
49
# **ADVERSE EFFECTS**
**fever**, **chills**, and/or phlebitis at the infusion site
**flushing** (**red man syndrome**) and **shock**
Vancomycin
50
# **Mode of Action of Antibiotics That Inhibit Cell Wall Synthesis**
ANTIBIOTIC: **VANCOMYCIN, BACITRACIN**
PROCESS INTERRUPTED: ____
mucopeptide synthesis
50
# **Mode of Action of Antibiotics That Inhibit Cell Wall Synthesis**
ANTIBIOTIC: **PENICILLIN, CEPHALOSPORINS**
PROCESS INTERRUPTED: ____
cell wall cross-linking
51
# **Mode of Action of Antibiotics That Inhibit Cell Wall Synthesis**
ANTIBIOTIC: **CYCLOSERINE**
PROCESS INTERRUPTED: ____
synthsis of cell wall peptides
52
# **Inhibition of Cell Membrane Function**
If the **functional integrity** of the cytoplasmic membrane
is ____, macromolecules and ions **escape** from the cell, and cell **damage** or **death** ensues.
DISRUPTED
53
# **Inhibition of Cell Membrane Function**
If the **functional integrity** of the cytoplasmic membrane is **disrupted**, macromolecules and ions ____ from the cell, and cell **damage** or **death** ensues.
ESCAPE
54
# **Inhibition of Cell Membrane Function**
* **Binds** to cell membranes **rich** in **phosphatidylethanolamine**
* **Active** against gram-**negative** rods, especially **P. aeruginosa**, **Acinetobacter baumannii**, and **carbapenemase**-producing **Enterobacteriaceae**.
* **Bactericidal**
POLYMYXIN E (COLISTIN)
55
# **Inhibition of Cell Membrane Function | POLYMYXIN E (COLISTIN)**
**binds** to cell membrane **rich** in ____
phosphatidylethanolamine
56
# **Inhibition of Cell Membrane Function**
* Induces **depolarization** of bacterial membrane potential resulting to **release of potassium**
* This agent is given to organisms **highly resistant** to **β-lactam agents** and **vancomycin**.
* Bactericidal
DAPTOMYCIN
56
# **Inhibition of Cell Membrane Function | DAPTOMYCIN**
Induces ____ of bacterial membrane potential resulting to **release of potassium**
depolarization
56
# **Inhibition of Cell Membrane Function | POLYMYXIN E (COLISTIN)**
active against ____
gram negative rods
56
# **Inhibition of Cell Membrane Function | DAPTOMYCIN**
**Induces depolarization** of bacterial membrane potential resulting to release of ____
potassium
57
# **Inhibition of Cell Membrane Function | DAPTOMYCIN**
This agent is given to organisms **highly resistant** to ____ and ____
β-lactam agents and vancomycin
57
*Amika**cin***
Genta**micin**
Neo**mycin**
Strepto**mycin**
Tobra**mycin**
AMINOGLYCOSIDES
57
antibiotics that targets **30s** ribosomes
Aminoglycosdies
Tetracycline
Tigecycline
| buy **AT** 30
57
**blocks** functioning of **initiation complex** & causes **misreading** of **mRNA**
Aminoglycosides
57
antibiotics that target the **50s** ribosomes
Chloramphenicol
Erythromycin
Linezolid
Clindamycin
Macrolides
Quinupristin / Dalfopristin
| **CELL** at **50**
58
blocks **tRNA** binding to ribosome
tetracycline
58
type of activity: **aminoglycosides**
bactericidal
58
blocks **protein translation**
tigecycline
59
**mycin** source
streptomyces
60
# **ADVERSE EFFECTS**
ototoxicity (vestibular & cochlear)
**Nephrotoxicity** (NTG)
Neuromuscular paralysis
Allergic reactions
AMINOGLYCOSIDES
61
Demeclo**cycline**
Doxy**cycline**
Mino**cycline**
Tetra**cycline**
TETRACYCLINES
62
# **ADVERSE EFFECTS**
**Gastric discomfort**
Effects on calcified tissue
Fatal hepatotoxicity
**Photoxicity**
Vestibular problems
Pseudotumor cerebri
Superinfections
causes **yellow tooth discoloration**
**Fancomi syndrome** - acquired by taking an **expired drug**
TETRACYCLINES
63
blocks **peptidyltransferase**
Chloramphenicol
64
blocks **translocation**
macrolides
65
causes **premature release** of peptide chain
Quinupristin / Dalfopristin
65
blocks **peptide bond formation**
Clindamycin
66
blocks **early step** in ribosome formation
Linezolid
67
# **ADVERSE EFFECTS**
hemolytic anemia
**gray baby syndrome** - **cyanosis**, **not** administered to babies
CYP450 inhibitor
**rare: aplastic anemia - fatal**
Chloramphenicol
68
# **ADVERSE EFFECTS**
epigastric distress
**cholestatic jaundice - bilirubin**
ototoxicity
