ANTIBIOTICS Flashcards
He introduced the concept of survival of the fittest, “antibiosis”.
Vuillemin
“An antibiotic or antibiotic substance is a substance produced by microorganisms, which has the capacity of inhibiting the growth and even of destroying other microorganisms.”
S.A. Waksman
MECHANISM OF RESISTANCE
Penicillin/Cephalosphorins
Antibiotic destruction or modification
MECHANISM OF RESISTANCE
Tetracyclines
Antibiotic efflux
MECHANISM OF RESISTANCE
Macrolides
Alteration or replacement of targets
MECHANISM OF RESISTANCE
Penicillin/Cephalosporins
Identify the enzyme activity.
Cleavage by beta-lactamase
Antibiotic destruction or modification
MECHANISM OF RESISTANCE
Macrolides
Identify the enzyme activity.
rRNA methylation
Alteration or replacement of targets
MECHANISM OF RESISTANCE
Tetracyclines
Identify the enzyme activity.
Efflux by TetA
Antibiotic efflux
TYPE OF ACTIVITY
Site of action:
Cell Wall and Cell Membrane
-Cidal or -Static
-Cidal
TYPE OF ACTIVITY
Site of action:
Ribosomes, 50s
-Cidal or -Static
-Static
SITE OF ACTION
Bacitracin
Cell Wall
SITE OF ACTION
Cephalosphorins
Cell Wall
SITE OF ACTION
Penicillins
Cell Wall
SITE OF ACTION
Vancomycin
Cell Wall
SITE OF ACTION
Teicoplanin
Cell Wall
SITE OF ACTION
Amphotericin B
Cell Membrane
SITE OF ACTION
Nystatin
Cell Membrane
SITE OF ACTION
Polymyxins
Cell Membrane
SITE OF ACTION
Chloramphenicol (CMC)
Ribosomes
SITE OF ACTION
Erythromycins
50s
SITE OF ACTION
Lincomycins
50s
SITE OF ACTION
Pancidals
DNA/RNA
SITE OF ACTION
Anti-cancers
DNA/RNA
Pancidals
4-membered cyclic amide
B-lactam ring
B-LACTAMS
B-lactam antibiotics have potent and rapid bactericidal action against bacteria in the ____ phase
Growth
PENICILLINS
First biosynthetic penicillin
Phenoxymethylpenicillin
(Pen V)
PENICILLINS
Earliest known antibiotic (historical prototype)
Benzyl penicillin (Pen G)
PENICILLINS
Commercial source of penicillin
Penicillium chrysogenum
PENICILLINS
Source of penicillin discovered by Alexander Fleming
Penicillium notatum
PENICILLINS
Pen G Sodium units
1667 units
PENICILLINS
Pen G Procaine units
1009 units
PENICILLINS
Pen G Potassium units
1530 units
PENICILLINS
Antidote for penicillin anaphylaxis
Epinephrine
PENICILLINS
Hepatotoxic penicillin
Isoxazoyl penicillin
PENICILLINS
How can penicillin cause adverse effect?
Open beta lactam ring -> Reactive Penicilloyl group
PENICILLINS
Two penicillins in repository (depot) form
- Procaine
- Benzathine
PENICILLINS
Anti-pseudomonal penicillins
- Carboxy
- Ureido
PENICILLINS
Penicillinase-sensitive, acid sensitive
- Pen G
- Mezlocillin
- Carbenicillin
- Ticarcillin
- Piperacillin
G MEZ CAR TI PIP
PENICILLINS
Penicillinase-sensitive, acid resistant
- Pen V
- Ampicillin
- Amoxicillin
PENICILLINS
Penicillinase-resistant, acid sensitive
Methicillin
PENICILLINS
Penicillinase-resistant, acid resistant
- Oxacillin
- Cloxacillin
- Dicloxacillin
Isoxazoyl penicillins
PENICILLINS
Nafcillin
acid resistant or acid sensitive
Acid Resistant
PENICILLINS
2nd synthetic, can cause interstitial nephritis
Methicillin
PENICILLINS
Type of penicillins with narrow spectrum of activity and active against G+ cocci
Penicillinase-resistant
PENICILLINS
Isostere of carbenicillin that has greater potency against P. aeruginosa & Bacteroides
Ticarcillin
PENICILLINS
Carboxypenicillins for UTI
Extended spectrum penicillins
Carbenicillin
(Disodium and Indanyl sodium salts)
PENICILLINS
Acylureidopenicillins
Extended spectrum penicillins
- Mezlocillin
- Piperacillin
PENICILLINS
Macrolides used as penicillin substitute
- Erythromycin
- Clarithromycin
For G(+)
PENICILLINS
Quinolones used as penicillin substitute
- Ciprofloxacin
- Lovofloxacin
For G(+)
PENICILLINS
Other penicillin substitutes
- Fusidic acid
- Rifampicin
- Clindamycin
For G(+)
PENICILLINS
Used as penicillin substitute for serious infections
Glycopeptides
B-LACTAMASE INHIBITORS
B-lactamase inhibitors are known as ____.
