5- Antimicrobial Agents Flashcards
Antibiotics acting through Inhibition of cell wall synthesis ?
Penicillins Cephalosporins Imipenem/Meropenem Aztreonam Vancomycin
Antibiotics acting through inhibition of bacterial protein synthesis ?
Aminoglycosides Chloramphenicol Macrolides Tetracyclines Streptogramines Linezolid Clindamycin
Antibiotics acting through inhibition of nucleic synthesis ?
Fluoroquinolones
Rifampin
Antibiotics acting through inhibition of folic acid synthesis ?
Sulfonamides
Trimethoprim
Pyrimethamine
Narrow spectrum penicillins ? Their spectrum ?
Penicillin G
Penicillin V
Streptococci
Pneumococci
Meningococci
Treponema pallidum
Very narrow spectrum penicillins ? Their spectrum ?
Nafcillin
Oxacillin
Methicillin
Staphylococci
Broad spectrum penicillins ? Their spectrum ?
Amoxicillin
Ampicillin
Both : gram +ve cocci except staph , E coli , H influenza
Ampicillin : listeria monocytogenes
Amoxicillin : borrelia , H pylori
Extended spectrum penicillins ? Their spectrum ?
Ticarcillin
Piperacillin
Increased activity against gram -ve rods including Pseudomonas
Examples for suicide inhibitors ?
Clavulanic acid
Sulbactam
Aminoglycosides with ticarcillin synergistic against ?
Pseudomonas
Aminoglycosides with amoxicillin synergistic against ?
Enterococcal species
Nafcillin and oxacillin eliminated largely in ?
Bile
Firist generation cephalosporins ? Their spectrum ? Use ?
Cefazolin
Cephalexin
Gram +ve cocci ( not MRSA )
E coli
Klebsiella pneumoniae
Some proteus species
In surgical prophylaxis
Second generation cephalosporins ? Their spectrum ?
Cefotetan
Cefaclor
Cefuroxime
Increased gram -ve coverage including some anaerobes
Third generation cephalosporins ? Their spectrum ? Use ?
Ceftriaxone IM
Cefotaxime parenteral
Cefdinir
Cefixime oral
Gram +ve and gram -ve cocci
Many gram -ve rods
Important in empiric management of meningitis and sepsis
Fourth generation cephalosporins? Spectrum ?
Cefepime IV
Wider than third generation
Organisms not covered by cephalosporins?
LAME Listeria monocytogenes Atypicals ( Chlamydia) MRSA Enterococci
Tubular secretion of penicillins and cephalosporins is blocked by ?
Probenecid
In case of allergy to penicillins what drugs to choose to combat bacteria ?
For gram +ve organisms : Macrolides
For gram -ve rods : aztreonam
Imipenem and Meropenem spectrum ?
Gram +ve cocci
Gram -ve rods
Anaerobes
Imipenem is given with ? Why ?
Cilastatin
a renal dehydropeptidase inhibitor which inhibits imipenem metabolism to a nephrotoxic metabolite
Aztreonam spectrum ? Mode of administration ?
Gram -ve rods
IV
Vancomycin spectrum ?
MRSA
Enterococci
Clostridium difficile
Streptomycin is the DOC for ?
Bubonic plague
Tularemia
Antibiotics not used in pregnancy?
Aminoglycosides
Fluoroquinolones
Sulfonamides
Tetracyclines
Doxycycline is useful in ttt of ?
Prostatitis
Minocyclin is used in ?
Meningococcal carrier state
Tigecyclin is used in ?
Complicated skin , soft tissue and intestinal infections
Antibiotics that causes phototoxicity ?
Tetracyclines
Sulfonamides
Quinolones
Chloramphenicol is metabolized by ?
Hepatic glucuronidation
Macrolides spectrum ?
Gram +ve cocci Atypical organisms Legionella pneumophila Campylobacter jejuni Helicobacter pylori Mycobacterium avium intracellulare
Telithromycin ?
A ketolide active against macrolide resistant S. Pneumonia
Clindamycin spectrum ?
Gram +ve
Anaerobes
Clindamycin side effect ?
