Antimicrobial Therapy

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Carbapenems

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bacterial products, beta lactam based. Used with other drugs to prevent breakdown of liver. ex) bacitracin

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Vancomycin

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Last resort treatments for infections. poorly with gram negative. Power and often toxic antibiotic.

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Penicillin

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fungal product based on B lactam ring. if B lactam ring is broken, they are inactivated. It is used better against gram positives.

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Cephalosporins

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Ppl use this for ppl that are allergic to penicillin. More expensive than penicillin.

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Polymixins

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Attack bacterial membrane but not eukaryotic cells. good against gram negatives and used in creams.

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4 things that inhibit bacterial protein synthesis

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Tetracycline, streptomycin, chloramphenicol, erythromycin

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2 things that act as cell membrane disrupters

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Polymixin and Tyrocidins

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inhibits bacterial nucleic acid synthesis

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Rifamycin-->Rifampin
Quinolones,

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Examples of antimicrobial agents that act on bacterial cell walls?(5)

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Penicillin, Cephalosporin, Carbapenems, Bacitracin, Carbapenems, Vancomycin

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Antimicrobial agents that damage the bacterial cell membrane(2)

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Polymixin, Tryrocidin

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Antimicrobal that inhibit bacterial protein synthesis(4)

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Strephomycin, Tetracyclines, Chloramphenicol, Macrolides

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Antimicrobal agents that inhibit bacterial nucleic acid synthesis(2)

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Rifampin, Quinolones

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Antimicrobial agents that act as antimetabolites(2)

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Sulforamides, Isoniazid

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Chemotherapeutic agents

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drugs used to control pathogenic organisms

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antibiotics

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anti life, chemical agents taken by humans against microbial infections

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antiseptics

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agents that can be safety used on our skin that could not be used internally. included in many creams and lotions

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antimicrobial agent

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chemical agent of any origin that is used to treat infections

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Sulfa drug

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The first successful antimicrobial agent used widely. Made be Gerhard Domagk in 1932.

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Gerhard Domagk

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Made sulfa drug from red dye prontosil in 1932

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Salvasan

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developed by Enrlich, a agent that was found limited use in the treatment of syphilis.

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peniciliin

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Found by Alexander flemming and made practical by Florey and Chain

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Selman Waksman

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He isolated streptomycin it from soil bacteria

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specific toxicity

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antimicrobial agent that attacks and kills microbes but does not harm or kills us

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wide spectrum of activity
narrow spectrum of activity

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Kills a wide range of types of microbes
Kills a smaller number of types of microbes

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Desired properties of antimicrobial agents

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selective, stable toxicity, non allergenic, reasonable cost, etc

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Bactercidal

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antimicrobial agent kills a bacterium

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Bacteriostatic

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does not kill it but prevents its growth

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antimicrobial agents that attack bacterial cell walls

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drugs that inhibits peptidoglycin synthesis, so that when bacterial cell reproduce it weakens cell wall and it bursts

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peptidoglycin

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helps bacteria cell wall resist the high internal osmotic pressure of the cell.

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Why are penicillin and other agents more effect against gram positive than gram negative?

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More effective against gram positive because they don't have outer membrane to protect them from bursting.

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Penicillin and related antibiotics only attack peptidoglycan as it is being newly synthesized while the bacterium is reproducing

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Bacterium are invulnerable to penicillin as long as they don't undertake cell division. This is why it is important to eat all the antibiotic prescribed.

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Bacitracin

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attack cell wall of bacteria.toxic produced by bacterium bacillus licheniformis. Used internally to treat severe resistant. Often included in skin treatments.

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Antimicrobial agents that damage the bacterial cell membrane

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attack bacterial cell membranes but not those of eukaryotics

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Tyrocidins

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used against gram positives would infections. Attack bacterial membrane but not eukaryotic cells.

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Antimicrobial agents that inhibit bacterial protein synthesis

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antibodies bind to and inhibits the activity of bacterial ribosomes in a number of ways, but do not affect eukaryotic ribosomes.

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Antimicrobial agents that inhibit bacterial nucleic acid synthesis

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Agents bind to bacterial RNA ploymerase enzymes and inhibits them but do not affect ours.

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Streptomycin

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one of the first antimicrobial agents, but many bacteria are resistant to it now. Work well with penicillin in treatment of wound and burn infections. One of the first to have useful effect against tuberculosis.

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Tetracycline

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widest spectrum of all antibacterial agents and good at killing bacteria inside our cell. Cause teeth mottling and can cause liver and kidney toxic. Calcium inactivates it.

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Chloramphenicol

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bacterial origins but synthetic now. Cause rare but fatal anemia, reserved for certain severe resistant infections.