Suicide Substrates
B-LACTAMASE INHIBITORS
Have a heteroatom (S,O) leaving group at position 1
Class 1 β-lactamase inhibitors
B-LACTAMASE INHIBITORS
Clavulanic Acid + ____
Penicillin
Amoxicillin
Co-Amoxiclav
B-LACTAMASE INHIBITORS
Sulbactam + ____
Penicillin
Ampicillin
Sultamicillin
B-LACTAMASE INHIBITORS
Tazobactam + ____
Piperacillin
Piptaz
B-LACTAMASE INHIBITORS
Imipenem / Cilastatin inhibits ____
DPH-1
Dehydropeptidase 1
B-LACTAMASE INHIBITORS
2nd Generation Carbapenems
- Meropenem
- Biapenem
B-LACTAMASE INHIBITORS
N-formimidoylthienamycin
Imipenem
B-LACTAMASE INHIBITORS
Used for septicemia or sepsis
Imipenem
B-LACTAMASE INHIBITORS
____ has the largest/broadest spectrum of activity and has no cross sensitivity with other beta lactamases.
Imipenem
MONOBACTAMS
Monobactams began with the independent isolation of ____.
Sulfazecin
MONOBACTAMS
Monobactams have synergistic effect with ____
Aminoglycosides
Penicillin increase entry
MONOBACTAMS
Relatively resistant to beta-lactamases and active against Gram ____ rods
(-)
MONOBACTAMS
Orally active
Tigemonam
MONOBACTAMS
Poor oral bioavailability and relatively non-toxic
Aztreonam
MONOBACTAMS
Monobactam interaction with static drugs
Antagonism
MONOBACTAMS
Monobactam interaction with probenecid
Potentiation
Inhibits renal excretion of penicillin
CEPHALOSPORINS
Steroid with minimal antibacterial activity
THREE PRINCIPAL ANTIBIOTIC COMPONENTS
Cephalosporin P1
CEPHALOSPORINS
Gram Negative > Gram Positive
THREE PRINCIPAL ANTIBIOTIC COMPONENTS
Cephalosporin N
(Penicillin N)
CEPHALOSPORINS
Dihydrothiazine ring
THREE PRINCIPAL ANTIBIOTIC COMPONENTS
Cephalosporin C
CEPHALOSPORINS
Cephalosphorins can be pyrogenic if administered ____.
IV/IM
CEPHALOSPORINS
3 Disulfiram-ike cephalosphorins with bleeding problems (warfarin-like)
- Cefamandole
- Cefotetan
- Cefoperazone
CEPHALOSPORINS
1st generation cephalosphorins have the highest activity against ____.
Gram (+)
CEPHALOSPORINS
4th generation cephalosphorins have the highest activity against ____.
Gram (-)
CEPHALOSPORINS
Generations of cephalosphorins that do not cross the BBB
Identify the generation.
1st, 2nd
CEPHALOSPORINS
Inactive against Methicillin-resistant Staphylococcus aureus (MRSA) caused by staph bacteria
Identify the generation.
