A.bac: DNA Syn inhibitors and Folate inhibitors Flashcards
DNA Synthesis inhibitors
Folate Inhibitors
Dna: Fq,Quinolones, Metronidazole
Folate: Sulfonamides, Trimethoprim
MOA of FQ/Q
DNA gyrase inhibitor (topoisomerase II) and topoisomerase IV: makes cell inaccessible and leads to cell death.
Nalidixic acid (urinary disinfectant)
Different quinolones inhibits different extent of topoisomerase II and IV
Fq are indicated for?
Cipro, Levo, Moxi dosage forms.
PO and IV
FQ drug generations
1st: Nalidixic acid, Norflox- least acty to +-ve
2nd: Oflax, Cipro- most eff. for -ve
3rd: Levoflox (respiratory), both Gati Moxi improved for +ve
4th: Travoflox, basiflox
Grams for Gyrase and Topo.
Nalidixic
DNA gyrase seems more important in gram –ve. Topoisomerase IV in gram +ve. Nalidixic acid is primarily against gram -ve
Q chelation
Quinolones chelate with polyvalent ions such as Fe, Al, Mg, Ca to form less water-soluble and complexes and thus decrease considerable potency.
FQ and Qs are CI in children, less than 18 year, pregnant women due to its?
Cartilage erosion
Fluroquinolone increase INR in patient receiving warfarin, therefore monitor?
Fluroquinolones can cause hypo or hyperglycemia, therefore monitor?
prothrombin time (PT) blood sugar levels in diabetic patient
Fluroquinolones at higher alkaline pH can cause?
Cipro is the drug of choice.
The only Quinolone that is taken empty stomach?
crystalluria
travelers diarrhea
norfloxacin (*no food)
Metronidazole drug, classification, MOA
Nitroimidazole class - as an anti protozoal antibiotic
Inhibit nucleic acid synthesis by disrupting DNA of microbial cells.
Metronidazole is effective against
C. difficle, B. fragilis, amebia, C. vaginalis (bacterial vaginitis), Giardiasis, trichomonas, H. pylori, and P.colitis
Metro inhibits CYP2C9 which will interact to drugs metabolized by this enzyme.
Warfarin, Lomitapide
*metro will discolor urine and CI in preg
Sulfa drugs MOA
inhibit synthesis of dihydropteroic acid
Folate antagonist sulfa drugs (Cotrimoxazole) MOA on DNA synthesis
Dihydroteroate diphosphate + PABA DHP synthase ⬇️ ✖️sulfonamides dihydroteroic acid ➡️ dihydrofolic acid DHF reductase⬇️ ✖️Trimethoprim tetrahydrofolic acid ➡️ thymidine ➡️ DNA
A 22-year-old patient currently using cotrimoxazole for UTI, reported sever blisters on mucus membrane, and eyes. What are the possible reactions?
Stevens Johnson Syndrome, it is a hypersensitive reaction of sulfadrugs.