Antibiotics Flashcards
Aminopenicillins:
Penicillin with extended spectrum : Gram+ and Gram-
Examples are Ampicillin and Amoxicillin
Beta lactamase Sensitive
Sterptogramins (Quinupristin/dalphopristin):
Mode of Action, Target, Effect
MOA: Binding 50S -prevents peptide bond elongation, as well as initiates premature
release of peptide
For VRSA and VRA
Bactericidal
Cephalosporins:
Side Effects
Allergy - Cross Reaction with Peniciline
Might Cause Gallstones - Ceftriaxone
Penicillin types according to Introduction
G - IV introduced
V - Orally Introduced
Cephalosporins:
5th Generation - Examples and Targets
Ceftarolin - For MRSA
Ceftobiprole - For Pseudomonas
Glycopeptides:
Examples
Toxicity
Absorption
Effect
Vancomycin and Teicoplanin
Oto- and Nephrotoxic
Local Effect and Treatment for MRSA
Cephalosporins:
3rd Generation - Examples and Targets
Ceftriaxone
For Gram+ and Gram-
Cephalosporins:
2nd Generation - Examples and Targets
Cefuroxime, Cefprozil and Cefaclor
For Gram+ and Gram-
Daptomycin:
Targets and Spectrum
Used against Vancomycin resistant Enterococci and Staph. Infections.
Only efficient for Gram+ (Cannot cross Gram- Membrane)
ESBL
Targets
Bacteria capable of producing it
Genetic Component containing it
Extended Spectrum Beta Lactamase
Hydrolyze Penicillines and Cephlosporines (up to 3rd Generation)
Gram Negative Bacteria
Plasmids
Peniciliinase (Beta-Lactamase) Resistnat Peniciline :
Side Effects
Allergy - Breaking down the penicilline is forming derivaties and these molecules are antigenic - Induce antibody production causing: Erythema, Fever, Arthritis.
Might cause Diarrhea
Aminoglicosides:
Resistance Options and Side effects
Resistance Options:
Receptor Mutation of 30S/ Enzymatic Degredation coded by Plasmids/ Efflux-Pump
Side Effects:
Oto- and Nephrotoxicity
In high doses it is Neurotoxic
Chloramphenicol:
Spectrum, Effect and MOA
Spectrum: Gram+ and Gram-
Effect: Bactriostatic, binds to 50S -Peptidyltransferase
What is the key component for the resistance of VRSA and PRP?
Penicillin Binding Protein (PBP)
Aminoglicosides:
Examples and Mode of Action
Streptomycin, Gentamycin, Amikacin, Kanamycin, Tobramycin, Netilmicin
Proteins Synthesis Inhibitor: Irreiversible Binding to 30S subunit, as a result tRNA cannot bind to ribosome - Bactericidal

Polymyxin Resistance Mechanism
LPS calation with Mg and Ca causes positive charge to trap Polymyxin outside the cell
Tetracycline:
Side effects and Resistance
Side effects: Forms a complex in bone with Calcium which colorize enamel
Resistance: Mutation
Macrolides:
Examples and Spectrum
Erythromycin,Azithromycin,Clarithromycin,Spiramycin
Gram+ Cocci, Legionella, Mycoplasma, Chlamydia Trachomatis
Daptomycin:
Assembly with.. , MOA
Binds Calcium to form oligomeric Assemby with Lipid tails pointing inwards.
Loose micelles serve to deliver Daptomycin to the bacterial membrane in Detergent form - Leading to Leakage of Cytosolic Contents
Cephalosporins:
1st Generation - Examples and Targets
Cephlexin and Cefazolin
For Gram + Cocci
Rifamycin B (Rifampin):
MOA, Spectrum
Inhibition of mRNA Synthesis
Spectrum - Gram+ Cocci and Mycobacteria
(Sketchy mentions some Gram- too…)
Lincosamides (Clindamycin):
Mode of Action, Effect, Antagonism with what drug
Binding 50S - Inhibits peptidyl-transferase
Bacterostatic
Antagonistic with Macrolides

Metronidazole - Nitroimidazole:
Conditions of Effectiveness, MOA, Overall Effect
Only in Anaerobic Conditions - Reduction to Radicals
MOA - Damage to Nucleic acids synthesis by Radicals
Bactericidal

Chloramphicol, Clindamycin, Macrolides, Sulfonamides, Tetracyclines and Timethoprim are all Bacterio_____ antibiotics.
Chloramphicol, Clindamycin, Macrolides, Sulfonamides, Tetracyclines and Timethoprim are all Bacteriostatic antibiotics.
Peniciliinase (Beta-Lactamase) Resistnat Peniciline :
Examples
(Aka Very Narrow Spectrum)
Methicilline
Nafcillin
Oxacillin
Cloxacillin

