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86 Cards in this Set
- Front
- Back
What are the three Beta-lactamase resistant penicillins?
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Methicillin (no longer used), Nafcillin (use Naf for Staph), and Oxacillin (oral); (MNO)
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Name the penicillins that targets Pseudomona aeruginosa and other gram-negative aerobes.
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Ticarcillin, Carbenicillin, and Piperacillin (Takes Care of Pseudomonas)
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Amoxicillin (oral) and Ampicillin HELPS
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Haemophilus, E. coli, Listeria, Proteus, Salmonella
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What is the molecule found in the cell wall of bacteria that is triggered by penicillins that aid in the destruction of the bacterium through the formation of a spheroplast?
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peptidoglycan hydrolase
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What medication (used as a uricosouric) is used to increase the half life of penicillin by blocking the excretion of penicillin in the PCT of the kidney?
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Probenecid
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What multiple of the MIC of penicillin is used for a systemic infection? How about a CNS infection?
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4, 10
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What is the indications for Penicillin G?
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Streptococcus infections, Syphilis (Benzathine Penicillin G), Neisseria meningitidis, anaerobes (e.g. Clostridium perfringens)
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How does a penicillin become resistant to a penicillinase?
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Either through addition of clavulinic acid or through increasing the -R group of the penicillin molecule
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What happens when you increase the size of the -R group, when you are trying to make a penicillinase-resistant penicillin?
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The penicillin becomes less potent, so you must increase the dose.
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What are the penicillinase-resistant penicillins generally good for?
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Skin infections (Methicillin/Nafcillin IV; Oxacillin oral)
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Name five general penicillins that are targeted to Gram negatives.
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Ampicillin, Amoxacillin, Ticarcillin, Carbenicillin, and Pipercillin
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What is special about the amino groups on the R-groups of the aminopenicillins (e.g. ampicillin and amoxacillin)
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They increase the penetration of the Gram negative's outer membrane
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Which two antibiotics do you often see a skin rash with?
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Aminopenicillins (amoxicillin and ampicillin) and sulfamethoxazole
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Which form of antibiotics are more likely to cause diarrhea: oral or IV/IM?
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Oral (amoxicillin vs. ampicillin)
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Name two antibiotics that are most associated with pseudomembraneous colitis.
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Amoxicillin and clindamycin
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Is ticarcillin and pipercillin effective against Pseudomonas? Bacteroides fragilis (Gram negative anaerobe)?
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Yes, yes
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Name three bacteria that pipercillin is more affective against versus ticarcillin.
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Pseudomonas, Proteus, Klebsiella (PiPerKillin)
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What is the Gold Standard for treating Gram negative aerobes?
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Aminoglycosides (GNATS: Gentamycin, Neomycin, Amakacin, Tobramycin, Streptomycin)
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What is an excellent synergistic combination of antibiotics against Pseudomonas?
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Aminoglycosides and Ticarcillin/Carbenicillin/Pipercillin
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What is a potential side effect of having to use such a high dose of anti-pseudomonas penicillinases (low potency due to large R-group)?
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Sodium salt overload; bad for hypertension
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What is the main structural difference between penicillins and cephalosporins?
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Cephalosporins have two R-groups, whereas penicillins have one R-group
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Will the cephalosporins resist the Staph penicillinase?
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The first (Cephalexin and Cefazolin) and fourth (cepepime) generations will, but not the second (cefotetan, cefoxitin, and cefuroxime) and third (ceftriaxone, cefotaxime, and ceftazadime) generations.
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Which cephalosporin is highly effective against anaerobes (especially Bacteroides fragilis)?
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Cefoxitin (Second generation; send the fox down the pipe to get the B. fragilis).
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Which generation(s) of cephalosporin is effective against Pseudomonas?
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Third and fourth
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What percent of patients having an allergic reaction to penicillins will have an allergic reaction to cephalosporins? Is it worth risking?
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10%; probably not
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What is the broadest spectrum Beta-lactam? What does it cover?
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imipenem. Aerobe/anaerobe Gram positive/negative
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What must you watch about using imipenem?
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Imipenem should not be used first because the bacteria will secrete massive amounts of lactamase because imipenem won't even bind the lactamase.
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What compound must you take with imipenem in order to prevent the kidney's breakdown of imipenem by a dipeptidase?
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Cilastatin; the kill is LASTIN with CiLASTATIN.
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Aztreonam (aka Monobactam): spectrum and MOA
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Gram negative aerobes; MOA similar to Pen G
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Mupirocin: use? MOA?
