chemotherapy part 1 (4) Flashcards
sulfonamides: sulfamethoxazole
- bacteria manufacture their own _____
- sulfonamides inhibit _____ synthesis
- sulfonamides resemble _____ as structural analogues
- resistance may occur:
- -increase synthesis of _____
- -alter _____ structure
- -reduce _____ uptake
- clinical uses:
- -systemic: UTI
- -topical: conjunctivitis, corneal ulcer
folic acid folic acid PABA PABA enzyme sulfonamide
sulfonamides: adverse effects
- blood dyscrasias
- _____
- _____ syndrome
- allergy- metabolite (PABA)
- renal damage from _____
-hallmark symptom of stevens-johnson syndrome: _____ lesion
photosensitivity
stevens-johnson
crystalluria
bulls eye
trimethoprim
- 40,000 times greater affinity for bacterial DHFR
- minimal effects on mammalian cells
- _____ and _____ (1:5 ratio) act in concert with each other
- brand names: bactrim, septra, cotrim, co-trimoxazole
- resistance:
- -increase synthesis of _____ (DHFR)
- -reduce _____ to trimethoprim
trimethoprim
sufamethoxazole
enzyme
permeability
nucleic acid synthesis inhibitors
- fluoroquinolones
- -ciprofloxacin
- -levofloxacin
- -gatifloxacin
- -moxifloxacin
- -ofloxacin
- -norfloxacin
- FDA: black box warnings on all fluoroquinolones/ increased risk of _____ damage
- 2016: disabling and potentially permanent serious side effects can involve the tendons, muscles, joints, nerves, and central nervous system, low blood sugar and mental health problems were added in 2018
tendon
fluoroquinolones
- ciprofloxacin, norfoxacin, levofloxacin
- -mechanism of action
- – inhibits bacterial _____
- —DNA gyrase converts closed circular DNA into _____ configuration
- –prevents _____, stops _____
- -resistance:
- alteration of _____
- decrease _____
DNA gyrase supercoiled supercoiling DNA replication DNA gyrase permeability
fluoroquinolones
- ciprofloxacin
- -_____ spectrum
- –most _____ gram _____ and some gram _____
- –_____
- -adverse effects, mild (relative)
- –GI upset: nausea vomiting diarrhea
- -CNS: _____, _____, _____
- -children: _____ damage
- -not used in children under 18 year old
- -not used in elderly patients/ _____
broad aerobic negative positive bactericidal dizziness headaches confusion cartilage tendonitis
metronidazole (flagyl)
- chemically reduced to a _____ metabolite
- -this reaction is unique to _____ bacteria
- toxic metabolite interacts with _____
- results in loss of _____ structure, strand breakage and resultant inhibition of nucleic acid synthesis and _____
- _____
toxic anaerobic DNA helical cell death bactericidal
metronidazole
-adverse effects:
–CNS disturbances, dizziness, lightheadedness
-GI disturbances: abdominal pain and cramps; nausea and vomiting; diarrhea
-taste: changes in _____, sharp _____ taste
-dry mouth, dark urine
seizures (high doses)
-_____ like reaction
sensation
metallic
disulfiram
metronidazole drug interactions
- _____: disulfiram-like reaction: nausea, giddiness, flushing, abdominal cramps; accumulation of _____
- this results due to the non conversion of _____
- disulfiram- confusion psychotic reactions, convulsions; 2 week washout period recommended
- _____: inhibit metabolism; increase plasma levels; monitor _____ time
- barbiturates- decrease metronidazole effect
- phenytoin: phenytoin toxicity
alcohol acetaldehyde acetaldehyde anticoagulants prothrombin
vancomycin
- mechanism of action
- -acts by binding to _____ strand of cell wall and preventing further growth
- effective against _____
- pharmacokinetics
- -not absorbed from the GI
- -excreted unchanged via the kidneys
- clinical uses
- -oral, for serious GI infection
- -slow infusion, serious systemic infection
- -_____ injection: _____ syndrome
peptidoglycan
MRSA
bolus IV
red man
aminoglycosides
- _____ is a prototype drug
- gentamicin, tobramycin, amikacin
- bind to _____ subunit and inhibit protein synthesis
- virtually the same spectrum as _____ plus enterococci
- used for sepsis, pneumonia
- given only _____, at low cost ($3 a day)
- drug monitoring required
- hardest drug to dose
streptomycin
30S
flurorquinolones
IV
aminoglycosides side effects
- _____ toxicity (irreversible) loss of _____, _____ and _____ (ototoxic)
- _____ toxicity (reversible) monitor _____ (nephrotoxic)
- neuromuscular blockade can occur during surgery because aminoglycosides have an additive effect with paralyzing agents
- adding furosemide or other nephrotoxic drugs increases risk of renal damage
- can also happen if patient is given an overdose
vestibular balance hearing dizziness renal creatinine
super bugs
- MRSA: methicillin resistant staph aureus
- -isolate patient and wash hands!!
- -Rx: _____ 1g IV q12h
- -resistant to all _____ and _____
vancomycin
penicillins
cephalosporins
super bugs
- VRE (vancomycin resistant enterococci)
- -infects immunocompromised patients
- -routine identification procedures in critical care areas with _____ of colonized patients
isolation
future directions
- _____: FDA 1999
- -mix of dalfoprastin (GpA) and quinupristin (GpB)
- -used for vancomycin resistant strep pyogenes
- -50S binding: combination provides potency
- -_____: FDA 2000 linezolid
- -gram positive including MRSA/VRE
- 50S binding along with binding to the tRNA
- _____: FDA 2007: retapamulin
- -topical therapy for bacterial infections
- -bind to 50S
streptogramins
oxazolidinones
pleuromutilins
