Chapter 11a (antibacterials) Flashcards
most common cause of death in world
infectious disease
many antibiotics originally came from…
natural sources
Louis Pasteur discovered…
anthrax and rabies vaccines; that microorganisms inhibit replication of other microorganisms
Dr. Ehrlich
discovered “magic bullet”; an organic arsenic compound (Salvarsan) used to treat syphilis and trypanosomiasis
Salvarsan
organic arsenic compound used to treat syphilis and trypanosomiasis; discovered at turn of 20th century
Gerhard Domagk
discovered first sulfa drug from injecting dye into daughter with sepsis; Prontosil (sulfanilamide)
Prontosil
sulfanilamide; pro-drug sulfa antibiotic. First named sulfa drug. Gets converted into sulfanilamide in body.
sulfa drugs
sulfonamide based drugs; some have antimicrobial properties while others are antiinflammatory or anticonvulsant
Rarely used now as antibiotics b/c of resistance, but many diabetic and diuretic medications use sulfa compounds
sulfa drugs or penicillin on skin
never used b/c they are too sensitizing
sulfonamide antibacterials
stop folic acid synthesis so bacteria cannot synthesize DNA
sulfonamide antibacterials often mixed with…
trimethoprim, because both stop folic acid synthesis so synergism occurs.
trimethoprim stops dihydrofolatase and sulfa drugs inhibit tetrahydrofolatereductase
qualities of a good antibiotic
- reaches site of infection
- penetrates cell
- reaches target and kills it
mercury compounds
used to be injected intraurethrally to treat syphilis
mechanisms of resistance
- decreased permeability (eg pseudomonas)
- antibiotic efflux pump (S. pneumonia vs. quinolones and macrolides)
- drug inactivation (eg B-lactamase from H. influenzae, staph, E.coli, and Klebsiella)
- altered target site (eg S. pneumonia with altered PBPs, S. pneu against macrolides with ribosomal methylase, S pneu against quinolones with GyrA and Topo4)
porin channels found in what bacteria?
gram negative
B lactamase…
breaks open B-lactam ring which renders penicillins, cephalosporins, monobactams, and carbepenems useless
PBPs
penicillin binding proteins; penicillin binds to these and then prevents cell wall synthesis
sulfadiazine
modern sulfa antibiotic; one of main ingredients in silver sulfadiazine cream which is used extensively for burns
sulfamethoxazole
one of time ingredients in Septra and Bactrim combination antibacterials
Alexander Flemming
recognized the importance of the antibiotic action of penicillin
Penicillins
kill bacteria by interfering with cell wall synthesis and by destabalizing transmembrane potential to cause cell lysis; all have common beta-lactam ring structure
first penicillins
could not be given orally b/c they were inactivated by gastric acids
penicillin V
stable in acid so can be given orally;
“pen-vee”
aminopenicillins
penicillin base with amino group added; like amoxicillin or ampicillin
broad-spectrum penicillins
from resistance, now only some of the newer, more expensive penicillins are broad-spectrum; those in the 3rd and 4th generation
Bicillin
penicillin G; not acid stable so can’t be given orally; given by IM or IV, first mass-produced antibiotic in US (in 1940s)
ampicillin is very similar to
amoxicillin; both are aminopenicillins
ticarcillin
has extended spectrum of action against gram negative bacteria beyond that of earlier penicillins
4th gen; antipseudomonal penicillin; given by IM or IV
Augmentin
amoxicillin/clavulanate combination used against penicillinase producing bacteria; oral
increased antibiotic resistance comes from…
overuse of antibiotics; inappropriate antibiotic given; low dose given (subinhibitory exposure or not long enough time taking antibiotic)
Quinolones
interfere with genetic duplication of bacteria by interfering with DNA gyrase and topoisomerase IV (the enzymes that untwist DNA so it can be read and then fold it back up)
penicillin hives
true drug allergy to penicillin (raised welt-like bumps), just a rash w/o raised bumps is not an actual allergy and it is okay to take penicillin again, unlike if person actually has allergy then 2nd exposure could cause bronchoconstriction and serious allergy response
aminoglycosides
inhibit bacterial protein synthesis; most have to be administered parenterally or topically, usually in the hospital with blood level monitoring b/c of kindey and hearing toxicities