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119 Cards in this Set
- Front
- Back
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Penicllin
forms MOA |
Penicillin G (IV), penicillin V (oral)
MOA-- 1) Binds penicillin binding proteins 2) blocks transpeptidase cross linking of cell wall 3) Activates autolytic enzymes |
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Penicillin
Clinical use |
bacteriacidal for gram negative cocci, gram + rods, gram+ cocci, and spirochetes
Not penicillinase rresistant |
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Penicillin
SE |
hypersensitivity rxts
hemolytic anemia |
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Methicilin, nafcillin, dicloxacillin
Mechanism |
same as penicillin---review
penicillinase resistant dt bulkier R group |
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Methicilin, nafcillin, dicloxacillin
clinical use |
S. aureus
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Methicilin, nafcillin, dicloxacillin:
SE |
Hypersensitivity rxts
methicillin--interstitial nephritis |
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Ampicillin, amoxicillin
MOA |
same as penicillin--review
Wider spectrum--can combine with clavulanic acid to enhance spectrum AmOxicillin has greater Oral bioavailability vs ampicillin Penicillinase sensitive |
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Ampicillin, amoxicillin:
clinical use |
extended coverage penicillin: HELPS kills enterococci (gram + bacteria and gram - rods)
Haemophilus influenza E coli Listeria monocytogenes Proteus mirabilis Salmonella enterococci |
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Ampicillin, amoxicillin: Tox
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Hypersensitivity rxts
ampicillin rash pseudomembranous colitis |
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carbenicillin, piperacillin, ticarcillin
MOA |
same as penicillin, extended spectrum
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carbenicillin, piperacillin, ticarcillin:
Clinical use |
Pseudomonas spp
gram -rods susceptible to penicillinase use with clavulanic acid |
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carbenicillin, piperacillin, ticarcillin: SE
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Hypersensitivity rxts
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Cephalosporins:
MOA |
B lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases
bacteriacidal |
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Cephalosporins:Clinical use
Generation 1 |
PEcK:
proteus mirabilis E coli Klebsiella pneu gram + cocci |
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Cephalosporins: clinical use
Generation 2 |
HEN PEcKS
gram + cocci H. influenza Enterobacter aerogenes Neisseria spp Proteus mirabilis E coli Klebsiella pneu Serratia marcescens |
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Cephalosporins: clinical use
3 generation |
serious gram - infectiosn resistant to other B lactams
meningitis ie) ceftazidime for Pseudomonas ceftriaxone for gonorrhea |
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Cephalosporins: clinical use
4 generation |
increased activity against pseudomonas and gram + organisms
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Cephalosporins: tox
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Hypersensitivity rxts--cross hypersensitivity with penicillin occurs in 5-10% of patients
increased nephrotoxicity of aminoglycosides disulfiram like reaction with ETOH (in cephalosporins with a methylthiotetrazole group ie cefamandole) |
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Aztreonam
MOA |
monobactam resistant to B lactamases
Bind PBP and inhibit cell wall synthesis Synergistic with aminoglycosides No cross allergicity with penicillins |
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Aztreonam: Clinical use
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Gram - rods: klebsiella spp, Pseudomonas spp, Serratia spp,
no activity against gram + or anaerobes Use with pts who are penicillin allergic or who have renal insufficiency and cannot handle aminoglycosides |
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Aztreonam: SE
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Usually non-toxic
occasional GI upset |
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Imipenem/Cilastatin:
MOA |
broad spectrum, B lactamase resistant carbapenem
Always administered with cilastatin (inhibitor of renal dihydropeptidases) to increase inactivation of renal tubules |
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Imipenem/Cilastatin: Clinical use
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Gram + cocci
gram - rods anaerobes drug of choice for Enterobacter |
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Imipenem/Cilastatin: SE
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GI distress
skin rash CNS toxicity--seizures at high plasma levels |
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vancomyocin:
MOA resistance |
binds D-Ala D-ala and prevents cell wall mucopeptide formation
bacteriacidal resistance occurs with changes of D-ala to D lac |
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vancomyocin:
Clinical use |
serious, gram positive MDR organisms including S Aureus, C. difficile (pseudomembranous colitis)
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vancomyocin: tox
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Well tolerated, NOT many problems
Nephrotoxicity Ototoxicity Thrombophlebitis diffuse flushing--Red Man syndrome (prevent with antihystamines or slow infusion) |
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Protein Synthesis inhibitors
name them |