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Impetigo cause by Staph and Strep (even lactamase-secreting Staph); Bacterial protein and RNA synthesis are inhibited
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Vancomycin: MOA; Use; toxicities
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inhibits bacterial cell wall synthesis; MRSA, Enterococcus faecalis/faecium, C. difficile (should use metronidazole though); NOT (nephrotoxicity, ototoxicity, thrombophlebitis (Red Man Syndrome (histamine release; take with aspirin and give slower))
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Explain the Davis model as to why aminoglycosides are bacteriocidal.
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When a [small] of aminoglycosides gets inside the bacterial cell, it causes an altered protein product, which implants within the bacterial membrane and serves as a pore. Through this pore flows additional aminoglycosides that serve to finish off the bacterial cell.
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Name the members of the aminoglycoside family.
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GNATS: Gentamycin, Neomycin, Amikacin, Tobramycin, and Streptomycin
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What feature of aminoglycosides make them similar to vancomycin, as far as oral dosing remaining within the GI tract?
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All the amino groups pick up positive charges, and cannot cross membranes very well (vancomycin is just so damn big)
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What is a downstream consequence of the amino groups on the aminoglycosides (think kidney)?
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These molecules are mistaken as amino acids in the PCT of the kidney, where 35% of the dose is accumulated, leading to inhibition of lysosomal enzymes, leading to lysosomal burst and renal toxicity
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What are the three main toxicities of aminoglycosides?
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NON or amiNOglycosides: Nephrotoxicity, Ototoxicity, and neuromuscular block (treat with neostigmine; usually follows bowel rupture)
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Name three mechanisms for resistance to aminoglycosides.
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1) ribosomal resistance, 2) decreased drug uptake, and 3) aminoglycoside modifying enzymes
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What distinguishes the newer Amikacin from the older kanamycin aminoglycosides?
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Amikacin has a larger R-group that inhibits many modifying enzymes
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What is the main use for aminoglycosides?
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Combo therapy with a beta-lactam to treat Gram negative infections or sometimes Staph/Strep infections (aminoglycosides are exclusively targeted against aerobes)
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How well do aminoglycosides enter the CNS?
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None, due to amino groups
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Must you monitor serum drug concentrations and kidney functions when administering aminoglycosides?
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YES
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What are the indications for aminoglycoside use?
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Serious aerobic gram-negative infections, including Pseudomonas aeruginosa
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What is unique about the newer tetracyclines doxycycline and minocycline?
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They are more lipophilic, have higher protein binding, lower renal excretion, higher half life, and very little renal excretion (doxycycline can be used in renal failure patients).
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Which tetracycline can be used in renal failure patients?
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Doxycycline (higher lipophilicity with excretion in fecal matter and bile)
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Which two antibiotics must you not take with food, milk, other dairy products, and antacids?
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Tetracyclines and Floroquinolones (both like bone/cartilage)
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What is a negative side effect of tetracycline dosing in children younger than 12?
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Gray/brown stained teeth.
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How does tetracycline gain access to the bacterial cell?
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It is actively pumped in (it is confused with a natural nutrient).
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Which antibiotic is known for producing a blistering rash?
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Tetracyclines
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What are the indications for tetracyclines?
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Pulmonary infections (Mycobacterium pneumoniae, Haemophilus influenzae, Streptococcus pneumoniae), Chlamydia (DOC), Rickettsia (DOC), and Lyme disease (DOC)
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What antibiotic spectrum does Chloramphenicol have in common?
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Tetracyclines
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Which side effect of Chloramphenicol put this antibiotic off the market, and how common is it?
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Aplastic anemia, which is idiosyncratic, occurs in 1/30000 patients
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Name the Macrolides
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ACE: Azithromycin, Clarithromycin, and Erythromycin.
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What is the DOC for Legionella?
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Erythromycin
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What are the indications for Marcrolides (ACE)?
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UPS: URI:Gram positive (Staph and Strep), Staph aureus (resistant to penicillinases); Pneumonia: Mycoplasma pneumoniae, Haemophilus influenzae; STD: Chlamydia
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What are macrolides known for?
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Their ability to penetrate tissues well (ears, lungs).
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What is the most common side effect associated with Macrolides (ACE)?
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GI disturbances (erythromycin causes a motilin-like activity).
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Linezolid: uses, price, interaction, and SEs
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VRE, MRSA; $45/pill; inhibits MAO; causes BM suppression
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Name the antibiotic with an activity similar to vancomycin, without resistance, used to treat nasty Gram positive organisms like VRE and MRSA.
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Daptomycin
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Clindamycin has activity similar to which antibiotic? If you have resistance to clindamycin, which other antibiotic will you most likely also have resistance to?
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Erythromycin, erythromycin
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What is the indications for Clindamycin?
