ANTI INFECTIVE DRUGS Flashcards
Common illnesses due to action of bacteria, fungi, parasites and viruses
Infection wherein a patient does not show any positive signs or symptoms of infection
Most important therapeutic evaluation for designing a therapeutic plan
Type of therapy wherein the physician prescribes the possible, most potent drug available, hoping that it would hit the causative agent
Agents that work against the common metabolic pathway required for survival of pathogenic cells
Antibacterial agents that slow down or inhibit the growth of pathogenic cell
Antibacterial agents that kill the pathogenic cell
First marketed agents in the form of sulfanilamides
Discovered by Domagk from protonsil (azo dye)
MOA: inhibits dihydropteroate synthase from adding PABA to folic acid precursor
PABA meaning
Used for toxoplasmosis, UTI and pyrimethamine
SAR: sulfonamide N is attached to H for similar pKa as PABA
SAR: no other ring substitutions
SAR: aromatic N4 is required for activity
SAR: N1 acetylation = prodrug, must hydrolyze in gut
Usually taken together with sulfomethoxazole
SAR: inhibits dihydrofolate reductase, preventing conversion of dihydrofolic acid to tetrahydrofolic acid
Use: UTI
SAR: serves as analog of dihydrofolic acid
Active form of dihydrofolic acid
Derived from nalidixic acid (1st generation)
MOA: inhibits DNA gyrase and topoisomerase IV used for DNA replication
Use: UTI, STDs, respiratory tract infection (RTI), bone infection
SAR of quinolone is (dependent/independent) on substitution
SAR: COOH and ketone binds to the gyrase (most important component)
SAR: R1 for potency; must be ethyl or cyclopropyl
SAR: C6-F improves penetration of bacterial cell wall
SAR: C7-heterocyclic substitution increase gram (-) activity
SAR: R8 affects activity especially when fused with R1
Should not be taken with metal-containing preparations as it could cause precipitation; sometimes causes phototoxicity