buy AT 30, CELL at 5o
30: Aminoglycosides--streptomycin,tobramycin, amikacin tetracyline-- 50: Chloramphenical Erythromycin Lincomycin cLindamycin |
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Protein Synthesis Inhibitors:
bacteriacidal bacteriostatic |
cidal--Aminoglycosides
static--tetracycline, Chloramphenical, Erythromycin, Lincomycin, cLindamycin |
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Aminoglycosides--
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streptomycin
tobramycin amikacin |
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Aminoglycosides..name them
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Gentamycin, neomycin, amikacin,tobramycin,streptomycin
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Aminoglycosides:
MOA |
Bacteriacidal
inhibit formation of initiating complex and cause misreading of mRNA Require O2 for uptake so are ineffective against anaerobes |
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Aminoglycosides;
clinical use |
severe gram negative rod infection
synergistic with b lactam Ab Neomycin for bowel surgery |
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Aminoglycosides:
SE/Tox |
Nephrotoxicity (esp when used with a cephalosporin)
Ototoxicity--esp with a loop diuretic |
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tetracyclines name
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Tetracycline, doxycycline, democlocycline, minocycline
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Tetracyclines MOA
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bacteriostatic
binds 30S and prevents attachment of aminoacyl-tRNA limited CNS penetration Doxycycline is fecally eliminated and cannot be used with pts who are renal failure Inhibited by divalent ions inhibit absoprtion in gut (milk, antacids, iron-containing preps) |
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Tetracyclines Clinical use
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VACUUM your Bed Room Tonight
V. cholera Acne Chlamydia Ureaplasma Urealyticum M. Pneumonia Borrelia (lyme) Rickettsia Tularemia |
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Tetracyclines..SE/Tox
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Gi distres
discoloration of teeth and inhibition of growth in children photosensitivity |
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Macrolides--name
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Erythromycin
Azithromycin Clarithromycin |
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Macrolides MOA
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prevent protein synthesis by blocking translocation
bind 23S RNA of 50S Bacteriostatic |
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Macrolides--Clinical use
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URI
pneumonia STD gram + cocci (strptoccocal inf in pts allergic to penicillin) Mycoplasma Legionella Chlamydia Neisseria |
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Macrolides--Tox, SE
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GI discomfort
Acute cholestatic hepatitis eosinophilia skin rashes |
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Chloramphenicol MOA
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Bacteriostatic
Inhibits 50S peptidyltransferase |
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Chloramphenicol Clinical use
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Meningitis -- H. INfl, N. meningitidis, Strep Pneumo
Use conservatively dt toxicities |
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Chloramphenicol--SE/ Tox
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Anemia--dose dependent
Aplastic anemia--dose dependent gray baby syndrome (preemies without UDP glucuronyl transferase |
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Clindamycin--MOA
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block peptide bond formation at 50S
bacteriostatic |
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Clindamycin--Clinical use
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Anaerobic infections (bacteriodes fragilis, clostridium perfringens)
Anaerobes above the diaphragm |
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Clindamycin--Tox
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Psuedomambranous Colitis
fever diarrhea |
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Sulfonamides name
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Sulfamethoxazole (SMX), sulfisoxazole, triple sulfas, sulfadiazine
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Sulfonamides MOA
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PABA antimetabolites inhibit dihydropteroate synthase
Bacteriostatic |
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Sulfonamides--Clinical use
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Gram +
Gram - Nocardia Chlamydia Triple sulfas or SMX for simple UTIs |
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Sulfonamides--SE/Tox
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Hypsty rxts
hemolysis if G6PD deficient nephrotoxicity kernicterus in infants displaces other drug from albumin (warfarin) |
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Trimethoprim MOA
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Inhibits bacterial dihydrofolate reductase
bacteriostatic |
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Trimethoprim Clinical use
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Used in combo with sulfonamides (TMP-SMX) causing sequential block of folate synthesis
Combo used for recurrent UTIs shigella, Salmonella, P. carini |
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Trimethoprim SE/Tox
