Chemotherapeutic drug

alex0624's version from 2016-07-12 12:49


Question Answer
Treatment of systemic infections with specific drugs that selectively suppress the infecting microorganism without significantly affecting the recipient. Referred to as Antibacterial agents Chemotherapy
Antibacterial agents can be(2):Bactericidal and bacteriostatic
Cause death of the microorganismBactericidal
Examples for bactericidal Penicillins, Aminoglycosides, Cephalosporins
Inhibits the growth of the microorganismBacteriostatic
Bacteriostatic examplesSulfonamides, Tetracyclines, Erythromycin
Targets of actions of antimicrobialsProtein synthesis, Cell wall(peptydoglycan synthesis), Nucleic acid(DNA) and metabolic pathways(folate)
Inhhibition of cell wall synthesisPenicillins, Cephalosporins, carbapenems, monobactum, Vancomycin(glycopeptides)
Cell wall inhibitors(peptidoglycan synthesis)B-lactams , bacitracin and glycoprotein.
all beta lactam drugs are composed ofThiazolidine ring and a beta lactam ring
Some organism(s.aureus) create recistance to B-lactam drugs by producingPenicillinase
Bacterial cell wall is made of______ with 2 main sugar molecules named as ______Peptidoglycan, NAG/NAM
Croslinking of bacterial wallCroslinking of the pentapet...
Removed terminal D-ALA and make cross-linking with adjacent pentamer.Transpeptidase (penicillin binding protein)
Bind to active site of transpeptidase(PBP) and prevent crosslinkingB-Lactam drugs
Affect the cell wall by acting on transglycosilationVancomycin
Brings the sugars together(NAM/NAG)Transglycosilation
Cell wall is thickGram Positive Bacteria
Thin cell wall with two membrane layersGram Negative Bacteria
Mechanism of resistance of StaphylococciPenicillinase break the betalactam ring
Alteration of penicillin-binding proteinsS. Aureus resistant to MRSA, penicillin resistant pneumococci
Drugs for S. AureusNafcilin, Methilin and Vancomycin(if MRSA).
Susceptible to pellicinasePenicillin G(parenteral) will not be effective
Only gram negative bacteria were penicillin g will workMeningococcemia
Penicillin G can be used in what bacterial infectionsStreptococci, pneumococci, meningococci, treponema pallidum, actinomyces
Narrow spectrum (penicillinase resistant):Methicillin, naficillin , oxacillin, cloxacillin, dicloxacillin
DOC for Actinomyces an Treponema PallidumPenicillin G
Why Penicillin G cannot work in Pseudomonas(gram negative)Because cant penetrate thick cell wall???
DOC for Staph aureus(Penicillinase resitant drugs)Methicillin, naficillin , oxacillin, cloxacillin, dicloxacillin
For Gram negative E. coliBroad spectrum(penicillinace susceptible: Ampicillin and amoxicillin
DOC for Gram positive cocci, Haemophillus influenza, listeria monocytogenes, H.pylori, enterococcusAmpicillin and amoxicillin Broad spectrum antibacterial.
Associated with peptic ulcersH. Pylory
H. Pylori treatmentOmeprazole, Amoxicilin, metronidazole
DOC for Listeria MonocytogenesAmpicillin
common organism causing Cystic fibrosis. Also present in burn...Pseudomonas
DOC for pseudomonasTicarcillin, piperacillin and azlocillin
Route of administration of Penicillin G is alwaysParenterally(IV) because is acid labile
Repository penicillin G(Long acting)Procaine(24hr) and Benzathine penicillin G
Drug which enhanced uric acid excretion(treatment of Gout)Probenecid
competitively inhibits the renal tubular secretion of penicillin. Thus it increases the concentration of penicillin and prolongs its activityProbenecid
DOC for actinomysisPenicillin G
DOC for syphilis(Treponema Pallidum)Benzathine Penicillin/Procaine
Used in Streptococcal, meningococcal, gram positive bacilli infectionsPenicillin G
DOC for Staph aureusMethicillin, Nafcillin and Oxacillin
No longer commonly recommended for clinical use because of its nephrotoxicityMethicillin (only use for check for Penicillin resistant)
used in Infections due to enterococci, E. coli, Proteus mirabilis, Haemophilus influenzaeAmpicillin and amoxicillin
DOC for Listeria monocytogenes(bacterial meningitis)Ampicillin
used in endocarditis before major procedures H.pylori infection(peptic ulcers)Amoxicillin
Test for diagnosed H.PyloriUrea breath test
Antimicrobial for H pyloriAmoxicillin, metronidazole, tetracyclin and clarithromycin(macrolide)
Prophylactic drug for bacterial endocarditis (prevents septicemia).Ampicillin and Amoxicillin
this drug can be used in combination with clavulanic acid and sulbactumAmpicillin and Amoxicillin
beta lactamase inhibitorsClavulonic acid and sulbactam (Tazobactam not an antibiotic/irreversible binding)
DOC for Pseudomonas and enterobacter infectionsTicarcillin and piperacillin