Pseudomembranous colitis
Linezolid uses ?
Ttt of :
VRSA
VRE
Drug resistant pneumococci
Side effects of linezolid ?
Bone marrow suppression
MOA-a and b inhibitor
Streptogramins ?
Dalfopristin
Quinupristin
Spectrum of streptogramins ?
VRSA
VRE
Drug resistant gram +ve cocci
Sulfonamides inhibit ?
Dihydropteroate synthase
Inhibitors of dihydrofolate reductase ?
Trimethoprim
Pyrimethamine
DOC in Nocardia ?
Cotrimoxazole
Sulfonamides are metabolized by ?
Hepatic acetylation
Mechanism of action of Amphotericin B and nystatin ? Their uses ?
Interact with ergosterol in fungal membranes to form artificial pores which disrupts membrane permeability
Amphotericin B : DOC for severe infections caused by cryptococcus and mucor
Nystatin : used topically for localized infections ( candidiasis )
Mechanism of action of Azoles ?
Inhibit 14-alpha demethylase
Itraconazole is DOC for ?
Blastomycoses
Sporotrichoses
Aspergillosis
Flucytosine mechanism of action ?
Activated by fungal cytosine deaminase to 5-fluorouracil which after triphosphorylation is incorporated into fungal RNA
5-FU also forms 5-fluorodeoxyuridine monophosphate which inhibits thymidylate synthase
Mechanism of action of Acyclovir ?
Monophosphorylated by viral thymidine kinase to acyclovir triphosphate which is both a substrate for and inhibitor of viral DNA polymerase
When incorporated into the DNA molecule acts as a chain terminator
Ganciclovir uses ? Side effects ?
Mostly used in prophylaxis and ttt of CMV infections including retinitis in AIDS and transplant patients
Hematotoxicity Mucositis Fever Rash Crystalluria
Foscarnet side effects ?
Nephrotoxicity with acute tubular necrosis , electrolyte imbalance with hypocalcemia
Side effects of Zidovudine?
Hematotoxicity
Myopathy
Peripheral neuropathy
Side effects of Didanosine ?
Pancreatitis
Peripheral neuropathy
Hyperuricemia
Liver dysfunction
Side effect of protease inhibitors ?
Metabolic syndrome
Side effect of Ritonavir ?
Induces CYP 1A2 and inhibit the major P450 isoforms ( 3A4 , 2D6 )
Integrase inhibitor ?
Raltegravir
Fusion inhibitors ?
Enfuvirtide
Maraviroc
MOA of Enfuvirtide?
Binds to gp41 and inhibits the fusion HIV-1 to CD4+ cells
MOA of Maraviroc ?
Blocks the binding of the gp120 HIV protein to CCR5 on macrophage surface to prevent viral entry
MOA of Zanamivir and Oseltamivir ?
Inhibit neuraminidases of influenza A and B —> decreases the likelihood that the virus will penetrate uninfected cells
Ribavorin MOA ?
Monophosphorylated form inhibits IMP dehydrogenase
Triphosphorylated form inhibits viral RNA polymerase and end-capping of viral RNA
Uses of Ribavirin ?
Adjunct to alpha interferons in hepatitis C
Respiratory syncytial virus
Lassa fever
Hantavirus
Side effects of Ribavirin ?
Hematotoxic
Upper airway irritation
Teratogenic
Sofosbuvir MOA ?
Nucleotide analog that inhibits RNA polymerase
Simeprevir MOA ?
Hepatitis C protease inhibitor
Ledipasvir MOA ? Combined with ?
Inhibits HCV NS5A protein that play a key role in RNA replication
Combined with Sofosbuvir
DOC for lechmaniasis ?
Stibogluconate
DOC for Trypanosomiasis ?
Chagas disease : Nifurtimox
African : Arsenicals
Side effects of metronidazole ?
Metallic taste
Disulfiram like action
Ttt of malaria in chloroquine resistant regions ?
Quinine +- ( doxycycline or clindamycin or pyrimethamine)
MOA of albendazole ?
Decrease glucose uptake
Decrease microtubular structure
MOA of praziquantel?
Increase Ca influx
Increase vacuolization