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Anaerobic infections (e.g. Bacteroides fragilis); but also covers Staph aureus, Strep pyogenes and Strep pneumoniae
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What is the most common side effect of Clindamycin?
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SPECTACULAR DIARRHEA often (20% of time) leading to pseudomembranous colitis (do NOT treat diarrhea with kaopectate or loperamide)
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What is the treatment of choice for Clostridium difficile
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Vancomycin, or metronidazole
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Metronidazole: things to know
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GET GAP (Giardia, Entameba, Trichomonas, Gardnerella, Anaerobes, H. pylori); don't drink (disulfiram like reaction); alters DNA helical coiling
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Sulfamethoxazole: MOA; main SOA; Resistance; Toxicity
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Inhibits DHF synthetase; UTI; increase PABA or salvage of aas/purines/pyrimidines from environment (this is why you can't use sulfamethoxazole on an abscess); skin rashes and displaces bilirubin from albumin
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Trimethoprim: MOA
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DHF reductase
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TMP-SMX indications
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the Super Sport for UTIs and URIs:
Salmonella, Shigella UTI: E. coli URI: Strep pneumo, H. influenzae, S. aureus, PCP! |
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Quinolones: MOA; specialty; indications
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Inhibits DNA gyrase (topoisomerase II); oral antibiotics for gram negative infections (including P. aeruginosa)
Indications: Ciprofloxacin (not for respiratory bugs, just gram -s) Levofloxacin (gram negative bugs plus Staph/Strept) Moxifloxacin (gram negative bugs, Staph/Strep, anaerobes) |
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What is the main toxicity associated with quinolones?
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Cartilage and tendon damage
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Best antibiotic for the following combo of bugs: Neisseria, Bacteroides fragilis, and E. coli
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Cefoxitin
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Name two polyenes, and their MOA (antifungals)
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Nystatin and Amphotericin B; irreversibly binds ergosterol
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What is the MOA of the azoles (antifungals)?
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Interfere with the biosynthesis of ergosterol by inhibiting 14 alpha-sterol demethylase
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Name an azole that is used as a losenge for the treatment of oral candidiasis.
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Clotrimazole
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What is so special about Griseofulvin? MOA? Indications?
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Oral pill for topical infections; Inhibits microtubule formation; surface fungal infections
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Terbinafine: MOA? Indications?
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Inhibits ergosterol formation by inhibiting squalene monooxygenase; Indicated for onychomycosis (3 month treatment)
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Caspofungin: MOA? Indications?
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Inhibits formation of Beta-Glucan in cell wall; Used for systemic candida infections ("Ca"spofungin for "Ca"ndida)
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Which antifungal is most commonly used to treat Cryptococcus?
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Fluconazole
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Acyclovir and Gancyclovir: MOA? Indications?
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Phosphorylated by viral Tyrosine Kinase and cellular kinases, where they inhibit DNA polymerase; Herpes, and CMV
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How do you deal with the short half life of acyclovir?
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Add a valine to it, producing valacyclovir!
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Amantadine and Rimatadine: MOA? Indications?
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Inhibit M2 protein, inhibiting viral uncoating; use as prophylaxis for Influenza A (90% are resistant now)
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Zanamivir and Oseltamivir: MOA? Indications?
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Inhibits neuraminidase; prophylaxis of Influenza (Oseltamivir decreases mortality associated with H5N1 bird flu and H1N1 swine flu)
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Name four Nucleoside Reverse Transcriptase Inhibitors (NRTI) for HIV treatment.
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LADZ: Lamivudine (pancreatitis), Abacavir (newer, less SEs), Didanosine (peripheral neuropathy and pancreatitis), and Zidovudine (anemia and granulocytopenia)
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What is the MOA of HIV NRTI?
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Inhibits the RNA-dependent DNA polymerase (reverse transcriptase). The NRTIs are lacking the 3'OH.
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Name the suffix for protease inhibitors. MOA?
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(Navir TEASE a proTEASE) -navir (e.g. saquinavir); inhibit maturation of HIV viral proteins.
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Name three NNRTI for HIV treatment. MOA?
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NED: Neviripine, Efavirenz, Delavirdine; inhibits Reverse Transcriptase.
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What is the MOA for Enfuvirtide? What is the drug?
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HIV drug; inhibits viral attachment and entry of the HIV virus, through blocking CD41 molecule folding.
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Name four drugs used for tuberculosis treatment, along with their toxicities.
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RIPE for treatment;
Rifampin (turns excretions red/orange, Red Lobster Man), Isoniazide (DOC; hepatitis and peripheral neuropathy, supplement with vitamin B6) Pyrazinamide (hepatitis) Ethambutol (retrobulbar neuritis, leading to blurry vision and red/green color blindness) Need 6 months of treatment |