________ have a synergistic action with ____________ against pseudomonal and enterococal speciesPiperacillin and Ticarcillin(cell wall inh), aminoglycosides(Protein synt. inhibitor)
Drug combination for prevent resistance to b lactam drugs:B lactam drug + beta lactamase inhibitor
Prophilactic for Rheumatic feverBenzathine penicillin(long acting penicillin every 3 weeks)
Prophylactic for Gonorrhoea & Syphillis in sexual partnerBenzathine or procaine penicillin
Preferred drug for bacterial endocarditisAmoxicillin.
Combination of amoxicillin and clavulonic acidAugmentin
B-lactam drug + B-lactamase drug combinationsAmoxicillin/ticarcillin +clavulanic acid; Ampicillin+sulbactum; Piperacillin+Tazobactum
B- lactamase producing microorganismstaphylococci, H.influenza, N.gonorrhoea, E.coli, Proteus
Adverse effects of penicillinsHypersensitivities itching, flushing, rash, urticaria, angioedema, bronchospasm, hypotension Cross-sensitivity between individual penicillins possible
cause interstitial nephritisMethicillin and nafcillin
Produce maculopapular rash as a side effect(hypersensitivity reaction)Ampicillin
cause diarrhea- pseudomembranous enterocolits (superinfection)Ampicillin(long term use of any antibiotic)
Have the same MOA of penicillinsCephalosporins
First generation cephalosporinsCephalexin(oral), Cefazolin(parenteral)
use in Gram +ve cocci, Proteus, E.coli, klebsiella pneumonia (PEcK)first generation Cephalosporins
cephalosporisn used in surgical prophylaxis cefazolin
Used in Klebsiella pneumoniafirst generation cephalosporins
2nd generation cephalosporinsCefoxitin, Cefotetan, Cefaclor, Cefamandole & Cefuroxime
More active on Gram –ve bacteria; Haemophilus influenza, Enterobacter, Neisseria, Proteus, E.coli, Klebsiella pneumoniae, Serratia (HEN PEcKS) Cefoxitin, Cefotetan, Cefaclor, Cefamandole & Cefuroxime
have extra effect on CNSCefuroxamine
used for Bacteroids fragilis(mild intra-abdominal & pelvic infections)Cefoxitin, cefotetan
DOC for bacterial meningitis3rd generation cephalosporins
third generation cephalosporinsCefotaxime, Ceftriaxone(IM), Ceftazidime, cefoperazone, Cefixime (oral)
Rx of bacterial meningitis (except Listeria)Cefotaxime and ceftriaxone
Very good activity against PseudomonasCefoperazone, Ceftazidime
First choice Rx of gonorrhoeaCeftriaxone (parenteral) & Cefixime (oral)
Rx of S.typhi (typhoid/enetericfever)(Salmonella)Ceftriaxone, cefotaxime, cefaperazone
Drug combination for PseudomonasPiperalicine + tazobactam; Piperacillin +gentamicin
Fourth generation cephalosporinsCefipime(IV), cefpirome
Cephalosporin if given with _______ increased the chances of nephrotoxicityaminoglycosides
Cause interstitial nephrititsMethicillin
Cephalosporins that contains methylthiotetrazoleCefamandole, Cefoperazone & Cefotetan
may cause disulfiram like reactions with ethanolCefamandole, Cefoperazone & Cefotetan
Vitamin K deficiency causing hypoprothrombinemia and bleeding disorderCefamandole, Cefoperazone & Cefotetan
Monobactams drugAztreonam(IV)
Has a single ring, same MOA as penicillins and cephalosporinsAztreonam(IV)
Resistant to B-lactamasesaztreonam
Only for Gram - infections especially in patints allergic to penicillins/cephalosporinsAztreonam
No cross hypersensitivity reaction between penicillins and _____Aztreonam(IV)
Carbapenems drugsImipenem, Meropenem, ertapenem, Doripenem
Imipenem is rapidly inactivated by _____renal dehydropeptidase
inhibitor of renal dehydropeptidasecilastatin
Those which have renal defects may develop seizures when this drug is administeredCarbapenems
Primary effect of vancomycinby binding to D-ALA-D-ALA terminal of the nascent peptidoglycan pentapeptide side chain
Transglycosilation is made byglycosiltranferase
Brings two sugar moiety togetherglycosiltransferase
Bind to the terminal D-ALA D-ALA preventing cross linkingvancomycin
2nd effect of vancomycininhibits transglycosilase which help to ling sugar residues together
Resistance to vancomycin is bychange the terminal D-ALA to D lactate.
Pseudomembranous enterocolitis due to Clostridium difficile (adminstered orally)Vancomycin
Used in MRSAVancomycin
Red mans syndrome because of release of histamine (flushing, redness of face, hypotension), this can be prevented by slow i.V infusion and pretreatment with antihistaminesVancomycin
because of release of histamine (flushing, redness of face, hypotension), this can be prevented by slow i.V infusion and pretreatment with antihistamines.Red man syndrome
Vancomycin plus _______ may lead to nephrotoxicityAminoglycosides
Nephrotoxicity, neuromuscular blockage and ototoxicity are effects ofAmynoglycosides

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