enzyme inhibitor
MACROLIDES
69
# **ADVERSE EFFECTS**
Pseudomembranous colitis
Clindamycin
70
Ery**thromycin**
Azi**thromycin**
Clari**thromycin**
Teli**thromycin**
MACROLIDES
71
erythromycin was named
Ilosone
Ilotycin
72
# **THERAPEUTIC APPLICATIONS**
some **anaerobes** & **certain** gram **negative** bacteria
STREPTOGRAMINS
72
# **ADVERSE EFFECTS**
Phlebitis
arthralgias
myalgias
STRETOGRAMINS
Quinupristin / Dalfopristin
73
# **ADVERSE EFFECTS**
Gastrointestinal - N&V, diarrhea
Linezolid
74
# **THERAPEUTIC APPLICATIONS**
**Vancomycin-resistant**
Linezolid
75
# **THERAPEUTIC APPLICATIONS**
gram positive bacterias
Macrolides
76
# **THERAPEUTIC APPLICATIONS**
**bacteroides** & other **anaerobes**
Clindamycin
77
# **THERAPEUTIC APPLICATIONS**
Salmonellae, Meningococci, H. influenzae
Chloramphenicol
78
# **INHIBITION OF NUCLEIC ACID SYNTHESIS**
Inhibition of bacterial DNA synthesis by **blocking** of **DNA gyrase** and **topoisomerase IV**
FLUOROQUINOLONES
79
topoisomerase produced by gram **negative**
tropoisomerase II
80
topoisomerase produced by gram **positive**
topoisomerase IV
81
# **QUINOLONE | GENERATION**
Nalidixic acid
1st gen
82
a **quinolone** that has **no fluorine** in its **structure**
nalidixic acid
83
# **QUINOLONE | GENERATION**
**Cip**rofloxacin
**Of**loxacin
**Nor**floxacin
2nd gen
84
# **QUINOLONE | GENERATION**
**Levo**floxacin
3rd gen
85
# **QUINOLONE | GENERATION**
**Moxi**floxacin
4th gen
86
# **QUINOLONE | GENERATION**
* used **less often** today
* have **moderate** gram-**negative** activity
* achieve **minimal serum** concentrations
* **restricted** to the treatment of **uncomplicated** **urinary tract infections**
FIRST GEN
86
# **QUINOLONE | GENERATION**
* have **expanded** gram **negative** activity
* have **some** activity **against** gram **positive** and **atypical organisms** such as **Mycoplasma pneumoniae** and **Chlamydia pnuemoniae**
2nd gen
87
# **QUINOLONE | GENERATION**
* **retain** **expanded** gram **negative** activity
* show **improved** activity against **atypical** organisms and **specific** gram **positive** bacteria
3rd gen
87
# **QUINOLONE | GENERATION**
* shows **improved** gram **positive** coverage
* **maintains** gram **negative** activity
* **gains anaerobic** coverage
4th gen
87
# **ADVERSE EFFECTS**
N&V, diarrhea
HA or dizziness
Phototoxicity - sensitivity to light
Cartilage erosion (arthropathy) - not advisable for <18 y/o, affects tendon
Contraindicated to patients with arrythmia
Drug interactions with antacids and cations
FLUOROQUINOLONES
88
# **ADVERSE EFFECTS**
* Toxic effects are manifested by fever, skin rashes, gastrointestinal disturbances, **depression of the bone marrow leading to anemia or agranulocytosis**, hemolytic anemia, and liver and kidney function abnormalities
* **SJS - Stevens Johnson Syndrome**
* **crystalluria**
* **jaundice**
* **kernicterus**
SULFONAMIDES
89
# **Drugs for Tuberculosis**
* binds to **DNA-dependent RNA polymerase** and thus **inhibits RNA synthesis** in bacteria
* has **different mechanism**, targets nucleic acid synthesis
* ADVERSE REACTION: **orange color** to urine, saliva, and sweat (harmless)
RIFAMPIN
89
90
# **Drugs for Tuberculosis**
* inhibits **mycolic acid synthesis**
* targets **cell wall** of the MO
* ADVERSE REACTION: **Liver toxicity**, P**eripheral neuritis (nerves)**
ISONIAZID
| + VIT B6
91
92
# **Drugs for Tuberculosis**
* inhibits **mycolic acid synthesis**
* targets the **cell wall** of the MO
* ADVERSE REACTION: **Hepatoxicity**, N&V, **hypersensitivity**, **hyperuricemia**
Pyrazinamide
93
# **Drugs for Tuberculosis**
* inhibits the **synthesis of arabnogalactan**
* targets the **cell wall** of the MO
* ADVERSE REACTIONS: **Optic neuritis** w/ blurred vision, **red-green color blindness**
Ethambutol
94
o **Leprosy**
o SE: **hemolytic anemia**, **gastrointestinal intolerance**, **fever**, **itching**, and **rashes**
DAPSONE
95
o **Antiprotozoal** and for bacterial **anaerobic** infections
o SE: **Stomatitis**, **diarrhea**, and **nausea**
METRONIDAZOLE
96