1st
CEPHALOSPORINS
PEcK
* Proteus mirabilis
* Escherichia coli (E. coli)
* Klebsiella pneumoniae
Identify the generation.
1st
CEPHALOSPORINS
HENPEcK
* Haemophilus influenza (H. influenza)
* Enterobacteriaceae
* Neisseria spp.
Identify the generation.
2nd
CEPHALOSPORINS
Active against Citrobacter, Providencia
Identify the generation.
3rd
CEPHALOSPORINS
HENPEcKSSS
* Shigella
* Salmonella
* Serratia
Identify the generation.
3rd
CEPHALOSPORINS
More resistant to hydrolysis by chromosomal beta-lactamase
Identify the generation.
4th
CEPHALOSPORINS
PESS
* Pseudomonas aeruginosa
* Enterobacter
* Staphylococcus aureus
* Staphylococcal pneumoniae
Identify the generation.
4th
CEPHALOSPORINS
ESKAPE
* Enterococcus faecium
* Staphylococcus aureus
* Klebsiella pneumonia
* Acinetobacter baumannii
* Pseudomonas aeruginosa
* Enterobacter spp.
Identify the generation.
5th
CEPHALOSPORINS
Cephalosphorins has cross sensitivity with ____.
Penicillins
AMINOGLYCOSIDES
First aminoglycoside antibiotic to be in chemotherapy
Streptomycin
AMINOGLYCOSIDES
2 adverse effects of aminoglycosides
- Nephrotoxic
- Ototoxic
AmiNOglycosides
AMINOGLYCOSIDES
Bacteriostatic MOA of aminoglycosides
30s ribosome binding
AMINOGLYCOSIDES
Bacteriocidal MOA of aminoglycosides
misreading of mRNA
AMINOGLYCOSIDES
Aminoglycosides are mainly used to treat nosocomial infections and against gram ____ bacteria
(-)
AMINOGLYCOSIDES
Neuromuscular blockade by aminooglycosides can be managed by ____ and ____.
Calcium gluconate and Neostigmine
AMINOGLYCOSIDES
Aminooglycosides have ____ effect with Beta-Lactams
Synergistic
AMINOGLYCOSIDES
Aminooglycosides have ____ effect with CMC
Antagonistic
AMINOGLYCOSIDES
Streptomycin
Identify the source.
Streptomyces griseus
AMINOGLYCOSIDES
Neomycin
Identify the source.
Streptomyces fradiae
AMINOGLYCOSIDES
Paromomycin
Identify the source.
Streptomyces rimosus
AMINOGLYCOSIDES
Kanamycin
Identify the source.
Streptomyces kanamyceticus
AMINOGLYCOSIDES
Tobramycin
Identify the source.
Streptomyces tenebrarius
AMINOGLYCOSIDES
Gentamicin
Identify the source.
Micromonospora purpurea
AMINOGLYCOSIDES
First anti-TB antibiotic
Streptomycin
AMINOGLYCOSIDES
Anti-amebic
Paromycin
AMINOGLYCOSIDES
For Bacillary Dysentery
Kanamycin
AMINOGLYCOSIDES
Most active nebramycin useful for conjuctivity
Tobramycin
AMINOGLYCOSIDES
Gentamycin dosing:
5 or 7mg/kg (____ nomogram)
Hartford
TETRACYCLINES
Tetracyclines are isolated from ____.
Streptomyces spp.
TETRACYCLINES
Short-acting Tetracyclines
- Tetracycline
- Oxytetracycline
TO-S
TETRACYCLINES
Intermediate-acting Tetracyclines
- Limecycline
- Demelocycline
L-I-D
TETRACYCLINES
Long-acting Tetracyclines
- Doxycycline
- Minocycline
L-DM
TETRACYCLINES
Tetracyclines are ____.
-static or -cidal
-Static
TETRACYCLINES
Tetracyclines are derivatives of ____.
Octahydronaphthacene
TETRACYCLINES
Tetracyclines can chelate except ____.
Doxycycline
TETRACYCLINES
Tetracyclines can cause ____ in children.
Contraindicated for children under 7 years old.