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Megaloblastic anemia
Leukopenia granulocytopenia May alleviate with supplemental folic acid |
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Fluroquinolones name
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Cipro-
Norflox- oflox- sparflox- moxiflox- gatiflo- enoxacin nalidixic acid (quinolone) |
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Fluoroquninolones MOA
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Inhibit DNA gyrase (Topoisomerase II)
bacteriacidal |
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Fluoroquninolones Clinical use
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gram negative rods of urinary and GI tracts including pseudomonas, Neisseria, some gram +
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Fluoroquninolones--SE, Tox
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Gi upset
superinfections skin rashes HA dizzy Contraindicated --pregnant, children dt damage to cartilage (Tendonitis, tendon rupture) |
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Metronidazole--MOA
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Forms toxic metabolites in bacterial cell wall
bacteriacidal |
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Metronidazole--Clinical use
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Antiprotozoal GET on METRO
Giardia Entamoeba Trichomonas Gardnerella vaginalis anaerobes bacteriodes Clostridium Used with bismuth adn amoxicillin (or tetracycline) for "triple therapy" against H. pylori |
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Metronidazole SE/Tox
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Disulfram like reaction with alcohol
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Polymixins--MOA
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Bind to cell membranes of bacteria and disrupt their osmotic properties
Cationic, basic proteins that act like detergents |
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Polymixins--Clinical use
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resistant gram - infections
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Polymixins--SE, TOX
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Neurotoxicity, acute tubular necrosis
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Anti-Tb drugs
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Rifampin
Ethambutol Streptomycin Pyrazinamide Isoniazid All hepatotoxic |
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Isoniazid--MOA
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decrease synthesis of mycolic acid
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Isoniazid--clinical use
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M. Tb---the only agent used as solo prophylaxis against TB
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Isoniazid--TOX
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INH Injures Neurons and Hepatocytes
Hemolysis if G6PD deficient neurotoxic hepatotoxic SLE like syndrome Pyridoxine (vit B6) can prevent neurotoxicity |
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Rifampin--MOA
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Inhibits DNA dependent RNA pol
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Rifampin--Clinical use
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M. TB--delays resistance to dapsone when used for leprosy
Used for meningococcal prophylaxis and chemoprophylaxis in contacts of children with H inf Type B |
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Rifampin--Tox
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minor hepatotoxicity and drug interactions (P450)
What are the 4 Rs of Rifampin?? (p290) |
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resistances mechanism for:
1) penicillin/cephalosporins 2) Aminoglycosides 3) vancomycin 4) Chloramphenicol |
1) B lactamase cleavage of B lactam ring
2) Modification via acetylation, adenylation, phosphorolation 3)Terminal D-Ala of cell wall replaced with D-lac which reduces afinity 4)Acetylation |
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resistances mechanism for:
1)Macrolides 2) Tetracycline 3)Sulfonamides |
1) Methylation of rRNA near erythromycins ribosome binding site
2)decreased uptake or increased transport out of cell 3)Altered enzyme (bacterial dihydropteroate synthetase), decreased uptake, increased PABA synthesis |
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nonsurgical antimicrobial prophylaxis
1) meningococcal 2)Gonorrhea 3) Syphilis 4)recurrent UTIs 5) P. carinii pneumonia |
1) rifampin (drug of choice)
2) Ceftriaxone 3)benzathine penicillin G 4) TMP-SMX 5) TMP-SMX (drug of choice) aerosolized pentamidine ^ |
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Amphotericin B
MOA |
Binds ergosterol and forms membrane pores that allow leakage of electrolytes
Ergosterol is unique to fungi |
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Amphotericin B Clinical use
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Side spectrum use for mycoses
Cryptococcus Blastomyces Coccidioides Aspergillus Histoplasmosis Candida Mucor (systemic mycoses) Intrathecally for fungal menigitis doe snot cross BBB |
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Amphotericin B Tox
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fever and chills (shake and bake)
Hypotension nephrotoxicity arrythmias (amphoterrible) |
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Nystatin...
MOA Cinical use |
Binds to ergosterol nad disrupts fungal membranes
Swish and swallow for oral candidiasis |
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Azoles...
