VII - Topnotch Pharma Flash Cards - Chemotherapeutic Drugs
Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls
Penicillin, Cephalosporins (TOPNOTCH)
DOC for syphillis, for streptococcal, meningococcal, G+ bacilli, spirochete infection
Natural Penicillins: Penicillin G, Penicillin V (narrow spectrum penicillin) (TOPNOTCH)
For staphylococcal infections
Anti-Staphylococcal Penicillins: Methicillin, nafcillin, oxacillin, cloxacillin (very narrow spectrum) (TOPNOTCH)
all penicillins are excreted unchanged in the urine EXCEPT for _____which is excreted in the bile
Nafcillin (TOPNOTCH)
Pens For enterococci, Listeria, E. coli, Proteus, H. influenza, Moraxella
Extended Spectrum Penicillin: Ampicillin, Amoxicillin (TOPNOTCH)
Pens For Pseudomonas, Enterobacter, Klebsiella
Antipseudomonal Penicillin: Piperacillin, ticarcillin, carbenicillin (TOPNOTCH)
all Cephs have renal excretion EXCEPT ______
Cefoperazone and Ceftriaxone (TOPNOTCH)
Cephs for For surgical prophylaxis, bone infections, infections due to staph and strep, E. coli, Klebsiella, G+ cocci
First Generation Cephs (TOPNOTCH)
Increases nephrotoxicity of aminoglycosides
Cephs (TOPNOTCH)
For surgical prophylaxis, bone infections, infections due to staph strep and E. coli, Enterobacter, Neisseria, infections against anaerobes (Bacteroides), sinus ear and respiratory infections by Klebsiella andHemophilus
Second Generation Cephs (TOPNOTCH)
Second Generation Cephs
Cefamandole, cefaclor, cefonicid, cefuroxime, cefprozil, loracarbef, ceforanide, cefoxitin, cefmetazole, cefotetan (TOPNOTCH)
First Generation Cephs
Cefazolin, cefadroxil, cephalothin, cephapirin, cephradine, cephalexin (TOPNOTCH)
Cephs with slight less activity against G+ but extended G- activity
Second Generation Cephs (TOPNOTCH)
decreased gram + coverage, increased gram - activity (pseudomonas, bacteroides), against Providencia, Serratia, Neiserria, Haemophilus ; DOC for gonorrhea
Third Generation Cephs (TOPNOTCH)
DOC for gonorrhea
Ceftriaxone and Cefixime (TOPNOTCH)
Third Generation Cephs
Cefoperazone, cefotaxime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, ceftibuten (TOPNOTCH)
all can Third gen Cephs can penetrate the BBB EXCEPT _____
Cefoperazone and Cefixime (TOPNOTCH)
More resistant to beta-lactamase produced by Enterobacter, Haemophilus, Neisseria and Pneumococcal
Fourth Generation Cephs (TOPNOTCH)
Fourth Generation Cephs
Cefipime (TOPNOTCH)
Binds to penicillin-binding proteins, inhibits transpeptidation in bacterial cell walls, wide coverage against gram + gram - bacteria and anaerobes ; For infections resistant to other antibiotics EXCEPT MRSA, DOC for Enterobacter, Citrobacter and Serratia
Carbapenems (TOPNOTCH)
Carbapenems
Imipenem-cilastatin , ertapenem, meropenem (TOPNOTCH)
Imipenem given with Cilastatin which acts as ______
Dehydropeptidase enzyme inhibitor (TOPNOTCH)
Monobactam
Aztreonam (TOPNOTCH)
Resistant to beta-lactamase, no activity against gram + bacteria or anaerobes
Aztreonam (TOPNOTCH)
No cross-allergenicity with Pens
Aztreonam (TOPNOTCH)
Inhibits inactivation of penicillins by bacterial beta-lactamase (penicillinase)
Beta-Lactamase Inhibitors (TOPNOTCH)
Beta-Lactamase Inhibitors
Clavulanic acid , sulbactam, tazobactam (TOPNOTCH)
Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan –> inhibit transglycosylation –> prevent elongation and cross-linking of peptidoglycan chain
Glycopeptides: Vancomycin, teicoplanin, telavancin (TOPNOTCH)
For MRSA, PRSP, as alternative for pseudomembranous colitis
Vancomycin (TOPNOTCH)
SE: red man syndrome, nephrotoxicity, ototoxicity, chills, fever, phlebitis
Vancomycin (TOPNOTCH)
Interferes with a late stage in cell wall synthesis in gram + organisms ; For gram + bacteria
Bacitracin (TOPNOTCH)
Reserved for topical use only due to marked nephrotoxicity
Bacitracin (TOPNOTCH)
Blocks incorporation of D-Ala into the pentapeptide side chain of the peptidoglycan ; For drug-resistant TB
