chemotherapy part 1 (2) Flashcards
penicillins
- _____ penicllin G/ _____ penicillin V: used for mixed _____ infections of the head and neck and _____ infections
- _____: structurally resistant to beta lactamase. skin and soft tissue infections
- -oxacillin, cloxacillin, methicillin, nafcillin
- _____: (ear, nose and throat, H pylori)
- -ampicillin, amoxicillinm and clavulinic acid
- carboxypenicillins (broad spectrum: enterobacter)
- -carbenicillin, ticarcillin and clavulanate
- ureidopenicillins: (klebsiella and enterococci)
- -pipercillin and mezlocillin
parenteral oral aerobic-anaerobic dental antistaphylococcal penicillins aminopenicillins
penicillins: MOA
- bind to _____
- -inhibit _____
- –inhibit the cross-linkages between the _____ strands
- -promote _____
- –autolysin is an enzyme that breaks section of _____ to permit bacteria cell growth and cell lysis
–most effective against growing and dividing cells
penicillin binding proteins transpeptidases peptidoglycan polymer autolysins cell wall
penicillin G (benzylpenicillin)
- _____ use only (IV)
- narrow spectrum (gram _____ and some gram _____)
- _____
- susceptible to _____
- administration: IM; IV (but not oral)
- -not used routinely for out-patients
- -emergency Rx: IV for ludwigs angina
parenteral positive negative bactericidal beta lactamase
penicillins ADRx -incidence less frequent --\_\_\_\_\_ (\_\_\_\_\_, rash) -candidiasis (oral and vaginal) exfoliative dermatitis (red, scaly skin) --GI reactions: ---loss of taste and apetite ---mild diarrhea; nausea and vomiting
- incidence rare
- -clostridium difficile
- –_____
- -mental disturbances
- leukopenia (fever)
- thrombocytopenia (unusual bleeding or bruising)
- -seizures (very high close and renal impairment)
allergy
anaphylaxis
pseudomembranous colitis
penicillin allergy
- all penicillins are cross sensitizing and cross reacting although many are non toxic
- antigens are degradation products
- > 95% of fatal reactions occur within _____
60 mins
penicillins- drug interactions
- _____: ______renal tubular secretion of penicillin, thus used therapeutically for ______serum concentration
- _____ (gentamicin) - inactivation
- _____: hepatic enzyme induction CYP 450, thus failure of OC and pregnancy
- combination use with other antibiotics
probenecid decerease increase aminoglycosides oral contraceptives
aminopenicillins
- _____, _____, _____
- effective against: gram _____ cocci, gram _____ cocci such as Neisseria g and m and gram negative rods such as hemophilus and E. coli
- not resistant to _____
- _______spectrum
- used for uncomplicated ENT infections and component of triple therapy for H pylori
- ________: better oral absorption; can be taken with food, less adverse effects than ampicillin
ampicillin amoxicillin bacampicillin positive negative beta lactams extended H pylori amoxicillin
betalactamases: penicillinase
- an enzyme produced by some bacteria
- -_____ and _____ are ineffective against these bacteria
- -the enzyme degrades or inactivates these antibiotics
- -two strategies to overcome these resistant bacteria
- –use penicillins that are resistant to the enzyme (_____)
- –use _____ and _____ combination
- –_____
penicillin V amoxicillin cloxacillin amoxicillin clavulanic acid augmentin
penicillin and beta lactamase inhibitor
- amoxicillin and clavulanate (augmentin)
- -clavulanic acid (cluvalanate) inhibits _____
- -molecular structure is similar to _____
- -effective against staph aureus, H influenza, N gonorrhea, salmonella and E coli
- -used in immunocompromised patients with mixed infections
beta lactamase
beta lactam
cephalosporins
- similar structure to _____ except a _____ membered ring instead of _____ in penicillin
- stable against _____
- possess 7-aminocephalosporanic acid ring instead of 6-aminopenicillanic acid
- 4 generations
penicillins
6
5
beta lactamases
cephalosporins
-1st generation destroyed by beta lactamases
–_____, _____: streptococci, pneumonocci and staph
–used for UTI and soft tissue abscess
–drug of choice for
_______ prophylaxis
- 2nd generation more resistance to lactamases: _____ and _____
- -effective against all bacteria of first generation plus gram _____ (klebsiella, H influenza)
- -_____: used to treat sinusitis, otitis and lower respiratory tract infections
cephalexin cefazolin surgical cefuroxime cefoxitin negative cefuroxime (entire respiratory tract)
third and fourth generation
- third generation: _____, _____
- -expanded gram _____ coverage with resistance to _____
- -able to cross _____
- -used in _____ caused by pneumocci, meningococci and h influenza
- -sepsis in immunocompromised patients
- fourth generation: _____: highly active against Neisseria, H influenza, P aeruginosa
- -not approved for the treatment of _____
cefotaxime ceftriaxone negative beta lactamases blood brain barrier meningitis cefepime meningitis
fifth generation
- ______ is distinct in being active against MDR staph aureus, methicillin resistant (MRSA), vancomycin resistant staph aureus
- approved by the FDA for _________ skin infections and pneumonia
- _____
- -approval from the US food and drug administration (2010) for the treatment of community-acquired _____ and acute bacterial _____ infections
ceftaroline community acquired teflaro bacterial pneumonia skin
cephalosporins: adverse effects
- similar to penicillins
- -_______ reactions; GI
- allergic reactions have penicillin cross- sensitivity
- toxicity: local irritation after IM injection and _____ after IV injection
- _____: nephritis and tubular necrosis
- have been known to cause _____ and _____ disorders in some
allergic thrombophlebitis renal toxicity hypothrombinemia bleeding