MOA |
inhibit ergosterol (fungal steroid) synthesis
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Azoles..Clinical use
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Systemic mycoses
Fluconazole for cryptoccocal meningitis in AIDS pts and candidal infections in all types Ketoconazole for blastomyces, Coccidiodes, Histoplasma, C. Albicans, hypercortilism |
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Azoles..Tox
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Hormone sysnthesis inhibition (gynecomastia)
liver dysfunction (inhibits P450) fever chills |
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Flucytosine
MOA |
Inhibits DNA synthesis by converting to fluorouracil which competes with uracil
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Flucytosine...Clinical Use
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Systemic funal infections (Candida, Cryptococus)
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Flucytosine SE/Tox
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Nausea
vomiting BM suppression |
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caspofungin MOA
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Inhibits cell wall synthesis
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caspofungin Clinical use
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invasive aspergillosis
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caspofungin SE/Tox
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GI upset, flushing
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Terbinafine MOA
Clinical use |
Inhbits fungal enzyme squalene epoxidase
dermatophytes especially onychomycosis |
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Griseofulvin MOA
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Interferes with microtubule fxn
disrupts mitosis deposits in keratin containing tissue |
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Griseofulvin Clinical use
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oral treatment of superficial infections
inhibits growth of dermatophytes (tinea and ringworm) |
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Griseofulvin..Tox
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teratogenic
carcinogenic confusion HA inc warfarin metabolism |
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Amantadine MOA
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Blocks viral penetration and uncoating
may buffer pH of endosome causes the release of dopamine from intact nerves |
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Amantadine Clinical use
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prophylaxis for inf A
Parkinsons dz |
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Amantadine SE, Tox
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Amantadine blocks influenz A and rubellA and causes problems with the cerebellA
ataxia, dizziness, slurred speech rimantidine is derivative with fewer side effects |
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Zanamivir, Oseltamivir
MOA Clinical use |
Inhibits influenza neuraminidase
Both A and B |
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Ribavarin
MOA |
inhibits synthesis of guanine by competitively inhibiting IMP dehydrogenase
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Amantadine Clinical use
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RSV, chronic Hep C
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Amantadine Tox
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Hemolytic anemia
severe teratogen |
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Acyclovir MOA
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preferentially inhibits viral DNA pol when phophorylated by viral thymidine kinase
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Amantadine Clinical use
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HSV
VZV EBV mucocutaneous and genital herpes lesions prophylaxis in immunocompromised pts |
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Amantadine SE, Tox
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Delirium
tremor nephrotoxicity |
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Ganciclovir MOA
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Phosphorylation by viral kinase
preferentially inhibits CMV DNA pol |
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Ganciclovir Clinical use
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CMV
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Ganciclovir Tox
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Leukopenia
neutropenia thrombocytopenia renal tox More toxic to hosts than acyclovir |
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Foscarnet MOA
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Viral DNA pol inhibitor that binds to the pyrophosphate binding site of the enzyme
Does not require activation by viral kinase |
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Foscarnet Clinical use
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CMV retinitis in immunocompromised pts when ganciclovir fails
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Foscarnet Tox, SE
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Nephrotoxicity
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Interferons MOA
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glycoproteins from human leukocytes that block various stages of viral DNA and RNA synthesis
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Interferons Clinical use
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Chronic Hep B and C
Kaposi's sarcoma |
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Interferons Tox
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Neutropenia
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HIV
Protease inhibitors: name |
Saquinavir
Ritonavir Nelfinavir Amprenavir |
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HIV
Protease inhibitors: MOA |
Block protease enzyme and prevents new virus from being made
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HIV
Protease inhibitors: Tox |
GI intolerance (D, N)
hyperglycemia lipid abnormalities thrombocytopenia (indinavir) |
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HIV
RT Inhibitors: MOA |
Inhibit RT and prevent incorporation of viral genome into host DNA
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HIV
RT Inhibitors: TOX |
BM suppression (neutropenia, anemia)
peripheral neuropathy lactic acidosis (nucleosides) rash (non nucleosides) megaloblastic anemia ( AZT) |
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HIV
RT Inhibitors: Nucleoside- |
AZT (zidovudine)
didanosine (ddI) zalcitabine (ddC) stavudine (d4T) lamivudine (3TC) abacavir |
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HIV
RT Inhibitors: non-nucleosides |
Nevirapine
delaviridine efavirenz |
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HIV treatment Clinical use
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HAART includes combo therapy of Protease inhibitirs and RT inhibitors
started with low CD4 (<500) or high viral load AZT used during pregnancy |
