Pharm II MOAs Flashcards
Sulfonamide MOA?
PABA agonist inhibiting folic acid synthesis
Diaminopyrimidines MOA?
Folic acid inhibitor. Reversibly binds and inhibits dihydrofolate reducatase enzyme.
Sulfonamides and Diaminopyrimidines are static or cidal?
Static
Beta-Lactam MOA?
Inhibits bacterial cell wall synthesis via transpeptidase enzyme inhibition
Beta-lactam resistance achieved by?
- Production of b-lactamase enzyme. 2. Permeability of cell wall decreased (gram -). 3. Reduced sensitivity of penicillin binding protein.
30S ribosomal subunit protein synthesis inhibitors?
Aminoglycosides, Tetracyclines
50s Ribosomal subunit protein synthesis inhibitors?
- Macrolides, 2. Lincosamides, 3. Chloramphenicol derivatives
All protein synthesis inhibitors are bacteriostatic except?
Aminoglycosides
MOA of Flouroquinolones and Metronidazole MOA?
DNA inhibitors
MOA of Rifampin
RNA inhibitor
MOA of Bacitracin
Inhibits peptidoglican synthesis in bacteria by non-specifically blocking phosphorylase reactions
MOA of Nitrofurans
Inhibits energy production
MOA of Virginamycin
Protein synthesis inhibitor via 23S ribosomal subunit
Antimicrobials interfering with cell membrane?
Polymyxin B, Colistin (poly E)
MOA Benzimidazoles?
Irreversibly binds to nematodal tubulin, specifically beta-tubulin
Levamisole MOA?
Ganlionic stimulant and direct cholinergic drug. Causes paralysis. Can also act as an immune stimulant at low intermittent dosage.
Depolarizing neuromuscular blocking agents?
Pyrantel, Morantel, Epsiprantel
Organophosphate compounds MOA?
Irreversible inhibition of acetylcholinesterase
Macrocyclic Lactones MOA?
- Bind selectively with high affinity to glutamate-gated chloride channels. 2. Increases release of GABA from nervous system. 3. Affects egg formation and causes sterility.
Praziquantel MOA?
Ca2+ ion flux across surface membranes of exposed parasite-> paralysis, surface swellings, lesions -> lyse
Rafoxanide / Closantel MOA?
ATP production inhibition.
Clorsulon MOA
Affects glycolytic enzymes and deprives the fluke of its main source of metabolic energy
Nitromidazole / Nitrofurans MOA?
Nitro group is cleaved off -> produces unstable intermediates -> DNA destruction
Polyether ionophor MOA?
Lipophilic complexes with alkali metals -> change membrane integrity/ internal osmolality
Arsenieals MOA?
Binds to disulphide bridges inhibiting enzyme systems
Thiamine analog MOA?
Analogue of thiamine -> inhibition of active thiamine transport to protozoa
Thiazine derivatives MOA?
Act on apicoplasts
Organophosphates MOA
Irreversible inhibition of Ache
Carbomates MOA?
Reversible inhibition of Ache
Pyrethrins/Pyrethroids MOA?
Interacts with Na channels in membrane
Fipronil MOA
GABA and Glutamate Cl ion channel blockers
Imidacloprid MOA?
Competitive inhibition of post=synaptic nicotiic receptor (nAChe)
Amitraz MOA?
Inhibition of monoamino exidase
IGRs and IDIs MOA?
Mimic juvenile hormone resp. inhibition of chitin synthesis
Where do anti-fungals act?
Wall, Membrane, intracellular
Intracellular anti-fungals and their MOAs?
Flucytosine - pyrimidine analogue: DNA synthesis interference via thymidylate synthesis. Griseofulvin - Mitotic inhibitor: Interferes with mitosis by binding to microtubules
Wall anti-fungal and MOAs?
Echinocandins - Inhibits fungal beta glucan synthesis -> exposure of antigens -> host immune response
Anti-fungal acting on cell membrane and MOA? (hint: ergosterol)
Polyenes - Form pores in funcal membrane by binding to ergosterol -> electrolyte imbalance. Azoles - Selectively blocks ergosterol synthesis by inhibiting demethylation of lanosterol -> ergosterol. Allylamines - inhibits squalene epoxidase to block ergos