Quinolones, Folic acid antagonists and Urinary antiseptics Flashcards
Fluoroquinolone targets _________ in Gram negatives and _________ in Gram positive bacteria
DNA gyrase, topoisomerase IV
Name 3 fluoroquinolones
ciprofloxacin, levofloxacin, moxifloxacin
Fluroquinolones should be administered at least _________ hours before consumption of dairy products or substances that contain divalent cations
2 hours
Best on empty stomach
- just like tetracycline
Indications for fluroquinolones
Ciprofloxacin (2nd gen)
- gram -ve & enteric coliforms (GNR)
- traveller’s diarrhoea (e coli)/food pois (salmo)
- X UTI, MRSA (resistance)
- prostatitis (high [ ] in prostatic tissue)
Levo & moxifloxacin– Gram +ve & atypicals
Name the two respiratory quinolones
Levofloxacin and moxifloxacin
Name at least 3 adverse effects associated with the use of fluroquinolones.
- Phototoxicity
- Tendinitis or tendon rupture
- Prolong QT interval
- Peripheral Neuropathy
- GI distress– CDAD
- Arthropathy
Which antibiotics are known to cause phototoxicity?
Tetracyclines, fluoroquinolones
Fluoroquinolones are contraindicated in _________
- Children < 18 years old
- Pregnant/Lactating women
- Myasthenia gravis pt
Name 3 folate synthesis inhibitors
Sulfonamides (sulfamethoxazole), trimethoprim, cotrimoxazole
Folic acid is vitamin B9 that is needed in humans to produce healthy ___________
red blood cells
Which enzyme does sulfonamide inhibit?
Dihydropteroate synthase (thus humans aren’t affected)
Which enzyme does trimethoprim inhibit?
Dihydrofolate reductase
decrease tetrahydrof acid–> aa, purine, thymidine
Cotrimoxazole is a combination of which 2 antibiotics, and in what ratio?
Trimethoprim and sulfamethoxazole, 1:5 respectively
Combination of sulfonamide & trimethoprim has _______ effect
synergistic
bactericidal as block tetrahydrofolate pathway
**Sulfonamides are only effective in bacteria that synthesize their own __________?
folic acid
Sulfonamides can cause nephrotoxicity as a result of __________?
crystalluria
sulfonamide acetylated & conj in liver - retains toxicity to ppt at neutral/acidic pH
Trimethoprim can cause __________ deficiency in humans
folic acid deficiency–> megaloblastic anemia, leukopenia, thrombocytopenia
AVOID in 1st & 3rd trimester pregnancy
Usage of sulfonamides in last trimester can cause __________ in newborns
kernicterus
G6PD deficient patients using sulfonamides can suffer from __________
hemolytic anemia
Adverse effects of sulfonamides
- Hemolytic anaemia in G6PD deficient pt
- Crystalluria (cloudy urine)– nephrotoxicty: can alkalinise urine or hydration
- Kernicterus newborns: drug taken late in preg
- Hypersensitivity
Folic acid deficiency caused by trimethoprim can be managed by giving the patients _____________ .
Folinic acid (does not take part in pathway but is interchangeable conversion to tetrahydrf)
Name at LEAST two indications for cotrimoxazole
- Uncomplicated UTI
- Pneumocystis pneumonia (Pneumocystis jiroveci)
- MRSA
? meningitis as good CSF penetration/ cross BBB
Name at LEAST 3 adverse effects related to the use of cotrimoxazole
other than that of sulf & trimethoprim
- Glossitis
- Rash
What’s a urinary antiseptic agent?
Nitrofurantoin
What is nitrofurantoin’s mechanism of action?
It is converted by the bacteria to a *highly active intermediate, which disrupts the synthesis of DNA, RNA and metabolic processes.
Nitrofurantoin is effective in treatment of _________ .
lower UTI
- E coli
- Enterococci
X Pseudomonas, proteus, klebsiella, enterobacter
How is nitrofurantoin cleared?
Renal clearance
rapidly absorbed & rapidly cleared to urine
Nitrofurantoin can cause urine colour to turn _________ .
brown
** tell pt otherwise think it’s blood
Adverse effects of nitrofurantoin
- in elderly *pulm toxicity, peripheral neuropathies (rare) –> consider instead cotrimoxazole
- GI symptoms– use microcrystalline
- X GP6D Def
- Chol jaundice/hepatocellular damage w nitro-redu metab producing free radicals (rare)
G6PD deficient patients using nitrofurantoin are susceptible to ___________ .
Hematologic disturbances such as hemolytic anemia, leukopenia
What is G6PD, and why is it important in red blood cells?
The glucose-6-phosphate dehydrogenase (G6PD) enzyme is the central factor of the antioxidant defense system in red blood cells, which helps maintain high levels of reduced glutathione (GSH) and nicotine adenine dinucleotide phosphate (NADPH), to protect the RBC from oxidative damage caused by reactive oxygen species.
Name 3 groups of patients in whom nitrofurantoin may be contraindicated.
- Patients with impaired renal function
- Pregnant women (at term > 37 weeks)
- Infants <1 mth of age
What would be examples of recommended treatment options for simple UTI in healthy women of reproductive age?
- Cotrimoxazole
2. Nitrofurantoin
Upper UTI
- IV ceftriaxone
Tx atypicals
- tetracycline
- macrolides (pregnant pt)
- fluoroquinolones