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| this lecture focuses primarily on the function of |
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| fleming was studying microbes in lab growing cultures, when whe came back one of the cultures had been contaminated by a mold and around that mold there was no |
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| in the vicinity of the contamination no growth of |
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| fleming wondered why there was no |
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| priduced a substance that killed the acteria |
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| florey and chain developed a purification method for |
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| floery and chain also showed |
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| how it could cure incrable abacteria |
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| n principle drugs that inhibit |
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| bacterial cell wall synthesis. |
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| penicllin has a narrow spectrum against |
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| we can change the penicllin molecule to alter its |
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| because of their safet and lack of toxicity-they are |
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| bactericidal and non toxic to human cells |
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| drug resistance is usually due to the |
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| creation of a beta lacatamse |
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| pharmaceutical companies have created |
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| beta lactamase inhibitors |
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| there are some beta lactamases that can't bind to the |
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| a target alteration in a penicillin binding protien. |
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penicillin
cealosporin
monobactam
cephalosporins
carpapenams |
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| the hydrogens in carpapenams are in |
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| trans may confer resistance to beta lactamases |
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| bacterial cell wall syntehseis |
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1) syntehssiz the moomer
2) polymerize
3) cross link |
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| nacetyl glucosamine and n acetyl muriamic acid created |
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| monosacharride with 5 amino acid |
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| target is unique to bacteria and this makes them |
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| each type of beta lactam- you can change subsiituents |
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differ in their target, differing ability to traverse porins,
various biological activitie, resistance to beta lactamase. |
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mono sacchardie plus five amino acids two sugars to which amino acids are added and the process requires UTP
2 alanines on the end are the target
beta lactams
penta peptide attached to a lipid carrier |
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| bactoprenol transfers the monomer to teh |
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| the more cross linking the more |
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| various drugs inhibit different steps. |
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bacitracin inhibits monomer
vanvomycin inhibits polymerizations
beta lactams inhibits cross linking |
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| bacitracin inhibits the creation of the |
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| cross linking involves a trans peptidase reaction |
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d-ala-d-ala
glycine attacks and transpeptidases
glycine--> alanine |
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| d-ala d-ala is the substrate for |
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| normally there is a transient complex form |
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| between transpeptidase and dala dala but if it attaches to pencillin then it is a stable bond |
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| penicllin binding proteins |
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1) pencillin carbon 14
2) incubate the pencillin with ecoli
3) proteins covalently bond
turns out htey are transpeptidases |
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| some transpeptidases responsible for |
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| pencillin binding proteins differe among _____ |
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| PBPs differ in their affinitites towards |
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| Pencillin binding proteins. |
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| bacteria can differ in their susceptibility to beta lactam drugs because their _____ enaymes are different |
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| mutations in ____ can confer resistance to ______ |
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| why does a staphlyococcus explode |
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| the cell wall is weakened and the itnernal osmotic presure (hypertonic) so it explodes |
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| What would happen if it were in a hypertonic envronment? |
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| It might remain intact because without a cell wall |
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| enzymes that cleave beta lactams |
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beta lactamase at the n-c bond in bpenicllin-usually acquired via horizontal transmission in plasmid
pencillin acylase-removes acyl subsitituent formt eh beta lactam ring
6-aminipenicllianic acid-a lead compund for generationg new semi-syntehtic penicllins with novel properties. ( new types of drug development)
100 different beta lactamases.
there are drugs that inhibit beta lactamases. |
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| c-n bond in the penicllin |
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| the r subsitutent of the penicllin which leaves the 6 aminopenicllanic acid |
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| the r subsitutent of the penicllin which leaves the 6 aminopenicllanic acid |
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| lead peptide for new drug development |
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| what properties of penicllin do we want to influence? What ened to happen for a beta lactam to kill a gram negative bacteria? |
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beta lactams must penetrate the outer membrane
escape inactivation
bind to target enzymess
resistance can be due to
lack of membrane penetration
inactivation by beta lactams
altered target PBPs |
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| to get in to throught he otuer membrane |
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| gram positive makes lots/little beta lactamse |
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| lots because other wise it will diffuse |
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| in gram negative htey pridcue mroe or less beta lactamse |
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| less because the outer membrane |
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lack fo membrane penetration
inactivation of beta lactamase
altered target PBPs |
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improve pentration trhough porins
decrease beta lactamase susceptibility, broadening spectrum
alter PBP ninding pattern |
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oral forms of various penicllins
subject to inactivation by gastric acid |
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| repository forms (procain penicillin G nad benzathine penicllin G |
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| absorbed slowly producing prolonged concentrations of drug |
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| procaine is not used much due to resistance |
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sterp pyogenes
strep throat
rehumatic fever/glomerular nefritis
sequelae could kill you |
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| penicllin only enters the CNS |
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| when the meninges are inflamed |
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| pencillins are _____ and eliminated by the _____ |
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| Should you increase or reduce the dosage in a person with sever kidne damage |
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| many organic acids such as pencillin are secreted via |
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| prebenicid is administered, secretions go _____- |
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| when pencillin was first introudced they collected the urine and recrystallized the pencillin |
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| main type of pencillin toxicity |
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| pencillin G undergoes isomerization t benzopenacyllemic acid and this combines with a protein |
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| leads to an IgG and an IgE reaction |
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| allergic reactions include |
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| skin rash, serum sickness, anaphylaxis (IgE) |
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| Go can occur due to aleterations in |
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| colitis (staph aureus) and mucositis (overgrwoth of c. albicans) |
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| results from changes to normal flora |
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| in renal filure _____ and ____ can cause seizures |
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