DNA SYNTHESIS INHIBITOR Flashcards
4 classifications of quinolones and give examples
1st generation (Norfloxacin) 2nd generation (Ciprofloxacine, Ofloxacine) 3rd generation (Levofloxacine, Sparfloxacine) 4th generation (Gemifloxacine, Moxifloxacine)
Fluoroquinolones are eliminated by?
Renal mechanism which are tubular secretion or glomerular filtration
Mechanism of action
6 steps
- DNA gyrase (topoisomerase II) nikes double- stranded DNA, relaxes supercoils
- Topoisomerase IV bikes and unlinks DNA for following DNA replication
- Quinolones block bacterial DNA synthesis by inhibiting bacteria DNA gyrase and topoisomerase IV
- Inhibition of DNA Gyrase, prevents relaxation of positively supercoiled DNA (required for normal transcription and replication)
- Inhibition of topoisomerase IV interferes with separation of replicated chromosomal DNA into respective daughter cells during cell division
- And Block bacterial DNA synthesis .
:)
Antibacterial spectrum consists of?
Gram negative ( E.coli, salmonella shigella and more )
Gram positive ( cocci)
Other ( Atypical pneumonia, mycobacteria and anaerobes)
Indications ( clinical use)
- UTI (E.coli)
- Enteric Fever ( salmonella)
- ‘Bacillary Dysentery (shigella)
- Gonorrhea (neisseria)
Gram positive Cocci
- Skin and soft tissue infection
- Bones and joint infections
- Prophylaxis and treatment of Anthrax (bacillus anthrax)
- Gram negative septicemia
- Upper (gram +) & lower(gram -) respiratory tract infections
Adverse Effect
Give as much as you remember :/
GIT upset ( Nausea, Vomiting, diarrhea)
Rash, photosensitivity
Arthopathy: Children(< 3 years)
Tendonitis & rupture tendon: athletes
Haemolysis ( G6PD deficiency patient)
What’s Antimetabolite?
:)
- drug that through chemical similarity is able to interfere with role of an endogenous compound in cellular metabolism
Mechanism of action of Antimetabolite/sulphonamides ? :|
- Sulphoamides are structurally similar to PABA
- Drug inhibits dihydropteroate synthase enzyme that normally converts PABA to dihydrofolic acid
- Trimethoprim act at the subsequent stage and inhibit dihydrofolate Reductase enzyme which converts dihydrofolate to tetrahydrofolate
- And inhibit Bacterial DNA synthesis
Indication of use of Antimetabolite
Oral and IV
UTI
Pneuomocystitis carinii infection
Pneumonia
Toxoplasmosis
In chloroquine resistant malaria ( sulphonamide combination)
What do you know about Co-Trimoxazole? ■_■
- bactericidal drug
- mechanism of action = Sulfonamide
- inhibits subsequent steps of DNA synthesis
- produces chemotherapeutic Potentiation
- has more antimicrobial activity than Sulfanomides
- can be given orally and parenterally
Almost there buddy! :)
Adverse effects of Antimetabolite? O_o
Allergic Disorder
Stomatitis
Hepatitis
Renal disorder ( crystalluria, haematuria,anuria)
Haemopoietic disturbance ( hemolytic anemia in patients who G6PD deficiency when given sulphanomides)
Fighthing!! <3
Adverse effects of Antimetabolite? O_o
Allergic Disorder
Stomatitis
Hepatitis
Renal disorder ( crystalluria, haematuria,anuria)
Haemopoietic disturbance ( hemolytic anemia in patients who G6PD deficiency when given sulphanomides)
Fighthing!! <3