Agents Targeting Cellular Machinery Flashcards
what drugs are aminoglycosides
Amikacin
Gentamicin
Kanamycin
Neomycin
Streptomycin
Tobramycin
what drug type is azithromycin, clarithromycin, erythromycin
Macrolides
what types of drugs are protein synthesis inhibitors
Tetracyclines
Aminoglycosides
Macrolides
Clindamycin, Chloramphenicol, Linezolid
what groups of drugs target DNA
Sulfonamides
Trimethoprim
Fluoquinolones
Metronidazole
what group is “-floxacin”?
Fluoroquinolones
what drugs are protein synthesis inhibitors
Aminoglycosides
Macrolides
Tetracycline
Do protein synthesis inhibitors exert a bacteriostatic or bacteriocidal effect?
Bacrteriostatic, some can be bactericidal
HOW do protein synthesis inhibitors work?
disrupt process of translation by targeting the molecular machinery needed to translate mRNA to protein
Name aminoglycosides (protein synthesis inhibitors)
streptomycin
gentamicin
kanamycin
amikacin
tobramycin
neomycin
Aminoglycosides are considered to have a 1 spectrum of activity resulting in a 2 (bacteriostatic/-cidal) effect
- broad
2. bactericidal
what organisms to aminoglycosides work against
aerobic organisms (uptake is oxygen dependent)
Aminoglycosides are 1 inhibitors. They are used in combo with 2 to treat serious gram 3 infections (penumonia, UTI) and are not absorbed will from the 4
- protein synthesis
- beta-lactams
- gut
MOA of aminoglycosides
binds to 30S and blocks formation of initiation complex
Key adverse effects of aminoglycosides
nephrotoxicity
ototoxicity
Macrolides mainly target gram + but some gram -. But overall narrow in spectrum. list the drugs in order from broadest to lowest spectrum
Azithromycin>Clarithromycin>Erythromycin
which macrolide has a long 1/2 life
Azithromyucin
where does azithromycin concentrate
Lungs
Tonsils
Cerivx
Key adverse effects of macrolides
GI issues
CV: prolong QT interval
drugs that are tetracyclines
tetracycline
minocycline
tigecycline
doxycycline
MOA of macrolides
Impairs translocation - blocking elongation or growing
MOA of tetracyclines
Binds to 30S subunit of ribosomes and prevents binding of tRNA
Tetracyclines are a 1 spectrum antibiotic that exerts a 2 effect
- broad
2. bacteriostatic
Key adverse effects of tetracyclines
Nutrient interactions: bind calcium which disrupts in growth of calcified tissue (bone, teeth) particularly during growth, discoloration of teeth
Ecological effect: disrupt normal flora
photosensitivity
whcih tetracyclines absorption is not affected by food
doxycycline
which tetracycline undergoes urine excretion, so kidney function must be considered
tetracycline
minocycline
tigecycline
which tetracycline undergoes liver excretion, so hepatic function must be considered
doxycycline
what is clindamycins spectrum of activity? what is it used for
relatively narrow
soft tissue infections caused b streptococci and staphylococci
community acquired MRSA of skin and soft tissue
MOA of clindamycin
prevents formation of initiation complex
key adverse effects of clindamycin
GI
C. diff infection**
Chloramphenicol is a 1 spectrum antibiotic that exerts a 2 effect
Rarely used except for serious infections such as 3 and 4. Can also be used to treat 5 infections
- broad
- bacteriostatic
- typhus
- rocky mountain spotted fever
- eye
MOA of chloramphenicol
prevents transpeptidation or peptidyl bond formation
key adverse effects of chloramphenicol
blood: suppression of RBC production
Gray baby syndrome: infants lack glucuronic acid conjugation
Linezolid is effective against most gram 1 organisms.
positive
because of its unique mechanism which protein synthesis inhibitor is effect against penicillin, methicillin, and vancomycin resistant organisms
Linezolid
MOA of linezolid
inhibits formation of the ribosomal-fMet-tRNA complex
Key adverse effect of linezolid
myelosuppression
what protein synthesis inhibitor is good for hospital acquired MRSA and resistance strains
Linezolid
what protein synthesis inhibitor has 100% bioavailability
Linezolid
Sulfonamides are 1 agents that are 2 spectrum.
- antifolate
2. broad
MOA of sulfonamides
structural similarity to PABA. Agents compete with PABA for the enzyme dihydropteroate synthase and block dihydrofolic acid synthesis and thus DNA synthesis
key adverse effects of sulfonamides
photosensitivity
what drug classes are folate synthesis inhibitors
sulfonamides
trimethroprim (and pyrimethamine)
Trimethorpim and pyrimethamine spectrum of activity includes 1 bacteria. Used commonly to treat 2
- gram -
2. UTI
MOA of trimethoprim and pyrimethamine
inhibitor of bacterial dihydrofolate reductase resuling in impaired DNA synthesis
key SE of trimethoprim and pyrimethamine
blood: bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia
Trimethoprim-sulfamethoxazole is a 1 agent that is commonly used to treat 2 and 3. MOA includes 4 activity when combining the 2 drugs
- antifolate
- UTI
- prostatitis
- synergistic
what drug is a DNA gyrase inhibitor
fluoroquinolones
Fluorquinolones are 1 spectrum antibiotics that work against gram 2 bacteria
- broad
2. + and -
MOA of fluoroquinolones
dirsupt the winding of DNA and separation of DNA strands during transcription and replication
inhibit topoisomerase II (DNA gyrase) and IV
key SE of fluorquinolones
GI
drug-nutrient interaction: bind divalent cations and prevent absorption
Cardio: QT elongation
least active florquinolone
norflaxacin
fluorquinolones that work well againsts gram - and some activity against +
group 2
- ciprofloxacin
- levofloxacin
- ofloxacin
fluoroquinolones that have best activity against gram +
group 3
- gatifloxacin
- gemifloxacin
- moxifloxacin
what type of drug is DNA damaging agents
Metronidazole
Metronidazole is also effective against 1. Its spectrum of activity is limited to 2 bacteria. It is used in tx of 3
- protozoa
- anaerobic
- c. diff
MOA of metronidazole
Prodrug - rxn metabolites bind to DNA and disrupt function causing damage
key adverse effects of metronidazole
GI
metabolism: disulfiram-effect (avoid alcohol)
what does ciprofloxacin treat
UTI
abdominal
respiratory
skin soft tissue
anthrax