Cycloserine (TOPNOTCH)
inhibits cytosolic enolpyruvate transferase –> prevents formation of N-acetylmuramic acid
Fosfomycin (TOPNOTCH)
same spectrum of activity as Vancomycin ; For VRE, VRSA, for G+ activity, against endocarditis and sepsis
Daptomycin (TOPNOTCH)
Inhibits transpeptidation (catalyzed by peptidyl transferase) by blocking the binding of aminoacyl moiety of the charged tRNA to the acceptor site o mRNA at 50S subunit, basteriostatic
Chloramphenicol (TOPNOTCH)
For meningitis (Strep pneumonia, H influenza, Neisseria meningitides), back up for Salmonella, Rickettsia, Bacteroides, Wide spectrum antibiotic
Chloramphenicol (TOPNOTCH)
Binds 30s ribosomal subunit thus preveting the binding of tRNA to mRNA, bacteriostatic ; Broad/Wide Spectrum (G+ and G-), anaerobes and atypicals
Tetracyclines (TOPNOTCH)
_____ has the broadest spectrum of all tetracyclines and has the longest t1/2 (30-36hrs)
Tigecycline (TOPNOTCH)
SE: GI disturbances (enetrocolitis, nausea, diarrhea, vomiting), teratogen (tooth enamel dysplasia/discoloration), hepatotoxicity, nephrotoxicity, photosensitivity n(esp. demeclocycline), vestibulotoxicity, candidiasis, bacterial superinfection with S. aureus and C. difficile, Fanconi syndrome
Tetracyclines (TOPNOTCH)
Tetracyclines
Tetracycline, doxycycline, minocycline, tigecycline, demeclocycline (TOPNOTCH)
Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For community-acquired pneumonia, pertussis, diphtheria, chlamydial infections
Macrolides (TOPNOTCH)
Macrolides
Erythromycin, azithromycin, clarithromycin, telithromycin (TOPNOTCH)
______ is used as an alternative Ceftriaxone in Gonorrhea and to Pen G in syphilis
Azithromycin (TOPNOTCH)
______ is used for macrolide-resistance
telithromycin (TOPNOTCH)
a narrow spectrum macrolide, for G+ and anaerobe, low oral bioavailability
Fidaxomicin (TOPNOTCH)
as effective as Vancomycin as treatment for C. difficile possibly with lower relapse rate
Fidaxomicin (TOPNOTCH)
GI disturbance, skin rash, neutropenia, hepatic dysfunction, possible superinfection (Pseudomembranous colitis - C. difficile overgrowth)
Lincosamides: Clindamycin, lincomycin (TOPNOTCH)
Binds 30s ribosomal subunit, inhibit transpeptidation, bacteriostatic ; For anaerobic infections (Bacteroides), alternative against gram + cocci (MRSA), endocarditis prophylaxis esp in those allergic to Pens, PCP pneumonia, toxoplasmosis (+ Pyrimethamine), skin and soft tissue infection
Lincosamides: Clindamycin, lincomycin (TOPNOTCH)
Binds 50s ribosomal subunit, constricting the channel where polypeptides are extruded thus tRNA synthetase is also inhibited –> decreased free tRNA
Streptogramin: Quinupristin-Dalfopristin (TOPNOTCH)
Binds 23S rRNA of 50s ribosomal subunit, inhibit initiation by blockin formation of the tRNA-ribosome-mRNA ternary complex, bacteriostatic ; Reserved for infections caused by drug-resistant gram + cocci (MRSA, VRE, PRSP), Listeria, Corynebacteria
Oxazolidinone: Linezolid (TOPNOTCH)
For serious infections caused by aerobic gram _ bacteria (E.coli, Enterobacter, Klebsiella, Proteus, Providencia, Pseudomonas, Serratia, Haemophilus, Moraxella, Shigella), endocarditis, ocular infections
Aminoglycosides (TOPNOTCH)
Least resistance and narrowest therapeutic window ; used for streptomycin-resistant TB
Amikacin (TOPNOTCH)
For TB, tularaemia, bubonic plague, brucellosis
Streptomycin (TOPNOTCH)
SE: nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade
Aminoglycosides in general (TOPNOTCH)
SE: hypersensitivity, nephrotoxicity (reversible), ototoxicity (irreversible), neuromuscular blockade, teratogen (congenital deafness), injection site reactions
Streptomycin (TOPNOTCH)
_____ is most ototoxic of all Aminoglycosides (AG) while _____ has the most skin reactions
kanamycin ; Neomycin (TOPNOTCH)
For drug-resistant gonorrhoea, gonorrhoea in penicillin allergic patients
Spectinomycin (TOPNOTCH)