Monobactam (Aztreonam)
Beta-Lactamase Resistant
ONLY for Gram- Aerobics like: Neisseria and Pseudomonas
Methicillin Side Effects
Haematouria
Albuminuria
Nephritis
Gram Postive Bacteria have natural resistance to _____, and Nalidixic acid (Quinalone).
Gram Postive Bacteria have natural resistance to Polymyxin and Nalidixic acid (Quinalone).
Chloramphenicol:
Side Effects, Resistance
Side effect: Bone Marrow Dysfunction, Gray-Syndrome, Aplastic Anemia
Resistance: Acetyl-Transferase action
Gram Negative Bacteria have natural resistance to Penicillins , ________, Vancomycin and _______.
Gram Negative Bacteria have natural resistance to Penicillins , Macrolides, Vancomycin and Mupirucin.

Penicillin Side Effects
Hypersensitivity I - Allergy
Jarish-Herxmeir Reaction
IV use - Venous Wall inflammation
High doses - Kidney Failure and Seizures
Penicillin catagories according to spectrum
Extanded - Carboxypenicillines and Uriedopenicilines
Broad - Aminopenicillines
Narrow - Penicilin
Very Narrow - Methicilline, Nafcilline, Oxacilline
Carbapenems (Imipenem,Meropenem)
For Gram+ and Gram-
NOT for MRSA
But RESERVED for MDR (Multidrug Resistant) Bacteria
Trimethoprim with
Sulfamethoxazole:
MOA, Overall effect
Inhibition of Tetrahydrofolic Acid Synthesis (So DNA also) by blocking of Dihydrofolate Reductase action
Bacteriostatic
Fluoroquinolons :
MOA, Overall Effect
Synthesis of DNA - Replication Block
Inhibition of DNA-gyrase in Gram Negative
Inhibition of Topoisomerases type 4 in Gram Positive
Bactericidal
Tetracyclins:
Examples, Effect and Mode of Action
Oxy-tetracyclin and Doxacyclin
MOA: Bacteriostatic - binds to 30S subunit: tRNA cannot bind
Example for Antibiotics with
Site of action :Inside the cytoplasm
and
MOA - Inhibition of DNA Replication
Flouroquinalons
Cross Resistance
Bacteria is resistant to all Durgs with the same structure
Example for Antibiotics with
Site of action :Inside the cytoplasm
and
MOA - Inhibition of RNA Synthesis
Rifampicin
MBL
Targets
Bacteria containing it
Genetic Component containing it
Metallo-Beta Lactamases
Hydrolyze Carbapenems
Gram Negative
Transposons
Anaerobe bacteria have natural resistance to _________ and _________.
Anaerobe bacteria have natural resistance to Aminoglycosides and Quinalones.
Polyresistance
The Bacteria is resistant to several drugs with different Structures simultaneously
Which molecule is mimicked by penicillin?
Why?
D-Ala-D-Ala (crossed linked NAM by transpeptidase forming Peptidoglycan)
This is a beta-Lactam ring which is part of peptidoglycan.
When penicillin binds the active site (competitive inhibition) and leads to ultimately membrane weakening.
Cephalosporins:
Structure and Mode of action
7-Amino-Cephalosporic Acid
Mode of Action: Like Penicillin
Methicillin is acid _____ while cloxacilline is acid ______ .
Methicillin is acid labile while cloxacilline is acid Resistant.
Ciprofloxacin with Tetracycline
or
Beta-Lactams with Macrolides
are examples for ______ releationship between antibiotics.
Ciprofloxacin with Tetracycline
or
Beta-Lactams with Macrolides
are examples for Antagonistic releationship between antibiotics.

What is the MOA of Beta Lactamase Inhibitors?
Contain Beta-Lactam ring therefore interfere with the Beta-Lactamase action - Suicide Inhibitors
No anti bacterial Activity
Rifamycin side effects
Hepatitis and Orange body fluids
Fluroquinonolons side effect
Tendon and cartilage damage