Hypoplasia
TETRACYCLINES
MOA of tetracyclines
30s binding
TETRACYCLINES
Eradication of asymptomatic nasopharyngeal meningococcal carrier
Minocycline
TETRACYCLINES
For gonococcal infection
Doxycycline
TETRACYCLINES
For chronic hyponatremia in SIADH
Demelocycline
TETRACYCLINES
Tetracyclines are used as prophylaxis for ____.
Doxycycline or Minocycline
Acne
TETRACYCLINES
Tetracyclines are drugs of choice for ____, ____, and ____.
- Mycoplasma pneumonia
- Chlamydia
- Rickettsial infections
Class of antibiotics which has a large lactone ring, ketone group, and glycosidically-linked amino sugar
Macrolides
MACROLIDES
MOA of macrolides
50s binding
MACROLIDES
Macrolides are isolated from ____.
Actinomyces
MACROLIDES
Macrolides has the same spectrum of activity as ____ and is - ____ at high doses.
Penicillins, -cidal
MACROLIDES
Inactivated by gastric acid
Erythromycin
MACROLIDES
For Mycobacterium avium complex (MAC) and H. pylori
Clarithromycin
MACROLIDES
Co-drug of choice for chlamydia
+ Tetracylines (Doxycycline)
Azithromycin
MACROLIDES
Sulfur-containing macrolide
Lincomycin
MACROLIDES
Macrolides can cause arrhythmia when taken with ____ and ____.
- Terfenadine
- Astemizole
POLYPEPTIDES
Polypeptides are the most powerful bactericidal antibiotics characterized by the presence of sever ____ linkages
– CONH
POLYPEPTIDES
2 adverse effects of polypeptides
- Neurotoxicity
- Nephrotoxicity
POLYPEPTIDES
Drug of choice for pseudomembranous colitis (PO)
Vancomycin
POLYPEPTIDES
Adverse effect of vancomycin that is characterized by flushing due to histamine release caused by rapid infusion
“Red man” Syndrome
Na-experience ni sir
POLYPEPTIDES
Source of vancomycin
Strep. orientalis
POLYPEPTIDES
MOA of vancomycin
Cell wall synthesis inhibition
Dala-D-ala terminus
POLYPEPTIDES
Mechanism of resistance of vancomycin
Replacement of terminal D-ala with d-lactate
POLYPEPTIDES
Teicoplanin is from ____.
Actinoplanes teichomyceticus
POLYPEPTIDES
MOA of teicoplanin
Cell wall synthesis inhibition
peptidoglycan layer
POLYPEPTIDES
Bacitracin is isolated from ____.
Bacillus subtillis
POLYPEPTIDES
Bacitracin has enhanced activity with ____.
Topical only
Zinc
POLYPEPTIDES
Polymyxin B is isolated from ____.
Bacillus polymyxa
POLYPEPTIDES
Colistin is isolated from ____.
Aerobacillus colistinus
POLYPEPTIDES
Gramicidin A is isolated from ____.
Bacillus brevis
UNCLASSIFIED
Drug of choice for typhoid fever
Chloramphenicol
UNCLASSIFIED
MOA of chloramphenicol
50s inhibition
UNCLASSIFIED
Chloramphenicol has a ____ group used for broad spectrum, life-threatening infections.
Nitro
UNCLASSIFIED
Chloramphenicol can cause ____ in infants.
Gray baby syndrome (cyanosis)
UNCLASSIFIED
MOA of mupirocin
Topical
Interference with RNA and protein synthesis
UNCLASSIFIED
MOA of linezolid
Protein synthesis inhibition
30S and 70S binding
UNCLASSIFIED
MOA of fosfomycin tromethamine
NAM synthesis inhibition
UNCLASSIFIED
Analog of PEP that is used for uncomplicated UTI for female only
PEP = female
Fosfomycin tromethamine
UNCLASSIFIED
MOA of Quinupristin (Dalfopristin)
50s binding
Antibiotics contraindicated during pregnancy
- Aminoglycosides
- Clarithromycin
- Erythromycin estolate
- TCNs
ACET