For Treatment of serious infections caused by organisms resistant to other aminoglycosides
Netilmicin (TOPNOTCH)
Inhibits dihydropteroate synthase, bacteriostatic
Sulfonamides (TOPNOTCH)
low solubility in acidic urine causing formation of stones
Sulfonamides (TOPNOTCH)
Sequential blockade of dihydropteroate synthase and dihydrofolate reductase , bactericidal
Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)
SE: GI upset, acute hemolysis in G6PD deficiency, nephrotoxicity, hypersensitivity, hematotoxicity, kernicterus ; antifolate effects (megaloblastic anemia, leukopenia, granulocytopenia)
Co-trimoxazole (Sulfamethoxazole + Trimethoprim) (TOPNOTCH)
Inhibits DNA replication by binding to DNA gyrase and topoisomerase IV (G+) and Topoisomerase II (G-)
Fluoroquinolones (TOPNOTCH)
For infections of the urogenital and GI tract by G- (gonococci, E. coli, Klebsiela, Campylobacter, Enterobacter, Pseudomonas, Salmonella, Shigella), respiratory tract, skin and soft tissue infection
Fluoroquinolones (TOPNOTCH)
CI in pregnancy and in children (damage growing cartilage –> arthropathy)
Fluoroquinolones (TOPNOTCH)
GI distress, skin rashes, HA, dizziness, insomnia, increased LFT, phototoxicity, CNS effects (dizziness, headache), tendinitis and tendon rupture, opportunistic infection by Candida and Streptococci
Fluoroquinolones (TOPNOTCH)
Second Generation Fluoroquinolones
Ciprofloxacin, ofloxacin (TOPNOTCH)
First Generation Fluoroquinolones
Norfloxacin, Nalidixic acid (TOPNOTCH)
Third Generation Fluoroquinolones
Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)
Respiratory Quinolones
Levofloxacin, Gemifloxacin, Moxifloxacin (TOPNOTCH)
newest members of the Fluoroquinolone family and are condisered to have the broadest spectrum of activity with increased activity aginst anaerobes ang atypical agents
Moxifloxacin and Gemifloxacin (TOPNOTCH)
Fourth Generation Fluoroquinolones
Trovafloxacin, Gatifloxacin (TOPNOTCH)
FQ elimination is via kidneys by tubular secretion (may compete with probenecid for excretion) EXCEPT
Moxifloxacin (TOPNOTCH)
additional SE of which FQs: diabetes, hepatotoxicity
diabetes (gatifloxacin), hepatotoxicity (trovafloxacin) (TOPNOTCH)
Reactive reduction by ferredoxin forming free radicals that disrupt electron transport chain, bactericidal
Metronidazole, tinidazole (TOPNOTCH)
For anaerobic or mixed intra-abdominal infections, vaginitis (trichomonas, gardnerella), pseudomembranous colitis, brain abscess, protozoal infections
Metronidazole, tinidazole (TOPNOTCH)
DOC for amoebiasis, giardiasis and Pseudomembranous colitis
Metronidazole (TOPNOTCH)
single OD dose can prevent recurrent UTI
Nitrofurantoin (TOPNOTCH)
SE: GI irritation, metallic taste, headache, dark urine, leukopenia, dizziness, ataxia, neuropathy, seizures and disulfiram reaction
Metronidazole (TOPNOTCH)
acidification of urine enhances activity ; adjust dose in renal patients
Nitrofurantoin (TOPNOTCH)
Forms multiple reactive intermediates when acted upon by bacterial nitrofuran reductase, bactericidal ; For UTI (except Proteus and Pseudomonas)
Nitrofurantoin (TOPNOTCH)
Inhibits mycolic acid synthesis, bactericidal
Isoniazid (TOPNOTCH)
SE: hepatotoxicity, neurotoxicity (seizures, peripheral neuritis, insomnia, restlessness, muscle twitching), acute hemolysis in G6PD deficiency, drug-induced lupus
Isoniazid (TOPNOTCH)
Most impt drug in TB
Isoniazid (TOPNOTCH)
prevent neurotoxicity of Isoniazid by giving
pyridoxine (vit B6) (TOPNOTCH)
given as a sole drug for prophylaxis of close contacts of TB Px and skin test converters
Isoniazid (TOPNOTCH)
Inhibits DNA-dependent RNA polymerase, bactericidal
Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)
red-orange urine, light chain proteinuria, skin rash, thrombocytopenia, nephritis, hepatotoxicity, flulike syndrome, anemia, impair antibody response
Rifamycin derivatives: Rifampicin, rifabutin, rifapentine, rifamixin (TOPNOTCH)
CYP450 inhibitor: Rifampicin or INH
INH (TOPNOTCH)