Examples for Antibiotics with
Site of action :Inside the Cytoplasm
and
MOA - Inhibition of Protein Synthesis
Macrolides
Clindamycin
Chloramphenicol
Tetracyclin
Gentamycin
Oxazolidinone - Linzolid:
Mode of Action, Effect, Spectrum
Spectrum: Gram+
MOA: Binding 50s than not allowing 70S complex formation (N-Formilmethionil-tRNA can not bind)
Effect: Bacteriostatic
Polymyxin (B):
Spectrum, MOA and Example
Gram-, Bactericidal
Binds Membrane Phospholipids and Inhibits membrane transport
Colistin
Bacitracin:
Spectrum, Structure, Target
Broad: Gram+ and Gram-
Complex Polypeptide
Inhibitor of Peptidoglycan Synthesis - NO Translocation of Precursor across membrane
What is the way to determine quantitively if the Bacteria has Resistance?
MIC is Larger than the Dosis Maxima Tolerate
Examples for Antibiotics with
Site of action :Outside of cytoplasm
and
MOA - Cell wall Synthesis damage
Beta Lactams - Penicilins and Cephlosporins
Vancomycin
Aerobe bacteria have natural resistance to __________.
Aerobe bacteria have natural resistance to Metronidazole.
Combination of Vancomycin and Aminoglycosides in treatment could lead to -
Kidney failure
Beta-Lactams, Isoniazid, Metronidazole, Ploymyxin, Rifampin, Vancomycin, Aminoglycosides, Bacitracin and Quinalones are all Bacterio_____ antibiotics.
Beta-Lactams, Isoniazid, Metronidazole, Ploymyxin, Rifampin, Vancomycin, Aminoglycosides, Bacitracin and Quinalones are all Bacteriocidal antibiotics.
Streptoccoci and Enterococci are both with natural resistance to ________ but only enterococci are naturally resistant to ________ .
Streptoccoci and Enterococci are both with natural resistance to Aminoglycosides but only enterococci are naturally resistant to Cephalosporins.
Mupirocin
Mode of Action, Effect , Resistance
MOA : Isoleusil-tRNA Synthase INHIBITION
Bactericidal
Resistance - Modification of traget enzymes
Example for Antibiotics with
Site of action :Cytoplasm membrane
and
MOA - Altering the ion Permiability
Polymyxin
Resistance to Daptomycin:
Cause, VISA
Mutations in genes that encode enzymes involved in the synthesis of Phosphatydilaglycerol (therfore mem. Phospholipids).
VISA - Vancomycin-Intermediate Staph. Aureus; Impaired access through the thickened cell wall.
What are the Beta Lactamase inhibitors possible to give with Penicilline for Enhanced effect?
Clavulanic Acid
Sulbactam
Tazobactam
(P-Amino-Benzol-) Sulfonamides:
MOA, Antagonism, Overall Effect
MOA - Inhibition of Folic Acid Synthesis (So DNA also)
Antagonist of PABA
Bacteriostatic
Nystatin:
Spectrum, MOA, Adminstration method
Narrow - Antifungal
Binds to Steroid of Membrane and cause Disintegration
Too Toxic - Local Adminstration
Uriedopenicillin:
Penicillin with extended spectrum : Gram+ and Gram-
Effective against -Pseudomonas
(Pepper in the picture with Pseudomona)
Beta lactamase Sensitive
Glycopeptides:
Spectrum
Narrow
Gram+
Bactericidal
Cephalosporins:
4th Generation - Examples and Targets
Cefepime
For Gram+ and Gram-
Glycopeptides:
Mode of Action and Resistnace
Inhibition of Cell wall Synthesis
Bind Terminal Sequence D-Ala-D-Ala and Block Crosslinkage with Pentaglycin Bridge
Resistance - Bacteria Modifies Terminal Sequence to -
D-Ala-D-Lactate
Side effects of Polymyxin
Nephrotoxicity
Carboxypenicilines:
Penicillin with extended spectrum : Gram+ and Gram-
Effective against - Proteus and Pseudomonas
(Ticarcillin in the picture looking at Pseuodomona)
Beta lactamase Sensitive
Fosfomycin - Monoural:
Spectrum, Target, Structural Similarity
Broad Spectrum
Against UTIs, Inhibits very early stage Synthesis of Peptidoglycan
Structural Similarity to PEP: Phosphoenolpyruvate
Cephalosporins:
Mechanism of Resistance to it and Spectrum
Harder time to Penetrate and Lack of binding Protein unlike Penicilline.
Broken Down by Beta-Lactamase
Spectrum - Broad, Bactericidal
Macrolides:
Effect, Modes of Action and Resistance
MOA :Binds 50S subunit - : Prevent the movement of mRNA
Bacteriostatic
Resistance :Target Modification and Efflux Pump
Trimethoprim with
Sulfamethoxazole:
Resistance and Side effects
Resistance mechanism:
Altered enzyme- dihydropteric acid synthetase
Toxicity: Thrombocytopenia, Leucopenia and Hyperkalemia
Gentamicin and Penicillin interaction is _________
Gentamicin and Penicillin interaction is Synergistic