Antimicrobial Drugs Flashcards
Chemotherapy
The use of drugs to treat a disease.
Antimicrobial drugs
Interfere with growth of microbes within a host
Antibiotic
A substance produced by a microbe that, in small amounts, inhibits another microbe
Selective toxicity
Killing harmful microbes without damaging the host.
Who discovered Penicillin, produced by Penicillium?
Fleming (1928)
What is Prontosil red dye used for?
Streptococcal infections- a sulfanilamide: sulfur based
When were the first clinical trial of penicillin?
1940
Today there’s a growth problem of:
Antibiotic resistance
In 1940, who performed the first clinical trials of penicillin?
Howard Florey and Ernst Chain
Narrow spectrum of microbial activity:
Drugs that affect a narrow range of microbial types
Broad-spectrum antibiotics
Affects a broad range of gram + or gram - bacteria.
Bacteriocidal
Kills microbe directly (a drug used to kill bacteria)
Bacteriostatic
Prevents microbes from growing
Superinfection
overgrowth of normal microbiota that is resistant to antibiotics
5 major action modes of antimicrobial drugs
1st action
- inhibition of cell wall synthesis: penicillins, cephalosporins, bacitracin, vancomycin
5 major action modes of antimicrobial drugs
2nd action:
Inhibition of protein synthesis: erythryomycin, tetracyclines, streptomycin, chloramphenicol.
5 major action modes of antimicrobial drugs
3rd action
- Inhibition of nucleic acid replication and transcription: quinolone, rifampin. (Drugs that are usually specific t viruses)
5 major action modes of antimicrobial drugs
4th action
- Injury to plasma membrane: polymyxin B
5 major action modes of antimicrobial drugs
5th action:
Inhibition of essential metabolite synthesis: sulfanimide, trimethoprim
Inhibitors of cell wall synthesis (inhibit new cell wall formation)
-penicillin
-natural penicillins
-semisynthetic penicillins
-extended-spectrum penicillins
Penicillin contains:
β-lactam ring: active ingredient that prevents cross-linking
The types are differentiated by the chemical side chains attached to the ring
Penicillin prevents
The cross-linking of peptidoglycans, interfering with cell wall construction (especially gram positives)
Natural penicillins extracted from:
Penicillium cultures: penicillin G (injected) and penicillin V (oral)
Natural penicillins are susceptible to:
penicillinases (β-lactamases)
- narrow spectrum of activity
Semisynthetic penicillins
• Contain chemically added side chains, making them resistant to penicillinases
Oxacillin:
Narrow spectrum, only gram-positives, but resistant to penicillinase
Ampicillin:
Extended spectrum, many gram-negatives
Penicillinase-resistant penicillins
Methicillin and oxacillin
Extended-spectrum penicillins
Effective against gram-negatives as well as gram-positives
• Aminopenicillins: ampicillin, amoxicillin
Penicillins plus β-lactamase inhibitors
Contain clavulanic acid, a noncompetitive inhibitor of penicillinase
Carbapenems
Substitute a C for an S and add a double bond to the penicillin nucleus
• Broad spectrum
• Primaxin, doripenem
• Monobactam
Synthetic; single ring instead of the β-lactam double ring
• Low toxicity; works against only certain gram-negatives
• Aztreonam
Cephalosporins
Work similar to penicillins
• β-lactam ring differs from penicillin
• Grouped according to their generation of development
Polypeptide antibiotics
Bacitracin (wounds; first aid ointment
• Topical application; works against gram-positives
• Vancomycin
• Glycopeptide
• Last line against antibiotic-resistant MRSA
Antimycobacterial Antibiotics:
Isoniazid (INH)
• Inhibits the mycolic acid synthesis in mycobacteria
Antimycobacterial Antibiotics
Ethambutol
• Inhibits incorporation of mycolic acid into the cell wall
Inhibition of Cell Wall Synthesis
Prevent bacteria from increasing amount of peptidoglycan
• Have no effect on fully formed bacteria
• Effective only for growing, young populations
Inhibition of Cell Wall Synthesis= No effect on plant or animal cells; Why?
Cross bridges are already in place
None of these cell walls have peptidoglycan
Inhibiting Protein Synthesis
Target bacterial 70S ribosomes
• Large or small subunit
• Chloramphenicol, erythromycin, streptomycin, tetracyclines
Chloramphenicol inhibits
Peptide bond formation
Chloramphenicol binds to:
50S subunit of the 70S ribosome
Chloramphenicol can suppress ______ and affect ________
Bone marrow
Blood cell formation
Can be synthesized chemically; broad spectrum
Aminoglycosides are
• Amino sugars linked by glycoside bonds
Aminoglycosides change
the shape of the 30S subunit of the 70S ribosome
Aminoglycosides can cause
auditory damage (not recommended for pregnant) • Streptomycin, neomycin, gentamicin
• Teratogenic – harmful to a pregnancy
Some antibiotics are known to be teratogenic and should be avoided entirely during pregnancy. These
include ____________ and _____________ (which may cause hearing loss) and tetracycline (which can lead to weakening, hypoplasia, and discoloration of long bones and teeth).
Streptomycin and kanamycin