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Macrolides

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bacteriostatic, low toxicity and used in combinations with other antimicrobial agents.

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Rifampin

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blocks transcription of RNA. key drug in treatment of tuberculosis. Liver toxic. produced by streptomyces bacteria.

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Quinolones

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blocks unwinding of DNA and thus interferes with transcription and cell division. ex) nalidixic acid

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antimicrobial agents that act as anti metabolites

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those type of antibiotics look like on of the natural substrate molecules(structural analogues) but NOT THE SAME, b/c they interferes with the enzyme and take the proper substrate's place

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Sulfa Drug

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they are similar to an essential metabolite needed to form folic acid in bacteria and takes that subtrate's place

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sulfonamides

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the sulfa drug. used with trimethoprim to improve effectiveness. inhibits different step in the bacterial folic acid synthesis pathway.

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Isoniazid

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antimetabolite to the production by mycobacteria of nicain and vitamin B6 used to treat tuberculosis in combination with other drugs

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Side effects of anti microbial agents

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Toxicity, Allergy, Disruption of normal gut flora

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normal gut flora

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long term use or high dose can kill gut bacteria and disrupt normal gut functions.

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5 examples of the genetic basis of resistance

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1. Alternation of the target of an antibiotic
2.Alternation of membrane and permeability
3.Alternation of or acquisition of enzymes that inactive antibiotics
4.alternation of enzymes in a target pathway
5.alternation of a metabolic pathway

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Alternation of the target of an antibiotic

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bacterial ribosome produce an altered ribsome that still functions normally, but has subtle alternation in shape so that the agents can no longer bind to it to disrupt protein synthesis

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Alternation of membrane and permeability

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when the microbacterial agent can not longer get into the cell in order to on its target

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Alternation of or acquisition of enzymes that inactive antibiotics

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when they acquire an enzyme that can inactivate an antimicrobial agent and destroy the active stricture of penicillin type agent.

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alternation of enzymes in a target pathway

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subtle changes that causes an antimetabolite to be unable to bind with the enzyme and inactivate it, the enzyme continues to function( enzyme not recognize the anti metabolites)

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alternation of a metabolic pathway

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The step that would be inhibit by an antimetabolite no longer is functional, but the product of the pathway is still formed. OR the bacterium is able to obtain that product from its environment instead of having to make it.

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3 Number of ways to limit appearance of drug resistance bacteria

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1) Do not take bacterial antimicrobial agents unless you need them
2) when taking antibacterial antimicrobial agents appropriately, take all of them and finish the course
3) Use antimicrobial agents only for their intended purposes.

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1)Synergistic effect
2)Antagonistic effect

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1)an additive effect where two chemicals have a greater combined effect than when used separately. ex) clavulanic acid with amoxicillin
2)when one agent acts against the effectiveness of another

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Kirby Bauer

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paper discs placed in lawn of bacteria to test the zone of inhibition that will appear around the discs. Clear rings tells us that the bacteria did not grow b/c of the antimicrobial agent diffusing from the disc.

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4 anti fungal agents. Since those are eukaryotic, they are more toxic than antibacterial agents when taken interanally

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Imidazoles/triazoles, polyenes;amphotericin B, Tolnaftate, Nystatin, Griseofulvin, flucytosine, terbinafine

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Imidazoles/triazoles

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disrupt fungal cell membranes by interfering with sterol synthesis. An anti-fungal agents.

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polyenes;amphotericin B

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common used antifungal agents for internal infections. several side effects. Nystain is used like amphotericin B, but it is a better agent to treat intestinal fungal infections. An anti-fungal agents.

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Griseofulvin

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Used for entrenched skin infections by fungi. An anti-fungal agents.

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Tolnaftate,flucytosine, terbinafine

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newer drugs against problems such as athlete foot and jock itch. An anti-fungal agents.

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Anti viral agents

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incorprate into replicating DNA chains during viral gene replication an cause their synthesis to be disrupted and terminated.

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AZT( azidothymidine)

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Used to treat AIDS are nucleotide analogues.Anti viral agents

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Amantadine

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used to treat established influenza, but has a lot of risks. Anti viral agents

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Interferons

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natural animal cell products that function in a form of deference against viral infections.Anti viral agents

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Anti-protozoan agents(2)

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Artemisin, Metronidazole

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Agents used against worms(2)

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Piperazine, ivermectin used against round worms and nematodes

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Artemisin

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anti malaria drug developed from ancient Chinese practises. Anti-protozoan agents

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Metronidazole

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used to treat trichmonas and giardia. b/c it acts against DNA, but it may cause birth defects and cancer. Anti-protozoan agents