1 Flashcards
Gentamicin
diminished renal clearance in pts with renal failure
Erythromycin
stimulates gut motilin receptors and may induce nausea
Components of interaction
Pharmacokinetics Pharmacodynamic Immunity Resistance Sepsis Selective toxicity
General taxonomy depending on mechanism of action
ribosomal inhibitors (macrolides), Cell wall disrupters (B-lactams), DNA disturbers (fluoroquinolones), metabolic poisons (trimethoprim-sulfamethoxazole)
Antibiotics also classified based on laboratory
assessment of the interaction of pathogen and
antibiotic drug
Static
Cidal
Arsenic
1800s for syphilis
Sulfonamides
1935 synthetic antimicrobial agents
Sulphonamides
Nh2 is essential
Benzene ring attached to sulfur
Causes nausea rashes dyscrasia precipitation and stones
Structural analogs and competitive competitive antagonist for PABA
Cotrimoxazole- Trimethoprim
Combination (Bactrim, Septrin,
Balakatrin):
One of the few, still used, sulfa drugs. – Very effective fixed combination. – No resistance. – Very useful in UTI, RTI, Salmonella, and Pneumocystis pneumonia, an opportunistic infection in AIDS patients.
Quinolones
Interfere with cell division of bacteria.
Nalidixic acid
Very old urinary antiseptic
Norfloxacin
UTI
3 day course
fluorinated 4-quinolones
Ciprofloxacin
moxifloxacin
(AVELOX), and gatifloxacin (TEQUIN)
Ciprofloxacin
Prophylactic for meningitis
Wide range of activity botulinum
Cause gi upset and epilepsy
Quinolones
Carboxylic acid group at position 3 Chromophore group target bacterial DNA gyrase and Topoisomeras which is responsible for the continuous introduction of negative supercoils into DNA inhibit the nicking and closing activity of the gyrase and also block the activity of topoisomerase IV
Nitrofurans
A number of 5-nitro-2-furaldehyde derivatives
treatment and/or prophylaxis
of microbial infections, primarily in the urinary
tract
• modify various bacterial macromolecules that
affect a variety of biochemical processes (e.g.,
DNA and RNA synthesis, protein synthesis )
the slower reduction by
mammalian cells prevents high serum concentrations.
gramnegative bacteria (E. coli, P. mirabilis is variable) and
some susceptible gram-positive organisms, such as
S. aureus and Enterococcus faecalis
Nitrofurans
The singular indication for nitrofurantoin is the treatment and longterm prophylaxis of lower UTIs caused by susceptible bacteria
• it is not used as a bacterial suppressant.
• It is often used prophylactically post intercourse in women with
chronic UTIs
greater than 100 ug/mL ensures bactericidal activity
Nausea and vomiting
Methenamine
have two major effects :
bactericidal ( formaldehyde) / bacteriostatic ( lowering urine pH )
mandelic (Mandelamine) or
hippuric (Hiprex, Urex) acid.
administered orally and is well absorbed from
the intestinal tract.
10 to 30% decomposes in the stomach unless the tablets are
protected by an enteric coating
inactive form (methenamine) is distributed to virtually
every bodyfluid
Prophylaxis of uti
Sterilise urine
Beta lactam antibiotics
Contain b lac ring
Inhibit cell wall synthesis
•Oldest antibiotics, but still growing and
new agents are still discovered and added
to the group.
Penicillin g
Lactamase
Penicillins
Are the most widely used antibiotics.
◼ Penicillin G was found very effective against the
most common and important Gram positive
bacteria like Staph, Strept, Pneumococcus, and
many others.
Penicillinase
Inactivates penicillin by breaking the beta lactam ring
Clavulanic acid combined with ampicillin inhibits it = augmentin /amoclan
Penicillin actions
The cell walls of bacteria are essential for their normal growth and development •Peptidoglycan provides rigid mechanical stability gram-positive microorganisms, the cell wall is 50 to 100 molecules thick, • but it is only 1 or 2 molecules thick in gram-negative bacteria last step in peptidoglycan synthesis that is inhibited by the β-lactam antibiotics
B lactamase inhibitors
Clavulanic acid
Sublactam
Tazobacta
Penicillin g
Benzyl penicillin Deep IM injection Highly active against sensitive strains of gram + cocci Hydrolyzed by penicillinase Ineffective s aureus
Procain benzyl penicillin
Painless, prolonged
action injection
Phenoxymethyl penicillin
Oral not destroyed by gastric acid